CN102197032B - 杂环pim-激酶抑制剂 - Google Patents
杂环pim-激酶抑制剂 Download PDFInfo
- Publication number
- CN102197032B CN102197032B CN200980142961.3A CN200980142961A CN102197032B CN 102197032 B CN102197032 B CN 102197032B CN 200980142961 A CN200980142961 A CN 200980142961A CN 102197032 B CN102197032 B CN 102197032B
- Authority
- CN
- China
- Prior art keywords
- pyridin
- amino
- difluorophenyl
- tert
- amine
- 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
Links
- 0 *[C@@]1[C@](**=C)C*CC1 Chemical compound *[C@@]1[C@](**=C)C*CC1 0.000 description 2
- DXSXSTLEHBAQBL-OLZOCXBDSA-N CC(C)(C)OC(N([C@H](CN(CC1)c(ccnc2)c2N)[C@H]1O1)C1=O)=O Chemical compound CC(C)(C)OC(N([C@H](CN(CC1)c(ccnc2)c2N)[C@H]1O1)C1=O)=O DXSXSTLEHBAQBL-OLZOCXBDSA-N 0.000 description 1
- UEWSOQWPBLRFJI-NUHJPDEHSA-N CC(C)(C)OC(NC(CN(CC1)c(ccnc2)c2N)[C@H]1F)=O Chemical compound CC(C)(C)OC(NC(CN(CC1)c(ccnc2)c2N)[C@H]1F)=O UEWSOQWPBLRFJI-NUHJPDEHSA-N 0.000 description 1
- YFAUGTRGVNCMSI-JTQLQIEISA-N CC(C)(C)OC(N[C@@H](CCC1)CN1c(ncnc1)c1N)=O Chemical compound CC(C)(C)OC(N[C@@H](CCC1)CN1c(ncnc1)c1N)=O YFAUGTRGVNCMSI-JTQLQIEISA-N 0.000 description 1
- KQQULFXHZGYBEV-NWDGAFQWSA-N CC(C)(C)OC(N[C@@H](C[C@H](C1)OC)CN1c(ccnc1)c1[N+]([O-])=O)=O Chemical compound CC(C)(C)OC(N[C@@H](C[C@H](C1)OC)CN1c(ccnc1)c1[N+]([O-])=O)=O KQQULFXHZGYBEV-NWDGAFQWSA-N 0.000 description 1
- RZYYTLKFSSYXMI-UHFFFAOYSA-N CC(CC(C1)NC(OC(C)(C)C)=O)CN1c(ccnc1)c1[N+]([O-])=O Chemical compound CC(CC(C1)NC(OC(C)(C)C)=O)CN1c(ccnc1)c1[N+]([O-])=O RZYYTLKFSSYXMI-UHFFFAOYSA-N 0.000 description 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
-
- 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
- A61P35/00—Antineoplastic agents
- A61P35/02—Antineoplastic agents specific for leukemia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
- A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/08—Antiallergic agents
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
Landscapes
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Immunology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Transplantation (AREA)
- Pulmonology (AREA)
- Hematology (AREA)
- Oncology (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US9366408P | 2008-09-02 | 2008-09-02 | |
| US61/093,664 | 2008-09-02 | ||
| PCT/EP2009/061188 WO2010026122A1 (en) | 2008-09-02 | 2009-08-31 | Heterocyclic pim-kinase inhibitors |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN102197032A CN102197032A (zh) | 2011-09-21 |
| CN102197032B true CN102197032B (zh) | 2014-07-23 |
Family
ID=41170173
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN200980142961.3A Expired - Fee Related CN102197032B (zh) | 2008-09-02 | 2009-08-31 | 杂环pim-激酶抑制剂 |
Country Status (11)
| Country | Link |
|---|---|
| US (1) | US8759338B2 (https=) |
| EP (1) | EP2344473B1 (https=) |
| JP (1) | JP5584215B2 (https=) |
| KR (1) | KR20110056399A (https=) |
| CN (1) | CN102197032B (https=) |
| AU (1) | AU2009289317A1 (https=) |
| BR (1) | BRPI0918846A2 (https=) |
| CA (1) | CA2735782A1 (https=) |
| EA (1) | EA201100427A1 (https=) |
| MX (1) | MX2011002362A (https=) |
| WO (1) | WO2010026122A1 (https=) |
Families Citing this family (37)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2455382B1 (en) | 2005-12-13 | 2016-10-26 | Incyte Holdings Corporation | Heteroaryl substituted pyrrolo[2,3-b]pyridines and pyrrolo[2,3-b]pyrimidines as Janus kinase inhibitors |
| EP3070090B1 (en) | 2007-06-13 | 2018-12-12 | Incyte Holdings Corporation | Use of salts of the janus kinase inhibitor (r)-3-(4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)-1h- pyrazol-1-yl)-3- cyclopentylpropanenitrile |
| SG176111A1 (en) | 2009-05-22 | 2011-12-29 | Incyte Corp | 3-[4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)-1h-pyrazol-1-yl]octane- or heptane-nitrile as jak inhibitors |
| JP5775070B2 (ja) | 2009-05-22 | 2015-09-09 | インサイト・コーポレイションＩｎｃｙｔｅ Ｃｏｒｐｏｒａｔｉｏｎ | ヤヌスキナーゼ阻害剤としてのピラゾール−４−イル−ピロロ［２，３−ｄ］ピリミジンおよびピロール−３−イル−ピロロ［２，３−ｄ］ピリミジンのＮ−（ヘテロ）アリール−ピロリジン誘導体 |
| AR078012A1 (es) | 2009-09-01 | 2011-10-05 | Incyte Corp | Derivados heterociclicos de las pirazol-4-il- pirrolo (2,3-d) pirimidinas como inhibidores de la quinasa janus |
| PT3354652T (pt) | 2010-03-10 | 2020-07-20 | Incyte Holdings Corp | Derivados de piperidin-4-ilazetidina como inibidores de jak1 |
| RS54824B1 (sr) | 2010-05-21 | 2016-10-31 | Incyte Holdings Corp | Topikalna formulacija za inhibiciju jak-a |
| WO2012068440A1 (en) | 2010-11-19 | 2012-05-24 | Incyte Corporation | Heterocyclic-substituted pyrrolopyridines and pyrrolopyrimidines as jak inhibitors |
| CA2818542A1 (en) | 2010-11-19 | 2012-05-24 | Incyte Corporation | Cyclobutyl substituted pyrrolopyridine and pyrrolopyrimidine derivatives as jak inhibitors |
| MY165963A (en) | 2011-06-20 | 2018-05-18 | Incyte Holdings Corp | Azetidinyl phenyl, pyridyl or pyrazinyl carboxamide derivatives as jak inhibitors |
| EP2734205B1 (en) | 2011-07-21 | 2018-03-21 | Tolero Pharmaceuticals, Inc. | Heterocyclic protein kinase inhibitors |
| TW201313721A (zh) | 2011-08-18 | 2013-04-01 | Incyte Corp | 作為ｊａｋ抑制劑之環己基氮雜環丁烷衍生物 |
| UA111854C2 (uk) | 2011-09-07 | 2016-06-24 | Інсайт Холдінгс Корпорейшн | Способи і проміжні сполуки для отримання інгібіторів jak |
| TW201406761A (zh) | 2012-05-18 | 2014-02-16 | Incyte Corp | 做爲ｊａｋ抑制劑之哌啶基環丁基取代之吡咯并吡啶及吡咯并嘧啶衍生物 |
| CN113384546A (zh) | 2012-11-15 | 2021-09-14 | 因赛特公司 | 鲁索利替尼的缓释剂型 |
| JP6437452B2 (ja) | 2013-01-14 | 2018-12-12 | インサイト・ホールディングス・コーポレイションＩｎｃｙｔｅ Ｈｏｌｄｉｎｇｓ Ｃｏｒｐｏｒａｔｉｏｎ | Ｐｉｍキナーゼ阻害剤として有用な二環式芳香族カルボキサミド化合物 |
| RS60244B1 (sr) | 2013-01-15 | 2020-06-30 | Incyte Holdings Corp | Jedinjenja tiazolkarboksamida i piridinkarboksamida korisna kao inhibitori pim kinaze |
| WO2014138168A1 (en) | 2013-03-06 | 2014-09-12 | Incyte Corporation | Processes and intermediates for making a jak inhibitor |
| SG10201801069QA (en) | 2013-08-07 | 2018-03-28 | Incyte Corp | Sustained release dosage forms for a jak1 inhibitor |
| CN105658653A (zh) | 2013-08-23 | 2016-06-08 | 因赛特公司 | 可用作pim激酶抑制剂的呋喃并-和噻吩并-吡啶甲酰胺化合物 |
| US9498467B2 (en) | 2014-05-30 | 2016-11-22 | Incyte Corporation | Treatment of chronic neutrophilic leukemia (CNL) and atypical chronic myeloid leukemia (aCML) by inhibitors of JAK1 |
| US9580418B2 (en) | 2014-07-14 | 2017-02-28 | Incyte Corporation | Bicyclic aromatic carboxamide compounds useful as Pim kinase inhibitors |
| WO2016010897A1 (en) | 2014-07-14 | 2016-01-21 | Incyte Corporation | Bicyclic heteroaromatic carboxamide compounds useful as pim kinase inhibitors |
| WO2016196244A1 (en) | 2015-05-29 | 2016-12-08 | Incyte Corporation | Pyridineamine compounds useful as pim kinase inhibitors |
| TWI734699B (zh) | 2015-09-09 | 2021-08-01 | 美商英塞特公司 | Ｐｉｍ激酶抑制劑之鹽 |
| US9920032B2 (en) | 2015-10-02 | 2018-03-20 | Incyte Corporation | Heterocyclic compounds useful as pim kinase inhibitors |
| CN108373476B (zh) * | 2017-01-13 | 2021-06-01 | 成都地奥制药集团有限公司 | 一种激酶抑制剂及其制备和应用 |
| AR113922A1 (es) | 2017-12-08 | 2020-07-01 | Incyte Corp | Terapia de combinación de dosis baja para el tratamiento de neoplasias mieloproliferativas |
| EA202091830A1 (ru) | 2018-01-30 | 2020-12-29 | Инсайт Корпорейшн | Способы и промежуточные соединения для получения ингибитора jak |
| MD3773593T2 (ro) | 2018-03-30 | 2024-10-31 | Incyte Corp | Tratament hidradenitei supurative utilizând inhibitori ai JAK |
| CN117838695A (zh) | 2018-04-13 | 2024-04-09 | 住友制药肿瘤公司 | 用于治疗骨髓增殖性肿瘤和与癌症相关的纤维化的pim激酶抑制剂 |
| CN109369513B (zh) * | 2018-11-20 | 2020-08-25 | 都创(上海)医药科技有限公司 | 一种fbdd常用分子片段的制备方法 |
| CN111362922A (zh) * | 2018-12-26 | 2020-07-03 | 上海喆邺生物科技有限公司 | 2,4-二氨基嘧啶衍生物及其用途 |
| NZ778055A (en) | 2019-02-12 | 2025-11-28 | Sumitomo Pharma America Inc | Formulations comprising heterocyclic protein kinase inhibitors |
| US11833155B2 (en) | 2020-06-03 | 2023-12-05 | Incyte Corporation | Combination therapy for treatment of myeloproliferative neoplasms |
| TW202237119A (zh) | 2020-12-10 | 2022-10-01 | 美商住友製藥腫瘤公司 | Ａｌｋ﹘５抑制劑和彼之用途 |
| EP4611753A1 (en) | 2022-10-31 | 2025-09-10 | Sumitomo Pharma America, Inc. | Pim1 inhibitor for treating myeloproliferative neoplasms |
Family Cites Families (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB9312891D0 (en) * | 1993-06-22 | 1993-08-04 | Boots Co Plc | Therapeutic agents |
| US6184226B1 (en) | 1998-08-28 | 2001-02-06 | Scios Inc. | Quinazoline derivatives as inhibitors of P-38 α |
| GB0226724D0 (en) * | 2002-11-15 | 2002-12-24 | Merck Sharp & Dohme | Therapeutic agents |
| WO2004081000A1 (en) | 2003-03-10 | 2004-09-23 | Astrazeneca Ab | Quinazoline derivatives |
| WO2004108707A1 (en) | 2003-06-05 | 2004-12-16 | Astrazeneca Ab | Pyridazinil quinazoline derivatives for use in the treatment of tumours |
| WO2005028467A1 (en) | 2003-09-15 | 2005-03-31 | Anadys Pharmaceuticals, Inc. | Antibacterial 3,5-diaminopiperidine-substitute aromatic and heteroaromatic compounds |
| AU2004278382B2 (en) * | 2003-09-30 | 2008-09-18 | Amgen Inc. | Vanilloid receptor ligands and their use in treatments |
| US7781591B2 (en) | 2006-06-13 | 2010-08-24 | Wyeth Llc | Substituted 3-cyanopyridines as protein kinase inhibitors |
| EP1781293A1 (en) * | 2004-06-04 | 2007-05-09 | Amphora Discovery Corporation | Quinoline- and isoquinoline-based compounds exhibiting atp-utilizing enzyme inhibitory activity, and compositions, and uses thereof |
| JP2009506123A (ja) * | 2005-08-29 | 2009-02-12 | 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 | 非受容体型チロシンキナーゼのｔｅｃファミリーの阻害剤として有用な３，５−二置換ピリド−２−オン |
| US7989461B2 (en) * | 2005-12-23 | 2011-08-02 | Amgen Inc. | Substituted quinazolinamine compounds for the treatment of cancer |
| RU2008139079A (ru) | 2006-06-13 | 2010-07-20 | Вайет (Us) | Замещенные 3-цианопиридины в качестве ингибиторов протеинкиназы |
| US7956064B2 (en) * | 2006-09-01 | 2011-06-07 | Cylene Pharmaceuticals, Inc. | Fused tricyclic compounds as serine-threonine protein kinase and PARP modulators |
| WO2008153947A2 (en) * | 2007-06-07 | 2008-12-18 | Amgen Inc. | Heterocyclic compounds as raf kinase modulators |
-
2009
- 2009-08-31 AU AU2009289317A patent/AU2009289317A1/en not_active Abandoned
- 2009-08-31 JP JP2011524404A patent/JP5584215B2/ja not_active Expired - Fee Related
- 2009-08-31 EA EA201100427A patent/EA201100427A1/ru unknown
- 2009-08-31 CA CA2735782A patent/CA2735782A1/en not_active Abandoned
- 2009-08-31 WO PCT/EP2009/061188 patent/WO2010026122A1/en not_active Ceased
- 2009-08-31 US US13/061,009 patent/US8759338B2/en not_active Expired - Fee Related
- 2009-08-31 BR BRPI0918846A patent/BRPI0918846A2/pt not_active IP Right Cessation
- 2009-08-31 EP EP09782379.3A patent/EP2344473B1/en not_active Not-in-force
- 2009-08-31 CN CN200980142961.3A patent/CN102197032B/zh not_active Expired - Fee Related
- 2009-08-31 KR KR1020117007561A patent/KR20110056399A/ko not_active Withdrawn
- 2009-08-31 MX MX2011002362A patent/MX2011002362A/es not_active Application Discontinuation
Also Published As
| Publication number | Publication date |
|---|---|
| AU2009289317A1 (en) | 2010-03-11 |
| EP2344473B1 (en) | 2014-04-16 |
| US20110195956A1 (en) | 2011-08-11 |
| KR20110056399A (ko) | 2011-05-27 |
| JP5584215B2 (ja) | 2014-09-03 |
| JP2012501313A (ja) | 2012-01-19 |
| CN102197032A (zh) | 2011-09-21 |
| MX2011002362A (es) | 2011-04-04 |
| US8759338B2 (en) | 2014-06-24 |
| BRPI0918846A2 (pt) | 2019-09-24 |
| WO2010026122A1 (en) | 2010-03-11 |
| EP2344473A1 (en) | 2011-07-20 |
| EA201100427A1 (ru) | 2011-10-31 |
| CA2735782A1 (en) | 2010-03-11 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| C06 | Publication | ||
| PB01 | Publication | ||
| C10 | Entry into substantive examination | ||
| SE01 | Entry into force of request for substantive examination | ||
| C53 | Correction of patent of invention or patent application | ||
| CB02 | Change of applicant information |
Address after: Basel Applicant after: Novartis Ag Address before: Basel Applicant before: Novartis AG |
|
| COR | Change of bibliographic data |
Free format text: CORRECT: APPLICANT; FROM: NOVARTIS AG TO: NOVARTIS CO., LTD. |
|
| C14 | Grant of patent or utility model | ||
| GR01 | Patent grant | ||
| CF01 | Termination of patent right due to non-payment of annual fee |
Granted publication date: 20140723 Termination date: 20150831 |
|
| EXPY | Termination of patent right or utility model |