JP2015537001A5 - - Google Patents
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- JP2015537001A5 JP2015537001A5 JP2015542038A JP2015542038A JP2015537001A5 JP 2015537001 A5 JP2015537001 A5 JP 2015537001A5 JP 2015542038 A JP2015542038 A JP 2015542038A JP 2015542038 A JP2015542038 A JP 2015542038A JP 2015537001 A5 JP2015537001 A5 JP 2015537001A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- alkoxy
- optionally substituted
- pharmaceutically acceptable
- acceptable salt
- 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
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- 125000000217 alkyl group Chemical group 0.000 claims description 299
- 125000003545 alkoxy group Chemical group 0.000 claims description 203
- 150000001875 compounds Chemical class 0.000 claims description 107
- 125000001153 fluoro group Chemical group F* 0.000 claims description 60
- 150000003839 salts Chemical class 0.000 claims description 46
- 229910052736 halogen Inorganic materials 0.000 claims description 43
- 150000002367 halogens Chemical class 0.000 claims description 43
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims description 42
- 125000005842 heteroatom Chemical group 0.000 claims description 41
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 39
- 239000012453 solvate Substances 0.000 claims description 34
- 125000004429 atom Chemical group 0.000 claims description 28
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims description 22
- -1 hydroxyl-carbonyl Chemical group 0.000 claims description 20
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 claims description 19
- 125000004093 cyano group Chemical group *C#N 0.000 claims description 18
- 208000002193 Pain Diseases 0.000 claims description 17
- 229910052760 oxygen Inorganic materials 0.000 claims description 15
- PQIOSYKVBBWRRI-UHFFFAOYSA-N methylphosphonyl difluoride Chemical group CP(F)(F)=O PQIOSYKVBBWRRI-UHFFFAOYSA-N 0.000 claims description 14
- 230000008878 coupling Effects 0.000 claims description 13
- 238000010168 coupling process Methods 0.000 claims description 13
- 238000005859 coupling reaction Methods 0.000 claims description 13
- 125000000623 heterocyclic group Chemical group 0.000 claims description 13
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 13
- 238000000034 method Methods 0.000 claims description 12
- 206010028980 Neoplasm Diseases 0.000 claims description 11
- 201000011510 cancer Diseases 0.000 claims description 11
- 229910052717 sulfur Inorganic materials 0.000 claims description 11
- 125000004390 alkyl sulfonyl group Chemical group 0.000 claims description 10
- 125000004043 oxo group Chemical group O=* 0.000 claims description 10
- 125000004414 alkyl thio group Chemical group 0.000 claims description 9
- 229910052757 nitrogen Inorganic materials 0.000 claims description 9
- 125000002252 acyl group Chemical group 0.000 claims description 8
- 125000004453 alkoxycarbonyl group Chemical group 0.000 claims description 8
- ORTFAQDWJHRMNX-UHFFFAOYSA-N hydroxidooxidocarbon(.) Chemical group O[C]=O ORTFAQDWJHRMNX-UHFFFAOYSA-N 0.000 claims description 8
- 125000001424 substituent group Chemical group 0.000 claims description 8
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 claims description 6
- 208000032131 Diabetic Neuropathies Diseases 0.000 claims description 6
- 201000009273 Endometriosis Diseases 0.000 claims description 6
- 208000000450 Pelvic Pain Diseases 0.000 claims description 6
- 208000021386 Sjogren Syndrome Diseases 0.000 claims description 6
- 125000005157 alkyl carboxy group Chemical group 0.000 claims description 6
- 125000005422 alkyl sulfonamido group Chemical group 0.000 claims description 6
- 125000002393 azetidinyl group Chemical group 0.000 claims description 6
- 229910052799 carbon Inorganic materials 0.000 claims description 6
- 125000004432 carbon atom Chemical group C* 0.000 claims description 6
- 125000004966 cyanoalkyl group Chemical group 0.000 claims description 6
- 208000027866 inflammatory disease Diseases 0.000 claims description 6
- 230000004770 neurodegeneration Effects 0.000 claims description 6
- 208000015122 neurodegenerative disease Diseases 0.000 claims description 6
- 125000004433 nitrogen atom Chemical group N* 0.000 claims description 6
- 125000003566 oxetanyl group Chemical group 0.000 claims description 6
- 201000007094 prostatitis Diseases 0.000 claims description 6
- 208000011580 syndromic disease Diseases 0.000 claims description 6
- 125000001889 triflyl group Chemical group FC(F)(F)S(*)(=O)=O 0.000 claims description 6
- 206010061218 Inflammation Diseases 0.000 claims description 5
- 229910052739 hydrogen Inorganic materials 0.000 claims description 5
- 239000001257 hydrogen Substances 0.000 claims description 5
- 230000004054 inflammatory process Effects 0.000 claims description 5
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical group [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims description 4
- 125000004694 alkoxyaminocarbonyl group Chemical group 0.000 claims description 4
- 150000001408 amides Chemical class 0.000 claims description 4
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 claims description 4
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims description 4
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 4
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims description 4
- 208000015181 infectious disease Diseases 0.000 claims description 4
- 229920006395 saturated elastomer Polymers 0.000 claims description 4
- NVBFHJWHLNUMCV-UHFFFAOYSA-N sulfamide Chemical compound NS(N)(=O)=O NVBFHJWHLNUMCV-UHFFFAOYSA-N 0.000 claims description 4
- 241000124008 Mammalia Species 0.000 claims description 3
- 125000006163 5-membered heteroaryl group Chemical group 0.000 claims description 2
- 208000031261 Acute myeloid leukaemia Diseases 0.000 claims description 2
- 206010009944 Colon cancer Diseases 0.000 claims description 2
- 208000001333 Colorectal Neoplasms Diseases 0.000 claims description 2
- 208000035473 Communicable disease Diseases 0.000 claims description 2
- 201000010915 Glioblastoma multiforme Diseases 0.000 claims description 2
- 208000033776 Myeloid Acute Leukemia Diseases 0.000 claims description 2
- 101150111783 NTRK1 gene Proteins 0.000 claims description 2
- 206010029260 Neuroblastoma Diseases 0.000 claims description 2
- 206010033701 Papillary thyroid cancer Diseases 0.000 claims description 2
- 206010060862 Prostate cancer Diseases 0.000 claims description 2
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims description 2
- 230000004913 activation Effects 0.000 claims description 2
- SIISYXWWQBUDOP-UHFFFAOYSA-N bis(1h-imidazol-2-yl)methanethione Chemical compound N=1C=CNC=1C(=S)C1=NC=CN1 SIISYXWWQBUDOP-UHFFFAOYSA-N 0.000 claims description 2
- PFKFTWBEEFSNDU-UHFFFAOYSA-N carbonyldiimidazole Chemical compound C1=CN=CN1C(=O)N1C=CN=C1 PFKFTWBEEFSNDU-UHFFFAOYSA-N 0.000 claims description 2
- 201000010989 colorectal carcinoma Diseases 0.000 claims description 2
- 125000001995 cyclobutyl group Chemical group [H]C1([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims description 2
- 239000003085 diluting agent Substances 0.000 claims description 2
- MKRTXPORKIRPDG-UHFFFAOYSA-N diphenylphosphoryl azide Chemical compound C=1C=CC=CC=1P(=O)(N=[N+]=[N-])C1=CC=CC=C1 MKRTXPORKIRPDG-UHFFFAOYSA-N 0.000 claims description 2
- 201000010099 disease Diseases 0.000 claims description 2
- 208000035475 disorder Diseases 0.000 claims description 2
- 239000003814 drug Substances 0.000 claims description 2
- 229940079593 drug Drugs 0.000 claims description 2
- 230000008482 dysregulation Effects 0.000 claims description 2
- 208000021045 exocrine pancreatic carcinoma Diseases 0.000 claims description 2
- 206010017758 gastric cancer Diseases 0.000 claims description 2
- 208000010749 gastric carcinoma Diseases 0.000 claims description 2
- 208000005017 glioblastoma Diseases 0.000 claims description 2
- 201000001441 melanoma Diseases 0.000 claims description 2
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims description 2
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 2
- 201000002120 neuroendocrine carcinoma Diseases 0.000 claims description 2
- 208000002154 non-small cell lung carcinoma Diseases 0.000 claims description 2
- 125000004430 oxygen atom Chemical group O* 0.000 claims description 2
- 208000008443 pancreatic carcinoma Diseases 0.000 claims description 2
- 239000008194 pharmaceutical composition Substances 0.000 claims description 2
- 125000006239 protecting group Chemical group 0.000 claims description 2
- 125000006413 ring segment Chemical group 0.000 claims description 2
- 206010041823 squamous cell carcinoma Diseases 0.000 claims description 2
- 201000000498 stomach carcinoma Diseases 0.000 claims description 2
- 208000030045 thyroid gland papillary carcinoma Diseases 0.000 claims description 2
- UCPYLLCMEDAXFR-UHFFFAOYSA-N triphosgene Chemical compound ClC(Cl)(Cl)OC(=O)OC(Cl)(Cl)Cl UCPYLLCMEDAXFR-UHFFFAOYSA-N 0.000 claims description 2
- 208000029729 tumor suppressor gene on chromosome 11 Diseases 0.000 claims description 2
- 239000000203 mixture Substances 0.000 claims 15
- 208000000094 Chronic Pain Diseases 0.000 claims 1
- 206010065390 Inflammatory pain Diseases 0.000 claims 1
- 208000005298 acute pain Diseases 0.000 claims 1
- 230000002757 inflammatory effect Effects 0.000 claims 1
- 208000004296 neuralgia Diseases 0.000 claims 1
- 208000021722 neuropathic pain Diseases 0.000 claims 1
- 238000001356 surgical procedure Methods 0.000 claims 1
- 125000004422 alkyl sulphonamide group Chemical group 0.000 description 2
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 description 1
- 125000001072 heteroaryl group Chemical group 0.000 description 1
- 125000004950 trifluoroalkyl group Chemical group 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201261725925P | 2012-11-13 | 2012-11-13 | |
| US61/725,925 | 2012-11-13 | ||
| PCT/US2013/069951 WO2014078454A1 (en) | 2012-11-13 | 2013-11-13 | Bicyclic urea, thiourea, guanidine and cyanoguanidine compounds useful for the treatment of pain |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2017211949A Division JP2018016649A (ja) | 2012-11-13 | 2017-11-01 | 疼痛の治療に有用な二環式尿素、チオ尿素、グアニジン、およびシアノグアニジン化合物 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2015537001A JP2015537001A (ja) | 2015-12-24 |
| JP2015537001A5 true JP2015537001A5 (https=) | 2016-12-08 |
| JP6345684B2 JP6345684B2 (ja) | 2018-06-20 |
Family
ID=49667614
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015542038A Expired - Fee Related JP6345684B2 (ja) | 2012-11-13 | 2013-11-13 | 疼痛の治療に有用な二環式尿素、チオ尿素、グアニジン、およびシアノグアニジン化合物 |
| JP2017211949A Withdrawn JP2018016649A (ja) | 2012-11-13 | 2017-11-01 | 疼痛の治療に有用な二環式尿素、チオ尿素、グアニジン、およびシアノグアニジン化合物 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2017211949A Withdrawn JP2018016649A (ja) | 2012-11-13 | 2017-11-01 | 疼痛の治療に有用な二環式尿素、チオ尿素、グアニジン、およびシアノグアニジン化合物 |
Country Status (30)
| Country | Link |
|---|---|
| US (2) | US10351575B2 (https=) |
| EP (1) | EP2920166B1 (https=) |
| JP (2) | JP6345684B2 (https=) |
| KR (1) | KR102181913B1 (https=) |
| CN (1) | CN104903310B (https=) |
| AU (3) | AU2013344886B2 (https=) |
| BR (1) | BR112015011010B1 (https=) |
| CA (1) | CA2891334C (https=) |
| CL (1) | CL2015001282A1 (https=) |
| CR (1) | CR20150264A (https=) |
| CY (1) | CY1118468T1 (https=) |
| DK (1) | DK2920166T3 (https=) |
| ES (1) | ES2610975T3 (https=) |
| HR (1) | HRP20161613T1 (https=) |
| HU (1) | HUE031557T2 (https=) |
| IL (1) | IL238498A (https=) |
| LT (1) | LT2920166T (https=) |
| ME (1) | ME02879B (https=) |
| MX (1) | MX366761B (https=) |
| PH (1) | PH12015500938B1 (https=) |
| PL (1) | PL2920166T3 (https=) |
| PT (1) | PT2920166T (https=) |
| RS (1) | RS55593B1 (https=) |
| RU (1) | RU2664541C2 (https=) |
| SG (1) | SG11201503731SA (https=) |
| SI (1) | SI2920166T1 (https=) |
| SM (2) | SMT201700034T1 (https=) |
| UA (1) | UA117573C2 (https=) |
| WO (1) | WO2014078454A1 (https=) |
| ZA (1) | ZA201503580B (https=) |
Families Citing this family (60)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2010033941A1 (en) | 2008-09-22 | 2010-03-25 | Array Biopharma Inc. | Substituted imidazo[1,2b]pyridazine compounds as trk kinase inhibitors |
| MY169791A (en) | 2008-10-22 | 2019-05-15 | Array Biopharma Inc | Substituted pyrazolo [1,5-a] pyrimidine compounds as trk kinase inhibitors |
| AR077468A1 (es) | 2009-07-09 | 2011-08-31 | Array Biopharma Inc | Compuestos de pirazolo (1,5 -a) pirimidina sustituidos como inhibidores de trk- quinasa |
| ME03376B (me) | 2010-05-20 | 2020-01-20 | Array Biopharma Inc | Makrociklička jedinjenja kао inhibiтori trk kinaze |
| CA2835835C (en) | 2011-05-13 | 2019-04-02 | Array Biopharma Inc. | Pyrrolidinyl urea and pyrrolidinyl thiourea compounds as trka kinase inhibitors |
| WO2014078331A1 (en) | 2012-11-13 | 2014-05-22 | Array Biopharma Inc. | N-(arylalkyl)-n'-pyrazolyl-urea, thiourea, guanidine and cyanoguanidine compounds as trka kinase inhibitors |
| MX374242B (es) | 2012-11-13 | 2025-03-05 | Array Biopharma Inc | Compuestos de n-pirrolidinil, n' -pirazolil-urea, tiourea, guanidina y cianoguanidina como inhibidores de trka cinasa. |
| WO2014078325A1 (en) | 2012-11-13 | 2014-05-22 | Array Biopharma Inc. | N-(monocyclic aryl),n'-pyrazolyl-urea, thiourea, guanidine and cyanoguanidine compounds as trka kinase inhibitors |
| US9981959B2 (en) | 2012-11-13 | 2018-05-29 | Array Biopharma Inc. | Thiazolyl and oxazolyl urea, thiourea, guanidine and cyanoguanidine compounds as TrkA kinase inhibitors |
| WO2014078328A1 (en) | 2012-11-13 | 2014-05-22 | Array Biopharma Inc. | N-bicyclic aryl,n'-pyrazolyl urea, thiourea, guanidine and cyanoguanidine compounds as trka kinase inhibitors |
| RS55593B1 (sr) | 2012-11-13 | 2017-06-30 | Array Biopharma Inc | Jedinjenja biciklične uree, tiouree, guanidina i cijanoguanidina korisna za lečenje bola |
| WO2014078378A1 (en) | 2012-11-13 | 2014-05-22 | Array Biopharma Inc. | Pyrrolidinyl urea, thiourea, guanidine and cyanoguanidine compounds as trka kinase inhibitors |
| WO2014078372A1 (en) | 2012-11-13 | 2014-05-22 | Array Biopharma Inc. | Pyrrolidinyl urea, thiourea, guanidine and cyanoguanidine compounds as trka kinase inhibitors |
| WO2014078417A1 (en) | 2012-11-13 | 2014-05-22 | Array Biopharma Inc. | Pyrazolyl urea, thiourea, guanidine and cyanoguanidine compounds as trka kinase inhibitors |
| US9822118B2 (en) | 2012-11-13 | 2017-11-21 | Array Biopharma Inc. | Bicyclic heteroaryl urea, thiourea, guanidine and cyanoguanidine compounds as TrkA kinase inhibitors |
| MA40434B1 (fr) | 2014-05-15 | 2019-09-30 | Array Biopharma Inc | 1-((3s,4r)-4-(3-fluorophényl)-1-(2-méthoxyéthyl)pyrrolidin-3-yl)-3-(4-méthyl-3-(2-méthylpyrimidin-5-yl)-1-phényl-1h-pyrazol-5-yl)urée comme inhibiteur de la kinase trka |
| WO2016021629A1 (ja) | 2014-08-06 | 2016-02-11 | 塩野義製薬株式会社 | TrkA阻害活性を有する複素環および炭素環誘導体 |
| CN113354649B (zh) | 2014-11-16 | 2024-12-10 | 阵列生物制药公司 | 一种新的晶型 |
| JP6812059B2 (ja) | 2015-07-07 | 2021-01-13 | 塩野義製薬株式会社 | TrkA阻害活性を有する複素環誘導体 |
| BR112018000808A2 (pt) | 2015-07-16 | 2018-09-04 | Array Biopharma Inc | compostos de pirazolo[1,5-a]piridina substituída como inibidores de ret cinase |
| WO2017063509A1 (zh) | 2015-10-15 | 2017-04-20 | 江苏恒瑞医药股份有限公司 | 氧杂螺环类衍生物、其制备方法及其在医药上的应用 |
| EP3368039A1 (en) | 2015-10-26 | 2018-09-05 | The Regents of The University of Colorado, A Body Corporate | Point mutations in trk inhibitor-resistant cancer and methods relating to the same |
| WO2017135399A1 (ja) | 2016-02-04 | 2017-08-10 | 塩野義製薬株式会社 | TrkA阻害活性を有する含窒素複素環および炭素環誘導体 |
| AU2017246547B2 (en) | 2016-04-04 | 2023-02-23 | Loxo Oncology, Inc. | Methods of treating pediatric cancers |
| FI3439662T3 (fi) | 2016-04-04 | 2024-09-04 | Loxo Oncology Inc | (s)-n-(5-((r)-2-(2,5-difluorifenyyli)pyrrolidin-1-yyli)pyratsolo[1,5-a]pyrimidin-3-yyli)-3-hydroksipyrrolidiini-1-karboksamidin nesteformulaatioita |
| US10045991B2 (en) | 2016-04-04 | 2018-08-14 | Loxo Oncology, Inc. | Methods of treating pediatric cancers |
| EP3458456B1 (en) | 2016-05-18 | 2020-11-25 | Loxo Oncology Inc. | Preparation of (s)-n-(5-((r)-2-(2,5-difluorophenyl)pyrrolidin-1-yl)pyrazolo[1,5-a]pyrimidin-3-yl)-3-hydroxypyrrolidine-1-carboxamide |
| MA45795A (fr) | 2016-07-29 | 2019-06-05 | Sunovion Pharmaceuticals Inc | Composés et compositions, et utilisations associées |
| PT3494119T (pt) | 2016-07-29 | 2024-12-10 | Pgi Drug Discovery Llc | Compostos e composições e seus usos |
| 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 |
| TWI752098B (zh) | 2016-10-10 | 2022-01-11 | 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 |
| JOP20190092A1 (ar) | 2016-10-26 | 2019-04-25 | Array Biopharma Inc | عملية لتحضير مركبات بيرازولو[1، 5-a]بيريميدين وأملاح منها |
| WO2018079759A1 (ja) * | 2016-10-31 | 2018-05-03 | 塩野義製薬株式会社 | TrkA阻害活性を有する縮合複素環および縮合炭素環誘導体 |
| WO2018119142A1 (en) | 2016-12-21 | 2018-06-28 | Amgen Inc. | Anti-tnf alpha antibody formulations |
| WO2018136663A1 (en) | 2017-01-18 | 2018-07-26 | Array Biopharma, Inc. | Ret inhibitors |
| WO2018136661A1 (en) | 2017-01-18 | 2018-07-26 | Andrews Steven W | SUBSTITUTED PYRAZOLO[1,5-a]PYRAZINE COMPOUNDS AS RET KINASE INHIBITORS |
| JOP20190213A1 (ar) | 2017-03-16 | 2019-09-16 | Array Biopharma Inc | مركبات حلقية ضخمة كمثبطات لكيناز ros1 |
| ES2992887T3 (en) * | 2017-04-27 | 2024-12-19 | Mochida Pharm Co Ltd | Novel tetrahydronaphthyl urea derivatives as inhibitors of tropomyosin receptor kinase a for the treatment of pain |
| CA3070993C (en) | 2017-08-02 | 2025-05-20 | Sunovion Pharmaceuticals Inc. | ISOCHROMANE COMPOUNDS AND THEIR USES |
| WO2019054450A1 (ja) * | 2017-09-14 | 2019-03-21 | 持田製薬株式会社 | ジアルキルジヒドロナフタレン誘導体の製造方法 |
| JP7134983B2 (ja) * | 2017-09-15 | 2022-09-12 | 持田製薬株式会社 | テトラヒドロナフチルウレア誘導体の結晶 |
| TWI876442B (zh) | 2017-10-10 | 2025-03-11 | 美商絡速藥業公司 | 6-(2-羥基-2-甲基丙氧基)-4-(6-(6-((6-甲氧基吡啶-3-基)甲基)-3,6-二氮雜雙環[3.1.1]庚-3-基)吡啶-3-基)吡唑并[1,5-a]吡啶-3-甲腈之調配物 |
| TWI791053B (zh) | 2017-10-10 | 2023-02-01 | 美商亞雷生物製藥股份有限公司 | 6-(2-羥基-2-甲基丙氧基)-4-(6-(6-((6-甲氧基吡啶-3-基)甲基)-3,6-二氮雜雙環[3.1.1]庚-3-基)吡啶-3-基)吡唑并[1,5-a]吡啶-3-甲腈之結晶形式及其醫藥組合物 |
| WO2019084285A1 (en) | 2017-10-26 | 2019-05-02 | Qian Zhao | FORMULATIONS OF A MACROCYCLIC TRK KINASE INHIBITOR |
| US11472802B2 (en) | 2018-01-18 | 2022-10-18 | Array Biopharma Inc. | Substituted pyrazolyl[4,3-c]pyridine compounds as RET kinase inhibitors |
| EP3740490A1 (en) | 2018-01-18 | 2020-11-25 | Array Biopharma, Inc. | Substituted pyrazolo[3,4-d]pyrimidine compounds as ret kinase inhibitors |
| JP7060694B2 (ja) | 2018-01-18 | 2022-04-26 | アレイ バイオファーマ インコーポレイテッド | Retキナーゼ阻害剤としての置換ピロロ[2,3-d]ピリミジン化合物 |
| WO2019191659A1 (en) | 2018-03-29 | 2019-10-03 | Loxo Oncology, Inc. | Treatment of trk-associated cancers |
| WO2019189717A1 (ja) * | 2018-03-30 | 2019-10-03 | 持田製薬株式会社 | テトラヒドロナフチルウレア誘導体の製造方法 |
| CN110467596A (zh) * | 2018-05-11 | 2019-11-19 | 持田制药株式会社 | 四氢萘基脲衍生物的晶体 |
| CN117285467A (zh) | 2018-07-31 | 2023-12-26 | 罗索肿瘤学公司 | 喷雾干燥的分散体和制剂 |
| CN112996794A (zh) | 2018-09-10 | 2021-06-18 | 阿雷生物药品公司 | 作为ret激酶抑制剂的稠合杂环化合物 |
| EP3898626A1 (en) | 2018-12-19 | 2021-10-27 | Array Biopharma, Inc. | Substituted pyrazolo[1,5-a]pyridine compounds as inhibitors of fgfr tyrosine kinases |
| US12351571B2 (en) | 2018-12-19 | 2025-07-08 | Array Biopharma Inc. | Substituted quinoxaline compounds as inhibitors of FGFR tyrosine kinases |
| CN109575006A (zh) * | 2018-12-30 | 2019-04-05 | 中南民族大学 | 一种二唑吡唑酰胺类衍生物及其微波水热合成法与应用 |
| EP3938045A1 (en) | 2019-03-14 | 2022-01-19 | Sunovion Pharmaceuticals Inc. | Salts of a isochromanyl compound and crystalline forms, processes for preparing, therapeutic uses, and pharmaceutical compositions thereof |
| CN110950872A (zh) * | 2019-12-25 | 2020-04-03 | 武汉九州钰民医药科技有限公司 | 制备靶向抗癌药avapritinib的方法 |
| CN113683535B (zh) * | 2020-05-18 | 2022-08-30 | 中国药科大学 | 含氰胍结构的化合物及其制备方法与用途 |
| CN114031556B (zh) * | 2021-11-08 | 2023-03-31 | 温州大学 | 一种绿色的一锅法制备5-氨基-n-芳基-3-芳基吡唑类化合物的合成方法 |
| JP2025507542A (ja) * | 2022-02-23 | 2025-03-21 | バイオヘイブン・セラピューティクス・リミテッド | Kv7チャネル活性化剤としてのピラゾリル化合物 |
Family Cites Families (78)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU679887B2 (en) | 1995-09-11 | 1997-07-10 | Nihon Nohyaku Co., Ltd. | Azole derivatives, their use, production and usage |
| CA2206201A1 (en) | 1996-05-29 | 1997-11-29 | Yoshiaki Isobe | Pyrazole derivatives and their pharmaceutical use |
| US6083986A (en) | 1996-07-26 | 2000-07-04 | Icagen, Inc. | Potassium channel inhibitors |
| US5998424A (en) | 1997-06-19 | 1999-12-07 | Dupont Pharmaceuticals Company | Inhibitors of factor Xa with a neutral P1 specificity group |
| EP1028953A1 (en) | 1997-11-03 | 2000-08-23 | Boehringer Ingelheim Pharmaceuticals Inc. | Aromatic heterocyclic compounds as anti-inflammatory agents |
| US7329670B1 (en) | 1997-12-22 | 2008-02-12 | Bayer Pharmaceuticals Corporation | Inhibition of RAF kinase using aryl and heteroaryl substituted heterocyclic ureas |
| ATE529109T1 (de) | 1997-12-22 | 2011-11-15 | Bayer Healthcare Llc | Hemmung der p38 kinase aktivität durch substituierte heterocyclische harnstoffe |
| IL136768A0 (en) | 1997-12-22 | 2001-06-14 | Bayer Ag | INHIBITION OF p38 KINASE ACTIVITY USING ARYL AND HETEROARYL SUBSTITUTED HETEROCYCLIC UREAS |
| US6197798B1 (en) | 1998-07-21 | 2001-03-06 | Novartis Ag | Amino-benzocycloalkane derivatives |
| KR100711538B1 (ko) | 1998-12-25 | 2007-04-27 | 아스카 세이야쿠 가부시키가이샤 | 아미노피라졸 유도체 |
| UA73492C2 (en) | 1999-01-19 | 2005-08-15 | Aromatic heterocyclic compounds as antiinflammatory agents | |
| US6387900B1 (en) | 1999-08-12 | 2002-05-14 | Pharmacia & Upjohn S.P.A. | 3(5)-ureido-pyrazole derivatives process for their preparation and their use as antitumor agents |
| US6410533B1 (en) | 2000-02-10 | 2002-06-25 | Genzyme Corporation | Antibacterial compounds |
| JP2004517805A (ja) | 2000-06-30 | 2004-06-17 | ブリストル−マイヤーズ・スクイブ・ファーマ・カンパニー | ケモカイン受容体活性調節剤としてのn−ウレイドヘテロシクロアルキル−ピペリジン |
| EP1389194A2 (en) | 2001-04-27 | 2004-02-18 | Vertex Pharmaceuticals Incorporated | Inhibitors of bace |
| GB0110901D0 (en) | 2001-05-02 | 2001-06-27 | Smithkline Beecham Plc | Novel Compounds |
| WO2003037274A2 (en) | 2001-11-01 | 2003-05-08 | Icagen, Inc. | Pyrazole-amides and-sulfonamides |
| CA2468159A1 (en) | 2001-11-27 | 2003-06-05 | Merck & Co., Inc. | 4-aminoquinoline compounds |
| SE0104248D0 (sv) * | 2001-12-14 | 2001-12-14 | Astrazeneca Ab | Method of treatment |
| EP1601666A2 (en) | 2002-07-02 | 2005-12-07 | Schering Corporation | New neuropeptide y y5 receptor antagonists |
| ZA200502612B (en) | 2002-10-08 | 2007-07-25 | Rinat Neuroscience Corp | Methods for treating post-surgical pain by administering a nerve crowth factor antagonist and compositions containing the same |
| US7202257B2 (en) | 2003-12-24 | 2007-04-10 | Deciphera Pharmaceuticals, Llc | Anti-inflammatory medicaments |
| US7144911B2 (en) | 2002-12-31 | 2006-12-05 | Deciphera Pharmaceuticals Llc | Anti-inflammatory medicaments |
| WO2005024755A2 (en) | 2002-12-31 | 2005-03-17 | Deciphera Pharmaceuticals, Llc. | Medicaments for the treatment of neurodegenerative disorders or diabetes |
| US20040171075A1 (en) | 2002-12-31 | 2004-09-02 | Flynn Daniel L | Modulation of protein functionalities |
| KR101138216B1 (ko) | 2003-06-12 | 2012-09-05 | 아보트 러보러터리즈 | 바닐로이드 수용체 아형 1(vr1) 수용체를 억제하는융합 화합물 |
| EP1684762A4 (en) | 2003-11-13 | 2009-06-17 | Ambit Biosciences Corp | UREA DERIVATIVES AS MODULATORS OF KINASE |
| US20080220497A1 (en) | 2003-12-24 | 2008-09-11 | Flynn Daniel L | Modulation of protein functionalities |
| JP4573223B2 (ja) | 2004-01-23 | 2010-11-04 | 東レ・ファインケミカル株式会社 | 光学活性trans−4−アミノ−1−ベンジル−3−ピロリジノールの製造方法 |
| EP2295426A1 (en) | 2004-04-30 | 2011-03-16 | Bayer HealthCare, LLC | Substituted pyrazolyl urea derivatives useful in the treatment of cancer |
| WO2006068591A1 (en) | 2004-12-20 | 2006-06-29 | Astrazeneca Ab | Novel pyrazole derivatives and their use as modulators of nicotinic acetylcholine receptors |
| AU2005325676A1 (en) | 2004-12-23 | 2006-08-03 | Deciphera Pharmaceuticals, Llc | Anti-inflammatory medicaments |
| CA2592118C (en) | 2004-12-23 | 2015-11-17 | Deciphera Pharmaceuticals, Llc | Urea derivatives as enzyme modulators |
| WO2006070198A1 (en) | 2004-12-30 | 2006-07-06 | Astex Therapeutics Limited | Pyrazole derivatives as that modulate the activity of cdk, gsk and aurora kinases |
| GB0510141D0 (en) | 2005-05-18 | 2005-06-22 | Addex Pharmaceuticals Sa | Novel compounds B3 |
| EP1960394A2 (en) * | 2005-11-15 | 2008-08-27 | Bayer HealthCare AG | Pyrazolyl urea derivatives useful in the treatment of cancer |
| US7514435B2 (en) | 2005-11-18 | 2009-04-07 | Bristol-Myers Squibb Company | Pyrrolotriazine kinase inhibitors |
| US20110195110A1 (en) * | 2005-12-01 | 2011-08-11 | Roger Smith | Urea compounds useful in the treatment of cancer |
| WO2008016811A2 (en) | 2006-07-31 | 2008-02-07 | Neurogen Corporation | Aminopiperidines and realted compounds |
| WO2008021859A1 (en) | 2006-08-09 | 2008-02-21 | Bristol-Myers Squibb Company | Pyrrolotriazine kinase inhibitors |
| US7897762B2 (en) | 2006-09-14 | 2011-03-01 | Deciphera Pharmaceuticals, Llc | Kinase inhibitors useful for the treatment of proliferative diseases |
| US8188113B2 (en) | 2006-09-14 | 2012-05-29 | Deciphera Pharmaceuticals, Inc. | Dihydropyridopyrimidinyl, dihydronaphthyidinyl and related compounds useful as kinase inhibitors for the treatment of proliferative diseases |
| US7790756B2 (en) | 2006-10-11 | 2010-09-07 | Deciphera Pharmaceuticals, Llc | Kinase inhibitors useful for the treatment of myleoproliferative diseases and other proliferative diseases |
| WO2008131276A1 (en) | 2007-04-20 | 2008-10-30 | Deciphera Pharmaceuticals, Llc | Kinase inhibitors useful for the treatment of myleoproliferative diseases and other proliferative diseases |
| WO2008150899A1 (en) | 2007-05-29 | 2008-12-11 | Emory University | Combination therapies for treatment of cancer and inflammatory diseases |
| ITMI20071731A1 (it) | 2007-09-06 | 2009-03-07 | Univ Degli Studi Genova | Nuovi derivati ureici dell'acido 1h-pirazol-4-carbossilico con attivita inibente nei confronti della chemiotassi di neutrofili |
| KR101324804B1 (ko) | 2008-05-13 | 2013-11-01 | 아이알엠 엘엘씨 | 키나제 억제제로서의 질소 함유 융합 헤테로사이클 및 그의 조성물 |
| US8592454B2 (en) | 2008-09-19 | 2013-11-26 | Takeda Pharmaceutical Company Limited | Nitrogen-containing heterocyclic compound and use of same |
| WO2010033941A1 (en) | 2008-09-22 | 2010-03-25 | Array Biopharma Inc. | Substituted imidazo[1,2b]pyridazine compounds as trk kinase inhibitors |
| BRPI0920306A2 (pt) | 2008-10-09 | 2019-09-24 | Hoffmann La Roche | derivados de n-benzil pirrolidina |
| MY169791A (en) | 2008-10-22 | 2019-05-15 | Array Biopharma Inc | Substituted pyrazolo [1,5-a] pyrimidine compounds as trk kinase inhibitors |
| JP2012509338A (ja) | 2008-11-19 | 2012-04-19 | メリアル リミテッド | 二量体1−アリールピラゾール誘導体 |
| JP5752601B2 (ja) | 2008-12-08 | 2015-07-22 | ブイエム ファーマ エルエルシー | タンパク質受容体チロシンキナーゼ阻害薬の組成物 |
| SG172352A1 (en) | 2008-12-23 | 2011-07-28 | Abbott Lab | Anti-viral compounds |
| EP2398323A4 (en) | 2009-02-19 | 2012-08-08 | Univ Connecticut | NEW HETEROPYRROLANALOGES THAT ACTIVATE ON CANNABINOID RECEPTORS |
| US20120071475A1 (en) | 2009-04-27 | 2012-03-22 | Shionogi & Co., Ltd. | Urea derivatives having pi3k-inhibiting activity |
| CA2764694A1 (en) | 2009-06-09 | 2010-12-16 | Topotarget A/S | Pyridinyl derivatives asinhibitors of enzyme nicotinamide phosphoribosyltransferase |
| AR077468A1 (es) * | 2009-07-09 | 2011-08-31 | Array Biopharma Inc | Compuestos de pirazolo (1,5 -a) pirimidina sustituidos como inhibidores de trk- quinasa |
| EP2485589A4 (en) | 2009-09-04 | 2013-02-06 | Biogen Idec Inc | HETEROARYL-BTK INHIBITORS |
| US20120220564A1 (en) | 2009-09-18 | 2012-08-30 | Zalicus Pharmaceuticals Ltd. | Selective calcium channel modulators |
| ME03376B (me) | 2010-05-20 | 2020-01-20 | Array Biopharma Inc | Makrociklička jedinjenja kао inhibiтori trk kinaze |
| CA2835835C (en) | 2011-05-13 | 2019-04-02 | Array Biopharma Inc. | Pyrrolidinyl urea and pyrrolidinyl thiourea compounds as trka kinase inhibitors |
| EP2770987B1 (en) | 2011-10-27 | 2018-04-04 | Merck Sharp & Dohme Corp. | Novel compounds that are erk inhibitors |
| US8969325B2 (en) | 2011-12-19 | 2015-03-03 | Abbvie Inc. | TRPV1 antagonists |
| WO2013176970A1 (en) | 2012-05-22 | 2013-11-28 | Merck Sharp & Dohme Corp. | TrkA KINASE INHIBITORS, COMPOSITIONS AND METHODS THEREOF |
| RU2660429C2 (ru) | 2012-09-28 | 2018-07-06 | Мерк Шарп И Доум Корп. | Новые соединения, которые являются ингибиторами erk |
| WO2014052566A1 (en) | 2012-09-28 | 2014-04-03 | Merck Sharp & Dohme Corp. | Novel compounds that are erk inhibitors |
| RS55593B1 (sr) | 2012-11-13 | 2017-06-30 | Array Biopharma Inc | Jedinjenja biciklične uree, tiouree, guanidina i cijanoguanidina korisna za lečenje bola |
| WO2014078328A1 (en) | 2012-11-13 | 2014-05-22 | Array Biopharma Inc. | N-bicyclic aryl,n'-pyrazolyl urea, thiourea, guanidine and cyanoguanidine compounds as trka kinase inhibitors |
| WO2014078325A1 (en) | 2012-11-13 | 2014-05-22 | Array Biopharma Inc. | N-(monocyclic aryl),n'-pyrazolyl-urea, thiourea, guanidine and cyanoguanidine compounds as trka kinase inhibitors |
| WO2014078331A1 (en) | 2012-11-13 | 2014-05-22 | Array Biopharma Inc. | N-(arylalkyl)-n'-pyrazolyl-urea, thiourea, guanidine and cyanoguanidine compounds as trka kinase inhibitors |
| WO2014078417A1 (en) | 2012-11-13 | 2014-05-22 | Array Biopharma Inc. | Pyrazolyl urea, thiourea, guanidine and cyanoguanidine compounds as trka kinase inhibitors |
| US9822118B2 (en) | 2012-11-13 | 2017-11-21 | Array Biopharma Inc. | Bicyclic heteroaryl urea, thiourea, guanidine and cyanoguanidine compounds as TrkA kinase inhibitors |
| WO2014078372A1 (en) | 2012-11-13 | 2014-05-22 | Array Biopharma Inc. | Pyrrolidinyl urea, thiourea, guanidine and cyanoguanidine compounds as trka kinase inhibitors |
| US9981959B2 (en) | 2012-11-13 | 2018-05-29 | Array Biopharma Inc. | Thiazolyl and oxazolyl urea, thiourea, guanidine and cyanoguanidine compounds as TrkA kinase inhibitors |
| MX374242B (es) | 2012-11-13 | 2025-03-05 | Array Biopharma Inc | Compuestos de n-pirrolidinil, n' -pirazolil-urea, tiourea, guanidina y cianoguanidina como inhibidores de trka cinasa. |
| WO2014078378A1 (en) | 2012-11-13 | 2014-05-22 | Array Biopharma Inc. | Pyrrolidinyl urea, thiourea, guanidine and cyanoguanidine compounds as trka kinase inhibitors |
| WO2015039333A1 (en) | 2013-09-22 | 2015-03-26 | Merck Sharp & Dohme Corp. | TrkA KINASE INHIBITORS, COMPOSITIONS AND METHODS THEREOF |
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