JP2015524835A5 - - Google Patents
Download PDFInfo
- Publication number
- JP2015524835A5 JP2015524835A5 JP2015527004A JP2015527004A JP2015524835A5 JP 2015524835 A5 JP2015524835 A5 JP 2015524835A5 JP 2015527004 A JP2015527004 A JP 2015527004A JP 2015527004 A JP2015527004 A JP 2015527004A JP 2015524835 A5 JP2015524835 A5 JP 2015524835A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- alkoxy
- substituted
- halogen
- substituents
- 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.)
- Ceased
Links
- 150000002367 halogens Chemical group 0.000 claims 53
- 229910052736 halogen Inorganic materials 0.000 claims 51
- 125000001424 substituent group Chemical group 0.000 claims 45
- 229910052799 carbon Inorganic materials 0.000 claims 41
- -1 amino, hydroxy, methoxy, methyl Chemical group 0.000 claims 35
- 150000003839 salts Chemical class 0.000 claims 34
- 239000012453 solvate Substances 0.000 claims 34
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims 33
- 125000000229 (C1-C4)alkoxy group Chemical group 0.000 claims 33
- 150000001875 compounds Chemical class 0.000 claims 31
- 229910052739 hydrogen Inorganic materials 0.000 claims 28
- 239000001257 hydrogen Substances 0.000 claims 28
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 24
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims 24
- 125000004076 pyridyl group Chemical group 0.000 claims 24
- 125000004093 cyano group Chemical group *C#N 0.000 claims 22
- 125000003545 alkoxy group Chemical group 0.000 claims 21
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 21
- 125000000217 alkyl group Chemical group 0.000 claims 20
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 20
- 229910052757 nitrogen Inorganic materials 0.000 claims 19
- 150000002431 hydrogen Chemical class 0.000 claims 18
- 150000001721 carbon Chemical group 0.000 claims 17
- 125000001153 fluoro group Chemical group F* 0.000 claims 16
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 10
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical compound FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 claims 8
- 125000000753 cycloalkyl group Chemical group 0.000 claims 8
- 229910052731 fluorine Inorganic materials 0.000 claims 8
- 239000011737 fluorine Substances 0.000 claims 8
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 7
- ZAMOUSCENKQFHK-UHFFFAOYSA-N Chlorine atom Chemical compound [Cl] ZAMOUSCENKQFHK-UHFFFAOYSA-N 0.000 claims 6
- 229910052801 chlorine Inorganic materials 0.000 claims 6
- 239000000460 chlorine Substances 0.000 claims 6
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 6
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 6
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims 6
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 6
- 125000000876 trifluoromethoxy group Chemical group FC(F)(F)O* 0.000 claims 6
- 241001430294 unidentified retrovirus Species 0.000 claims 6
- 239000008194 pharmaceutical composition Substances 0.000 claims 5
- WKBOTKDWSSQWDR-UHFFFAOYSA-N Bromine atom Chemical compound [Br] WKBOTKDWSSQWDR-UHFFFAOYSA-N 0.000 claims 4
- GDTBXPJZTBHREO-UHFFFAOYSA-N bromine Substances BrBr GDTBXPJZTBHREO-UHFFFAOYSA-N 0.000 claims 4
- 229910052794 bromium Inorganic materials 0.000 claims 4
- 125000000623 heterocyclic group Chemical group 0.000 claims 4
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 4
- 241000700605 Viruses Species 0.000 claims 3
- 208000015181 infectious disease Diseases 0.000 claims 3
- 230000002265 prevention Effects 0.000 claims 3
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 2
- 125000006272 (C3-C7) cycloalkyl group Chemical group 0.000 claims 2
- ICSNLGPSRYBMBD-UHFFFAOYSA-N 2-aminopyridine Chemical group NC1=CC=CC=N1 ICSNLGPSRYBMBD-UHFFFAOYSA-N 0.000 claims 2
- 125000003349 3-pyridyl group Chemical group N1=C([H])C([*])=C([H])C([H])=C1[H] 0.000 claims 2
- 125000000339 4-pyridyl group Chemical group N1=C([H])C([H])=C([*])C([H])=C1[H] 0.000 claims 2
- 241001465754 Metazoa Species 0.000 claims 2
- 125000003282 alkyl amino group Chemical group 0.000 claims 2
- 125000004786 difluoromethoxy group Chemical group [H]C(F)(F)O* 0.000 claims 2
- 230000006806 disease prevention Effects 0.000 claims 2
- 239000003814 drug Substances 0.000 claims 2
- 238000004519 manufacturing process Methods 0.000 claims 2
- 238000000034 method Methods 0.000 claims 2
- 239000002671 adjuvant Substances 0.000 claims 1
- 201000010099 disease Diseases 0.000 claims 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 1
- PQIOSYKVBBWRRI-UHFFFAOYSA-N methylphosphonyl difluoride Chemical group CP(F)(F)=O PQIOSYKVBBWRRI-UHFFFAOYSA-N 0.000 claims 1
- 231100000252 nontoxic Toxicity 0.000 claims 1
- 230000003000 nontoxic effect Effects 0.000 claims 1
- 230000003612 virological effect Effects 0.000 claims 1
- 0 CC(**C1=C2[U]NC1=O)=C2Cl Chemical compound CC(**C1=C2[U]NC1=O)=C2Cl 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| DE102012016908.6A DE102012016908A1 (de) | 2012-08-17 | 2012-08-17 | Tris-(Hetero)Aryl-Pyrazole und ihre Verwendung |
| DE102012016908.6 | 2012-08-17 | ||
| PCT/EP2013/067201 WO2014027112A1 (de) | 2012-08-17 | 2013-08-16 | Tris-(hetero)aryl-pyrazole und ihre verwendung |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2015524835A JP2015524835A (ja) | 2015-08-27 |
| JP2015524835A5 true JP2015524835A5 (https=) | 2016-08-12 |
Family
ID=48986151
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015527004A Ceased JP2015524835A (ja) | 2012-08-17 | 2013-08-16 | トリ（ヘテロ）アリールピラゾール及びその使用 |
Country Status (27)
| Country | Link |
|---|---|
| US (1) | US9249148B2 (https=) |
| EP (1) | EP2885300A1 (https=) |
| JP (1) | JP2015524835A (https=) |
| KR (1) | KR20150042841A (https=) |
| CN (1) | CN104684913B (https=) |
| AP (1) | AP2015008325A0 (https=) |
| AR (1) | AR092145A1 (https=) |
| AU (1) | AU2013303993A1 (https=) |
| BR (1) | BR112015003115A2 (https=) |
| CA (1) | CA2881997A1 (https=) |
| CL (1) | CL2015000362A1 (https=) |
| CU (1) | CU20150015A7 (https=) |
| DE (1) | DE102012016908A1 (https=) |
| EA (1) | EA201500232A1 (https=) |
| HK (1) | HK1212327A1 (https=) |
| IL (1) | IL237298A0 (https=) |
| MA (1) | MA37928A1 (https=) |
| MX (1) | MX2015002046A (https=) |
| NZ (1) | NZ704727A (https=) |
| PE (1) | PE20150869A1 (https=) |
| PH (1) | PH12015500322B1 (https=) |
| SG (1) | SG11201501183VA (https=) |
| TN (1) | TN2015000045A1 (https=) |
| TW (1) | TW201412720A (https=) |
| UA (1) | UA112488C2 (https=) |
| WO (1) | WO2014027112A1 (https=) |
| ZA (1) | ZA201501078B (https=) |
Families Citing this family (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE102012016908A1 (de) | 2012-08-17 | 2014-02-20 | Aicuris Gmbh & Co. Kg | Tris-(Hetero)Aryl-Pyrazole und ihre Verwendung |
| AR099428A1 (es) * | 2014-02-14 | 2016-07-20 | Aicuris Gmbh & Co Kg | Combinaciones de principios activos farmacéuticos con compuestos basados en tri(hetero)aril pirazoles |
| EP3263567A1 (en) * | 2016-07-01 | 2018-01-03 | AiCuris Anti-infective Cures GmbH | Carboxamide-substituted pyrazoles and tri(hetero)aryl-pyrazoles for use in methods of treating and / or preventing cardiovascular diseases and / or comorbidities thereof |
| MX2020010433A (es) * | 2018-04-04 | 2020-10-28 | Japan Tobacco Inc | Compuestos de pirazol sustituidos con heteroarilo y uso farmaceutico de los mismos. |
Family Cites Families (38)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| PH27357A (en) | 1989-09-22 | 1993-06-21 | Fujisawa Pharmaceutical Co | Pyrazole derivatives and pharmaceutical compositions comprising the same |
| IL104311A (en) | 1992-02-05 | 1997-07-13 | Fujisawa Pharmaceutical Co | Pyrazole derivatives, processes for the preparation thereof and pharmaceutical compositions containing the same |
| FR2692575B1 (fr) | 1992-06-23 | 1995-06-30 | Sanofi Elf | Nouveaux derives du pyrazole, procede pour leur preparation et compositions pharmaceutiques les contenant. |
| US6277847B1 (en) | 1999-04-02 | 2001-08-21 | Fmc Corporation | Herbicidal isoindolinonyl-and 3,4-dihydroisoquinolonyl-substituted heterocycles |
| AU2002363250A1 (en) | 2001-11-01 | 2003-05-12 | Icagen, Inc. | Pyrazole-amides and-sulfonamides |
| US6649638B1 (en) * | 2002-08-14 | 2003-11-18 | Ppd Discovery, Inc. | Prenylation inhibitors and methods of their synthesis and use |
| KR20050083761A (ko) | 2002-12-02 | 2005-08-26 | 후지사와 야꾸힝 고교 가부시키가이샤 | Ｃｏｘ－ｉ저해제로서 유용한 피라졸 유도체 |
| KR20050096956A (ko) | 2003-02-07 | 2005-10-06 | 다이이찌 세이야꾸 가부시기가이샤 | 피라졸 유도체 |
| ATE440085T1 (de) | 2004-02-20 | 2009-09-15 | Astrazeneca Ab | 3-substituierte 1,5-diphenylpyrazolderivate, die sich als cb1-modulatoren eignen |
| PT1732892E (pt) | 2004-03-26 | 2008-12-22 | Hoffmann La Roche | Tetra-hidrocarbazóis e os seus derivados |
| US20080064682A1 (en) | 2004-07-01 | 2008-03-13 | Daiichi Pharmaceutical Co., Ltd. | Pyrazole Derivatives |
| GB0417910D0 (en) | 2004-08-11 | 2004-09-15 | Novartis Ag | Organic compounds |
| DE102004054666A1 (de) | 2004-11-12 | 2006-05-18 | Bayer Cropscience Gmbh | Substituierte Pyrazol-3-carboxamide, Verfahren zur Herstellung und Verwendung als Herbizide und Pflanzenwachstumsregulatoren |
| US8703805B2 (en) | 2005-06-27 | 2014-04-22 | Exelixis Patent Company Llc | Modulators of LXR |
| EP1743637A1 (en) | 2005-07-15 | 2007-01-17 | Laboratorios Del Dr. Esteve, S.A. | Use of substituted pyrazole compounds and combinations thereof for the treatment of the metabolic syndrome |
| WO2007009701A2 (en) | 2005-07-15 | 2007-01-25 | Laboratorios Del Dr. Esteve, S.A. | Use of substituted pyrazole compounds and combinations thereof for the treatment of the metabolic syndrome |
| GB0516661D0 (en) | 2005-08-13 | 2005-09-21 | Astrazeneca Ab | Therapeutic agents |
| NZ566036A (en) | 2005-09-13 | 2010-06-25 | Janssen Pharmaceutica Nv | 2-Aniline-4-aryl substituted thiazole derivatives that modulate the alpha7 nicotinic receptor |
| EP1957076A2 (en) | 2005-11-29 | 2008-08-20 | Merck & Co., Inc. | Thiazole derivatives as cxcr3 receptor modulators |
| JP2009518298A (ja) | 2005-12-01 | 2009-05-07 | バイエル ヘルスケア リミティド ライアビリティ カンパニー | 癌治療に有用な尿素化合物 |
| US20100256357A1 (en) | 2006-08-09 | 2010-10-07 | Agouron Pharmaceuticals, Inc. | Heterocycles useful as inhibitors of carbonic anhydrase |
| 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 |
| GB0625196D0 (en) | 2006-12-18 | 2007-01-24 | 7Tm Pharma As | Modulators of cannabinoid receptor |
| JP4994295B2 (ja) * | 2007-04-20 | 2012-08-08 | 田辺三菱製薬株式会社 | 医薬組成物 |
| JP5498392B2 (ja) | 2007-11-30 | 2014-05-21 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | １，５−ジヒドロ−ピラゾロ［３，４−ｄ］ピリミジン−４−オン誘導体及びｃｎｓ障害の治療のためのｐｄｅ９ａモジュレーターとしてのそれらの使用 |
| AR069650A1 (es) | 2007-12-14 | 2010-02-10 | Actelion Pharmaceuticals Ltd | Derivados de aminopirazol como agonistas no peptidicos del receptor alx humano |
| AU2009216825A1 (en) | 2008-02-18 | 2009-08-27 | F. Hoffmann-La Roche Ag | 4, 5-dihydro-oxazol-2-yl amine derivatives |
| DE102008015033A1 (de) | 2008-03-17 | 2009-09-24 | Aicuris Gmbh & Co. Kg | Substituierte (Pyrazolyl-carbonyl)imidazolidinone und ihre Verwendung |
| DE102008015032A1 (de) | 2008-03-17 | 2009-09-24 | Aicuris Gmbh & Co. Kg | Substituierte Pyrazolamide und ihre Verwendung |
| TW201041888A (en) * | 2009-05-06 | 2010-12-01 | Plexxikon Inc | Compounds and methods for kinase modulation, and indications therefor |
| TW201100441A (en) * | 2009-06-01 | 2011-01-01 | Osi Pharm Inc | Amino pyrimidine anticancer compounds |
| BR112012005960A2 (pt) | 2009-09-17 | 2016-03-15 | Janssen Pharmaceutica Nv | n-fenil-1-(4-piridinil)-1h-pirazol-3-aminas substituídas |
| KR20130049766A (ko) | 2009-11-13 | 2013-05-14 | 메르크 세로노 에스. 에이. | 트리사이클릭 피라졸 아민 유도체 |
| US20130210809A1 (en) | 2010-07-14 | 2013-08-15 | Christelle Boléa | Novel 2-amino-4-pyrazolyl-thiazole derivatives and their use as allosteric modulators of metabotropic glutamate receptors |
| EP2632461A4 (en) | 2010-10-29 | 2014-04-02 | Merck Sharp & Dohme | Isoindolinone PDE10 INHIBITORS |
| US9938269B2 (en) | 2011-06-30 | 2018-04-10 | Abbvie Inc. | Inhibitor compounds of phosphodiesterase type 10A |
| DE102012016908A1 (de) | 2012-08-17 | 2014-02-20 | Aicuris Gmbh & Co. Kg | Tris-(Hetero)Aryl-Pyrazole und ihre Verwendung |
| AR099428A1 (es) | 2014-02-14 | 2016-07-20 | Aicuris Gmbh & Co Kg | Combinaciones de principios activos farmacéuticos con compuestos basados en tri(hetero)aril pirazoles |
-
2012
- 2012-08-17 DE DE102012016908.6A patent/DE102012016908A1/de not_active Withdrawn
-
2013
- 2013-08-15 AR ARP130102907A patent/AR092145A1/es unknown
- 2013-08-16 NZ NZ704727A patent/NZ704727A/en not_active IP Right Cessation
- 2013-08-16 MX MX2015002046A patent/MX2015002046A/es unknown
- 2013-08-16 EA EA201500232A patent/EA201500232A1/ru unknown
- 2013-08-16 JP JP2015527004A patent/JP2015524835A/ja not_active Ceased
- 2013-08-16 MA MA37928A patent/MA37928A1/fr unknown
- 2013-08-16 KR KR20157006414A patent/KR20150042841A/ko not_active Withdrawn
- 2013-08-16 SG SG11201501183VA patent/SG11201501183VA/en unknown
- 2013-08-16 HK HK15112600.0A patent/HK1212327A1/xx unknown
- 2013-08-16 AU AU2013303993A patent/AU2013303993A1/en not_active Abandoned
- 2013-08-16 BR BR112015003115A patent/BR112015003115A2/pt not_active IP Right Cessation
- 2013-08-16 WO PCT/EP2013/067201 patent/WO2014027112A1/de not_active Ceased
- 2013-08-16 UA UAA201502210A patent/UA112488C2/uk unknown
- 2013-08-16 CN CN201380044128.1A patent/CN104684913B/zh not_active Expired - Fee Related
- 2013-08-16 PE PE2015000171A patent/PE20150869A1/es not_active Application Discontinuation
- 2013-08-16 AP AP2015008325A patent/AP2015008325A0/xx unknown
- 2013-08-16 US US14/422,191 patent/US9249148B2/en not_active Expired - Fee Related
- 2013-08-16 CA CA2881997A patent/CA2881997A1/en not_active Abandoned
- 2013-08-16 TW TW102129567A patent/TW201412720A/zh unknown
- 2013-08-16 EP EP13750087.2A patent/EP2885300A1/de not_active Withdrawn
-
2015
- 2015-02-12 TN TNP2015000045A patent/TN2015000045A1/fr unknown
- 2015-02-13 PH PH12015500322A patent/PH12015500322B1/en unknown
- 2015-02-16 ZA ZA2015/01078A patent/ZA201501078B/en unknown
- 2015-02-16 CL CL2015000362A patent/CL2015000362A1/es unknown
- 2015-02-17 IL IL237298A patent/IL237298A0/en unknown
- 2015-02-17 CU CUP2015000015A patent/CU20150015A7/es unknown