JP2006522035A5 - - Google Patents
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- Publication number
- JP2006522035A5 JP2006522035A5 JP2006504584A JP2006504584A JP2006522035A5 JP 2006522035 A5 JP2006522035 A5 JP 2006522035A5 JP 2006504584 A JP2006504584 A JP 2006504584A JP 2006504584 A JP2006504584 A JP 2006504584A JP 2006522035 A5 JP2006522035 A5 JP 2006522035A5
- Authority
- JP
- Japan
- Prior art keywords
- atoms
- hal
- cycloalkyl
- unsubstituted
- het
- 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
- 125000001997 phenyl group Chemical class [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 2
- 125000004432 carbon atom Chemical group C* 0.000 claims 8
- 125000000753 cycloalkyl group Chemical group 0.000 claims 4
- 108091032151 5-hydroxytryptamine receptor family Proteins 0.000 claims 1
- HBAQYPYDRFILMT-UHFFFAOYSA-N 8-[3-(1-cyclopropylpyrazol-4-yl)-1H-pyrazolo[4,3-d]pyrimidin-5-yl]-3-methyl-3,8-diazabicyclo[3.2.1]octan-2-one Chemical class C1(CC1)N1N=CC(=C1)C1=NNC2=C1N=C(N=C2)N1C2C(N(CC1CC2)C)=O HBAQYPYDRFILMT-UHFFFAOYSA-N 0.000 claims 1
- 102000014630 G protein-coupled serotonin receptor activity proteins Human genes 0.000 claims 1
- 125000003342 alkenyl group Chemical group 0.000 claims 1
- 125000004183 alkoxy alkyl group Chemical group 0.000 claims 1
- 125000000217 alkyl group Chemical group 0.000 claims 1
- 125000002618 bicyclic heterocycle group Chemical group 0.000 claims 1
- 150000001875 compounds Chemical class 0.000 claims 1
- 230000006806 disease prevention Effects 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 125000005842 heteroatom Chemical group 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 150000003839 salts Chemical class 0.000 claims 1
- 229920006395 saturated elastomer Polymers 0.000 claims 1
- 239000012453 solvate Substances 0.000 claims 1
- 125000003118 aryl group Chemical group 0.000 description 1
- 125000000962 organic group Chemical group 0.000 description 1
Description
Arは、芳香族有機基、特に非置換であるか、またはAおよび/またはHal、OR5、OOCR5、COOR5、CON(R5)2、CN、NO2、NH2、NHCOR5、CF3あるいはSO2CH3 により単置換もしくは多置換されているフェニル基を示し、
nは、0、1、2、3、4または5を示し、
Halは、F、Cl、BrまたはIを示す、
nは、0、1、2、3、4または5を示し、
Halは、F、Cl、BrまたはIを示す、
Claims (1)
- 式I
式中、
Xは、CHまたはNを示し、
R1は、H、A、Hal、(CH2)nHet、(CH2)nAr、3〜7個のC原子を有するシクロアルキル、CF3、NO2、CN、C(NH)NOHまたはOCF3を示し、
R2は、(CH2)nHet、(CH2)nAr、3〜7個のC原子を有するシクロアルキルまたはCF3を示し、
R3、R4は、
を示し、ここで、各々の場合において、基R3またはR4の1つは、Hの意味を有し、
R5は、HまたはAを示し、
Aは、1〜10個のC原子を有する直鎖状もしくは分枝状アルキルまたはシクロアルキル、2〜10個のC原子を有するアルケニル、2〜10個のC原子を有するアルコキシアルキルまたは4〜7個のC原子を有するシクロアルキルを示し、この各々は、非置換であるか、またはHalもしくはCNにより置換されており、
Hetは、好ましくは、1〜15個のC原子を有し、非置換であるか、またはAおよび/またはHalにより単置換もしくは多置換されている、飽和、不飽和または芳香族単環式または二環式複素環式基、あるいは1個または2個のヘテロ原子を含む、1〜15個のC原子を有する直鎖状基を示し、
Arは、非置換であるか、またはAおよび/またはHal、OR5、OOCR5、COOR5、CON(R5)2、CN、NO2、NH2、NHCOR5、CF3あるいはSO2CH3 により単置換もしくは多置換されているフェニル基を示し、
nは、0、1、2、3、4または5を示し、
Halは、F、Cl、BrまたはIを示す、
で表される化合物並びにこれらの塩および溶媒和物、鏡像体およびラセミ体の、式Iで表される化合物の5HTレセプターへの結合により影響され得る疾患の処置および予防のための医薬の製造のための使用。
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| DE10315572.4 | 2003-04-05 | ||
| DE10315572A DE10315572A1 (de) | 2003-04-05 | 2003-04-05 | Substituierte Pyrazole |
| PCT/EP2004/002353 WO2004089931A1 (de) | 2003-04-05 | 2004-03-08 | Substituierte pyrazole |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2011037046A Division JP2011148803A (ja) | 2003-04-05 | 2011-02-23 | 置換ピラゾール |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2006522035A JP2006522035A (ja) | 2006-09-28 |
| JP2006522035A5 true JP2006522035A5 (ja) | 2011-04-14 |
| JP4740115B2 JP4740115B2 (ja) | 2011-08-03 |
Family
ID=32981073
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2006504584A Expired - Fee Related JP4740115B2 (ja) | 2003-04-05 | 2004-03-08 | 置換ピラゾール |
| JP2011037046A Pending JP2011148803A (ja) | 2003-04-05 | 2011-02-23 | 置換ピラゾール |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2011037046A Pending JP2011148803A (ja) | 2003-04-05 | 2011-02-23 | 置換ピラゾール |
Country Status (14)
| Country | Link |
|---|---|
| US (1) | US20060264419A1 (ja) |
| EP (1) | EP1626967A1 (ja) |
| JP (2) | JP4740115B2 (ja) |
| KR (1) | KR20050119193A (ja) |
| CN (1) | CN1768051A (ja) |
| AR (1) | AR043837A1 (ja) |
| AU (1) | AU2004228120B2 (ja) |
| BR (1) | BRPI0409164A (ja) |
| CA (1) | CA2521201A1 (ja) |
| DE (1) | DE10315572A1 (ja) |
| MX (1) | MXPA05010652A (ja) |
| PL (1) | PL377844A1 (ja) |
| WO (1) | WO2004089931A1 (ja) |
| ZA (1) | ZA200508948B (ja) |
Families Citing this family (37)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE10315573A1 (de) | 2003-04-05 | 2004-10-14 | Merck Patent Gmbh | Substituierte Pyrazole |
| DE10315569A1 (de) * | 2003-04-05 | 2004-10-14 | Merck Patent Gmbh | Substituierte Pyrazolverbindungen |
| DE10315571A1 (de) * | 2003-04-05 | 2004-10-14 | Merck Patent Gmbh | Pyrazolverbindungen |
| EP1669348A4 (en) | 2003-09-30 | 2009-03-11 | Eisai R&D Man Co Ltd | NEW ANTIPILIC AGENT CONTAINING A HETEROCYCLIC COMPOUND |
| EP1670460B1 (en) * | 2003-10-10 | 2014-11-26 | Bristol-Myers Squibb Company | Pyrazole derivatives as cannabinoid receptor modulators |
| US20050241110A1 (en) * | 2004-04-09 | 2005-11-03 | Bruce Baker | Ergonomic handles, especially for garden tools |
| US20090227799A1 (en) * | 2004-08-09 | 2009-09-10 | Kazutaka Nakamoto | Novel Antimalarial Agent Containing Heterocyclic Compound |
| US7829585B2 (en) | 2005-03-30 | 2010-11-09 | Eisai R&D Management Co., Ltd. | Antifungal agent containing pyridine derivative |
| AU2006309762B2 (en) | 2005-10-31 | 2010-02-25 | Eisai R&D Management Co., Ltd. | Heterocyclic substituted pyridine derivatives and antifungal agent containing same |
| TWI385169B (zh) | 2005-10-31 | 2013-02-11 | Eisai R&D Man Co Ltd | 經雜環取代之吡啶衍生物及含有彼之抗真菌劑 |
| GB0524814D0 (en) * | 2005-12-05 | 2006-01-11 | Glaxo Group Ltd | Compounds |
| EP2004627A2 (en) * | 2006-04-10 | 2008-12-24 | Arena Pharmaceuticals, Inc. | 3-pyridinyl-pyrazole derivatives as modulators of the 5-ht2a serotonin receptor useful for the treatment of disorders related thereto |
| US8183264B2 (en) * | 2006-09-21 | 2012-05-22 | Eisai R&D Managment Co., Ltd. | Pyridine derivative substituted by heteroaryl ring, and antifungal agent comprising the same |
| EP1938686A1 (de) * | 2006-12-29 | 2008-07-02 | Bayer CropScience AG | Substituierte 1-(3-Pyridinyl)pyrazol-4-yl-essigsäuren, Verfahren zu deren Herstellung und deren Verwendung als Herbizide und Pflanzenwachstumsregulatoren |
| TW200841879A (en) | 2007-04-27 | 2008-11-01 | Eisai R&D Man Co Ltd | Pyridine derivatives substituted by heterocyclic ring and phosphonoamino group, and anti-fungal agent containing same |
| CN101622251B (zh) | 2007-04-27 | 2012-07-04 | 卫材R&D管理有限公司 | 杂环取代吡啶衍生物的盐或其结晶 |
| US7977358B2 (en) | 2007-07-26 | 2011-07-12 | Hoffmann-La Roche Inc. | Pyrazol derivatives |
| US8513287B2 (en) | 2007-12-27 | 2013-08-20 | Eisai R&D Management Co., Ltd. | Heterocyclic ring and phosphonoxymethyl group substituted pyridine derivatives and antifungal agent containing same |
| EP2135865A1 (de) | 2008-06-17 | 2009-12-23 | Bayer CropScience AG | Substituierte 1-(Diazinyl) pyrazol-4-yl-essigsäuren, Verfahren zu deren Herstellung und deren Verwendung als Herbizide und Pflanzenwachstumsregulatoren |
| WO2010032874A1 (ja) * | 2008-09-19 | 2010-03-25 | 住友化学株式会社 | 農業用組成物 |
| US8188119B2 (en) | 2008-10-24 | 2012-05-29 | Eisai R&D Management Co., Ltd | Pyridine derivatives substituted with heterocyclic ring and γ-glutamylamino group, and antifungal agents containing same |
| EP2194052A1 (de) | 2008-12-06 | 2010-06-09 | Bayer CropScience AG | Substituierte 1-(Thiazolyl)- und 1-(Isothiazolyl)pyrazol-4-yl-essigsäuren, Verfahren zu deren Herstellung und deren Verwendung als Herbizide und Pflanzenwachstumsregulatoren |
| WO2011073098A1 (de) | 2009-12-15 | 2011-06-23 | Bayer Cropscience Ag | 1-(heteroaryl)-pyrazol-4-yl-essigsäuren, verfahren zu deren herstellung und deren verwendung als herbizide und pflanzenwachstumsregulatoren |
| WO2012008528A1 (ja) * | 2010-07-15 | 2012-01-19 | 大日本住友製薬株式会社 | ピラゾール化合物 |
| WO2014144659A1 (en) | 2013-03-14 | 2014-09-18 | Epizyme, Inc. | Pyrazole derivatives as prmt1 inhibitors and uses thereof |
| WO2014153172A1 (en) | 2013-03-14 | 2014-09-25 | Epizyme, Inc. | Pyrazole derivatives as prmt1 inhibitors and uses thereof |
| US9120757B2 (en) | 2013-03-14 | 2015-09-01 | Epizyme, Inc. | Arginine methyltransferase inhibitors and uses thereof |
| US9765035B2 (en) | 2013-03-14 | 2017-09-19 | Epizyme, Inc. | Arginine methyltransferase inhibitors and uses thereof |
| EP2970131B1 (en) | 2013-03-14 | 2017-11-15 | Epizyme, Inc. | Arginine methyltransferase inhibitors and uses thereof |
| WO2014153208A1 (en) | 2013-03-14 | 2014-09-25 | Epizyme, Inc. | Arginine methyltransferase inhibitors and uses thereof |
| CA2903264A1 (en) | 2013-03-14 | 2014-11-06 | Epizyme, Inc. | Pyrazole derivatives as arginine methyltransferase inhibitors and uses thereof |
| BR112015022785A2 (pt) | 2013-03-14 | 2017-07-18 | Epizyme Inc | composto; composição farmacêutica; kit ou artigo farmacêutico embalado; método de inibição de uma arginina metil transferase (rmt); método de modulação da expressão genética; método de modulação da transcrição; e método de tratamento de um distúrbio mediado por rmt |
| WO2014153090A1 (en) * | 2013-03-14 | 2014-09-25 | Epizyme, Inc. | Pyrazole derivatives asprmt1 inhibitors and uses thereof |
| EP2970136A1 (en) | 2013-03-14 | 2016-01-20 | Epizyme, Inc. | Arginine methyl transferase inhibtors and uses thereof |
| US11034669B2 (en) | 2018-11-30 | 2021-06-15 | Nuvation Bio Inc. | Pyrrole and pyrazole compounds and methods of use thereof |
| CN116554144B (zh) * | 2022-01-27 | 2025-12-19 | 司马健 | 一种sj系列芳基苯胺类化合物及其制备方法与医药用途 |
| DE202022104072U1 (de) | 2022-07-19 | 2022-07-29 | Siva Subramanian Narayanasamy | Heterozyklisch substituierte pyridinderivate antimykotische Mittel |
Family Cites Families (15)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4146721A (en) * | 1969-09-12 | 1979-03-27 | Byk Gulden Lomberg Chemische Fabrik Gmbh | Pyrazol-4-acetic acid compounds |
| BE793955A (fr) * | 1972-01-15 | 1973-07-12 | Merck Patent Gmbh | Arylpiperazines et leur procede de preparation |
| DE2906252A1 (de) * | 1979-02-19 | 1980-08-28 | Merck Patent Gmbh | Pyrazolderivate, diese enthaltende pharmazeutische zubereitungen und verfahren zu ihrer herstellung |
| US4631343A (en) * | 1983-11-07 | 1986-12-23 | Eli Lilly And Company | Cyanopyrazole intermediates |
| US6011028A (en) * | 1995-04-20 | 2000-01-04 | G.D. Searle & Co. | Cyclic amidino agents useful as nitric oxide synthase inhibitors |
| US6150393A (en) * | 1998-12-18 | 2000-11-21 | Arena Pharmaceuticals, Inc. | Small molecule modulators of non-endogenous, constitutively activated human serotonin receptors |
| US20010044445A1 (en) * | 1999-04-08 | 2001-11-22 | Bamaung Nwe Y. | Azole inhibitors of cytokine production |
| US6632815B2 (en) * | 1999-09-17 | 2003-10-14 | Millennium Pharmaceuticals, Inc. | Inhibitors of factor Xa |
| BR0210391A (pt) * | 2001-06-12 | 2004-06-15 | Elan Pharm Inc | Composto, métodos de tratar um paciente que tenha ou de prevenir um paciente de contrair uma doença ou condição e de preparar um composto, e, uso de um composto |
| DE10149370A1 (de) * | 2001-10-06 | 2003-04-10 | Merck Patent Gmbh | Pyrazolderivate |
| CA2481934A1 (en) * | 2002-04-18 | 2003-10-30 | Pharmacia Corporation | Combinations of cox-2 inhibitors and other agents for the treatment of parkinson's disease |
| DE10315571A1 (de) * | 2003-04-05 | 2004-10-14 | Merck Patent Gmbh | Pyrazolverbindungen |
| DE10315569A1 (de) * | 2003-04-05 | 2004-10-14 | Merck Patent Gmbh | Substituierte Pyrazolverbindungen |
| DE10315573A1 (de) * | 2003-04-05 | 2004-10-14 | Merck Patent Gmbh | Substituierte Pyrazole |
| US20070093492A1 (en) * | 2004-03-09 | 2007-04-26 | Weir-Torn Jiaang | Pyrrolidine derivatives |
-
2003
- 2003-04-05 DE DE10315572A patent/DE10315572A1/de not_active Withdrawn
-
2004
- 2004-03-08 EP EP04718277A patent/EP1626967A1/de not_active Withdrawn
- 2004-03-08 KR KR1020057018895A patent/KR20050119193A/ko not_active Withdrawn
- 2004-03-08 CN CNA2004800085729A patent/CN1768051A/zh active Pending
- 2004-03-08 CA CA002521201A patent/CA2521201A1/en not_active Abandoned
- 2004-03-08 BR BRPI0409164-7A patent/BRPI0409164A/pt not_active Application Discontinuation
- 2004-03-08 MX MXPA05010652A patent/MXPA05010652A/es not_active Application Discontinuation
- 2004-03-08 PL PL377844A patent/PL377844A1/pl unknown
- 2004-03-08 US US10/552,065 patent/US20060264419A1/en not_active Abandoned
- 2004-03-08 JP JP2006504584A patent/JP4740115B2/ja not_active Expired - Fee Related
- 2004-03-08 WO PCT/EP2004/002353 patent/WO2004089931A1/de not_active Ceased
- 2004-03-08 AU AU2004228120A patent/AU2004228120B2/en not_active Ceased
- 2004-04-02 AR ARP040101119A patent/AR043837A1/es unknown
-
2005
- 2005-11-04 ZA ZA200508948A patent/ZA200508948B/en unknown
-
2011
- 2011-02-23 JP JP2011037046A patent/JP2011148803A/ja active Pending
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