CN100503572C - 天冬氨酸特异性半胱氨酸蛋白酶抑制剂及其用途 - Google Patents

天冬氨酸特异性半胱氨酸蛋白酶抑制剂及其用途 Download PDF

Info

Publication number
CN100503572C
CN100503572C CNB038187930A CN03818793A CN100503572C CN 100503572 C CN100503572 C CN 100503572C CN B038187930 A CNB038187930 A CN B038187930A CN 03818793 A CN03818793 A CN 03818793A CN 100503572 C CN100503572 C CN 100503572C
Authority
CN
China
Prior art keywords
compound
disease
halogen
acid
hydrogen
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
CNB038187930A
Other languages
English (en)
Chinese (zh)
Other versions
CN1675184A (zh
Inventor
R·尼格特尔
M·莫特默尔
J·斯塔德利
D·米伦
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.)
Vertex Pharmaceuticals Inc
Original Assignee
Vertex Pharmaceuticals 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 Vertex Pharmaceuticals Inc filed Critical Vertex Pharmaceuticals Inc
Publication of CN1675184A publication Critical patent/CN1675184A/zh
Application granted granted Critical
Publication of CN100503572C publication Critical patent/CN100503572C/zh
Anticipated expiration legal-status Critical
Expired - Fee Related legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C07D239/72—Quinazolines; Hydrogenated quinazolines
    • C07D239/86—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 4
    • C07D239/88—Oxygen atoms
    • C07D239/90—Oxygen atoms with acyclic radicals attached in position 2 or 3
    • 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
    • A61P1/04—Drugs 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
    • 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
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/18—Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • 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
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/14—Drugs for dermatological disorders for baldness or alopecia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • 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
    • A61P21/02—Muscle relaxants, e.g. for tetanus or cramps
    • 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
    • A61P21/04—Drugs for disorders of the muscular or neuromuscular system for myasthenia gravis
    • 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
    • A61P25/08—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
    • A61P25/28—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
    • 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
    • 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
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • 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
    • 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
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04—Antibacterial agents
    • A61P31/06—Antibacterial agents for tuberculosis
    • 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
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • 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
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A61P31/18—Antivirals for RNA viruses for HIV
    • 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
    • A61P31/12—Antivirals
    • A61P31/20—Antivirals for DNA viruses
    • 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
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/04—Antineoplastic agents specific for metastasis
    • 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
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • 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
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • 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
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/04—Antihaemorrhagics; Procoagulants; Haemostatic agents; Antifibrinolytic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/06—Antianaemics
    • 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
    • A61P9/02—Non-specific cardiovascular stimulants, e.g. drugs for syncope, antihypotensives
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D217/00—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems
    • C07D217/22—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to carbon atoms of the nitrogen-containing ring
    • C07D217/24—Oxygen atoms

Landscapes

  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Neurology (AREA)
  • Oncology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Immunology (AREA)
  • Cardiology (AREA)
  • Communicable Diseases (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Virology (AREA)
  • Diabetes (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Rheumatology (AREA)
  • Hematology (AREA)
  • Dermatology (AREA)
  • Pulmonology (AREA)
  • Molecular Biology (AREA)
  • Pain & Pain Management (AREA)
  • Urology & Nephrology (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Obesity (AREA)
  • Biotechnology (AREA)
  • Emergency Medicine (AREA)
CNB038187930A 2002-06-28 2003-06-27 天冬氨酸特异性半胱氨酸蛋白酶抑制剂及其用途 Expired - Fee Related CN100503572C (zh)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US39259202P 2002-06-28 2002-06-28
US60/392,592 2002-06-28
US43507302P 2002-12-20 2002-12-20
US60/435,073 2002-12-20

Publications (2)

Publication Number Publication Date
CN1675184A CN1675184A (zh) 2005-09-28
CN100503572C true CN100503572C (zh) 2009-06-24

Family

ID=30003264

Family Applications (1)

Application Number Title Priority Date Filing Date
CNB038187930A Expired - Fee Related CN100503572C (zh) 2002-06-28 2003-06-27 天冬氨酸特异性半胱氨酸蛋白酶抑制剂及其用途

Country Status (19)

Country Link
US (2) US7553852B2 (enExample)
EP (1) EP1539701A1 (enExample)
JP (2) JP4616643B2 (enExample)
KR (1) KR20050013260A (enExample)
CN (1) CN100503572C (enExample)
AR (1) AR040350A1 (enExample)
AU (1) AU2003248758A1 (enExample)
BR (1) BR0312232A (enExample)
CA (1) CA2493646A1 (enExample)
IL (1) IL165986A0 (enExample)
MX (1) MXPA05000069A (enExample)
NO (1) NO20050851L (enExample)
NZ (1) NZ537807A (enExample)
PE (1) PE20040728A1 (enExample)
PL (1) PL374598A1 (enExample)
RU (1) RU2005102094A (enExample)
TW (1) TW200404783A (enExample)
UY (1) UY27872A1 (enExample)
WO (1) WO2004002961A1 (enExample)

Families Citing this family (31)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PE20011350A1 (es) 2000-05-19 2002-01-15 Vertex Pharma PROFARMACO DE UN INHIBIDOR DE ENZIMA CONVERTIDORA DE INTERLEUCINA-1ß (ICE)
BR0312232A (pt) 2002-06-28 2005-05-10 Vertex Pharma Inibidores de caspases e seus usos
JP4675628B2 (ja) * 2002-12-20 2011-04-27 バーテックス ファーマシューティカルズ インコーポレイテッド ４−オキソ−３−（１−オキソ−１ｈ−イソキノリン−２−イルアセチルアミノ）−ペンタン酸のエステル誘導体およびアミド誘導体、ならびにカスパーゼインヒビターとしてのそれらの使用
PE20050159A1 (es) 2003-05-27 2005-04-19 Vertex Pharma Derivados de acido 3-[2-(3-amino-2-oxo-2h-piridin-1-il)-acetilamino]-4-oxo-pentanoico como inhibidores de caspasa
CA2559303C (en) 2004-03-12 2013-09-10 Vertex Pharmaceuticals Incorporated Processes and intermediates for the preparation of aspartic acetal caspase inhibitors
CN102362867A (zh) 2004-05-15 2012-02-29 沃泰克斯药物股份有限公司 使用ice抑制剂治疗癫痫发作
EP1778221A2 (en) 2004-05-27 2007-05-02 Vertex Pharmaceuticals Incorporated Ice inhibitors for the treatment of autoinflammatory diseases
CA2569763C (en) 2004-06-08 2013-03-12 Decode Chemistry, Inc. 2,4-diaminoquinazolines for spinal muscular atrophy
AU2005272627A1 (en) * 2004-08-13 2006-02-23 Amgen Inc. Substituted benzofused heterocycles
EP1796660B1 (en) 2004-09-17 2016-11-23 BioMAS Ltd. Use of ammonium trichloro(dioxyethylene-o,o')tellurate (as101) for the inhibition of interleukin-1beta-converting enzyme
CN101098855B (zh) * 2004-11-24 2012-06-06 沃泰克斯药物股份有限公司 3-[2-(3-酰氨基-2-氧代-2h-吡啶-1-基)-乙酰氨基]-4-氧代-戊酸衍生物及其作为天冬氨酸特异性半胱氨酸蛋白酶抑制剂的用途
CA2593005A1 (en) * 2005-01-03 2006-07-13 Myriad Genetics Inc. Pharmaceutical compounds as activators of caspases and inducers of apoptosis and the use thereof
EP1898940A4 (en) * 2005-06-07 2010-05-26 Univ Pennsylvania Alpha2beta1 / GPIa IIA INTEGRIN INHIBITORS
US8987306B2 (en) * 2005-06-07 2015-03-24 The Trustees Of The University Of Pennsylvania Inhibitors of integrin alpha2beta1 based on prolyl diaminopropionic acid scaffold
JP2009502922A (ja) * 2005-07-28 2009-01-29 バーテックス ファーマシューティカルズ インコーポレイテッド カスパーゼ阻害剤プロドラッグ
WO2007027742A2 (en) * 2005-08-31 2007-03-08 The Trustees Of The University Of Pennsylvania SMALL MOLECULE INTEGRIN α2βl/GPIa-IIa ANTAGONISTS
WO2008016973A1 (en) 2006-08-01 2008-02-07 Families Of Spinal Muscular Atrophy 2,4-diaminoquinazolines for spinal muscular atrophy
ATE523493T1 (de) * 2006-09-11 2011-09-15 Organon Nv 2-(1-oxo-1h-isochinolin-2-yl) acetamid-derivate
WO2008073388A2 (en) * 2006-12-11 2008-06-19 Mutual Pharmaceutical Company, Inc. Alfuzosin formulations, methods of making and methods of use
US20100092556A1 (en) * 2006-12-11 2010-04-15 Kristin Arnold Alfuzosin formulations, methods of making, and methods of use
FR2923160B1 (fr) 2007-11-02 2013-07-26 Pasteur Institut Composes destines a prevenir ou traiter une infection virale.
EP2635906A4 (en) 2010-11-05 2014-04-02 Univ Brandeis Ice inhibiting compounds and uses thereof
US9956260B1 (en) 2011-07-22 2018-05-01 The J. David Gladstone Institutes Treatment of HIV-1 infection and AIDS
CA2862084C (en) 2012-01-26 2021-05-11 Ptc Therapeutics, Inc. 1h-isochromen-1-one derivatives and compositions thereof for treating spinal muscular atrophy
WO2015175381A1 (en) 2014-05-12 2015-11-19 Conatus Pharmaceuticals, Inc. Treatment of the complications of chronic liver disease with caspase inhibitors
WO2017079566A1 (en) 2015-11-05 2017-05-11 Conatus Pharmaceuticals, Inc. Caspase inhibitors for use in the treatment of liver cancer
JP2019500397A (ja) 2015-12-31 2019-01-10 クオナトウス ファーマシューティカルズ，インコーポレイテッド カスパーゼ阻害剤を肝疾患の治療に使用する方法
RU2019113150A (ru) 2016-10-05 2020-11-06 Новартис Аг Комбинация композиций, содержащих агонисты fxr, предназначенная для лечения или предупреждения фиброзирующего, цирротического заболевания или нарушения
EP3935042B1 (en) * 2019-03-07 2024-08-28 NOBO Medicine Inc. Caspase inhibitors and methods of use thereof
WO2022123062A1 (en) 2020-12-11 2022-06-16 INSERM (Institut National de la Santé et de la Recherche Médicale) Blocking caspase and/or fasl for preventing fatal outcome in covid-19 patients
KR102670554B1 (ko) * 2022-01-04 2024-05-30 주식회사 이노보테라퓨틱스 캐스파제 저해제로서의 신규한 이소인돌리논 유도체 화합물

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DD232699A1 (de) * 1983-11-18 1986-02-05 Adw Ddr Verfahren zur herstellung von chinazolin-4-on-3-alkansaeuren und deren estern
WO2001042216A2 (en) * 1999-12-08 2001-06-14 Vertex Pharmaceuticals Incorporated Caspase inhibitors and uses thereof

Family Cites Families (23)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6204261B1 (en) 1995-12-20 2001-03-20 Vertex Pharmaceuticals Incorporated Inhibitors of interleukin-1β Converting enzyme inhibitors
FR2582514B1 (fr) * 1985-05-30 1988-02-19 Rhone Poulenc Sante Medicaments a base d'amides, nouveaux amides et leur preparation
US5714484A (en) 1993-12-08 1998-02-03 Prototek, Inc. α-(1,3-dicarbonylenol ether) methyl ketones as cysteine protease inhibitors
US5756466A (en) * 1994-06-17 1998-05-26 Vertex Pharmaceuticals, Inc. Inhibitors of interleukin-1β converting enzyme
US5847135A (en) * 1994-06-17 1998-12-08 Vertex Pharmaceuticals, Incorporated Inhibitors of interleukin-1β converting enzyme
US6420522B1 (en) * 1995-06-05 2002-07-16 Vertex Pharmaceuticals Incorporated Inhibitors of interleukin-1β converting enzyme
US5716929A (en) * 1994-06-17 1998-02-10 Vertex Pharmaceuticals, Inc. Inhibitors of interleukin-1β converting enzyme
EP0761680A3 (en) 1995-09-12 1999-05-06 Ono Pharmaceutical Co., Ltd. Tetrazole compounds having Interleukin-1beta converting enzyme inhibitory activity
US6063794A (en) * 1996-10-11 2000-05-16 Cor Therapeutics Inc. Selective factor Xa inhibitors
AU738341B2 (en) 1996-10-11 2001-09-13 Abbott Gmbh & Co. Kg Asparate ester inhibitors of interleukin-1beta converting enzyme
KR20000049047A (ko) 1996-10-11 2000-07-25 로즈 암스트롱, 크리스틴 에이. 트러트웨인 술폰아미드 인터루킨-1β 전환 효소 억제제
WO1998018781A2 (en) 1996-10-28 1998-05-07 Versicor, Inc. Fused 2,4-pyrimidinedione combinatorial libraries, their preparation and the use of fused 2,4-pyrimidinediones derivatives as antimicrobial agents
US6972296B2 (en) 1999-05-07 2005-12-06 Encysive Pharmaceuticals Inc. Carboxylic acid derivatives that inhibit the binding of integrins to their receptors
ES2296625T3 (es) 1999-05-07 2008-05-01 Encysive Pharmaceuticals, Inc Derivados del acido carboxilico que inhiben el enlace de las integrinas con sus receptores.
SI20876B (sl) 1999-05-07 2009-08-31 Texas Biotechnology Corp Derivati propanojske kisline, ki inhibirajo vezavo integrinov na njihove receptorje
EP1289993B9 (en) 2000-06-07 2008-08-20 Vertex Pharmaceuticals Incorporated Caspase inhibitors and uses thereof
AU2002348533A1 (en) * 2001-10-09 2003-05-26 Vertex Pharmaceuticals Incorporated Process for synthesizing aspartic and glutamic acid derivatives and diazoketone intermediates thereof
AU2003211052A1 (en) * 2002-02-11 2003-09-04 Vertex Pharmaceuticals Incorporated Phospholipids as caspase inhibitor prodrugs
AU2003225088A1 (en) 2002-04-19 2003-11-03 Vertex Pharmaceuticals Incorporated Regulation of tnf-alpha
BR0312232A (pt) 2002-06-28 2005-05-10 Vertex Pharma Inibidores de caspases e seus usos
JP4675628B2 (ja) 2002-12-20 2011-04-27 バーテックス ファーマシューティカルズ インコーポレイテッド ４−オキソ−３−（１−オキソ−１ｈ−イソキノリン−２−イルアセチルアミノ）−ペンタン酸のエステル誘導体およびアミド誘導体、ならびにカスパーゼインヒビターとしてのそれらの使用
PE20050159A1 (es) * 2003-05-27 2005-04-19 Vertex Pharma Derivados de acido 3-[2-(3-amino-2-oxo-2h-piridin-1-il)-acetilamino]-4-oxo-pentanoico como inhibidores de caspasa
CN101098855B (zh) 2004-11-24 2012-06-06 沃泰克斯药物股份有限公司 3-[2-(3-酰氨基-2-氧代-2h-吡啶-1-基)-乙酰氨基]-4-氧代-戊酸衍生物及其作为天冬氨酸特异性半胱氨酸蛋白酶抑制剂的用途

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DD232699A1 (de) * 1983-11-18 1986-02-05 Adw Ddr Verfahren zur herstellung von chinazolin-4-on-3-alkansaeuren und deren estern
WO2001042216A2 (en) * 1999-12-08 2001-06-14 Vertex Pharmaceuticals Incorporated Caspase inhibitors and uses thereof

Also Published As

Publication number Publication date
EP1539701A1 (en) 2005-06-15
IL165986A0 (en) 2006-01-15
NZ537807A (en) 2007-05-31
JP2010143942A (ja) 2010-07-01
AR040350A1 (es) 2005-03-30
AU2003248758A1 (en) 2004-01-19
US20040072850A1 (en) 2004-04-15
CN1675184A (zh) 2005-09-28
JP2005533825A (ja) 2005-11-10
JP4616643B2 (ja) 2011-01-19
RU2005102094A (ru) 2006-02-27
TW200404783A (en) 2004-04-01
US20090281128A1 (en) 2009-11-12
WO2004002961A1 (en) 2004-01-08
BR0312232A (pt) 2005-05-10
KR20050013260A (ko) 2005-02-03
UY27872A1 (es) 2003-12-31
NO20050851L (no) 2005-03-29
MXPA05000069A (es) 2005-04-11
PE20040728A1 (es) 2004-10-23
US8129381B2 (en) 2012-03-06
PL374598A1 (en) 2005-10-31
CA2493646A1 (en) 2004-01-08
US7553852B2 (en) 2009-06-30

Similar Documents

Publication Publication Date Title
CN100503572C (zh) 天冬氨酸特异性半胱氨酸蛋白酶抑制剂及其用途
CN100415718C (zh) 天冬氨酸特异性半胱氨酸蛋白酶抑制剂及其用途
US20020061853A1 (en) Caspase inhibtors and uses thereof
US7074782B2 (en) Carbamate caspase inhibitors and uses thereof
JP2003516393A5 (enExample)
WO2002085899A1 (en) Heterocyclyldicarbamides as caspase inhibitors
CN100366612C (zh) 4-氧代-3-(1-氧代-1h-异喹啉-2-基乙酰氨基)-戊酸酯和酰胺衍生物及其作为天冬氨酸特异性半胱氨酸蛋白酶抑制剂的用途
WO2011054171A1 (zh) 酪氨酸衍生物类组蛋白去乙酰化酶抑制剂及其应用
CN101098855A (zh) 3-[2-(3-酰氨基-2-氧代-2h-吡啶-1-基)-乙酰氨基]-4-氧代-戊酸衍生物及其作为天冬氨酸特异性半胱氨酸蛋白酶抑制剂的用途
HK1087701B (en) 4-oxo-3-(1-oxo-1h-isoquinolin-2-ylacetylamino)-pentanoic acid ester and amide derivatives and their use as caspase inhibitors

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: 1081179

Country of ref document: HK

C14 Grant of patent or utility model
GR01 Patent grant
C17 Cessation of patent right
CF01 Termination of patent right due to non-payment of annual fee

Granted publication date: 20090624

Termination date: 20100627

REG Reference to a national code

Ref country code: HK

Ref legal event code: WD

Ref document number: 1081179

Country of ref document: HK