ES2896943T3 - Compuesto de amino pirazolopirimidina usado como inhibidor de receptores con actividad tirosina quinasa de factores neurotróficos - Google Patents
Compuesto de amino pirazolopirimidina usado como inhibidor de receptores con actividad tirosina quinasa de factores neurotróficos Download PDFInfo
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- ES2896943T3 ES2896943T3 ES17863410T ES17863410T ES2896943T3 ES 2896943 T3 ES2896943 T3 ES 2896943T3 ES 17863410 T ES17863410 T ES 17863410T ES 17863410 T ES17863410 T ES 17863410T ES 2896943 T3 ES2896943 T3 ES 2896943T3
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- alkyl
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- -1 Amino pyrazolopyrimidine compound Chemical class 0.000 title claims abstract description 201
- 230000000694 effects Effects 0.000 title claims description 20
- 108091008598 receptor tyrosine kinases Proteins 0.000 title claims description 7
- 102000027426 receptor tyrosine kinases Human genes 0.000 title claims description 7
- 108010025020 Nerve Growth Factor Proteins 0.000 title description 7
- 102000007072 Nerve Growth Factors Human genes 0.000 title description 5
- 239000003900 neurotrophic factor Substances 0.000 title description 5
- 239000003112 inhibitor Substances 0.000 title description 2
- 150000001875 compounds Chemical class 0.000 claims abstract description 179
- 125000001424 substituent group Chemical group 0.000 claims abstract description 85
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims abstract description 83
- 125000000217 alkyl group Chemical group 0.000 claims abstract description 77
- 229910052739 hydrogen Inorganic materials 0.000 claims abstract description 77
- 239000001257 hydrogen Substances 0.000 claims abstract description 77
- 125000003118 aryl group Chemical group 0.000 claims abstract description 53
- 125000004093 cyano group Chemical group *C#N 0.000 claims abstract description 53
- 125000003545 alkoxy group Chemical group 0.000 claims abstract description 31
- 125000000753 cycloalkyl group Chemical group 0.000 claims abstract description 25
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims abstract description 25
- 150000003839 salts Chemical class 0.000 claims abstract description 22
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims abstract description 15
- 125000000719 pyrrolidinyl group Chemical group 0.000 claims abstract description 13
- 125000002757 morpholinyl group Chemical group 0.000 claims abstract description 11
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- 125000000008 (C1-C10) alkyl group Chemical group 0.000 claims abstract description 7
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 claims abstract description 7
- 125000000623 heterocyclic group Chemical group 0.000 claims abstract description 5
- YPJKMVATUPSWOH-UHFFFAOYSA-N nitrooxidanyl Chemical group [O][N+]([O-])=O YPJKMVATUPSWOH-UHFFFAOYSA-N 0.000 claims abstract description 4
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims abstract description 4
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims abstract 22
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- 125000005843 halogen group Chemical group 0.000 claims description 59
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 43
- 125000001153 fluoro group Chemical group F* 0.000 claims description 41
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- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims description 23
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- 125000003226 pyrazolyl group Chemical group 0.000 claims description 17
- 201000010099 disease Diseases 0.000 claims description 16
- 125000000842 isoxazolyl group Chemical group 0.000 claims description 16
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- 125000001995 cyclobutyl group Chemical group [H]C1([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims description 14
- 125000001511 cyclopentyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims description 14
- 125000003373 pyrazinyl group Chemical group 0.000 claims description 14
- 125000004029 hydroxymethyl group Chemical group [H]OC([H])([H])* 0.000 claims description 13
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- 125000004172 4-methoxyphenyl group Chemical group [H]C1=C([H])C(OC([H])([H])[H])=C([H])C([H])=C1* 0.000 claims description 11
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- 125000000168 pyrrolyl group Chemical group 0.000 claims description 11
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- LMBFAGIMSUYTBN-MPZNNTNKSA-N teixobactin Chemical compound C([C@H](C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CO)C(=O)N[C@H](CCC(N)=O)C(=O)N[C@H]([C@@H](C)CC)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CO)C(=O)N[C@H]1C(N[C@@H](C)C(=O)N[C@@H](C[C@@H]2NC(=N)NC2)C(=O)N[C@H](C(=O)O[C@H]1C)[C@@H](C)CC)=O)NC)C1=CC=CC=C1 LMBFAGIMSUYTBN-MPZNNTNKSA-N 0.000 claims description 6
- 125000003507 tetrahydrothiofenyl group Chemical group 0.000 claims description 6
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 5
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- WKBOTKDWSSQWDR-UHFFFAOYSA-N Bromine atom Chemical group [Br] WKBOTKDWSSQWDR-UHFFFAOYSA-N 0.000 claims description 3
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- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims description 3
- 125000004454 (C1-C6) alkoxycarbonyl group Chemical group 0.000 claims description 2
- SBUKLPSBNFWJCU-UHFFFAOYSA-N ClIBr Chemical group ClIBr SBUKLPSBNFWJCU-UHFFFAOYSA-N 0.000 claims description 2
- 125000000587 piperidin-1-yl group Chemical group [H]C1([H])N(*)C([H])([H])C([H])([H])C([H])([H])C1([H])[H] 0.000 claims description 2
- 125000004482 piperidin-4-yl group Chemical group N1CCC(CC1)* 0.000 claims description 2
- 150000002431 hydrogen Chemical class 0.000 claims 27
- MDFFNEOEWAXZRQ-UHFFFAOYSA-N aminyl Chemical compound [NH2] MDFFNEOEWAXZRQ-UHFFFAOYSA-N 0.000 claims 1
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- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract 1
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- YMWUJEATGCHHMB-UHFFFAOYSA-N Dichloromethane Chemical compound ClCCl YMWUJEATGCHHMB-UHFFFAOYSA-N 0.000 description 99
- 239000000243 solution Substances 0.000 description 94
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- XBXCNNQPRYLIDE-UHFFFAOYSA-M n-tert-butylcarbamate Chemical compound CC(C)(C)NC([O-])=O XBXCNNQPRYLIDE-UHFFFAOYSA-M 0.000 description 1
- XWESXZZECGOXDQ-UHFFFAOYSA-N n-tert-butylhydroxylamine Chemical compound CC(C)(C)NO XWESXZZECGOXDQ-UHFFFAOYSA-N 0.000 description 1
- 125000001624 naphthyl group Chemical group 0.000 description 1
- 125000001971 neopentyl group Chemical group [H]C([*])([H])C(C([H])([H])[H])(C([H])([H])[H])C([H])([H])[H] 0.000 description 1
- 230000030363 nerve development Effects 0.000 description 1
- 230000001537 neural effect Effects 0.000 description 1
- 210000002569 neuron Anatomy 0.000 description 1
- 125000004433 nitrogen atom Chemical group N* 0.000 description 1
- 125000006574 non-aromatic ring group Chemical group 0.000 description 1
- 125000002868 norbornyl group Chemical group C12(CCC(CC1)C2)* 0.000 description 1
- XZTSFVPMMQNIAJ-UHFFFAOYSA-N o-(2-ethenoxyethyl)hydroxylamine Chemical group NOCCOC=C XZTSFVPMMQNIAJ-UHFFFAOYSA-N 0.000 description 1
- 239000002674 ointment Substances 0.000 description 1
- 239000008203 oral pharmaceutical composition Substances 0.000 description 1
- 150000007524 organic acids Chemical class 0.000 description 1
- NFHFRUOZVGFOOS-UHFFFAOYSA-N palladium;triphenylphosphane Chemical compound [Pd].C1=CC=CC=C1P(C=1C=CC=CC=1)C1=CC=CC=C1.C1=CC=CC=C1P(C=1C=CC=CC=1)C1=CC=CC=C1.C1=CC=CC=C1P(C=1C=CC=CC=1)C1=CC=CC=C1.C1=CC=CC=C1P(C=1C=CC=CC=1)C1=CC=CC=C1 NFHFRUOZVGFOOS-UHFFFAOYSA-N 0.000 description 1
- 238000007911 parenteral administration Methods 0.000 description 1
- 239000006072 paste Substances 0.000 description 1
- 230000037361 pathway Effects 0.000 description 1
- 239000013610 patient sample Substances 0.000 description 1
- 238000002732 pharmacokinetic assay Methods 0.000 description 1
- 239000012071 phase Substances 0.000 description 1
- 229910052698 phosphorus Inorganic materials 0.000 description 1
- 239000011574 phosphorus Substances 0.000 description 1
- 239000003757 phosphotransferase inhibitor Substances 0.000 description 1
- 229920000642 polymer Polymers 0.000 description 1
- 238000002600 positron emission tomography Methods 0.000 description 1
- 229910000027 potassium carbonate Inorganic materials 0.000 description 1
- 239000000843 powder Substances 0.000 description 1
- 239000002244 precipitate Substances 0.000 description 1
- 230000008569 process Effects 0.000 description 1
- 238000012545 processing Methods 0.000 description 1
- 230000006920 protein precipitation Effects 0.000 description 1
- 125000000714 pyrimidinyl group Chemical group 0.000 description 1
- 238000010791 quenching Methods 0.000 description 1
- 125000002943 quinolinyl group Chemical group N1=C(C=CC2=CC=CC=C12)* 0.000 description 1
- 238000011084 recovery Methods 0.000 description 1
- 238000011160 research Methods 0.000 description 1
- 125000002914 sec-butyl group Chemical group [H]C([H])([H])C([H])([H])C([H])(*)C([H])([H])[H] 0.000 description 1
- 125000003548 sec-pentyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])[H] 0.000 description 1
- 102000034285 signal transducing proteins Human genes 0.000 description 1
- 108091006024 signal transducing proteins Proteins 0.000 description 1
- 239000011780 sodium chloride Substances 0.000 description 1
- BEOOHQFXGBMRKU-UHFFFAOYSA-N sodium cyanoborohydride Chemical compound [Na+].[B-]C#N BEOOHQFXGBMRKU-UHFFFAOYSA-N 0.000 description 1
- QDRKDTQENPPHOJ-UHFFFAOYSA-N sodium ethoxide Chemical compound [Na+].CC[O-] QDRKDTQENPPHOJ-UHFFFAOYSA-N 0.000 description 1
- CMZUMMUJMWNLFH-UHFFFAOYSA-N sodium metavanadate Chemical compound [Na+].[O-][V](=O)=O CMZUMMUJMWNLFH-UHFFFAOYSA-N 0.000 description 1
- 239000012439 solid excipient Substances 0.000 description 1
- 239000007858 starting material Substances 0.000 description 1
- 239000008174 sterile solution Substances 0.000 description 1
- 230000004936 stimulating effect Effects 0.000 description 1
- 230000000638 stimulation Effects 0.000 description 1
- 238000007920 subcutaneous administration Methods 0.000 description 1
- 239000000829 suppository Substances 0.000 description 1
- 239000003765 sweetening agent Substances 0.000 description 1
- OWRVZENYEUUFKU-QFBILLFUSA-N tert-butyl (2R,4S)-2-(2,5-difluorophenyl)-4-(4-nitrobenzoyl)oxypyrrolidine-1-carboxylate Chemical compound FC1=C(C=C(C=C1)F)[C@@H]1N(C[C@H](C1)OC(C1=CC=C(C=C1)[N+](=O)[O-])=O)C(=O)OC(C)(C)C OWRVZENYEUUFKU-QFBILLFUSA-N 0.000 description 1
- SYENXVCLSYZWBK-GXFFZTMASA-N tert-butyl (2R,4S)-2-(2,5-difluorophenyl)-4-fluoropyrrolidine-1-carboxylate Chemical compound FC1=C(C=C(C=C1)F)[C@@H]1N(C[C@H](C1)F)C(=O)OC(C)(C)C SYENXVCLSYZWBK-GXFFZTMASA-N 0.000 description 1
- SYENXVCLSYZWBK-GWCFXTLKSA-N tert-butyl (2S,4S)-2-(2,5-difluorophenyl)-4-fluoropyrrolidine-1-carboxylate Chemical compound FC1=C(C=C(C=C1)F)[C@H]1N(C[C@H](C1)F)C(=O)OC(C)(C)C SYENXVCLSYZWBK-GWCFXTLKSA-N 0.000 description 1
- GJJYYMXBCYYXPQ-UHFFFAOYSA-N tert-butyl 2-oxopyrrolidine-1-carboxylate Chemical compound CC(C)(C)OC(=O)N1CCCC1=O GJJYYMXBCYYXPQ-UHFFFAOYSA-N 0.000 description 1
- UDCCOLDRWMCMFI-NNJIEVJOSA-N tert-butyl N-[(2R)-2-[tert-butyl(dimethyl)silyl]oxy-4-(2,5-difluorophenyl)-4-hydroxybutyl]carbamate Chemical compound [Si](C)(C)(C(C)(C)C)O[C@@H](CNC(OC(C)(C)C)=O)CC(O)C1=C(C=CC(=C1)F)F UDCCOLDRWMCMFI-NNJIEVJOSA-N 0.000 description 1
- BCNZYOJHNLTNEZ-UHFFFAOYSA-N tert-butyldimethylsilyl chloride Chemical compound CC(C)(C)[Si](C)(C)Cl BCNZYOJHNLTNEZ-UHFFFAOYSA-N 0.000 description 1
- 125000001981 tert-butyldimethylsilyl group Chemical group [H]C([H])([H])[Si]([H])(C([H])([H])[H])[*]C(C([H])([H])[H])(C([H])([H])[H])C([H])([H])[H] 0.000 description 1
- 238000012360 testing method Methods 0.000 description 1
- DPKBAXPHAYBPRL-UHFFFAOYSA-M tetrabutylazanium;iodide Chemical compound [I-].CCCC[N+](CCCC)(CCCC)CCCC DPKBAXPHAYBPRL-UHFFFAOYSA-M 0.000 description 1
- 125000005958 tetrahydrothienyl group Chemical group 0.000 description 1
- 125000003831 tetrazolyl group Chemical group 0.000 description 1
- 230000001225 therapeutic effect Effects 0.000 description 1
- 201000002510 thyroid cancer Diseases 0.000 description 1
- 210000001519 tissue Anatomy 0.000 description 1
- 238000003354 tissue distribution assay Methods 0.000 description 1
- 230000000699 topical effect Effects 0.000 description 1
- 230000001988 toxicity Effects 0.000 description 1
- 231100000419 toxicity Toxicity 0.000 description 1
- 125000004306 triazinyl group Chemical group 0.000 description 1
- 125000001425 triazolyl group Chemical group 0.000 description 1
- 239000001993 wax Substances 0.000 description 1
Classifications
-
- 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
-
- 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
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
-
- 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
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
Landscapes
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Epidemiology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201610970314 | 2016-10-28 | ||
| CN201710044000 | 2017-01-21 | ||
| PCT/CN2017/108100 WO2018077246A1 (zh) | 2016-10-28 | 2017-10-27 | 用作神经营养因子酪氨酸激酶受体抑制剂的氨基吡唑并嘧啶化合物 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ES2896943T3 true ES2896943T3 (es) | 2022-02-28 |
Family
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ES17863410T Active ES2896943T3 (es) | 2016-10-28 | 2017-10-27 | Compuesto de amino pirazolopirimidina usado como inhibidor de receptores con actividad tirosina quinasa de factores neurotróficos |
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| EP (1) | EP3533796B1 (enExample) |
| JP (1) | JP7046940B2 (enExample) |
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| CN (1) | CN109890820B (enExample) |
| AU (1) | AU2017348826B2 (enExample) |
| CA (1) | CA3041942C (enExample) |
| DK (1) | DK3533796T3 (enExample) |
| ES (1) | ES2896943T3 (enExample) |
| HU (1) | HUE057733T2 (enExample) |
| MX (1) | MX380283B (enExample) |
| PL (1) | PL3533796T3 (enExample) |
| PT (1) | PT3533796T (enExample) |
| RU (1) | RU2764523C2 (enExample) |
| WO (1) | WO2018077246A1 (enExample) |
Families Citing this family (16)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| PT3658148T (pt) * | 2017-07-28 | 2024-08-26 | Turning Point Therapeutics Inc | Compostos macrocíclicos e utilizações dos mesmos |
| KR102619444B1 (ko) | 2017-08-23 | 2023-12-29 | 치아타이 티안큉 파마수티컬 그룹 주식회사 | 아미노피라졸 및 피리미딘을 함유하는 마크로사이클 및 그의 약학적 조성물 및 용도 |
| CN108794370A (zh) * | 2018-07-31 | 2018-11-13 | 上海弈柯莱生物医药科技有限公司 | 一种拉罗替尼中间体的制备方法 |
| TW202033526A (zh) * | 2018-12-07 | 2020-09-16 | 大陸商貝達藥業股份有限公司 | 用作酪胺酸激酶抑制劑的化合物、包含其的藥物組合物及其用途 |
| WO2020187291A1 (zh) | 2019-03-19 | 2020-09-24 | 华中师范大学 | 吡唑并嘧啶化合物和药物组合物及其应用 |
| CN112979654B (zh) * | 2019-12-16 | 2024-03-19 | 赛诺哈勃药业（成都）有限公司 | 杂芳基稠环化合物、其制备方法及应用 |
| WO2021249450A1 (zh) * | 2020-06-11 | 2021-12-16 | 贝达药业股份有限公司 | 酪氨酸激酶抑制剂的盐型、晶型、药物组合物及其用途 |
| CN111620881B (zh) * | 2020-07-08 | 2023-03-31 | 浙江合聚生物医药有限公司 | 拉罗替尼衍生物及其制备方法和应用 |
| CN113563343B (zh) * | 2020-07-27 | 2022-05-24 | 杭州邦顺制药有限公司 | 取代的吡唑并[1,5-a]嘧啶化合物及其用途 |
| CN112010860B (zh) * | 2020-08-05 | 2023-03-10 | 南京纳丁菲医药科技有限公司 | 苄氧基吡唑并嘧啶化合物和药物组合物及其应用 |
| CN114437075B (zh) * | 2020-11-03 | 2026-01-30 | 上海瑶琪生物科技有限公司 | 用作ntrk激酶抑制剂的化合物及其应用 |
| CN113200963A (zh) * | 2021-03-31 | 2021-08-03 | 广东石油化工学院 | N-(吡咯基)-3-吡唑基胺及其制备方法 |
| EP4335441B1 (en) * | 2021-05-03 | 2025-05-28 | JBKLAB Co., Ltd. | Pharmaceutical composition for preventing, alleviating, or treating cancer, containing 2,6-dichloro-4-(4-(4-hydroxycyclohexylamino)-7h-pyrrolo[2,3-d]pyrimidin-5-yl)phenol as active ingredient |
| CN117751121A (zh) * | 2021-07-30 | 2024-03-22 | 正大天晴药业集团股份有限公司 | 氨基吡唑并嘧啶化合物的晶体 |
| WO2023011616A1 (zh) * | 2021-08-06 | 2023-02-09 | 正大天晴药业集团股份有限公司 | 氨基吡唑并嘧啶化合物在治疗trk激酶介导的肿瘤中的用途 |
| CN117088800B (zh) * | 2023-08-18 | 2024-05-28 | 龙曦宁（上海）医药科技有限公司 | 一种5-甲基吡咯烷-3-醇盐酸盐的制备方法 |
Family Cites Families (15)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE10356579A1 (de) * | 2003-12-04 | 2005-07-07 | Merck Patent Gmbh | Aminderivate |
| CA2722418C (en) | 2008-05-13 | 2013-09-17 | Irm Llc | Fused nitrogen containing heterocycles and compositions thereof as kinase inhibitors |
| CA2727250A1 (en) | 2008-07-01 | 2010-01-07 | Genentech, Inc. | Bicyclic heterocycles as mek kinase inhibitors |
| SI2350075T1 (sl) | 2008-09-22 | 2014-06-30 | Array Biopharma, Inc. | Substituirane imidazo (1,2b)piridazinske spojine kot Trk kinazni inhibitorji |
| CN102264736B (zh) * | 2008-10-22 | 2013-08-14 | 阵列生物制药公司 | 作为TRK激酶抑制剂的取代的吡唑并[1,5-a]嘧啶化合物 |
| AR077468A1 (es) | 2009-07-09 | 2011-08-31 | Array Biopharma Inc | Compuestos de pirazolo (1,5 -a) pirimidina sustituidos como inhibidores de trk- quinasa |
| WO2012034095A1 (en) * | 2010-09-09 | 2012-03-15 | Irm Llc | Compounds and compositions as trk inhibitors |
| BR112013021638A2 (pt) | 2011-02-25 | 2016-08-02 | Irm Llc | "compostos inibidores de trk, seu uso e composições que os compreendem" |
| WO2013028263A1 (en) * | 2011-08-24 | 2013-02-28 | Glaxosmithkline Llc | Pyrazolopyrimidine derivatives as pi3 kinase inhibitors |
| KR20140105508A (ko) | 2011-12-12 | 2014-09-01 | 닥터 레디스 레보러터리즈 리미티드 | 트로포미오신 수용체 키나제(Trk) 억제제인 치환된 피라졸로[1,5-a]피리딘 |
| MX362181B (es) | 2013-02-19 | 2019-01-08 | Ono Pharmaceutical Co | Compuesto inhibidor de cinasa del receptor de tropomiosina (trk). |
| EP2970288A1 (en) * | 2013-03-15 | 2016-01-20 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of atr kinase |
| CN104650092B (zh) | 2013-11-16 | 2017-11-10 | 广东东阳光药业有限公司 | 取代的杂芳基化合物及其组合物和用途 |
| HUE046727T2 (hu) * | 2013-12-06 | 2020-03-30 | Vertex Pharma | Az ATR-kináz inhibitoraként használható vegyület, 2-amino-6-fluoro-N-[5-fluoro-piridin-3-IL]-pirazolo-[1,5-A]-pirimidin-3-karboxamid, ennek elõállítása, különbözõ szilárd formái és ezek radioaktív nyomjelzett származékai |
| HUE067779T2 (hu) * | 2014-12-15 | 2024-11-28 | Cmg Pharmaceutical Co Ltd | Kondenzált gyûrûs heteroaril vegyületek és azok felhasználása TRK inhibitorokként |
-
2017
- 2017-10-27 AU AU2017348826A patent/AU2017348826B2/en active Active
- 2017-10-27 ES ES17863410T patent/ES2896943T3/es active Active
- 2017-10-27 PL PL17863410T patent/PL3533796T3/pl unknown
- 2017-10-27 DK DK17863410.1T patent/DK3533796T3/da active
- 2017-10-27 WO PCT/CN2017/108100 patent/WO2018077246A1/zh not_active Ceased
- 2017-10-27 US US16/345,679 patent/US10829492B2/en active Active
- 2017-10-27 HU HUE17863410A patent/HUE057733T2/hu unknown
- 2017-10-27 RU RU2019114600A patent/RU2764523C2/ru active
- 2017-10-27 EP EP17863410.1A patent/EP3533796B1/en active Active
- 2017-10-27 MX MX2019004847A patent/MX380283B/es unknown
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- 2017-10-27 CA CA3041942A patent/CA3041942C/en active Active
- 2017-10-27 PT PT178634101T patent/PT3533796T/pt unknown
- 2017-10-27 KR KR1020197015241A patent/KR102616249B1/ko active Active
- 2017-10-27 CN CN201780064022.6A patent/CN109890820B/zh active Active
Also Published As
| Publication number | Publication date |
|---|---|
| PL3533796T3 (pl) | 2022-01-17 |
| DK3533796T3 (da) | 2021-11-08 |
| MX2019004847A (es) | 2019-08-29 |
| AU2017348826A1 (en) | 2019-05-23 |
| MX380283B (es) | 2025-03-12 |
| RU2019114600A3 (enExample) | 2021-02-20 |
| JP7046940B2 (ja) | 2022-04-04 |
| CN109890820A (zh) | 2019-06-14 |
| CA3041942C (en) | 2023-03-14 |
| RU2764523C2 (ru) | 2022-01-18 |
| US20190352306A1 (en) | 2019-11-21 |
| KR102616249B1 (ko) | 2023-12-21 |
| BR112019008656A8 (pt) | 2022-06-07 |
| JP2019537588A (ja) | 2019-12-26 |
| HUE057733T2 (hu) | 2022-06-28 |
| CN109890820B (zh) | 2020-11-03 |
| PT3533796T (pt) | 2021-11-18 |
| RU2019114600A (ru) | 2020-11-30 |
| CA3041942A1 (en) | 2018-05-03 |
| EP3533796A4 (en) | 2020-06-03 |
| EP3533796B1 (en) | 2021-09-29 |
| US10829492B2 (en) | 2020-11-10 |
| BR112019008656A2 (pt) | 2019-07-09 |
| WO2018077246A1 (zh) | 2018-05-03 |
| KR20190067913A (ko) | 2019-06-17 |
| AU2017348826B2 (en) | 2021-12-02 |
| EP3533796A1 (en) | 2019-09-04 |
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