JP2006522039A5 - - Google Patents
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- Publication number
- JP2006522039A5 JP2006522039A5 JP2006504620A JP2006504620A JP2006522039A5 JP 2006522039 A5 JP2006522039 A5 JP 2006522039A5 JP 2006504620 A JP2006504620 A JP 2006504620A JP 2006504620 A JP2006504620 A JP 2006504620A JP 2006522039 A5 JP2006522039 A5 JP 2006522039A5
- Authority
- JP
- Japan
- Prior art keywords
- solvate
- compound according
- het
- formula
- salt
- 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 description 22
- 201000010099 disease Diseases 0.000 claims description 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 2
- 230000002265 prevention Effects 0.000 claims description 2
- 150000003839 salts Chemical class 0.000 claims 17
- 239000012453 solvate Substances 0.000 claims 15
- 239000000203 mixture Substances 0.000 claims 9
- 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 8
- 125000004432 carbon atom Chemical group C* 0.000 claims 6
- 239000003814 drug Substances 0.000 claims 5
- 238000004519 manufacturing process Methods 0.000 claims 5
- GVNVAWHJIKLAGL-UHFFFAOYSA-N 2-(cyclohexen-1-yl)cyclohexan-1-one Chemical compound O=C1CCCCC1C1=CCCCC1 GVNVAWHJIKLAGL-UHFFFAOYSA-N 0.000 claims 3
- -1 5-oxazolyl Chemical group 0.000 claims 3
- 101150065749 Churc1 gene Proteins 0.000 claims 3
- 102100038239 Protein Churchill Human genes 0.000 claims 3
- 125000000217 alkyl group Chemical group 0.000 claims 3
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 3
- 125000004198 2-fluorophenyl group Chemical group [H]C1=C([H])C(F)=C(*)C([H])=C1[H] 0.000 claims 2
- 125000000175 2-thienyl group Chemical group S1C([*])=C([H])C([H])=C1[H] 0.000 claims 2
- 125000004180 3-fluorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C(F)=C1[H] 0.000 claims 2
- 125000001541 3-thienyl group Chemical group S1C([H])=C([*])C([H])=C1[H] 0.000 claims 2
- 125000001255 4-fluorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C([H])=C1F 0.000 claims 2
- 108091032151 5-hydroxytryptamine receptor family Proteins 0.000 claims 2
- 102000014630 G protein-coupled serotonin receptor activity proteins Human genes 0.000 claims 2
- 208000021384 Obsessive-Compulsive disease Diseases 0.000 claims 2
- 239000002253 acid Substances 0.000 claims 2
- 230000003042 antagnostic effect Effects 0.000 claims 2
- 150000007514 bases Chemical class 0.000 claims 2
- 125000000753 cycloalkyl group Chemical group 0.000 claims 2
- 239000007788 liquid Substances 0.000 claims 2
- 238000000034 method Methods 0.000 claims 2
- 239000008194 pharmaceutical composition Substances 0.000 claims 2
- 125000002941 2-furyl group Chemical group O1C([*])=C([H])C([H])=C1[H] 0.000 claims 1
- 125000004105 2-pyridyl group Chemical group N1=C([*])C([H])=C([H])C([H])=C1[H] 0.000 claims 1
- 125000004361 3,4,5-trifluorophenyl group Chemical group [H]C1=C(F)C(F)=C(F)C([H])=C1* 0.000 claims 1
- 125000003682 3-furyl group Chemical group O1C([H])=C([*])C([H])=C1[H] 0.000 claims 1
- 125000003349 3-pyridyl group Chemical group N1=C([H])C([*])=C([H])C([H])=C1[H] 0.000 claims 1
- 125000004801 4-cyanophenyl group Chemical group [H]C1=C([H])C(C#N)=C([H])C([H])=C1* 0.000 claims 1
- 125000000339 4-pyridyl group Chemical group N1=C([H])C([H])=C([*])C([H])=C1[H] 0.000 claims 1
- KDDQRKBRJSGMQE-UHFFFAOYSA-N 4-thiazolyl Chemical compound [C]1=CSC=N1 KDDQRKBRJSGMQE-UHFFFAOYSA-N 0.000 claims 1
- 102000049773 5-HT2A Serotonin Receptor Human genes 0.000 claims 1
- 108010072564 5-HT2A Serotonin Receptor Proteins 0.000 claims 1
- CWDWFSXUQODZGW-UHFFFAOYSA-N 5-thiazolyl Chemical group [C]1=CN=CS1 CWDWFSXUQODZGW-UHFFFAOYSA-N 0.000 claims 1
- 208000032841 Bulimia Diseases 0.000 claims 1
- 206010006550 Bulimia nervosa Diseases 0.000 claims 1
- 208000030814 Eating disease Diseases 0.000 claims 1
- 208000019454 Feeding and Eating disease Diseases 0.000 claims 1
- 208000012902 Nervous system disease Diseases 0.000 claims 1
- 208000025966 Neurological disease Diseases 0.000 claims 1
- 206010036618 Premenstrual syndrome Diseases 0.000 claims 1
- 239000002671 adjuvant Substances 0.000 claims 1
- 125000003342 alkenyl group Chemical group 0.000 claims 1
- 125000004183 alkoxy alkyl group Chemical group 0.000 claims 1
- 125000003545 alkoxy group Chemical group 0.000 claims 1
- 206010002026 amyotrophic lateral sclerosis Diseases 0.000 claims 1
- 208000022531 anorexia Diseases 0.000 claims 1
- 125000003118 aryl group Chemical group 0.000 claims 1
- 125000002618 bicyclic heterocycle group Chemical group 0.000 claims 1
- 229910052799 carbon Inorganic materials 0.000 claims 1
- 206010061428 decreased appetite Diseases 0.000 claims 1
- 235000014632 disordered eating Nutrition 0.000 claims 1
- 239000002552 dosage form Substances 0.000 claims 1
- 125000005842 heteroatom Chemical group 0.000 claims 1
- 125000002183 isoquinolinyl group Chemical group C1(=NC=CC2=CC=CC=C12)* 0.000 claims 1
- 125000002911 monocyclic heterocycle group Chemical group 0.000 claims 1
- 125000000962 organic group Chemical group 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 125000003373 pyrazinyl group Chemical group 0.000 claims 1
- 125000002943 quinolinyl group Chemical group N1=C(C=CC2=CC=CC=C12)* 0.000 claims 1
- 229920006395 saturated elastomer Polymers 0.000 claims 1
- 239000007787 solid Substances 0.000 claims 1
- 239000004480 active ingredient Substances 0.000 description 2
- 208000024172 Cardiovascular disease Diseases 0.000 description 1
- BGHDUTQZGWOQIA-VQSKNWBGSA-N Ergovaline Chemical compound C1=CC(C=2[C@H](N(C)C[C@@H](C=2)C(=O)N[C@]2(C(=O)N3[C@H](C(N4CCC[C@H]4[C@]3(O)O2)=O)C(C)C)C)C2)=C3C2=CNC3=C1 BGHDUTQZGWOQIA-VQSKNWBGSA-N 0.000 description 1
- 208000027776 Extrapyramidal disease Diseases 0.000 description 1
- 208000018522 Gastrointestinal disease Diseases 0.000 description 1
- 208000010412 Glaucoma Diseases 0.000 description 1
- 206010020772 Hypertension Diseases 0.000 description 1
- 241001465754 Metazoa Species 0.000 description 1
- 208000007536 Thrombosis Diseases 0.000 description 1
- 206010070863 Toxicity to various agents Diseases 0.000 description 1
- 206010047163 Vasospasm Diseases 0.000 description 1
- 210000000748 cardiovascular system Anatomy 0.000 description 1
- 208000030172 endocrine system disease Diseases 0.000 description 1
- BGHDUTQZGWOQIA-RKUMIMICSA-N ergovaline Natural products O=C(N[C@@]1(C)C(=O)N2[C@H](C(C)C)C(=O)N3[C@@H]([C@]2(O)O1)CCC3)[C@@H]1C=C2[C@H](N(C)C1)Cc1c3c([nH]c1)cccc23 BGHDUTQZGWOQIA-RKUMIMICSA-N 0.000 description 1
- 208000031424 hyperprolactinemia Diseases 0.000 description 1
- 230000004410 intraocular pressure Effects 0.000 description 1
- 201000000980 schizophrenia Diseases 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| DE10315569.4 | 2003-04-05 | ||
| DE2003115569 DE10315569A1 (de) | 2003-04-05 | 2003-04-05 | Substituierte Pyrazolverbindungen |
| PCT/EP2004/002453 WO2004089932A1 (de) | 2003-04-05 | 2004-03-10 | Substituierte pyrazolverbindungen |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2011041150A Division JP2011153144A (ja) | 2003-04-05 | 2011-02-28 | 置換ピラゾール化合物 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2006522039A JP2006522039A (ja) | 2006-09-28 |
| JP2006522039A5 true JP2006522039A5 (https=) | 2011-04-28 |
| JP4740117B2 JP4740117B2 (ja) | 2011-08-03 |
Family
ID=32981070
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2006504620A Expired - Fee Related JP4740117B2 (ja) | 2003-04-05 | 2004-03-10 | 置換ピラゾール化合物 |
| JP2011041150A Pending JP2011153144A (ja) | 2003-04-05 | 2011-02-28 | 置換ピラゾール化合物 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2011041150A Pending JP2011153144A (ja) | 2003-04-05 | 2011-02-28 | 置換ピラゾール化合物 |
Country Status (15)
| Country | Link |
|---|---|
| US (1) | US7842695B2 (https=) |
| EP (1) | EP1611122B1 (https=) |
| JP (2) | JP4740117B2 (https=) |
| KR (1) | KR20050119192A (https=) |
| CN (1) | CN1768052A (https=) |
| AR (1) | AR043835A1 (https=) |
| AT (1) | ATE364601T1 (https=) |
| BR (1) | BRPI0408986A (https=) |
| CA (1) | CA2521227A1 (https=) |
| DE (2) | DE10315569A1 (https=) |
| ES (1) | ES2287710T3 (https=) |
| MX (1) | MXPA05010650A (https=) |
| PL (1) | PL377604A1 (https=) |
| WO (1) | WO2004089932A1 (https=) |
| ZA (1) | ZA200508923B (https=) |
Families Citing this family (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE10315573A1 (de) | 2003-04-05 | 2004-10-14 | Merck Patent Gmbh | Substituierte Pyrazole |
| DE10315572A1 (de) * | 2003-04-05 | 2004-10-14 | Merck Patent Gmbh | Substituierte Pyrazole |
| DE10315571A1 (de) * | 2003-04-05 | 2004-10-14 | Merck Patent Gmbh | Pyrazolverbindungen |
| WO2005037199A2 (en) | 2003-10-10 | 2005-04-28 | Bristol-Myers Squibb Company | Pyrazole derivatives as cannabinoid receptor modulators |
| BRPI0612287A8 (pt) | 2005-06-27 | 2019-01-22 | Exelixis Inc | composição para uso farmacêutico no tratamento de doenças através da medicina nuclear e métodos de uso e para modulação de atividade de receptor nuclear |
| JP2008169191A (ja) * | 2006-02-20 | 2008-07-24 | Eisai R & D Management Co Ltd | 運動ニューロン疾患治療剤 |
| WO2007120600A2 (en) * | 2006-04-10 | 2007-10-25 | Arena Pharmaceuticals, Inc. | 3-pyridinyl-pyrazole derivatives as modulators of the 5-ht2a serotonin receptor useful for the treatment of disorders related thereto |
| KR20090094125A (ko) | 2006-12-08 | 2009-09-03 | 엑셀리시스, 인코포레이티드 | Ｌｘｒ 및 ｆｘｒ 조절자 |
| EP2375899B1 (en) * | 2009-01-12 | 2015-02-25 | Array Biopharma Inc. | Piperidine-containing compounds and use thereof in the treatment of diabetes |
| AU2011277426B2 (en) | 2010-07-15 | 2015-04-23 | Sumitomo Pharma Co., Ltd. | Pyrazole compound |
| CA3121202A1 (en) | 2018-11-30 | 2020-06-04 | Nuvation Bio Inc. | Pyrrole and pyrazole compounds and methods of use thereof |
Family Cites Families (30)
| 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 |
| CH518155A (de) | 1970-08-18 | 1972-01-31 | Schaerer Willy | Verfahren zur Erleichterung des Schleifens schraubenlinienförmiger Nuten, bei einer Serie von unter sich gleichen Werkstücken mit je mindestens einer schraubenlinienförmig eingefrästen Nut und Simuliergerät zur Durchführung des Verfahrens |
| BE793955A (fr) | 1972-01-15 | 1973-07-12 | Merck Patent Gmbh | Arylpiperazines et leur procede de preparation |
| DE2258033A1 (de) | 1972-11-27 | 1974-05-30 | Merck Patent Gmbh | Verfahren zur herstellung von pyrazolderivaten |
| 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 |
| JPH089599B2 (ja) * | 1988-08-02 | 1996-01-31 | 三井東圧化学株式会社 | ピラゾールカルボン酸類の製造方法 |
| DE4425146A1 (de) * | 1994-07-15 | 1996-01-18 | Basf Ag | Verwendung heterocyclischer Verbindungen |
| US6159393A (en) | 1994-08-06 | 2000-12-12 | Merck Patent Gesellschaft Mit Beschrankter Haftung | Benzene derivatives and liquid-crystalline medium |
| DE69629364T2 (de) | 1995-04-20 | 2004-06-09 | G.D. Searle & Co., Chicago | Zyclische amidino mittel als stickstoffoxid-synthase inhibitoren |
| JPH09227555A (ja) * | 1996-02-16 | 1997-09-02 | Taisho Pharmaceut Co Ltd | チエニルピラゾール誘導体 |
| DE69822449T2 (de) | 1997-01-21 | 2005-01-27 | Smithkline Beecham Corp. | Neue cannabinoidrezeptor-modulatoren |
| 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 |
| MXPA02004004A (es) * | 1999-10-29 | 2002-10-23 | Boehringer Ingelheim Pharma | Proceso para la preparacion de pirazoles substituidos. |
| JP2003513075A (ja) | 1999-11-05 | 2003-04-08 | スミスクライン ビーチャム パブリック リミテッド カンパニー | 複合５ｈｔ１ａ、５ｈｔ１ｂおよび５ｈｔ１ｄ受容体活性を有するイソキノリンおよびキナゾリン誘導体 |
| AP2002002460A0 (en) * | 2001-03-09 | 2002-06-30 | Pfizer Prod Inc | Novel benzimidazole anti-inflammatory compounds. |
| EP1395257A1 (en) * | 2001-06-12 | 2004-03-10 | Elan Pharmaceuticals, Inc. | Macrocycles useful in the treatment of alzheimer's disease |
| US20030130199A1 (en) * | 2001-06-27 | 2003-07-10 | Von Hoersten Stephan | Dipeptidyl peptidase IV inhibitors and their uses as anti-cancer agents |
| DE10149370A1 (de) | 2001-10-06 | 2003-04-10 | Merck Patent Gmbh | Pyrazolderivate |
| GR1004118B (el) | 2001-10-11 | 2003-01-21 | Ηλεκτροχημικη μεθοδος υγρης οξειδωσης-αποστειρωσης υγρων αποβλητων απο σφαγεια ψαριων | |
| US20040034083A1 (en) * | 2002-04-18 | 2004-02-19 | Stephenson Diane T. | Combination therapy for the treatment of Parkinson's disease with cyclooxygenase-2 (COX2) inhibitor(s) |
| US20060148858A1 (en) | 2002-05-24 | 2006-07-06 | Tsuyoshi Maekawa | 1, 2-Azole derivatives with hypoglycemic and hypolipidemic activity |
| WO2004024705A1 (ja) | 2002-09-10 | 2004-03-25 | Takeda Pharmaceutical Company Limited | ５員複素環化合物 |
| AU2003287965A1 (en) | 2002-10-24 | 2004-05-13 | Carex Sa | Modulation of peroxisome proliferator activated receptors activity |
| DE10315572A1 (de) * | 2003-04-05 | 2004-10-14 | Merck Patent Gmbh | Substituierte Pyrazole |
| DE10315573A1 (de) * | 2003-04-05 | 2004-10-14 | Merck Patent Gmbh | Substituierte Pyrazole |
| DE10315571A1 (de) * | 2003-04-05 | 2004-10-14 | Merck Patent Gmbh | Pyrazolverbindungen |
| US20070093492A1 (en) * | 2004-03-09 | 2007-04-26 | Weir-Torn Jiaang | Pyrrolidine derivatives |
-
2003
- 2003-04-05 DE DE2003115569 patent/DE10315569A1/de not_active Withdrawn
-
2004
- 2004-03-10 KR KR1020057018893A patent/KR20050119192A/ko not_active Withdrawn
- 2004-03-10 DE DE502004004089T patent/DE502004004089D1/de not_active Expired - Lifetime
- 2004-03-10 MX MXPA05010650A patent/MXPA05010650A/es not_active Application Discontinuation
- 2004-03-10 CA CA002521227A patent/CA2521227A1/en not_active Abandoned
- 2004-03-10 US US10/552,064 patent/US7842695B2/en not_active Expired - Fee Related
- 2004-03-10 ES ES04718926T patent/ES2287710T3/es not_active Expired - Lifetime
- 2004-03-10 AT AT04718926T patent/ATE364601T1/de not_active IP Right Cessation
- 2004-03-10 PL PL377604A patent/PL377604A1/pl unknown
- 2004-03-10 JP JP2006504620A patent/JP4740117B2/ja not_active Expired - Fee Related
- 2004-03-10 BR BRPI0408986-3A patent/BRPI0408986A/pt not_active Application Discontinuation
- 2004-03-10 CN CNA2004800086030A patent/CN1768052A/zh active Pending
- 2004-03-10 EP EP04718926A patent/EP1611122B1/de not_active Expired - Lifetime
- 2004-03-10 WO PCT/EP2004/002453 patent/WO2004089932A1/de not_active Ceased
- 2004-04-02 AR ARP040101117A patent/AR043835A1/es unknown
-
2005
- 2005-11-03 ZA ZA200508923A patent/ZA200508923B/xx unknown
-
2011
- 2011-02-28 JP JP2011041150A patent/JP2011153144A/ja active Pending
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