JP2010532386A5 - - Google Patents
Download PDFInfo
- Publication number
- JP2010532386A5 JP2010532386A5 JP2010515269A JP2010515269A JP2010532386A5 JP 2010532386 A5 JP2010532386 A5 JP 2010532386A5 JP 2010515269 A JP2010515269 A JP 2010515269A JP 2010515269 A JP2010515269 A JP 2010515269A JP 2010532386 A5 JP2010532386 A5 JP 2010532386A5
- Authority
- JP
- Japan
- Prior art keywords
- compound according
- alkyl
- compound
- formula
- fluoro
- 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
- 150000001875 compounds Chemical class 0.000 claims description 130
- -1 CH 2 F Chemical compound 0.000 claims description 65
- 125000000623 heterocyclic group Chemical group 0.000 claims description 22
- 125000004429 atom Chemical group 0.000 claims description 14
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 14
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 14
- GLUUGHFHXGJENI-UHFFFAOYSA-N Piperazine Chemical compound C1CNCCN1 GLUUGHFHXGJENI-UHFFFAOYSA-N 0.000 claims description 12
- RWRDLPDLKQPQOW-UHFFFAOYSA-N Pyrrolidine Chemical compound C1CCNC1 RWRDLPDLKQPQOW-UHFFFAOYSA-N 0.000 claims description 12
- 229910052799 carbon Inorganic materials 0.000 claims description 10
- 201000010099 disease Diseases 0.000 claims description 10
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 10
- 238000000034 method Methods 0.000 claims description 9
- UFWIBTONFRDIAS-UHFFFAOYSA-N Naphthalene Chemical compound C1=CC=CC2=CC=CC=C21 UFWIBTONFRDIAS-UHFFFAOYSA-N 0.000 claims description 8
- NQRYJNQNLNOLGT-UHFFFAOYSA-N Piperidine Chemical compound C1CCNCC1 NQRYJNQNLNOLGT-UHFFFAOYSA-N 0.000 claims description 8
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical group [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims description 8
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 8
- 125000004186 cyclopropylmethyl group Chemical group [H]C([H])(*)C1([H])C([H])([H])C1([H])[H] 0.000 claims description 8
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims description 8
- 230000001404 mediated effect Effects 0.000 claims description 8
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims description 8
- 239000008194 pharmaceutical composition Substances 0.000 claims description 8
- 150000003839 salts Chemical class 0.000 claims description 8
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 claims description 6
- 241000124008 Mammalia Species 0.000 claims description 6
- 229910052736 halogen Inorganic materials 0.000 claims description 6
- 125000004043 oxo group Chemical group O=* 0.000 claims description 6
- 125000003854 p-chlorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C([H])=C1Cl 0.000 claims description 6
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims description 4
- ICSNLGPSRYBMBD-UHFFFAOYSA-N 2-aminopyridine Chemical compound NC1=CC=CC=N1 ICSNLGPSRYBMBD-UHFFFAOYSA-N 0.000 claims description 4
- 125000004800 4-bromophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C([H])=C1Br 0.000 claims description 4
- 125000004801 4-cyanophenyl group Chemical group [H]C1=C([H])C(C#N)=C([H])C([H])=C1* 0.000 claims description 4
- 125000004199 4-trifluoromethylphenyl group Chemical group [H]C1=C([H])C(=C([H])C([H])=C1*)C(F)(F)F 0.000 claims description 4
- HBAQYPYDRFILMT-UHFFFAOYSA-N 8-[3-(1-cyclopropylpyrazol-4-yl)-1H-pyrazolo[4,3-d]pyrimidin-5-yl]-3-methyl-3,8-diazabicyclo[3.2.1]octan-2-one Chemical class C1(CC1)N1N=CC(=C1)C1=NNC2=C1N=C(N=C2)N1C2C(N(CC1CC2)C)=O HBAQYPYDRFILMT-UHFFFAOYSA-N 0.000 claims description 4
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims description 4
- JUJWROOIHBZHMG-UHFFFAOYSA-N Pyridine Chemical compound C1=CC=NC=C1 JUJWROOIHBZHMG-UHFFFAOYSA-N 0.000 claims description 4
- 208000035475 disorder Diseases 0.000 claims description 4
- 239000003814 drug Substances 0.000 claims description 4
- 150000002367 halogens Chemical class 0.000 claims description 4
- 125000005842 heteroatom Chemical group 0.000 claims description 4
- 238000004519 manufacturing process Methods 0.000 claims description 4
- 125000004201 2,4-dichlorophenyl group Chemical group [H]C1=C([H])C(*)=C(Cl)C([H])=C1Cl 0.000 claims description 2
- 125000004189 3,4-dichlorophenyl group Chemical group [H]C1=C([H])C(Cl)=C(Cl)C([H])=C1* 0.000 claims description 2
- 125000004179 3-chlorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C(Cl)=C1[H] 0.000 claims description 2
- 125000004180 3-fluorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C(F)=C1[H] 0.000 claims description 2
- 125000001255 4-fluorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C([H])=C1F 0.000 claims description 2
- 208000024172 Cardiovascular disease Diseases 0.000 claims description 2
- WTKZEGDFNFYCGP-UHFFFAOYSA-N Pyrazole Chemical compound C=1C=NNC=1 WTKZEGDFNFYCGP-UHFFFAOYSA-N 0.000 claims description 2
- 125000000319 biphenyl-4-yl group Chemical group [H]C1=C([H])C([H])=C([H])C([H])=C1C1=C([H])C([H])=C([*])C([H])=C1[H] 0.000 claims description 2
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 claims description 2
- 125000005843 halogen group Chemical group 0.000 claims description 2
- 230000003463 hyperproliferative effect Effects 0.000 claims description 2
- 208000027866 inflammatory disease Diseases 0.000 claims description 2
- 230000002401 inhibitory effect Effects 0.000 claims description 2
- 125000000959 isobutyl group Chemical group [H]C([H])([H])C([H])(C([H])([H])[H])C([H])([H])* 0.000 claims description 2
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims description 2
- MOZRQQTUYAYCQT-FQEVSTJZSA-N n-[[(3s)-3-amino-1-(5-ethyl-7h-pyrrolo[2,3-d]pyrimidin-4-yl)pyrrolidin-3-yl]methyl]-2,4-difluorobenzamide Chemical group C([C@]1(CCN(C1)C=1N=CN=C2NC=C(C=12)CC)N)NC(=O)C1=CC=C(F)C=C1F MOZRQQTUYAYCQT-FQEVSTJZSA-N 0.000 claims description 2
- 230000004770 neurodegeneration Effects 0.000 claims description 2
- 208000015122 neurodegenerative disease Diseases 0.000 claims description 2
- UMJSCPRVCHMLSP-UHFFFAOYSA-N pyridine Natural products COC1=CC=CN=C1 UMJSCPRVCHMLSP-UHFFFAOYSA-N 0.000 claims description 2
- 125000003944 tolyl group Chemical group 0.000 claims description 2
- 239000000203 mixture Substances 0.000 claims 5
- 125000006661 (C4-C6) heterocyclic group Chemical group 0.000 claims 1
- 125000000217 alkyl group Chemical group 0.000 description 12
- 0 C*C1(*)c2ncnc(N(CC3)C(*)CN3C(C(*)C3C(*)C*C(*)(*)*3)=O)c2C(*)(*)C1 Chemical compound C*C1(*)c2ncnc(N(CC3)C(*)CN3C(C(*)C3C(*)C*C(*)(*)*3)=O)c2C(*)(*)C1 0.000 description 4
- 125000006569 (C5-C6) heterocyclic group Chemical group 0.000 description 1
- 125000001412 tetrahydropyranyl group Chemical group 0.000 description 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US94813807P | 2007-07-05 | 2007-07-05 | |
| US60/948,138 | 2007-07-05 | ||
| US2008808P | 2008-01-09 | 2008-01-09 | |
| US61/020,088 | 2008-01-09 | ||
| PCT/US2008/069144 WO2009006567A2 (en) | 2007-07-05 | 2008-07-03 | Pyrimidyl cyclopentanes as akt protein kinase inhibitors |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2013207007A Division JP2014028842A (ja) | 2007-07-05 | 2013-10-02 | Ａｋｔプロテインキナーゼ阻害剤としてのピリミジルシクロペンタン |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2010532386A JP2010532386A (ja) | 2010-10-07 |
| JP2010532386A5 true JP2010532386A5 (https=) | 2012-07-26 |
| JP5628028B2 JP5628028B2 (ja) | 2014-11-19 |
Family
ID=40076864
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2010515269A Active JP5628028B2 (ja) | 2007-07-05 | 2008-07-03 | Ａｋｔプロテインキナーゼ阻害剤としてのピリミジルシクロペンタン |
| JP2013207007A Withdrawn JP2014028842A (ja) | 2007-07-05 | 2013-10-02 | Ａｋｔプロテインキナーゼ阻害剤としてのピリミジルシクロペンタン |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2013207007A Withdrawn JP2014028842A (ja) | 2007-07-05 | 2013-10-02 | Ａｋｔプロテインキナーゼ阻害剤としてのピリミジルシクロペンタン |
Country Status (19)
| Country | Link |
|---|---|
| US (1) | US8618097B2 (https=) |
| EP (1) | EP2170863B1 (https=) |
| JP (2) | JP5628028B2 (https=) |
| KR (2) | KR101650956B1 (https=) |
| CN (2) | CN103396409B (https=) |
| AR (1) | AR067413A1 (https=) |
| AU (1) | AU2008272830B8 (https=) |
| BR (1) | BRPI0813999A2 (https=) |
| CA (1) | CA2692502C (https=) |
| CO (1) | CO6251283A2 (https=) |
| CR (1) | CR11229A (https=) |
| EC (1) | ECSP109937A (https=) |
| ES (1) | ES2551352T3 (https=) |
| MA (1) | MA31679B1 (https=) |
| NZ (1) | NZ582692A (https=) |
| RU (1) | RU2486181C2 (https=) |
| SG (1) | SG185274A1 (https=) |
| TW (1) | TWI450720B (https=) |
| WO (1) | WO2009006567A2 (https=) |
Families Citing this family (35)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2008036540A2 (en) | 2006-09-20 | 2008-03-27 | Boehringer Ingelheim International Gmbh | Rho kinase inhibitors |
| US8455513B2 (en) | 2007-01-10 | 2013-06-04 | Aerie Pharmaceuticals, Inc. | 6-aminoisoquinoline compounds |
| US9409886B2 (en) | 2007-07-05 | 2016-08-09 | Array Biopharma Inc. | Pyrimidyl cyclopentanes as AKT protein kinase inhibitors |
| US8846683B2 (en) | 2007-07-05 | 2014-09-30 | Array Biopharma, Inc. | Pyrimidyl cyclopentanes as Akt protein kinase inhibitors |
| US8841304B2 (en) | 2008-01-08 | 2014-09-23 | Array Biopharma, Inc. | Pyrrolopyridines as kinase inhibitors |
| CA2711782C (en) | 2008-01-09 | 2017-01-03 | Array Biopharma Inc. | 5h-cyclopenta[d]pyrimidines as akt protein kinase inhibitors |
| CN102015708B (zh) * | 2008-01-09 | 2014-03-26 | 阵列生物制药公司 | 作为akt蛋白激酶抑制剂的嘧啶基环戊烷 |
| NZ586346A (en) | 2008-01-09 | 2012-02-24 | Array Biopharma Inc | Hydroxylated pyrimidyl cyclopentanes as akt protein kinase inhibitors |
| US8853216B2 (en) | 2008-01-09 | 2014-10-07 | Array Biopharma, Inc. | Hydroxylated pyrimidyl cyclopentane as AKT protein kinase inhibitor |
| CN101965347B (zh) | 2008-01-09 | 2013-01-02 | 阵列生物制药公司 | 作为激酶抑制剂的吡唑并吡啶 |
| US8450344B2 (en) | 2008-07-25 | 2013-05-28 | Aerie Pharmaceuticals, Inc. | Beta- and gamma-amino-isoquinoline amide compounds and substituted benzamide compounds |
| EP3053913B1 (en) | 2009-05-01 | 2018-03-07 | Aerie Pharmaceuticals, Inc. | Dual mechanism inhibitors for the treatment of disease |
| MX2012011887A (es) | 2010-04-16 | 2012-11-30 | Genentech Inc | Foxo 3a como biomarcador predictivo para la eficacia del inhibidor de la via de quinasa pi3k/akt. |
| EP3617330B1 (en) | 2011-04-01 | 2023-12-27 | Genentech, Inc. | Biomarkers for predicting sensitivity to cancer treatments |
| HRP20200992T1 (hr) | 2012-05-17 | 2020-10-16 | Genentech, Inc. | Amorfni oblik pirimidinil-ciklopentanskog spoja koji inhibira akt, te njegovi pripravci i postupci |
| JP6163205B2 (ja) | 2012-06-20 | 2017-07-12 | ノバルティス アーゲー | 補体経路モジュレーターおよびその使用 |
| CA2901126C (en) | 2013-02-25 | 2022-01-25 | Genentech, Inc. | Methods and compositions for detecting and treating drug resistant akt mutant |
| DK3811943T3 (da) | 2013-03-15 | 2023-04-03 | Aerie Pharmaceuticals Inc | Forbindelse til anvendelse til behandling af øjenlidelser |
| US9643927B1 (en) | 2015-11-17 | 2017-05-09 | Aerie Pharmaceuticals, Inc. | Process for the preparation of kinase inhibitors and intermediates thereof |
| US10550087B2 (en) | 2015-11-17 | 2020-02-04 | Aerie Pharmaceuticals, Inc. | Process for the preparation of kinase inhibitors and intermediates thereof |
| US10722484B2 (en) | 2016-03-09 | 2020-07-28 | K-Gen, Inc. | Methods of cancer treatment |
| AU2017281907B2 (en) | 2016-06-23 | 2021-10-21 | St. Jude Children's Research Hospital, Inc. | Small molecule modulators of pantothenate kinases |
| KR102568079B1 (ko) | 2016-08-31 | 2023-08-17 | 에어리 파마슈티컬즈, 인코포레이티드 | 안과용 조성물 |
| EP3532464A4 (en) | 2016-10-28 | 2020-07-08 | Icahn School of Medicine at Mount Sinai | COMPOSITIONS AND METHODS FOR THE TREATMENT OF EZH2 MEDIATION CANCER |
| KR20190135027A (ko) | 2017-03-31 | 2019-12-05 | 에어리 파마슈티컬즈, 인코포레이티드 | 아릴 시클로프로필-아미노-이소퀴놀리닐 아미드 화합물 |
| KR102728619B1 (ko) | 2017-12-27 | 2024-11-08 | 세인트 쥬드 칠드런즈 리써치 호스피탈, 인코포레이티드 | 판토테네이트 키나제의 소분자 조절제 |
| CA3092677A1 (en) * | 2018-03-06 | 2019-09-12 | Icahn School Of Medicine At Mount Sinai | Serine threonine kinase (akt) degradation / disruption compounds and methods of use |
| KR20210006356A (ko) * | 2018-04-04 | 2021-01-18 | 아비나스 오퍼레이션스, 인코포레이티드 | 단백질분해 조절제 및 연관된 사용 방법 |
| CA3104298A1 (en) | 2018-06-21 | 2019-12-26 | Icahn School Of Medicine At Mount Sinai | Wd40 repeat domain protein 5 (wdr5) degradation / disruption compounds and methods of use |
| AU2019337703B2 (en) | 2018-09-14 | 2023-02-02 | Aerie Pharmaceuticals, Inc. | Aryl cyclopropyl-amino-isoquinolinyl amide compounds |
| CA3135011A1 (en) * | 2019-03-27 | 2020-10-01 | St. Jude Children's Research Hospital | Small molecule modulators of pank |
| CN118908962A (zh) | 2019-05-06 | 2024-11-08 | 西奈山伊坎医学院 | 作为hpk1的降解剂的异双功能化合物 |
| US12103924B2 (en) | 2020-06-01 | 2024-10-01 | Icahn School Of Medicine At Mount Sinai | Mitogen-activated protein kinase kinase (MEK) degradation compounds and methods of use |
| CN117677614A (zh) * | 2021-12-17 | 2024-03-08 | 中国医药研究开发中心有限公司 | 具有akt激酶抑制活性的杂环化合物及其制备方法和医药用途 |
| CN121419983A (zh) | 2023-01-26 | 2026-01-27 | 阿尔维纳斯运营股份有限公司 | 基于小脑蛋白的kras降解protac及其相关用途 |
Family Cites Families (102)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3885035A (en) | 1972-04-05 | 1975-05-20 | Sandoz Ag | Method for treating arrhythmia by using 1,4-bis(4 quinazolinyl) piperazines |
| US3956495A (en) | 1973-10-30 | 1976-05-11 | Eli Lilly And Company | 2,4-Diaminoquinazolines as antithrombotic agents |
| US3966936A (en) | 1974-02-21 | 1976-06-29 | Pfizer Inc. | Piperazino quinazoline bronchodilators |
| US4060615A (en) | 1976-02-18 | 1977-11-29 | Mead Johnson & Company | 2-Piperazinyl-6,7-dimethoxyquinazolines |
| JPS562968A (en) | 1979-06-21 | 1981-01-13 | Mitsubishi Yuka Yakuhin Kk | Novel pyrimidine derivative |
| US4749704A (en) | 1985-03-07 | 1988-06-07 | Sankyo Company Limited | Cyclopenta[d]pyrimidine derivatives and use as antidepressants |
| MX19185A (es) | 1989-01-20 | 1993-12-01 | Pfizer | Procedimiento para preparar 3-(1,2,5,6-tretrahidropiridil)-pirrolopiridinas. |
| WO1994007890A1 (fr) | 1992-10-05 | 1994-04-14 | Ube Industries, Ltd. | Compose pyrimidine |
| WO1995003286A1 (en) | 1993-07-23 | 1995-02-02 | The Green Cross Corporation | Triazole derivative and pharmaceutical use thereof |
| GB9416189D0 (en) | 1994-08-10 | 1994-09-28 | Merck Sharp & Dohme | Therapeutic agents |
| JP2896532B2 (ja) | 1994-08-13 | 1999-05-31 | ユーハン コーポレーション | 新規なピリミジン誘導体およびその製造方法 |
| US5525625A (en) | 1995-01-24 | 1996-06-11 | Warner-Lambert Company | 2-(2-Amino-3-methoxyphenyl)-4-oxo-4H-[1]benzopyran for treating proliferative disorders |
| US7125880B1 (en) | 1995-06-06 | 2006-10-24 | Pfizer Inc. | Corticotropin releasing factor antagonists |
| ZA979961B (en) | 1996-11-15 | 1999-05-05 | Lilly Co Eli | 5-HT1F agonists |
| UA73073C2 (uk) | 1997-04-03 | 2005-06-15 | Уайт Холдінгз Корпорейшн | Заміщені 3-ціанохіноліни, спосіб їх одержання та фармацевтична композиція |
| NZ501276A (en) | 1997-07-01 | 2000-10-27 | Warner Lambert Co | 4-bromo or 4-iodo phenylamino benzhydroxamic acid derivatives and their use as MEK inhibitors in treating proliferative disorders |
| CA2290509A1 (en) | 1997-07-01 | 1999-01-14 | Warner-Lambert Company | 2-(4-bromo or 4-iodo phenylamino) benzoic acid derivatives and their use as mek inhibitors |
| US6310060B1 (en) | 1998-06-24 | 2001-10-30 | Warner-Lambert Company | 2-(4-bromo or 4-iodo phenylamino) benzoic acid derivatives and their use as MEK inhibitors |
| US6821963B2 (en) | 1997-07-01 | 2004-11-23 | Warner-Lambert Company | 4-Bromo or 4-iodo phenylamino benzhydroxamic acid derivatives and their use as MEK inhibitors |
| US6506798B1 (en) | 1997-07-01 | 2003-01-14 | Warner-Lambert Company | 4-Arylamino, 4-aryloxy, and 4-arylthio diarylamines and derivatives thereof as selective MEK inhibitors |
| DE69943144D1 (de) | 1998-03-31 | 2011-03-03 | Kyowa Hakko Kirin Co Ltd | Stickstoffenthaltende heterocyclische verbindungen |
| 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 |
| AU2203800A (en) | 1999-01-07 | 2000-07-24 | Warner-Lambert Company | Antiviral method using mek inhibitors |
| JP2002534380A (ja) | 1999-01-07 | 2002-10-15 | ワーナー−ランバート・カンパニー | Ｍｅｋ阻害剤による喘息の治療 |
| CA2348236A1 (en) | 1999-01-13 | 2000-07-20 | Stephen Douglas Barrett | 4-arylamino, 4-aryloxy, and 4-arylthio diarylamines and derivatives thereof as selective mek inhibitors |
| CA2355470C (en) | 1999-01-13 | 2008-09-30 | Warner-Lambert Company | Benzoheterocycles and their use as mek inhibitors |
| EP1144372B1 (en) | 1999-01-13 | 2005-11-30 | Warner-Lambert Company Llc | Sulphohydroxamic acids and sulphohydroxamates and their use as mek inhibitors |
| CA2349832A1 (en) | 1999-01-13 | 2000-07-20 | Warner-Lambert Company | Benzenesulfonamide derivatives and their use as mek inhibitors |
| HUP0105092A3 (en) | 1999-01-13 | 2003-12-29 | Warner Lambert Co | 1-heterocycle substituted diarylamines and medicaments containing them |
| EP1150950A2 (en) | 1999-01-13 | 2001-11-07 | Warner-Lambert Company | Anthranilic acid derivatives |
| GB9910577D0 (en) | 1999-05-08 | 1999-07-07 | Zeneca Ltd | Chemical compounds |
| EP1202732A2 (en) | 1999-07-16 | 2002-05-08 | Warner-Lambert Company Llc | Method for treating chronic pain using mek inhibitors |
| CA2377092A1 (en) | 1999-07-16 | 2001-01-25 | Warner-Lambert Company | Method for treating chronic pain using mek inhibitors |
| JP2003504401A (ja) | 1999-07-16 | 2003-02-04 | ワーナー−ランバート・カンパニー | Ｍｅｋ阻害剤を用いる慢性疼痛の治療方法 |
| JP2003504400A (ja) | 1999-07-16 | 2003-02-04 | ワーナー−ランバート・カンパニー | Ｍｅｋ阻害剤を用いた慢性痛の治療方法 |
| BR0109188A (pt) | 2000-03-15 | 2003-03-18 | Warner Lambert Co | Diarilaminas 5-amida substituìdas como inibidores de mex |
| DZ3401A1 (fr) | 2000-07-19 | 2002-01-24 | Warner Lambert Co | Esters oxygenes d'acides 4-iodophenylamino benzhydroxamiques |
| KR20030059115A (ko) | 2000-08-25 | 2003-07-07 | 워너-램버트 캄파니 엘엘씨 | Ｎ-아릴-안트라닐산 및 그의 유도체의 제조 방법 |
| EP1317450B1 (en) * | 2000-09-15 | 2006-11-22 | Vertex Pharmaceuticals Incorporated | Pyrazole compounds useful as protein kinase inhibitors |
| EP1337524A1 (en) | 2000-11-02 | 2003-08-27 | AstraZeneca AB | Substituted quinolines as antitumor agents |
| WO2002083139A1 (en) | 2001-04-10 | 2002-10-24 | Merck & Co., Inc. | Inhibitors of akt activity |
| IL158062A0 (en) | 2001-04-30 | 2004-03-28 | Glaxo Group Ltd | Fused pyrimidines as antagonists of the corticotropin releasing factor (crf) |
| AU2002336462A1 (en) | 2001-09-06 | 2003-03-24 | Millennium Pharmaceuticals, Inc. | Piperazine and homopiperazine compounds |
| US20030187026A1 (en) | 2001-12-13 | 2003-10-02 | Qun Li | Kinase inhibitors |
| TW200306819A (en) | 2002-01-25 | 2003-12-01 | Vertex Pharma | Indazole compounds useful as protein kinase inhibitors |
| US7235537B2 (en) | 2002-03-13 | 2007-06-26 | Array Biopharma, Inc. | N3 alkylated benzimidazole derivatives as MEK inhibitors |
| SG2013013339A (en) | 2002-03-13 | 2014-12-30 | Array Biopharma Inc | N3 alkylated benzimidazole derivatives as mek inhibitors |
| EP1482944A4 (en) | 2002-03-13 | 2006-04-19 | Array Biopharma Inc | NZ ALKYL BENZIMIDAZOLE DERIVATIVES AS MEK INHIBITORS |
| CA2481241C (en) | 2002-04-08 | 2010-07-27 | Merck & Co., Inc. | Fused quinoxaline derivatives as inhibitors of akt activity |
| US7223738B2 (en) | 2002-04-08 | 2007-05-29 | Merck & Co., Inc. | Inhibitors of Akt activity |
| EP1494675A4 (en) | 2002-04-08 | 2006-07-19 | Merck & Co Inc | HEMMER OF ACT ACTIVITY |
| CA2480880C (en) | 2002-04-08 | 2011-03-22 | Merck & Co., Inc. | Inhibitors of akt activity |
| JP2005534632A (ja) | 2002-05-10 | 2005-11-17 | ニューロクライン バイオサイエンセズ， インコーポレイテッド | メラノコルチンレセプターリガンドとしての置換ピペラジン |
| US20040102360A1 (en) | 2002-10-30 | 2004-05-27 | Barnett Stanley F. | Combination therapy |
| JP2006507299A (ja) | 2002-10-30 | 2006-03-02 | メルク エンド カムパニー インコーポレーテッド | Ａｋｔ活性の阻害薬 |
| GB0308208D0 (en) | 2003-04-09 | 2003-05-14 | Glaxo Group Ltd | Chemical compounds |
| EP1620095A4 (en) | 2003-04-24 | 2009-04-01 | Merck & Co Inc | HEMMER OF ACT ACTIVITY |
| DE602004022819D1 (de) | 2003-06-06 | 2009-10-08 | Vertex Pharma | Von atp-bindende kassette transportern |
| ZA200601859B (en) | 2003-08-05 | 2008-03-26 | Vertex Pharma | Condensed pyrimidine compounds as inhibitors of voltagegated ion channels |
| JP2007501821A (ja) | 2003-08-12 | 2007-02-01 | エフ．ホフマン−ラ ロシュ アーゲー | Ｃｆｒアンタゴニストとしてのテトラヒドロキナゾリン誘導体 |
| MXPA06002618A (es) | 2003-09-09 | 2006-06-05 | Ono Pharmaceutical Co | Antagonistas del factor de liberacion de corticotropina (crf) y compuestos heterobiciclicos. |
| US20050182061A1 (en) | 2003-10-02 | 2005-08-18 | Jeremy Green | Phthalimide compounds useful as protein kinase inhibitors |
| CA2546754A1 (en) * | 2003-11-21 | 2005-06-09 | Array Biopharma Inc. | Akt protein kinase inhibitors |
| WO2005117909A2 (en) | 2004-04-23 | 2005-12-15 | Exelixis, Inc. | Kinase modulators and methods of use |
| WO2005113762A1 (en) | 2004-05-18 | 2005-12-01 | Pfizer Products Inc. | CRYSTAL STRUCTURE OF PROTEIN KINASE B-α (AKT-1) AND USES THEREOF |
| US20060025074A1 (en) | 2004-07-30 | 2006-02-02 | Chih-Ming Liang | Bluetooth-based headset |
| US7521457B2 (en) | 2004-08-20 | 2009-04-21 | Boehringer Ingelheim International Gmbh | Pyrimidines as PLK inhibitors |
| GB0419161D0 (en) | 2004-08-27 | 2004-09-29 | Novartis Ag | Organic compounds |
| TWM266655U (en) | 2004-09-23 | 2005-06-01 | Blueexpert Technology Corp | Bluetooth earphone device capable of wirelessly receiving and transmitting stereo sound signal and digital information signal |
| TW200621257A (en) * | 2004-10-20 | 2006-07-01 | Astellas Pharma Inc | Pyrimidine derivative fused with nonaromatic ring |
| UY29177A1 (es) | 2004-10-25 | 2006-05-31 | Astex Therapeutics Ltd | Derivados sustituidos de purina, purinona y deazapurina, composiciones que los contienen métodos para su preparación y sus usos |
| CA2590961C (en) * | 2004-12-28 | 2013-11-26 | Exelixis, Inc. | [1h-pyrazolo[3,4-d]pyrimidin-4-yl]-piperidine or -piperazine compounds as serine-threonine kinase modulators (p70s6k, atk1 and atk2) for the treatment of immunological, inflammatory and proliferative diseases |
| US20090111805A1 (en) | 2005-02-24 | 2009-04-30 | Pfizer Inc. | Bicyclic heteroaromatic derivatives useful as anticancer agents |
| US20090029982A1 (en) * | 2005-04-28 | 2009-01-29 | Supergen, Inc. | Protein kinase inhibitors |
| WO2006127587A1 (en) | 2005-05-20 | 2006-11-30 | Vertex Pharmaceuticals Incorporated | Pyrrolopyridines useful as inhibitors of protein kinase |
| US8008317B2 (en) | 2005-06-10 | 2011-08-30 | Merck Sharp & Dohme Corp. | Inhibitors of akt activtiy |
| UY29610A1 (es) | 2005-06-21 | 2007-01-31 | Cancer Rec Tech Ltd | Aril-alquilaminas y heteroaril-alquilaminas como inhibidores de la quinasa proteínica |
| WO2007042298A1 (en) | 2005-10-13 | 2007-04-19 | Glaxo Group Limited | Pyrrolopyrimidine derivatives as syk inhibitors |
| CA2635541A1 (en) | 2005-12-28 | 2007-07-12 | Takeda Pharmaceutical Company Limited | Fused heterocyclic compounds and their use as mineralocorticoid receptor ligands |
| JP2009534454A (ja) | 2006-04-25 | 2009-09-24 | アステックス、セラピューティックス、リミテッド | 医薬化合物 |
| RU2008152171A (ru) | 2006-07-05 | 2010-08-10 | Интермьюн, Инк. (Us) | Новые ингибиторы вирусной репликации гепатита с |
| GB0613518D0 (en) | 2006-07-06 | 2006-08-16 | Phytopharm Plc | Chemical compounds |
| US8063050B2 (en) * | 2006-07-06 | 2011-11-22 | Array Biopharma Inc. | Hydroxylated and methoxylated pyrimidyl cyclopentanes as AKT protein kinase inhibitors |
| US8329701B2 (en) * | 2006-07-06 | 2012-12-11 | Array Biopharma Inc. | Dihydrofuro pyrimidines as AKT protein kinase inhibitors |
| EP2049500B1 (en) | 2006-07-06 | 2011-09-07 | Array Biopharma, Inc. | Cyclopenta [d] pyrimidines as akt protein kinase inhibitors |
| US7910747B2 (en) | 2006-07-06 | 2011-03-22 | Bristol-Myers Squibb Company | Phosphonate and phosphinate pyrazolylamide glucokinase activators |
| CA2655675A1 (en) | 2006-07-06 | 2008-01-10 | Glaxo Group Limited | Substituted n-phenylmethyl -5-oxo-proline-2-amides as p2x7-receptor antagonists and their methods of use |
| UA95641C2 (xx) | 2006-07-06 | 2011-08-25 | Эррей Биофарма Инк. | Гідроксильовані піримідильні циклопентани як інгібітори акт протеїнкінази$гидроксилированные пиримидильные циклопентаны как ингибиторы акт протеинкиназы |
| WO2008012635A2 (en) | 2006-07-26 | 2008-01-31 | Pfizer Products Inc. | Amine derivatives useful as anticancer agents |
| US8329159B2 (en) * | 2006-08-11 | 2012-12-11 | Bristol-Myers Squibb Company | Hepatitis C virus inhibitors |
| US7659270B2 (en) * | 2006-08-11 | 2010-02-09 | Bristol-Myers Squibb Company | Hepatitis C virus inhibitors |
| JP5228912B2 (ja) * | 2006-09-08 | 2013-07-03 | 三菱瓦斯化学株式会社 | 高血圧改善剤 |
| US7741347B2 (en) * | 2007-05-17 | 2010-06-22 | Bristol-Myers Squibb Company | Hepatitis C virus inhibitors |
| CN101918373B (zh) * | 2007-07-05 | 2013-06-05 | 阵列生物制药公司 | 作为akt蛋白激酶抑制剂的嘧啶基环戊烷 |
| US8629171B2 (en) * | 2007-08-08 | 2014-01-14 | Bristol-Myers Squibb Company | Crystalline form of methyl ((1S)-1-((25)-2-(5-(4'-(2-((25)-1((2S)-2-((methoxycarbonyl)amino)-3-methylbutanoyl)-2-pyrrolidinyl)-1H-imidazol-2-yl)-1-pyrrolidinyl)carbonyl)-2-methylpropyl)carbamate dihydrochloride salt |
| US8853216B2 (en) * | 2008-01-09 | 2014-10-07 | Array Biopharma, Inc. | Hydroxylated pyrimidyl cyclopentane as AKT protein kinase inhibitor |
| CA2711782C (en) * | 2008-01-09 | 2017-01-03 | Array Biopharma Inc. | 5h-cyclopenta[d]pyrimidines as akt protein kinase inhibitors |
| NZ586346A (en) * | 2008-01-09 | 2012-02-24 | Array Biopharma Inc | Hydroxylated pyrimidyl cyclopentanes as akt protein kinase inhibitors |
| US7704992B2 (en) * | 2008-02-13 | 2010-04-27 | Bristol-Myers Squibb Company | Hepatitis C virus inhibitors |
| US7906655B2 (en) * | 2008-08-07 | 2011-03-15 | Bristol-Myers Squibb Company | Hepatitis C virus inhibitors |
| WO2010096462A1 (en) * | 2009-02-17 | 2010-08-26 | Enanta Pharmaceuticals, Inc | Linked diimidazole derivatives |
| PT3309157T (pt) * | 2009-05-13 | 2019-12-02 | Gilead Pharmasset Llc | Compostos antivirais |
-
2008
- 2008-07-03 CN CN201310128477.3A patent/CN103396409B/zh active Active
- 2008-07-03 CA CA2692502A patent/CA2692502C/en not_active Expired - Fee Related
- 2008-07-03 RU RU2010103813/04A patent/RU2486181C2/ru active
- 2008-07-03 ES ES08781337.4T patent/ES2551352T3/es active Active
- 2008-07-03 BR BRPI0813999A patent/BRPI0813999A2/pt not_active Application Discontinuation
- 2008-07-03 TW TW097125055A patent/TWI450720B/zh not_active IP Right Cessation
- 2008-07-03 JP JP2010515269A patent/JP5628028B2/ja active Active
- 2008-07-03 WO PCT/US2008/069144 patent/WO2009006567A2/en not_active Ceased
- 2008-07-03 KR KR1020107002558A patent/KR101650956B1/ko not_active Expired - Fee Related
- 2008-07-03 US US12/667,848 patent/US8618097B2/en active Active
- 2008-07-03 AU AU2008272830A patent/AU2008272830B8/en not_active Ceased
- 2008-07-03 KR KR1020157020046A patent/KR20150089099A/ko not_active Ceased
- 2008-07-03 SG SG2012073854A patent/SG185274A1/en unknown
- 2008-07-03 AR ARP080102885A patent/AR067413A1/es unknown
- 2008-07-03 NZ NZ582692A patent/NZ582692A/en not_active IP Right Cessation
- 2008-07-03 CN CN2008801058695A patent/CN101801955B/zh active Active
- 2008-07-03 EP EP08781337.4A patent/EP2170863B1/en active Active
-
2010
- 2010-01-19 CR CR11229A patent/CR11229A/es unknown
- 2010-01-29 CO CO10009431A patent/CO6251283A2/es active IP Right Grant
- 2010-02-04 EC EC2010009937A patent/ECSP109937A/es unknown
- 2010-02-05 MA MA32596A patent/MA31679B1/fr unknown
-
2013
- 2013-10-02 JP JP2013207007A patent/JP2014028842A/ja not_active Withdrawn
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| JP2010532386A5 (https=) | ||
| RU2486181C2 (ru) | Пиримидилциклопентаны как ингибиторы акт-протеинкиназ | |
| JP2011509309A5 (https=) | ||
| RU2455288C2 (ru) | Соединения и композиции 5-(4-(галогеналкокси)фенил)пиримидин-2-амина в качестве ингибиторов киназ | |
| RU2500673C2 (ru) | Гетероциклические ингибиторы мек и способы их применения | |
| JP2020033357A5 (https=) | ||
| TWI579284B (zh) | 咪唑并吡咯啶酮化合物 | |
| RU2477723C2 (ru) | Ингибиторы протеинкиназ (варианты), их применение для лечения онкологических заболеваний и фармацевтическая композиция на их основе | |
| JP2010533715A5 (https=) | ||
| RU2015154987A (ru) | Гетероциклические производные | |
| JP2018530571A5 (https=) | ||
| RU2007141892A (ru) | 5-метил-1-(замещенный фенил)-2-(1н)-пиридон для производства медикаментов для лечения фиброза в органах и тканях | |
| JP2017512191A5 (https=) | ||
| JP2020515575A5 (https=) | ||
| RU2015122414A (ru) | Соединения n-пирролидинилмочевины, n'-пиразолилмочевины, тиомочевины, гуанидина и цианогуанидина как ингибиторы киназы trka | |
| JP2016519156A5 (https=) | ||
| JP2010505832A5 (https=) | ||
| JP2010502727A (ja) | 血小板過剰を治療するｂｃｌインヒビター | |
| WO2014181287A1 (en) | Heterocyclyl compounds and uses thereof | |
| JP2018519323A5 (https=) | ||
| JP2011502958A5 (https=) | ||
| JP2004506718A5 (https=) | ||
| RU2015133171A (ru) | Бензиламиновые производные | |
| AR089134A1 (es) | Arilos y heteroarilos biciclicos inhibidores de los canales de sodio | |
| RU2018111106A (ru) | Производные карбоксизамещенных (гетеро)ароматических колец, способ их получения и применение |