CN1416346A - 蛋白酶抑制剂 - Google Patents

蛋白酶抑制剂 Download PDF

Info

Publication number
CN1416346A
CN1416346A CN01806446A CN01806446A CN1416346A CN 1416346 A CN1416346 A CN 1416346A CN 01806446 A CN01806446 A CN 01806446A CN 01806446 A CN01806446 A CN 01806446A CN 1416346 A CN1416346 A CN 1416346A
Authority
CN
China
Prior art keywords
methyl
alkyl
pyridine
butyl
amide
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.)
Pending
Application number
CN01806446A
Other languages
English (en)
Chinese (zh)
Inventor
马克斯韦尔·D·卡明斯
小罗伯特·W·马奎斯
汝玉
斯科特·K·汤普森
丹尼尔·F·维伯
丹尼斯·S·雅马什塔
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 Corp
Original Assignee
SmithKline Beecham Corp
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 Corp filed Critical SmithKline Beecham Corp
Publication of CN1416346A publication Critical patent/CN1416346A/zh
Pending legal-status Critical Current

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C271/00Derivatives of carbamic acids, i.e. compounds containing any of the groups, the nitrogen atom not being part of nitro or nitroso groups
    • C07C271/06Esters of carbamic acids
    • C07C271/08Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms
    • C07C271/10Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms
    • C07C271/12Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms to hydrogen atoms or to carbon atoms of unsubstituted hydrocarbon radicals
    • 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
    • A61P1/02Stomatological preparations, e.g. drugs for caries, aphtae, periodontitis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • 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
    • A61P19/08Drugs 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
    • A61P19/00Drugs for skeletal disorders
    • A61P19/08Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • 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
    • A61P31/04Antibacterial agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00Antiparasitic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00Antiparasitic agents
    • A61P33/02Antiprotozoals, e.g. for leishmaniasis, trichomoniasis, toxoplasmosis
    • A61P33/06Antimalarials
    • 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C271/00Derivatives of carbamic acids, i.e. compounds containing any of the groups, the nitrogen atom not being part of nitro or nitroso groups
    • C07C271/06Esters of carbamic acids
    • C07C271/08Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms
    • C07C271/10Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms
    • C07C271/14Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms to carbon atoms of hydrocarbon radicals substituted by halogen atoms or by nitro or nitroso groups
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D223/00Heterocyclic compounds containing seven-membered rings having one nitrogen atom as the only ring hetero atom
    • C07D223/02Heterocyclic compounds containing seven-membered rings having one nitrogen atom as the only ring hetero atom not condensed with other rings
    • C07D223/04Heterocyclic compounds containing seven-membered rings having one nitrogen atom as the only ring hetero atom not condensed with other rings with only hydrogen atoms, halogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D223/00Heterocyclic compounds containing seven-membered rings having one nitrogen atom as the only ring hetero atom
    • C07D223/02Heterocyclic compounds containing seven-membered rings having one nitrogen atom as the only ring hetero atom not condensed with other rings
    • C07D223/06Heterocyclic compounds containing seven-membered rings having one nitrogen atom as the only ring hetero atom not condensed with other rings 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 ring carbon atoms
    • C07D223/08Oxygen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • 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
    • C07D405/02Heterocyclic 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 two hetero rings
    • C07D405/12Heterocyclic 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 two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D491/00Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D495/00Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/04Ortho-condensed systems
    • YGENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02ATECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
    • Y02A50/00TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
    • Y02A50/30Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change

Landscapes

  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Rheumatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Pain & Pain Management (AREA)
  • Oncology (AREA)
  • Immunology (AREA)
  • Communicable Diseases (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Peptides Or Proteins (AREA)
CN01806446A 2000-03-21 2001-03-07 蛋白酶抑制剂 Pending CN1416346A (zh)

Applications Claiming Priority (8)

Application Number Priority Date Filing Date Title
US19100000P 2000-03-21 2000-03-21
US60/191,000 2000-03-21
US20634100P 2000-05-23 2000-05-23
US60/206,341 2000-05-23
US21175900P 2000-06-14 2000-06-14
US60/211,759 2000-06-14
US21744500P 2000-07-10 2000-07-10
US60/217,445 2000-07-10

Publications (1)

Publication Number Publication Date
CN1416346A true CN1416346A (zh) 2003-05-07

Family

ID=27497873

Family Applications (1)

Application Number Title Priority Date Filing Date
CN01806446A Pending CN1416346A (zh) 2000-03-21 2001-03-07 蛋白酶抑制剂

Country Status (26)

Country Link
US (2) US7071184B2 (enExample)
EP (1) EP1307203A4 (enExample)
JP (1) JP2003527429A (enExample)
KR (1) KR20020082896A (enExample)
CN (1) CN1416346A (enExample)
AP (1) AP1540A (enExample)
AR (1) AR032877A1 (enExample)
AU (2) AU4344101A (enExample)
BG (1) BG106962A (enExample)
BR (1) BR0109356A (enExample)
CA (1) CA2404206A1 (enExample)
CZ (1) CZ20023168A3 (enExample)
DZ (1) DZ3318A1 (enExample)
EA (1) EA005893B1 (enExample)
HU (1) HUP0300068A2 (enExample)
IL (1) IL150964A0 (enExample)
MX (1) MXPA02009305A (enExample)
MY (1) MY141596A (enExample)
NO (1) NO20024528L (enExample)
NZ (1) NZ520588A (enExample)
OA (1) OA12323A (enExample)
PE (1) PE20011233A1 (enExample)
PL (1) PL357727A1 (enExample)
SK (1) SK13632002A3 (enExample)
UY (1) UY26625A1 (enExample)
WO (1) WO2001070232A1 (enExample)

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN103275070A (zh) * 2013-05-10 2013-09-04 郑彪 调节单核细胞增殖的四环化合物及其应用
CN116194114A (zh) * 2020-03-26 2023-05-30 葛兰素史密斯克莱知识产权发展有限公司 用于防止或治疗病毒感染的组织蛋白酶抑制剂

Families Citing this family (32)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20020128476A1 (en) * 1996-08-08 2002-09-12 Smithkline Beecham Corporation Inhibitors of cysteine protease
US20030144175A1 (en) 1998-12-23 2003-07-31 Smithkline Beecham Corporation Protease inhibitors
AU1474801A (en) 1999-11-10 2001-06-06 Smithkline Beecham Corporation Protease inhibitors
EP1232155A4 (en) 1999-11-10 2002-11-20 Smithkline Beecham Corp PROTEASE INHIBITORS
EP1232154A4 (en) 1999-11-10 2004-06-23 Smithkline Beecham Corp PROTEASE INHIBITORS
BR0109356A (pt) 2000-03-21 2003-06-03 Smithkline Beecham Corp Inibidores de protease
CO5280093A1 (es) * 2000-04-18 2003-05-30 Smithkline Beecham Corp Metodos de tratamiento
CO5280088A1 (es) * 2000-04-18 2003-05-30 Smithkline Beecham Corp Inhibidores de proteasa
WO2002017924A1 (en) * 2000-09-01 2002-03-07 Smithkline Beecham Corporation Method of treatment
BR0115473A (pt) * 2000-11-22 2004-09-28 Smithkline Beecham Corp Inibidores de protease
WO2003045909A2 (en) * 2001-11-21 2003-06-05 Smithkline Beecham Corporation Methods and intermediates for the synthesis of azepines
EP1511745A4 (en) * 2002-05-22 2006-11-15 Smithkline Beecham Corp PROTEASE INHIBITORS
US20060166966A1 (en) * 2002-10-08 2006-07-27 Cameron Black 4-amino-azepan-3-one compounds as cathepsin k inhibitors useful in the treatment of osteoporosis
US20040192674A1 (en) * 2003-02-14 2004-09-30 Marquis Robert W. Cathepsin L inhibitors
JP2007520491A (ja) * 2004-01-23 2007-07-26 スミスクライン・ビーチャム・コーポレイション ベンゾフラン−2−カルボン酸{(s)−3−メチル−1−[(4s,7r)−7−メチル−3−オキソ−1−(ピリジン−2−スルホニル)−アゼパン−4−イルカルバモイル]−ブチル}−アミドの製造方法
KR100603014B1 (ko) * 2004-07-21 2006-07-24 황호연 라벨용 포장필름의 제조방법, 상기 제조방법으로 제조된라벨용 포장필름 및 상기 포장필름의 사용방법
WO2006042150A1 (en) * 2004-10-07 2006-04-20 Vitae Pharmaceuticals, Inc. Diaminoalkane aspartic protease inhibitors
PE20070171A1 (es) 2005-06-30 2007-03-08 Boehringer Ingelheim Int GLICINAMIDAS SUSTITUIDAS CON EFECTO ANTITROMBOTICO E INHIBIDOR DEL FACTOR Xa
TWI411607B (zh) * 2005-11-14 2013-10-11 Vitae Pharmaceuticals Inc 天門冬胺酸蛋白酶抑制劑
CL2007002689A1 (es) 2006-09-18 2008-04-18 Vitae Pharmaceuticals Inc Compuestos derivados de piperidin-1-carboxamida, inhibidores de la renina; compuestos intermediarios; composicion farmaceutica; y uso en el tratamiento de enfermedades tales como hipertension, insuficiencia cardiaca, fibrosis cardiaca, entre otras.
CN101970007A (zh) 2007-06-08 2011-02-09 日本化学医药株式会社 脑动脉瘤的治疗或预防药
EP2170815A2 (en) * 2007-06-20 2010-04-07 Vitae Pharmaceuticals, Inc. Renin inhibitors
WO2009096996A1 (en) * 2007-06-20 2009-08-06 Smithkline Beecham Corporation Renin inhibitors
US20100331545A1 (en) 2007-10-24 2010-12-30 Nippon Chemiphar Co., Ltd. Regulator for signaling toll-like receptor, which comprises cathepsin inhibitor as active ingredient
EP2719700A1 (en) 2008-01-09 2014-04-16 Amura Therapeutics Limited Tetrahydrofuro(3,2-b)pyrrol-3-one derivatives as inhibitors of cysteine proteinases
CA2727987A1 (en) * 2008-06-20 2009-12-23 Vitae Pharmaceuticals, Inc. Renin inhibitors and method of use thereof
CN102088850A (zh) * 2008-06-26 2011-06-08 生命医药公司 甲基2-((r)-(3-氯苯基)((r)-1-((s)-2-(甲氨基)-3((r)-四氢-2h-吡喃-3-基)丙基氨甲酰基)哌啶-3-基)甲氧基)氨基甲酸乙酯的盐
AR077692A1 (es) * 2009-08-06 2011-09-14 Vitae Pharmaceuticals Inc Sales de 2-((r)-(3-clorofenil) ((r)-1-((s) -2-(metilamino)-3-((r)-tetrahidro-2h-piran-3-il) propilcarbamoil) piperidin -3-il) metoxi) etilcarbamato de metilo
CN103687593B (zh) 2011-05-16 2016-09-28 拜耳知识产权有限责任公司 组织蛋白酶k抑制用于治疗和/或预防肺动脉高压和/或心力衰竭的用途
JP6226437B2 (ja) * 2013-06-14 2017-11-08 生化学工業株式会社 α−オキソアシルアミノカプロラクタム体
EP3009444B1 (en) * 2013-06-14 2017-12-20 Seikagaku Corporation Alpha-oxoacyl amino-caprolactam derivative
EP4480541A3 (en) 2016-09-16 2025-04-30 Lighthouse Pharmaceuticals, Inc. Ketone inhibitors of lysine gingipain

Family Cites Families (101)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4038247A (en) 1970-05-19 1977-07-26 Ciba-Geigy Corporation Stabilizing polyolefins with diacyl dihydrazides
US5142056A (en) 1989-05-23 1992-08-25 Abbott Laboratories Retroviral protease inhibiting compounds
US5057525A (en) 1981-10-01 1991-10-15 Janssen Pharmaceutica N.V. Novel N-(3-hydroxy-4-piperidinyl) benzamide derivatives
IT1195287B (it) 1981-11-05 1988-10-12 Ausonia Farma Srl Derivato tiazolico,procedimento per la sua preparazione e relative composizioni farmaceutiche
ZA829141B (en) 1981-12-14 1983-09-28 Merck & Co Inc Process for reducing lactams
ZA839532B (en) 1982-12-27 1985-08-28 Merck & Co Inc Lactams and bicyclic lactams as antihypertensive agents
US4518528A (en) 1983-05-19 1985-05-21 Rasnick David W α Amino fluoro ketones
US4749792A (en) 1984-09-26 1988-06-07 E. R. Squibb & Sons, Inc. Diamino ketones and alcohols as analgesic agents
US4638101A (en) 1985-01-02 1987-01-20 General Electric Company Compositions
US4638010A (en) * 1985-02-28 1987-01-20 E. R. Squibb & Sons, Inc. Ester substituted aminoalkanoylureido amino and imino acid and ester compounds
JP2570686B2 (ja) 1985-12-23 1997-01-08 日産化学工業株式会社 ピラゾ−ル誘導体
DE3600288A1 (de) 1986-01-08 1987-07-16 Bayer Ag Verwendung von amiden zur verbesserung der kulturpflanzen-vertraeglichkeit von herbizid wirksamen sulfonylharnstoff-derivaten
JPS62252779A (ja) 1986-03-14 1987-11-04 シンテツクス(ユ−・エス・エイ)インコ−ポレイテツド トランスグルタミナ−ゼ阻害剤
DE3618004A1 (de) 1986-05-28 1987-12-03 Bayer Ag Verwendung von amiden zur verbesserung der kulturpflanzen-vertraeglichkeit von herbizid wirksamen sulfonyliso(thio)-harnstoff-derivaten
US5374637A (en) 1989-03-22 1994-12-20 Janssen Pharmaceutica N.V. N-(3-hydroxy-4-piperidinyl)(dihydrobenzofuran, dihydro-2H-benzopyran or dihydrobenzodioxin)carboxamide derivatives
US4994471A (en) 1989-05-12 1991-02-19 Boc, Inc. N-aryl-N-(1-substituted-3-alkoxy-4-piperidinyl)amides and pharmaceutical compositions and methods employing such compounds
WO1991009844A1 (en) 1990-01-04 1991-07-11 Pfizer Inc. Substance p antagonists
GB9019558D0 (en) 1990-09-07 1990-10-24 Szelke Michael Enzyme inhibitors
EP0504938A3 (en) 1991-03-22 1993-04-14 Suntory Limited Prophylactic and therapeutic agent for bone diseases comprising di- or tripeptide derivative as active ingredient
JP3190431B2 (ja) 1991-07-01 2001-07-23 三菱化学株式会社 ケトン誘導体
JPH05140063A (ja) 1991-11-19 1993-06-08 Suntory Ltd ジペプチド誘導体及びそれを有効成分とする骨疾患の予防及び治療剤
US5216168A (en) 1992-04-01 1993-06-01 G. D. Searle & Co. 2- and 3- amino and azido derivatives of 1,5-iminosugars
US5206251A (en) 1992-04-01 1993-04-27 G. D. Searle & Co. 2- and 3- amino and azido derivatives of 1,5-iminosugars
AU4544993A (en) 1992-06-24 1994-01-24 Cortex Pharmaceuticals, Inc. Use of calpain inhibitors in the inhibition and treatment of medical conditions associated with increased calpain activity
US5374623A (en) 1992-08-20 1994-12-20 Prototek, Inc. Cysteine protease inhibitors effective for in vivo use
ATE171171T1 (de) 1992-12-25 1998-10-15 Mitsubishi Chem Corp Alpha-aminoketon derivate
CA2111930A1 (en) 1992-12-25 1994-06-26 Ryoichi Ando Aminoketone derivatives
JPH06199850A (ja) 1992-12-28 1994-07-19 Tanabe Seiyaku Co Ltd インドール含有ペプチド及びその製法
JP2848232B2 (ja) 1993-02-19 1999-01-20 武田薬品工業株式会社 アルデヒド誘導体
WO1994023033A1 (en) 1993-04-06 1994-10-13 Forsyth Dental Infirmary For Children Human osteoclast-specific and -related genes
CA2122227A1 (en) 1993-04-29 1994-10-30 Roland E. Dolle Peptide analogs as irreversible interleukin-1.beta. protease inhibitors
US5866545A (en) 1993-08-13 1999-02-02 Merck & Co., Inc. Substituted ketone derivatives as inhibitors of interleukin-1β converting enzyme
US5501969A (en) 1994-03-08 1996-03-26 Human Genome Sciences, Inc. Human osteoclast-derived cathepsin
AU2223595A (en) 1994-04-13 1995-11-10 Takeda Chemical Industries Ltd. Aziridine derivatives, their production and use
US5585387A (en) 1994-10-07 1996-12-17 Torcan Chemical Ltd. Prepration of cisapride
US6544767B1 (en) 1994-10-27 2003-04-08 Axys Pharmaceuticals, Inc. Cathespin O2 protease
US5734977A (en) * 1994-11-10 1998-03-31 Telefonaktiebolaget Lm Ericsson Fraud detection in radio communications network
TW438591B (en) 1995-06-07 2001-06-07 Arris Pharm Corp Reversible cysteine protease inhibitors
CA2209109A1 (en) 1995-10-30 1997-05-09 Thomas Joseph . Carr Method of inhibiting cathepsin k
JP2000500742A (ja) 1995-10-30 2000-01-25 スミスクライン・ビーチャム・コーポレイション プロテアーゼ阻害剤
US6083947A (en) * 1996-01-29 2000-07-04 The Regents Of The University Of California Method for treating sexual dysfunctions
US5902882A (en) 1996-04-17 1999-05-11 Hoffmann-La Roche Inc. Assymetric synthesis of azepines
WO1997049668A1 (en) 1996-06-13 1997-12-31 Smithkline Beecham Corporation Inhibitiors of cysteine protease
AU6333296A (en) 1996-06-14 1998-01-07 Human Genome Sciences, Inc. Cathepsin k gene
US5861298A (en) 1996-06-17 1999-01-19 Smithkline Beecham Corporation Cathepsin K gene
DZ2285A1 (fr) 1996-08-08 2002-12-25 Smithkline Beecham Corp Inhibiteurs de protéase de la cystéine.
WO1998008802A1 (en) 1996-08-28 1998-03-05 Smithkline Beecham Corporation Inhibitors of cysteine protease
US5830850A (en) 1996-08-28 1998-11-03 Mount Sinai School Of Medicine Of The City Of New York Methods for the treatment of bone resorption disorders, including osteoporosis
NZ334490A (en) 1996-09-19 2000-08-25 Hoechst Marion Roussel Inc 3-mercaptoacetylamino-1,5-substituted-2-oxo-azepan derivatives as inhibitors of matrix metalloproteinase
US5948669A (en) 1997-02-26 1999-09-07 Smithkline Beecham Corporation Rat cathepsin K polynucleotide and polypeptide sequence
AR012374A1 (es) 1997-04-15 2000-10-18 Smithkline Beecham Corp Inhibidores de proteasas, composiones farmaceuticas y usos para la preparacion de medicamentos.
PE68599A1 (es) 1997-04-25 1999-09-26 Smithkline Beecham Corp Inhibidores de proteasas
MA26487A1 (fr) 1997-04-29 2004-12-20 Smithkline Beecham Corp Heterocyclecetohydrazides inhibiteurs de proteases, procede pour leur preparation et compositions pharmaceutiques les contenant .
US6566373B2 (en) 1997-05-06 2003-05-20 Smithkline Beecham Corporation Protease inhibitors
HUP0002951A3 (en) 1997-05-08 2002-10-28 Smithkline Beecham Corp Bis-aminomethylcarbonyl compounds as protease inhibitors and pharmaceutical compositions containing them
AU7288598A (en) 1997-05-08 1998-11-27 Smithkline Beecham Corporation Protease inhibitors
MA26540A1 (fr) 1997-09-04 2004-12-20 Smithkline Beecham Corp Composes nouveaux inhibiteurs de proteases et compositions pharmaceutiques les contenant.
MA26618A1 (fr) 1998-04-09 2004-12-20 Smithkline Beecham Corp Composes et compositions pharmaceutiques pour le traitement du paludisme
MA26631A1 (fr) 1998-05-21 2004-12-20 Smithkline Beecham Corp Composes a fonction bis-aminomethyl-carbonyle nouveaux, procede pour leur preparation et compositions pharmaceutiques les contenant
AU9110298A (en) 1998-05-21 1999-12-06 Smithkline Beecham Corporation Protease inhibitors
DZ2815A1 (fr) 1998-06-12 2003-12-01 Smithkline Beecham Corp Inhibiteurs de protéase.
AR018915A1 (es) 1998-06-24 2001-12-12 Smithkline Beecham Corp Inhibidores de proteasas diacilhidrazinicos, composicion farmaceutica que la comprenden, usos de los mismos para la manufactura de un medicamento, unprocedimiento de fabricacion de dichos compuestos
WO2000009653A2 (en) 1998-08-14 2000-02-24 Smithkline Beecham Corporation Method of inhibiting cathepsin k
CO5150165A1 (es) 1998-11-13 2002-04-29 Smithkline Beecham Plc Inhibidores de proteasa: tipo catepsina k
CO5180541A1 (es) 1998-12-23 2002-07-30 Smithkline Beechman Corp Inhibidores de proteasa del tipo de 1,3-diaminocetonas con anillo de 8-14 miembros
CN1253441C (zh) * 1998-12-23 2006-04-26 史密丝克莱恩比彻姆公司 蛋白酶抑制剂
US20030044399A1 (en) 1998-12-23 2003-03-06 Smithkline Beecham Corporation Method of treatment
EP1175405A4 (en) 1999-02-09 2002-05-15 Bristol Myers Squibb Co LACTAM INHIBITORS OF FACTOR Xa AND ASSOCIATED METHOD
DZ3083A1 (fr) 1999-02-19 2004-06-02 Smithkline Beecham Corp Composés nouveaux inhibiteurs de protéases, procédé pour leur préparation et compositions pharmaceutiques les conentant.
UY26026A1 (es) 1999-03-16 2000-10-31 Smithkline Beecham Corportion Inhibidores de proteasas
UY26088A1 (es) 1999-03-31 2000-10-31 Smithkline Beecham Corp Inhibidores de proteasas
JP4829449B2 (ja) 1999-07-28 2011-12-07 アベンティス・ファーマスーティカルズ・インコーポレイテツド 置換オキソアザヘテロシクリル化合物
EP1232155A4 (en) 1999-11-10 2002-11-20 Smithkline Beecham Corp PROTEASE INHIBITORS
JP2003513926A (ja) 1999-11-10 2003-04-15 スミスクライン・ビーチャム・コーポレイション プロテアーゼ阻害剤
EP1232154A4 (en) 1999-11-10 2004-06-23 Smithkline Beecham Corp PROTEASE INHIBITORS
AU1474701A (en) 1999-11-10 2001-06-06 Smithkline Beecham Corporation Protease inhibitors
WO2001034154A1 (en) 1999-11-10 2001-05-17 Smithkline Beecham Corporation Protease inhibitors
WO2001034153A1 (en) 1999-11-10 2001-05-17 Smithkline Beecham Corporation Protease inhibitors
WO2001034157A1 (en) 1999-11-10 2001-05-17 Smithkline Beecham Corporation Protease inhibitors
JP2003513928A (ja) 1999-11-10 2003-04-15 スミスクライン・ビーチャム・コーポレイション プロテアーゼ阻害剤
JP2003513956A (ja) 1999-11-10 2003-04-15 スミスクライン・ビーチャム・コーポレイション プロテアーゼ阻害剤
JP2003513927A (ja) 1999-11-10 2003-04-15 スミスクライン・ビーチャム・コーポレイション プロテア−ゼ阻害剤
AU1474801A (en) * 1999-11-10 2001-06-06 Smithkline Beecham Corporation Protease inhibitors
WO2001034155A1 (en) 1999-11-10 2001-05-17 Smithkline Beecham Corporation Protease inhibitors
DE10004572A1 (de) * 2000-02-02 2001-08-09 Boehringer Ingelheim Pharma Neue positive allosterische AMPA-Rezeptor Modulatoren (PAARM), Verfahren zu deren Herstellung und deren Verwendung als Arzneimittel
BR0109356A (pt) * 2000-03-21 2003-06-03 Smithkline Beecham Corp Inibidores de protease
US20030114437A1 (en) 2002-10-17 2003-06-19 Cummings Maxwell D. Protease inhibitors
WO2002017924A1 (en) 2000-09-01 2002-03-07 Smithkline Beecham Corporation Method of treatment
BR0115473A (pt) 2000-11-22 2004-09-28 Smithkline Beecham Corp Inibidores de protease
US20040034013A1 (en) 2001-04-17 2004-02-19 Cummings Maxwell D Methods of treatment
AU2002342682A1 (en) 2001-05-17 2002-11-25 Smithkline Beecham Corporation Protease inhibitors
WO2003026770A1 (en) 2001-09-24 2003-04-03 Smithkline Beecham Corporation Method for removing metal from the products of olefin metathesis reactions
WO2003045909A2 (en) 2001-11-21 2003-06-05 Smithkline Beecham Corporation Methods and intermediates for the synthesis of azepines
EP1534292A4 (en) 2002-05-22 2008-04-02 Smithkline Beecham Corp PROTEASE INHIBITORS
AU2003304496A1 (en) 2002-05-22 2005-04-27 Smithkline Beecham Corporation Protease inhibitors
WO2003103574A2 (en) 2002-05-22 2003-12-18 Smithkline Beecham Corporation Protease inhibitors
EP1532115A4 (en) 2002-05-22 2006-01-11 Smithkline Beecham Corp INHIBITORS OF PROTEASE
EP1511745A4 (en) 2002-05-22 2006-11-15 Smithkline Beecham Corp PROTEASE INHIBITORS
US20050030912A1 (en) 2002-08-22 2005-02-10 Enikia L.L.C. Use of hybrid (HW/DSP/MCU/SW) architectures for powerline OFDM communication field
WO2005013909A2 (en) 2003-08-07 2005-02-17 Smithkline Beecham Corporation Novel cathepsin k inhibitors
US7366462B2 (en) 2003-10-24 2008-04-29 Qualcomm Incorporated Method and apparatus for seamlessly switching reception between multimedia streams in a wireless communication system

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN103275070A (zh) * 2013-05-10 2013-09-04 郑彪 调节单核细胞增殖的四环化合物及其应用
CN116194114A (zh) * 2020-03-26 2023-05-30 葛兰素史密斯克莱知识产权发展有限公司 用于防止或治疗病毒感染的组织蛋白酶抑制剂

Also Published As

Publication number Publication date
KR20020082896A (ko) 2002-10-31
AP1540A (en) 2006-01-11
MXPA02009305A (es) 2003-03-12
NO20024528L (no) 2002-11-19
NZ520588A (en) 2004-06-25
MY141596A (en) 2010-05-31
US7071184B2 (en) 2006-07-04
WO2001070232A1 (en) 2001-09-27
BG106962A (bg) 2003-03-31
EA005893B1 (ru) 2005-06-30
DZ3318A1 (fr) 2001-09-27
SK13632002A3 (sk) 2003-02-04
IL150964A0 (en) 2003-02-12
PE20011233A1 (es) 2002-02-07
AP2002002593A0 (en) 2002-09-30
NO20024528D0 (no) 2002-09-20
CA2404206A1 (en) 2001-09-27
HUP0300068A2 (en) 2003-05-28
AU2001243441B2 (en) 2004-11-25
BR0109356A (pt) 2003-06-03
EA200201001A1 (ru) 2003-02-27
CZ20023168A3 (cs) 2003-02-12
EP1307203A1 (en) 2003-05-07
US7563784B2 (en) 2009-07-21
AR032877A1 (es) 2003-12-03
AU4344101A (en) 2001-10-03
UY26625A1 (es) 2001-09-28
US20040044201A1 (en) 2004-03-04
OA12323A (en) 2006-05-15
US20060194787A1 (en) 2006-08-31
EP1307203A4 (en) 2005-08-17
PL357727A1 (en) 2004-07-26
JP2003527429A (ja) 2003-09-16

Similar Documents

Publication Publication Date Title
CN1416346A (zh) 蛋白酶抑制剂
CN1253441C (zh) 蛋白酶抑制剂
CN1171870C (zh) 半胱氨酸蛋白酶抑制剂
CN1303067C (zh) 用作半光氨酸蛋白酶可逆抑制剂的螺杂环腈
CN1213040C (zh) 丝氨酸蛋白酶抑制剂
CN1177821C (zh) 基质金属蛋白酶抑制剂
CN1324022C (zh) 酪氨酸激酶抑制剂
CN1044117C (zh) 用于抑制人免疫缺陷病毒蛋白酶的化合物及其制备方法和药物用途
CN1221529C (zh) 取代的n-[(氨基亚氨基甲基或氨甲基)苯基]丙基酰胺
CN1105706C (zh) 用作氧化氮合成酶抑制剂的环状脒基制剂
CN1305470A (zh) 脒化合物
CN1723196A (zh) 作为二肽酶抑制剂的氟代吡咯烷
CN1898199A (zh) 用于治疗阿尔茨海默病的苯基酰胺和吡啶基酰胺类β-分泌酶抑制剂
CN1255162A (zh) 蛋白酶抑制剂
CN1913886A (zh) 杂环天冬氨酰蛋白酶抑制剂
CN1342145A (zh) 稠环化合物及其药物用途
CN1585749A (zh) 类大麻苷受体配体
CN1863797A (zh) 具有苯甲酰胺取代基的环胺bace-1抑制剂
CN1265645A (zh) 尿激酶抑制剂
CN1681789A (zh) 1-吡啶-4-基-脲衍生物
CN1296354C (zh) 具有药物活性的吡咯烷衍生物
CN1620424A (zh) 治疗炎性疾病的化合物
CN1255161A (zh) 蛋白酶抑制剂
CN1079396C (zh) 用作选择性凝血酶抑制剂的芳族脒衍生物
CN1606443A (zh) 作为催产素拮抗剂的取代的二酮哌嗪类

Legal Events

Date Code Title Description
C06 Publication
PB01 Publication
C10 Entry into substantive examination
SE01 Entry into force of request for substantive examination
C12 Rejection of a patent application after its publication
RJ01 Rejection of invention patent application after publication