WO2010042759A3 - Gaba conjugates and methods of use thereof - Google Patents

Gaba conjugates and methods of use thereof Download PDF

Info

Publication number
WO2010042759A3
WO2010042759A3 PCT/US2009/060058 US2009060058W WO2010042759A3 WO 2010042759 A3 WO2010042759 A3 WO 2010042759A3 US 2009060058 W US2009060058 W US 2009060058W WO 2010042759 A3 WO2010042759 A3 WO 2010042759A3
Authority
WO
WIPO (PCT)
Prior art keywords
methods
gaba
conjugates
present
gaba conjugates
Prior art date
Application number
PCT/US2009/060058
Other languages
French (fr)
Other versions
WO2010042759A2 (en
Inventor
Inc. Kyphia Pharmaceuticals
Feng Xu
Original Assignee
Kyphia Pharmaceuticals Inc
Feng Xu
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Kyphia Pharmaceuticals Inc, Feng Xu filed Critical Kyphia Pharmaceuticals Inc
Priority to CN200980145237.6A priority Critical patent/CN102216257B/en
Priority to AU2009302241A priority patent/AU2009302241B2/en
Priority to KR1020117010420A priority patent/KR101810246B1/en
Priority to CA2740087A priority patent/CA2740087C/en
Priority to JP2011531180A priority patent/JP2012505238A/en
Priority to EP09819911.0A priority patent/EP2344447B1/en
Priority to ES09819911.0T priority patent/ES2589915T3/en
Priority to BRPI0919811-3A priority patent/BRPI0919811B1/en
Publication of WO2010042759A2 publication Critical patent/WO2010042759A2/en
Publication of WO2010042759A3 publication Critical patent/WO2010042759A3/en

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D221/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom as the only ring hetero atom, not provided for by groups C07D211/00 - C07D219/00
    • C07D221/02—Heterocyclic compounds containing six-membered rings having one nitrogen atom as the only ring hetero atom, not provided for by groups C07D211/00 - C07D219/00 condensed with carbocyclic rings or ring systems
    • C07D221/22—Bridged ring systems
    • C07D221/28—Morphinans
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/19—Carboxylic acids, e.g. valproic acid
    • A61K31/195—Carboxylic acids, e.g. valproic acid having an amino group
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/19—Carboxylic acids, e.g. valproic acid
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/19—Carboxylic acids, e.g. valproic acid
    • A61K31/191—Carboxylic acids, e.g. valproic acid having two or more hydroxy groups, e.g. gluconic acid
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/19—Carboxylic acids, e.g. valproic acid
    • A61K31/192—Carboxylic acids, e.g. valproic acid having aromatic groups, e.g. sulindac, 2-aryl-propionic acids, ethacrynic acid 
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/19—Carboxylic acids, e.g. valproic acid
    • A61K31/195—Carboxylic acids, e.g. valproic acid having an amino group
    • A61K31/197—Carboxylic acids, e.g. valproic acid having an amino group the amino and the carboxyl groups being attached to the same acyclic carbon chain, e.g. gamma-aminobutyric acid [GABA], beta-alanine, epsilon-aminocaproic acid, pantothenic acid
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/21—Esters, e.g. nitroglycerine, selenocyanates
    • A61K31/27—Esters, e.g. nitroglycerine, selenocyanates of carbamic or thiocarbamic acids, meprobamate, carbachol, neostigmine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/66—Phosphorus compounds
    • A61K31/675—Phosphorus compounds having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/54—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/08—Antiepileptics; Anticonvulsants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/20—Hypnotics; Sedatives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/22—Anxiolytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/24—Antidepressants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C269/00—Preparation of derivatives of carbamic acid, i.e. compounds containing any of the groups, the nitrogen atom not being part of nitro or nitroso groups
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C269/00—Preparation of derivatives of carbamic acid, i.e. compounds containing any of the groups, the nitrogen atom not being part of nitro or nitroso groups
    • C07C269/04—Preparation of derivatives of carbamic acid, i.e. compounds containing any of the groups, the nitrogen atom not being part of nitro or nitroso groups from amines with formation of carbamate groups
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C271/00—Derivatives of carbamic acids, i.e. compounds containing any of the groups, the nitrogen atom not being part of nitro or nitroso groups
    • C07C271/06—Esters of carbamic acids
    • C07C271/08—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms
    • C07C271/10—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms
    • C07C271/22—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms to carbon atoms of hydrocarbon radicals substituted by carboxyl groups
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/16—Amides, e.g. hydroxamic acids
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2601/00—Systems containing only non-condensed rings
    • C07C2601/12—Systems containing only non-condensed rings with a six-membered ring
    • C07C2601/14—The ring being saturated

Abstract

In one aspect, the present invention provides a composition of a covalent conjugate of a GABA analog with a drug. In another aspect, the present invention provides methods for treating pain and neurological disorders using the conjugates of GABA analogs.
PCT/US2009/060058 2008-10-08 2009-10-08 Gaba conjugates and methods of use thereof WO2010042759A2 (en)

Priority Applications (8)

Application Number Priority Date Filing Date Title
CN200980145237.6A CN102216257B (en) 2008-10-08 2009-10-08 Gaba conjugate and using method thereof
AU2009302241A AU2009302241B2 (en) 2008-10-08 2009-10-08 GABA conjugates and methods of use thereof
KR1020117010420A KR101810246B1 (en) 2008-10-08 2009-10-08 Gaba conjugates and methods of use thereof
CA2740087A CA2740087C (en) 2008-10-08 2009-10-08 Gaba conjugates and methods of use thereof
JP2011531180A JP2012505238A (en) 2008-10-08 2009-10-08 GABA conjugates and methods for their use
EP09819911.0A EP2344447B1 (en) 2008-10-08 2009-10-08 Gaba conjugates and methods of use thereof
ES09819911.0T ES2589915T3 (en) 2008-10-08 2009-10-08 GABA conjugates and their methods of use
BRPI0919811-3A BRPI0919811B1 (en) 2008-10-08 2009-10-08 GABA conjugates and methods of using them

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US10380008P 2008-10-08 2008-10-08
US61/103,800 2008-10-08

Publications (2)

Publication Number Publication Date
WO2010042759A2 WO2010042759A2 (en) 2010-04-15
WO2010042759A3 true WO2010042759A3 (en) 2010-07-15

Family

ID=42101220

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US2009/060058 WO2010042759A2 (en) 2008-10-08 2009-10-08 Gaba conjugates and methods of use thereof

Country Status (11)

Country Link
US (3) US8268887B2 (en)
EP (2) EP2344447B1 (en)
JP (2) JP2012505238A (en)
KR (1) KR101810246B1 (en)
CN (2) CN102216257B (en)
AU (1) AU2009302241B2 (en)
BR (1) BRPI0919811B1 (en)
CA (1) CA2740087C (en)
ES (1) ES2589915T3 (en)
HK (1) HK1220970A1 (en)
WO (1) WO2010042759A2 (en)

Families Citing this family (26)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
BRPI0919811B1 (en) 2008-10-08 2022-04-19 Xgene Pharmaceutical Inc GABA conjugates and methods of using them
AU2010223045A1 (en) * 2009-03-12 2011-11-03 Luitpold Pharmaceuticals, Inc. GABA-linked anthracycline-lipid conjugates
SI2421808T1 (en) 2009-04-23 2013-12-31 Concert Pharmaceuticals Inc. 4-hydroxybutyric acid analogs
WO2012025213A2 (en) * 2010-08-23 2012-03-01 Grünenthal GmbH Novel therapeutic compounds
CN103370289B (en) * 2011-02-14 2015-09-09 康塞特医药品有限公司 4 hydroxybutyric acid deuterated analogue
WO2012161798A1 (en) * 2011-02-25 2012-11-29 Catabasis Pharmaceuticals, Inc. Fatty acid gamma aminobutyric acid (gaba) conjugates and their uses
CN103193669B (en) * 2013-02-27 2014-10-01 南京医科大学 nNOS-Capon uncoupling compound, preparation method and application thereof
EP3148969B1 (en) * 2014-06-02 2020-11-11 Ketogen Inc. Compounds for the treatment of seizures and other central nervous system disorders and conditions
CA3045004A1 (en) * 2015-12-16 2017-06-22 Achelios Therapeutics, Inc. Methods and compositions for treating peripheral neuropathy
CN105777586A (en) * 2016-04-14 2016-07-20 安徽省逸欣铭医药科技有限公司 S(+)vigabatrin ester derivative and preparation method and application thereof
US11602513B1 (en) 2016-07-22 2023-03-14 Flamel Ireland Limited Modified release gamma-hydroxybutyrate formulations having improved pharmacokinetics
UY37341A (en) 2016-07-22 2017-11-30 Flamel Ireland Ltd FORMULATIONS OF GAMMA-MODIFIED RELEASE HYDROXIBUTIRATE WITH IMPROVED PHARMACOCINETICS
US11602512B1 (en) 2016-07-22 2023-03-14 Flamel Ireland Limited Modified release gamma-hydroxybutyrate formulations having improved pharmacokinetics
US11504347B1 (en) 2016-07-22 2022-11-22 Flamel Ireland Limited Modified release gamma-hydroxybutyrate formulations having improved pharmacokinetics
EP3528784B1 (en) * 2016-10-21 2023-08-02 APIRX Pharmaceutical USA, LLC Suppositories comprising cannabinoids
HUE050829T2 (en) * 2017-02-02 2021-01-28 Otolanum Ag Intranasal composition comprising betahistine
CN112424158A (en) * 2018-05-14 2021-02-26 昌郁医药公司 Crystalline forms of 1- (acyloxy) -alkyl carbamate drug conjugates of naproxen and pregabalin
CN108863873A (en) * 2018-06-26 2018-11-23 台州学院 A kind of sulphur allyl carbonate esters compound and preparation method thereof
KR102107304B1 (en) * 2018-08-24 2020-05-06 (주)엠앤씨생명과학 Natural liposome comprising red yeast rice, process for the preparation thereof, and food composition comprising the same
JP2022522270A (en) 2019-03-01 2022-04-15 フラメル アイルランド リミテッド Gamma-hydroxybutyrate composition with improved pharmacokinetics in dietary intake
WO2023019154A1 (en) * 2021-08-11 2023-02-16 Tris Pharma, Inc. Oxybate polyethylene glycol prodrugs
CN114452256A (en) * 2021-12-31 2022-05-10 浙江大学 Spinal cord injury targeted drug, polymer-hydrophobic compound micelle and preparation method thereof
US11779557B1 (en) 2022-02-07 2023-10-10 Flamel Ireland Limited Modified release gamma-hydroxybutyrate formulations having improved pharmacokinetics
US11583510B1 (en) 2022-02-07 2023-02-21 Flamel Ireland Limited Methods of administering gamma hydroxybutyrate formulations after a high-fat meal
WO2023215323A1 (en) * 2022-05-02 2023-11-09 The Regents Of The University Of California Intranasal baclofen
CN116585298A (en) * 2023-06-30 2023-08-15 江苏海洋大学 Coupling medicine, composition and application thereof

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20030087803A1 (en) * 2001-11-05 2003-05-08 Yatvin Milton B. Covalent conjugates of biologically-active compounds with amino acids and amino acid derivatives for targeting to physiologically-protected sites
US20040242570A1 (en) * 2001-09-27 2004-12-02 Abraham Nudelman Conjugated psychotropic drugs and uses thereof
WO2008010222A2 (en) * 2006-07-17 2008-01-24 Ramot At Tel Aviv University Ltd. Conjugates comprising a gaba- or glycine compound, pharmaceutical compositions and combinations thereof and their use in treating cns disorders

Family Cites Families (56)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US404175A (en) 1889-05-28 O g o o o
US3625214A (en) 1970-05-18 1971-12-07 Alza Corp Drug-delivery device
US3845770A (en) 1972-06-05 1974-11-05 Alza Corp Osmatic dispensing device for releasing beneficial agent
US3916899A (en) * 1973-04-25 1975-11-04 Alza Corp Osmotic dispensing device with maximum and minimum sizes for the passageway
DE2460891C2 (en) * 1974-12-21 1982-09-23 Gödecke AG, 1000 Berlin 1-aminomethyl-1-cycloalkaneacetic acids and their esters, processes for their preparation and medicaments containing these compounds
IL67445A (en) * 1982-12-09 1985-11-29 Teva Pharma Ethoxycarbonyloxy ethyl esters of non-steroidal anti-inflammatory carboxylic acids
US4906474A (en) * 1983-03-22 1990-03-06 Massachusetts Institute Of Technology Bioerodible polyanhydrides for controlled drug delivery
EP0130119B1 (en) 1983-06-23 1988-11-09 Merck & Co. Inc. (acyloxyalkoxy) carbonyl derivatives as bioreversible prodrug moieties for primary and secondary amine functions in drugs, their preparation and pharmaceutical compositions containing said derivatives
US4789734A (en) * 1985-08-06 1988-12-06 La Jolla Cancer Research Foundation Vitronectin specific cell receptor derived from mammalian mesenchymal tissue
US5023252A (en) * 1985-12-04 1991-06-11 Conrex Pharmaceutical Corporation Transdermal and trans-membrane delivery of drugs
ES2035824T3 (en) * 1986-03-14 1993-05-01 Fujisawa Pharmaceutical Co., Ltd. PROCEDURE FOR PREPARING PROFARMAC COMPOUNDS AND PREPARATIONS CONTAINING THEM.
JP2876058B2 (en) 1986-08-18 1999-03-31 エミスフィア・テクノロジーズ・インコーポレイテッド Drug delivery system
US5811128A (en) * 1986-10-24 1998-09-22 Southern Research Institute Method for oral or rectal delivery of microencapsulated vaccines and compositions therefor
US5075109A (en) 1986-10-24 1991-12-24 Southern Research Institute Method of potentiating an immune response
US5001139A (en) 1987-06-12 1991-03-19 American Cyanamid Company Enchancers for the transdermal flux of nivadipine
US4992445A (en) 1987-06-12 1991-02-12 American Cyanamid Co. Transdermal delivery of pharmaceuticals
US4897268A (en) 1987-08-03 1990-01-30 Southern Research Institute Drug delivery system and method of making the same
US5766573A (en) 1988-12-06 1998-06-16 Riker Laboratories, Inc. Medicinal aerosol formulations
AU9137091A (en) 1990-11-27 1992-06-25 Northwestern University Gaba and l-glutamic acid analogs for antiseizure treatment
US6197819B1 (en) * 1990-11-27 2001-03-06 Northwestern University Gamma amino butyric acid analogs and optical isomers
US5190029A (en) 1991-02-14 1993-03-02 Virginia Commonwealth University Formulation for delivery of drugs by metered dose inhalers with reduced or no chlorofluorocarbon content
PT641330E (en) 1992-05-20 2002-03-28 Univ Northwestern ANALOGS OF GABA AND L-GLUTAMIC ACID FOR THE TREATMENT OF DISEASES OF THE CENTRAL NERVOUS SYSTEM
US5376359A (en) 1992-07-07 1994-12-27 Glaxo, Inc. Method of stabilizing aerosol formulations
EP0678034B1 (en) * 1993-01-11 1999-05-26 Dana Farber Cancer Institute Inducing cytotoxic t lymphocyte responses
EA001534B1 (en) 1996-02-07 2001-04-23 Варнер-Ламберт Компани Derivatives of cyclic amino acid or pharmaceutically acceptable salts thereof, pharmaceutical composition and method of treatment depression, panic conditions, states of fear and pain
JP2000506861A (en) 1996-03-14 2000-06-06 ワーナー―ランバート・コンパニー New substituted cyclic amino acids as pharmaceuticals
EA001214B1 (en) 1996-03-14 2000-12-25 Варнер-Ламберт Компани Novel bridged cyclic amino acids as pharmaceutically acceptable agents
JP2002514187A (en) 1996-10-23 2002-05-14 ワーナー―ランバート・コンパニー Substituted γ-aminobutyric acid as a drug
AU8668598A (en) 1997-08-20 1999-03-08 University Of Oklahoma, The Gaba analogs to prevent and treat gastrointestinal damage
CA2296336C (en) 1997-09-08 2004-04-20 Warner-Lambert Company Analgesic compositions comprising anti-epileptic compounds and methods of using same
JP3756761B2 (en) 1997-10-27 2006-03-15 ワーナー−ランバート・カンパニー、リミテッド、ライアビリティ、カンパニー Cyclic amino acids and their derivatives useful as pharmaceuticals
IL135314A0 (en) 1997-12-16 2001-05-20 Warner Lambert Co Novel amines as pharmaceutical agents
KR20010033158A (en) 1997-12-16 2001-04-25 로즈 암스트롱, 크리스틴 에이. 트러트웨인 1-Substituted-1-Aminomethyl-Cycloalkane Derivatives (=Gabapentin Analogues), Their Preparation and Their Use in the Treatment of Neurological Disorders
CA2304967C (en) 1997-12-16 2005-06-14 Warner-Lambert Company 4(3)substituted-4(3)-aminomethyl-(thio)pyran or -piperidine derivatives (=gabapentin analogues), their preparation and their use in the treatment of neurological disorders
US6316638B1 (en) 1998-05-26 2001-11-13 Warner-Lambert Company Conformationally constrained amino acid compounds having affinity for the alpha2delta subunit of a calcium channel
GB9819926D0 (en) 1998-09-14 1998-11-04 Mead Corp A tray container and blank
CA2339273C (en) 1998-09-14 2005-10-18 Warner-Lambert Company Branched alkyl pyrrolidine-3-carboxylic acids
WO2000031020A1 (en) 1998-11-25 2000-06-02 Warner-Lambert Company Improved gamma amino butyric acid analogs
EP1031350A1 (en) 1999-02-23 2000-08-30 Warner-Lambert Company Use of a gabapentin-analog for the manufacture of a medicament for preventing and treating visceral pain
EP1161263A1 (en) 1999-03-10 2001-12-12 Warner-Lambert Company Llc Analgesic compositions comprising anti-epileptic compounds and methods of using same
ATE390133T1 (en) 2000-06-26 2008-04-15 Warner Lambert Co GABAPENTINE ANALOGUES FOR SLEEP DISORDERS
EP1399161B1 (en) * 2001-06-05 2011-04-20 Control Delivery Systems Sustained-release analgesic compounds
US6818787B2 (en) * 2001-06-11 2004-11-16 Xenoport, Inc. Prodrugs of GABA analogs, compositions and uses thereof
WO2003026563A2 (en) * 2001-09-27 2003-04-03 Ramot At Tel Aviv University Ltd. Conjugated anti-psychotic drugs and uses thereof
ITMI20022658A1 (en) 2002-12-17 2004-06-18 Nicox Sa DRUGS FOR CHRONIC PAIN.
GB0405200D0 (en) 2004-03-08 2004-04-21 Pfizer Ltd Combinations comprising alpha-2-delta ligands
WO2005102390A2 (en) 2004-04-22 2005-11-03 Pfizer Japan, Inc. Combinations comprising alpha-2-delta ligands and nmda receptor antagonists
CN101232868A (en) 2005-04-19 2008-07-30 阿尔扎公司 Combination of tramadol and substances that comprise gabapentin
CN101247837B (en) * 2005-06-07 2013-03-20 特拉维夫大学拉莫特有限公司 Novel salts of conjugated psychotropic drugs and processes of preparing same
US7994220B2 (en) 2005-09-28 2011-08-09 Cypress Bioscience, Inc. Milnacipran for the long-term treatment of fibromyalgia syndrome
MXPA05011735A (en) 2005-11-01 2007-04-30 Leopoldo Espinosa Abdala Pharmaceutical compositions combining analgesics and anticonvulsant agents for the treatment of chronic and acute pain.
EP1820502A1 (en) 2006-02-10 2007-08-22 Laboratorios Del Dr. Esteve, S.A. Active substance combination comprising azolylcarbinol compounds
WO2008011016A2 (en) 2006-07-18 2008-01-24 Dynogen Pharmaceuticals, Inc. Treating gastroesophageal reflux disease with 5-ht3- and gaba receptor agonists
WO2008009663A1 (en) 2006-07-19 2008-01-24 Boehringer Ingelheim International Gmbh Treatment of pain
US20080161393A1 (en) * 2006-12-08 2008-07-03 Barrett Ronald W Use of prodrugs of GABA analogs for treating disease
BRPI0919811B1 (en) 2008-10-08 2022-04-19 Xgene Pharmaceutical Inc GABA conjugates and methods of using them

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20040242570A1 (en) * 2001-09-27 2004-12-02 Abraham Nudelman Conjugated psychotropic drugs and uses thereof
US20030087803A1 (en) * 2001-11-05 2003-05-08 Yatvin Milton B. Covalent conjugates of biologically-active compounds with amino acids and amino acid derivatives for targeting to physiologically-protected sites
WO2008010222A2 (en) * 2006-07-17 2008-01-24 Ramot At Tel Aviv University Ltd. Conjugates comprising a gaba- or glycine compound, pharmaceutical compositions and combinations thereof and their use in treating cns disorders

Also Published As

Publication number Publication date
CN102216257B (en) 2015-11-25
JP2012505238A (en) 2012-03-01
WO2010042759A2 (en) 2010-04-15
BRPI0919811B1 (en) 2022-04-19
EP3075722A1 (en) 2016-10-05
CA2740087A1 (en) 2010-04-15
US10478412B2 (en) 2019-11-19
ES2589915T3 (en) 2016-11-17
EP2344447B1 (en) 2016-06-08
US20130035352A1 (en) 2013-02-07
HK1220970A1 (en) 2017-05-19
KR20110081839A (en) 2011-07-14
EP2344447A2 (en) 2011-07-20
CA2740087C (en) 2019-07-23
AU2009302241B2 (en) 2015-10-29
CN102216257A (en) 2011-10-12
BRPI0919811A8 (en) 2017-10-03
KR101810246B1 (en) 2017-12-18
US8268887B2 (en) 2012-09-18
US20160256558A1 (en) 2016-09-08
US20100113497A1 (en) 2010-05-06
CN105330603A (en) 2016-02-17
BRPI0919811A2 (en) 2017-08-29
AU2009302241A1 (en) 2010-04-15
JP2015120740A (en) 2015-07-02
US9186341B2 (en) 2015-11-17
JP6167123B2 (en) 2017-07-19
EP2344447A4 (en) 2012-04-25

Similar Documents

Publication Publication Date Title
WO2010042759A3 (en) Gaba conjugates and methods of use thereof
GB2463833A (en) Methods and compositions for the treatment of neurological disorders
EP2526933A3 (en) Inhibitors of bruton's tyrosine kinase
WO2008010222A3 (en) Conjugates comprising a gaba- or glycine compound, pharmaceutical compositions and combinations thereof and their use in treating cns disorders
WO2006095029A3 (en) Di-polymer protein conjugates and processes for their preparation
ZA200901826B (en) Treating pain, diabetes, and lipid metabolism disorders
WO2010056919A3 (en) Eflornithine prodrugs, conjugates and salts, and methods of use thereof
WO2005118609A3 (en) Small molecule stimulators of neuronal growth
WO2007084857A3 (en) Methods and compositions for treating cell proliferative disorders
HUE050319T2 (en) Compositions and methods for treating alcohol use disorders, pain and other diseases
WO2008097924A3 (en) Pharmaceutical compositions comprising dextromethorphan analogs for the treatment of neurological disorders
EP2094281A4 (en) Use of lipid conjugates in the treatment of diseases or disorders of the eye
EP2278972A4 (en) Treatment for neurological and mental disorders
WO2009105585A3 (en) Postsynaptically targeted chemodenervation agents and their methods of use
WO2008109230A3 (en) Therapeutic composition with enhanced endothelium targeting
IL198196A0 (en) Treatment of demyelinating disorders with soluble lymphotoxin-beta-receptor
WO2011005510A3 (en) Peptide conjugates and uses thereof
GB0917645D0 (en) Therapy for hyperglycemia, related disorders and erectile dysfunction
WO2008051421A3 (en) Peptide-cytotoxic conjugates
WO2008094054A3 (en) 6, 8-dichlorchroman-3-yl-l, 3-dihydroimidazole-2-thione derivatives and their use for the treatment of cardiovascular disorders
WO2008125902A8 (en) Peripheral and neural inflammatory crosstalk
ZA200902453B (en) PAI-1 binding modulators for the treatment of ocular disorders
WO2007104768A3 (en) Di-polymer protein conjugates and processes for their preparation
ME01951B (en) Use of agomelatin in the manufacture of a medicament for the treatment of bipolar disorders
WO2009137436A3 (en) Peptide conjugates

Legal Events

Date Code Title Description
WWE Wipo information: entry into national phase

Ref document number: 200980145237.6

Country of ref document: CN

121 Ep: the epo has been informed by wipo that ep was designated in this application

Ref document number: 09819911

Country of ref document: EP

Kind code of ref document: A2

WWE Wipo information: entry into national phase

Ref document number: 2011531180

Country of ref document: JP

NENP Non-entry into the national phase

Ref country code: DE

WWE Wipo information: entry into national phase

Ref document number: 2740087

Country of ref document: CA

Ref document number: 2009302241

Country of ref document: AU

WWE Wipo information: entry into national phase

Ref document number: 2009819911

Country of ref document: EP

ENP Entry into the national phase

Ref document number: 20117010420

Country of ref document: KR

Kind code of ref document: A

WWE Wipo information: entry into national phase

Ref document number: 3418/DELNP/2011

Country of ref document: IN

ENP Entry into the national phase

Ref document number: 2009302241

Country of ref document: AU

Date of ref document: 20091008

Kind code of ref document: A

ENP Entry into the national phase

Ref document number: PI0919811

Country of ref document: BR

Kind code of ref document: A2

Effective date: 20110408