CN103228631B - Kat ii 抑制剂 - Google Patents

Kat ii 抑制剂 Download PDF

Info

Publication number
CN103228631B
CN103228631B CN201180057792.0A CN201180057792A CN103228631B CN 103228631 B CN103228631 B CN 103228631B CN 201180057792 A CN201180057792 A CN 201180057792A CN 103228631 B CN103228631 B CN 103228631B
Authority
CN
China
Prior art keywords
compound
pharmaceutically acceptable
acceptable salt
acid
mmol
Prior art date
Legal status (The legal status 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 status listed.)
Expired - Fee Related
Application number
CN201180057792.0A
Other languages
English (en)
Chinese (zh)
Other versions
CN103228631A (zh
Inventor
A·B·杜奈
C·J·赫拉尔
J·B·塔特尔
P·R·维尔霍斯特
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
SmithKline Beecham Ltd
Original Assignee
SmithKline Beecham Ltd
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 SmithKline Beecham Ltd filed Critical SmithKline Beecham Ltd
Publication of CN103228631A publication Critical patent/CN103228631A/zh
Application granted granted Critical
Publication of CN103228631B publication Critical patent/CN103228631B/zh
Expired - Fee Related legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/58—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems with hetero atoms directly attached to the ring nitrogen atom
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/08—Drugs for disorders of the alimentary tract or the digestive system for nausea, cinetosis or vertigo; Antiemetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/06—Anti-spasmodics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular 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
    • 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
    • A61P25/06—Antimigraine agents
    • 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
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/16—Otologicals
    • 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]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04—Antibacterial agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Pain & Pain Management (AREA)
  • Psychiatry (AREA)
  • Cardiology (AREA)
  • Hospice & Palliative Care (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Urology & Nephrology (AREA)
  • Psychology (AREA)
  • Oncology (AREA)
  • Addiction (AREA)
  • Communicable Diseases (AREA)
  • Immunology (AREA)
  • Vascular Medicine (AREA)
  • Rheumatology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Anesthesiology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Otolaryngology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Quinoline Compounds (AREA)
CN201180057792.0A 2010-12-01 2011-11-18 Kat ii 抑制剂 Expired - Fee Related CN103228631B (zh)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US41879110P 2010-12-01 2010-12-01
US61/418,791 2010-12-01
US41923210P 2010-12-02 2010-12-02
US61/419,232 2010-12-02
PCT/IB2011/055190 WO2012073146A1 (en) 2010-12-01 2011-11-18 Kat ii inhibitors

Publications (2)

Publication Number Publication Date
CN103228631A CN103228631A (zh) 2013-07-31
CN103228631B true CN103228631B (zh) 2015-04-29

Family

ID=45315857

Family Applications (1)

Application Number Title Priority Date Filing Date
CN201180057792.0A Expired - Fee Related CN103228631B (zh) 2010-12-01 2011-11-18 Kat ii 抑制剂

Country Status (13)

Country Link
US (1) US8487104B2 (https=)
EP (1) EP2646417A1 (https=)
JP (1) JP5868994B2 (https=)
KR (1) KR101522803B1 (https=)
CN (1) CN103228631B (https=)
AR (1) AR084051A1 (https=)
AU (1) AU2011336217B2 (https=)
CA (1) CA2819106C (https=)
IL (1) IL226668A (https=)
MX (1) MX2013005915A (https=)
SG (1) SG190246A1 (https=)
WO (1) WO2012073146A1 (https=)
ZA (1) ZA201303412B (https=)

Families Citing this family (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2861593A1 (en) * 2012-06-15 2015-04-22 Pfizer Inc. Tricyclic compounds as kat ii inhibitors
US20140206667A1 (en) 2012-11-14 2014-07-24 Michela Gallagher Methods and compositions for treating schizophrenia
CA2946702C (en) * 2014-04-23 2022-06-28 Mitsubishi Tanabe Pharma Corporation Bicyclic or tricyclic heterocyclic compound
WO2016191288A1 (en) 2015-05-22 2016-12-01 Agenebio, Inc. Extended release pharmaceutical compositions of levetiracetam
WO2017069275A1 (ja) * 2015-10-22 2017-04-27 田辺三菱製薬株式会社 新規二環性複素環化合物

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1077192A (zh) * 1992-03-16 1993-10-13 默克专利股份有限公司 2-氧代喹啉衍生物
US5594006A (en) * 1993-03-18 1997-01-14 Otsuka Pharmaceutical Co., Ltd. Carbostyril derivatives as matrix metalloproteinases inhibitors
WO2005007111A2 (en) * 2003-07-11 2005-01-27 Bristol-Myers Squibb Company Tetrahydroquinoline derivatives as cannabinoid receptor modulators
WO2009064836A2 (en) * 2007-11-15 2009-05-22 University Of Maryland, Baltimore Kynurenine-aminotransferase inhibitors

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPH0881443A (ja) * 1994-09-12 1996-03-26 Otsuka Pharmaceut Co Ltd 細胞外マトリックス金属プロテアーゼ阻害剤
BRPI1011784A2 (pt) * 2009-06-18 2016-03-22 Pfizer compostos bicíclicos e tricíclicos como inibidores de kat ii
JP2013544277A (ja) 2010-12-01 2013-12-12 ファイザー・インク Ｋａｔｉｉ阻害剤

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1077192A (zh) * 1992-03-16 1993-10-13 默克专利股份有限公司 2-氧代喹啉衍生物
US5594006A (en) * 1993-03-18 1997-01-14 Otsuka Pharmaceutical Co., Ltd. Carbostyril derivatives as matrix metalloproteinases inhibitors
WO2005007111A2 (en) * 2003-07-11 2005-01-27 Bristol-Myers Squibb Company Tetrahydroquinoline derivatives as cannabinoid receptor modulators
WO2009064836A2 (en) * 2007-11-15 2009-05-22 University Of Maryland, Baltimore Kynurenine-aminotransferase inhibitors

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
Synthesis and antibacterial activities of some chloro analogs of 3-amino-3,4-dihydro-1-hydroxycarbostyril;Alvie L. Davis等;《J. Med. Chem.》;19751231;第18卷(第7期);第752-755页 *
Synthesis and microbiological properties of some substituted derivatives of 3-amino-3,4-dihydrocarbostyril;Alvie L. Davis等;《J. Med. Chem.》;19701231;第13卷(第3期);第549-550页 *

Also Published As

Publication number Publication date
SG190246A1 (en) 2013-06-28
AU2011336217B2 (en) 2015-10-01
US8487104B2 (en) 2013-07-16
JP2014500885A (ja) 2014-01-16
ZA201303412B (en) 2014-07-30
JP5868994B2 (ja) 2016-02-24
EP2646417A1 (en) 2013-10-09
IL226668A (en) 2016-07-31
AU2011336217A1 (en) 2013-06-06
KR20130098421A (ko) 2013-09-04
KR101522803B1 (ko) 2015-05-26
AR084051A1 (es) 2013-04-17
US20120142729A1 (en) 2012-06-07
CA2819106A1 (en) 2012-06-07
MX2013005915A (es) 2013-07-03
CA2819106C (en) 2015-12-29
HK1187611A1 (en) 2014-04-11
CN103228631A (zh) 2013-07-31
WO2012073146A1 (en) 2012-06-07

Similar Documents

Publication Publication Date Title
CN105579444B (zh) 哌啶基吲哚衍生物和它们作为补体因子b抑制剂的用途
JP6063567B2 (ja) Ｐａｄ４阻害剤としての２−（アザインドール−２−イル）ベンズイミダゾール
CN108834412B (zh) 嘧啶及其变体、及其用途
EP2683721B1 (en) 3,4-DIHYDRO-PYRROLO[1,2-a]PYRAZIN-1-YLAMINE DERIVATIVES USEFUL AS INHIBITORS OF BETA-SECRETASE (BACE)
TW201639819A (zh) 苯并氮呯二甲醯胺化合物
EP2277858A1 (en) Amide compound
MX2012015170A (es) Derivados de 3-amino-5,6-dihidro-1h-pirazin-2-ona utiles para el tratamiento de la enfermedad de alzheimer y otras formas de demencia.
KR20130090793A (ko) 베타-세크레타아제(ｂａｃｅ) 저해제로 유용한 5-아미노-3,6-디하이드로-1ｈ-피라진-2-온 유도체
EA022649B1 (ru) ПРОИЗВОДНЫЕ 6,7-ДИГИДРОПИРАЗОЛО[1,5-a]ПИРАЗИН-4-ИЛАМИНА, ПРИГОДНЫЕ В КАЧЕСТВЕ ИНГИБИТОРОВ БЕТА-СЕКРЕТАЗЫ (BACE)
CN103228631B (zh) Kat ii 抑制剂
KR20140093750A (ko) 신규 1-아릴-3-아자바이사이클로［3.1.0］헥산：제조 방법 및 신경 정신 질환 치료를 위한 용도
JPH09512528A (ja) バソプレッシン拮抗物質としてのベンズアミド誘導体
JP2020023512A (ja) Ｓ１ｐ３アンタゴニスト
US20110009379A1 (en) Indolinone compound
HK1257567A1 (zh) 作为htra1抑制剂的新型二氟酮酰胺衍生物
WO2019112024A1 (ja) ピロリジン化合物
KR20200035077A (ko) 통증 및 통증 관련 상태 치료를 위한 새로운 프로판아민 유도체
WO2025026209A1 (zh) Arf1抑制剂及其应用
KR20260034665A (ko) 치환된 환형 화합물 및 페닐케톤뇨증 및 기타 아미노산뇨증의 치료 방법
TW201922690A (zh) 環－amp反應元素結合蛋白的抑制劑
HK1187611B (en) Kat ii inhibitors
BG105154A (bg) Производни на хидроксамова киселина като инхибитори за получаване на човешки cd23 и отделяне на tnf
CN121712748A (zh) 作为sstr4激动剂的(2s,5r)-5-(羟甲基)吗啉-2-甲酰胺
TW202417434A (zh) 用於治療之parp14之靶向蛋白質降解
JP2024509016A (ja) 新規なヘテロビサイクリック残基を有するインジルビン誘導体およびその用途

Legal Events

Date Code Title Description
C06 Publication
PB01 Publication
C10 Entry into substantive examination
SE01 Entry into force of request for substantive examination
REG Reference to a national code

Ref country code: HK

Ref legal event code: DE

Ref document number: 1187611

Country of ref document: HK

C14 Grant of patent or utility model
GR01 Patent grant
REG Reference to a national code

Ref country code: HK

Ref legal event code: GR

Ref document number: 1187611

Country of ref document: HK

CF01 Termination of patent right due to non-payment of annual fee

Granted publication date: 20150429

Termination date: 20171118

CF01 Termination of patent right due to non-payment of annual fee