JP2010524953A5 - - Google Patents
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- Publication number
- JP2010524953A5 JP2010524953A5 JP2010504198A JP2010504198A JP2010524953A5 JP 2010524953 A5 JP2010524953 A5 JP 2010524953A5 JP 2010504198 A JP2010504198 A JP 2010504198A JP 2010504198 A JP2010504198 A JP 2010504198A JP 2010524953 A5 JP2010524953 A5 JP 2010524953A5
- Authority
- JP
- Japan
- Prior art keywords
- aryl
- cycloalkyl
- alkyl
- heteroaryl
- heterocyclyl
- 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.)
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- 125000000753 cycloalkyl group Chemical group 0.000 claims 140
- 125000000217 alkyl group Chemical group 0.000 claims 137
- 125000003118 aryl group Chemical group 0.000 claims 137
- 125000001072 heteroaryl group Chemical group 0.000 claims 121
- 229910005965 SO 2 Inorganic materials 0.000 claims 83
- 125000000623 heterocyclic group Chemical group 0.000 claims 82
- 125000003831 tetrazolyl group Chemical group 0.000 claims 69
- 125000003545 alkoxy group Chemical group 0.000 claims 66
- -1 SOCR 2 R 2a Inorganic materials 0.000 claims 64
- 125000001188 haloalkyl group Chemical group 0.000 claims 50
- 125000004414 alkyl thio group Chemical group 0.000 claims 48
- 125000004104 aryloxy group Chemical group 0.000 claims 48
- 229910052736 halogen Inorganic materials 0.000 claims 39
- 150000002367 halogens Chemical class 0.000 claims 39
- 125000003342 alkenyl group Chemical group 0.000 claims 36
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 34
- 229910052739 hydrogen Inorganic materials 0.000 claims 32
- 239000001257 hydrogen Substances 0.000 claims 32
- 125000004435 hydrogen atom Chemical class [H]* 0.000 claims 32
- 125000005236 alkanoylamino group Chemical group 0.000 claims 27
- 125000003710 aryl alkyl group Chemical group 0.000 claims 27
- 125000004659 aryl alkyl thio group Chemical group 0.000 claims 27
- 125000002102 aryl alkyloxo group Chemical group 0.000 claims 27
- 125000005418 aryl aryl group Chemical group 0.000 claims 27
- 125000004658 aryl carbonyl amino group Chemical group 0.000 claims 27
- 125000005160 aryl oxy alkyl group Chemical group 0.000 claims 27
- 125000005325 aryloxy aryl group Chemical group 0.000 claims 27
- 125000001316 cycloalkyl alkyl group Chemical group 0.000 claims 27
- 125000005112 cycloalkylalkoxy group Chemical group 0.000 claims 27
- 125000005114 heteroarylalkoxy group Chemical group 0.000 claims 27
- 125000004446 heteroarylalkyl group Chemical group 0.000 claims 27
- 125000005553 heteroaryloxy group Chemical group 0.000 claims 27
- UUEVFMOUBSLVJW-UHFFFAOYSA-N oxo-[[1-[2-[2-[2-[4-(oxoazaniumylmethylidene)pyridin-1-yl]ethoxy]ethoxy]ethyl]pyridin-4-ylidene]methyl]azanium;dibromide Chemical compound [Br-].[Br-].C1=CC(=C[NH+]=O)C=CN1CCOCCOCCN1C=CC(=C[NH+]=O)C=C1 UUEVFMOUBSLVJW-UHFFFAOYSA-N 0.000 claims 23
- 125000003282 alkyl amino group Chemical group 0.000 claims 21
- 125000001769 aryl amino group Chemical group 0.000 claims 21
- 125000004391 aryl sulfonyl group Chemical group 0.000 claims 21
- 125000005110 aryl thio group Chemical group 0.000 claims 21
- 125000004438 haloalkoxy group Chemical group 0.000 claims 21
- 125000005241 heteroarylamino group Chemical group 0.000 claims 21
- 125000002252 acyl group Chemical group 0.000 claims 18
- 125000005843 halogen group Chemical group 0.000 claims 18
- 125000002768 hydroxyalkyl group Chemical group 0.000 claims 18
- 125000003396 thiol group Chemical class [H]S* 0.000 claims 18
- 150000001875 compounds Chemical class 0.000 claims 15
- 125000004103 aminoalkyl group Chemical group 0.000 claims 14
- 239000003814 drug Substances 0.000 claims 14
- 125000001424 substituent group Chemical group 0.000 claims 13
- 229910052717 sulfur Inorganic materials 0.000 claims 13
- 229910052760 oxygen Inorganic materials 0.000 claims 11
- 125000002619 bicyclic group Chemical group 0.000 claims 9
- 239000003795 chemical substances by application Substances 0.000 claims 9
- 229940079593 drug Drugs 0.000 claims 9
- 150000003839 salts Chemical class 0.000 claims 5
- 125000005842 heteroatom Chemical group 0.000 claims 4
- 229940124597 therapeutic agent Drugs 0.000 claims 4
- 208000028698 Cognitive impairment Diseases 0.000 claims 3
- 208000032928 Dyslipidaemia Diseases 0.000 claims 3
- 208000010412 Glaucoma Diseases 0.000 claims 3
- 206010020772 Hypertension Diseases 0.000 claims 3
- 208000017170 Lipid metabolism disease Diseases 0.000 claims 3
- 208000001145 Metabolic Syndrome Diseases 0.000 claims 3
- 208000008589 Obesity Diseases 0.000 claims 3
- 201000000690 abdominal obesity-metabolic syndrome Diseases 0.000 claims 3
- 230000001708 anti-dyslipidemic effect Effects 0.000 claims 3
- 239000003472 antidiabetic agent Substances 0.000 claims 3
- 208000010877 cognitive disease Diseases 0.000 claims 3
- 235000020824 obesity Nutrition 0.000 claims 3
- 102000004277 11-beta-hydroxysteroid dehydrogenases Human genes 0.000 claims 2
- 108090000874 11-beta-hydroxysteroid dehydrogenases Proteins 0.000 claims 2
- 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 2
- 206010033645 Pancreatitis Diseases 0.000 claims 2
- 230000000879 anti-atherosclerotic effect Effects 0.000 claims 2
- 230000001315 anti-hyperlipaemic effect Effects 0.000 claims 2
- 230000003276 anti-hypertensive effect Effects 0.000 claims 2
- 239000002260 anti-inflammatory agent Substances 0.000 claims 2
- 230000002253 anti-ischaemic effect Effects 0.000 claims 2
- 230000003063 anti-neuropathic effect Effects 0.000 claims 2
- 230000003579 anti-obesity Effects 0.000 claims 2
- 239000003524 antilipemic agent Substances 0.000 claims 2
- 239000002830 appetite depressant Substances 0.000 claims 2
- 125000004429 atom Chemical group 0.000 claims 2
- 239000002475 cognitive enhancer Substances 0.000 claims 2
- 206010012601 diabetes mellitus Diseases 0.000 claims 2
- 201000001421 hyperglycemia Diseases 0.000 claims 2
- 239000003112 inhibitor Substances 0.000 claims 2
- 239000003695 memory enhancer Substances 0.000 claims 2
- 239000008194 pharmaceutical composition Substances 0.000 claims 2
- 230000002265 prevention Effects 0.000 claims 2
- 125000006272 (C3-C7) cycloalkyl group Chemical group 0.000 claims 1
- 206010060378 Hyperinsulinaemia Diseases 0.000 claims 1
- 208000017442 Retinal disease Diseases 0.000 claims 1
- 206010038923 Retinopathy Diseases 0.000 claims 1
- 229940127003 anti-diabetic drug Drugs 0.000 claims 1
- 230000000326 anti-hypercholesterolaemic effect Effects 0.000 claims 1
- 230000002058 anti-hyperglycaemic effect Effects 0.000 claims 1
- 229940121363 anti-inflammatory agent Drugs 0.000 claims 1
- 229940124599 anti-inflammatory drug Drugs 0.000 claims 1
- 229940125708 antidiabetic agent Drugs 0.000 claims 1
- 239000008280 blood Substances 0.000 claims 1
- 210000004369 blood Anatomy 0.000 claims 1
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 201000008980 hyperinsulinism Diseases 0.000 claims 1
- 208000017169 kidney disease Diseases 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 239000000203 mixture Substances 0.000 claims 1
- 229910052757 nitrogen Inorganic materials 0.000 claims 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 1
- 208000037803 restenosis Diseases 0.000 claims 1
- 230000002966 stenotic effect Effects 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US91218607P | 2007-04-17 | 2007-04-17 | |
| US4495108P | 2008-04-15 | 2008-04-15 | |
| PCT/US2008/060395 WO2008130951A1 (en) | 2007-04-17 | 2008-04-16 | Fused heterocyclic 11-beta-hydroxysteroid dehydrogenase type i inhibitors |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2010524953A JP2010524953A (ja) | 2010-07-22 |
| JP2010524953A5 true JP2010524953A5 (enExample) | 2011-05-19 |
Family
ID=39580690
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2010504198A Withdrawn JP2010524953A (ja) | 2007-04-17 | 2008-04-16 | 縮合ヘテロ環１１−β−ヒドロキシステロイドデヒドロゲナーゼＩ型阻害剤 |
Country Status (5)
| Country | Link |
|---|---|
| US (1) | US8546394B2 (enExample) |
| EP (2) | EP2474549A1 (enExample) |
| JP (1) | JP2010524953A (enExample) |
| CN (1) | CN101687873A (enExample) |
| WO (1) | WO2008130951A1 (enExample) |
Families Citing this family (42)
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| ES2668775T3 (es) | 2009-06-10 | 2018-05-22 | Chugai Seiyaku Kabushiki Kaisha | Compuestos tetracíclicos |
| TW201107329A (en) * | 2009-07-30 | 2011-03-01 | Oncotherapy Science Inc | Fused imidazole derivative having ttk inhibitory action |
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| PH12012501361A1 (en) | 2009-12-31 | 2012-10-22 | Centro Nac De Investigaciones Oncologicas Cnio | Tricyclic compounds for use as kinase inhibitors |
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| US8530413B2 (en) | 2010-06-21 | 2013-09-10 | Sanofi | Heterocyclically substituted methoxyphenyl derivatives with an oxo group, processes for preparation thereof and use thereof as medicaments |
| TW201215388A (en) | 2010-07-05 | 2012-04-16 | Sanofi Sa | (2-aryloxyacetylamino)phenylpropionic acid derivatives, processes for preparation thereof and use thereof as medicaments |
| TW201221505A (en) | 2010-07-05 | 2012-06-01 | Sanofi Sa | Aryloxyalkylene-substituted hydroxyphenylhexynoic acids, process for preparation thereof and use thereof as a medicament |
| TW201215387A (en) | 2010-07-05 | 2012-04-16 | Sanofi Aventis | Spirocyclically substituted 1,3-propane dioxide derivatives, processes for preparation thereof and use thereof as a medicament |
| MX355836B (es) | 2010-08-20 | 2018-05-02 | Chugai Pharmaceutical Co Ltd | Composicion que comprende compuestos tetraciclicos. |
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| WO2013045413A1 (en) | 2011-09-27 | 2013-04-04 | Sanofi | 6-(4-hydroxy-phenyl)-3-alkyl-1h-pyrazolo[3,4-b]pyridine-4-carboxylic acid amide derivatives as kinase inhibitors |
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| US9422290B2 (en) | 2012-11-13 | 2016-08-23 | Boehringer Ingelheim International Gmbh | Triazolopyridazine |
| US9266891B2 (en) | 2012-11-16 | 2016-02-23 | Boehringer Ingelheim International Gmbh | Substituted [1,2,4]triazolo[4,3-A]pyrazines that are BRD4 inhibitors |
| JP6522502B2 (ja) | 2013-07-29 | 2019-05-29 | 協和発酵キリン株式会社 | Ｗｎｔシグナル阻害剤 |
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| NZ723203A (en) | 2014-02-13 | 2020-08-28 | Incyte Corp | Cyclopropylamines as lsd1 inhibitors |
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| US9527835B2 (en) | 2014-02-13 | 2016-12-27 | Incyte Corporation | Cyclopropylamines as LSD1 inhibitors |
| KR102421235B1 (ko) | 2014-02-13 | 2022-07-15 | 인사이트 코포레이션 | Lsd1 저해제로서 사이클로프로필아민 |
| EP3135671B1 (en) | 2014-04-25 | 2019-09-18 | Chugai Seiyaku Kabushiki Kaisha | Novel crystal of tetracyclic compound |
| WO2015163448A1 (ja) | 2014-04-25 | 2015-10-29 | 中外製薬株式会社 | ４環性化合物を高用量含有する製剤 |
| WO2015166370A1 (en) | 2014-04-28 | 2015-11-05 | Pfizer Inc. | Heteroaromatic compounds and their use as dopamine d1 ligands |
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| WO2016007731A1 (en) | 2014-07-10 | 2016-01-14 | Incyte Corporation | Imidazopyridines and imidazopyrazines as lsd1 inhibitors |
| US9758523B2 (en) | 2014-07-10 | 2017-09-12 | Incyte Corporation | Triazolopyridines and triazolopyrazines as LSD1 inhibitors |
| US9695180B2 (en) | 2014-07-10 | 2017-07-04 | Incyte Corporation | Substituted imidazo[1,2-a]pyrazines as LSD1 inhibitors |
| US9580420B2 (en) * | 2014-08-06 | 2017-02-28 | Bristol-Meyers Squibb Company | Process for the preparation of 4-(8-(2-chlorophenoxy)-[1,2,4]triazolo[4,3-a]pyridin-3-yl)bicyclo[2.2.1]heptan-1-ol and novel intermediates therefor |
| TWI831347B (zh) | 2014-08-08 | 2024-02-01 | 日商中外製藥股份有限公司 | 包含４環性化合物的非晶質體之固體分散體及製劑 |
| JP6741596B2 (ja) | 2015-01-16 | 2020-08-19 | 中外製薬株式会社 | 併用医薬 |
| UA122688C2 (uk) * | 2015-04-03 | 2020-12-28 | Інсайт Корпорейшн | Гетероциклічні сполуки як інгібітори lsd1 |
| CN107922396B (zh) * | 2015-07-20 | 2022-08-05 | 建新公司 | 集落刺激因子-1受体(csf-1r)抑制剂 |
| JP7427363B2 (ja) | 2015-08-12 | 2024-02-05 | インサイト・ホールディングス・コーポレイション | Ｌｓｄ１阻害剤の塩 |
| US10166221B2 (en) | 2016-04-22 | 2019-01-01 | Incyte Corporation | Formulations of an LSD1 inhibitor |
| CN112384223B (zh) | 2018-06-29 | 2024-08-27 | 中外制药株式会社 | 含有难溶性碱性药剂的药物组合物 |
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| EP4267573A1 (en) | 2020-12-23 | 2023-11-01 | Genzyme Corporation | Deuterated colony stimulating factor-1 receptor (csf-1r) inhibitors |
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| WO2004107863A1 (en) | 2003-05-05 | 2004-12-16 | Neurogen Corporation | Sustituted imidazolopyrazine and triazolopyrazine derivatives: gabaa receptor ligands |
| ES2278345T3 (es) * | 2003-07-25 | 2007-08-01 | Neurogen Corporation | Imidazo-pirimidinas y triazolo-pirimidinas: ligandos de receptores de benzodiazepinas. |
| US7419978B2 (en) * | 2003-10-22 | 2008-09-02 | Bristol-Myers Squibb Company | Phenyl-aniline substituted bicyclic compounds useful as kinase inhibitors |
| WO2005077953A1 (ja) * | 2004-02-18 | 2005-08-25 | Banyu Pharmaceutical Co., Ltd. | 含窒素縮合へテロ芳香環誘導体 |
| CA2576465A1 (en) * | 2004-08-23 | 2006-03-02 | Merck & Co., Inc. | Fused triazole derivatives as dipeptidyl peptidase-iv inhibitors for the treatment or prevention of diabetes |
| US7572807B2 (en) | 2005-06-09 | 2009-08-11 | Bristol-Myers Squibb Company | Heteroaryl 11-beta-hydroxysteroid dehydrogenase type I inhibitors |
| US7629342B2 (en) * | 2005-06-17 | 2009-12-08 | Bristol-Myers Squibb Company | Azabicyclic heterocycles as cannabinoid receptor modulators |
| US7632837B2 (en) | 2005-06-17 | 2009-12-15 | Bristol-Myers Squibb Company | Bicyclic heterocycles as cannabinoid-1 receptor modulators |
| US7855206B2 (en) * | 2006-11-14 | 2010-12-21 | Merck Sharp & Dohme Corp. | Tricyclic heteroaromatic compounds as dipeptidyl peptidase-IV inhibitors for the treatment or prevention of diabetes |
-
2008
- 2008-04-16 WO PCT/US2008/060395 patent/WO2008130951A1/en not_active Ceased
- 2008-04-16 EP EP12163063A patent/EP2474549A1/en not_active Withdrawn
- 2008-04-16 JP JP2010504198A patent/JP2010524953A/ja not_active Withdrawn
- 2008-04-16 CN CN200880020554A patent/CN101687873A/zh active Pending
- 2008-04-16 EP EP08745903.8A patent/EP2142551B1/en not_active Not-in-force
- 2008-04-16 US US12/595,524 patent/US8546394B2/en active Active
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