JP2015509535A5 - - Google Patents
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- Publication number
- JP2015509535A5 JP2015509535A5 JP2014561024A JP2014561024A JP2015509535A5 JP 2015509535 A5 JP2015509535 A5 JP 2015509535A5 JP 2014561024 A JP2014561024 A JP 2014561024A JP 2014561024 A JP2014561024 A JP 2014561024A JP 2015509535 A5 JP2015509535 A5 JP 2015509535A5
- Authority
- JP
- Japan
- Prior art keywords
- halo
- cyano
- optionally substituted
- pharmaceutical composition
- hydrocarbyl
- 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
- 125000005843 halogen group Chemical group 0.000 claims 43
- 125000004093 cyano group Chemical group *C#N 0.000 claims 40
- 239000008194 pharmaceutical composition Substances 0.000 claims 37
- 125000001183 hydrocarbyl group Chemical group 0.000 claims 33
- 150000001875 compounds Chemical class 0.000 claims 31
- 238000006467 substitution reaction Methods 0.000 claims 30
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 22
- 239000001257 hydrogen Substances 0.000 claims 20
- 229910052739 hydrogen Inorganic materials 0.000 claims 20
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 14
- 150000002431 hydrogen Chemical class 0.000 claims 13
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 8
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 7
- RAXXELZNTBOGNW-UHFFFAOYSA-N imidazole Natural products C1=CNC=N1 RAXXELZNTBOGNW-UHFFFAOYSA-N 0.000 claims 6
- 150000003839 salts Chemical class 0.000 claims 6
- 125000000623 heterocyclic group Chemical group 0.000 claims 5
- 208000002193 Pain Diseases 0.000 claims 4
- YTPLMLYBLZKORZ-UHFFFAOYSA-N Thiophene Chemical compound C=1C=CSC=1 YTPLMLYBLZKORZ-UHFFFAOYSA-N 0.000 claims 4
- 201000010099 disease Diseases 0.000 claims 4
- 208000035475 disorder Diseases 0.000 claims 4
- 208000004296 neuralgia Diseases 0.000 claims 4
- 208000021722 neuropathic pain Diseases 0.000 claims 4
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 4
- RWRDLPDLKQPQOW-UHFFFAOYSA-N Pyrrolidine Chemical compound C1CCNC1 RWRDLPDLKQPQOW-UHFFFAOYSA-N 0.000 claims 3
- 229910052757 nitrogen Inorganic materials 0.000 claims 3
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 3
- 125000004076 pyridyl group Chemical group 0.000 claims 3
- 125000003341 7 membered heterocyclic group Chemical group 0.000 claims 2
- 208000024827 Alzheimer disease Diseases 0.000 claims 2
- 208000020925 Bipolar disease Diseases 0.000 claims 2
- 208000001640 Fibromyalgia Diseases 0.000 claims 2
- 208000018737 Parkinson disease Diseases 0.000 claims 2
- GLUUGHFHXGJENI-UHFFFAOYSA-N Piperazine Chemical compound C1CNCCN1 GLUUGHFHXGJENI-UHFFFAOYSA-N 0.000 claims 2
- 125000000217 alkyl group Chemical group 0.000 claims 2
- 125000004122 cyclic group Chemical group 0.000 claims 2
- 230000000694 effects Effects 0.000 claims 2
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 2
- 239000003112 inhibitor Substances 0.000 claims 2
- 230000001404 mediated effect Effects 0.000 claims 2
- 230000002093 peripheral effect Effects 0.000 claims 2
- 125000003386 piperidinyl group Chemical group 0.000 claims 2
- 201000000980 schizophrenia Diseases 0.000 claims 2
- 229930192474 thiophene Natural products 0.000 claims 2
- 108091000080 Phosphotransferase Proteins 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 238000000034 method Methods 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 102000020233 phosphotransferase Human genes 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201261608765P | 2012-03-09 | 2012-03-09 | |
| US61/608,765 | 2012-03-09 | ||
| PCT/US2013/029056 WO2013134228A1 (en) | 2012-03-09 | 2013-03-05 | PYRAZOLO[1,5-a]PYRIMIDINE-BASED COMPOUNDS, COMPOSITIONS COMPRISING THEM, AND METHODS OF THEIR USE |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2015509535A JP2015509535A (ja) | 2015-03-30 |
| JP2015509535A5 true JP2015509535A5 (https=) | 2016-04-21 |
| JP6418950B2 JP6418950B2 (ja) | 2018-11-07 |
Family
ID=47892052
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2014561024A Active JP6418950B2 (ja) | 2012-03-09 | 2013-03-05 | ピラゾロ［１，５−ａ］ピリミジン系化合物、それを含む組成物、及びそれらを使用する方法 |
Country Status (25)
| Country | Link |
|---|---|
| US (3) | US8946415B2 (https=) |
| EP (1) | EP2834243B1 (https=) |
| JP (1) | JP6418950B2 (https=) |
| KR (1) | KR101965025B1 (https=) |
| CN (1) | CN104302649B (https=) |
| AR (1) | AR090292A1 (https=) |
| AU (1) | AU2013230128B2 (https=) |
| BR (1) | BR112014022000A8 (https=) |
| CA (1) | CA2866143C (https=) |
| DK (1) | DK2834243T3 (https=) |
| ES (1) | ES2676224T3 (https=) |
| HU (1) | HUE038786T2 (https=) |
| IL (1) | IL234486A (https=) |
| IN (1) | IN2014DN07384A (https=) |
| MX (2) | MX381849B (https=) |
| NZ (1) | NZ630721A (https=) |
| PL (1) | PL2834243T3 (https=) |
| PT (1) | PT2834243T (https=) |
| RU (1) | RU2014140735A (https=) |
| SG (1) | SG11201405561RA (https=) |
| TR (1) | TR201808280T4 (https=) |
| TW (1) | TW201341386A (https=) |
| UY (1) | UY34668A (https=) |
| WO (1) | WO2013134228A1 (https=) |
| ZA (1) | ZA201406149B (https=) |
Families Citing this family (34)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN104302649B (zh) | 2012-03-09 | 2017-06-23 | 莱西肯医药有限公司 | 基于吡唑并[1,5‑a]嘧啶的化合物、包含它们的组合物及其使用方法 |
| WO2013134219A1 (en) | 2012-03-09 | 2013-09-12 | Lexicon Pharmaceuticals, Inc. | Imidazo [1, 2 - b] pyridazine - based compounds, compositions comprising them, and uses thereof |
| US8901305B2 (en) | 2012-07-31 | 2014-12-02 | Bristol-Myers Squibb Company | Aryl lactam kinase inhibitors |
| JP2016509066A (ja) | 2013-02-22 | 2016-03-24 | ブリストル−マイヤーズ スクイブ カンパニーＢｒｉｓｔｏｌ−Ｍｙｅｒｓ Ｓｑｕｉｂｂ Ｃｏｍｐａｎｙ | アダプター関連キナーゼ１（ａａｋ１）の阻害剤としての５ｈ−クロメノ［３，４−ｃ］ピリジン |
| TW201542550A (zh) * | 2013-09-06 | 2015-11-16 | Lexicon Pharmaceuticals Inc | 吡唑并［１，５－ａ］嘧啶基化合物、包含彼之組合物以及使用彼之方法 |
| EP3054955B1 (en) | 2013-10-11 | 2018-05-30 | Bristol-Myers Squibb Company | Pyrrolotriazine kinase inhibitors |
| ES2933350T3 (es) | 2014-01-24 | 2023-02-06 | Turning Point Therapeutics Inc | Macrociclos de diarilo como moduladores de proteína quinasas |
| MX2016009352A (es) * | 2014-01-31 | 2016-10-13 | Bristol Myers Squibb Co | Inhibidores de quinasa a base de quinolina. |
| TW201620911A (zh) * | 2014-03-17 | 2016-06-16 | 雷西肯製藥股份有限公司 | 銜接子關聯激酶１之抑制劑、包含其之組成物、及其使用方法 |
| WO2016053794A1 (en) * | 2014-09-30 | 2016-04-07 | Bristol-Myers Squibb Company | Quinazoline-based kinase inhibitors |
| CA2971024C (en) * | 2014-12-15 | 2023-09-26 | Handok Inc. | Fused ring heteroaryl compounds and their use as trk inhibitors |
| ES2740224T3 (es) | 2015-04-10 | 2020-02-05 | Bristol Myers Squibb Co | 6H-isocromeno[3,4-c]piridinas y benzo[c][1,7]naftiridin-6-(5H)-onas como inhibidores de la cinasa asociada a adaptador 1 (AAK1) |
| AU2016287568B2 (en) | 2015-07-02 | 2020-08-20 | Turning Point Therapeutics, Inc. | Chiral diaryl macrocycles as modulators of protein kinases |
| RU2765181C2 (ru) | 2015-07-06 | 2022-01-26 | Тёрнинг Поинт Терапьютикс, Инк. | Полиморфная форма диарильного макроцикла |
| PT3733187T (pt) | 2015-07-21 | 2024-11-08 | Turning Point Therapeutics Inc | Macrociclo de diarilo quiral e utilização do mesmo no tratamento do cancro |
| ES2765738T3 (es) * | 2015-11-02 | 2020-06-10 | Janssen Pharmaceutica Nv | Compuesto de [1,2,4]triazolo[1,5-a]pirimidin-7-ilo |
| US10689400B2 (en) | 2016-07-28 | 2020-06-23 | Turning Point Therapeutics, Inc. | Macrocycle kinase inhibitors |
| MX385576B (es) * | 2016-11-02 | 2025-03-18 | Janssen Pharmaceutica Nv | Derivados de [1,2,4]triazol[1,5-a]pirimidina como inhibidores de pde2 |
| CA3038916A1 (en) | 2016-11-02 | 2018-05-11 | Janssen Pharmaceutica Nv | [1,2,4]triazolo[1,5-a]pyrimidine compounds as pde2 inhibitors |
| AU2017353313C1 (en) | 2016-11-02 | 2022-06-09 | Janssen Pharmaceutica Nv | (1,2,4)triazolo(1,5-a)pyrimidine compounds as PDE2 inhibitors |
| TWI808958B (zh) | 2017-01-25 | 2023-07-21 | 美商特普醫葯公司 | 涉及二芳基巨環化合物之組合療法 |
| CN111182903A (zh) | 2017-07-28 | 2020-05-19 | 特普医药公司 | 巨环化合物及其用途 |
| SI3658557T1 (sl) | 2017-07-28 | 2024-10-30 | Takeda Pharmaceutical Company Limited | Zaviralci TYK2 in njihova uporaba |
| SG11202005237SA (en) * | 2017-12-15 | 2020-07-29 | Pyramid Biosciences Inc | 5-(2-(2,5-difluorophenyl)pyrrolidin-1 -yl)-3-(1h-pyrazol-1-yl)pyrazolo[1,5-a]pyrimidine derivatives and related compounds as trk kinase inhibitors for treating cancer |
| LT3728271T (lt) | 2017-12-19 | 2022-12-12 | Turning Point Therapeutics, Inc. | Makrocikliniai junginiai, skirti ligų gydymui |
| EP3730492A4 (en) * | 2017-12-22 | 2021-08-11 | Shenzhen TargetRx, Inc. | SUBSTITUTED PYRAZOLO [1,5-A] PYRIMIDINE COMPOUND AND PHARMACEUTICAL COMPOSITION AND USE THEREOF |
| US11345703B2 (en) | 2018-01-23 | 2022-05-31 | Shenzhen Targetrx, Inc. | Substituted pyrazolo[1,5-a]pyrimidine macrocyclic compound |
| CN112771047A (zh) * | 2018-09-27 | 2021-05-07 | 重庆复创医药研究有限公司 | 作为RET激酶抑制剂的取代的咪唑[1,2-a]吡啶和[1,2,4]三唑[1,5-a]吡啶化合物 |
| CN113271940A (zh) * | 2018-10-15 | 2021-08-17 | 林伯士拉克许米公司 | Tyk2抑制剂和其用途 |
| AU2021259419A1 (en) | 2020-04-21 | 2022-11-10 | Lexicon Pharmaceuticals, Inc. | AAK1 inhibitors for use in treating viral infections |
| AU2021258128A1 (en) | 2020-04-21 | 2022-11-03 | Lexicon Pharmaceuticals, Inc. | 4-(3-(pyridin-3-yl)pyrazolo(1,5-a)pyrimidin-5-yl)piperazine for use in the the treatment of COV-229E or COV-OC43 coronaviruses infections |
| US11478733B2 (en) | 2020-11-24 | 2022-10-25 | Caterpillar Inc. | Filter interlock with tabs mating with a pedestal or a housing |
| AU2024338138A1 (en) * | 2023-09-08 | 2026-03-19 | Satellos Bioscience Inc. | Ap2 associated kinase 1 inhibitors and uses thereof |
| WO2025230262A1 (ko) * | 2024-04-29 | 2025-11-06 | 심플렉스 주식회사 | 신규한 헤테로아릴 유도체 및 이의 aak1 억제 용도 |
Family Cites Families (16)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5464764A (en) | 1989-08-22 | 1995-11-07 | University Of Utah Research Foundation | Positive-negative selection methods and vectors |
| WO1993004169A1 (en) | 1991-08-20 | 1993-03-04 | Genpharm International, Inc. | Gene targeting in animal cells using isogenic dna constructs |
| US6194410B1 (en) * | 1998-03-11 | 2001-02-27 | Hoffman-La Roche Inc. | Pyrazolopyrimidine and pyrazolines and process for preparation thereof |
| JP4847275B2 (ja) * | 2005-10-21 | 2011-12-28 | 田辺三菱製薬株式会社 | ピラゾロ［１，５−ａ］ピリミジン化合物 |
| WO2008037477A1 (en) | 2006-09-29 | 2008-04-03 | Novartis Ag | Pyrazolopyrimidines as p13k lipid kinase inhibitors |
| US20120058997A1 (en) * | 2006-11-06 | 2012-03-08 | Supergen, Inc. | Imidazo[1,2-b]pyridazine and pyrazolo[1,5-a]pyrimidine derivatives and their use as protein kinase inhibitors |
| KR101324804B1 (ko) * | 2008-05-13 | 2013-11-01 | 아이알엠 엘엘씨 | 키나제 억제제로서의 질소 함유 융합 헤테로사이클 및 그의 조성물 |
| 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 |
| US8865726B2 (en) | 2009-09-03 | 2014-10-21 | Array Biopharma Inc. | Substituted pyrazolo[1,5-a]pyrimidine compounds as mTOR inhibitors |
| WO2011087999A1 (en) * | 2010-01-14 | 2011-07-21 | Merck Sharp & Dohme Corp. | Pyrazolo[1,5-a]pyrimidines as mark inhibitors |
| EP3812387A1 (en) * | 2011-07-21 | 2021-04-28 | Sumitomo Dainippon Pharma Oncology, Inc. | Heterocyclic protein kinase inhibitors |
| WO2013134219A1 (en) | 2012-03-09 | 2013-09-12 | Lexicon Pharmaceuticals, Inc. | Imidazo [1, 2 - b] pyridazine - based compounds, compositions comprising them, and uses thereof |
| DK2822555T3 (en) * | 2012-03-09 | 2018-02-05 | Lexicon Pharmaceuticals Inc | Inhibition of adapter-associated kinase 1 for the treatment of pain |
| CN104302649B (zh) | 2012-03-09 | 2017-06-23 | 莱西肯医药有限公司 | 基于吡唑并[1,5‑a]嘧啶的化合物、包含它们的组合物及其使用方法 |
| TW201620911A (zh) * | 2014-03-17 | 2016-06-16 | 雷西肯製藥股份有限公司 | 銜接子關聯激酶１之抑制劑、包含其之組成物、及其使用方法 |
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2013
- 2013-03-05 CN CN201380012483.0A patent/CN104302649B/zh active Active
- 2013-03-05 NZ NZ630721A patent/NZ630721A/en unknown
- 2013-03-05 MX MX2017002117A patent/MX381849B/es unknown
- 2013-03-05 MX MX2014010589A patent/MX345830B/es active IP Right Grant
- 2013-03-05 US US13/785,355 patent/US8946415B2/en active Active
- 2013-03-05 PL PL13710250T patent/PL2834243T3/pl unknown
- 2013-03-05 TR TR2018/08280T patent/TR201808280T4/tr unknown
- 2013-03-05 BR BR112014022000A patent/BR112014022000A8/pt not_active Application Discontinuation
- 2013-03-05 AU AU2013230128A patent/AU2013230128B2/en active Active
- 2013-03-05 ES ES13710250.5T patent/ES2676224T3/es active Active
- 2013-03-05 SG SG11201405561RA patent/SG11201405561RA/en unknown
- 2013-03-05 PT PT137102505T patent/PT2834243T/pt unknown
- 2013-03-05 DK DK13710250.5T patent/DK2834243T3/en active
- 2013-03-05 KR KR1020147028071A patent/KR101965025B1/ko active Active
- 2013-03-05 CA CA2866143A patent/CA2866143C/en active Active
- 2013-03-05 WO PCT/US2013/029056 patent/WO2013134228A1/en not_active Ceased
- 2013-03-05 RU RU2014140735A patent/RU2014140735A/ru not_active Application Discontinuation
- 2013-03-05 IN IN7384DEN2014 patent/IN2014DN07384A/en unknown
- 2013-03-05 EP EP13710250.5A patent/EP2834243B1/en active Active
- 2013-03-05 HU HUE13710250A patent/HUE038786T2/hu unknown
- 2013-03-05 JP JP2014561024A patent/JP6418950B2/ja active Active
- 2013-03-08 TW TW102108283A patent/TW201341386A/zh unknown
- 2013-03-11 UY UY0001034668A patent/UY34668A/es not_active Application Discontinuation
- 2013-03-11 AR ARP130100765A patent/AR090292A1/es unknown
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2014
- 2014-08-21 ZA ZA2014/06149A patent/ZA201406149B/en unknown
- 2014-09-07 IL IL234486A patent/IL234486A/en active IP Right Grant
- 2014-09-11 US US14/483,898 patent/US9403832B2/en active Active
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2016
- 2016-07-12 US US15/207,677 patent/US20170129896A1/en not_active Abandoned