CN1161340C - 为玻连蛋白受体拮抗剂的苯并咪唑化合物 - Google Patents
为玻连蛋白受体拮抗剂的苯并咪唑化合物 Download PDFInfo
- Publication number
- CN1161340C CN1161340C CNB998158429A CN99815842A CN1161340C CN 1161340 C CN1161340 C CN 1161340C CN B998158429 A CNB998158429 A CN B998158429A CN 99815842 A CN99815842 A CN 99815842A CN 1161340 C CN1161340 C CN 1161340C
- Authority
- CN
- China
- Prior art keywords
- compound
- alkyl
- resin
- ester
- acceptable salt
- 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
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Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic 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
- C07D405/02—Heterocyclic 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
- C07D405/12—Heterocyclic 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
-
- 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
- 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
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- 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
- C07D235/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
- C07D235/02—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
- C07D235/04—Benzimidazoles; Hydrogenated benzimidazoles
- C07D235/06—Benzimidazoles; Hydrogenated benzimidazoles with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 2
- C07D235/14—Radicals substituted by nitrogen atoms
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Veterinary Medicine (AREA)
- Life Sciences & Earth Sciences (AREA)
- Engineering & Computer Science (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Physical Education & Sports Medicine (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Rheumatology (AREA)
- Vascular Medicine (AREA)
- Urology & Nephrology (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Ophthalmology & Optometry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
Description
实施例 | Q | MS m/e[M+H]+ | HPLC保留时间,分 |
5-96 | Cbz | 603 | 5.22 |
5-97 | n-BuO2C | 569 | 4.98 |
实施例 | IC50,nM |
5-1 | 5.4 |
5-2 | 6.5 |
5-3 | 1.9 |
5-4 | 2.9 |
实施例 | IC50,nM |
5-5 | 0.42 |
5-6 | ~500 |
5-7 | ~500 |
5-8 | ~500 |
5-9 | ~500 |
5-10 | ~500 |
实施例 | IC50,nM | 特异性αⅡbβ3/αvβ3 |
5-11 | 3.4 | 70 |
5-12 | 5.6 | 87 |
5-13 | 3.1 | 38 |
5-14 | 5.8 | 117 |
5-15 | 4.3 | 95 |
5-16 | 4.4 | 899 |
5-17 | 4.6 | 76 |
5-18 | 4.4 | 82 |
5-19 | 8.9 | 34 |
5-20 | 7.2 | 15 |
5-21 | 4.4 | 41 |
5-22 | 6.4 | 26 |
5-23 | 5.5 | 22 |
实施例 | IC50,nM | 特异性αIIbβ3/αvβ3 |
5-24 | 5.3 | 14 |
5-25 | 4.5 | 52 |
5-26 | 3.5 | 91 |
5-27 | 1.56 | 481 |
5-28 | 0.65 | 1136 |
5-29 | 4.3 | 144 |
5-30 | 2.3 | 296 |
5-31 | 6.0 | 80 |
5-32 | 6.5 | 151 |
5-33 | 17 | 128 |
5-34 | 2.3 | 421 |
5-35 | 8.1 | 240 |
5-36 | 11.7 | 129 |
5-37 | 5.3 | 203 |
5-38 | 13.6 | 49 |
5-139 | 3.1 | 223 |
5-40 | 5.7 | 288 |
5-41 | 2.8 | 19 |
5-42 | 1.8 | 39 |
5-43 | 2.2 | 585 |
5-44 | 19.6 | 66.3 |
5-45 | 2.2 | 1333 |
实施例 | IC50,nM | 特异性αIIbβ3/αvβ3 |
5-46 | 2.7 | 1065 |
5-7 | 2.2 | 1252 |
5-48 | 1.0 | 2028 |
5-49 | 4.2 | 504 |
5-50 | 3.0 | 805 |
5-51 | 1.1 | 1210 |
5-52 | 4.0 | 448 |
5-53 | 3.8 | 483 |
5-54 | 2.0 | 413 |
5-55 | 2.5 | 620 |
5-56 | 1.6 | 514 |
实施例 | IC50,nM | 特异性αIIbβ3/αvβ3 |
5-57 | 1293 | 1.43 |
5-58 | 118 | 46 |
5-59 | 129 | 65 |
实施例 | IC50,nM | 特异性αIIbβ3/αvβ3 |
5-60 | 25 | 90 |
5-61 | 17 | 324 |
5-62 | 30 | 419 |
5-63 | 20 | 293 |
5-64 | 16 | 499 |
实施例 | IC50,nM | 特异性αIIbβ3/αvβ3 |
5-65 | 9,227 | 0.4 |
5-66 | 9.468 | 0.4 |
5-67 | 7,373 | 0.5 |
5-68 | 6,630 | 0.4 |
5-69 | 10,514 | 0.4 |
实施例 | IC50nM | 特异性αIIbβ3/αvβ3 |
5-70 | 413 | 0.2 |
5-71 | 266 | 0.3 |
5-72 | 559 | 0.5 |
5-73 | 170 | 0.7 |
5-74 | 238 | 0.6 |
实施例 | IC50,nM | 特异性αIIbβ3/αvβ3 |
5-75 | 306 | 10.2 |
5-76 | 50 | 6.7 |
5-77 | 49 | 12.4 |
5-78 | 21 | 33.9 |
5-79 | 33 | 19.0 |
实施例 | IC50,nM | 特异性αIIbβ3/αvβ3 |
5-80 | 4.4 | 11 |
5-81 | 8.2 | 8.0 |
5-82 | 2.2 | 1259 |
5-83 | 1.8 | 1689 |
5-84 | 3.6 | 712 |
5-85 | 1.8 | 1223 |
5-86 | 3.3 | 793 |
5-87 | 2.0 | 1569 |
5-88 | 2.0 | 1657 |
5-89 | 3.3 | 1094 |
5-90 | 2.6 | 1697 |
5-91 | 2.8 | 1183 |
5-92 | 7.6 | 174 |
实施例 | IC50,nM | 特异性αIIbβ3/αvβ3 |
5-93 | 6.7 | 124 |
5-94 | 3.8 | 399 |
5-95 | 1.7 | 775 |
5-96 | 3.4 | 528 |
5-97 | 4.3 | 2600 |
号 | 成分 | mg/片 | mg/片 |
1 | 活性化合物 | 100 | 5 |
2 | 乳糖USP | 122 | 40 |
3 | 玉米淀粉,食品级,为在纯水中的10%糊状物 | 30 | 25 |
4 | 玉米淀粉,食品级 | 45 | 25 |
5 | 硬脂酸镁 | 3 | 5 |
总量 | 300 | 100 |
号 | 成分 | mg/胶囊 | mg/胶囊 |
1 | 活性化合物 | 100 | 5 |
2 | 乳糖USP | 106 | 45 |
3 | 玉米淀粉,食品级 | 40 | 45 |
4 | 硬脂酸镁NF | 7 | 5 |
总量 | 253 | 100 |
Claims (21)
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US20161198A | 1998-11-30 | 1998-11-30 | |
US09/201611 | 1998-11-30 |
Publications (2)
Publication Number | Publication Date |
---|---|
CN1333755A CN1333755A (zh) | 2002-01-30 |
CN1161340C true CN1161340C (zh) | 2004-08-11 |
Family
ID=22746536
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
CNB998158429A Expired - Fee Related CN1161340C (zh) | 1998-11-30 | 1999-09-29 | 为玻连蛋白受体拮抗剂的苯并咪唑化合物 |
Country Status (12)
Country | Link |
---|---|
EP (1) | EP1135374B9 (zh) |
JP (1) | JP4480117B2 (zh) |
CN (1) | CN1161340C (zh) |
AR (1) | AR021427A1 (zh) |
AT (1) | ATE338751T1 (zh) |
AU (1) | AU1908400A (zh) |
CA (1) | CA2353063C (zh) |
CO (1) | CO5140112A1 (zh) |
DE (1) | DE69933135T2 (zh) |
ES (1) | ES2273517T3 (zh) |
PE (1) | PE20001427A1 (zh) |
WO (1) | WO2000032578A1 (zh) |
Families Citing this family (15)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
KR20010112408A (ko) * | 1999-04-07 | 2001-12-20 | 모리타 다카카즈 | N-치환되고-N'-치환된 우레아 유도체 및 TNF-α 생성억제제로서의 그의 용도 |
HUP0201033A3 (en) * | 1999-05-17 | 2003-03-28 | Novo Nordisk As | Glucagon antagonists/inverse agonists, process for their preparation and their use |
FR2809396B1 (fr) | 2000-05-24 | 2005-10-14 | Centre Nat Rech Scient | Nouvelles molecules possedant une activite calcimimetique et leur mode de preparation |
US6562807B2 (en) | 2000-06-23 | 2003-05-13 | Novo Nordisk A/S | Glucagon antagonists/inverse agonists |
EP2164958B1 (en) | 2007-06-07 | 2014-08-13 | Novozymes A/S | Method of preparing a dough-based product |
US10390538B2 (en) | 2010-07-21 | 2019-08-27 | Novozymes A/S | Process for preparing a baked product with anti-staling amylase and peptidase |
PE20170143A1 (es) | 2014-02-11 | 2017-03-19 | Bayer Pharma AG | Benzimidazol-2-aminas como inhibidores de midh1 |
ES2732902T3 (es) | 2014-02-11 | 2019-11-26 | Deutsches Krebsforschungszentrum Stiftung Des Oeffentlichen Rechts | Bencimidazol-2-aminas como inhibidores de MIDH1 |
CN104694290A (zh) * | 2014-05-07 | 2015-06-10 | 宁波职业技术学院 | 一种洗脚皂 |
ES2814151T3 (es) | 2014-10-23 | 2021-03-26 | Deutsches Krebsforschungszentrum Stiftung Des Oeffentlichen Rechts | 1-Ciclohexilo-2-fenilaminobenzimidazoles como inhibidores de MIDH1 para el tratamiento de tumores |
US10138226B2 (en) | 2014-10-23 | 2018-11-27 | Bayer Pharma Aktiengesellschaft | Benzimidazol-2-amines as MIDH1 inhibitors |
WO2016198322A1 (en) | 2015-06-08 | 2016-12-15 | Bayer Pharma Aktiengesellschaft | N-menthylbenzimidazoles as midh1 inhibitors |
US10414734B2 (en) | 2015-07-16 | 2019-09-17 | Bayer Pharma Aktiengesellschaft | 5-hydroxyalkylbenzimidazoles as mIDH1 inhibitors |
TW202146416A (zh) | 2019-12-11 | 2021-12-16 | 德商拜耳廠股份有限公司 | 吡唑并三𠯤 |
EP4114528A1 (en) | 2020-03-06 | 2023-01-11 | Bayer Aktiengesellschaft | Imidazotriazines acting on cancer via inhibition of cdk12 |
Family Cites Families (2)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
WO1995032710A1 (en) * | 1994-05-27 | 1995-12-07 | Merck & Co., Inc. | Compounds for inhibiting osteoclast-mediated bone resorption |
MX9700041A (es) * | 1994-06-29 | 1997-04-30 | Smithkline Beecham Corp | Antagonistas de receptor de vitronectina. |
-
1999
- 1999-09-29 CN CNB998158429A patent/CN1161340C/zh not_active Expired - Fee Related
- 1999-11-29 EP EP99962691A patent/EP1135374B9/en not_active Expired - Lifetime
- 1999-11-29 AR ARP990106061A patent/AR021427A1/es unknown
- 1999-11-29 CA CA002353063A patent/CA2353063C/en not_active Expired - Fee Related
- 1999-11-29 JP JP2000585220A patent/JP4480117B2/ja not_active Expired - Lifetime
- 1999-11-29 AT AT99962691T patent/ATE338751T1/de not_active IP Right Cessation
- 1999-11-29 AU AU19084/00A patent/AU1908400A/en not_active Abandoned
- 1999-11-29 ES ES99962691T patent/ES2273517T3/es not_active Expired - Lifetime
- 1999-11-29 DE DE69933135T patent/DE69933135T2/de not_active Expired - Lifetime
- 1999-11-29 WO PCT/US1999/026023 patent/WO2000032578A1/en active IP Right Grant
- 1999-11-30 PE PE1999001198A patent/PE20001427A1/es not_active Application Discontinuation
- 1999-11-30 CO CO99075257A patent/CO5140112A1/es unknown
Also Published As
Publication number | Publication date |
---|---|
EP1135374B1 (en) | 2006-09-06 |
JP4480117B2 (ja) | 2010-06-16 |
CA2353063A1 (en) | 2000-06-08 |
EP1135374A1 (en) | 2001-09-26 |
PE20001427A1 (es) | 2000-12-18 |
ATE338751T1 (de) | 2006-09-15 |
ES2273517T3 (es) | 2007-05-01 |
JP2002531441A (ja) | 2002-09-24 |
AR021427A1 (es) | 2002-07-17 |
CO5140112A1 (es) | 2002-03-22 |
AU1908400A (en) | 2000-06-19 |
EP1135374B9 (en) | 2007-02-21 |
DE69933135D1 (de) | 2006-10-19 |
WO2000032578A8 (en) | 2002-02-07 |
WO2000032578A1 (en) | 2000-06-08 |
CA2353063C (en) | 2009-06-16 |
DE69933135T2 (de) | 2007-08-09 |
CN1333755A (zh) | 2002-01-30 |
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GR01 | Patent grant | ||
CI01 | Publication of corrected invention patent application |
Correction item: International application date Correct: 19991129 False: 19990929 Number: 32 Page: 441 Volume: 20 |
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C19 | Lapse of patent right due to non-payment of the annual fee | ||
CF01 | Termination of patent right due to non-payment of annual fee |