DK1104760T3 - Sulfamoylheteroarylpyrazolforbindelser som anti-inflammatoriske/analgetiske midler - Google Patents

Sulfamoylheteroarylpyrazolforbindelser som anti-inflammatoriske/analgetiske midler

Info

Publication number
DK1104760T3
DK1104760T3 DK00310441T DK00310441T DK1104760T3 DK 1104760 T3 DK1104760 T3 DK 1104760T3 DK 00310441 T DK00310441 T DK 00310441T DK 00310441 T DK00310441 T DK 00310441T DK 1104760 T3 DK1104760 T3 DK 1104760T3
Authority
DK
Denmark
Prior art keywords
compounds
halo
heteroarylpyrazole
sulfamoyl
inflammatory
Prior art date
Application number
DK00310441T
Other languages
English (en)
Inventor
Kazuo Pfizer Pharmaceutic Ando
Kiyoshi Pfizer Pharma Kawamura
Original Assignee
Pfizer Prod Inc
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 Pfizer Prod Inc filed Critical Pfizer Prod Inc
Application granted granted Critical
Publication of DK1104760T3 publication Critical patent/DK1104760T3/da

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/06Antiasthmatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/12Drugs for disorders of the urinary system of the kidneys
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • A61P15/06Antiabortive agents; Labour repressants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/02Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/06Antigout agents, e.g. antihyperuricemic or uricosuric agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/08Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16Anti-Parkinson drugs
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/04Antihaemorrhagics; Procoagulants; Haemostatic agents; Antifibrinolytic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/06Antianaemics
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
DK00310441T 1999-12-03 2000-11-24 Sulfamoylheteroarylpyrazolforbindelser som anti-inflammatoriske/analgetiske midler DK1104760T3 (da)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US16888999P 1999-12-03 1999-12-03

Publications (1)

Publication Number Publication Date
DK1104760T3 true DK1104760T3 (da) 2003-06-30

Family

ID=22613376

Family Applications (1)

Application Number Title Priority Date Filing Date
DK00310441T DK1104760T3 (da) 1999-12-03 2000-11-24 Sulfamoylheteroarylpyrazolforbindelser som anti-inflammatoriske/analgetiske midler

Country Status (11)

Country Link
US (2) US6603008B1 (da)
EP (1) EP1104760B1 (da)
JP (2) JP3338027B2 (da)
AT (1) ATE234299T1 (da)
BR (1) BR0005703A (da)
CA (1) CA2327385A1 (da)
DE (1) DE60001623T2 (da)
DK (1) DK1104760T3 (da)
ES (1) ES2193921T3 (da)
MX (1) MXPA00011844A (da)
PT (1) PT1104760E (da)

Families Citing this family (352)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6833373B1 (en) 1998-12-23 2004-12-21 G.D. Searle & Co. Method of using an integrin antagonist and one or more antineoplastic agents as a combination therapy in the treatment of neoplasia
PT1104760E (pt) * 1999-12-03 2003-06-30 Pfizer Prod Inc Compostos de sulfamoil-heteroarilpirazole como agentes analgesicos e anti-inflamatorios
US6555581B1 (en) 2001-02-15 2003-04-29 Jones Pharma, Inc. Levothyroxine compositions and methods
ATE297913T1 (de) 2001-07-05 2005-07-15 Pfizer Prod Inc Sulfonyl-heteroaryl-triazole als entzündungshemmende und analgetische mittel
DE10135027A1 (de) * 2001-07-18 2003-02-06 Solvay Pharm Gmbh Verwendung Trifluoracetylalkyl-substituierter Phenyl-, Phenol- und Benzoylderivate in der Behandlung und/oder Prophylaxe von Obestias und deren Begleit- und/oder Folgeerkrankungen
WO2003037874A1 (en) 2001-11-02 2003-05-08 Pfizer Products Inc. An efficient synthesis of 5-heteroatom-containing-pyrazoles
WO2003037330A1 (en) 2001-11-02 2003-05-08 Pfizer Products Inc. Sulfonyl-and sulfonylheteroaryl-pyrazoles with a hydrazinyl or nitrogen oxide substituent at the 5-position for use as cyclooxygenase inhibitors
WO2003037352A1 (en) * 2001-11-02 2003-05-08 Pfizer Products Inc. 1-phenyl-5-n-heterocyclyl-pyrazoles as cyclooxygenase inhibitors for the treatment of inflammation associated disorders
WO2003037351A1 (en) 2001-11-02 2003-05-08 Pfizer Products Inc. Heterocyclo-alkylsulfonyl pyrazoles and their use as cox-2 inhibitors
WO2003037335A1 (en) 2001-11-02 2003-05-08 Pfizer Products Inc. 5-heteroatom-substituted pyrazoles
DE10162121A1 (de) * 2001-12-12 2003-06-18 Berolina Drug Dev Ab Svedala Deuterierte substituierte Pyrazolyl-Benzolsulfonamide sowie diese Verbindungen enthaltende Arzneimittel
SG128438A1 (en) 2002-03-15 2007-01-30 Sumitomo Chemical Co Polymer compound and polymer light emitting deviceusing the same
US7235560B2 (en) * 2002-08-19 2007-06-26 Glaxo Group Limited Pyrimidine derivative as selective COX-2 inhibitors
DE10261807A1 (de) * 2002-12-19 2004-07-01 Turicum Drug Development Ag Deuterierte Catecholaminderivate sowie diese Verbindungen enthaltende Arzneimittel
JP2004326857A (ja) 2003-04-22 2004-11-18 Sony Corp 光磁気ディスクおよびその記録再生方法
WO2005041885A2 (en) * 2003-10-31 2005-05-12 Metaphore Pharmaceuticals, Inc. Compositions and methods for treating, preventing, reversing and inhibiting pain
US7863274B2 (en) * 2005-07-29 2011-01-04 Concert Pharmaceuticals Inc. Deuterium enriched analogues of tadalafil as PDE5 inhibitors
KR101380190B1 (ko) * 2005-07-29 2014-04-11 콘서트 파마슈티컬즈, 인크. 벤조 〔d〕〔1,3〕―디옥솔 유도체
CA2624179A1 (en) * 2005-10-06 2007-04-12 Auspex Pharmaceuticals, Inc. Deuterated inhibitors of gastric h+, k+-atpase with enhanced therapeutic properties
DK1954669T3 (da) 2005-12-01 2015-10-12 Auspex Pharmaceuticals Inc Substituerede phenethylaminer med serotonerg og/eller norepinephrinerg aktivitet
UA97795C2 (uk) * 2006-02-17 2012-03-26 Бьордз Фарма Гмбх Бероліна Інновейтів Ресерч Унд Девелопмент Сервісіз Дейтеровані похідні катехоламіну і медикаменти, що містять згадані сполуки
EP1993994A2 (en) * 2006-03-16 2008-11-26 Vertex Pharmceuticals Incorporated Deuterated hepatitis c protease inhibitors
WO2007140189A2 (en) * 2006-05-26 2007-12-06 Auspex Pharmaceuticals, Inc. Preparation and utility of substituted carboxylic acid compounds
AU2007256893A1 (en) * 2006-06-05 2007-12-13 Auspex Pharmaceuticals, Inc. Preparation and utility of substituted imidazopyridine compounds with hypnotic effects
US20080039473A1 (en) * 2006-08-08 2008-02-14 Auspex Pharmaceuticals, Inc. Preparation and utility of substituted quinazoline compounds with alpha-adrenergic blocking effects
US20110053964A1 (en) * 2006-08-22 2011-03-03 Roger Tung 4-aminoquinazoline derivatives and methods of use thereof
JP2010501572A (ja) * 2006-08-22 2010-01-21 コンサート ファーマシューティカルズ インコーポレイテッド 4−アミノキナゾリン誘導体およびその使用方法
US20080103154A1 (en) * 2006-08-24 2008-05-01 Concert Pharmaceuticals Inc. 3, 4-dihydro-2(IH)-quinolinone and 2(1H)-quinolinone derivatives
JP2010507585A (ja) * 2006-10-19 2010-03-11 オースペックス・ファーマシューティカルズ・インコーポレイテッド 置換インドール
WO2008066620A2 (en) * 2006-10-20 2008-06-05 Concert Pharmaceuticals Inc. Dibenzothiazepine derivatives
US20080280927A1 (en) * 2006-10-20 2008-11-13 Concert Pharmaceuticals Inc. 3-(dihydro-1h-pyrazolo[4,3-d]pyrimidin-5-yl)-4-propoxybenzenesulfonamide derivatives and methods of use
US20090270425A1 (en) * 2006-10-20 2009-10-29 Concert Pharmaceuticals Inc. 3-(dihydro-1h-pyrazolo[4,3-d]pyrimidin-5-yl)-4-propoxybenzenesulfonamide derivatives and methods of use
AU2007329728A1 (en) * 2006-10-20 2008-06-12 Concert Pharmaceuticals Inc. 3-(dihydro-1H-pyrazolo (4,3-d) pyrimidin-5-yl)-4-propoxybenzenesulfonamide derivatives and methods of use
US20090197899A1 (en) * 2006-10-20 2009-08-06 Concert Pharmaceuticals Inc. 3-(Dihydro-1H-pyrazolo[4,3-d]pyrimidin-5-yl)-4-propoxybenzenesulfonamide Derivatives and Methods of Use
US8796267B2 (en) * 2006-10-23 2014-08-05 Concert Pharmaceuticals, Inc. Oxazolidinone derivatives and methods of use
CA2703011A1 (en) * 2006-10-23 2008-10-23 Concert Pharmaceuticals Inc. Oxazolidinone derivatives and methods of use
US7932235B2 (en) * 2006-11-17 2011-04-26 Concert Pharmaceuticals, Inc. Triazolyl tropane derivatives
US20080146573A1 (en) * 2006-12-04 2008-06-19 Auspex Pharmaceuticals, Inc. Preparation and utility of substituted oxzolidinones
EP2121572A2 (en) * 2006-12-08 2009-11-25 Auspex Pharmaceuticals Inc. Preparation and utility of substituted allylamines
US20100260674A1 (en) * 2006-12-15 2010-10-14 Concert Pharmaceuticals, Inc. Quinazoline derivatives and methods of treatment
US8343950B2 (en) * 2006-12-15 2013-01-01 Concert Pharmaceuticals, Inc. Quinazoline derivatives and methods of treatment
US20090325976A1 (en) * 2006-12-21 2009-12-31 Concert Pharmaceuticals Inc. Prostacyclin derivatives
US8080549B2 (en) * 2007-01-12 2011-12-20 Concert Pharmaceuticals, Inc. Endothelin receptor antagonists
WO2008088727A2 (en) * 2007-01-12 2008-07-24 Concert Pharmaceuticals, Inc. Endothelin receptor antagonists
US20080262006A1 (en) * 2007-02-02 2008-10-23 Harbeson Scott L Selective endothelin type-a antagonists
US20100076010A1 (en) * 2007-02-26 2010-03-25 Concert Pharmaceuticals, Inc. Alpha 1a-adrenoceptor antagonists
WO2008106125A2 (en) * 2007-02-26 2008-09-04 Concert Pharmaceuticals, Inc. Deuterated derivatives of silodosin as alpha la-adrenoceptor antagonists
ES2395241T3 (es) * 2007-03-07 2013-02-11 Concert Pharmaceuticals Inc. Derivados deuterados de piperazina como compuestos antianginosos
EP3103790B1 (en) 2007-03-15 2018-05-09 Auspex Pharmaceuticals, Inc. Substituted phenethylamine with serotoninergic and/or norepinephrinergic activity
ES2559838T3 (es) 2007-03-16 2016-02-16 Concert Pharmaceuticals, Inc. Inhibidores de proteína de transferencia de ésteres de colesterol
WO2008122010A1 (en) * 2007-04-02 2008-10-09 Concert Pharmaceuticals, Inc. Pharmaceutical calcimimetics
KR101502959B1 (ko) * 2007-04-11 2015-03-16 깃세이 야쿠힌 고교 가부시키가이샤 5원환 헤테로환 유도체 및 그 의약 용도
US8198305B2 (en) * 2007-04-13 2012-06-12 Concert Pharmaceuticals Inc. 1,2-benzisoxazol-3-yl compounds
US8349817B2 (en) * 2007-04-25 2013-01-08 Concert Pharmaceuticals, Inc. Analogues of cilostazol
EP2527336A1 (en) * 2007-04-25 2012-11-28 Concert Pharmaceuticals Inc. Deuterated analogues of cilostazol
CN101687868B (zh) * 2007-05-01 2012-12-12 康塞特医药品公司 吗啡烷化合物
EP2150525A1 (en) * 2007-05-01 2010-02-10 Concert Pharmaceuticals Inc. Naphthyl(ethyl) acetamides
FI3825306T3 (fi) 2007-05-01 2023-08-23 Concert Pharmaceuticals Inc Morfinaaniyhdisteitä
US20080280991A1 (en) * 2007-05-08 2008-11-13 Auspex Pharmaceuticals, Inc. Substituted naphthalenes
WO2008141021A1 (en) * 2007-05-08 2008-11-20 Concert Pharmaceuticals, Inc. Deuterated derivatives of tetrahydrotriazolopyrazine compounds and their use as dpp-iv inhibitors
US20080306151A1 (en) * 2007-06-11 2008-12-11 Protia, Llc Deuterium-enriched fenofibrate
DE602008000255D1 (de) 2007-06-12 2009-12-17 Concert Pharmaceuticals Inc Azapeptid-Derivate als HIV-Protease-Inhibitoren
JP2010529994A (ja) * 2007-06-13 2010-09-02 オースペックス・ファーマシューティカルズ・インコーポレイテッド 置換ピペラジン
US20090005366A1 (en) * 2007-06-19 2009-01-01 Protia, Llc Deuterium-enriched olanzapine
US20080318920A1 (en) * 2007-06-19 2008-12-25 Protia, Llc Deuterium-enriched ezetimibe
US20080319004A1 (en) * 2007-06-19 2008-12-25 Protia, Llc Deuterium-enriched clopidogrel
EP2170828B1 (en) 2007-06-20 2012-11-21 Auspex Pharmaceuticals, Inc. Substituted n-aryl pyridinones as fibrotic inhibitors
US20080318915A1 (en) * 2007-06-20 2008-12-25 Protia, Llc Deuterium-enriched fluticasone propionate
US7915309B2 (en) * 2007-06-20 2011-03-29 Protia, Llc Deuterium-enriched oseltamivir
WO2009009531A2 (en) * 2007-07-09 2009-01-15 Concert Pharmaceuticals Inc. Pyrimidinecarboxamide derivatives for the treatment of hiv infections
EP2170825A2 (en) * 2007-07-30 2010-04-07 Auspex Pharmaceuticals, Inc. Substituted indoles
ES2425183T3 (es) * 2007-08-14 2013-10-11 Concert Pharmaceuticals Inc. Derivados de oxazolidinonas sustituidas
US20090062283A1 (en) * 2007-08-29 2009-03-05 Protia, Llc Deuterium-enriched linezolid
US20090062305A1 (en) * 2007-08-29 2009-03-05 Protia, Llc Deuterium-enriched cetirizine
US20090062385A1 (en) * 2007-08-29 2009-03-05 Protia, Llc Deuterium-enriched fesoterodine
US20090062399A1 (en) * 2007-08-29 2009-03-05 Protia, Llc Deuterium-enriched sertraline
US20090062561A1 (en) * 2007-08-29 2009-03-05 Protia, Llc Deuterium-enriched latanoprost
US20090062393A1 (en) * 2007-08-29 2009-03-05 Protia, Llc Deuterium-enriched pregabalin
US20090062299A1 (en) * 2007-08-29 2009-03-05 Protia, Llc Deuterium-enriched doxazosin
US20090062316A1 (en) * 2007-08-29 2009-03-05 Protia, Llc Deuterium-enriched pelitrexol
US20090062374A1 (en) * 2007-08-29 2009-03-05 Protia, Llc Deuterium-enriched lasofoxifene
US20090069375A1 (en) * 2007-09-09 2009-03-12 Protia, Llc Deuterium-enriched miglustat
US20090069357A1 (en) * 2007-09-09 2009-03-12 Protia, Llc Deuterium-enriched iclaprim
US20090069413A1 (en) * 2007-09-09 2009-03-12 Protia, Llc Deuterium-enriched olopatadine
US20090069410A1 (en) * 2007-09-09 2009-03-12 Protia, Llc Deuterium-enriched paclitaxel
US20090069352A1 (en) * 2007-09-09 2009-03-12 Protia, Llc Deuterium-enriched clazosentan
US20090131485A1 (en) * 2007-09-10 2009-05-21 Concert Pharmaceuticals, Inc. Deuterated pirfenidone
US20090069339A1 (en) * 2007-09-11 2009-03-12 Protia, Llc Deuterium-enriched ciprofloxacin
EP2197847B1 (en) * 2007-09-12 2012-11-07 Concert Pharmaceuticals Inc. Deuterated 4 -oxoquinoline derivative for the treatment of hiv infection
US20090069431A1 (en) * 2007-09-12 2009-03-12 Protia, Llc Deuterium-enriched milnacipran
US8288414B2 (en) * 2007-09-12 2012-10-16 Deuteria Pharmaceuticals, Inc. Deuterium-enriched lenalidomide
US20090076165A1 (en) * 2007-09-12 2009-03-19 Protia, Llc Deuterium-enriched memantine
CA2698808A1 (en) 2007-09-13 2009-03-19 Concert Pharmaceuticals, Inc. Synthesis of deuterated catechols and benzo[d][1,3] dioxoles and derivatives thereof
US7919516B2 (en) * 2007-09-13 2011-04-05 Protia, Llc Deuterium-enriched ondansetron
US20090076118A1 (en) * 2007-09-13 2009-03-19 Protia, Llc Deuterium-enriched saxagliptin
US20090076116A1 (en) * 2007-09-13 2009-03-19 Protia, Llc Deuterium-enriched carvediolo
US20090076010A1 (en) * 2007-09-13 2009-03-19 Protia, Llc Deuterium-enriched lamotrigine
US20090076112A1 (en) * 2007-09-13 2009-03-19 Protia, Llc Deuterium-enriched eltrombopag
US20090076161A1 (en) * 2007-09-13 2009-03-19 Protia, Llc Deuterium-enriched bupropion
US20090075965A1 (en) * 2007-09-13 2009-03-19 Protia, Llc Deuterium-enriched amoxicilin
US20090076038A1 (en) * 2007-09-14 2009-03-19 Protia, Llc Deuterium-enriched entecavir
US20090075991A1 (en) * 2007-09-14 2009-03-19 Protia, Llc Deuterium-enriched efavirenz
US20090075994A1 (en) * 2007-09-14 2009-03-19 Protia, Llc Deuterium-enriched radafaxine
US20090076102A1 (en) * 2007-09-14 2009-03-19 Protia, Llc Deuterium-enriched muraglitazar
US20090076025A1 (en) * 2007-09-14 2009-03-19 Protia, Llc Deuterium-enriched dasatinib
US20090076148A1 (en) * 2007-09-14 2009-03-19 Protia, Llc Deuterium-enriched pravastatin
US20090076039A1 (en) * 2007-09-14 2009-03-19 Protia, Llc Deuterium-enriched valacyclovir
US20090076034A1 (en) * 2007-09-14 2009-03-19 Protia, Llc Deuterium-enriched bms-690514
US20090076000A1 (en) * 2007-09-15 2009-03-19 Protia, Llc Deuterium-enriched mycophenolate mofetil
US20090076018A1 (en) * 2007-09-15 2009-03-19 Protia, Llc Deuterium-enriched ranolazine
US20090076017A1 (en) * 2007-09-15 2009-03-19 Protia, Llc Deuterium-enriched trabectedin
US20090076157A1 (en) * 2007-09-15 2009-03-19 Protia, Llc Deuterium-enriched senicapoc
US20090076164A1 (en) * 2007-09-15 2009-03-19 Protia, Llc Deuterium-enriched tapentadol
US20090076163A1 (en) * 2007-09-15 2009-03-19 Protia, Llc Deuterium-enriched dapoxetine
US20090076028A1 (en) * 2007-09-15 2009-03-19 Protia, Llc Deuterium-enriched itraconazole
US20090076040A1 (en) * 2007-09-15 2009-03-19 Protia, Llc Deuterium-enriched valganciclovir
US20090076138A1 (en) * 2007-09-15 2009-03-19 Protia, Llc Deuterium-enriched darunavir
US20090075953A1 (en) * 2007-09-15 2009-03-19 Protia, Llc Deuterium-enriched ed-71
US20090076264A1 (en) * 2007-09-15 2009-03-19 Protia, Llc Deuterium-enriched rivaroxaban
US20090076128A1 (en) * 2007-09-15 2009-03-19 Protia Llc Deuterium-enriched topiramate
US20090075944A1 (en) * 2007-09-15 2009-03-19 Protia, Llc Deuterium-enriched ibandronate
US20090076167A1 (en) * 2007-09-17 2009-03-19 Protia, Llc Deuterium-enriched tramiprosate
US20090076117A1 (en) * 2007-09-17 2009-03-19 Protia, Llc Deuterium-enriched laropiprant
US20090076126A1 (en) * 2007-09-17 2009-03-19 Protia, Llc Deuterium-enriched enalapril
US20090118238A1 (en) * 2007-09-17 2009-05-07 Protia, Llc Deuterium-enriched alendronate
US20090076027A1 (en) * 2007-09-17 2009-03-19 Protia, Llc Deuterium-enriched lurasidone
US20090075947A1 (en) * 2007-09-17 2009-03-19 Protia, Llc Deuterium-enriched fospropofol
US20090076134A1 (en) * 2007-09-17 2009-03-19 Protia, Llc Deuterium-enriched simvastatin
US20090076144A1 (en) * 2007-09-17 2009-03-19 Protia, Llc Deuterium-enriched bazedoxifene
US20090076058A1 (en) * 2007-09-17 2009-03-19 Protia, Llc Deuterium-enriched finasteride
US20090076153A1 (en) * 2007-09-17 2009-03-19 Protia, Llc Deuterium-enriched tigecycline
US20090076154A1 (en) * 2007-09-17 2009-03-19 Protia, Llc Deuterium-enriched vorinostat
US20090075997A1 (en) * 2007-09-19 2009-03-19 Protia, Llc Deuterium-enriched satavaptan
US20090076127A1 (en) * 2007-09-19 2009-03-19 Protia, Llc Deuterium-enriched larotaxel
US20090076159A1 (en) * 2007-09-19 2009-03-19 Protia, Llc Deuterium-enriched eplivanserin
US20090076011A1 (en) * 2007-09-19 2009-03-19 Protia, Llc Deuterium-enriched tirapazamine
US20090082334A1 (en) * 2007-09-25 2009-03-26 Protia, Llc Deuterium-enriched quetiapine
US20090082323A1 (en) * 2007-09-25 2009-03-26 Protia, Llc Deuterium-enriched fulvestrant
US20090082382A1 (en) * 2007-09-25 2009-03-26 Protia, Llc Deuterium-enriched naltrexone
US20090082454A1 (en) * 2007-09-25 2009-03-26 Protia, Llc Deuterium-enriched disufenton
US20090082380A1 (en) * 2007-09-25 2009-03-26 Protia, Llc Deuterium-enriched rosuvastatin
US20090082312A1 (en) * 2007-09-25 2009-03-26 Protia, Llc Deuterium-enriched zoledronic acid
US20090082462A1 (en) * 2007-09-25 2009-03-26 Protia, Llc Deuterium-enriched armodafinil
US20090082376A1 (en) * 2007-09-26 2009-03-26 Protia, Llc Deuterium-enriched alogliptin
US20090082436A1 (en) * 2007-09-26 2009-03-26 Protia, Llc Deuterium-enriched rivastigmine
US20090082363A1 (en) * 2007-09-26 2009-03-26 Protia, Llc Deuterium-enriched posaconazole
US20090082471A1 (en) * 2007-09-26 2009-03-26 Protia, Llc Deuterium-enriched fingolimod
US20090082432A1 (en) * 2007-09-26 2009-03-26 Protia, Llc Deuterium-enriched ramelteon
US8722710B2 (en) 2007-09-26 2014-05-13 Deuterx, Llc Deuterium-enriched pioglitazone
US20090082318A1 (en) * 2007-09-26 2009-03-26 Protia, Llc Deuterium-enriched mometasone
US20090082442A1 (en) * 2007-09-26 2009-03-26 Protia, Llc Deuterium-enriched lubiprostone
US20090082387A1 (en) * 2007-09-26 2009-03-26 Protia, Llc Deuterium-enriched nvp-bez234
US20090082364A1 (en) * 2007-09-26 2009-03-26 Protia, Llc Deuterium-enriched levocedtirizine
US20090082335A1 (en) * 2007-09-26 2009-03-26 Protia, Llc Deuterium-enriched oxcarbazepine
US20090082452A1 (en) * 2007-09-26 2009-03-26 Protia, Llc Deuterium-enriched lumiracoxib
US20090082459A1 (en) * 2007-09-26 2009-03-26 Protia, Llc Deuterium-enriched guanfacine
WO2009051747A1 (en) * 2007-10-15 2009-04-23 Concert Pharmaceuticals, Inc. Deuterated lorcaserin
EP2212298B1 (en) * 2007-10-18 2013-03-27 Concert Pharmaceuticals Inc. Deuterated etravirine
WO2009054964A1 (en) * 2007-10-22 2009-04-30 Concert Pharmaceuticals, Inc. Alpha-aminoamide derivatives
US20090131363A1 (en) * 2007-10-26 2009-05-21 Harbeson Scott L Deuterated darunavir
US8592487B2 (en) * 2007-10-26 2013-11-26 Concert Pharmaceuticals, Inc. Deuterated darunavir
US8093276B2 (en) * 2007-10-31 2012-01-10 Bristol-Myers Squibb Company Alpha-(N-sulfonamido)acetamide compound as an inhibitor of beta amyloid peptide production
WO2009061374A2 (en) * 2007-11-02 2009-05-14 Concert Pharmaceuticals, Inc. Deuterated fingolimod
JP2011503231A (ja) * 2007-11-20 2011-01-27 コンサート ファーマシューティカルズ インコーポレイテッド Hcv感染処置のためのペプチド
ES2396366T3 (es) * 2007-12-10 2013-02-21 Concert Pharmaceuticals Inc. Inhibidores heterocíclicos de quinasas
US8084464B2 (en) * 2007-12-18 2011-12-27 Concert Pharmaceuticals, Inc. Tetrahydroisoquinoline derivatives
WO2009094210A1 (en) * 2008-01-22 2009-07-30 Concert Pharmaceuticals Inc. Vandetanib derivatives
EP2242493B1 (en) * 2008-01-22 2013-06-05 Concert Pharmaceuticals Inc. Derivatives of gefitinib
WO2009102707A2 (en) * 2008-02-11 2009-08-20 Auspex Pharmaceuticals, Inc. Substituted oxazaphosphorines
US20090209550A1 (en) * 2008-02-20 2009-08-20 Auspex Pharmaceuticals, Inc. Substituted triazolopyridines
EP2265334A2 (en) 2008-02-29 2010-12-29 Concert Pharmaceuticals, Inc. Substituted xanthine derivatives
WO2009114814A2 (en) 2008-03-14 2009-09-17 Retrotope, Inc. Therapeutic substances that modulate genome methylation
EP2268604B1 (en) * 2008-03-14 2017-02-15 Retrotope, Inc. Therapies for cancer using isotopically substituted lysine
JP2011516426A (ja) * 2008-03-28 2011-05-26 コンサート ファーマシューティカルズ インコーポレイテッド キナゾリン誘導体および治療方法
JP2011518783A (ja) * 2008-04-09 2011-06-30 コンサート ファーマシューティカルズ インコーポレイテッド 3−(2−ヒドロキシ−5−メチルフェニル)−n,n−ジイソプロピル−3−フェニルプロピルアミンの誘導体およびその使用方法
US8168814B2 (en) * 2008-04-10 2012-05-01 New Mexico Highlands University Synthesis of phosphonic acid labeled compounds
US20100120786A1 (en) * 2008-04-17 2010-05-13 Concert Pharmaceuticals, Inc. Piperazine Derivatives
US20110129549A1 (en) * 2008-04-17 2011-06-02 Liu Julie F Tricyclic benzo[5,6]cyclohepta[1,2-b]pyridine derivatives and uses thereof
WO2009128947A1 (en) * 2008-04-17 2009-10-22 Concert Pharmaceuticals, Inc. Piperazine derivatives
US20090285811A1 (en) * 2008-05-13 2009-11-19 Auspex Pharmaceuticals, Inc. Anti-inflammatory and immunosuppressive glucocorticoid steroids
US20110160253A1 (en) * 2008-05-28 2011-06-30 Harbeson Scott L Deuterated tizanidine
US8354557B2 (en) * 2008-06-17 2013-01-15 Concert Pharmaceuticals, Inc. Synthesis of deuterated morpholine derivatives
US20110294815A1 (en) * 2008-06-27 2011-12-01 Harbeson Scott L Prostacyclin analogs
US20100016365A1 (en) * 2008-07-17 2010-01-21 Auspex Pharmaceuticals, Inc. Substituted 4-amino-piperidines
WO2010011868A2 (en) * 2008-07-23 2010-01-28 Auspex Pharmaceuticals Pyridine sulfonamide modulators of endothelin-a-receptor
WO2010019557A1 (en) * 2008-08-12 2010-02-18 Concert Pharmaceuticals Inc. N-phenyl-2-pyrimidineamine derivatives
PL2328414T3 (pl) 2008-08-29 2014-05-30 Concert Pharmaceuticals Inc Podstawione pochodne triazolo-pirydazyny
US20100105755A1 (en) * 2008-09-12 2010-04-29 Auspex Pharmaceuticals, Inc. Substituted benzamide modulators of dopamine receptor
US8704001B2 (en) * 2008-09-16 2014-04-22 Concert Pharmaceuticals, Inc. Deuterated 2-amino-3-hydroxypropanoic acid derivatives
WO2010033270A1 (en) * 2008-09-17 2010-03-25 Auspex Pharmaceuticals, Inc. Dibenzothiazepine modulators of dopamine, alpha adrenergic, and serotonin receptors
BRPI0913457B8 (pt) * 2008-09-18 2021-08-31 Auspex Pharmaceutical Inc Composto e composição farmacêutica
BRPI0918760A2 (pt) 2008-09-19 2015-12-29 Concert Pharmaceuticals Inc compostos morfinanos
US20100087455A1 (en) * 2008-10-06 2010-04-08 Auspex Pharmaceuticals, Inc. Substituted xanthine compounds
US20100099701A1 (en) * 2008-10-20 2010-04-22 Auspex Pharmaceuticals, Inc. Isoquinolinone modulators of 5-ht3 receptors
US20100113431A1 (en) * 2008-11-05 2010-05-06 Auspex Pharmaceuticals, Inc. N-methyl piperazine modulators of h1 receptor
US20100120733A1 (en) * 2008-11-07 2010-05-13 Auspex Pharmaceuticals, Inc. Steroid modulators of glucocorticoid receptor
US8227451B2 (en) * 2008-11-12 2012-07-24 Auspex Pharmaceuticals Phenylacetic acid inhibitors of cyclooxygenase
US9045453B2 (en) 2008-11-14 2015-06-02 Concert Pharmaceuticals, Inc. Substituted dioxopiperidinyl phthalimide derivatives
US20100137215A1 (en) * 2008-11-25 2010-06-03 Concert Pharmaceuticals Inc. Novel tetrahydro-1h-pyrido[4,3-b]indoles
WO2010065755A1 (en) * 2008-12-04 2010-06-10 Concert Pharmaceuticals, Inc. Deuterated pyridinones
US20100143354A1 (en) * 2008-12-04 2010-06-10 Auspex Pharmaceuticals, Inc. Triazine dna modifiers
US20100144657A1 (en) * 2008-12-09 2010-06-10 Auspex Pharmaceuticals, Inc. PHENYLPIPERIDINE MODULATORS OF mu-OPIOID RECEPTORS
WO2010075086A2 (en) * 2008-12-15 2010-07-01 Auspex Pharmaceuticals, Inc. Pyrrolidinone inhibitors of pde-4
AU2009330131B2 (en) * 2008-12-23 2015-09-03 Aquilus Pharmaceuticals, Inc Compounds and methods for the treatment of pain and other diseases
US20120053159A1 (en) * 2009-02-11 2012-03-01 Muller George W Isotopologues of lenalidomide
US8263601B2 (en) * 2009-02-27 2012-09-11 Concert Pharmaceuticals, Inc. Deuterium substituted xanthine derivatives
US8952016B2 (en) * 2009-02-27 2015-02-10 Concert Pharmaceuticals, Inc. Substituted xanthine derivatives
US8563554B2 (en) 2009-03-17 2013-10-22 Concert Pharmaceuticals, Inc. Deuterated pyrazinoisoquinoline compounds
US8044077B2 (en) * 2009-03-19 2011-10-25 Bristol-Myers Squibb Company Alpha-(N-sulfonamido)acetamide compounds incorporating deuterium as inhibitors of beta amyloid peptide production
US8778998B2 (en) 2009-04-10 2014-07-15 Auspex Pharmaceuticals, Inc. Biphenyl-3-carboxylic acid modulators of beta-3-adrenoreceptor
CA2759026C (en) * 2009-04-20 2019-01-15 Auspex Pharmaceuticals, Inc. Piperidine inhibitors of janus kinase 3
US20100291151A1 (en) * 2009-04-21 2010-11-18 Auspex Pharmaceuticals, Inc. 1-methylpyrazole modulators of substance p, calcitonin gene-related peptide, adrenergic receptor, and/or 5-ht receptor
US8461197B2 (en) 2009-04-23 2013-06-11 Concert Pharmaceuticals, Inc. 4-hydroxybutyric acid analogs
US20100305173A1 (en) * 2009-04-30 2010-12-02 Concert Pharmaceuticals, Inc. Hydroxyethylamino sulfonamide derivatives
US9468637B2 (en) 2009-05-13 2016-10-18 Intra-Cellular Therapies, Inc. Organic compounds
US8410082B2 (en) 2009-05-22 2013-04-02 Concert Pharmaceuticals, Inc. Fluorinated diaryl urea derivatives
US20110053968A1 (en) * 2009-06-09 2011-03-03 Auspex Pharmaceuticals, Inc. Aminopyrimidine inhibitors of tyrosine kinase
US20120077851A1 (en) * 2009-06-09 2012-03-29 Medolution Limited Urea Derivatives as Kinase Inhibitors
US8586760B2 (en) * 2009-06-15 2013-11-19 Auspex Pharmaceuticals, Inc. Aminothiazole modulators of beta-3-adrenoreceptor
ME01883B (me) 2009-06-18 2014-12-20 Concert Pharmaceuticals Inc Deuterijumski derivati izoindolin-1,3-diona kao inhibitori pde4 i tnf-alfa
US8501738B2 (en) 2009-06-23 2013-08-06 Concert Pharmaceuticals, Inc. Substituted triazolo-pyridazine derivatives
US20100325228A1 (en) * 2009-06-23 2010-12-23 Alon Novy Systems and methods for distributed activity management system
WO2011009075A2 (en) * 2009-07-17 2011-01-20 Rigel Pharmaceuticals, Inc. Deuterated 2, 4-pyrimidinediamine compounds and prodrugs thereof and their uses
EP2456311A4 (en) * 2009-07-24 2013-01-23 Concert Pharmaceuticals Inc SUBSTITUTED IMIDASOTRIAZINES
US8802850B2 (en) 2009-07-27 2014-08-12 Auspex Pharmaceuticals, Inc. Cyclopropyl modulators of P2Y12 receptor
US8575348B2 (en) * 2009-07-28 2013-11-05 Auspex Pharmaceuticals, Inc Quinolone inhibitors of lipoprotein-associated phospholipase A2
US9512104B2 (en) 2009-07-28 2016-12-06 Auspex Pharmaceuticals, Inc. Quinolone inhibitors of lipoprotein-associated phospholipase A2
US8637524B2 (en) * 2009-07-28 2014-01-28 Auspex Pharmaceuticals, Inc Pyrimidinone inhibitors of lipoprotein-associated phospholipase A2
US8618116B2 (en) * 2009-08-03 2013-12-31 Daljit Singh Dhanoa Deuterium-enriched pyrimidine compounds and derivatives
EP2464355A4 (en) * 2009-08-14 2013-01-02 Concert Pharmaceuticals Inc SUBSTITUTED TRIAZOLPHTHALAZINE DERIVATIVES
WO2011028820A1 (en) 2009-09-02 2011-03-10 Concert Pharmaceuticals, Inc. Substituted derivatives of bicyclic [4.3.0] heteroaryl compounds
US8278460B2 (en) * 2009-10-15 2012-10-02 Concert Pharmaceuticals, Inc. Substituted benzimidazoles
US9260424B2 (en) * 2009-10-26 2016-02-16 Auspex Pharmaceuticals, Inc. 4,6-diaminopyrimidine stimulators of soluble guanylate cyclase
KR20120092142A (ko) * 2009-10-28 2012-08-20 애나디스 파마슈티칼스, 인코포레이티드 중수소화 5,6-다이하이드로-1h-파이리딘-2-온 화합물
US20110117214A1 (en) * 2009-11-16 2011-05-19 Auspex Pharmaceuticals, Inc. Cyclohexyl urea modulators of d2 receptors and/or d3 receptors
US8471034B2 (en) * 2009-11-18 2013-06-25 Concert Pharmaceuticals, Inc. Niacin prodrugs and deuterated versions thereof
WO2011061243A1 (en) * 2009-11-21 2011-05-26 F. Hoffmann-La Roche Ag Heterocyclic antiviral compounds
US20110152303A1 (en) * 2009-12-18 2011-06-23 Glaxosmithkline Llc Chemical Compounds
US20110178180A1 (en) * 2010-01-18 2011-07-21 Kurt Nielsen Deuterium-enriched colchicine, thiocolchicine, and derivatives thereof; methods of preparation; and use thereof
US20110195066A1 (en) * 2010-02-05 2011-08-11 Auspex Pharmaceuticals, Inc. Quinoline inhibitors of tyrosine kinase
BR112012020585A2 (pt) * 2010-02-24 2018-04-17 Auspex Pharmaceuticals Inc composto, composição farmacêutica e método de tratamento de um distúrbio mediado por tirosina quinase
EP2542075A4 (en) * 2010-03-01 2014-11-05 Concert Pharmaceuticals Inc Fluorouracil DERIVATIVES
WO2011109464A1 (en) * 2010-03-02 2011-09-09 Concert Pharmaceuticals Inc. Deuterated tetrahydronaphthalene derivatives
US8575361B2 (en) 2010-03-02 2013-11-05 Concert Pharmaceuticals Inc. Tetrahydronaphthalene derivatives
US8575221B2 (en) 2010-03-17 2013-11-05 Concert Pharmaceuticals, Inc. Derivatives of dimethylcurcumin
WO2012009446A1 (en) 2010-07-16 2012-01-19 Concert Pharmaceuticals Inc. Novel pyrimidinecarboxamide derivatives
WO2012031072A1 (en) 2010-09-01 2012-03-08 Concert Pharmaceuticals, Inc. Process for preparing an enantiomerically enriched, deuterated secondary alcohol from a corresponding ketone without reducing deuterium incorporation
US9074233B2 (en) 2010-09-01 2015-07-07 Concert Pharmaceuticals, Inc. Process for preparing an enantiomerically enriched, deuterated secondary alcohol from a corresponding ketone without reducing deuterium incorporation
CA2810092A1 (en) * 2010-09-03 2012-03-08 IVAX International GmbH Deuterated analogs of pridopidine useful as dopaminergic stabilizers
IT1402047B1 (it) * 2010-10-19 2013-08-28 Cross Pharma Sa Uso del mexiprostil nel trattamento delle malattie infiammatorie intestinali
CN102464652B (zh) * 2010-11-02 2013-08-28 北京欧博方医药科技有限公司 咪唑衍生物、制备方法及用途
CN103619334A (zh) * 2011-01-19 2014-03-05 朱红文 噻唑烷衍生物和其治疗用途
WO2012102387A1 (ja) * 2011-01-27 2012-08-02 日産化学工業株式会社 ピラゾール誘導体及び有害生物防除剤
ES2804540T3 (es) 2011-02-14 2021-02-08 Concert Pharmaceuticals Inc Análogos deuterados de ácido 4–hidroxibutírico
WO2012112558A1 (en) 2011-02-14 2012-08-23 The Regents Of The University Of Michigan Compositions and methods for the treatment of obesity and related disorders
US9145390B2 (en) 2011-03-03 2015-09-29 Concert Pharmaceuticals, Inc. Derivatives of pyrazole-substituted amino-heteroaryl compounds
US8889687B2 (en) 2011-03-04 2014-11-18 Concert Pharmaceuticals, Inc. Deuterated pyrazinoisoquinoline compounds
AU2012225611B2 (en) 2011-03-08 2016-09-15 Auspex Pharmaceuticals, Inc. Substituted N-Aryl pyridinones
WO2012135299A1 (en) 2011-03-28 2012-10-04 Deuteria Pharmaceuticals Inc 2',6'-dioxo-3'-deutero-piperdin-3-yl-isoindoline compounds
US20140213553A1 (en) * 2011-05-03 2014-07-31 Concert Pharmaceuticals Inc. Carbamoylpyridone derivatives
WO2012151343A1 (en) * 2011-05-04 2012-11-08 Balance Therapeutics, Inc. Pentylenetetrazole derivatives
HUE047354T2 (hu) 2011-05-18 2020-04-28 Vertex Pharmaceuticals Europe Ltd Ivacaftor deuterizált származékai
EP2739617A4 (en) * 2011-07-27 2015-01-28 Nanjing Allgen Pharma Co Ltd SPIROCYCLIC MOLECULES AS PROTEIN KINASE INHIBITORS
US8389723B1 (en) * 2011-08-24 2013-03-05 Glaxosmithkline Llc Deuterated benzene sulfonamide thiazole compounds
IL298436B1 (en) 2012-01-23 2024-03-01 Sage Therapeutics Inc Pharmaceutical preparations that include allopregnanolone
BR112014019351A8 (pt) * 2012-02-08 2017-07-11 Merck Patent Gmbh Análogos de tiazolidinona deuterados como agonistas para o receptor do hormônio folículo estimulante
IN2014DN08443A (da) * 2012-04-13 2015-05-08 Concert Pharmaceuticals Inc
WO2013159026A1 (en) 2012-04-20 2013-10-24 Concert Pharmaceuticals, Inc. Deuterated rigosertib
WO2013168013A2 (en) * 2012-05-10 2013-11-14 Mahesh Kandula Compositions and methods for the treatment of chronic diseases and inflammatory disorders
US20150197525A1 (en) * 2012-06-15 2015-07-16 Concert Pharmaceuticals, Inc. Deuterated derivatives of ruxolitinib
WO2014008417A1 (en) 2012-07-04 2014-01-09 Concert Pharmaceuticals, Inc. Deuterated vercirnon
EP2885267B1 (en) 2012-07-12 2018-09-05 Concert Pharmaceuticals, Inc. Deuterated idebenone
MX2015001246A (es) 2012-07-30 2015-04-10 Concert Pharmaceuticals Inc Ibrutinib deuterado.
GB201214169D0 (en) * 2012-08-08 2012-09-19 Biostatus Ltd New compounds and uses thereof
EA031716B1 (ru) 2012-08-17 2019-02-28 Консерт Фармасьютикалс, Инк. Дейтерированный барицитиниб
US20150210624A1 (en) * 2012-08-22 2015-07-30 Concert Pharmaceuticals, Inc. Deuterated 4-hydroxybutyric acid analogs
AU2013312420A1 (en) * 2012-09-07 2015-02-26 Axikin Pharmaceuticals, Inc. Isotopically enriched arylsulfonamide CCR3 antagonists
NZ705372A (en) 2012-09-18 2018-07-27 Auspex Pharmaceuticals Inc Formulations pharmacokinetics of deuterated benzoquinoline inhibitors of vesicular monoamine transporter 2
US9550780B2 (en) 2012-09-18 2017-01-24 Auspex Pharmaceuticals, Inc. Formulations pharmacokinetics of deuterated benzoquinoline inhibitors of vesicular monoamine transporter 2
US9643950B2 (en) 2012-10-22 2017-05-09 Concert Pharmaceuticals, Inc. Solid forms of {s-3-(4-amino-1-oxo-isoindolin-2-yl)(piperidine-3,4,4,5,5-d5)-2,6-dione}
AU2014205472B2 (en) 2013-01-09 2018-05-10 Concert Pharmaceuticals Inc. Deuterated momelotinib
CA2935495C (en) 2013-01-14 2021-04-20 Deuterx, Llc 3-(5-substituted-4-oxoquinazolin-3(4h)-yl)-3-deutero-piperidine-2,6-dione derivatives
JP2016506957A (ja) * 2013-01-31 2016-03-07 オースペックス・ファーマシューティカルズ・インコーポレイテッドAuspex Pharmaceuticals, Inc. Vmat2のベンゾキノロン阻害剤
US20140221369A1 (en) * 2013-02-01 2014-08-07 Deuterx, Llc 5-deutero-2,4-thiazolidinedione and 5-deutero-2,4-oxazolidinedione derivatives and compositions comprising and methods of using the same
GB201302368D0 (en) * 2013-02-11 2013-03-27 Univ Bath Compound
US9801882B2 (en) 2013-02-17 2017-10-31 Intra-Cellular Therapies, Inc. Phosphodiesterase-1 inhibitors and their use in treatment of cardiovascular diseases
WO2014152843A1 (en) 2013-03-14 2014-09-25 Deuterx, Llc Deuterium-enriched 2,4-thiazolidinediones and methods of treatment
WO2014152833A1 (en) 2013-03-14 2014-09-25 Deuterx, Llc 3-(substituted-4-oxo-quinazolin-3(4h)-yl)-3-deutero-piperidine-2,6-dione derivatives
CA2906396A1 (en) 2013-03-15 2014-09-25 Concert Pharmaceuticals Inc. Inhibitors of the enzyme udp-glucose: n-acyl-sphingosine glucosyltransferase
US9365581B2 (en) * 2013-05-02 2016-06-14 The Regents Of The University Of Michigan Deuterated amlexanox
WO2015031741A1 (en) 2013-08-30 2015-03-05 Concert Pharmaceuticals, Inc. Deuterated derivatives of a thienotriazolodiazapine bromodomain-containing protein inhibitor
AU2014332080B2 (en) 2013-10-08 2020-02-27 AI Therapeutics, Inc. Rapamycin for the treatment of lymphangioleiomyomatosis
EA201791466A1 (ru) 2013-12-03 2017-11-30 Оспекс Фармасьютикалз, Инк. Способы получения соединений бензохинолина
DK3077397T3 (da) * 2013-12-06 2019-12-16 Vertex Pharma 2-amino-6-fluor-n-[5-fluor-pyridin-3-yl]pyrazolo[1,5-a]pyrimidin-3-carboxamidforbindelse anvendelig som atr-kinase-inhibitor, dens fremstilling, forskellige faste former og radiomarkerede derivater deraf
US9732031B2 (en) 2013-12-20 2017-08-15 Deuterx, Llc Methods of treating neurological and other disorders using enantiopure deuterium-enriched bupropion
WO2015109037A1 (en) 2014-01-15 2015-07-23 Deuterx, Llc Methods of treating neurological, metabolic, and other disorders using enantiopure deuterium-enriched pioglitazone
AU2015209330A1 (en) * 2014-01-27 2016-07-28 Auspex Pharmaceuticals, Inc. Benzoquinoline inhibitors of vesicular monoamine transporter 2
CN104817559B (zh) * 2014-01-30 2021-05-25 苏州泽璟生物制药股份有限公司 氘代喹唑啉酮化合物以及包含该化合物的药物组合物
JP6526060B2 (ja) 2014-02-10 2019-06-05 コンサート ファーマシューティカルズ インコーポレイテッド 置換トリアゾロベンゾジアゼピン
US10301268B2 (en) 2014-03-13 2019-05-28 The Salk Institute For Biological Studies Analogs of fexaramine and methods of making and using
EP3125893B1 (en) * 2014-04-04 2023-09-20 Intra-Cellular Therapies, Inc. Deuterated heterocycle fused gamma-carbolines as antagonists of 5-ht2a receptors
JP6525285B2 (ja) 2014-04-04 2019-06-05 エイアイ・セラピューティクス・インコーポレーテッド 加齢関連状態を処置するための吸入可能なラパマイシン配合物
CN104059030B (zh) * 2014-05-30 2016-05-04 镇江圣安医药有限公司 [(苯硫烷基)-苯基]哌嗪的衍生物及其药物组合物和用途
US9884872B2 (en) * 2014-06-20 2018-02-06 Intra-Cellular Therapies, Inc. Organic compounds
DK3177627T3 (da) 2014-08-07 2019-10-21 Intra Cellular Therapies Inc Imidazo[1,2-a]-pyrazolo[4,3-e]-pyrimidin-4-on-derivater med pde1-hæmmende aktivitet
KR20170095807A (ko) * 2014-10-07 2017-08-23 램 테라퓨틱스, 인코포레이티드 폐 고혈압의 치료를 위한 흡입가능 라파마이신 제제
US10160778B2 (en) 2014-10-27 2018-12-25 Concert Pharmaceuticals, Inc. Pyrimidine phosphonic acid esters
US11578097B2 (en) 2014-11-26 2023-02-14 Enanta Pharmaceuticals, Inc. Tetrazole derivatives of bile acids as FXR/TGR5 agonists and methods of use thereof
CA2966452A1 (en) * 2014-12-17 2016-06-23 Samuel David Brown Substituted bicyclic compounds as bromodomain inhibitors
US20180022710A1 (en) 2015-01-29 2018-01-25 Signal Pharmaceuticals, Llc Isotopologues of 2-(tert-butylamino)-4-((1r,3r,4r)-3-hydroxy-4-methylcyclohexylamino)-pyrimidine-5-carboxamide
CN105985396A (zh) * 2015-02-16 2016-10-05 苏州泽璟生物制药有限公司 氘代鹅去氧胆酸衍生物以及包含该化合物的药物组合物
EA201791977A1 (ru) 2015-03-06 2018-01-31 Оспекс Фармасьютикалз, Инк. Способы лечения патологических непроизвольных движений
WO2016160945A1 (en) 2015-03-31 2016-10-06 Concert Pharmaceuticals, Inc. Deuterated vx-661
EP3280420B1 (en) * 2015-04-10 2024-03-27 Sage Therapeutics, Inc. Compositions and methods for treating cns disorders
US10683305B2 (en) * 2015-04-27 2020-06-16 Concert Pharmaceuticals, Inc. Deuterated OTX-015
CN107698620A (zh) * 2015-06-23 2018-02-16 江苏天士力帝益药业有限公司 一种氘代噻吩并哌啶衍生物、制备方法及其应用
JP6595011B2 (ja) * 2015-06-26 2019-10-23 重▲慶▼迪康▲爾▼▲楽▼制▲薬▼有限公司 新規ホスホジエステラーゼ5阻害剤とその使用
US9809603B1 (en) 2015-08-18 2017-11-07 Deuterx, Llc Deuterium-enriched isoindolinonyl-piperidinonyl conjugates and oxoquinazolin-3(4H)-yl-piperidinonyl conjugates and methods of treating medical disorders using same
MA42954A (fr) 2015-09-25 2018-08-01 Vertex Pharmaceuticals Europe Ltd Potentialisateurs cftr deutérés
EP3365336B1 (en) * 2015-10-21 2023-07-26 Neuform Pharmaceuticals, Inc. Deuterated compounds for treating hematologic malignancies, and compositions and methods thereof
WO2017087795A1 (en) 2015-11-19 2017-05-26 Concert Pharmaceuticals, Inc. Deuterated epi-743
EP3407888B1 (en) 2016-01-26 2020-12-30 Intra-Cellular Therapies, Inc. Pyridopyrroloquinoxaline compounds, their compositions and uses
EP3407974A4 (en) 2016-01-29 2019-08-28 The Regents Of The University Of Michigan ANALOGUES OF AMLEXANOX
WO2017133360A1 (zh) * 2016-02-02 2017-08-10 深圳市塔吉瑞生物医药有限公司 一种甾体类化合物及包含该化合物的组合物及其用途
EP3416629A4 (en) 2016-02-16 2019-08-07 CoNCERT Pharmaceuticals, Inc. DEUTERATED GFT-505
US10364267B2 (en) * 2016-02-23 2019-07-30 Enanta Pharmaceuticals, Inc. Deuterated bile acid derivatives as FXR/TGR5 agonists and methods of use thereof
MA43815A (fr) 2016-03-08 2021-04-07 Sage Therapeutics Inc Stéroïdes neuroactifs, compositions, et leurs utilisations
EP3888656A1 (en) 2016-03-25 2021-10-06 Intra-Cellular Therapies, Inc. Deuterated heterocyclic gamma-carboline compounds and their use in the treatment or prophylaxis of a central nervous system disorder
JP2019510039A (ja) 2016-03-28 2019-04-11 イントラ−セルラー・セラピーズ・インコーポレイテッドIntra−Cellular Therapies, Inc. 新規組成物および方法
WO2018002673A1 (en) 2016-07-01 2018-01-04 N4 Pharma Uk Limited Novel formulations of angiotensin ii receptor antagonists
WO2018126143A1 (en) 2016-12-29 2018-07-05 Intra-Cellular Therapies, Inc. Organic compounds
WO2018126140A1 (en) 2016-12-29 2018-07-05 Intra-Cellular Therapies, Inc. Organic compounds
CN114805211A (zh) 2017-03-21 2022-07-29 润佳(苏州)医药科技有限公司 同位素富集3-氨基-1-丙磺酸衍生物、药物组合物及其用途
MX2021013640A (es) 2017-03-24 2022-08-31 Intra Cellular Therapies Inc Composiciones novedosas y metodos.
WO2018187804A1 (en) 2017-04-07 2018-10-11 Enanta Pharmaceuticals, Inc. Process for preparation of sulfonyl carbamate bile acid derivatives
CA3063901A1 (en) * 2017-05-16 2018-11-22 Vertex Pharmaceuticals Incorporated Deuterated pyridone amides and prodrugs thereof as modulators of sodium channels
WO2019104179A1 (en) 2017-11-22 2019-05-31 Concert Pharmaceuticals, Inc. Deuterated analogs of d-serine and uses thereof
SG11202004264VA (en) 2017-12-01 2020-06-29 Vertex Pharma Processes for making modulators of cystic fibrosis transmembrane conductance regulator
JP7150356B2 (ja) * 2017-12-22 2022-10-11 深▲チェン▼市塔吉瑞生物医薬有限公司 置換ピラゾロ[1,5-a]ピリミジン化合物並びにその医薬組成物および使用
WO2019144885A1 (zh) 2018-01-23 2019-08-01 深圳市塔吉瑞生物医药有限公司 取代的吡唑并[1,5-a]嘧啶类的大环化合物
WO2019152697A1 (en) 2018-01-31 2019-08-08 Intra-Cellular Therapies, Inc. Novel uses
CN109970745B (zh) * 2018-04-16 2020-12-08 深圳市塔吉瑞生物医药有限公司 取代的吡咯并三嗪类化合物及其药物组合物及其用途
EP3810134A4 (en) * 2018-06-19 2022-03-30 Celecor Therapeutics, Inc. DEUTERED RUC-4
US20210283132A1 (en) * 2018-07-12 2021-09-16 Shenzhen Targetrx, Inc. Diarylpyrazole compound, composition comprising same, and use thereof
BR112021003655A2 (pt) 2018-08-31 2021-05-18 Intra-Cellular Therapies, Inc. métodos novos
CA3108558A1 (en) 2018-08-31 2020-03-05 Intra-Cellular Therapies, Inc. Novel methods
CN111116492B (zh) * 2019-01-25 2021-07-09 青岛吉澳医药科技有限公司 氘代苯甲氨嘧啶二酮衍生物及其用途
US11116737B1 (en) 2020-04-10 2021-09-14 University Of Georgia Research Foundation, Inc. Methods of using probenecid for treatment of coronavirus infections
US11319313B2 (en) 2020-06-30 2022-05-03 Poxel Sa Crystalline forms of deuterium-enriched pioglitazone
US11767317B1 (en) 2020-06-30 2023-09-26 Poxel Sa Methods of synthesizing enantiopure deuterium-enriched pioglitazone
US20230150965A1 (en) * 2021-11-05 2023-05-18 Terran Biosciences, Inc. Isotopically enriched n-methyl-1,3-benzodioxolylbutanamine (mbdb) and stereoisomers thereof
US20230202998A1 (en) 2021-11-17 2023-06-29 Terran Biosciences, Inc. Phenethylamine compounds salts, polymorphic forms and methods of use thereof

Family Cites Families (17)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PH27357A (en) 1989-09-22 1993-06-21 Fujisawa Pharmaceutical Co Pyrazole derivatives and pharmaceutical compositions comprising the same
IL104311A (en) 1992-02-05 1997-07-13 Fujisawa Pharmaceutical Co Pyrazole derivatives, processes for the preparation thereof and pharmaceutical compositions containing the same
US5474995A (en) 1993-06-24 1995-12-12 Merck Frosst Canada, Inc. Phenyl heterocycles as cox-2 inhibitors
US5401765A (en) 1993-11-30 1995-03-28 G. D. Searle 1,4,5-triphenyl pyrazolyl compounds for the treatment of inflammation and inflammation-related disorders
US5434178A (en) 1993-11-30 1995-07-18 G.D. Searle & Co. 1,3,5 trisubstituted pyrazole compounds for treatment of inflammation
US5475018A (en) 1993-11-30 1995-12-12 G. D. Searle & Co. 1,5-diphenyl pyrazole compounds for treatment of inflammation
CN1061036C (zh) 1993-11-30 2001-01-24 G·D·瑟尔公司 用于治疗炎症的取代的吡唑基苯磺酰胺类化合物
CA2195847A1 (en) 1994-07-27 1996-02-08 John J. Talley Substituted thiazoles for the treatment of inflammation
US5620999A (en) 1994-07-28 1997-04-15 Weier; Richard M. Benzenesulfonamide subtituted imidazolyl compounds for the treatment of inflammation
US5585504A (en) 1994-09-16 1996-12-17 Merck & Co., Inc. Process of making cox-2 inhibitors having a lactone bridge
CA2206978A1 (en) 1994-12-21 1996-06-27 Merck Frosst Canada Inc. Diaryl-2-(5h)-furanones as cox-2 inhibitors
US5691374A (en) 1995-05-18 1997-11-25 Merck Frosst Canada Inc. Diaryl-5-oxygenated-2-(5H) -furanones as COX-2 inhibitors
US5756529A (en) * 1995-09-29 1998-05-26 G.D. Searle & Co. Substituted pyrazolyl benzenesulfonamides for use in veterinary therapies
GB9520584D0 (en) 1995-10-09 1995-12-13 Fujisawa Pharmaceutical Co Pyrazole derivatives,processes for preparation thereof and pharmaceutical composition comprising the same
UA57002C2 (uk) 1995-10-13 2003-06-16 Мерк Фросст Кенада Енд Ко./Мерк Фросст Кенада Енд Сі. Похідне (метилсульфоніл)феніл-2-(5н)-фуранону, фармацевтична композиція та спосіб лікування
DE69618820T2 (de) 1995-10-30 2002-06-20 Merck Frosst Canada Inc 3,4-diaryl-2-hydroxy-2,5-dihydrofurane als wirkstoffvorstufen von cox-2 inhibitoren
PT1104760E (pt) * 1999-12-03 2003-06-30 Pfizer Prod Inc Compostos de sulfamoil-heteroarilpirazole como agentes analgesicos e anti-inflamatorios

Also Published As

Publication number Publication date
BR0005703A (pt) 2001-07-31
MXPA00011844A (es) 2002-08-20
JP3338027B2 (ja) 2002-10-28
ES2193921T3 (es) 2003-11-16
JP2001163883A (ja) 2001-06-19
ATE234299T1 (de) 2003-03-15
EP1104760A1 (en) 2001-06-06
PT1104760E (pt) 2003-06-30
EP1104760B1 (en) 2003-03-12
DE60001623T2 (de) 2003-12-18
US6603008B1 (en) 2003-08-05
DE60001623D1 (de) 2003-04-17
US6951876B2 (en) 2005-10-04
US20030144280A1 (en) 2003-07-31
JP2002284682A (ja) 2002-10-03
CA2327385A1 (en) 2001-06-03

Similar Documents

Publication Publication Date Title
DK1104760T3 (da) Sulfamoylheteroarylpyrazolforbindelser som anti-inflammatoriske/analgetiske midler
DK1104759T3 (da) Heteroarylphenylpyrazolforbindelser som antiinflammatoriske/analgetiske midler
DE69528005T2 (de) Prolineamid-Derivate
FI953968A0 (fi) Antraniiliset happojohdannaiset
HUP0203971A2 (hu) Imidazoimidazolok és -triazolok mint gyulladásellenes szerek és ezeket tartalmazó gyógyszerkészítmények és alkalmazásuk
NO306778B1 (no) Heterocyklisk aromatisk oksazolforbindelse, mellomprodukter, farmasöytiske preparater inneholdende forbindelsene, rene cyklooksagenase-2 inhibitorer samt et antiinflammatorisk middel
LU91210I2 (fr) Emodepside & Praziquantel ainsi que leurs dérivés pharmaceutiqement acceptables (PROFENDER)
EA200200708A1 (ru) Производные бензазола и их применение в качестве модуляторов jnk
PT937722E (pt) Derivados de benzimidazole como inibidores de ciclooxigenase-2
AU7517400A (en) N-substituted 4-aminopteridines, synthesis and use thereof as pharmaceutical agent
FI940414A0 (fi) Kinoliini- tai kinatsoliinijohdannaiset, niiden valmistus ja käyttö
NO20022552L (no) Nye benzotiadiazinderivater, deres fremstilling og farmasöytiske sammensetninger inneholdende det samme
DE69600231T2 (de) N-Arylalkylphenylacetamidderivate
ES2074618T3 (es) 3-(1h-indazol-3-il)-4-piridinaminas, un procedimiento e intermediarios para su preparacion y su uso como medicamentos.
DE69528984D1 (de) Hemmung der leukotrienbiosynthese mittels harnstoffderivaten
DK316986A (da) Kemiske forbindelser, som er phosphodiesterase type iii inhibitorer