CN1044117C - 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 - Google Patents

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 Download PDF

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Publication number
CN1044117C
CN1044117C CN93112962A CN93112962A CN1044117C CN 1044117 C CN1044117 C CN 1044117C CN 93112962 A CN93112962 A CN 93112962A CN 93112962 A CN93112962 A CN 93112962A CN 1044117 C CN1044117 C CN 1044117C
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CN
China
Prior art keywords
amino
tert
butyl
aza
oxo
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Expired - Fee Related
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CN93112962A
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English (en)
Chinese (zh)
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CN1094399A (zh
Inventor
L·N·容海姆
T·A·谢泼德
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Eli Lilly and Co
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Eli Lilly and Co
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Filing date
Publication date
Priority claimed from US08/134,329 external-priority patent/US5733906A/en
Application filed by Eli Lilly and Co filed Critical Eli Lilly and Co
Publication of CN1094399A publication Critical patent/CN1094399A/zh
Application granted granted Critical
Publication of CN1044117C publication Critical patent/CN1044117C/zh
Anticipated expiration legal-status Critical
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/58—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems with hetero atoms directly attached to the ring nitrogen atom
    • C07D215/60—N-oxides
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic 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
    • C07D401/02—Heterocyclic 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
    • C07D401/06—Heterocyclic 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 carbon chain containing only aliphatic carbon atoms
    • 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
    • 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
    • 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
    • C07D217/26—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic 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
    • C07D401/02—Heterocyclic 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
    • C07D401/12—Heterocyclic 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

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Virology (AREA)
  • Public Health (AREA)
  • Oncology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Communicable Diseases (AREA)
  • Veterinary Medicine (AREA)
  • AIDS & HIV (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Molecular Biology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)
  • Thiazole And Isothizaole Compounds (AREA)
  • Other In-Based Heterocyclic Compounds (AREA)
  • Hydrogenated Pyridines (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Pyrrole Compounds (AREA)
  • Medicines Containing Plant Substances (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
CN93112962A 1992-12-22 1993-12-21 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 Expired - Fee Related CN1044117C (zh)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US134,329 1987-12-17
US99525692A 1992-12-22 1992-12-22
US995,256 1992-12-22
US134,429 1993-10-12
US08/134,329 US5733906A (en) 1993-10-12 1993-10-12 Inhibitors of HIV Protease useful for the treatment of Aids

Publications (2)

Publication Number Publication Date
CN1094399A CN1094399A (zh) 1994-11-02
CN1044117C true CN1044117C (zh) 1999-07-14

Family

ID=26832220

Family Applications (1)

Application Number Title Priority Date Filing Date
CN93112962A Expired - Fee Related CN1044117C (zh) 1992-12-22 1993-12-21 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

Country Status (21)

Country Link
US (1) US5905077A (enExample)
EP (1) EP0604185B1 (enExample)
JP (1) JPH06271534A (enExample)
KR (1) KR940014337A (enExample)
CN (1) CN1044117C (enExample)
AT (1) ATE178055T1 (enExample)
AU (1) AU667146B2 (enExample)
BR (1) BR9305162A (enExample)
CA (1) CA2112042A1 (enExample)
CZ (1) CZ281493A3 (enExample)
DE (1) DE69324120T2 (enExample)
ES (1) ES2132201T3 (enExample)
FI (1) FI935778A7 (enExample)
HU (1) HUT69693A (enExample)
IL (1) IL108092A (enExample)
MX (1) MX9308016A (enExample)
MY (1) MY131388A (enExample)
NO (1) NO934719L (enExample)
NZ (1) NZ250491A (enExample)
PL (1) PL301581A1 (enExample)
TW (1) TW262468B (enExample)

Cited By (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN103140474A (zh) * 2010-07-02 2013-06-05 吉里德科学公司 治疗aids的萘-2-基乙酸衍生物
US8987250B2 (en) 2012-04-20 2015-03-24 Gilead Sciences, Inc. Therapeutic compounds
US9006229B2 (en) 2011-04-21 2015-04-14 Gilead Sciences, Inc. Benzothiazole compounds and their pharmaceutical use
US9284323B2 (en) 2012-01-04 2016-03-15 Gilead Sciences, Inc. Naphthalene acetic acid derivatives against HIV infection
US9296758B2 (en) 2010-07-02 2016-03-29 Gilead Sciences, Inc. 2-quinolinyl-acetic acid derivatives as HIV antiviral compounds
US9376392B2 (en) 2012-01-04 2016-06-28 Gilead Sciences, Inc. 2-(tert-butoxy)-2-(7-methylquinolin-6-yl) acetic acid derivatives for treating AIDS

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USH1649H (en) 1987-07-31 1997-05-06 Barrish; Joel C. HIV protease inhibitor combinations
US6071895A (en) 1992-03-11 2000-06-06 Narhex Limited Polar-substituted hydrocarbons
US5888992A (en) 1992-03-11 1999-03-30 Narhex Limited Polar substituted hydrocarbons
JPH07504654A (ja) 1992-03-11 1995-05-25 ナルヘックス　リミテッド オキソ及びヒドロキシ置換炭化水素のアミン誘導体
US5484926A (en) 1993-10-07 1996-01-16 Agouron Pharmaceuticals, Inc. HIV protease inhibitors
US5461154A (en) * 1994-02-02 1995-10-24 Eli Lilly And Company Intermediate and process for making
TW472047B (en) * 1994-02-04 2002-01-11 Merck & Co Inc Process for making HIV protease inhibitors
ATE163642T1 (de) * 1994-11-04 1998-03-15 Yamakawa Chemical Ind Verfahren zur herstellung von optisch aktiven piperazinderivaten und zwischenprodukten für ihre herstellung
DE69616446T2 (de) * 1995-02-03 2002-05-16 Kaneka Corp., Osaka Verfahren zur herstellung von alpha-haloketonen, alpha-halohydrinen und epoxiden
US5618937A (en) * 1995-03-15 1997-04-08 Merck & Co., Inc. Process to make HIV protease inhibitor from (2S)-4-picolyl-2-piperazine-t-butylcarboxamide
US5932550A (en) * 1995-06-30 1999-08-03 Japan Energy Corporation Dipeptide compound or pharmaceutically acceptable salt thereof and medical use thereof
US6222043B1 (en) 1995-06-30 2001-04-24 Japan Energy Corporation Methods of preparing novel dipeptide compounds or pharmaceutically acceptable salts thereof
US6121468A (en) * 1995-09-26 2000-09-19 Japan Tobacco Inc. Process for producing amide derivatives and intermediate compounds
DE69634345T2 (de) 1995-09-26 2006-03-02 Japan Tobacco Inc. Verfahren zur herstellung von amid-derivaten und ihren zwischenverbindungen
ATE377006T1 (de) * 1995-11-28 2007-11-15 Cephalon Inc Aus d-aminosäuren abgeleitete cystein- und serinproteasehemmer
US5962725A (en) 1996-09-05 1999-10-05 Agouron Pharmaceuticals, Inc. Intermediate compounds useful for making HIV protease inhibitors such as nelfinavir
CA2249747A1 (en) 1996-12-27 1998-07-09 Tsutomu Mimoto Novel tripeptide compounds and anti-aids drugs
JP4006058B2 (ja) 1997-03-11 2007-11-14 第一三共株式会社 多臓器不全予防及び／又は治療剤
DE69836315T2 (de) 1997-03-14 2007-05-31 Daiichi Pharmaceutical Co., Ltd. Verwendung von TCF-II zur Behandlung von durch Krebs verursachtem Gewichtsverlust, Anaemie und TNF-Erhöhung
AU4862799A (en) * 1998-07-08 2000-02-01 G.D. Searle & Co. Retroviral protease inhibitors
HRP990246A2 (en) 1998-08-07 2000-06-30 Du Pont Pharm Co Succinoylamino benzodiazepines as inhibitors of a beta protein production
NZ525513A (en) 1998-08-07 2004-09-24 Pont Pharmaceuticals Du Succinoylamino lactams as inhibitors of Abeta protein production
CN1636011A (zh) 1998-12-24 2005-07-06 杜邦药品公司 作为Aβ蛋白产生抑制剂的琥珀酰氨基苯并二氮杂䓬
US6960576B2 (en) 1999-09-13 2005-11-01 Bristol-Myers Squibb Pharma Company Hydroxyalkanoylaminolactams and related structures as inhibitors of Aβ protein production
US6503902B2 (en) 1999-09-13 2003-01-07 Bristol-Myers Squibb Pharma Company Hydroxyalkanoylaminolactams and related structures as inhibitors of a β protein production
EP1218377A1 (en) 1999-10-08 2002-07-03 Bristol-Myers Squibb Pharma Company AMINO LACTAM SULFONAMIDES AS INHIBITORS OF A$g(b) PROTEIN PRODUCTION
WO2001060826A2 (en) 2000-02-17 2001-08-23 Bristol-Myers Squibb Pharma Company SUCCINOYLAMINO CARBOCYCLES AND HETEROCYCLES AS INHIBITORS OF Aβ PROTEIN PRODUCTION
US6495540B2 (en) 2000-03-28 2002-12-17 Bristol - Myers Squibb Pharma Company Lactams as inhibitors of A-β protein production
EP1268433A1 (en) 2000-04-03 2003-01-02 Bristol-Myers Squibb Pharma Company Cyclic lactams as inhibitors of a-beta-protein production
EP1268434A1 (en) 2000-04-03 2003-01-02 Bristol-Myers Squibb Pharma Company Cyclic lactams as inhibitors of a-beta protein production
US20100009966A1 (en) * 2001-04-11 2010-01-14 Bristol-Myers Squibb Pharma Company Substituted lactams as inhibitors of abeta protein production
EP1289966A1 (en) 2000-04-11 2003-03-12 Bristol-Myers Squibb Pharma Company SUBSTITUTED LACTAMS AS INHIBITORS OF A$g(b) PROTEIN PRODUCTION
WO2001087354A2 (en) * 2000-05-17 2001-11-22 Bristol-Myers Squibb Pharma Company Use of small molecule radioligands for diagnostic imaging
CA2379445C (en) 2000-06-01 2007-08-21 Bristol-Myers Squibb Pharma Company Lactams substituted by cyclic succinates as inhibitors of a.beta. protein production
GB0028483D0 (en) * 2000-11-22 2001-01-10 Hoffmann La Roche Hydroxyethylamine HIV protease inhibitors
JPWO2002064553A1 (ja) * 2001-02-14 2004-06-10 呉羽化学工業株式会社 ハロゲノアルコール誘導体の製造方法
US20090062256A1 (en) * 2001-06-01 2009-03-05 Bristol-Myers Squibb Pharma Company LACTAMS SUBSTITUTED BY CYCLIC SUCCINATES AS INHIBITORS OF Abeta PROTEIN PRODUCTION
GB0123467D0 (en) 2001-09-28 2001-11-21 Hoffmann La Roche Carbocyclic HIV Protease inhibitors
KR101155335B1 (ko) * 2005-01-07 2012-06-11 엘지전자 주식회사 이동통신 단말기의 멀티미디어 메시지 동작방법
WO2007015805A1 (en) 2005-07-20 2007-02-08 Eli Lilly And Company 1-amino linked compounds
CN101508664B (zh) * 2009-02-25 2012-08-22 江阴希迪医药科技有限公司 N-苄氧羰基-3-氨基-1-氯-4-苯硫基-2-丁醇合成方法

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US5142056A (en) * 1989-05-23 1992-08-25 Abbott Laboratories Retroviral protease inhibiting compounds
IL89900A0 (en) * 1988-04-12 1989-12-15 Merck & Co Inc Hiv protease inhibitors useful for the treatment of aids and pharmaceutical compositions containing them
CA1340588C (en) 1988-06-13 1999-06-08 Balraj Krishan Handa Amino acid derivatives
EP0361341A3 (en) * 1988-09-28 1991-07-03 Miles Inc. Therapeutics for aids based on inhibitors of hiv protease
GB8927913D0 (en) * 1989-12-11 1990-02-14 Hoffmann La Roche Amino acid derivatives
EP0558603B1 (en) * 1990-11-19 1998-08-26 Monsanto Company Retroviral protease inhibitors
CA2060844A1 (en) * 1991-02-08 1992-08-09 Yabe Yuichiro Beta-amino-alpha-hydroxycarboxylic acids and their use
US5430041A (en) * 1991-05-10 1995-07-04 Hoffmann-La Roche Inc. Amino acid derivatives having antiviral activity
CN1071930A (zh) 1991-07-10 1993-05-12 伊莱利利公司 用作治疗艾滋病的人免疫缺陷病毒蛋白酶的抑制剂
AU3278293A (en) 1991-12-20 1993-07-28 Syntex (U.S.A.) Inc. Cyclic amides of 3-amino-2-hydroxy-carboxylic acids as hiv-protease inhibitors
US5312820A (en) * 1992-07-17 1994-05-17 Merck & Co., Inc. Substituted carbamoyl and oxycarbonyl derivatives of biphenylmethylamines

Cited By (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN103140474A (zh) * 2010-07-02 2013-06-05 吉里德科学公司 治疗aids的萘-2-基乙酸衍生物
US9102614B2 (en) 2010-07-02 2015-08-11 Gilead Sciences, Inc. Naphth-2-ylacetic acid derivatives to treat AIDS
US9296758B2 (en) 2010-07-02 2016-03-29 Gilead Sciences, Inc. 2-quinolinyl-acetic acid derivatives as HIV antiviral compounds
US9006229B2 (en) 2011-04-21 2015-04-14 Gilead Sciences, Inc. Benzothiazole compounds and their pharmaceutical use
US9284323B2 (en) 2012-01-04 2016-03-15 Gilead Sciences, Inc. Naphthalene acetic acid derivatives against HIV infection
US9376392B2 (en) 2012-01-04 2016-06-28 Gilead Sciences, Inc. 2-(tert-butoxy)-2-(7-methylquinolin-6-yl) acetic acid derivatives for treating AIDS
US8987250B2 (en) 2012-04-20 2015-03-24 Gilead Sciences, Inc. Therapeutic compounds
US9096586B2 (en) 2012-04-20 2015-08-04 Gilead Sciences, Inc. Therapeutic compounds

Also Published As

Publication number Publication date
CA2112042A1 (en) 1994-06-23
NO934719L (no) 1994-06-23
NO934719D0 (no) 1993-12-20
IL108092A0 (en) 1994-04-12
MX9308016A (es) 1994-08-31
ES2132201T3 (es) 1999-08-16
AU5252893A (en) 1994-07-07
US5905077A (en) 1999-05-18
KR940014337A (ko) 1994-07-18
CN1094399A (zh) 1994-11-02
BR9305162A (pt) 1994-11-01
IL108092A (en) 1998-06-15
MY131388A (en) 2007-08-30
FI935778A0 (fi) 1993-12-21
JPH06271534A (ja) 1994-09-27
CZ281493A3 (en) 1994-07-13
NZ250491A (en) 1995-08-28
FI935778A7 (fi) 1994-06-23
ATE178055T1 (de) 1999-04-15
HUT69693A (en) 1995-09-28
EP0604185A1 (en) 1994-06-29
TW262468B (enExample) 1995-11-11
AU667146B2 (en) 1996-03-07
DE69324120T2 (de) 1999-11-25
PL301581A1 (en) 1994-06-27
DE69324120D1 (de) 1999-04-29
EP0604185B1 (en) 1999-03-24

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