JP2011526294A5 - - Google Patents
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- Publication number
- JP2011526294A5 JP2011526294A5 JP2011516646A JP2011516646A JP2011526294A5 JP 2011526294 A5 JP2011526294 A5 JP 2011526294A5 JP 2011516646 A JP2011516646 A JP 2011516646A JP 2011516646 A JP2011516646 A JP 2011516646A JP 2011526294 A5 JP2011526294 A5 JP 2011526294A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- cycloalkyl
- group
- alkoxy
- unsubstituted
- 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.)
- Pending
Links
- 150000001875 compounds Chemical class 0.000 claims description 101
- -1 heterocycloalkyloxy Chemical group 0.000 claims description 66
- 125000000217 alkyl group Chemical group 0.000 claims description 43
- 125000003545 alkoxy group Chemical group 0.000 claims description 42
- 229910052736 halogen Inorganic materials 0.000 claims description 38
- 150000002367 halogens Chemical class 0.000 claims description 37
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 36
- 125000004093 cyano group Chemical group *C#N 0.000 claims description 27
- 125000001316 cycloalkyl alkyl group Chemical group 0.000 claims description 24
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims description 24
- 125000003118 aryl group Chemical group 0.000 claims description 23
- 125000001072 heteroaryl group Chemical group 0.000 claims description 23
- 125000004183 alkoxy alkyl group Chemical group 0.000 claims description 20
- 125000000000 cycloalkoxy group Chemical group 0.000 claims description 19
- 125000001424 substituent group Chemical group 0.000 claims description 19
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims description 18
- 125000006413 ring segment Chemical group 0.000 claims description 18
- 125000004390 alkyl sulfonyl group Chemical group 0.000 claims description 14
- 125000005885 heterocycloalkylalkyl group Chemical group 0.000 claims description 14
- 229910052739 hydrogen Inorganic materials 0.000 claims description 14
- 239000008194 pharmaceutical composition Substances 0.000 claims description 14
- 125000003282 alkyl amino group Chemical group 0.000 claims description 12
- 125000005112 cycloalkylalkoxy group Chemical group 0.000 claims description 12
- 125000004663 dialkyl amino group Chemical group 0.000 claims description 12
- 239000001257 hydrogen Substances 0.000 claims description 12
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims description 12
- 125000004435 hydrogen atom Chemical class [H]* 0.000 claims description 10
- 125000004446 heteroarylalkyl group Chemical group 0.000 claims description 9
- 229910052757 nitrogen Inorganic materials 0.000 claims description 9
- 125000004001 thioalkyl group Chemical group 0.000 claims description 9
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims description 8
- 125000003368 amide group Chemical group 0.000 claims description 8
- 229910052799 carbon Inorganic materials 0.000 claims description 8
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims description 8
- 125000002950 monocyclic group Chemical group 0.000 claims description 8
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims description 8
- 150000003839 salts Chemical class 0.000 claims description 8
- 125000003710 aryl alkyl group Chemical group 0.000 claims description 7
- 125000004104 aryloxy group Chemical group 0.000 claims description 7
- 125000004429 atom Chemical group 0.000 claims description 7
- 125000005553 heteroaryloxy group Chemical group 0.000 claims description 7
- 208000008589 Obesity Diseases 0.000 claims description 6
- 125000004414 alkyl thio group Chemical group 0.000 claims description 6
- 125000005842 heteroatom Chemical group 0.000 claims description 6
- 235000020824 obesity Nutrition 0.000 claims description 6
- 229910052760 oxygen Inorganic materials 0.000 claims description 6
- SNOOUWRIMMFWNE-UHFFFAOYSA-M sodium;6-[(3,4,5-trimethoxybenzoyl)amino]hexanoate Chemical compound [Na+].COC1=CC(C(=O)NCCCCCC([O-])=O)=CC(OC)=C1OC SNOOUWRIMMFWNE-UHFFFAOYSA-M 0.000 claims description 6
- 229910052717 sulfur Inorganic materials 0.000 claims description 6
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims description 5
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims description 4
- 125000000229 (C1-C4)alkoxy group Chemical group 0.000 claims description 4
- 208000023105 Huntington disease Diseases 0.000 claims description 4
- 208000001145 Metabolic Syndrome Diseases 0.000 claims description 4
- 201000000690 abdominal obesity-metabolic syndrome Diseases 0.000 claims description 4
- 201000000980 schizophrenia Diseases 0.000 claims description 4
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical compound [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims description 3
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims description 3
- 230000002996 emotional effect Effects 0.000 claims description 3
- 239000001301 oxygen Substances 0.000 claims description 3
- 230000000698 schizophrenic effect Effects 0.000 claims description 3
- 239000011593 sulfur Substances 0.000 claims description 3
- 208000030814 Eating disease Diseases 0.000 claims description 2
- 208000019454 Feeding and Eating disease Diseases 0.000 claims description 2
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 2
- 125000002102 aryl alkyloxo group Chemical group 0.000 claims description 2
- 208000015114 central nervous system disease Diseases 0.000 claims description 2
- 206010012601 diabetes mellitus Diseases 0.000 claims description 2
- 235000014632 disordered eating Nutrition 0.000 claims description 2
- 239000003937 drug carrier Substances 0.000 claims description 2
- 125000005114 heteroarylalkoxy group Chemical group 0.000 claims description 2
- 201000003631 narcolepsy Diseases 0.000 claims description 2
- 150000002828 nitro derivatives Chemical class 0.000 claims description 2
- 239000000546 pharmaceutical excipient Substances 0.000 claims description 2
- 208000012201 sexual and gender identity disease Diseases 0.000 claims description 2
- 208000015891 sexual disease Diseases 0.000 claims description 2
- 208000019116 sleep disease Diseases 0.000 claims description 2
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 6
- CKUAXEQHGKSLHN-UHFFFAOYSA-N [C].[N] Chemical compound [C].[N] CKUAXEQHGKSLHN-UHFFFAOYSA-N 0.000 claims 5
- 125000005083 alkoxyalkoxy group Chemical group 0.000 claims 5
- CREMABGTGYGIQB-UHFFFAOYSA-N carbon carbon Chemical compound C.C CREMABGTGYGIQB-UHFFFAOYSA-N 0.000 claims 5
- 239000011203 carbon fibre reinforced carbon Substances 0.000 claims 5
- 125000001995 cyclobutyl group Chemical group [H]C1([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 5
- CSJDCSCTVDEHRN-UHFFFAOYSA-N methane;molecular oxygen Chemical compound C.O=O CSJDCSCTVDEHRN-UHFFFAOYSA-N 0.000 claims 5
- 125000001153 fluoro group Chemical group F* 0.000 claims 3
- 125000004043 oxo group Chemical group O=* 0.000 claims 3
- 125000001309 chloro group Chemical group Cl* 0.000 claims 2
- 208000014094 Dystonic disease Diseases 0.000 claims 1
- 206010034158 Pathological gambling Diseases 0.000 claims 1
- 206010043118 Tardive Dyskinesia Diseases 0.000 claims 1
- 208000010118 dystonia Diseases 0.000 claims 1
- 125000005843 halogen group Chemical group 0.000 claims 1
- 230000000391 smoking effect Effects 0.000 claims 1
- 0 **c(cc1)ccc1-c1c(*)cccc1 Chemical compound **c(cc1)ccc1-c1c(*)cccc1 0.000 description 23
- 125000005605 benzo group Chemical group 0.000 description 9
- KPCZJLGGXRGYIE-UHFFFAOYSA-N [C]1=CC=CN=C1 Chemical group [C]1=CC=CN=C1 KPCZJLGGXRGYIE-UHFFFAOYSA-N 0.000 description 4
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 description 4
- 125000005346 substituted cycloalkyl group Chemical group 0.000 description 3
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 description 2
- 150000001408 amides Chemical class 0.000 description 2
- 125000005338 substituted cycloalkoxy group Chemical group 0.000 description 2
- XTFIVUDBNACUBN-UHFFFAOYSA-N 1,3,5-trinitro-1,3,5-triazinane Chemical compound [O-][N+](=O)N1CN([N+]([O-])=O)CN([N+]([O-])=O)C1 XTFIVUDBNACUBN-UHFFFAOYSA-N 0.000 description 1
- IWSMBQGLMBANFK-UHFFFAOYSA-N CC(C)(C)N(C(CC1)C2)C1CC2=O Chemical compound CC(C)(C)N(C(CC1)C2)C1CC2=O IWSMBQGLMBANFK-UHFFFAOYSA-N 0.000 description 1
- HWTOGAWRASXJNF-UHFFFAOYSA-N CC(C)N(CC1)CC1=O Chemical compound CC(C)N(CC1)CC1=O HWTOGAWRASXJNF-UHFFFAOYSA-N 0.000 description 1
- HCTBGWWIFCBFGV-UHFFFAOYSA-N CC(C)N(CC1C2)C2CC1=O Chemical compound CC(C)N(CC1C2)C2CC1=O HCTBGWWIFCBFGV-UHFFFAOYSA-N 0.000 description 1
- SIKTVUHUQZNEPY-UHFFFAOYSA-N CN(CCC1)CC1=O Chemical compound CN(CCC1)CC1=O SIKTVUHUQZNEPY-UHFFFAOYSA-N 0.000 description 1
- YTZQMCKKXWLCFC-UHFFFAOYSA-N CN1C2COCC1C2 Chemical compound CN1C2COCC1C2 YTZQMCKKXWLCFC-UHFFFAOYSA-N 0.000 description 1
- 208000012661 Dyskinesia Diseases 0.000 description 1
- 125000003785 benzimidazolyl group Chemical group N1=C(NC2=C1C=CC=C2)* 0.000 description 1
- 125000002183 isoquinolinyl group Chemical group C1(=NC=CC2=CC=CC=C12)* 0.000 description 1
- 125000005647 linker group Chemical group 0.000 description 1
- 230000003274 myotonic effect Effects 0.000 description 1
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 description 1
- 125000004076 pyridyl group Chemical group 0.000 description 1
- 125000002943 quinolinyl group Chemical group N1=C(C=CC2=CC=CC=C12)* 0.000 description 1
- 230000005586 smoking cessation Effects 0.000 description 1
- 125000003107 substituted aryl group Chemical group 0.000 description 1
- 230000001225 therapeutic effect Effects 0.000 description 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US7559908P | 2008-06-25 | 2008-06-25 | |
| US61/075,599 | 2008-06-25 | ||
| US13885608P | 2008-12-18 | 2008-12-18 | |
| US61/138,856 | 2008-12-18 | ||
| PCT/US2009/048608 WO2009158467A2 (en) | 2008-06-25 | 2009-06-25 | Di-substituted phenyl compounds |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2011526294A JP2011526294A (ja) | 2011-10-06 |
| JP2011526294A5 true JP2011526294A5 (https=) | 2012-08-09 |
Family
ID=41137470
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2011516646A Pending JP2011526294A (ja) | 2008-06-25 | 2009-06-25 | ホスホジエステラーゼ１０阻害剤としての二置換フェニル化合物 |
Country Status (11)
| Country | Link |
|---|---|
| US (1) | US20110224204A1 (https=) |
| EP (1) | EP2297131A2 (https=) |
| JP (1) | JP2011526294A (https=) |
| KR (1) | KR20110025984A (https=) |
| CN (1) | CN102131798A (https=) |
| AU (1) | AU2009262150A1 (https=) |
| BR (1) | BRPI0914775A2 (https=) |
| CA (1) | CA2729220A1 (https=) |
| MX (1) | MX2011000177A (https=) |
| RU (1) | RU2011102587A (https=) |
| WO (1) | WO2009158467A2 (https=) |
Families Citing this family (23)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU2010311493B2 (en) * | 2009-10-30 | 2014-06-05 | Janssen Pharmaceutica Nv | Radiolabelled PDE10 ligands |
| EP2423181A1 (en) | 2010-07-28 | 2012-02-29 | Prous Institute For Biomedical Research S.A. | Multitarget substituted biphenyl diol derivatives |
| US8765760B2 (en) | 2011-01-11 | 2014-07-01 | Sunovion Pharmaceuticals, Inc. | [1,2,4] triazol [1,5-a] pyrazines useful as inhibitors of phosphodiesterases |
| CA2827724A1 (en) | 2011-02-18 | 2012-08-23 | Allergan, Inc. | Substituted 6,7-dialkoxy-3-isoquinolinol derivatives as inhibitors of phosphodiesterase 10 (pde10a) |
| US20120309796A1 (en) | 2011-06-06 | 2012-12-06 | Fariborz Firooznia | Benzocycloheptene acetic acids |
| GB201113538D0 (en) * | 2011-08-04 | 2011-09-21 | Karobio Ab | Novel estrogen receptor ligands |
| WO2014007228A1 (ja) * | 2012-07-03 | 2014-01-09 | 小野薬品工業株式会社 | ソマトスタチン受容体作動活性を有する化合物およびその医薬用途 |
| AU2013289284B2 (en) * | 2012-07-09 | 2017-03-30 | Janssen Pharmaceutica Nv | Inhibitors of phosphodiesterase 10 enzyme |
| WO2014071044A1 (en) | 2012-11-01 | 2014-05-08 | Allergan, Inc. | Substituted 6,7-dialkoxy-3-isoquinoline derivatives as inhibitors of phosphodiesterase 10 (pde10a) |
| US9198898B2 (en) | 2013-06-24 | 2015-12-01 | Tigercat Pharma, Inc. | Use of NK-1 receptor antagonists in pruritus |
| US8906951B1 (en) | 2013-06-24 | 2014-12-09 | Tigercat Pharma, Inc. | Use of NK-1 receptor antagonists in pruritus |
| EP2860177A3 (en) * | 2013-09-20 | 2015-06-10 | Bayer Intellectual Property GmbH | Synthesis of functionalized arenes |
| US9200016B2 (en) | 2013-12-05 | 2015-12-01 | Allergan, Inc. | Substituted 6, 7-dialkoxy-3-isoquinoline derivatives as inhibitors of phosphodiesterase 10 (PDE 10A) |
| EP3596062A4 (en) | 2017-03-16 | 2020-08-26 | Crinetics Pharmaceuticals, Inc. | SOMATOSTATIN MODULATORS AND THEIR USES |
| MA51840A (fr) | 2018-02-12 | 2021-05-19 | Crinetics Pharmaceuticals Inc | Modulateurs de somatostatine et leurs utilisations |
| BR112020018094A2 (pt) | 2018-03-08 | 2020-12-22 | Incyte Corporation | Compostos de aminopirazina diol como inibidores de pi3k-¿ |
| US11046658B2 (en) | 2018-07-02 | 2021-06-29 | Incyte Corporation | Aminopyrazine derivatives as PI3K-γ inhibitors |
| SMT202500155T1 (it) | 2018-09-18 | 2025-05-12 | Crinetics Pharmaceuticals Inc | Modulatori della somatostatina e loro usi |
| TWI841768B (zh) | 2019-08-14 | 2024-05-11 | 美商克林提克斯醫藥股份有限公司 | 非肽生長抑制素(somatostatin)5型受體激動劑及其用途 |
| KR102811543B1 (ko) | 2019-10-16 | 2025-05-23 | 삼성디스플레이 주식회사 | 유기 전계 발광 소자 및 유기 전계 발광 소자용 다환 화합물 |
| BR112023002159A2 (pt) * | 2020-08-04 | 2023-04-25 | Prec Bio Therapeutics S R L | Composto, uso do composto e composição famacêutica |
| JP2024506715A (ja) | 2021-02-17 | 2024-02-14 | クリネティックス ファーマシューティカルズ，インク． | ソマトスタチンモジュレーターの結晶形態 |
| TW202440164A (zh) | 2022-12-13 | 2024-10-16 | 美商克林提克斯醫藥股份有限公司 | 生長抑素亞型-2受體（sst2r）靶向治療劑及其用途 |
Family Cites Families (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB2244054B (en) * | 1990-04-19 | 1994-04-06 | Ici Plc | Pyridine derivatives |
| CA2051705A1 (en) * | 1990-06-19 | 1991-12-20 | Kiyoaki Katano | Pyridine derivatives having angiotensin ii antagonism |
| GB2264710A (en) * | 1992-03-04 | 1993-09-08 | Merck & Co Inc | Quinoline and azaquinoline angiotensin ii antagonists incorporating a substituted biphenyl element |
| WO2004002484A1 (ja) * | 2002-06-26 | 2004-01-08 | Kyowa Hakko Kogyo Co., Ltd. | ホスホジエステラーゼ阻害剤 |
| US7524870B2 (en) * | 2004-12-03 | 2009-04-28 | Hoffmann-La Roche Inc. | Biaryloxymethylarenecarboxylic acids as glycogen synthase activators |
| US20090176829A1 (en) * | 2006-05-02 | 2009-07-09 | Pfizer Inc | Bicyclic heteroaryl compounds as pde10 inhibitors |
| WO2008033455A2 (en) * | 2006-09-13 | 2008-03-20 | The Institutes For Pharmaceutical Discovery, Llc | Biphenyl and heteroaryl phenyl derivatives as protein tyrosine phosphatases inhibitors |
-
2009
- 2009-06-25 JP JP2011516646A patent/JP2011526294A/ja active Pending
- 2009-06-25 CA CA2729220A patent/CA2729220A1/en not_active Abandoned
- 2009-06-25 US US13/001,361 patent/US20110224204A1/en not_active Abandoned
- 2009-06-25 EP EP09770999A patent/EP2297131A2/en not_active Withdrawn
- 2009-06-25 MX MX2011000177A patent/MX2011000177A/es not_active Application Discontinuation
- 2009-06-25 RU RU2011102587/04A patent/RU2011102587A/ru not_active Application Discontinuation
- 2009-06-25 CN CN2009801332872A patent/CN102131798A/zh active Pending
- 2009-06-25 WO PCT/US2009/048608 patent/WO2009158467A2/en not_active Ceased
- 2009-06-25 KR KR1020117001927A patent/KR20110025984A/ko not_active Ceased
- 2009-06-25 BR BRPI0914775A patent/BRPI0914775A2/pt not_active IP Right Cessation
- 2009-06-25 AU AU2009262150A patent/AU2009262150A1/en not_active Abandoned
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