JP2014514360A5 - - Google Patents
Download PDFInfo
- Publication number
- JP2014514360A5 JP2014514360A5 JP2014510416A JP2014510416A JP2014514360A5 JP 2014514360 A5 JP2014514360 A5 JP 2014514360A5 JP 2014510416 A JP2014510416 A JP 2014510416A JP 2014510416 A JP2014510416 A JP 2014510416A JP 2014514360 A5 JP2014514360 A5 JP 2014514360A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- alkoxy
- independently selected
- optionally substituted
- compound
- 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
- 125000000217 alkyl group Chemical group 0.000 claims description 488
- 125000003545 alkoxy group Chemical group 0.000 claims description 237
- 150000001875 compounds Chemical class 0.000 claims description 131
- 229910052736 halogen Inorganic materials 0.000 claims description 75
- 150000002367 halogens Chemical class 0.000 claims description 72
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims description 61
- 150000003839 salts Chemical class 0.000 claims description 50
- 125000005842 heteroatom Chemical group 0.000 claims description 42
- 229910052760 oxygen Inorganic materials 0.000 claims description 41
- 229910052717 sulfur Inorganic materials 0.000 claims description 39
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 37
- 239000012453 solvate Substances 0.000 claims description 34
- 239000000651 prodrug Substances 0.000 claims description 33
- 229940002612 prodrug Drugs 0.000 claims description 33
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 32
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 claims description 30
- PQIOSYKVBBWRRI-UHFFFAOYSA-N methylphosphonyl difluoride Chemical group CP(F)(F)=O PQIOSYKVBBWRRI-UHFFFAOYSA-N 0.000 claims description 29
- 125000001424 substituent group Chemical group 0.000 claims description 29
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 claims description 26
- -1 hydroxyl-carbonyl Chemical group 0.000 claims description 24
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims description 23
- 125000004093 cyano group Chemical group *C#N 0.000 claims description 20
- 208000002193 Pain Diseases 0.000 claims description 19
- 125000000623 heterocyclic group Chemical group 0.000 claims description 18
- 229910052757 nitrogen Inorganic materials 0.000 claims description 17
- 229910052739 hydrogen Inorganic materials 0.000 claims description 16
- 125000004414 alkyl thio group Chemical group 0.000 claims description 15
- 125000004390 alkyl sulfonyl group Chemical group 0.000 claims description 13
- 125000004429 atom Chemical group 0.000 claims description 13
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 12
- ORTFAQDWJHRMNX-UHFFFAOYSA-N hydroxidooxidocarbon(.) Chemical group O[C]=O ORTFAQDWJHRMNX-UHFFFAOYSA-N 0.000 claims description 12
- 230000008878 coupling Effects 0.000 claims description 11
- 238000010168 coupling process Methods 0.000 claims description 11
- 238000005859 coupling reaction Methods 0.000 claims description 11
- 125000004029 hydroxymethyl group Chemical group [H]OC([H])([H])* 0.000 claims description 11
- 125000002252 acyl group Chemical group 0.000 claims description 10
- 125000004453 alkoxycarbonyl group Chemical group 0.000 claims description 10
- 239000001257 hydrogen Substances 0.000 claims description 10
- 238000000034 method Methods 0.000 claims description 10
- 125000004433 nitrogen atom Chemical group N* 0.000 claims description 9
- 229920006395 saturated elastomer Polymers 0.000 claims description 9
- 206010028980 Neoplasm Diseases 0.000 claims description 8
- 201000011510 cancer Diseases 0.000 claims description 8
- 125000000876 trifluoromethoxy group Chemical group FC(F)(F)O* 0.000 claims description 8
- 206010001935 American trypanosomiasis Diseases 0.000 claims description 7
- 208000024699 Chagas disease Diseases 0.000 claims description 7
- 206010061218 Inflammation Diseases 0.000 claims description 7
- 230000004054 inflammatory process Effects 0.000 claims description 7
- 230000004770 neurodegeneration Effects 0.000 claims description 7
- 208000015122 neurodegenerative disease Diseases 0.000 claims description 7
- 125000004950 trifluoroalkyl group Chemical group 0.000 claims description 7
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 6
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical group [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims description 6
- 125000005422 alkyl sulfonamido group Chemical group 0.000 claims description 6
- 201000010099 disease Diseases 0.000 claims description 6
- 208000035475 disorder Diseases 0.000 claims description 6
- NVBFHJWHLNUMCV-UHFFFAOYSA-N sulfamide Chemical compound NS(N)(=O)=O NVBFHJWHLNUMCV-UHFFFAOYSA-N 0.000 claims description 6
- 125000003282 alkyl amino group Chemical group 0.000 claims description 5
- 125000006163 5-membered heteroaryl group Chemical group 0.000 claims description 4
- 241000124008 Mammalia Species 0.000 claims description 4
- 125000005157 alkyl carboxy group Chemical group 0.000 claims description 4
- 125000002837 carbocyclic group Chemical group 0.000 claims description 4
- 150000002431 hydrogen Chemical class 0.000 claims description 4
- 125000006413 ring segment Chemical group 0.000 claims description 4
- 125000001889 triflyl group Chemical group FC(F)(F)S(*)(=O)=O 0.000 claims description 4
- 239000003085 diluting agent Substances 0.000 claims description 3
- 125000005843 halogen group Chemical group 0.000 claims description 3
- 239000008194 pharmaceutical composition Substances 0.000 claims description 3
- 125000004422 alkyl sulphonamide group Chemical group 0.000 claims description 2
- 150000001408 amides Chemical class 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
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 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
- 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
- 239000003814 drug Substances 0.000 claims description 2
- 150000007522 mineralic acids Chemical class 0.000 claims description 2
- 125000006239 protecting group Chemical group 0.000 claims description 2
- 125000004076 pyridyl group Chemical group 0.000 claims description 2
- 239000000203 mixture Substances 0.000 claims 14
- 125000001153 fluoro group Chemical group F* 0.000 claims 3
- 238000006467 substitution reaction Methods 0.000 claims 3
- 208000000094 Chronic Pain Diseases 0.000 claims 1
- 206010065390 Inflammatory pain Diseases 0.000 claims 1
- 208000005298 acute pain Diseases 0.000 claims 1
- 239000003795 chemical substances by application Substances 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
- 239000002585 base Substances 0.000 description 8
- NTOIKDYVJIWVSU-WOJBJXKFSA-N (2r,3r)-2,3-dihydroxy-2,3-bis(4-methylbenzoyl)butanedioic acid Chemical compound C1=CC(C)=CC=C1C(=O)[C@@](O)(C(O)=O)[C@](O)(C(O)=O)C(=O)C1=CC=C(C)C=C1 NTOIKDYVJIWVSU-WOJBJXKFSA-N 0.000 description 4
- CMIBUZBMZCBCAT-HOTGVXAUSA-N (2s,3s)-2,3-bis[(4-methylbenzoyl)oxy]butanedioic acid Chemical compound C1=CC(C)=CC=C1C(=O)O[C@H](C(O)=O)[C@@H](C(O)=O)OC(=O)C1=CC=C(C)C=C1 CMIBUZBMZCBCAT-HOTGVXAUSA-N 0.000 description 1
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 1
- 239000012458 free base Substances 0.000 description 1
- 150000007529 inorganic bases Chemical class 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201161485858P | 2011-05-13 | 2011-05-13 | |
| US61/485,858 | 2011-05-13 | ||
| PCT/US2012/037003 WO2012158413A2 (en) | 2011-05-13 | 2012-05-09 | Pyrrolidinyl urea and pyrrolidinyl thiourea compounds as trka kinase inhibitors |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016026184A Division JP6382867B2 (ja) | 2011-05-13 | 2016-02-15 | Ｔｒｋａキナーゼ阻害剤としてのピロリジニル尿素およびピロリジニルチオ尿素化合物 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2014514360A JP2014514360A (ja) | 2014-06-19 |
| JP2014514360A5 true JP2014514360A5 (OSRAM) | 2015-05-21 |
| JP5933902B2 JP5933902B2 (ja) | 2016-06-15 |
Family
ID=46614580
Family Applications (4)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2014510416A Active JP5933902B2 (ja) | 2011-05-13 | 2012-05-09 | Ｔｒｋａキナーゼ阻害剤としてのピロリジニル尿素およびピロリジニルチオ尿素化合物 |
| JP2016026184A Active JP6382867B2 (ja) | 2011-05-13 | 2016-02-15 | Ｔｒｋａキナーゼ阻害剤としてのピロリジニル尿素およびピロリジニルチオ尿素化合物 |
| JP2017090432A Withdrawn JP2017171672A (ja) | 2011-05-13 | 2017-04-28 | Ｔｒｋａキナーゼ阻害剤としてのピロリジニル尿素およびピロリジニルチオ尿素化合物 |
| JP2018172485A Pending JP2019001819A (ja) | 2011-05-13 | 2018-09-14 | Ｔｒｋａキナーゼ阻害剤としてのピロリジニル尿素およびピロリジニルチオ尿素化合物 |
Family Applications After (3)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016026184A Active JP6382867B2 (ja) | 2011-05-13 | 2016-02-15 | Ｔｒｋａキナーゼ阻害剤としてのピロリジニル尿素およびピロリジニルチオ尿素化合物 |
| JP2017090432A Withdrawn JP2017171672A (ja) | 2011-05-13 | 2017-04-28 | Ｔｒｋａキナーゼ阻害剤としてのピロリジニル尿素およびピロリジニルチオ尿素化合物 |
| JP2018172485A Pending JP2019001819A (ja) | 2011-05-13 | 2018-09-14 | Ｔｒｋａキナーゼ阻害剤としてのピロリジニル尿素およびピロリジニルチオ尿素化合物 |
Country Status (35)
| Country | Link |
|---|---|
| US (4) | US9562055B2 (OSRAM) |
| EP (1) | EP2712358B1 (OSRAM) |
| JP (4) | JP5933902B2 (OSRAM) |
| KR (2) | KR102001364B1 (OSRAM) |
| CN (3) | CN108329246B (OSRAM) |
| AR (1) | AR086367A1 (OSRAM) |
| AU (2) | AU2012256237B2 (OSRAM) |
| BR (1) | BR112013029201B1 (OSRAM) |
| CA (1) | CA2835835C (OSRAM) |
| CL (1) | CL2013003257A1 (OSRAM) |
| CO (1) | CO6821961A2 (OSRAM) |
| CR (1) | CR20130646A (OSRAM) |
| CY (1) | CY1119014T1 (OSRAM) |
| DK (1) | DK2712358T3 (OSRAM) |
| ES (1) | ES2615738T3 (OSRAM) |
| HR (1) | HRP20161786T1 (OSRAM) |
| HU (1) | HUE030791T2 (OSRAM) |
| IL (2) | IL229377A (OSRAM) |
| LT (1) | LT2712358T (OSRAM) |
| ME (1) | ME02583B (OSRAM) |
| MX (2) | MX369142B (OSRAM) |
| MY (1) | MY173181A (OSRAM) |
| NZ (1) | NZ618795A (OSRAM) |
| PH (1) | PH12013502319A1 (OSRAM) |
| PL (1) | PL2712358T3 (OSRAM) |
| PT (1) | PT2712358T (OSRAM) |
| RS (1) | RS55582B1 (OSRAM) |
| RU (1) | RU2606131C2 (OSRAM) |
| SG (2) | SG10201913053QA (OSRAM) |
| SI (1) | SI2712358T1 (OSRAM) |
| SM (2) | SMT201700035T1 (OSRAM) |
| TW (2) | TWI649315B (OSRAM) |
| UA (1) | UA114711C2 (OSRAM) |
| UY (1) | UY34067A (OSRAM) |
| WO (1) | WO2012158413A2 (OSRAM) |
Families Citing this family (96)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2116539A1 (en) | 2008-04-25 | 2009-11-11 | Laboratorios Del. Dr. Esteve, S.A. | 1-aryl-3-aminoalkoxy-pyrazoles as sigma ligands enhancing analgesic effects of opioids and attenuating the dependency thereof |
| SI2350075T1 (sl) | 2008-09-22 | 2014-06-30 | Array Biopharma, Inc. | Substituirane imidazo (1,2b)piridazinske spojine kot Trk kinazni inhibitorji |
| SG10201914059WA (en) | 2008-10-22 | 2020-03-30 | 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 |
| EP2353591A1 (en) | 2010-02-04 | 2011-08-10 | Laboratorios Del. Dr. Esteve, S.A. | Sigma ligands for potentiating the analgesic effect of opioids and opiates in post-operative pain and attenuating the dependency thereof |
| EP2353598A1 (en) | 2010-02-04 | 2011-08-10 | Laboratorios Del. Dr. Esteve, S.A. | Sigma ligands for use in the prevention and/or treatment of postoperative pain |
| EP2918588B1 (en) | 2010-05-20 | 2017-05-03 | Array Biopharma, Inc. | Macrocyclic compounds as TRK kinase inhibitors |
| EP2388005A1 (en) | 2010-05-21 | 2011-11-23 | Laboratorios Del. Dr. Esteve, S.A. | Sigma ligands for the prevention and/or treatment of emesis induced by chemotherapy or radiotherapy |
| EP2415471A1 (en) | 2010-08-03 | 2012-02-08 | Laboratorios Del. Dr. Esteve, S.A. | Use of sigma ligands in opioid-induced hyperalgesia |
| SI2712358T1 (sl) | 2011-05-13 | 2017-03-31 | Array Biopharma, Inc. | Spojine pirolidinil sečnine, pirolidinil tiosečnine in pirolidinil gvanidina kot inhibitorji kinaze trka |
| EP2524694A1 (en) | 2011-05-19 | 2012-11-21 | Laboratorios Del. Dr. Esteve, S.A. | Use of sigma ligands in diabetes type-2 associated pain |
| ES2664331T3 (es) * | 2012-11-13 | 2018-04-19 | Array Biopharma, Inc. | Compuestos de N-pirrolidinilo, N'-pirazolilurea, tiourea, guanidina y cianoguanidina como inhibidores de la cinasa Trka |
| 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 |
| 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 |
| US9828360B2 (en) | 2012-11-13 | 2017-11-28 | Array Biopharma Inc. | Pyrrolidinyl urea, thiourea, guanidine and cyanoguanidine compounds as TrkA kinase inhibitors |
| WO2014078322A1 (en) | 2012-11-13 | 2014-05-22 | 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 |
| RU2664541C2 (ru) | 2012-11-13 | 2018-08-20 | Эррэй Биофарма Инк. | Бициклические соединения мочевины, тиомочевины, гуанидина и цианогуанидина, пригодные для лечения боли |
| WO2014078408A1 (en) | 2012-11-13 | 2014-05-22 | Array Biopharma Inc. | Bicyclic heteroaryl urea, thiourea, guanidine and cyanoguanidine compounds as trka kinase inhibitors |
| US9809578B2 (en) | 2012-11-13 | 2017-11-07 | Array Biopharma Inc. | Pyrazolyl urea, thiourea, guanidine and cyanoguanidine compounds as trkA kinase inhibitors |
| US9790178B2 (en) | 2012-11-13 | 2017-10-17 | Array Biopharma Inc. | Pyrrolidinyl urea, thiourea, guanidine and cyanoguanidine compounds as TrkA kinase inhibitors |
| CN104918934B (zh) | 2013-01-18 | 2017-12-22 | 霍夫曼-拉罗奇有限公司 | 3‑取代的吡唑及其作为dlk抑制剂的用途 |
| EP2818166A1 (en) * | 2013-06-26 | 2014-12-31 | Laboratorios del Dr. Esteve S.A. | Use of sigma receptor ligands for the prevention and treatment of pain associated to interstitial cystitis/bladder pain syndrome (IC/BPS) |
| WO2015039334A1 (en) | 2013-09-22 | 2015-03-26 | Merck Sharp & Dohme Corp. | TrkA KINASE INHIBITORS, COMPOSITIONS AND METHODS THEREOF |
| WO2015039333A1 (en) * | 2013-09-22 | 2015-03-26 | Merck Sharp & Dohme Corp. | TrkA KINASE INHIBITORS, COMPOSITIONS AND METHODS THEREOF |
| RS57036B1 (sr) | 2013-11-28 | 2018-05-31 | Kyorin Pharmaceutical Co Ltd | Urea derivati ili njihove farmakološki prihvatljive soli korisni kao agonisti formil peptidnom receptoru-sličnom 1 (fprl-1) |
| SG11201604480PA (en) | 2013-12-17 | 2016-07-28 | Esteve Labor Dr | SEROTONIN-NOREPINEPHRINE REUPTAKE INHIBITORS (SNRIs) AND SIGMA RECEPTOR LIGANDS COMBINATIONS |
| US20160318897A1 (en) | 2013-12-18 | 2016-11-03 | Basf Se | Azole compounds carrying an imine-derived substituent |
| EP3083602A1 (en) | 2013-12-20 | 2016-10-26 | Pfizer Limited | N-acylpiperidine ether tropomyosin-related kinase inhibitors |
| WO2015143652A1 (en) | 2014-03-26 | 2015-10-01 | Merck Sharp & Dohme Corp. | TrkA KINASE INHIBITORS,COMPOSITIONS AND METHODS THEREOF |
| WO2015143654A1 (en) | 2014-03-26 | 2015-10-01 | Merck Sharp & Dohme Corp. | TrkA KINASE INHIBITORS,COMPOSITIONS AND METHODS THEREOF |
| WO2015143653A1 (en) | 2014-03-26 | 2015-10-01 | Merck Sharp & Dohme Corp. | TrkA KINASE INHIBITORS,COMPOSITIONS AND METHODS THEREOF |
| EP3131891A1 (en) | 2014-04-15 | 2017-02-22 | Pfizer Inc. | Tropomyosin-related kinase inhibitors containing both a 1h-pyrazole and a pyrimidine moiety |
| EP3140298A1 (en) | 2014-05-07 | 2017-03-15 | Pfizer Inc. | Tropomyosin-related kinase inhibitors |
| PT3154959T (pt) * | 2014-05-15 | 2019-09-24 | Array Biopharma Inc | 1-((3s,4r)-4-(3-fluorofenil)-1-(2-metoxietil)-pirrolidin-3-il)-3-(4-metil-3-(2-metilpirimidin-5-il)-1-fenil-1h-pirazol-5-il)ureia como inibidor da cinase trka |
| WO2016009296A1 (en) | 2014-07-16 | 2016-01-21 | Pfizer Inc. | N-acylpiperidine ether tropomyosin-related kinase inhibitors |
| WO2016020784A1 (en) | 2014-08-05 | 2016-02-11 | Pfizer Inc. | N-acylpyrrolidine ether tropomyosin-related kinase inhibitors |
| US10160727B2 (en) | 2014-08-06 | 2018-12-25 | Shionogi & Co., Ltd. | Heterocycle and carbocycle derivatives having TrkA inhibitory activity |
| US10799505B2 (en) | 2014-11-16 | 2020-10-13 | Array Biopharma, Inc. | Crystalline form of (S)-N-(5-((R)-2-(2,5-difluorophenyl)-pyrrolidin-1-yl)-pyrazolo[1,5-A]pyrimidin-3-yl)-3-hydroxypyrrolidine-1-carboxamide hydrogen sulfate |
| JP6611816B2 (ja) | 2014-12-08 | 2019-11-27 | エフ エム シー コーポレーション | ３−オキソ−３−（アリールアミノ）プロパノエイト、その製造方法、およびピロリジノンの製造におけるその使用 |
| WO2016161572A1 (en) | 2015-04-08 | 2016-10-13 | Merck Sharp & Dohme Corp. | TrkA KINASE INHIBITORS, COMPOSITIONS AND METHODS THEREOF |
| ES2814126T3 (es) * | 2015-05-27 | 2021-03-26 | Kyorin Seiyaku Kk | Derivado de urea o sal farmacológicamente aceptable del mismo |
| EP3722441A1 (en) | 2015-06-01 | 2020-10-14 | Loxo Oncology Inc. | Method of diagnosing a cancer for a treatment with a trk inhibitor |
| EP3330256B1 (en) * | 2015-07-07 | 2021-06-16 | Shionogi & Co., Ltd. | HETEROCYCLIC DERIVATIVE HAVING TrkA-INHIBITING ACTIVITY |
| DK3322706T3 (da) | 2015-07-16 | 2021-02-01 | Array Biopharma Inc | Substituerede pyrazolo[1,5-a]pyridin-forbindelser som ret-kinaseinhibitorer |
| JP2018534296A (ja) | 2015-10-26 | 2018-11-22 | ロクソ オンコロジー， インコーポレイテッドＬｏｘｏ Ｏｎｃｏｌｏｇｙ， Ｉｎｃ． | Ｔｒｋ阻害薬耐性がんにおける点変異およびそれに関連する方法 |
| MX2018007527A (es) | 2015-12-22 | 2018-09-07 | Syngenta Participations Ag | Derivados de pirazol activos como pesticidas. |
| 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 |
| RS65988B1 (sr) | 2016-04-04 | 2024-10-31 | Loxo Oncology Inc | Postupak lečenja pedijatrijskih karcinoma |
| US10045991B2 (en) | 2016-04-04 | 2018-08-14 | Loxo Oncology, Inc. | Methods of treating pediatric cancers |
| MX386416B (es) | 2016-04-04 | 2025-03-18 | Loxo Oncology Inc | Formulaciones liquidas de (s)-n-(5-((r)-2-(2,5-difluorofenil)-pirrolidin-1-il)-pirazolo[1,5-a]pirimidin-3-il)-3-hidroxipirrolidina-1-carboxamida. |
| HUE063877T2 (hu) | 2016-05-18 | 2024-02-28 | Loxo Oncology Inc | (S)-N-(5-((R)-2-(2,5-dlfluorofenil)pirolidin-1-il)plrazolo[1,5-A]pirimidin-3-il) -3-hidroxipirolidin-1-karboxamid elõállítása |
| JOP20190077A1 (ar) | 2016-10-10 | 2019-04-09 | Array Biopharma Inc | مركبات بيرازولو [1، 5-a]بيريدين بها استبدال كمثبطات كيناز ret |
| 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 |
| JOP20190092A1 (ar) | 2016-10-26 | 2019-04-25 | Array Biopharma Inc | عملية لتحضير مركبات بيرازولو[1، 5-a]بيريميدين وأملاح منها |
| CA3049136C (en) | 2017-01-18 | 2022-06-14 | Array Biopharma Inc. | Substituted pyrazolo[1,5-a]pyrazine compounds as ret kinase inhibitors |
| WO2018136663A1 (en) | 2017-01-18 | 2018-07-26 | Array Biopharma, Inc. | Ret inhibitors |
| JOP20190213A1 (ar) | 2017-03-16 | 2019-09-16 | Array Biopharma Inc | مركبات حلقية ضخمة كمثبطات لكيناز ros1 |
| US11472797B2 (en) | 2017-04-05 | 2022-10-18 | Syngenta Participations Ag | Pesticidally active pyrazole derivatives |
| UY37775A (es) | 2017-06-19 | 2019-01-31 | Syngenta Participations Ag | Derivados de pirazol activos como plaguicida |
| JP2019026646A (ja) * | 2017-08-03 | 2019-02-21 | 塩野義製薬株式会社 | 含窒素複素環および炭素環誘導体を含有する、疼痛の治療および／または予防用医薬組成物 |
| TWI812649B (zh) | 2017-10-10 | 2023-08-21 | 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 |
| MA50456A (fr) | 2017-10-26 | 2020-09-02 | Array Biopharma Inc | Formulations d'un inhibiteur de kinase trk macrocyclique |
| EP3710441A1 (en) * | 2017-11-17 | 2020-09-23 | Hepagene Therapeutics, Inc. | Urea derivatives as inhibitors of ask1 |
| WO2019143994A1 (en) | 2018-01-18 | 2019-07-25 | Array Biopharma Inc. | Substituted pyrazolyl[4,3-c]pyridinecompounds as ret kinase inhibitors |
| CA3087354C (en) | 2018-01-18 | 2023-01-03 | Array Biopharma Inc. | Substituted pyrrolo[2,3-d]pyrimidines compounds as ret kinase inhibitors |
| CA3087578C (en) | 2018-01-18 | 2023-08-08 | Array Biopharma Inc. | Substituted pyrazolo[3,4-d]pyrimidine compounds as ret kinase inhibitors |
| EA202092094A1 (ru) | 2018-03-05 | 2020-12-10 | Бристол-Маерс Сквибб Компани | Фенилпирролидиноновые агонисты формилпептидного рецептора 2 |
| EP3773725A1 (en) | 2018-03-29 | 2021-02-17 | Loxo Oncology Inc. | Treatment of trk-associated cancers |
| WO2020010092A1 (en) * | 2018-07-03 | 2020-01-09 | Ifm Due, Inc. | Compounds and compositions for treating conditions associated with sting activity |
| US11932652B2 (en) | 2018-07-12 | 2024-03-19 | Zhangzhou Pien Tze Huang Pharmaceutical Co., Ltd. | Pyrrolidinyl urea derivatives and application thereof in TrkA-related diseases |
| GB201811825D0 (en) | 2018-07-19 | 2018-09-05 | Benevolentai Bio Ltd | Organic compounds |
| KR102545594B1 (ko) | 2018-07-31 | 2023-06-21 | 록쏘 온콜로지, 인코포레이티드 | (s)-5-아미노-3-(4-((5-플루오로-2-메톡시벤즈아미도)메틸)페닐)-1-(1,1,1-트리플루오로프로판-2-일)-1h-피라졸-4-카르복스아미드의 분무-건조된 분산물 및 제제 |
| GB201813791D0 (en) | 2018-08-23 | 2018-10-10 | Benevolental Bio Ltd | Organic compounds |
| 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 |
| JP2022515197A (ja) | 2018-12-19 | 2022-02-17 | アレイ バイオファーマ インコーポレイテッド | がんを治療するためのｆｇｆｒ阻害剤としての７－（（３，５－ジメトキシフェニル）アミノ）キノキサリン誘導体 |
| WO2020127345A1 (en) | 2018-12-21 | 2020-06-25 | Syngenta Participations Ag | Pesticidally active pyrazole derivatives |
| AU2020242287A1 (en) | 2019-03-21 | 2021-09-02 | INSERM (Institut National de la Santé et de la Recherche Médicale) | A Dbait molecule in combination with kinase inhibitor for the treatment of cancer |
| KR20220098759A (ko) | 2019-11-08 | 2022-07-12 | 인쎄름 (엥스띠뛰 나씨오날 드 라 쌍떼 에 드 라 흐쉐르슈 메디깔) | 키나제 억제제에 대해 내성을 획득한 암의 치료 방법 |
| CN114555581B (zh) * | 2019-11-14 | 2024-05-24 | 优迈特株式会社 | 含氟吡唑化合物及其制备方法 |
| JP7289017B2 (ja) * | 2020-01-10 | 2023-06-08 | ▲ザン▼州片仔▲ファン▼薬業股▲フン▼有限公司 | ピロリジニルウレア誘導体の結晶及びその使用 |
| EP4089087B1 (en) * | 2020-01-10 | 2024-07-03 | Zhangzhou Pien Tze Huang Pharmaceutical Co., Ltd. | Method for preparing pyrrolidinyl urea derivative |
| MX2022008930A (es) | 2020-01-22 | 2022-10-18 | Benevolentai Bio Ltd | Composiciones farmaceuticas y sus usos. |
| MX2022008931A (es) | 2020-01-22 | 2022-10-18 | Benevolentai Bio Ltd | Composiciones farmaceuticas y sus usos. |
| WO2021148581A1 (en) | 2020-01-22 | 2021-07-29 | Onxeo | Novel dbait molecule and its use |
| WO2022003377A1 (en) | 2020-07-02 | 2022-01-06 | Uni-Pharma Kleon Tsetis Pharmaceutical Laboratories S.A. | Thieno[3,4-c]pyrazol-3-yl acetamides as autotaxin inhibitors |
| CN117529475A (zh) | 2021-01-08 | 2024-02-06 | 艾福姆德尤股份有限公司 | 用于治疗与sting活性有关的疾病的含脲或类似物的杂双环化合物及其化合物 |
| US20240308978A1 (en) * | 2021-01-08 | 2024-09-19 | Ifm Due, Inc. | Compounds and compositions for treating conditions associated with sting activity |
| EP4323353A4 (en) * | 2021-04-12 | 2025-04-02 | Cullgen (Shanghai), Inc. | TROPOMYOSIN RECEPTOR KINASE (TRK) DEGRADATION COMPOUNDS AND METHODS OF USE |
| WO2022234287A1 (en) | 2021-05-06 | 2022-11-10 | Benevolentai Bio Limited | Imidazopyridazine derivatives useful as trk inhibitors |
| 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 |
| EP4433458A4 (en) | 2021-11-19 | 2025-10-29 | Broad Inst Inc | Bifunctional chimeric molecules for labeling kinases with target bond fractions and their methods of use |
| WO2024240213A1 (zh) * | 2023-05-23 | 2024-11-28 | 上海海雁医药科技有限公司 | 稠合三环取代的异噁唑烷基脲衍生物、其药物组合物及应用 |
| US11970499B1 (en) * | 2023-12-22 | 2024-04-30 | King Faisal University | Pyrazolo[1,5-c]pyrimidine compounds as CK2 inhibitors |
Family Cites Families (108)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPS63198664A (ja) * | 1986-03-31 | 1988-08-17 | Sankyo Co Ltd | キノロンカルボン酸誘導体 |
| DE3906365A1 (de) * | 1988-07-15 | 1990-01-18 | Bayer Ag | 7-(1-pyrrolidinyl)-3-chinolon- und -naphthyridoncarbonsaeure-derivate, verfahren sowie substituierte (oxa)diazabicyclooctane und -nonane als zwischenprodukte zu ihrer herstellung, und sie enthaltende antibakterielle mittel und futterzusatzstoffe |
| NZ240883A (en) * | 1990-12-05 | 1994-09-27 | Synphar Lab Inc | Antibacterial 7-substituted-6-fluoro-1,4-dihydro-4-oxo- quinoline-3-carboxylic acid derivatives |
| JP3086837B2 (ja) * | 1991-06-06 | 2000-09-11 | 三協化学株式会社 | ３−アミノピロリジン類の製造方法 |
| ATE209645T1 (de) * | 1994-06-14 | 2001-12-15 | Dainippon Pharmaceutical Co | Neue verbindung, verfahren zu ihrer herstellung und antitumormittel |
| NZ299242A (en) | 1995-09-11 | 1997-12-19 | Nihon Nohyaku Co Ltd | N-phenyl-n'-(phenyl substituted imidazol-5-yl, -oxazol-4-yl, and -thiazol-4-yl)urea derivatives |
| 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 |
| CA2308428A1 (en) | 1997-11-03 | 1999-05-14 | Boehringer Ingelheim Pharmaceuticals, Inc. | Aromatic heterocyclic compounds as anti-inflammatory agents |
| DE69836563T2 (de) * | 1997-12-22 | 2007-05-16 | Bayer Pharmaceuticals Corp., West Haven | INHIBIERUNG DER p38 KINASE-AKTIVITÄT DURCH DIE VERWENDUNG VON ARYL- UND HETEROARYL-SUBSTITUIERTEN HARNSTOFFEN |
| US7329670B1 (en) | 1997-12-22 | 2008-02-12 | Bayer Pharmaceuticals Corporation | Inhibition of RAF kinase using aryl and heteroaryl substituted heterocyclic ureas |
| US6197798B1 (en) | 1998-07-21 | 2001-03-06 | Novartis Ag | Amino-benzocycloalkane derivatives |
| CA2356263C (en) | 1998-12-25 | 2009-04-21 | Teikoku Hormone Mfg. Co., Ltd. | Aminopyrazole derivatives |
| 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 |
| CA2384240A1 (en) * | 1999-10-15 | 2001-04-26 | Dean A. Wacker | Benzylcycloalkyl amines as modulators of chemokine receptor activity |
| US6410533B1 (en) | 2000-02-10 | 2002-06-25 | Genzyme Corporation | Antibacterial compounds |
| EP1296978A2 (en) | 2000-06-30 | 2003-04-02 | Bristol-Myers Squibb Company | N-ureidoheterocycloaklyl-piperidines as modulators of chemokine receptor activity |
| US20030095958A1 (en) | 2001-04-27 | 2003-05-22 | Bhisetti Govinda R. | Inhibitors of bace |
| GB0110901D0 (en) | 2001-05-02 | 2001-06-27 | Smithkline Beecham Plc | Novel Compounds |
| ATE455104T1 (de) | 2001-11-01 | 2010-01-15 | Icagen Inc | Pyrazolamide zur anwendung in der behandlung von schmerz |
| EP1451156A4 (en) | 2001-11-27 | 2005-05-25 | Merck & Co Inc | 4-AMINOCHINOLINVERBINDUNGEN |
| SE0104248D0 (sv) | 2001-12-14 | 2001-12-14 | Astrazeneca Ab | Method of treatment |
| US7041698B2 (en) | 2002-05-20 | 2006-05-09 | Bristol-Myers Squibb Company | Hepatitis C virus inhibitors |
| JP4498133B2 (ja) | 2002-07-02 | 2010-07-07 | シェーリング コーポレイション | 新規神経ペプチドｙｙ５レセプターアンタゴニスト |
| JP4584713B2 (ja) | 2002-10-08 | 2010-11-24 | ライナット ニューロサイエンス コーポレイション | 神経成長因子アンタゴニストを投与することによって術後疼痛を処置するための方法および神経成長因子アンタゴニストを含有する組成物 |
| KR101023035B1 (ko) * | 2002-10-30 | 2011-03-24 | 와쿠나가 세이야쿠 가부시키 가이샤 | 세펨 화합물 |
| US20040171075A1 (en) | 2002-12-31 | 2004-09-02 | Flynn Daniel L | Modulation of protein functionalities |
| 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 |
| US7202257B2 (en) | 2003-12-24 | 2007-04-10 | Deciphera Pharmaceuticals, Llc | Anti-inflammatory medicaments |
| PL2017265T3 (pl) | 2003-06-12 | 2011-11-30 | Abbvie Inc | Związki z pierścieniami skondensowanymi hamujące receptor waniloidowy podtypu 1 (VR1) |
| US20050165031A1 (en) | 2003-11-13 | 2005-07-28 | Ambit Biosciences Corporation | Urea derivatives as ABL modulators |
| MY141220A (en) * | 2003-11-17 | 2010-03-31 | Astrazeneca Ab | Pyrazole derivatives as inhibitors of receptor tyrosine kinases |
| 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 |
| CN101010315A (zh) * | 2004-04-30 | 2007-08-01 | 拜耳制药公司 | 用于治疗癌症的取代的吡唑基脲衍生物 |
| JP2008509179A (ja) * | 2004-08-09 | 2008-03-27 | グラクソ グループ リミテッド | グルタミン酸受容体を強化する化合物および医学におけるその使用 |
| US20080081833A1 (en) | 2004-12-20 | 2008-04-03 | Astrazeneca Ab | Novel Pyrazole Derivatives And Their Use As Modulators Of Nicotinic Acetylcholine Receptors |
| WO2006081034A2 (en) | 2004-12-23 | 2006-08-03 | Deciphera Pharmaceuticals, Llc | Anti-inflammatory medicaments |
| US20070078121A1 (en) | 2004-12-23 | 2007-04-05 | Flynn Daniel L | Enzyme modulators and treatments |
| WO2006067401A1 (en) | 2004-12-24 | 2006-06-29 | Astrazeneca Ab | Heterocyclic compounds as ccr2b antagonists |
| US20100160324A1 (en) | 2004-12-30 | 2010-06-24 | 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 |
| US20060281768A1 (en) | 2005-06-10 | 2006-12-14 | Gaul Michael D | Thienopyrimidine and thienopyridine kinase modulators |
| WO2007059202A2 (en) | 2005-11-15 | 2007-05-24 | 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 |
| MX2008006979A (es) | 2005-12-01 | 2009-01-14 | Bayer Healthcare Llc | Compuestos de urea utiles en el tratamiento contra el cancer. |
| JP5131990B2 (ja) | 2006-01-31 | 2013-01-30 | アレイ バイオファーマ、インコーポレイテッド | キナーゼ阻害剤およびその使用方法 |
| GB0607953D0 (en) | 2006-04-21 | 2006-05-31 | Novartis Ag | Organic compounds |
| 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 |
| TW200833690A (en) | 2006-12-15 | 2008-08-16 | Bayer Schering Pharma Ag | 3-H-pyrazolopyridines and salts thereof, pharmaceutical compositions comprising same, methods of preparing same and uses of same |
| KR101163847B1 (ko) * | 2007-04-20 | 2012-07-09 | 에프. 호프만-라 로슈 아게 | 이중 ｎｋ1/ｎｋ3 수용체 길항제로서의 피롤리딘 유도체 |
| EP2481736A1 (en) | 2007-04-20 | 2012-08-01 | 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 |
| BRPI0815562A2 (pt) | 2007-07-12 | 2015-02-18 | Novartis Ag | Soluções farmacêuticas orais contendo telbivudina. |
| 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 |
| EP2227460B1 (en) * | 2007-10-24 | 2012-06-20 | Cancer Research Technology Limited | Therapeutic oxy-phenyl-aryl compounds and their use |
| EP2070929A1 (en) * | 2007-12-11 | 2009-06-17 | Bayer Schering Pharma Aktiengesellschaft | Alkynylaryl compounds and salts thereof, pharmaceutical compositions comprising same, methods of preparing same and uses of same |
| KR101713501B1 (ko) | 2008-03-17 | 2017-03-07 | 암비트 바이오사이언시즈 코포레이션 | Ｒａｆ 키나아제 조절제로서의 퀴나졸린 유도체 및 그의 사용방법 |
| JP5492194B2 (ja) | 2008-05-13 | 2014-05-14 | アイアールエム・リミテッド・ライアビリティ・カンパニー | キナーゼ阻害剤としての縮合窒素含有ヘテロ環およびその組成物 |
| MX2010013311A (es) * | 2008-06-16 | 2010-12-21 | Hoffmann La Roche | Derivados de pirrolidina como antagonistas del receptor de nk2. |
| EP2334683B1 (en) | 2008-08-29 | 2017-03-22 | MSD Italia S.r.l. | Saturated bicyclic heterocyclic derivatives as smo antagonists |
| US8592454B2 (en) | 2008-09-19 | 2013-11-26 | Takeda Pharmaceutical Company Limited | Nitrogen-containing heterocyclic compound and use of same |
| SI2350075T1 (sl) | 2008-09-22 | 2014-06-30 | Array Biopharma, Inc. | Substituirane imidazo (1,2b)piridazinske spojine kot Trk kinazni inhibitorji |
| BRPI0920306A2 (pt) * | 2008-10-09 | 2019-09-24 | Hoffmann La Roche | derivados de n-benzil pirrolidina |
| SG10201914059WA (en) * | 2008-10-22 | 2020-03-30 | Array Biopharma Inc | Substituted pyrazolo[1,5-a]pyrimidine compounds as trk kinase inhibitors |
| US8022099B2 (en) * | 2008-11-03 | 2011-09-20 | Hoffmann-La Roche Inc. | N-benzyl pyrrolidine derivatives |
| CA2743553C (en) | 2008-11-19 | 2017-03-14 | Merial Limited | Dimeric 1-arylpyrazole derivatives |
| NZ593937A (en) | 2008-12-08 | 2014-05-30 | Vm Pharma Llc | Compositions of protein receptor tyrosine kinase inhibitors |
| MX2011006332A (es) | 2008-12-23 | 2011-06-27 | Abbott Lab | Compuestos antivirales. |
| CA2753061C (en) | 2009-02-19 | 2016-08-09 | Alexandros Makriyannis | Novel hetero pyrrole analogs acting on cannabinoid receptors |
| GB0904285D0 (en) * | 2009-03-12 | 2009-04-22 | Prosidion Ltd | Compounds for the treatment of metabolic disorders |
| US8680139B2 (en) * | 2009-04-01 | 2014-03-25 | Progenra | Anti-neoplastic compounds, compositions and methods |
| TW201103943A (en) | 2009-04-27 | 2011-02-01 | Shionogi & Co | Urea derivative having pi3k inhibitory activity |
| WO2010141817A1 (en) | 2009-06-05 | 2010-12-09 | Janssen Pharmaceutica Nv | Heteroaryl-substituted spirocyclic diamine urea modulators of fatty acid amide hydrolase |
| AR077468A1 (es) | 2009-07-09 | 2011-08-31 | Array Biopharma Inc | Compuestos de pirazolo (1,5 -a) pirimidina sustituidos como inhibidores de trk- quinasa |
| CN102470127A (zh) | 2009-08-19 | 2012-05-23 | 埃姆比特生物科学公司 | 联芳基化合物和其使用方法 |
| CA2771612A1 (en) | 2009-09-18 | 2011-03-24 | Zalicus Pharmaceuticals Ltd. | Selective calcium channel modulators |
| US20110144081A1 (en) * | 2009-12-15 | 2011-06-16 | Henner Knust | Pyrrolidine derivatives |
| US20110152233A1 (en) * | 2009-12-18 | 2011-06-23 | Henner Knust | Pyrrolidine compounds |
| EP2918588B1 (en) | 2010-05-20 | 2017-05-03 | Array Biopharma, Inc. | Macrocyclic compounds as TRK kinase inhibitors |
| WO2011150198A1 (en) | 2010-05-27 | 2011-12-01 | Ambit Biosciences Corporation | Azolyl urea compounds and methods of use thereof |
| ES2729754T3 (es) * | 2010-07-29 | 2019-11-06 | Merck Patent Gmbh | Carboxamidas azaheterocíclicas de aminas cíclicas |
| US9242981B2 (en) * | 2010-09-16 | 2016-01-26 | Merck Sharp & Dohme Corp. | Fused pyrazole derivatives as novel ERK inhibitors |
| AR083904A1 (es) * | 2010-11-18 | 2013-04-10 | Prosidion Ltd | Derivados de 1,4-pirrolidinas disustituidos y 3-il-aminas y sus usos en el tratamiento de desordenes metabolicos |
| SI2712358T1 (sl) | 2011-05-13 | 2017-03-31 | Array Biopharma, Inc. | Spojine pirolidinil sečnine, pirolidinil tiosečnine in pirolidinil gvanidina kot inhibitorji kinaze trka |
| US9023865B2 (en) | 2011-10-27 | 2015-05-05 | Merck Sharp & Dohme Corp. | Compounds that are ERK inhibitors |
| US8969325B2 (en) | 2011-12-19 | 2015-03-03 | Abbvie Inc. | TRPV1 antagonists |
| US9181261B2 (en) | 2012-05-22 | 2015-11-10 | Merck Sharp & Dohme Corp. | TrkA kinase inhibitors, compositions and methods thereof |
| EP2900223B1 (en) | 2012-09-28 | 2017-10-25 | Merck Sharp & Dohme Corp. | Novel compounds that are erk inhibitors |
| JP6280554B2 (ja) | 2012-09-28 | 2018-02-14 | メルク・シャープ・アンド・ドーム・コーポレーションＭｅｒｃｋ Ｓｈａｒｐ ＆ Ｄｏｈｍｅ Ｃｏｒｐ． | Ｅｒｋ阻害剤である新規化合物 |
| US9809578B2 (en) | 2012-11-13 | 2017-11-07 | Array Biopharma Inc. | Pyrazolyl urea, thiourea, guanidine and cyanoguanidine compounds as trkA kinase inhibitors |
| WO2014078408A1 (en) | 2012-11-13 | 2014-05-22 | Array Biopharma Inc. | Bicyclic heteroaryl 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 |
| 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 |
| US9790178B2 (en) | 2012-11-13 | 2017-10-17 | Array Biopharma Inc. | Pyrrolidinyl urea, thiourea, guanidine and cyanoguanidine compounds as TrkA kinase inhibitors |
| US9828360B2 (en) | 2012-11-13 | 2017-11-28 | Array Biopharma Inc. | Pyrrolidinyl 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 |
| ES2664331T3 (es) | 2012-11-13 | 2018-04-19 | Array Biopharma, Inc. | Compuestos de N-pirrolidinilo, N'-pirazolilurea, tiourea, guanidina y cianoguanidina como inhibidores de la cinasa Trka |
| RU2664541C2 (ru) | 2012-11-13 | 2018-08-20 | Эррэй Биофарма Инк. | Бициклические соединения мочевины, тиомочевины, гуанидина и цианогуанидина, пригодные для лечения боли |
| WO2014078322A1 (en) | 2012-11-13 | 2014-05-22 | Array Biopharma Inc. | Thiazolyl and oxazolyl 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 |
-
2012
- 2012-05-09 SI SI201230829A patent/SI2712358T1/sl unknown
- 2012-05-09 RS RS20170020A patent/RS55582B1/sr unknown
- 2012-05-09 EP EP12743553.5A patent/EP2712358B1/en active Active
- 2012-05-09 CA CA2835835A patent/CA2835835C/en active Active
- 2012-05-09 CN CN201810204068.XA patent/CN108329246B/zh active Active
- 2012-05-09 SG SG10201913053QA patent/SG10201913053QA/en unknown
- 2012-05-09 LT LTEP12743553.5T patent/LT2712358T/lt unknown
- 2012-05-09 NZ NZ618795A patent/NZ618795A/en unknown
- 2012-05-09 RU RU2013155456A patent/RU2606131C2/ru active
- 2012-05-09 MX MX2017006568A patent/MX369142B/es unknown
- 2012-05-09 JP JP2014510416A patent/JP5933902B2/ja active Active
- 2012-05-09 AU AU2012256237A patent/AU2012256237B2/en active Active
- 2012-05-09 KR KR1020197007332A patent/KR102001364B1/ko active Active
- 2012-05-09 KR KR1020137033192A patent/KR101960555B1/ko active Active
- 2012-05-09 PT PT127435535T patent/PT2712358T/pt unknown
- 2012-05-09 UA UAA201314472A patent/UA114711C2/uk unknown
- 2012-05-09 HU HUE12743553A patent/HUE030791T2/en unknown
- 2012-05-09 ES ES12743553.5T patent/ES2615738T3/es active Active
- 2012-05-09 US US14/117,615 patent/US9562055B2/en active Active
- 2012-05-09 MY MYPI2013702146A patent/MY173181A/en unknown
- 2012-05-09 DK DK12743553.5T patent/DK2712358T3/en active
- 2012-05-09 PH PH1/2013/502319A patent/PH12013502319A1/en unknown
- 2012-05-09 MX MX2013013342A patent/MX347952B/es active IP Right Grant
- 2012-05-09 WO PCT/US2012/037003 patent/WO2012158413A2/en not_active Ceased
- 2012-05-09 SM SM20170035T patent/SMT201700035T1/it unknown
- 2012-05-09 CN CN201510473903.6A patent/CN105130967B/zh active Active
- 2012-05-09 HR HRP20161786TT patent/HRP20161786T1/hr unknown
- 2012-05-09 BR BR112013029201-6A patent/BR112013029201B1/pt active IP Right Grant
- 2012-05-09 PL PL12743553T patent/PL2712358T3/pl unknown
- 2012-05-09 CN CN201280034583.9A patent/CN103649076B/zh active Active
- 2012-05-09 ME MEP-2017-7A patent/ME02583B/me unknown
- 2012-05-09 SG SG2013083498A patent/SG194902A1/en unknown
- 2012-05-11 UY UY0001034067A patent/UY34067A/es unknown
- 2012-05-11 TW TW106112291A patent/TWI649315B/zh active
- 2012-05-11 AR ARP120101675A patent/AR086367A1/es active IP Right Grant
- 2012-05-11 TW TW101116963A patent/TWI589573B/zh active
-
2013
- 2013-11-11 IL IL229377A patent/IL229377A/en active IP Right Grant
- 2013-11-13 CL CL2013003257A patent/CL2013003257A1/es unknown
- 2013-12-11 CR CR20130646A patent/CR20130646A/es unknown
- 2013-12-13 CO CO13291998A patent/CO6821961A2/es active IP Right Grant
-
2016
- 2016-02-15 JP JP2016026184A patent/JP6382867B2/ja active Active
- 2016-12-16 US US15/382,028 patent/US9878997B2/en active Active
-
2017
- 2017-01-19 SM SM201700035T patent/SMT201700035B/it unknown
- 2017-01-24 CY CY20171100107T patent/CY1119014T1/el unknown
- 2017-03-01 AU AU2017201418A patent/AU2017201418B2/en active Active
- 2017-04-28 JP JP2017090432A patent/JP2017171672A/ja not_active Withdrawn
- 2017-06-12 IL IL252841A patent/IL252841B/en active IP Right Grant
- 2017-12-12 US US15/839,706 patent/US10323022B2/en active Active
-
2018
- 2018-09-14 JP JP2018172485A patent/JP2019001819A/ja active Pending
-
2019
- 2019-05-02 US US16/402,080 patent/US20190359597A1/en not_active Abandoned
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| JP2014514360A5 (OSRAM) | ||
| JP2014511892A5 (OSRAM) | ||
| RU2016134751A (ru) | Соединения | |
| JP2016501191A5 (OSRAM) | ||
| JP2020505396A5 (OSRAM) | ||
| JP2018502877A5 (OSRAM) | ||
| JP2017504635A5 (OSRAM) | ||
| RU2014141579A (ru) | Гетероциклические соединения в качестве ингибиторов бета-лактамаз | |
| HRP20161786T1 (hr) | Pirolidinil urea, pirolidinil tiourea i pirolidinil gvanidin spojevi kao inhibitori trka kinaze | |
| AR073551A1 (es) | Pirimidinas macrociclicas como inhibidores de proteina cinasa | |
| JP2011509309A5 (OSRAM) | ||
| JP2013509431A5 (OSRAM) | ||
| JP2016506961A5 (OSRAM) | ||
| JP2016530283A5 (OSRAM) | ||
| JP2015522650A5 (OSRAM) | ||
| JP2013010792A5 (OSRAM) | ||
| JP2016506962A5 (OSRAM) | ||
| WO2009082268A3 (ru) | ЛИГАНДЫ α-АДРЕНОЦЕПТОРОВ, ДОПАМИНОВЫХ, ГИСТАМИНОВЫХ, ИМИДАЗОЛИНОВЫХ И СЕРОТОНИНОВЫХ РЕЦЕПТОРОВ И ИХ ПРИМЕНЕНИЕ | |
| JP2013512903A5 (OSRAM) | ||
| JP2018527295A5 (OSRAM) | ||
| JP2014037426A5 (OSRAM) | ||
| RU2015106434A (ru) | Производные типа азаиндазола или диазаиндазола для лечения боли | |
| JP2015535839A5 (OSRAM) | ||
| JP2016540803A5 (OSRAM) | ||
| JP2014502988A5 (OSRAM) |