CN103492384B - 作为trk抑制剂的化合物和组合物 - Google Patents
作为trk抑制剂的化合物和组合物 Download PDFInfo
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- CN103492384B CN103492384B CN201280019867.0A CN201280019867A CN103492384B CN 103492384 B CN103492384 B CN 103492384B CN 201280019867 A CN201280019867 A CN 201280019867A CN 103492384 B CN103492384 B CN 103492384B
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- Prior art keywords
- formula
- compound
- disease
- fluorophenyl
- pyrazolo
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- 0 CC1C[C@@](C)C(*)C1 Chemical compound CC1C[C@@](C)C(*)C1 0.000 description 10
- AGXKKIQEEVZOCF-NUHJPDEHSA-N C=[I]c1cc(C(C2)NC[C@H]2F)cc(C#N)c1 Chemical compound C=[I]c1cc(C(C2)NC[C@H]2F)cc(C#N)c1 AGXKKIQEEVZOCF-NUHJPDEHSA-N 0.000 description 1
- FSVWMTXMYKZYTA-HNNQXCQYSA-N CC(C)(C)/S(/O)=[O]\N[C@H](CCCO)c1cc(C#N)cc(F)c1 Chemical compound CC(C)(C)/S(/O)=[O]\N[C@H](CCCO)c1cc(C#N)cc(F)c1 FSVWMTXMYKZYTA-HNNQXCQYSA-N 0.000 description 1
- DBDIESYJMBSCPN-MDZDMXLPSA-N CC/C(/C(OCC)=O)=C(/C=C(C=C1)Br)\N1N Chemical compound CC/C(/C(OCC)=O)=C(/C=C(C=C1)Br)\N1N DBDIESYJMBSCPN-MDZDMXLPSA-N 0.000 description 1
- PQSLEXQFVUMCTQ-LLVKDONJSA-N CS(/[O]=C(\C1)/CN[C@H]1c1cccc(F)c1)(=O)=O Chemical compound CS(/[O]=C(\C1)/CN[C@H]1c1cccc(F)c1)(=O)=O PQSLEXQFVUMCTQ-LLVKDONJSA-N 0.000 description 1
- COKHMUBYEFXMPJ-VUWPPUDQSA-N N#Cc1cc(F)cc(C(C2)NC[C@H]2F)c1 Chemical compound N#Cc1cc(F)cc(C(C2)NC[C@H]2F)c1 COKHMUBYEFXMPJ-VUWPPUDQSA-N 0.000 description 1
- QNPMWTXQQSWIHE-UHFFFAOYSA-N NC(c1cc(C#N)cc(F)c1)=O Chemical compound NC(c1cc(C#N)cc(F)c1)=O QNPMWTXQQSWIHE-UHFFFAOYSA-N 0.000 description 1
- LJSGVSRHSBHOAJ-JFUPDXTOSA-N OC(c1c(cc(CC(CC(C2)c3cccc(F)c3)C[C@H]2F)cc2)[n]2nc1)=O Chemical compound OC(c1c(cc(CC(CC(C2)c3cccc(F)c3)C[C@H]2F)cc2)[n]2nc1)=O LJSGVSRHSBHOAJ-JFUPDXTOSA-N 0.000 description 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
-
- 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
- A61K31/437—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/06—Antiasthmatics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/04—Centrally acting analgesics, e.g. opioids
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- 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
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/08—Antiallergic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D207/04—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
- C07D207/08—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon radicals, substituted by hetero atoms, attached to ring carbon atoms
- C07D207/09—Radicals substituted by nitrogen atoms, not forming part of a nitro radical
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D207/04—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
- C07D207/10—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
Abstract
Description
Claims (21)
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US201161446572P | 2011-02-25 | 2011-02-25 | |
US61/446,572 | 2011-02-25 | ||
PCT/US2012/026377 WO2012116217A1 (en) | 2011-02-25 | 2012-02-23 | Compounds and compositions as trk inhibitors |
Publications (2)
Publication Number | Publication Date |
---|---|
CN103492384A CN103492384A (zh) | 2014-01-01 |
CN103492384B true CN103492384B (zh) | 2016-05-11 |
Family
ID=45815979
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
CN201280019867.0A Expired - Fee Related CN103492384B (zh) | 2011-02-25 | 2012-02-23 | 作为trk抑制剂的化合物和组合物 |
Country Status (27)
Country | Link |
---|---|
US (1) | US9102671B2 (zh) |
EP (1) | EP2678338B1 (zh) |
JP (1) | JP5959541B2 (zh) |
KR (1) | KR20140014184A (zh) |
CN (1) | CN103492384B (zh) |
AP (1) | AP2013007103A0 (zh) |
AU (1) | AU2012220572A1 (zh) |
BR (1) | BR112013021638A2 (zh) |
CA (1) | CA2828219A1 (zh) |
CL (1) | CL2013002430A1 (zh) |
CO (1) | CO6751270A2 (zh) |
CR (1) | CR20130410A (zh) |
CU (1) | CU20130115A7 (zh) |
DO (1) | DOP2013000192A (zh) |
EA (1) | EA201391230A1 (zh) |
ES (1) | ES2551592T3 (zh) |
GE (1) | GEP20156285B (zh) |
GT (1) | GT201300209A (zh) |
IL (1) | IL227987A0 (zh) |
MA (1) | MA34969B1 (zh) |
MX (1) | MX2013009767A (zh) |
NI (1) | NI201300073A (zh) |
PE (1) | PE20140378A1 (zh) |
SG (1) | SG192795A1 (zh) |
TN (1) | TN2013000348A1 (zh) |
WO (1) | WO2012116217A1 (zh) |
ZA (1) | ZA201306221B (zh) |
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CA2738026C (en) | 2008-09-22 | 2017-01-24 | Array Biopharma Inc. | Substituted imidazo[1,2b]pyridazine compounds as trk kinase inhibitors |
PT2725028T (pt) | 2008-10-22 | 2016-08-31 | Array Biopharma Inc | Compostos de pirazolo[1,5-]pirimidina substituídos como intermediários na síntese de inibidores de cinase trk |
AR077468A1 (es) | 2009-07-09 | 2011-08-31 | Array Biopharma Inc | Compuestos de pirazolo (1,5 -a) pirimidina sustituidos como inhibidores de trk- quinasa |
PL2918588T3 (pl) | 2010-05-20 | 2017-10-31 | Array Biopharma Inc | Związki makrocykliczne jako inhibitory kinazy TRK |
US9045479B2 (en) * | 2011-12-12 | 2015-06-02 | Dr. Reddy's Laboratories Ltd. | Substituted heterocyclic compounds as tropomyosin receptor kinase a (TrkA) inhibitors |
EP3628749A1 (en) | 2013-07-30 | 2020-04-01 | Blueprint Medicines Corporation | Ntrk2 fusions |
PL3087070T3 (pl) * | 2013-12-26 | 2018-03-30 | Ignyta, Inc. | Pochodne pirazolo[1,5-a]pirydyny i sposoby ich zastosowania |
DK3102555T3 (da) * | 2014-02-05 | 2021-08-09 | VM Oncology LLC | Sammensætninger af forbindelser og anvendelser deraf |
CN105524058B (zh) * | 2014-10-21 | 2018-03-27 | 广州艾格生物科技有限公司 | 吡唑并[1,5‑a]吡啶类化合物及其应用 |
KR102649887B1 (ko) | 2014-11-16 | 2024-03-22 | 어레이 바이오파마 인크. | (s)-n-(5-((r)-2-(2,5-디플루오로페닐)-피롤리딘-1-일)-피라졸로[1,5-a]피리미딘-3-일)-3-히드록시피롤리딘-1-카르복스아미드 히드로겐 술페이트의 결정질 형태 |
CN104529815B (zh) * | 2014-12-04 | 2016-08-24 | 宁波欧迅化学新材料技术有限公司 | 合成2,4-二硝基苯氧胺的方法 |
US20180177792A1 (en) * | 2015-05-29 | 2018-06-28 | Ignyta, Inc. | Compositions and methods for treating patients with rtk mutant cells |
CA2988423A1 (en) | 2015-06-01 | 2016-12-08 | Loxo Oncology, Inc. | Methods of diagnosing and treating cancer |
EA035049B1 (ru) | 2015-07-16 | 2020-04-22 | Аррэй Байофарма Инк. | СОЕДИНЕНИЯ ЗАМЕЩЕННОГО ПИРАЗОЛО[1,5-a]ПИРИДИНА В КАЧЕСТВЕ ИНГИБИТОРОВ RET КИНАЗЫ |
CN108697708A (zh) | 2015-10-26 | 2018-10-23 | 洛克索肿瘤学股份有限公司 | Trk抑制剂抗性癌症中的点突变以及与此相关的方法 |
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MA44612A (fr) | 2016-04-04 | 2019-02-13 | Loxo Oncology Inc | Méthodes de traitement de cancers pédiatriques |
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CN110049987B (zh) | 2016-05-18 | 2022-02-18 | 阵列生物制药公司 | 制备化合物及其盐的方法 |
EP3490974B1 (en) | 2016-08-01 | 2023-12-06 | Tenacia Biotechnology (Hong Kong) Co., Limited | Spiro-lactam nmda receptor modulators and uses thereof |
CN109937204B (zh) | 2016-08-01 | 2022-11-25 | 阿普廷伊克斯股份有限公司 | 螺-内酰胺nmda受体调节剂及其用途 |
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TWI704148B (zh) | 2016-10-10 | 2020-09-11 | 美商亞雷生物製藥股份有限公司 | 作為ret激酶抑制劑之經取代吡唑并[1,5-a]吡啶化合物 |
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BR112020003783A2 (pt) | 2017-08-23 | 2020-09-01 | Chia Tai Tianqing Pharmaceutical Group Co., Ltd. | macrociclo contendo aminopirazol e pirimidina e composição farmacêutica e uso da mesma |
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Also Published As
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CR20130410A (es) | 2013-10-17 |
IL227987A0 (en) | 2013-09-30 |
EP2678338A1 (en) | 2014-01-01 |
ZA201306221B (en) | 2014-04-30 |
EP2678338B1 (en) | 2015-09-09 |
EA201391230A1 (ru) | 2014-01-30 |
MX2013009767A (es) | 2013-10-01 |
PE20140378A1 (es) | 2014-03-28 |
CA2828219A1 (en) | 2012-08-30 |
GEP20156285B (en) | 2015-05-11 |
AU2012220572A1 (en) | 2013-08-29 |
BR112013021638A2 (pt) | 2016-08-02 |
CL2013002430A1 (es) | 2013-11-29 |
TN2013000348A1 (en) | 2015-01-20 |
US20130331397A1 (en) | 2013-12-12 |
MA34969B1 (fr) | 2014-03-01 |
WO2012116217A1 (en) | 2012-08-30 |
JP2014506599A (ja) | 2014-03-17 |
DOP2013000192A (es) | 2014-01-31 |
KR20140014184A (ko) | 2014-02-05 |
CN103492384A (zh) | 2014-01-01 |
CU20130115A7 (es) | 2013-12-27 |
GT201300209A (es) | 2015-06-02 |
ES2551592T3 (es) | 2015-11-20 |
CO6751270A2 (es) | 2013-09-16 |
SG192795A1 (en) | 2013-09-30 |
US9102671B2 (en) | 2015-08-11 |
AP2013007103A0 (en) | 2013-09-30 |
NI201300073A (es) | 2013-12-17 |
JP5959541B2 (ja) | 2016-08-02 |
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