JP2002522536A5 - - Google Patents
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- Publication number
- JP2002522536A5 JP2002522536A5 JP2000564948A JP2000564948A JP2002522536A5 JP 2002522536 A5 JP2002522536 A5 JP 2002522536A5 JP 2000564948 A JP2000564948 A JP 2000564948A JP 2000564948 A JP2000564948 A JP 2000564948A JP 2002522536 A5 JP2002522536 A5 JP 2002522536A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- group
- substituted
- different substituents
- aryl
- 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.)
- Granted
Links
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 description 47
- 125000001424 substituent group Chemical group 0.000 description 18
- 125000002887 hydroxy group Chemical group [H]O* 0.000 description 15
- 229910052757 nitrogen Inorganic materials 0.000 description 13
- 125000004433 nitrogen atom Chemical group N* 0.000 description 12
- 150000003839 salts Chemical class 0.000 description 11
- 150000001875 compounds Chemical class 0.000 description 10
- 125000003118 aryl group Chemical group 0.000 description 9
- 125000000229 (C1-C4)alkoxy group Chemical group 0.000 description 8
- 229910052739 hydrogen Inorganic materials 0.000 description 8
- 239000001257 hydrogen Substances 0.000 description 8
- 125000005842 heteroatom Chemical group 0.000 description 7
- 239000000203 mixture Substances 0.000 description 7
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 description 6
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 description 5
- -1 R 8 R 9 N Chemical group 0.000 description 5
- 125000000217 alkyl group Chemical group 0.000 description 5
- 125000004429 atom Chemical group 0.000 description 5
- 229910052736 halogen Inorganic materials 0.000 description 5
- 150000002367 halogens Chemical class 0.000 description 5
- 125000000623 heterocyclic group Chemical group 0.000 description 5
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 description 5
- 229910052760 oxygen Inorganic materials 0.000 description 4
- 125000004209 (C1-C8) alkyl group Chemical group 0.000 description 3
- 125000006763 (C3-C9) cycloalkyl group Chemical group 0.000 description 3
- 125000004435 hydrogen atom Chemical group [H]* 0.000 description 3
- 229910052717 sulfur Inorganic materials 0.000 description 3
- 125000001072 heteroaryl group Chemical group 0.000 description 2
- ORTFAQDWJHRMNX-UHFFFAOYSA-N hydroxidooxidocarbon(.) Chemical group O[C]=O ORTFAQDWJHRMNX-UHFFFAOYSA-N 0.000 description 2
- 125000004430 oxygen atom Chemical group O* 0.000 description 2
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 description 2
- 125000006531 (C2-C5) alkyl group Chemical group 0.000 description 1
- DNCYBUMDUBHIJZ-UHFFFAOYSA-N 1h-pyrimidin-6-one Chemical compound O=C1C=CN=CN1 DNCYBUMDUBHIJZ-UHFFFAOYSA-N 0.000 description 1
- 206010002383 Angina Pectoris Diseases 0.000 description 1
- 201000001320 Atherosclerosis Diseases 0.000 description 1
- 208000024172 Cardiovascular disease Diseases 0.000 description 1
- 206010052337 Diastolic dysfunction Diseases 0.000 description 1
- 206010048554 Endothelial dysfunction Diseases 0.000 description 1
- 208000010228 Erectile Dysfunction Diseases 0.000 description 1
- 208000011514 Familial renal glucosuria Diseases 0.000 description 1
- 206010016654 Fibrosis Diseases 0.000 description 1
- 206010019280 Heart failures Diseases 0.000 description 1
- 206010020772 Hypertension Diseases 0.000 description 1
- 102000007637 Soluble Guanylyl Cyclase Human genes 0.000 description 1
- 108010007205 Soluble Guanylyl Cyclase Proteins 0.000 description 1
- 208000006011 Stroke Diseases 0.000 description 1
- 208000007536 Thrombosis Diseases 0.000 description 1
- 230000003213 activating effect Effects 0.000 description 1
- 239000012190 activator Substances 0.000 description 1
- 125000004453 alkoxycarbonyl group Chemical group 0.000 description 1
- 150000001412 amines Chemical class 0.000 description 1
- 125000006615 aromatic heterocyclic group Chemical group 0.000 description 1
- 208000006673 asthma Diseases 0.000 description 1
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 description 1
- 125000002619 bicyclic group Chemical group 0.000 description 1
- 125000002837 carbocyclic group Chemical group 0.000 description 1
- 208000020832 chronic kidney disease Diseases 0.000 description 1
- 208000022831 chronic renal failure syndrome Diseases 0.000 description 1
- 230000007882 cirrhosis Effects 0.000 description 1
- 208000019425 cirrhosis of liver Diseases 0.000 description 1
- 239000003814 drug Substances 0.000 description 1
- 239000003937 drug carrier Substances 0.000 description 1
- 230000004064 dysfunction Effects 0.000 description 1
- 230000008694 endothelial dysfunction Effects 0.000 description 1
- 201000001881 impotence Diseases 0.000 description 1
- 208000030603 inherited susceptibility to asthma Diseases 0.000 description 1
- 238000004519 manufacturing process Methods 0.000 description 1
- 238000000034 method Methods 0.000 description 1
- 208000010125 myocardial infarction Diseases 0.000 description 1
- 125000001624 naphthyl group Chemical group 0.000 description 1
- 239000001301 oxygen Substances 0.000 description 1
- 239000000825 pharmaceutical preparation Substances 0.000 description 1
- 208000002815 pulmonary hypertension Diseases 0.000 description 1
- 208000007278 renal glycosuria Diseases 0.000 description 1
- 208000037803 restenosis Diseases 0.000 description 1
- 125000004434 sulfur atom Chemical group 0.000 description 1
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 description 1
- 125000005505 thiomorpholino group Chemical group 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| DE19836697A DE19836697A1 (de) | 1998-08-13 | 1998-08-13 | Substituierte 4-Amino-2-aryl-pyrimidine, ihre Herstellung, ihre Verwendung und sie enthaltende pharmazeutische Präparate |
| DE19836697.3 | 1998-08-13 | ||
| PCT/EP1999/005636 WO2000009496A1 (de) | 1998-08-13 | 1999-08-04 | Substituierte 4-amino-2-aryl-pyrimidine, ihre herstellung, ihre verwendung und sie enthaltende pharmazeutische präparate |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2002522536A JP2002522536A (ja) | 2002-07-23 |
| JP2002522536A5 true JP2002522536A5 (https=) | 2006-09-28 |
| JP4594526B2 JP4594526B2 (ja) | 2010-12-08 |
Family
ID=7877414
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2000564948A Expired - Fee Related JP4594526B2 (ja) | 1998-08-13 | 1999-08-04 | 置換４−アミノ−２−アリールピリミジン、それらの製造、それらの使用およびそれらを含有する医薬製剤 |
Country Status (14)
| Country | Link |
|---|---|
| US (1) | US6844347B1 (https=) |
| EP (1) | EP1112266B1 (https=) |
| JP (1) | JP4594526B2 (https=) |
| KR (1) | KR100971093B1 (https=) |
| AR (1) | AR020165A1 (https=) |
| AT (1) | ATE240315T1 (https=) |
| AU (1) | AU760988B2 (https=) |
| BR (1) | BR9913003B1 (https=) |
| CA (1) | CA2340405C (https=) |
| DE (2) | DE19836697A1 (https=) |
| DK (1) | DK1112266T3 (https=) |
| ES (1) | ES2196849T3 (https=) |
| PT (1) | PT1112266E (https=) |
| WO (1) | WO2000009496A1 (https=) |
Families Citing this family (28)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE19853278A1 (de) | 1998-11-19 | 2000-05-25 | Aventis Pharma Gmbh | Substituierte 4-Amino-2-aryl-cyclopenta[d]pyrimidine, ihre Herstellung, ihre Verwendung und sie enthaltende pharmazeutische Präparate |
| DE19904710A1 (de) | 1999-02-05 | 2000-08-10 | Aventis Pharma Gmbh | Substituierte 4-Amino-2-aryl-tetrahydrochinazoline, ihre Herstellung, ihre Verwendung und sie enthaltende pharmazeutische Präparate |
| EP1237849A1 (en) * | 1999-11-05 | 2002-09-11 | University College London | Activators of soluble guanylate cyclase |
| ES2242839T3 (es) * | 2001-04-20 | 2005-11-16 | Ciba Specialty Chemicals Holding Inc. | 4-amino-2- (piridin-2-il)pirimidina como sustancias activas microbicidas. |
| US7731985B2 (en) | 2002-03-15 | 2010-06-08 | Ciba Specialty Chemicals Corporation | 4-aminopyrimidines and their use for the antimicrobial treatment of surfaces |
| AU2003249369A1 (en) | 2002-06-21 | 2004-01-06 | Cellular Genomics, Inc. | Certain amino-substituted monocycles as kinase modulators |
| BR0313204A (pt) * | 2002-08-02 | 2005-06-28 | Pharmacia Corp | Métodos para tratamento e prevenção de condições gastrointestinais |
| CA2531619A1 (en) * | 2003-07-16 | 2005-01-27 | Neurogen Corporation | Biaryl piperazinyl-pyridine analogues |
| GB0323137D0 (en) * | 2003-10-03 | 2003-11-05 | Chang Lisa C W | 2,4,6- Trisubstituted pyrimidines and their different uses |
| CA2551944A1 (en) * | 2003-12-15 | 2005-06-30 | Almirall Prodesfarma Ag | 2, 6 bisheteroaryl-4-aminopyrimidines as adenosine receptor antagonists |
| GB0415364D0 (en) * | 2004-07-09 | 2004-08-11 | Astrazeneca Ab | Pyrimidine derivatives |
| GB0415367D0 (en) * | 2004-07-09 | 2004-08-11 | Astrazeneca Ab | Pyrimidine derivatives |
| GB0415365D0 (en) * | 2004-07-09 | 2004-08-11 | Astrazeneca Ab | Pyrimidine derivatives |
| MY145822A (en) | 2004-08-13 | 2012-04-30 | Neurogen Corp | Substituted biaryl piperazinyl-pyridine analogues |
| DE602006020864D1 (de) * | 2005-04-11 | 2011-05-05 | Almirall Sa | 2, 6-di-(hetero-)aryl-4-amido-pyrimidine als adenosin-rezeptor-antagonisten |
| JP2008540443A (ja) * | 2005-05-04 | 2008-11-20 | バーテックス ファーマシューティカルズ インコーポレイテッド | イオンチャネルのモジュレーターとして有用なピリミジンおよびピラジン |
| JP2010511727A (ja) * | 2006-12-04 | 2010-04-15 | ニューロクライン バイオサイエンシーズ，インコーポレイテッド | アデノシン受容体アンタゴニストとしての置換ピリミジン |
| WO2008116185A2 (en) * | 2007-03-21 | 2008-09-25 | Neurocrine Biosciences, Inc. | Substituted pyrimidines as adenosine receptor antagonists |
| WO2008128984A1 (en) * | 2007-04-20 | 2008-10-30 | Probiodrug Ag | Aminopyrimidine derivatives as glutaminyl cyclase inhibitors |
| WO2009068652A1 (en) * | 2007-11-30 | 2009-06-04 | Smithkline Beecham Corporation | 2, 6-disubstituted pyridines and 2, 4-disubstituted pyrimidines as soluble guanylate cyclase activators |
| AU2009322836B2 (en) * | 2008-11-25 | 2013-04-04 | Merck Sharp & Dohme Corp. | Soluble guanylate cyclase activators |
| US9284301B2 (en) | 2010-03-25 | 2016-03-15 | Merck Sharp & Dohme Corp. | Soluble guanylate cyclase activators |
| KR20140019004A (ko) | 2010-05-27 | 2014-02-13 | 머크 샤프 앤드 돔 코포레이션 | 가용성 구아닐레이트 시클라제 활성화제 |
| MX371331B (es) | 2012-04-24 | 2020-01-27 | Vertex Pharma | Inhibidores de la proteina cinasa dependiente de acido desoxirribonucleico(adn-pk). |
| ME03336B (me) | 2013-03-12 | 2019-10-20 | Vertex Pharma | Inhibitori dnk-pk |
| JP6408569B2 (ja) | 2013-10-17 | 2018-10-17 | バーテックス ファーマシューティカルズ インコーポレイテッドＶｅｒｔｅｘ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ Ｉｎｃｏｒｐｏｒａｔｅｄ | Ｄｎａ−ｐｋ阻害剤としての（ｓ）−ｎ−メチル−８−（１−（（２’−メチル−［４，５’−ビピリミジン］−６−イル）アミノ）プロパン−２−イル）キノリン−４−カルボキサミドおよびその重水素化誘導体の共結晶 |
| EP3518931A4 (en) | 2016-09-27 | 2020-05-13 | Vertex Pharmaceuticals Incorporated | METHOD FOR TREATING CANCER WITH A COMBINATION OF DNA-DAMAGING SUBSTANCES AND DNA-PK INHIBITORS |
| EP4011873A1 (en) | 2020-12-10 | 2022-06-15 | Bayer Aktiengesellschaft | Substituted pyrazolo piperidine carboxylic acids |
Family Cites Families (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DOP1981004033A (es) | 1980-12-23 | 1990-12-29 | Ciba Geigy Ag | Procedimiento para proteger plantas de cultivo de la accion fitotoxica de herbicidas. |
| EP0136976A3 (de) | 1983-08-23 | 1985-05-15 | Ciba-Geigy Ag | Verwendung von Phenylpyrimidinen als Pflanzenregulatoren |
| JPS63227879A (ja) * | 1987-02-27 | 1988-09-22 | チバーガイギ アクチエンゲゼルシヤルト | ポリエステル繊維材料染色物の光化学的安定性を向上させる方法 |
| JPH02149566A (ja) * | 1988-08-10 | 1990-06-08 | Sumitomo Chem Co Ltd | ４―置換―２，６―ジフェニルピリミジン誘導体、その製造法およびそれを有効成分とする除草剤 |
| JPH0449279A (ja) * | 1990-06-15 | 1992-02-18 | Nippon Bayeragrochem Kk | 除草性２，４，６―トリ置換芳香族ヘテロ環類 |
| KR930702312A (ko) * | 1990-08-31 | 1993-09-08 | 아만 히데아키 | 피리미딘 유도체 및 의약 |
| DE4034762A1 (de) * | 1990-11-02 | 1992-05-07 | Hoechst Ag | Pyridylpyrimidine, verfahren zu ihrer herstellung, sie enthaltende mittel und ihre verwendung als fungizide |
| JPH06192252A (ja) * | 1992-09-22 | 1994-07-12 | Nissan Chem Ind Ltd | ピラジン誘導体および除草剤 |
| GB2338957B (en) | 1997-02-19 | 2001-08-01 | Berlex Lab | N-heterocyclic derivatives as nos inhibitors |
| DE19744027A1 (de) | 1997-10-06 | 1999-04-08 | Hoechst Marion Roussel De Gmbh | Substituierte Pyrazolo[3,4-b]pyridine, ihre Herstellung und Verwendung in Arzneimitteln |
| DE19744026A1 (de) | 1997-10-06 | 1999-04-08 | Hoechst Marion Roussel De Gmbh | Pyrazol-Derivate, ihre Herstellung und ihre Verwendung in Arzneimitteln |
| DE19756388A1 (de) * | 1997-12-18 | 1999-06-24 | Hoechst Marion Roussel De Gmbh | Substituierte 2-Aryl-4-amino-chinazoline |
-
1998
- 1998-08-13 DE DE19836697A patent/DE19836697A1/de not_active Withdrawn
-
1999
- 1999-08-04 EP EP99944330A patent/EP1112266B1/de not_active Expired - Lifetime
- 1999-08-04 PT PT99944330T patent/PT1112266E/pt unknown
- 1999-08-04 DE DE59905572T patent/DE59905572D1/de not_active Expired - Lifetime
- 1999-08-04 DK DK99944330T patent/DK1112266T3/da active
- 1999-08-04 WO PCT/EP1999/005636 patent/WO2000009496A1/de not_active Ceased
- 1999-08-04 JP JP2000564948A patent/JP4594526B2/ja not_active Expired - Fee Related
- 1999-08-04 AT AT99944330T patent/ATE240315T1/de active
- 1999-08-04 CA CA002340405A patent/CA2340405C/en not_active Expired - Fee Related
- 1999-08-04 US US09/762,893 patent/US6844347B1/en not_active Expired - Lifetime
- 1999-08-04 AU AU57307/99A patent/AU760988B2/en not_active Ceased
- 1999-08-04 ES ES99944330T patent/ES2196849T3/es not_active Expired - Lifetime
- 1999-08-04 KR KR1020017001840A patent/KR100971093B1/ko not_active Expired - Fee Related
- 1999-08-04 BR BRPI9913003-3A patent/BR9913003B1/pt not_active IP Right Cessation
- 1999-08-11 AR ARP990104022A patent/AR020165A1/es active IP Right Grant
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