JP2002530385A5 - - Google Patents
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- Publication number
- JP2002530385A5 JP2002530385A5 JP2000583875A JP2000583875A JP2002530385A5 JP 2002530385 A5 JP2002530385 A5 JP 2002530385A5 JP 2000583875 A JP2000583875 A JP 2000583875A JP 2000583875 A JP2000583875 A JP 2000583875A JP 2002530385 A5 JP2002530385 A5 JP 2002530385A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- substituted
- group
- hydroxyl
- different substituents
- 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 33
- 125000001424 substituent group Chemical group 0.000 description 16
- 125000002887 hydroxy group Chemical group [H]O* 0.000 description 13
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 description 10
- 150000003839 salts Chemical class 0.000 description 9
- 150000001875 compounds Chemical class 0.000 description 8
- 229910052739 hydrogen Inorganic materials 0.000 description 7
- 239000001257 hydrogen Substances 0.000 description 7
- 125000001624 naphthyl group Chemical group 0.000 description 7
- 125000000229 (C1-C4)alkoxy group Chemical group 0.000 description 6
- 239000000203 mixture Substances 0.000 description 6
- 229910052757 nitrogen Inorganic materials 0.000 description 6
- 125000003118 aryl group Chemical group 0.000 description 5
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 description 5
- CYRMSUTZVYGINF-UHFFFAOYSA-N trichlorofluoromethane Chemical group FC(Cl)(Cl)Cl CYRMSUTZVYGINF-UHFFFAOYSA-N 0.000 description 5
- 125000000217 alkyl group Chemical group 0.000 description 4
- 125000000623 heterocyclic group Chemical group 0.000 description 4
- 125000004209 (C1-C8) alkyl group Chemical group 0.000 description 3
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 description 3
- 125000004435 hydrogen atom Chemical group [H]* 0.000 description 3
- 125000004433 nitrogen atom Chemical group N* 0.000 description 3
- 229910052717 sulfur Inorganic materials 0.000 description 3
- -1 Aryl halogen Chemical class 0.000 description 2
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 description 2
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 description 2
- 229910052736 halogen Inorganic materials 0.000 description 2
- 125000001072 heteroaryl group Chemical group 0.000 description 2
- 150000002431 hydrogen Chemical class 0.000 description 2
- 229910052760 oxygen Inorganic materials 0.000 description 2
- 125000004076 pyridyl group Chemical group 0.000 description 2
- 125000006763 (C3-C9) cycloalkyl 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
- 125000003545 alkoxy 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
- 125000004429 atom Chemical group 0.000 description 1
- 125000002619 bicyclic 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
- 125000000753 cycloalkyl group Chemical group 0.000 description 1
- 239000003814 drug Substances 0.000 description 1
- 239000003937 drug carrier Substances 0.000 description 1
- 230000008694 endothelial dysfunction Effects 0.000 description 1
- 150000002367 halogens Chemical class 0.000 description 1
- 125000005842 heteroatom Chemical group 0.000 description 1
- 201000001881 impotence Diseases 0.000 description 1
- 208000030603 inherited susceptibility to asthma Diseases 0.000 description 1
- 230000028252 learning or memory Effects 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
- 125000004430 oxygen atom Chemical group O* 0.000 description 1
- 239000000825 pharmaceutical preparation Substances 0.000 description 1
- 230000001766 physiological effect Effects 0.000 description 1
- 230000002265 prevention Effects 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
- 125000005505 thiomorpholino group Chemical group 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| DE19853278.4 | 1998-11-19 | ||
| DE19853278A DE19853278A1 (de) | 1998-11-19 | 1998-11-19 | Substituierte 4-Amino-2-aryl-cyclopenta[d]pyrimidine, ihre Herstellung, ihre Verwendung und sie enthaltende pharmazeutische Präparate |
| PCT/EP1999/008382 WO2000031047A1 (de) | 1998-11-19 | 1999-11-03 | Substituierte 4-amino-2-aryl-cyclopenta[d]pyrimidine, ihre herstellung, ihre verwendung und sie enthaltende pharmazeutische präparate |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2002530385A JP2002530385A (ja) | 2002-09-17 |
| JP2002530385A5 true JP2002530385A5 (enExample) | 2006-12-14 |
| JP4695262B2 JP4695262B2 (ja) | 2011-06-08 |
Family
ID=7888276
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2000583875A Expired - Fee Related JP4695262B2 (ja) | 1998-11-19 | 1999-11-03 | 置換４−アミノ−２−アリールシクロペンタ［ｄ］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 (10)
| Country | Link |
|---|---|
| US (2) | US6627628B1 (enExample) |
| EP (1) | EP1131302B1 (enExample) |
| JP (1) | JP4695262B2 (enExample) |
| AT (1) | ATE316964T1 (enExample) |
| AU (1) | AU1159400A (enExample) |
| CA (1) | CA2351488C (enExample) |
| DE (2) | DE19853278A1 (enExample) |
| ES (1) | ES2257103T3 (enExample) |
| PT (1) | PT1131302E (enExample) |
| WO (1) | WO2000031047A1 (enExample) |
Families Citing this family (24)
| 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 |
| US7031977B2 (en) * | 2002-02-28 | 2006-04-18 | Plumtree Software, Inc. | Efficiently storing indented threads in a threaded discussion application |
| AU2003288994A1 (en) * | 2002-12-10 | 2004-06-30 | Ono Pharmaceutical Co., Ltd. | Nitrogen-containing heterocyclic compounds and medicinal use thereof |
| AR045445A1 (es) * | 2003-08-05 | 2005-10-26 | Vertex Pharma | Compuestos ihinibidores de canales ionicos regulados por voltaje |
| ATE497949T1 (de) | 2003-12-03 | 2011-02-15 | Ym Biosciences Australia Pty | Tubulininhibitoren |
| TW200621257A (en) * | 2004-10-20 | 2006-07-01 | Astellas Pharma Inc | Pyrimidine derivative fused with nonaromatic ring |
| PL2049500T3 (pl) * | 2006-07-06 | 2012-02-29 | Array Biopharma Inc | Cyklopenta[d]pirymidyny jako inhibitory kinaz białkowych AKT |
| US8063050B2 (en) * | 2006-07-06 | 2011-11-22 | Array Biopharma Inc. | Hydroxylated and methoxylated pyrimidyl cyclopentanes as AKT protein kinase inhibitors |
| WO2008006025A1 (en) | 2006-07-06 | 2008-01-10 | Array Biopharma Inc. | Dihydrofuro pyrimidines as akt protein kinase inhibitors |
| WO2008006039A1 (en) | 2006-07-06 | 2008-01-10 | Array Biopharma Inc. | Dihydrothieno pyrimidines as akt protein kinase inhibitors |
| US9409886B2 (en) | 2007-07-05 | 2016-08-09 | Array Biopharma Inc. | Pyrimidyl cyclopentanes as AKT protein kinase inhibitors |
| BRPI0813999A2 (pt) | 2007-07-05 | 2019-10-01 | Array Biopharma Inc | ciclopentanos de pirimidil como inibidores de akt proteína cinase |
| US8846683B2 (en) | 2007-07-05 | 2014-09-30 | Array Biopharma, Inc. | Pyrimidyl cyclopentanes as Akt protein kinase inhibitors |
| EP2404907B1 (en) * | 2007-07-05 | 2015-01-14 | Array Biopharma, Inc. | Pyrimidyl cyclopentanes as AKT protein kinase inhibitors |
| JP5608097B2 (ja) | 2008-01-08 | 2014-10-15 | アレイ バイオファーマ、インコーポレイテッド | キナーゼ阻害薬としてのピロロピリジン |
| KR101624753B1 (ko) * | 2008-01-09 | 2016-05-26 | 어레이 바이오파마 인크. | Ａｋｔ 단백질 키나제 저해물질로서의 수산화된 피리미딜 시클로펜탄 |
| US8372842B2 (en) | 2008-01-09 | 2013-02-12 | Array Biopharma Inc. | Pyrazolopyridines as kinase inhibitors |
| AU2009204019B2 (en) | 2008-01-09 | 2014-02-20 | Array Biopharma Inc. | Hydroxylated pyrimidyl cyclopentane as AKT protein kinase inhibitor |
| BR112013025397A2 (pt) | 2011-04-01 | 2019-09-24 | Deepak Sampath | combinação de um composto, composto de fórmula i ou um sal farmaceuticamente aceitável do mesmo, uso, kit, produto, método para tratamento de um distúrbio hiperproliferativo e método para tratamento de uma doença ou afecção modulada por quinase akt em um mamífero |
| CA2831922C (en) | 2011-04-01 | 2019-12-31 | Genentech, Inc. | Combinations of akt inhibitor compounds and vemurafenib, and methods of use |
| JP2016504365A (ja) * | 2012-12-28 | 2016-02-12 | アメリカ合衆国 | Ｕｓｐ１／ｕａｆ１デユビキチナーゼ複合体阻害剤及びその使用 |
| EP4011873A1 (en) | 2020-12-10 | 2022-06-15 | Bayer Aktiengesellschaft | Substituted pyrazolo piperidine carboxylic acids |
| CN113880859B (zh) * | 2021-11-16 | 2022-06-21 | 江西科技师范大学 | 2-芳基-4-芳甲胺基嘧啶类化合物及其应用 |
Family Cites Families (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3346452A (en) | 1963-08-19 | 1967-10-10 | Ciba Geigy Corp | 5, 6-lower alkylene-pyrimidines |
| DE4029654A1 (de) * | 1990-09-19 | 1992-04-02 | Hoechst Ag | 2-phenyl-pyrimidine, verfahren zu ihrer herstellung, sie enthaltende mittel und ihre verwendung als fungizide |
| JP2928079B2 (ja) | 1994-02-14 | 1999-07-28 | 永信薬品工業股▲ふん▼有限公司 | １−（置換ベンジル）−３−（置換アリール）縮合ピラゾール類、その製造法及びその用途 |
| JPH07228573A (ja) | 1994-02-16 | 1995-08-29 | Dainippon Pharmaceut Co Ltd | ２−フェニルシクロアルカノピリミジン誘導体 |
| IL117659A (en) | 1995-04-13 | 2000-12-06 | Dainippon Pharmaceutical Co | Substituted 2-phenyl pyrimidino amino acetamide derivative process for preparing the same and a pharmaceutical composition containing same |
| AU2980797A (en) | 1996-06-11 | 1998-01-07 | Yoshitomi Pharmaceutical Industries, Ltd. | Fused heterocyclic compounds and medicinal uses thereof |
| DE19642255A1 (de) | 1996-10-14 | 1998-04-16 | Bayer Ag | Verwendung von 1-Benzyl-3-(substituierten-hetaryl) -kondensierten Pyrazol-Derivaten |
| ES2325045T3 (es) | 1996-10-14 | 2009-08-24 | Bayer Healthcare Ag | Nuevos derivados de pirazol heterociclilmetil sustituidos y su uso en el tratamiento de enfermedades cardiovasculares. |
| DE19836697A1 (de) | 1998-08-13 | 2000-02-17 | Hoechst Marion Roussel De Gmbh | Substituierte 4-Amino-2-aryl-pyrimidine, ihre Herstellung, ihre Verwendung und sie enthaltende pharmazeutische Präparate |
| 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 |
-
1998
- 1998-11-19 DE DE19853278A patent/DE19853278A1/de not_active Withdrawn
-
1999
- 1999-11-03 CA CA002351488A patent/CA2351488C/en not_active Expired - Fee Related
- 1999-11-03 AU AU11594/00A patent/AU1159400A/en not_active Abandoned
- 1999-11-03 WO PCT/EP1999/008382 patent/WO2000031047A1/de not_active Ceased
- 1999-11-03 JP JP2000583875A patent/JP4695262B2/ja not_active Expired - Fee Related
- 1999-11-03 PT PT99972626T patent/PT1131302E/pt unknown
- 1999-11-03 ES ES99972626T patent/ES2257103T3/es not_active Expired - Lifetime
- 1999-11-03 US US09/856,069 patent/US6627628B1/en not_active Expired - Lifetime
- 1999-11-03 AT AT99972626T patent/ATE316964T1/de active
- 1999-11-03 EP EP99972626A patent/EP1131302B1/de not_active Expired - Lifetime
- 1999-11-03 DE DE59913103T patent/DE59913103D1/de not_active Expired - Lifetime
-
2003
- 2003-09-12 US US10/660,489 patent/US7138398B2/en not_active Expired - Lifetime
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