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 |
|---|---|---|---|---|
| CN105979950A (zh) | 2013-10-11 | 2016-09-28 | 百时美施贵宝公司 | 吡咯并三嗪激酶抑制剂 |
| WO2016073889A1 (en) | 2014-11-06 | 2016-05-12 | Lysosomal Therapeutics Inc. | Substituted imidazo[1,5-a]pyrimidines and their use in the treatment of medical disorders |
| US20180185368A1 (en) | 2014-11-06 | 2018-07-05 | Lysosomal Therapeutics Inc. | Substituted pyrrolo[1,2-a]pyrimidines and their use in the treatment of medical disorders |
| EP3215511B1 (en) | 2014-11-06 | 2024-04-17 | Bial-R&D Investments, S.A. | Substituted pyrazolo(1,5-a)pyrimidines and their use in the treatment of medical disorders |
| WO2017176961A1 (en) | 2016-04-06 | 2017-10-12 | Lysosomal Therapeutics Inc. | Imidazo [1,5-a]pyrimidinyl carboxamide compounds and their use in the treatment of medical disorders |
| KR20180133461A (ko) | 2016-04-06 | 2018-12-14 | 리소소말 테라퓨틱스 인크. | 피라졸로[1,5-a]피리미디닐 카르복스아미드 화합물 및 의학적 장애의 치료에서의 그의 용도 |
| MX388912B (es) | 2016-04-06 | 2025-03-20 | Lysosomal Therapeutics Inc | Compuestos de pirrol[1,2-a]pirimidinil carboxamida y su uso en el tratamiento de trastornos médicos |
| WO2017192930A1 (en) | 2016-05-05 | 2017-11-09 | Lysosomal Therapeutics Inc. | SUBSTITUTED IMIDAZO[1,2-b]PYRIDAZINES, SUBSTITUTED IMIDAZO[1,5-b]PYRIDAZINES, RELATED COMPOUNDS, AND THEIR USE IN THE TREATMENT OF MEDICAL DISORDERS |
| WO2017192931A1 (en) | 2016-05-05 | 2017-11-09 | Lysosomal Therapeutics Inc. | SUBSTITUTED IMDAZO[1,2-α]PYRIDINES, SUBSTITUTED IMIDAZO[1,2-α]PYRAZINES, RELATED COMPOUNDS, AND THEIR USE IN THE TREATMENT OF MEDICAL DISORDERS |
| JP7619951B2 (ja) * | 2018-10-15 | 2025-01-22 | 武田薬品工業株式会社 | Ｔｙｋ２阻害剤およびその使用 |
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 |
| CA2483306A1 (en) * | 2002-04-23 | 2003-11-06 | Shionogi & Co., Ltd. | Pyrazolo[1,5-a]pyrimidine derivative and nad(p)h oxidase inhibitor containing the same |
| 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 |
| ATE463495T1 (de) * | 2005-09-27 | 2010-04-15 | Hoffmann La Roche | Oxadiazolylpyrazolopyrimidine als mglur2- antagonisten |
| 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 |
| WO2008045664A2 (en) * | 2006-10-06 | 2008-04-17 | Kalypsys, Inc. | Heterocyclic pde4 inhibitors as antiinflammatory agents |
| BRPI0718266A2 (pt) * | 2006-10-30 | 2014-01-07 | Novartis Ag | Compostos heterocíclicos como agentes anti-inflamatórios. |
| AR067326A1 (es) | 2007-05-11 | 2009-10-07 | Novartis Ag | Imidazopiridinas y pirrolo -pirimidinas sustituidas como inhibidores de cinasa de lipido |
| CA2722418C (en) * | 2008-05-13 | 2013-09-17 | Irm Llc | Fused nitrogen containing heterocycles and compositions thereof as kinase inhibitors |
| 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 |
| CN102264736B (zh) * | 2008-10-22 | 2013-08-14 | 阵列生物制药公司 | 作为TRK激酶抑制剂的取代的吡唑并[1,5-a]嘧啶化合物 |
| NZ596571A (en) * | 2009-05-20 | 2013-03-28 | Cylene Pharmaceuticals Inc | Pyrazolopyrimidines and related heterocycles as 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 |
| 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 |
| AU2012257513B2 (en) * | 2011-05-19 | 2017-05-11 | Fundación Del Sector Público Estatal Centro Nacional De Investigaciones Oncológicas Carlos III (F.S.P. CNIO) | Macrocyclic compounds as protein kinase inhibitors |
| DK2834243T3 (en) | 2012-03-09 | 2018-07-23 | Lexicon Pharmaceuticals Inc | Pyrazole [1,5-a] pyrimidine-based compounds, compositions comprising them and methods for their use |
| HK1199814A1 (en) | 2012-03-09 | 2015-07-24 | Lexicon Pharmaceuticals, Inc. | Inhibition of adaptor associated kinase 1 for the treatment of pain |
| 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 AU AU2014315113A patent/AU2014315113B2/en active Active
- 2014-09-05 DK DK14766634.1T patent/DK3041475T3/da active
- 2014-09-05 PT PT147666341T patent/PT3041475T/pt unknown
- 2014-09-05 CA CA2923317A patent/CA2923317C/en active Active
- 2014-09-05 WO PCT/US2014/054209 patent/WO2015035117A1/en not_active Ceased
- 2014-09-05 JP JP2016540405A patent/JP6472450B2/ja active Active
- 2014-09-05 US US14/478,089 patent/US20150175610A1/en not_active Abandoned
- 2014-09-05 ES ES14766634T patent/ES3009382T3/es active Active
- 2014-09-05 EP EP14766634.1A patent/EP3041475B1/en active Active
- 2014-09-05 CN CN201480049185.3A patent/CN105517553B/zh active Active
-
2016
- 2016-05-03 US US15/145,435 patent/US9862724B2/en active Active
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