JP2011509301A5 - - Google Patents
Download PDFInfo
- Publication number
- JP2011509301A5 JP2011509301A5 JP2010542341A JP2010542341A JP2011509301A5 JP 2011509301 A5 JP2011509301 A5 JP 2011509301A5 JP 2010542341 A JP2010542341 A JP 2010542341A JP 2010542341 A JP2010542341 A JP 2010542341A JP 2011509301 A5 JP2011509301 A5 JP 2011509301A5
- Authority
- JP
- Japan
- Prior art keywords
- compound according
- hydrogen
- compound
- alkyl
- phenyl
- 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 137
- 229910052739 hydrogen Inorganic materials 0.000 claims description 44
- 239000001257 hydrogen Substances 0.000 claims description 44
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 38
- -1 1-oxa-3,4-diazolyl Chemical group 0.000 claims description 24
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 24
- 125000000217 alkyl group Chemical group 0.000 claims description 21
- 229910052736 halogen Inorganic materials 0.000 claims description 16
- 150000002367 halogens Chemical class 0.000 claims description 16
- 238000011282 treatment Methods 0.000 claims description 13
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 10
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 9
- 238000000034 method Methods 0.000 claims description 9
- DFPAKSUCGFBDDF-UHFFFAOYSA-N Nicotinamide Chemical compound NC(=O)C1=CC=CN=C1 DFPAKSUCGFBDDF-UHFFFAOYSA-N 0.000 claims description 8
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 claims description 7
- 201000010099 disease Diseases 0.000 claims description 7
- 150000002431 hydrogen Chemical class 0.000 claims description 6
- 125000001072 heteroaryl group Chemical group 0.000 claims description 5
- 230000003463 hyperproliferative effect Effects 0.000 claims description 5
- 125000006569 (C5-C6) heterocyclic group Chemical group 0.000 claims description 4
- 125000001255 4-fluorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C([H])=C1F 0.000 claims description 4
- 101000777293 Homo sapiens Serine/threonine-protein kinase Chk1 Proteins 0.000 claims description 4
- 101000777277 Homo sapiens Serine/threonine-protein kinase Chk2 Proteins 0.000 claims description 4
- 102100031081 Serine/threonine-protein kinase Chk1 Human genes 0.000 claims description 4
- 102100031075 Serine/threonine-protein kinase Chk2 Human genes 0.000 claims description 4
- 125000004429 atom Chemical group 0.000 claims description 4
- 125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 claims description 4
- 239000003814 drug Substances 0.000 claims description 4
- 125000000623 heterocyclic group Chemical group 0.000 claims description 4
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims description 4
- 238000004519 manufacturing process Methods 0.000 claims description 4
- 229960003966 nicotinamide Drugs 0.000 claims description 4
- 235000005152 nicotinamide Nutrition 0.000 claims description 4
- 239000011570 nicotinamide Substances 0.000 claims description 4
- 229910052757 nitrogen Inorganic materials 0.000 claims description 4
- 125000004433 nitrogen atom Chemical group N* 0.000 claims description 4
- 239000008194 pharmaceutical composition Substances 0.000 claims description 4
- 150000003839 salts Chemical class 0.000 claims description 4
- 206010028980 Neoplasm Diseases 0.000 claims description 3
- 201000011510 cancer Diseases 0.000 claims description 3
- 230000002265 prevention Effects 0.000 claims description 3
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims description 2
- ZVXKYWHJBYIYNI-UHFFFAOYSA-N 1h-pyrazole-4-carboxamide Chemical compound NC(=O)C=1C=NNC=1 ZVXKYWHJBYIYNI-UHFFFAOYSA-N 0.000 claims description 2
- 125000004198 2-fluorophenyl group Chemical group [H]C1=C([H])C(F)=C(*)C([H])=C1[H] 0.000 claims description 2
- 125000000175 2-thienyl group Chemical group S1C([*])=C([H])C([H])=C1[H] 0.000 claims description 2
- 125000003762 3,4-dimethoxyphenyl group Chemical group [H]C1=C([H])C(OC([H])([H])[H])=C(OC([H])([H])[H])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
- 125000004207 3-methoxyphenyl group Chemical group [H]C1=C([H])C(*)=C([H])C(OC([H])([H])[H])=C1[H] 0.000 claims description 2
- 125000003349 3-pyridyl group Chemical group N1=C([H])C([*])=C([H])C([H])=C1[H] 0.000 claims description 2
- 125000004800 4-bromophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C([H])=C1Br 0.000 claims description 2
- 125000004172 4-methoxyphenyl group Chemical group [H]C1=C([H])C(OC([H])([H])[H])=C([H])C([H])=C1* 0.000 claims description 2
- CVICEEPAFUYBJG-UHFFFAOYSA-N 5-chloro-2,2-difluoro-1,3-benzodioxole Chemical group C1=C(Cl)C=C2OC(F)(F)OC2=C1 CVICEEPAFUYBJG-UHFFFAOYSA-N 0.000 claims description 2
- BCCUXBGEPLKSEX-UHFFFAOYSA-N 5-methylpyridine-3-carboxamide Chemical compound CC1=CN=CC(C(N)=O)=C1 BCCUXBGEPLKSEX-UHFFFAOYSA-N 0.000 claims description 2
- DFPAKSUCGFBDDF-ZQBYOMGUSA-N [14c]-nicotinamide Chemical compound N[14C](=O)C1=CC=CN=C1 DFPAKSUCGFBDDF-ZQBYOMGUSA-N 0.000 claims description 2
- 230000010933 acylation Effects 0.000 claims description 2
- 238000005917 acylation reaction Methods 0.000 claims description 2
- 230000001093 anti-cancer Effects 0.000 claims description 2
- 239000003153 chemical reaction reagent Substances 0.000 claims description 2
- 230000008878 coupling Effects 0.000 claims description 2
- 238000010168 coupling process Methods 0.000 claims description 2
- 238000005859 coupling reaction Methods 0.000 claims description 2
- 208000035475 disorder Diseases 0.000 claims description 2
- 239000003937 drug carrier Substances 0.000 claims description 2
- 239000003112 inhibitor Substances 0.000 claims description 2
- 238000011275 oncology therapy Methods 0.000 claims description 2
- 125000003854 p-chlorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C([H])=C1Cl 0.000 claims description 2
- 239000000546 pharmaceutical excipient Substances 0.000 claims description 2
- 125000003226 pyrazolyl group Chemical group 0.000 claims description 2
- 125000004076 pyridyl group Chemical group 0.000 claims description 2
- 125000001544 thienyl group Chemical group 0.000 claims description 2
- 239000000203 mixture Substances 0.000 claims 4
- 241000124008 Mammalia Species 0.000 description 4
- 0 C*(*)*(C)C(*)(CC*(C)N(*)*)C(O)=O Chemical compound C*(*)*(C)C(*)(CC*(C)N(*)*)C(O)=O 0.000 description 1
- 238000011321 prophylaxis Methods 0.000 description 1
- 238000002560 therapeutic procedure Methods 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US1978608P | 2008-01-08 | 2008-01-08 | |
| US61/019,786 | 2008-01-08 | ||
| PCT/US2009/030443 WO2009089352A1 (en) | 2008-01-08 | 2009-01-08 | Pyrrolopyridines as kinase inhibitors |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2014032761A Division JP2014129376A (ja) | 2008-01-08 | 2014-02-24 | キナーゼ阻害薬としてのピロロピリジン |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2011509301A JP2011509301A (ja) | 2011-03-24 |
| JP2011509301A5 true JP2011509301A5 (enExample) | 2013-02-07 |
| JP5608097B2 JP5608097B2 (ja) | 2014-10-15 |
Family
ID=40352263
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2010542341A Expired - Fee Related JP5608097B2 (ja) | 2008-01-08 | 2009-01-08 | キナーゼ阻害薬としてのピロロピリジン |
| JP2014032761A Withdrawn JP2014129376A (ja) | 2008-01-08 | 2014-02-24 | キナーゼ阻害薬としてのピロロピリジン |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2014032761A Withdrawn JP2014129376A (ja) | 2008-01-08 | 2014-02-24 | キナーゼ阻害薬としてのピロロピリジン |
Country Status (7)
| Country | Link |
|---|---|
| US (1) | US8841304B2 (enExample) |
| EP (1) | EP2242755B1 (enExample) |
| JP (2) | JP5608097B2 (enExample) |
| CN (1) | CN101959887B (enExample) |
| CA (1) | CA2711614A1 (enExample) |
| ES (1) | ES2394759T3 (enExample) |
| WO (1) | WO2009089352A1 (enExample) |
Families Citing this family (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2242757B1 (en) * | 2008-01-09 | 2012-08-01 | Array Biopharma, Inc. | Pyrazolopyridines as kinase inhibitors |
| AR071717A1 (es) | 2008-05-13 | 2010-07-07 | Array Biopharma Inc | Pirrolo[2,3-b]piridinas inhibidoras de quinasas chk1 y chk2,composiciones farmaceuticas que las contienen,proceso para prepararlas y uso de las mismas en el tratamiento y prevencion del cancer. |
| US8481557B2 (en) * | 2009-04-11 | 2013-07-09 | Array Biopharma Inc. | Method of treatment using checkpoint kinase 1 inhibitors |
| BR112012000422A2 (pt) * | 2009-07-08 | 2017-05-09 | Leo Pharma As | composto, composição farmacêutica, uso de um composto, e, método para a prevenir tratar ou melhorar doenças do sistema imune |
| US20140221370A1 (en) * | 2010-07-09 | 2014-08-07 | Array Biopharma Inc. | Pyrrolopyridines as kinase inhibitors |
| TW201304778A (zh) | 2010-11-16 | 2013-02-01 | Array Biopharma Inc | 檢查點激酶１抑制劑及ｗｅｅ１激酶抑制劑之組合 |
| US8791112B2 (en) | 2011-03-30 | 2014-07-29 | Arrien Pharmaceuticals Llc | Substituted 5-(pyrazin-2-yl)-1H-pyrazolo [3, 4-B] pyridine and pyrazolo [3, 4-B] pyridine derivatives as protein kinase inhibitors |
| GB201201566D0 (en) | 2012-01-30 | 2012-03-14 | Vernalis R&D Ltd | New chemical compounds |
| AU2013252514B2 (en) | 2012-04-23 | 2017-07-20 | Genentech, Inc. | Intermediates and processes for preparing compounds |
| KR102325163B1 (ko) * | 2013-08-22 | 2021-11-11 | 제넨테크, 인크. | 화합물의 제조 방법 |
| WO2016004305A2 (en) | 2014-07-02 | 2016-01-07 | Pharmacyclics Llc | Inhibitors of bruton's tyrosine kinase |
| WO2020150417A2 (en) * | 2019-01-17 | 2020-07-23 | Ifm Due, Inc. | Compounds and compositions for treating conditions associated with sting activity |
| PY2269135A (es) | 2021-08-10 | 2024-01-29 | Ifm Due Inc | Compuestos y composiciones para tratar afecciones asociadas con la actividad de sting |
Family Cites Families (47)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU3053999A (en) | 1998-03-31 | 1999-10-25 | Kyowa Hakko Kogyo Co. Ltd. | Nitrogenous heterocyclic compounds |
| 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 |
| US7115741B2 (en) | 2001-09-06 | 2006-10-03 | Levy Daniel E | 4-thieno[2,3-D]pyrimidin-4-YL piperazine compounds |
| WO2003028724A1 (en) | 2001-10-04 | 2003-04-10 | Smithkline Beecham Corporation | Chk1 kinase inhibitors |
| US6797825B2 (en) | 2001-12-13 | 2004-09-28 | Abbott Laboratories | Protein kinase inhibitors |
| 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 |
| US20050256157A1 (en) | 2002-08-23 | 2005-11-17 | Chiron Corporation | Combination therapy with CHK1 inhibitors |
| NZ545717A (en) | 2003-08-05 | 2009-12-24 | Vertex Pharma | Hydrogenated quinazoline derivatives as inhibitors of voltage-gated ion channels |
| MXPA06002618A (es) | 2003-09-09 | 2006-06-05 | Ono Pharmaceutical Co | Antagonistas del factor de liberacion de corticotropina (crf) y compuestos heterobiciclicos. |
| TW200526547A (en) | 2003-09-22 | 2005-08-16 | Theravance Inc | Amino-substituted ethylamino β2 adrenergic receptor agonists |
| US20050130954A1 (en) * | 2003-11-21 | 2005-06-16 | Mitchell Ian S. | AKT protein kinase inhibitors |
| GB0330043D0 (en) | 2003-12-24 | 2004-01-28 | Pharmacia Italia Spa | Pyrrolo [2,3-b] pyridine derivatives active as kinase inhibitors process for their preparation and pharmaceutical compositions comprising them |
| WO2005117909A2 (en) | 2004-04-23 | 2005-12-15 | Exelixis, Inc. | Kinase modulators and methods of use |
| GB0409080D0 (en) | 2004-04-23 | 2004-05-26 | Biofocus Discovery Ltd | Compounds which interact with protein kinases |
| 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 |
| US7994172B2 (en) | 2004-12-28 | 2011-08-09 | Exelixis, Inc. | [1H-pyrazolo[3, 4-D]pyrimidin-4-yl]-piperidine or -piperazine compounds as serine-theoronine kinase modulators (P70s6k, Atk1 and Atk2) for the treatment of immunological, inflammatory and proliferative diseases |
| PE20061119A1 (es) | 2005-01-19 | 2006-11-27 | Aventis Pharma Sa | PIRAZOLO PIRIDINAS SUSTITUIDAS COMO INHIBIDORES DE CINASAS FAK, KDR Y Tie |
| GB0501999D0 (en) | 2005-02-01 | 2005-03-09 | Sentinel Oncology Ltd | Pharmaceutical compounds |
| WO2006106326A1 (en) | 2005-04-06 | 2006-10-12 | Astrazeneca Ab | Substituted heterocycles and their use as chk1, pdk1 and pak inhibitors |
| KR20080016659A (ko) | 2005-05-20 | 2008-02-21 | 버텍스 파마슈티칼스 인코포레이티드 | 단백질 키나제의 억제제로서 유용한 피롤로피리딘 |
| WO2006130673A1 (en) | 2005-05-31 | 2006-12-07 | Janssen Pharmaceutica, N.V. | 3-benzoimidazolyl-pyrazolopyridines useful in treating kinase disorders |
| DK2395004T3 (en) | 2005-06-22 | 2016-03-21 | Plexxikon Inc | Pyrrolo [2,3-b] pyridine derivatives as protein kinase inhibitors |
| BRPI0616985B1 (pt) | 2005-10-06 | 2021-10-26 | Merck Sharp & Dohme Corp. | Composto de pirazolo[1,5-a]pirimidina, e, uso de um composto |
| CA2628179A1 (en) | 2005-11-15 | 2007-05-24 | Vertex Pharmaceuticals Incorporated | Azaindazoles useful as inhibitors of kinases |
| DE102006005180A1 (de) | 2006-02-06 | 2007-08-09 | Merck Patent Gmbh | Indazol-heteroaryl-derivate |
| DE102006005179A1 (de) | 2006-02-06 | 2007-08-09 | Merck Patent Gmbh | Aminoindazolderivate |
| MX2008011220A (es) | 2006-03-07 | 2008-09-11 | Array Biopharma Inc | Compuestos de pirazol heterobiciclicos y metodos de uso. |
| JP5606734B2 (ja) | 2006-04-25 | 2014-10-15 | 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 |
| US20090124610A1 (en) | 2006-04-25 | 2009-05-14 | Gordon Saxty | Pharmaceutical compounds |
| US8063050B2 (en) | 2006-07-06 | 2011-11-22 | Array Biopharma Inc. | Hydroxylated and methoxylated pyrimidyl cyclopentanes as AKT protein kinase inhibitors |
| ATE532789T1 (de) | 2006-07-06 | 2011-11-15 | Array Biopharma Inc | Dihydrothienopyrimidine als akt-proteinkinase- inhibitoren |
| CN101511842B (zh) | 2006-07-06 | 2012-10-31 | 阵列生物制药公司 | 作为akt蛋白激酶抑制剂的二氢呋喃并嘧啶 |
| WO2008006032A1 (en) | 2006-07-06 | 2008-01-10 | Array Biopharma Inc. | Cyclopenta [d] pyrimidines as akt protein kinase inhibitors |
| WO2008012635A2 (en) | 2006-07-26 | 2008-01-31 | Pfizer Products Inc. | Amine derivatives useful as anticancer agents |
| WO2008075007A1 (en) | 2006-12-21 | 2008-06-26 | Cancer Research Technology Limited | Morpholino-substituted bicycloheteroaryl compounds and their use as anti cancer agents |
| EP2170886A1 (en) | 2007-07-02 | 2010-04-07 | Cancer Research Technology Limited | 9h-pyrimido[4,5-b]indoles, 9h-pyrido[4',3':4,5]pyrrolo[2,3-d]pyridines, and 9h-1,3,6,9-tetraaza-fluorenes as chk1 kinase function inhibitors |
| US8618097B2 (en) | 2007-07-05 | 2013-12-31 | Array Biopharma, Inc. | Pyrimidyl cyclopentanes as AKT protein kinase inhibitors |
| SI2173723T1 (sl) | 2007-07-05 | 2011-12-30 | Array Biopharma Inc | Pirimidil ciklopentani kot inhibitorji AKT-protein-kinaze |
| AR069198A1 (es) | 2007-11-07 | 2010-01-06 | Schering Corp | Derivados de ribosil pirimidinas moduladores de quinasas de control chk1,y composiciones farmaceuticas que los comprenden utiles en el tratamiento del cancer. |
| EP2242757B1 (en) | 2008-01-09 | 2012-08-01 | Array Biopharma, Inc. | Pyrazolopyridines as kinase inhibitors |
| JP5346345B2 (ja) | 2008-01-09 | 2013-11-20 | アレイ バイオファーマ、インコーポレイテッド | Ａｋｔタンパク質キナーゼ阻害剤としての水酸化されたピリミジルシクロペンタン類 |
| CA2711782C (en) | 2008-01-09 | 2017-01-03 | Array Biopharma Inc. | 5h-cyclopenta[d]pyrimidines as akt protein kinase inhibitors |
| EP2240455B1 (en) | 2008-01-09 | 2012-12-26 | Array Biopharma, Inc. | Hydroxylated pyrimidyl cyclopentane as akt protein kinase inhibitor |
| AR071717A1 (es) | 2008-05-13 | 2010-07-07 | Array Biopharma Inc | Pirrolo[2,3-b]piridinas inhibidoras de quinasas chk1 y chk2,composiciones farmaceuticas que las contienen,proceso para prepararlas y uso de las mismas en el tratamiento y prevencion del cancer. |
| US8481557B2 (en) | 2009-04-11 | 2013-07-09 | Array Biopharma Inc. | Method of treatment using checkpoint kinase 1 inhibitors |
| CN102612365B (zh) | 2009-04-11 | 2017-04-12 | 阵列生物制药公司 | 用于强化dna损伤剂的检查点激酶1抑制剂 |
| TW201304778A (zh) | 2010-11-16 | 2013-02-01 | Array Biopharma Inc | 檢查點激酶１抑制劑及ｗｅｅ１激酶抑制劑之組合 |
-
2009
- 2009-01-08 CN CN2009801081982A patent/CN101959887B/zh not_active Expired - Fee Related
- 2009-01-08 CA CA2711614A patent/CA2711614A1/en not_active Abandoned
- 2009-01-08 JP JP2010542341A patent/JP5608097B2/ja not_active Expired - Fee Related
- 2009-01-08 WO PCT/US2009/030443 patent/WO2009089352A1/en not_active Ceased
- 2009-01-08 EP EP09700828A patent/EP2242755B1/en active Active
- 2009-01-08 ES ES09700828T patent/ES2394759T3/es active Active
- 2009-01-08 US US12/812,447 patent/US8841304B2/en not_active Expired - Fee Related
-
2014
- 2014-02-24 JP JP2014032761A patent/JP2014129376A/ja not_active Withdrawn
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| JP2011509302A5 (enExample) | ||
| JP2011509309A5 (enExample) | ||
| DK2900269T3 (en) | COMBINATION OF REGORAFENIB AND ACETYLSALICYLIC ACID FOR TREATMENT OF COLORECTAL CANCER. | |
| JP2022541483A5 (enExample) | ||
| TW202446772A (zh) | Ｓｔｉｎｇ促效化合物 | |
| JP2019517487A5 (enExample) | ||
| JP2010522765A5 (enExample) | ||
| RU2650895C2 (ru) | Соединения замещенных пиразолонов и способы использования | |
| JP2016517851A5 (enExample) | ||
| JP2005526723A5 (enExample) | ||
| JP2014500295A5 (enExample) | ||
| CA3071760A1 (en) | Combination of atr kinase inhibitors and pd-1/pd-l1 inhibitors | |
| JP2013515074A5 (enExample) | ||
| JP2012503018A5 (enExample) | ||
| TW202317532A (zh) | Aak1抑制劑及其用途 | |
| JP2014532716A5 (enExample) | ||
| JP2014503574A5 (enExample) | ||
| JP2014508811A5 (enExample) | ||
| JP2017514809A5 (enExample) | ||
| JP2012530779A5 (enExample) | ||
| JP2016525102A5 (enExample) | ||
| JP2013532668A5 (enExample) | ||
| JP2011526917A5 (enExample) | ||
| RU2009103307A (ru) | ПРОИЗВОДНЫЕ ИМИДАЗО[1, 2-a]ПИРИДИН-2-КАРБОКСАМИДОВ, ИХ ПОЛУЧЕНИЕ И ПРИМЕНЕНИЕ В ТЕРАПИИ | |
| JP2015500885A5 (enExample) |