CN100543017C - 作为组织蛋白酶抑制剂的酮基噁二唑衍生物 - Google Patents

作为组织蛋白酶抑制剂的酮基噁二唑衍生物 Download PDF

Info

Publication number
CN100543017C
CN100543017C CNB2004800389122A CN200480038912A CN100543017C CN 100543017 C CN100543017 C CN 100543017C CN B2004800389122 A CNB2004800389122 A CN B2004800389122A CN 200480038912 A CN200480038912 A CN 200480038912A CN 100543017 C CN100543017 C CN 100543017C
Authority
CN
China
Prior art keywords
acid
difluoro
morpholine
carbonyl
amino
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
CNB2004800389122A
Other languages
English (en)
Chinese (zh)
Other versions
CN1898219A (zh
Inventor
S·图赖拉特奈姆
D·J·奥尔德斯
V·勒罗伊
A·P·蒂姆
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.)
Aventis Pharmaceuticals Inc
Original Assignee
Aventis 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 Aventis Pharmaceuticals Inc filed Critical Aventis Pharmaceuticals Inc
Publication of CN1898219A publication Critical patent/CN1898219A/zh
Application granted granted Critical
Publication of CN100543017C publication Critical patent/CN100543017C/zh
Anticipated expiration legal-status Critical
Expired - Fee Related legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D263/00—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
    • C07D263/52—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings condensed with carbocyclic rings or ring systems
    • C07D263/54—Benzoxazoles; Hydrogenated benzoxazoles
    • C07D263/56—Benzoxazoles; Hydrogenated benzoxazoles with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 2
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D261/00—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings
    • C07D261/02—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings
    • C07D261/06—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings having two or more double bonds between ring members or between ring members and non-ring members
    • C07D261/08—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings having two or more double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • 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
    • A61P1/02—Stomatological preparations, e.g. drugs for caries, aphtae, periodontitis
    • 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
    • A61P1/14—Prodigestives, e.g. acids, enzymes, appetite stimulants, antidyspeptics, tonics, antiflatulents
    • 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
    • A61P19/00—Drugs for skeletal disorders
    • 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
    • A61P19/04—Drugs for skeletal disorders for non-specific disorders of the connective tissue
    • 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
    • A61P21/04—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
    • A61P25/04—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
    • A61P25/14—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
    • A61P25/28—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
    • 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
    • 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
    • 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
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/14—Drugs for disorders of the endocrine system of the thyroid hormones, e.g. T3, T4
    • A61P5/16—Drugs for disorders of the endocrine system of the thyroid hormones, e.g. T3, T4 for decreasing, blocking or antagonising the activity of the thyroid hormones
    • 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
    • C07D263/00—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
    • C07D263/02—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings
    • C07D263/30—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D263/32—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D267/00—Heterocyclic compounds containing rings of more than six members having one nitrogen atom and one oxygen atom as the only ring hetero atoms
    • C07D267/02—Seven-membered rings
    • C07D267/08—Seven-membered rings having the hetero atoms in positions 1 and 4
    • C07D267/10—Seven-membered rings having the hetero atoms in positions 1 and 4 not condensed with other rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D271/00—Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms
    • C07D271/02—Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms not condensed with other rings
    • C07D271/06—1,2,4-Oxadiazoles; Hydrogenated 1,2,4-oxadiazoles
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D271/00—Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms
    • C07D271/02—Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms not condensed with other rings
    • C07D271/10—1,3,4-Oxadiazoles; Hydrogenated 1,3,4-oxadiazoles
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D271/00—Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms
    • C07D271/02—Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms not condensed with other rings
    • C07D271/10—1,3,4-Oxadiazoles; Hydrogenated 1,3,4-oxadiazoles
    • C07D271/107—1,3,4-Oxadiazoles; Hydrogenated 1,3,4-oxadiazoles with two aryl or substituted aryl radicals attached in positions 2 and 5
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/16—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms
    • C07D295/18—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms by radicals derived from carboxylic acids, or sulfur or nitrogen analogues thereof
    • C07D295/195—Radicals derived from nitrogen analogues of carboxylic acids
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/16—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms
    • C07D295/20—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms by radicals derived from carbonic acid, or sulfur or nitrogen analogues thereof
    • C07D295/215—Radicals derived from nitrogen analogues of carbonic acid
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides
    • C07K5/06191—Dipeptides containing heteroatoms different from O, S, or N
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Immunology (AREA)
  • Rheumatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Diabetes (AREA)
  • Pulmonology (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Pain & Pain Management (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Molecular Biology (AREA)
  • Urology & Nephrology (AREA)
  • Genetics & Genomics (AREA)
  • Biophysics (AREA)
  • Biochemistry (AREA)
  • Endocrinology (AREA)
  • Hospice & Palliative Care (AREA)
  • Vascular Medicine (AREA)
  • Dermatology (AREA)
  • Emergency Medicine (AREA)
  • Obesity (AREA)
  • Psychiatry (AREA)
CNB2004800389122A 2003-10-24 2004-10-22 作为组织蛋白酶抑制剂的酮基噁二唑衍生物 Expired - Fee Related CN100543017C (zh)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US51437303P 2003-10-24 2003-10-24
US60/514,373 2003-10-24

Publications (2)

Publication Number Publication Date
CN1898219A CN1898219A (zh) 2007-01-17
CN100543017C true CN100543017C (zh) 2009-09-23

Family

ID=34520197

Family Applications (1)

Application Number Title Priority Date Filing Date
CNB2004800389122A Expired - Fee Related CN100543017C (zh) 2003-10-24 2004-10-22 作为组织蛋白酶抑制剂的酮基噁二唑衍生物

Country Status (18)

Country Link
US (1) US7482448B2 (enExample)
EP (1) EP1682524A1 (enExample)
JP (1) JP4769192B2 (enExample)
KR (1) KR20070008517A (enExample)
CN (1) CN100543017C (enExample)
AU (1) AU2004284089B2 (enExample)
BR (1) BRPI0415826A (enExample)
CA (1) CA2547591C (enExample)
IL (1) IL175106A0 (enExample)
MA (1) MA28170A1 (enExample)
ME (1) MEP39608A (enExample)
MX (1) MXPA06004422A (enExample)
NO (1) NO20062150L (enExample)
NZ (1) NZ546504A (enExample)
RS (1) RS20060280A (enExample)
RU (1) RU2346943C2 (enExample)
WO (1) WO2005040142A1 (enExample)
ZA (1) ZA200603183B (enExample)

Families Citing this family (19)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2006060810A1 (en) 2004-12-02 2006-06-08 Schering Aktiengesellschaft Sulfonamide compounds as cysteine protease inhibitors
PL1865940T3 (pl) 2005-03-21 2013-06-28 Virobay Inc Alfa-ketoamidowe związki jako inhibitory proteaz cysteinowych
JP5215167B2 (ja) 2005-03-22 2013-06-19 ビロベイ，インコーポレイティド システインプロテアーゼ阻害剤としてのスルホニル基含有化合物
ES2392675T3 (es) 2006-06-01 2012-12-12 Sanofi Nitrilos espirocíclicos como inhibidores de proteasa
DK2079683T3 (en) * 2006-10-04 2015-04-27 Virobay Inc Difluoro-containing compounds as cysteine protease inhibitors
US7893112B2 (en) 2006-10-04 2011-02-22 Virobay, Inc. Di-fluoro containing compounds as cysteine protease inhibitors
WO2008104271A2 (en) 2007-02-28 2008-09-04 Sanofi-Aventis Imaging probes
EP2262370A4 (en) * 2008-04-01 2011-08-31 Virobay Inc DIFLUOROUS COMPOUNDS AS A CYSTONE PROTEASE INHIBITOR
US7741327B2 (en) 2008-04-16 2010-06-22 Hoffmann-La Roche Inc. Pyrrolidinone glucokinase activators
BRPI0922283A2 (pt) * 2008-12-19 2015-12-29 Medivir Uk Ltd inibidores da cistéina protease
US7893099B2 (en) * 2009-06-11 2011-02-22 Hoffman-La Roche Inc. Cyclopentane derivatives
US20110021570A1 (en) 2009-07-23 2011-01-27 Nancy-Ellen Haynes Pyridone glucokinase activators
US8324417B2 (en) * 2009-08-19 2012-12-04 Virobay, Inc. Process for the preparation of (S)-2-amino-5-cyclopropyl-4,4-difluoropentanoic acid and alkyl esters and acid salts thereof
US8895497B2 (en) 2009-12-04 2014-11-25 Dcb-Usa, Llc Cathepsin S inhibitors
US8500766B2 (en) * 2009-12-18 2013-08-06 Colgate-Palmolive Company Oral care implement multiple soft tissue cleaner components
US8178689B2 (en) 2010-06-17 2012-05-15 Hoffman-La Roche Inc. Tricyclic compounds
KR20150046259A (ko) 2012-08-23 2015-04-29 앨리오스 바이오파마 인크. 파라믹소바이러스 바이러스성 감염의 치료용 화합물
AU2020250933A1 (en) 2019-04-05 2021-10-28 Centre Hospitalier Régional Et Universitaire De Brest Protease-activated receptor-2 inhibitors for the treatment of sensory neuropathy induced by a marine neurotoxic poisoning
CN122355874A (zh) * 2026-06-08 2026-07-10 天津楷特药业有限公司 一种手性α-羟基-偕胺肟醚的制备方法

Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1999064442A1 (en) * 1998-06-10 1999-12-16 Istituto Di Ricerche Di Biologia Molecolare P Angeletti S.P.A. Peptide inhibitors of hepatitis c virus ns3 protease
CN1297354A (zh) * 1998-03-16 2001-05-30 西托维亚公司 二肽卡斯帕酶抑制剂及其用途
CN1345314A (zh) * 1999-03-15 2002-04-17 Axys药物公司 用作蛋白酶抑制剂的胺衍生物
WO2002069901A2 (en) * 2001-03-02 2002-09-12 Merck Frosst Canada & Co. Cathepsin cysteine protease inhibitors
WO2002100849A2 (en) * 2001-06-08 2002-12-19 Boehringer Ingelheim Pharmaceuticals, Inc. Novel nitriles useful as reversible inhibitors of cysteine proteases
WO2003087069A2 (en) * 2002-04-09 2003-10-23 Eli Lilly And Company Dipeptidic growth hormone secretagogues

Family Cites Families (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR2381023A1 (fr) 1977-02-18 1978-09-15 Delalande Sa Nouveaux oligopeptides trifluoromethyles derives de la l-alanine, leur procede de preparation et leur application en therapeutique
FR2605009B1 (fr) * 1986-06-13 1989-06-09 Ayi Ayicoue Nouveaux peptides contenant un acide a-amine b-monofluore ou b,b-difluore dans leur structure dont des enkephalines et derives d'enkephalines
CA2045578A1 (en) * 1989-01-31 1990-08-01 Megumi Kawai Anaphylatoxin-receptor ligands
US5223485A (en) 1989-01-31 1993-06-29 Abbott Laboratories Anaphylatoxin-receptor ligands
JPH0449298A (ja) * 1990-06-19 1992-02-18 Univ New York State 新規なエンケファリン誘導体および鎮痛剤
JP3605158B2 (ja) * 1994-12-09 2004-12-22 塩野義製薬株式会社 Ｈｉｖプロテアーゼ阻害剤
DE19642591A1 (de) * 1996-10-15 1998-04-16 Basf Ag Neue Piperidin-Ketocarbonsäure-Derivate, deren Herstellung und Anwendung
SK112899A3 (en) * 1997-02-26 2001-05-10 Pfizer Heteroaryl-hexanoic acid amide derivatives, their preparation and their use as selective inhibitors of mip-1-alpha binding to its ccr1 receptor
ID20812A (id) 1997-07-09 1999-03-11 Takeda Chemical Industries Ltd Senyawa polyol, produk dan penggunaannya
EA200100972A1 (ru) * 1999-03-15 2002-02-28 Аксис Фармасьютикалз, Инк. Новые соединения и композиции как ингибиторы протеаз
GB0107924D0 (en) 2001-03-29 2001-05-23 Angeletti P Ist Richerche Bio Inhibitor of hepatitis C virus NS3 protease
JP2004535422A (ja) 2001-06-01 2004-11-25 アクシス・ファーマシューティカルズ・インコーポレイテッド カテプシン阻害剤としての新しい化合物および組成物
RU2312861C2 (ru) * 2002-03-05 2007-12-20 Мерк Фросст Кэнада Лтд. Ингибиторы катепсин-цистеинпротеазы
EP1503997A1 (en) 2002-05-14 2005-02-09 Axys Pharmaceuticals, Inc. Cysteine protease inhibitors

Patent Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1297354A (zh) * 1998-03-16 2001-05-30 西托维亚公司 二肽卡斯帕酶抑制剂及其用途
WO1999064442A1 (en) * 1998-06-10 1999-12-16 Istituto Di Ricerche Di Biologia Molecolare P Angeletti S.P.A. Peptide inhibitors of hepatitis c virus ns3 protease
CN1345314A (zh) * 1999-03-15 2002-04-17 Axys药物公司 用作蛋白酶抑制剂的胺衍生物
WO2002069901A2 (en) * 2001-03-02 2002-09-12 Merck Frosst Canada & Co. Cathepsin cysteine protease inhibitors
WO2002100849A2 (en) * 2001-06-08 2002-12-19 Boehringer Ingelheim Pharmaceuticals, Inc. Novel nitriles useful as reversible inhibitors of cysteine proteases
WO2003087069A2 (en) * 2002-04-09 2003-10-23 Eli Lilly And Company Dipeptidic growth hormone secretagogues

Non-Patent Citations (6)

* Cited by examiner, † Cited by third party
Title
New potent enkephalin analogs containingTrifluoromethylamino acid residues. Iwao Ojima et al.Bioorganic & Medicinal Chemistry Letters,Vol.2 No.3. 1992
Novel, potent phenethylamide inhibitors of the hepatitis Cvirus (HCV) NS3 protease: Probing the role ofP2 aryloxyprolines with hybrid structures. Federica Orvieto et al.Bioorganic & Medicinal Chemistry Letters,Vol.13 No.16. 2003
Synthesis of (2S)-4,4-difluoroproline, (2S,4R)-4-fluoroprolineand their derivatives from (S)-aspartic acid. Klaus Burger et al.Journal of Fluorine Chemistry,Vol.66 . 1994
The Conformation of de Novo Designed Amphiphilic Peptideswith Six or Nine L-2-(2,2,2-Trifluoroethyl)glycines as theHydrophobic Amino Acid. Toru Arai et al.Bull. Chem. Soc. Jpn.,Vol.73 No.2. 2000
The identification of α-ketoamides as potent inhibitorsofhepatitis c virus NS3-4A proteinase. J. M. Bennett et al.Bioorganic & Medicinal Chemistry Letters,Vol.11 . 2001
α-Aminoamides from a carbamoylsilane and aldehydeimines. Jianxin Chen et al.Tetrahedron Letters,Vol.44 No.43. 2003

Also Published As

Publication number Publication date
CN1898219A (zh) 2007-01-17
RS20060280A (sr) 2008-08-07
EP1682524A1 (en) 2006-07-26
CA2547591C (en) 2010-08-17
BRPI0415826A (pt) 2007-01-02
US20060189657A1 (en) 2006-08-24
IL175106A0 (en) 2006-09-05
ZA200603183B (en) 2007-09-26
US7482448B2 (en) 2009-01-27
KR20070008517A (ko) 2007-01-17
CA2547591A1 (en) 2005-05-06
WO2005040142A9 (en) 2005-06-09
AU2004284089B2 (en) 2009-11-26
JP4769192B2 (ja) 2011-09-07
MEP39608A (en) 2011-02-10
WO2005040142A1 (en) 2005-05-06
JP2007509175A (ja) 2007-04-12
RU2346943C2 (ru) 2009-02-20
AU2004284089A1 (en) 2005-05-06
WO2005040142B1 (en) 2005-07-14
MXPA06004422A (es) 2006-07-03
NO20062150L (no) 2006-05-12
NZ546504A (en) 2009-01-31
HK1101871A1 (zh) 2007-10-26
MA28170A1 (fr) 2006-09-01
RU2006117788A (ru) 2007-11-27

Similar Documents

Publication Publication Date Title
JP4769192B2 (ja) カテプシン阻害剤としての新規な化合物及び組成物
CN102884065A (zh) 杂芳基-环己基-四氮杂苯并[e]薁
AU2010319983A1 (en) Selective sphingosine 1 phosphate receptor modulators and methods of chiral synthesis
CN101119990A (zh) (1,5－二苯基－1h－吡唑－3－基)二唑衍生物，它们的制备及在治疗中的应用
CA2448418A1 (en) Chemical compounds and pharmaceutical compositions as cathepsin s inhibitors
JP2003519133A (ja) プロコラーゲンｃプロテイナーゼインヒビターとしてのオキサゾリル（オキサジアゾリル）ヒドロキサム酸
US7144901B2 (en) Oxadiazole derivatives and drugs containing these derivatives as the active ingredient
AU2002305790A1 (en) Chemical compounds and pharmaceutical compositions as cathepsin S inhibitors
JP2006506326A (ja) システインプロテアーゼ阻害剤
US20070203138A1 (en) Novel Compounds and Compositions as Cathepsin S Inhibitors
CN102574823B (zh) 酰胺衍生物
HK1101871B (en) Novel keto-oxadiazole derivatives as cathepsin inhibitors
CA2432643C (en) 3-ox(adi)azolylpropanohydroxamic acids useful as procollagen c-proteinase inhibitors
CN121889389A (zh) 靶向clpp1p2蛋白酶的蛋白酶体复合物抑制剂
AU2002357716A1 (en) Oligopeptides and compositions containing them as cathepsin S inhibitors
JPWO2001040204A1 (ja) １，３，４−オキサジアゾリン誘導体およびそれらを有効成分とする薬剤

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: 1101871

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: 1101871

Country of ref document: HK

C17 Cessation of patent right
CF01 Termination of patent right due to non-payment of annual fee

Granted publication date: 20090923

Termination date: 20121022