JP2016529315A5 - - Google Patents
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- Publication number
- JP2016529315A5 JP2016529315A5 JP2016540405A JP2016540405A JP2016529315A5 JP 2016529315 A5 JP2016529315 A5 JP 2016529315A5 JP 2016540405 A JP2016540405 A JP 2016540405A JP 2016540405 A JP2016540405 A JP 2016540405A JP 2016529315 A5 JP2016529315 A5 JP 2016529315A5
- Authority
- JP
- Japan
- Prior art keywords
- hydrocarbyl
- pharmaceutical composition
- halo
- optionally substituted
- cyano
- 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
- 150000001875 compounds Chemical class 0.000 claims 37
- 125000001183 hydrocarbyl group Chemical group 0.000 claims 37
- 239000008194 pharmaceutical composition Substances 0.000 claims 29
- 125000005843 halogen group Chemical group 0.000 claims 28
- 125000004093 cyano group Chemical group *C#N 0.000 claims 26
- 238000006467 substitution reaction Methods 0.000 claims 20
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 15
- 229910052739 hydrogen Inorganic materials 0.000 claims 11
- 239000001257 hydrogen Substances 0.000 claims 11
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 10
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 8
- 150000002431 hydrogen Chemical class 0.000 claims 7
- RAXXELZNTBOGNW-UHFFFAOYSA-N imidazole Natural products C1=CNC=N1 RAXXELZNTBOGNW-UHFFFAOYSA-N 0.000 claims 6
- 208000004296 neuralgia Diseases 0.000 claims 5
- 208000021722 neuropathic pain Diseases 0.000 claims 5
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 4
- 208000002193 Pain Diseases 0.000 claims 4
- YTPLMLYBLZKORZ-UHFFFAOYSA-N Thiophene Chemical compound C=1C=CSC=1 YTPLMLYBLZKORZ-UHFFFAOYSA-N 0.000 claims 4
- 125000004432 carbon atom Chemical group C* 0.000 claims 4
- 125000004122 cyclic group Chemical group 0.000 claims 4
- 201000010099 disease Diseases 0.000 claims 4
- 208000035475 disorder Diseases 0.000 claims 4
- 125000000623 heterocyclic group Chemical group 0.000 claims 4
- 150000003839 salts Chemical class 0.000 claims 4
- RWRDLPDLKQPQOW-UHFFFAOYSA-N Pyrrolidine Chemical compound C1CCNC1 RWRDLPDLKQPQOW-UHFFFAOYSA-N 0.000 claims 3
- 125000004043 oxo group Chemical group O=* 0.000 claims 3
- 208000024827 Alzheimer disease Diseases 0.000 claims 2
- 208000020925 Bipolar disease Diseases 0.000 claims 2
- 208000032131 Diabetic Neuropathies 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
- 230000000694 effects Effects 0.000 claims 2
- 230000001404 mediated effect Effects 0.000 claims 2
- 229910052757 nitrogen Inorganic materials 0.000 claims 2
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 2
- 125000004076 pyridyl group Chemical group 0.000 claims 2
- 201000000980 schizophrenia Diseases 0.000 claims 2
- 229930192474 thiophene Natural products 0.000 claims 2
- 125000004070 6 membered heterocyclic group Chemical group 0.000 claims 1
- 229940119498 AAK1 inhibitor Drugs 0.000 claims 1
- 108091000080 Phosphotransferase Proteins 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 1
- 239000003112 inhibitor Substances 0.000 claims 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 1
- 230000002093 peripheral effect Effects 0.000 claims 1
- 208000033808 peripheral neuropathy Diseases 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 1
- 102000020233 phosphotransferase Human genes 0.000 claims 1
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 claims 1
- 0 *N(C=CC(c(cc[n]1nc2)nc1c2-c1cccnc1)=C1)C1=O Chemical compound *N(C=CC(c(cc[n]1nc2)nc1c2-c1cccnc1)=C1)C1=O 0.000 description 2
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201361874395P | 2013-09-06 | 2013-09-06 | |
| US61/874,395 | 2013-09-06 | ||
| PCT/US2014/054209 WO2015035117A1 (en) | 2013-09-06 | 2014-09-05 | PYRAZOLO[1,5-a]PYRIMIDINE-BASED COMPOUNDS, COMPOSITIONS COMPRISING THEM, AND METHODS OF THEIR USE |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2016529315A JP2016529315A (ja) | 2016-09-23 |
| JP2016529315A5 true JP2016529315A5 (enExample) | 2017-10-05 |
| JP6472450B2 JP6472450B2 (ja) | 2019-02-20 |
Family
ID=51542502
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016540405A Active JP6472450B2 (ja) | 2013-09-06 | 2014-09-05 | ピラゾロ［１，５−ａ］ピリミジン系化合物、それを含む組成物、及びそれらの使用方法 |
Country Status (12)
| Country | Link |
|---|---|
| US (2) | US20150175610A1 (enExample) |
| EP (1) | EP3041475B1 (enExample) |
| JP (1) | JP6472450B2 (enExample) |
| CN (1) | CN105517553B (enExample) |
| AR (1) | AR097545A1 (enExample) |
| AU (1) | AU2014315113B2 (enExample) |
| CA (1) | CA2923317C (enExample) |
| DK (1) | DK3041475T3 (enExample) |
| ES (1) | ES3009382T3 (enExample) |
| PT (1) | PT3041475T (enExample) |
| TW (1) | TW201542550A (enExample) |
| WO (1) | WO2015035117A1 (enExample) |
Families Citing this family (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US9737542B2 (en) | 2013-10-11 | 2017-08-22 | Bristol-Myers Squibb Company | Pyrrolotriazine kinase inhibitors |
| US20170333435A1 (en) | 2014-11-06 | 2017-11-23 | Lysosomal Therapeutics Inc. | Substituted imidazo[1,5-a]pyrimidines and their use in the treatment of medical disorders |
| KR102662215B1 (ko) | 2014-11-06 | 2024-05-02 | 비알 - 알&디 인베스트먼츠, 에스.에이. | 치환된 피라졸로(1,5-a)피리미딘 및 의학적 장애의 치료에서의 그의 용도 |
| EP3215509B1 (en) | 2014-11-06 | 2020-02-26 | Lysosomal Therapeutics Inc. | Substituted pyrrolo[1,2-a]pyrimidines and their use in the treatment of medical disorders |
| BR112018070586A8 (pt) | 2016-04-06 | 2023-03-14 | Lysosomal Therapeutics Inc | Compostos de pirazol[1,5-a]pirimidinil carboxamida e seu uso no tratamento de distúrbios médicos |
| WO2017176962A1 (en) | 2016-04-06 | 2017-10-12 | Lysosomal Therapeutics, Inc. | Pyrrolo[1,2-a]pyrimidinyl carboxamide compounds and their use in the treatment of medical disorders |
| JP7046827B2 (ja) | 2016-04-06 | 2022-04-04 | リソソーマル・セラピューティクス・インコーポレイテッド | イミダゾ［１，５－ａ］ピリミジニルカルボキサミド化合物および医学的障害の処置におけるその使用 |
| CN109311902B (zh) | 2016-05-05 | 2022-07-15 | Bial研发投资股份有限公司 | 取代的咪唑并[1,2-b]哒嗪、咪唑并[1,5-b]哒嗪、相关化合物及其用途 |
| US11345698B2 (en) | 2016-05-05 | 2022-05-31 | Bial—R&D Investments, S.A. | Substituted imidazo[1,2-a]pyridines, substituted imidazo[1,2-a]pyrazines, related compounds, and their use in the treatment of medical disorders |
| 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 |
Family Cites Families (22)
| 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 |
| KR20040097375A (ko) * | 2002-04-23 | 2004-11-17 | 시오노기 앤드 컴파니, 리미티드 | 피라졸로[1, 5-에이]피리미딘 유도체 및 이를 함유한엔에이디(피)에이취 산화효소 저해제 |
| US7329662B2 (en) | 2003-10-03 | 2008-02-12 | Hoffmann-La Roche Inc. | Pyrazolo-pyridine |
| PT1863818E (pt) | 2005-03-23 | 2010-04-09 | Hoffmann La Roche | Derivados de acetilenil-pirazolo-pirimidina como antagonistas de mglur2 |
| JP5048675B2 (ja) * | 2005-09-27 | 2012-10-17 | エフ．ホフマン−ラ ロシュ アーゲー | ｍＧｌｕＲ２アンタゴニストとしてのオキサジアゾリルピラゾロ−ピリミジン類 |
| 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 |
| US20090275586A1 (en) | 2006-10-06 | 2009-11-05 | Kalypsys, Inc. | Heterocyclic inhibitors of pde4 |
| RU2009120389A (ru) * | 2006-10-30 | 2010-12-10 | Новартис АГ (CH) | Гетероциклические соединения в качестве противовоспалительных агентов |
| AR067326A1 (es) | 2007-05-11 | 2009-10-07 | Novartis Ag | Imidazopiridinas y pirrolo -pirimidinas sustituidas como inhibidores de cinasa de lipido |
| KR101324804B1 (ko) * | 2008-05-13 | 2013-11-01 | 아이알엠 엘엘씨 | 키나제 억제제로서의 질소 함유 융합 헤테로사이클 및 그의 조성물 |
| TWI491610B (zh) * | 2008-10-09 | 2015-07-11 | 必治妥美雅史谷比公司 | 作為激酶抑制劑之咪唑并嗒腈 |
| EP2350071B1 (en) * | 2008-10-22 | 2014-01-08 | Array Biopharma, Inc. | SUBSTITUTED PYRAZOLO[1,5-a]PYRIMIDINE COMPOUNDS AS TRK KINASE INHIBITORS |
| MX2011012369A (es) * | 2009-05-20 | 2012-03-16 | Cylene Pharmaceuticals Inc | Pirazolopirimidinas y heterociclos relacionados como inhibidores de cinasa. |
| AR077468A1 (es) * | 2009-07-09 | 2011-08-31 | Array Biopharma Inc | Compuestos de pirazolo (1,5 -a) pirimidina sustituidos como inhibidores de trk- quinasa |
| WO2011073316A1 (en) * | 2009-12-18 | 2011-06-23 | Novartis Ag | 4-aryl-butane-1,3-diamides |
| US8946237B2 (en) * | 2010-01-14 | 2015-02-03 | Merck Sharp & Dohme Corp. | Pyrazolo[1,5-A]pyrimidines as mark inhibitors |
| RU2598840C2 (ru) * | 2011-05-19 | 2016-09-27 | Фундасион Сентро Насиональ Де Инвестигасионес Онколохикас Карлос Iii | Новые соединения |
| CN104220071A (zh) | 2012-03-09 | 2014-12-17 | 莱西肯医药有限公司 | 抑制转接物关联激酶1以治疗疼痛 |
| WO2013134228A1 (en) * | 2012-03-09 | 2013-09-12 | Lexicon Pharmaceuticals, Inc. | PYRAZOLO[1,5-a]PYRIMIDINE-BASED COMPOUNDS, COMPOSITIONS COMPRISING THEM, AND METHODS OF THEIR USE |
| GB201205669D0 (en) * | 2012-03-30 | 2012-05-16 | Agency Science Tech & Res | Bicyclic heterocyclic derivatives as mnk2 and mnk2 modulators and uses thereof |
-
2014
- 2014-09-02 TW TW103130281A patent/TW201542550A/zh unknown
- 2014-09-03 AR ARP140103297A patent/AR097545A1/es unknown
- 2014-09-05 US US14/478,089 patent/US20150175610A1/en not_active Abandoned
- 2014-09-05 CN CN201480049185.3A patent/CN105517553B/zh active Active
- 2014-09-05 WO PCT/US2014/054209 patent/WO2015035117A1/en not_active Ceased
- 2014-09-05 ES ES14766634T patent/ES3009382T3/es active Active
- 2014-09-05 EP EP14766634.1A patent/EP3041475B1/en active Active
- 2014-09-05 CA CA2923317A patent/CA2923317C/en active Active
- 2014-09-05 JP JP2016540405A patent/JP6472450B2/ja active Active
- 2014-09-05 PT PT147666341T patent/PT3041475T/pt unknown
- 2014-09-05 DK DK14766634.1T patent/DK3041475T3/da active
- 2014-09-05 AU AU2014315113A patent/AU2014315113B2/en active Active
-
2016
- 2016-05-03 US US15/145,435 patent/US9862724B2/en active Active