JP2013504613A5 - - Google Patents
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- JP2013504613A5 JP2013504613A5 JP2012529335A JP2012529335A JP2013504613A5 JP 2013504613 A5 JP2013504613 A5 JP 2013504613A5 JP 2012529335 A JP2012529335 A JP 2012529335A JP 2012529335 A JP2012529335 A JP 2012529335A JP 2013504613 A5 JP2013504613 A5 JP 2013504613A5
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- Japan
- Prior art keywords
- independently
- disease
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- dementia
- compound according
- Prior art date
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- 150000001875 compounds Chemical class 0.000 claims 25
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 12
- 208000001072 type 2 diabetes mellitus Diseases 0.000 claims 12
- 208000035475 disorder Diseases 0.000 claims 10
- 206010012289 Dementia Diseases 0.000 claims 8
- 125000001931 aliphatic group Chemical group 0.000 claims 8
- 125000000217 alkyl group Chemical group 0.000 claims 8
- 208000010877 cognitive disease Diseases 0.000 claims 8
- 208000027534 Emotional disease Diseases 0.000 claims 6
- 208000002705 Glucose Intolerance Diseases 0.000 claims 6
- 206010022489 Insulin Resistance Diseases 0.000 claims 6
- 208000010125 myocardial infarction Diseases 0.000 claims 6
- 239000003814 drug Substances 0.000 claims 5
- 208000024827 Alzheimer disease Diseases 0.000 claims 4
- 208000019901 Anxiety disease Diseases 0.000 claims 4
- 208000028698 Cognitive impairment Diseases 0.000 claims 4
- 208000020406 Creutzfeldt Jacob disease Diseases 0.000 claims 4
- 208000003407 Creutzfeldt-Jakob Syndrome Diseases 0.000 claims 4
- 208000010859 Creutzfeldt-Jakob disease Diseases 0.000 claims 4
- 201000011240 Frontotemporal dementia Diseases 0.000 claims 4
- 206010020772 Hypertension Diseases 0.000 claims 4
- 208000001145 Metabolic Syndrome Diseases 0.000 claims 4
- 208000008589 Obesity Diseases 0.000 claims 4
- 201000000690 abdominal obesity-metabolic syndrome Diseases 0.000 claims 4
- 230000036506 anxiety Effects 0.000 claims 4
- 210000004027 cell Anatomy 0.000 claims 4
- 208000027866 inflammatory disease Diseases 0.000 claims 4
- 230000000302 ischemic effect Effects 0.000 claims 4
- 150000002632 lipids Chemical class 0.000 claims 4
- 208000027061 mild cognitive impairment Diseases 0.000 claims 4
- 230000004770 neurodegeneration Effects 0.000 claims 4
- 235000020824 obesity Nutrition 0.000 claims 4
- 201000009104 prediabetes syndrome Diseases 0.000 claims 4
- 102000008645 11-beta-Hydroxysteroid Dehydrogenase Type 1 Human genes 0.000 claims 3
- 108010088011 11-beta-Hydroxysteroid Dehydrogenase Type 1 Proteins 0.000 claims 3
- 241001465754 Metazoa Species 0.000 claims 3
- 206010065040 AIDS dementia complex Diseases 0.000 claims 2
- 208000004611 Abdominal Obesity Diseases 0.000 claims 2
- 208000036487 Arthropathies Diseases 0.000 claims 2
- 201000001320 Atherosclerosis Diseases 0.000 claims 2
- 208000024172 Cardiovascular disease Diseases 0.000 claims 2
- 206010065941 Central obesity Diseases 0.000 claims 2
- 208000006545 Chronic Obstructive Pulmonary Disease Diseases 0.000 claims 2
- 208000014311 Cushing syndrome Diseases 0.000 claims 2
- 206010012218 Delirium Diseases 0.000 claims 2
- 201000010374 Down Syndrome Diseases 0.000 claims 2
- 208000032928 Dyslipidaemia Diseases 0.000 claims 2
- 208000004930 Fatty Liver Diseases 0.000 claims 2
- 208000010412 Glaucoma Diseases 0.000 claims 2
- 206010018429 Glucose tolerance impaired Diseases 0.000 claims 2
- 208000023105 Huntington disease Diseases 0.000 claims 2
- 208000035150 Hypercholesterolemia Diseases 0.000 claims 2
- 208000031226 Hyperlipidaemia Diseases 0.000 claims 2
- 208000022559 Inflammatory bowel disease Diseases 0.000 claims 2
- 208000031773 Insulin resistance syndrome Diseases 0.000 claims 2
- 208000012659 Joint disease Diseases 0.000 claims 2
- 208000006264 Korsakoff syndrome Diseases 0.000 claims 2
- 206010049694 Left Ventricular Dysfunction Diseases 0.000 claims 2
- 208000009829 Lewy Body Disease Diseases 0.000 claims 2
- 201000002832 Lewy body dementia Diseases 0.000 claims 2
- 208000017170 Lipid metabolism disease Diseases 0.000 claims 2
- 206010049287 Lipodystrophy acquired Diseases 0.000 claims 2
- 208000026072 Motor neurone disease Diseases 0.000 claims 2
- 206010068871 Myotonic dystrophy Diseases 0.000 claims 2
- 208000010577 Niemann-Pick disease type C Diseases 0.000 claims 2
- 208000001132 Osteoporosis Diseases 0.000 claims 2
- 206010033307 Overweight Diseases 0.000 claims 2
- 208000016222 Pancreatic disease Diseases 0.000 claims 2
- 208000018737 Parkinson disease Diseases 0.000 claims 2
- 208000018262 Peripheral vascular disease Diseases 0.000 claims 2
- 206010034912 Phobia Diseases 0.000 claims 2
- 208000000609 Pick Disease of the Brain Diseases 0.000 claims 2
- 208000007048 Polymyalgia Rheumatica Diseases 0.000 claims 2
- 201000009916 Postpartum depression Diseases 0.000 claims 2
- 208000017442 Retinal disease Diseases 0.000 claims 2
- 206010038923 Retinopathy Diseases 0.000 claims 2
- 208000006011 Stroke Diseases 0.000 claims 2
- 206010044688 Trisomy 21 Diseases 0.000 claims 2
- 208000007930 Type C Niemann-Pick Disease Diseases 0.000 claims 2
- 201000004810 Vascular dementia Diseases 0.000 claims 2
- 206010063661 Vascular encephalopathy Diseases 0.000 claims 2
- 230000001154 acute effect Effects 0.000 claims 2
- 230000002411 adverse Effects 0.000 claims 2
- 230000032683 aging Effects 0.000 claims 2
- 206010003246 arthritis Diseases 0.000 claims 2
- 208000006673 asthma Diseases 0.000 claims 2
- 208000025748 atypical depressive disease Diseases 0.000 claims 2
- 208000015114 central nervous system disease Diseases 0.000 claims 2
- 206010008118 cerebral infarction Diseases 0.000 claims 2
- 230000003001 depressive effect Effects 0.000 claims 2
- 206010012601 diabetes mellitus Diseases 0.000 claims 2
- 201000010099 disease Diseases 0.000 claims 2
- 229940079593 drug Drugs 0.000 claims 2
- 208000024732 dysthymic disease Diseases 0.000 claims 2
- 230000002526 effect on cardiovascular system Effects 0.000 claims 2
- 230000000694 effects Effects 0.000 claims 2
- 208000010706 fatty liver disease Diseases 0.000 claims 2
- 210000001035 gastrointestinal tract Anatomy 0.000 claims 2
- 239000003862 glucocorticoid Substances 0.000 claims 2
- 208000019622 heart disease Diseases 0.000 claims 2
- 201000001421 hyperglycemia Diseases 0.000 claims 2
- 208000006575 hypertriglyceridemia Diseases 0.000 claims 2
- 230000005764 inhibitory process Effects 0.000 claims 2
- 208000006132 lipodystrophy Diseases 0.000 claims 2
- 208000005264 motor neuron disease Diseases 0.000 claims 2
- 201000006417 multiple sclerosis Diseases 0.000 claims 2
- 208000015122 neurodegenerative disease Diseases 0.000 claims 2
- 201000001119 neuropathy Diseases 0.000 claims 2
- 230000007823 neuropathy Effects 0.000 claims 2
- 208000008338 non-alcoholic fatty liver disease Diseases 0.000 claims 2
- 201000003077 normal pressure hydrocephalus Diseases 0.000 claims 2
- 208000033808 peripheral neuropathy Diseases 0.000 claims 2
- 208000019899 phobic disease Diseases 0.000 claims 2
- 201000010065 polycystic ovary syndrome Diseases 0.000 claims 2
- 201000009395 primary hyperaldosteronism Diseases 0.000 claims 2
- 201000002212 progressive supranuclear palsy Diseases 0.000 claims 2
- 208000020016 psychiatric disease Diseases 0.000 claims 2
- 208000037803 restenosis Diseases 0.000 claims 2
- 206010039073 rheumatoid arthritis Diseases 0.000 claims 2
- 150000003839 salts Chemical class 0.000 claims 2
- 201000000980 schizophrenia Diseases 0.000 claims 2
- 208000017520 skin disease Diseases 0.000 claims 2
- 239000012453 solvate Substances 0.000 claims 2
- 231100000240 steatosis hepatitis Toxicity 0.000 claims 2
- 230000035882 stress Effects 0.000 claims 2
- 125000001424 substituent group Chemical group 0.000 claims 2
- 229940037128 systemic glucocorticoids Drugs 0.000 claims 2
- 238000002560 therapeutic procedure Methods 0.000 claims 2
- 230000002792 vascular Effects 0.000 claims 2
- 230000003820 β-cell dysfunction Effects 0.000 claims 2
- 239000003937 drug carrier Substances 0.000 claims 1
- 150000004677 hydrates Chemical class 0.000 claims 1
- 238000000338 in vitro Methods 0.000 claims 1
- 230000002401 inhibitory effect Effects 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 238000000034 method Methods 0.000 claims 1
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 230000002265 prevention Effects 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US24282509P | 2009-09-16 | 2009-09-16 | |
| US61/242,825 | 2009-09-16 | ||
| PCT/GB2010/001732 WO2011033255A1 (en) | 2009-09-16 | 2010-09-14 | (4-phenyl-piperidin-1-yl)-[5-1h-pyrazol-4yl)-thiophen-3-yl]-methanone compounds and their use |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2013504613A JP2013504613A (ja) | 2013-02-07 |
| JP2013504613A5 true JP2013504613A5 (https=) | 2013-09-26 |
| JP5779181B2 JP5779181B2 (ja) | 2015-09-16 |
Family
ID=42946621
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2012529335A Expired - Fee Related JP5779181B2 (ja) | 2009-09-16 | 2010-09-14 | （４−フェニル−ピペリジン−１−イル）−［５−（１ｈ−ピラゾール−４−イル）−チオフェン−３−イル］−メタノン化合物及びそれらの使用 |
Country Status (11)
| Country | Link |
|---|---|
| US (1) | US8642621B2 (https=) |
| EP (1) | EP2477983B1 (https=) |
| JP (1) | JP5779181B2 (https=) |
| KR (1) | KR101702159B1 (https=) |
| AU (1) | AU2010297068B2 (https=) |
| CA (1) | CA2772504C (https=) |
| DK (1) | DK2477983T3 (https=) |
| ES (1) | ES2540547T3 (https=) |
| IL (1) | IL218315A (https=) |
| IN (1) | IN2012DN02590A (https=) |
| WO (1) | WO2011033255A1 (https=) |
Families Citing this family (17)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB0724251D0 (en) | 2007-12-12 | 2008-02-06 | Univ Edinburgh | Therapeutic compounds and their use |
| GB0804685D0 (en) | 2008-03-13 | 2008-04-16 | Univ Edinburgh | Therapeutic compounds and their use |
| EP2477983B1 (en) | 2009-09-16 | 2015-04-15 | The University Of Edinburgh | (4-phenyl-piperidin-1-yl)-[5-1h-pyrazol-4yl)-thiophen-3-yl]-methanone compounds and their use |
| WO2011135276A1 (en) * | 2010-04-29 | 2011-11-03 | The University Of Edinburgh | 3, 3 -disubstituted- ( 8 - aza - bicyclo [3.2.1] oct- 8 - yl) -[5- (1h - pyrazol - 4 -yl) -thiophen-3 -yl] methanones as inhibitors of 11 (beta) -hsd1 |
| WO2014125233A2 (fr) * | 2013-02-14 | 2014-08-21 | Galderma Research & Development | Procédé de synthèse de 4-piperidin-4-yl-benzène-1,3-diol et de ses sels et nouveau composé 4-(2,4-dihydroxy-phényl)-4-hydroxy-piperidine-1-carboxylate de tert-butyle |
| US9637450B2 (en) | 2013-03-14 | 2017-05-02 | The Trustees Of Columbia University In The City Of New York | Octahydrocyclopentapyrroles, their preparation and use |
| US9938291B2 (en) | 2013-03-14 | 2018-04-10 | The Trustess Of Columbia University In The City Of New York | N-alkyl-2-phenoxyethanamines, their preparation and use |
| EP2968304B1 (en) * | 2013-03-14 | 2018-10-10 | The Trustees of Columbia University in the City of New York | 4-phenylpiperidines, their preparation and use |
| US9944644B2 (en) | 2013-03-14 | 2018-04-17 | The Trustees Of Columbia University In The City Of New York | Octahydropyrrolopyrroles their preparation and use |
| EP4036094B1 (en) | 2014-04-30 | 2025-12-24 | The Trustees of Columbia University in the City of New York | Substituted 4-phenylpiperidines, their preparation and use |
| EP3373920A4 (en) | 2015-11-13 | 2019-07-17 | Pietro Paolo Sanna | METHOD AND COMPOSITIONS FOR TREATING ALCOHOL CONSUMPTION MALFUNCTIONS |
| TW202523658A (zh) * | 2019-05-24 | 2025-06-16 | 美商賽吉醫療公司 | 化合物、組合物及使用方法 |
| CN112028739A (zh) * | 2019-06-04 | 2020-12-04 | 湖北大学 | 邻二卤代芳烃化合物功能化的方法 |
| MX2022003845A (es) * | 2019-09-30 | 2022-06-22 | Actinogen Medical Ltd | Tratamientos cognitivos medicinales. |
| WO2022094668A1 (en) * | 2020-11-06 | 2022-05-12 | Actinogen Medical Limited | Process for preparing heterocyclic methanone compounds and aza-bicyclo intermediates thereof |
| JP2023550654A (ja) * | 2020-11-25 | 2023-12-04 | セージ セラピューティクス， インコーポレイテッド | 神経変性障害の治療のためのｃｙｐ４６ａ１阻害剤としての４－フルオロ－（４－（４－ベンジル）ピペリジン－１－イル）（２－（ピリミジン－４－イル）ピリジン－３－イル）メタノン誘導体および類似化合物 |
| JPWO2024172156A1 (https=) * | 2023-02-16 | 2024-08-22 |
Family Cites Families (23)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5087631A (en) | 1990-12-18 | 1992-02-11 | Glaxo Inc. | Oxathi(SIV)azol-5-one compounds |
| AR011913A1 (es) | 1997-03-06 | 2000-09-13 | Yamano Masaki | Derivados de 4,4-difluoro-2,3,4,5-tetrahidro-1h-1-benzoazepina y composiciones farmaceuticas de los mismos. |
| US6303593B1 (en) | 1999-03-02 | 2001-10-16 | Merck & Co., Inc. | 3-thienyl and 3-furanyl pyrrolidine modulators of chemokine receptor activity |
| AU2002353716A1 (en) | 2001-11-22 | 2003-06-10 | Biovitrum Ab | Inhibitors of 11-beta-hydroxy steroid dehydrogenase type 1 |
| SE0202430D0 (sv) | 2002-08-14 | 2002-08-14 | Astrazeneca Ab | New Compounds |
| ATE467616T1 (de) * | 2003-04-11 | 2010-05-15 | High Point Pharmaceuticals Llc | Verbindungen mit aktivität an der 11beta- hydroxasteroiddehydrogenase |
| US7700583B2 (en) | 2003-04-11 | 2010-04-20 | High Point Pharmaceuticals, Llc | 11β-hydroxysteroid dehydrogenase type 1 active compounds |
| GB0325745D0 (en) | 2003-11-05 | 2003-12-10 | Astrazeneca Ab | Chemical compounds |
| GB0326029D0 (en) | 2003-11-07 | 2003-12-10 | Astrazeneca Ab | Chemical compounds |
| RU2006146608A (ru) | 2004-06-09 | 2008-07-20 | Ф.Хоффманн-Ля Рош Аг (Ch) | ОКТАГИДРОПИРРОЛО[3,4-с]-ПРОИЗВОДНЫЕ И ИХ ПРИМЕНЕНИЕ В КАЧЕСТВЕ ПРОТИВОВИРУСНЫХ АГЕНТОВ |
| EP1894919B1 (en) | 2005-06-07 | 2012-03-28 | Shionogi & Co., Ltd. | Heterocyclic compound having type i 11 beta hydroxysteroid dehydrogenase inhibitory activity |
| US7803806B2 (en) | 2005-11-03 | 2010-09-28 | Sgx Pharmaceuticals, Inc. | Pyrimidinyl-thiophene kinase modulators |
| BRPI0710479A2 (pt) | 2006-01-18 | 2012-08-14 | Hoffmann La Roche | composto, processo para sua preparaÇço, composiÇço farmacÊutica, uso de um composto e mÉtodo de tratamento de doenÇa ou desosrdem metabàlica. |
| CN101484424B (zh) * | 2006-02-28 | 2014-05-14 | 达特神经科学(开曼)有限公司 | 治疗化合物 |
| UA95480C2 (uk) | 2006-06-08 | 2011-08-10 | Елі Ліллі Енд Компані | Заміщені карбоксаміди |
| US7666888B2 (en) | 2006-07-20 | 2010-02-23 | Amgen Inc. | Substituted azole aromatic heterocycles as inhibitors of 11β-HSD-1 |
| GB0724251D0 (en) | 2007-12-12 | 2008-02-06 | Univ Edinburgh | Therapeutic compounds and their use |
| US20100022590A1 (en) | 2008-01-17 | 2010-01-28 | Biovitrum Ab (Publ.) | Novel compounds |
| GB0804685D0 (en) | 2008-03-13 | 2008-04-16 | Univ Edinburgh | Therapeutic compounds and their use |
| CA2735204C (en) * | 2008-08-25 | 2017-06-20 | Boehringer Ingelheim International Gmbh | Aryl- and heteroarylcarbonyl derivatives of substituted nortropanes, medicaments containing such compounds and their use |
| EP2443113A1 (en) | 2009-06-15 | 2012-04-25 | The University Of Edinburgh | Amido-isothiazole compounds and their use as inhibitors of 11beta-hsd1 for the treatment of metabolic syndrome and related disorders |
| EP2477983B1 (en) | 2009-09-16 | 2015-04-15 | The University Of Edinburgh | (4-phenyl-piperidin-1-yl)-[5-1h-pyrazol-4yl)-thiophen-3-yl]-methanone compounds and their use |
| WO2011135276A1 (en) | 2010-04-29 | 2011-11-03 | The University Of Edinburgh | 3, 3 -disubstituted- ( 8 - aza - bicyclo [3.2.1] oct- 8 - yl) -[5- (1h - pyrazol - 4 -yl) -thiophen-3 -yl] methanones as inhibitors of 11 (beta) -hsd1 |
-
2010
- 2010-09-14 EP EP10755215.0A patent/EP2477983B1/en active Active
- 2010-09-14 DK DK10755215.0T patent/DK2477983T3/en active
- 2010-09-14 AU AU2010297068A patent/AU2010297068B2/en not_active Ceased
- 2010-09-14 JP JP2012529335A patent/JP5779181B2/ja not_active Expired - Fee Related
- 2010-09-14 US US13/395,963 patent/US8642621B2/en not_active Expired - Fee Related
- 2010-09-14 ES ES10755215.0T patent/ES2540547T3/es active Active
- 2010-09-14 KR KR1020127006255A patent/KR101702159B1/ko not_active Expired - Fee Related
- 2010-09-14 WO PCT/GB2010/001732 patent/WO2011033255A1/en not_active Ceased
- 2010-09-14 IN IN2590DEN2012 patent/IN2012DN02590A/en unknown
- 2010-09-14 CA CA2772504A patent/CA2772504C/en not_active Expired - Fee Related
-
2012
- 2012-02-26 IL IL218315A patent/IL218315A/en active IP Right Grant
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