JP2013527847A5 - - Google Patents
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- Publication number
- JP2013527847A5 JP2013527847A5 JP2013508120A JP2013508120A JP2013527847A5 JP 2013527847 A5 JP2013527847 A5 JP 2013527847A5 JP 2013508120 A JP2013508120 A JP 2013508120A JP 2013508120 A JP2013508120 A JP 2013508120A JP 2013527847 A5 JP2013527847 A5 JP 2013527847A5
- Authority
- JP
- Japan
- Prior art keywords
- ring
- independently
- membered heterocyclic
- atom
- halogen
- 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
- 229910052760 oxygen Inorganic materials 0.000 claims 28
- 125000005842 heteroatom Chemical group 0.000 claims 27
- 229910052717 sulfur Inorganic materials 0.000 claims 27
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 22
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 22
- 229910052736 halogen Inorganic materials 0.000 claims 21
- 150000002367 halogens Chemical class 0.000 claims 21
- 125000002373 5 membered heterocyclic group Chemical group 0.000 claims 18
- 150000001875 compounds Chemical class 0.000 claims 16
- 125000004043 oxo group Chemical group O=* 0.000 claims 15
- 125000004070 6 membered heterocyclic group Chemical group 0.000 claims 12
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 9
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 9
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical group N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 8
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 8
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 7
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 6
- 125000002098 pyridazinyl group Chemical group 0.000 claims 6
- 125000002837 carbocyclic group Chemical group 0.000 claims 5
- -1 tetrahydropyrimidinyl Chemical group 0.000 claims 5
- 125000000876 trifluoromethoxy group Chemical group FC(F)(F)O* 0.000 claims 5
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical group [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims 4
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical group [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims 4
- 229910052757 nitrogen Chemical group 0.000 claims 4
- 239000001301 oxygen Substances 0.000 claims 4
- 239000008194 pharmaceutical composition Substances 0.000 claims 4
- 239000011593 sulfur Chemical group 0.000 claims 4
- 125000001399 1,2,3-triazolyl group Chemical group N1N=NC(=C1)* 0.000 claims 3
- 125000004504 1,2,4-oxadiazolyl group Chemical group 0.000 claims 3
- 125000001376 1,2,4-triazolyl group Chemical group N1N=C(N=C1)* 0.000 claims 3
- 125000004506 1,2,5-oxadiazolyl group Chemical group 0.000 claims 3
- 125000000753 cycloalkyl group Chemical group 0.000 claims 3
- 125000005051 dihydropyrazinyl group Chemical group N1(CC=NC=C1)* 0.000 claims 3
- 125000004925 dihydropyridyl group Chemical group N1(CC=CC=C1)* 0.000 claims 3
- 125000005053 dihydropyrimidinyl group Chemical group N1(CN=CC=C1)* 0.000 claims 3
- 201000010099 disease Diseases 0.000 claims 3
- 208000035475 disorder Diseases 0.000 claims 3
- 229910052739 hydrogen Inorganic materials 0.000 claims 3
- 239000001257 hydrogen Substances 0.000 claims 3
- 125000004435 hydrogen atom Chemical class [H]* 0.000 claims 3
- 125000002883 imidazolyl group Chemical group 0.000 claims 3
- 125000002971 oxazolyl group Chemical group 0.000 claims 3
- 125000003373 pyrazinyl group Chemical group 0.000 claims 3
- 125000003226 pyrazolyl group Chemical group 0.000 claims 3
- 125000004076 pyridyl group Chemical group 0.000 claims 3
- 125000000714 pyrimidinyl group Chemical group 0.000 claims 3
- 125000000719 pyrrolidinyl group Chemical group 0.000 claims 3
- 150000003839 salts Chemical class 0.000 claims 3
- 125000003831 tetrazolyl group Chemical group 0.000 claims 3
- 125000000335 thiazolyl group Chemical group 0.000 claims 3
- 230000004913 activation Effects 0.000 claims 2
- 102000016959 beta-3 Adrenergic Receptors Human genes 0.000 claims 2
- 108010014502 beta-3 Adrenergic Receptors Proteins 0.000 claims 2
- 229910052799 carbon Inorganic materials 0.000 claims 2
- 125000001153 fluoro group Chemical group F* 0.000 claims 2
- 230000001404 mediated effect Effects 0.000 claims 2
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 claims 2
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims 1
- 206010020853 Hypertonic bladder Diseases 0.000 claims 1
- 206010027566 Micturition urgency Diseases 0.000 claims 1
- 208000009722 Overactive Urinary Bladder Diseases 0.000 claims 1
- 208000000921 Urge Urinary Incontinence Diseases 0.000 claims 1
- 206010046543 Urinary incontinence Diseases 0.000 claims 1
- 239000013543 active substance Substances 0.000 claims 1
- 125000000217 alkyl group Chemical group 0.000 claims 1
- 125000004429 atom Chemical group 0.000 claims 1
- 125000004093 cyano group Chemical group *C#N 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 125000000623 heterocyclic group Chemical group 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 208000020629 overactive bladder Diseases 0.000 claims 1
- 230000002265 prevention Effects 0.000 claims 1
- 125000006413 ring segment Chemical group 0.000 claims 1
- 125000001424 substituent group Chemical group 0.000 claims 1
- 0 C(*Cc1c2)c1ccc2C1=Cc2ccccc2*1 Chemical compound C(*Cc1c2)c1ccc2C1=Cc2ccccc2*1 0.000 description 2
- YXTKDOFTHKWCKQ-UHFFFAOYSA-N C(C1)CN2C1=NC=CC2 Chemical compound C(C1)CN2C1=NC=CC2 YXTKDOFTHKWCKQ-UHFFFAOYSA-N 0.000 description 1
- ZWETXQBHVRWLPW-UHFFFAOYSA-N C(C1)C[n]2c1ncc2 Chemical compound C(C1)C[n]2c1ncc2 ZWETXQBHVRWLPW-UHFFFAOYSA-N 0.000 description 1
- BRXYDRIZVHRXCQ-UHFFFAOYSA-N C(C1)C[n]2c1nnc2 Chemical compound C(C1)C[n]2c1nnc2 BRXYDRIZVHRXCQ-UHFFFAOYSA-N 0.000 description 1
- QCCKBDNIBZPFCH-UHFFFAOYSA-N C(C1)Cc2c1nc[s]2 Chemical compound C(C1)Cc2c1nc[s]2 QCCKBDNIBZPFCH-UHFFFAOYSA-N 0.000 description 1
- RMFVVPBBEDMZQI-UHFFFAOYSA-N C(CC1)Cc2c1[s]cn2 Chemical compound C(CC1)Cc2c1[s]cn2 RMFVVPBBEDMZQI-UHFFFAOYSA-N 0.000 description 1
- LQKUERRPRLVSLZ-UHFFFAOYSA-N C1C[n]2nccc2C1 Chemical compound C1C[n]2nccc2C1 LQKUERRPRLVSLZ-UHFFFAOYSA-N 0.000 description 1
- LFHLEABTNIQIQO-UHFFFAOYSA-N C1N=Cc2ccccc12 Chemical compound C1N=Cc2ccccc12 LFHLEABTNIQIQO-UHFFFAOYSA-N 0.000 description 1
- KLXLVXOOWGCLAG-UHFFFAOYSA-N C1NC=Nc2c1cc[s]2 Chemical compound C1NC=Nc2c1cc[s]2 KLXLVXOOWGCLAG-UHFFFAOYSA-N 0.000 description 1
- HCKWIDXZRSTLMG-UHFFFAOYSA-N C1NC=Nc2c1cn[nH]2 Chemical compound C1NC=Nc2c1cn[nH]2 HCKWIDXZRSTLMG-UHFFFAOYSA-N 0.000 description 1
- MXMZCLLIUQEKSN-UHFFFAOYSA-N C1Nc2ccccc2N1 Chemical compound C1Nc2ccccc2N1 MXMZCLLIUQEKSN-UHFFFAOYSA-N 0.000 description 1
- SIKJAQJRHWYJAI-UHFFFAOYSA-N c1c[nH]c2ccccc12 Chemical compound c1c[nH]c2ccccc12 SIKJAQJRHWYJAI-UHFFFAOYSA-N 0.000 description 1
- BAXOFTOLAUCFNW-UHFFFAOYSA-N c1n[nH]c2ccccc12 Chemical compound c1n[nH]c2ccccc12 BAXOFTOLAUCFNW-UHFFFAOYSA-N 0.000 description 1
- HYZJCKYKOHLVJF-UHFFFAOYSA-N c1nc2ccccc2[nH]1 Chemical compound c1nc2ccccc2[nH]1 HYZJCKYKOHLVJF-UHFFFAOYSA-N 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US33001310P | 2010-04-30 | 2010-04-30 | |
| US61/330,013 | 2010-04-30 | ||
| PCT/US2011/033741 WO2011137054A1 (en) | 2010-04-30 | 2011-04-25 | Novel beta 3 adrenergic receptor agonists |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2013527847A JP2013527847A (ja) | 2013-07-04 |
| JP2013527847A5 true JP2013527847A5 (enExample) | 2014-06-19 |
| JP5812500B2 JP5812500B2 (ja) | 2015-11-17 |
Family
ID=44861881
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2013508120A Expired - Fee Related JP5812500B2 (ja) | 2010-04-30 | 2011-04-25 | 新規なβ３アドレナリン作動性受容体アゴニスト |
Country Status (6)
| Country | Link |
|---|---|
| US (1) | US8748433B2 (enExample) |
| EP (1) | EP2563123B1 (enExample) |
| JP (1) | JP5812500B2 (enExample) |
| AU (1) | AU2011245499B2 (enExample) |
| CA (1) | CA2796877A1 (enExample) |
| WO (1) | WO2011137054A1 (enExample) |
Families Citing this family (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US9907767B2 (en) | 2010-08-03 | 2018-03-06 | Velicept Therapeutics, Inc. | Pharmaceutical compositions and the treatment of overactive bladder |
| PE20131341A1 (es) | 2010-08-03 | 2013-12-07 | Altherx Inc | Combinaciones de agonistas del receptor beta-3-adrenergico y antagonistas del receptor muscarinico para tratar vejiga hiperactiva |
| US9522129B2 (en) | 2010-08-03 | 2016-12-20 | Velicept Therapeutics, Inc. | Pharmaceutical Combination |
| ES2584427T3 (es) | 2011-10-27 | 2016-09-27 | Merck Sharp & Dohme Corp. | Proceso para la preparación de agonistas beta 3 y productos intermedios |
| WO2013062881A1 (en) | 2011-10-27 | 2013-05-02 | Merck Sharp & Dohme Corp. | Process for making beta 3 agonists and intermediates |
| JP6383403B2 (ja) | 2013-03-15 | 2018-08-29 | メルク・シャープ・アンド・ドーム・コーポレーションＭｅｒｃｋ Ｓｈａｒｐ ＆ Ｄｏｈｍｅ Ｃｏｒｐ． | β−３作動薬および中間体の製造方法 |
| MX2017007054A (es) | 2014-12-03 | 2018-05-02 | Velicept Therapeutics Inc | Composiciones y métodos para usar solabegron de liberación modificada para sintomas del tracto urinario inferior. |
| CN108290824B (zh) | 2015-10-23 | 2022-03-11 | B3Ar治疗股份有限公司 | 索拉贝隆两性离子及其应用 |
| KR20250099259A (ko) | 2017-06-06 | 2025-07-01 | 유로반트 사이언시즈 게엠베하 | 과민성 방광의 치료를 위한 비베그론의 용도 |
| CN108250194A (zh) * | 2018-02-12 | 2018-07-06 | 李化绪 | 一种二氟苯并噻唑类化合物及其在降血脂药物中的应用 |
| TW202038963A (zh) | 2018-12-05 | 2020-11-01 | 瑞士商優洛凡特科學公司 | 維貝隆（ｖｉｂｅｇｒｏｎ）於治療患有良性前列腺增生之男性中膀胱過動症症狀之用途 |
| WO2023056029A1 (en) * | 2021-10-01 | 2023-04-06 | The Board Of Trustees Of The Leland Stanford Junior University | Beta3-adrenergic agonists for treatment of disorders of hair growth |
Family Cites Families (40)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| NL124473C (enExample) | 1960-07-26 | |||
| US3480626A (en) | 1967-05-18 | 1969-11-25 | Chem Fab Dr R Pfleger | Certain azoniaspironortropine derivatives |
| DD106643A1 (enExample) | 1973-07-12 | 1974-06-20 | ||
| JPS5980664A (ja) | 1982-09-30 | 1984-05-10 | Fujisawa Pharmaceut Co Ltd | α−アリ−ル−α−ピリジル脂肪酸誘導体およびその製法 |
| US5382600A (en) | 1988-01-22 | 1995-01-17 | Pharmacia Aktiebolag | 3,3-diphenylpropylamines and pharmaceutical compositions thereof |
| IL91377A (en) | 1988-09-14 | 1996-09-12 | Nippon Shinyaku Co Ltd | Derivatives of botinylamine glycolate |
| GB8906166D0 (en) | 1989-03-17 | 1989-05-04 | Pfizer Ltd | Therapeutic agents |
| US5164190A (en) | 1990-12-11 | 1992-11-17 | Theratech, Inc. | Subsaturated transdermal drug delivery device exhibiting enhanced drug flux |
| ATE154935T1 (de) * | 1993-06-14 | 1997-07-15 | Pfizer | Zweite amine als antidiabetische mittel und für die behandlung von fettleibigkeit |
| JP3294961B2 (ja) | 1993-12-10 | 2002-06-24 | 杏林製薬株式会社 | 新規イミダゾール誘導体及びその製造法 |
| US5627200A (en) * | 1994-09-26 | 1997-05-06 | Pfizer Inc | β3 -Adrenoceptor agonists and antagonists for the treatment of intestinal motility disorders, depression, prostate disease and dyslipidemia |
| NO2005012I1 (no) | 1994-12-28 | 2005-06-06 | Debio Rech Pharma Sa | Triptorelin og farmasoytisk akseptable salter derav |
| US5601839A (en) | 1995-04-26 | 1997-02-11 | Theratech, Inc. | Triacetin as a penetration enhancer for transdermal delivery of a basic drug |
| EP0788353A1 (en) | 1995-09-18 | 1997-08-13 | Ligand Pharmaceuticals, Inc. | Ppar gamma antagonists for treating obesity |
| AU7692996A (en) | 1995-12-01 | 1997-06-27 | Ciba-Geigy Ag | Receptor antagonists |
| AU1328197A (en) | 1995-12-01 | 1997-06-19 | Synaptic Pharmaceutical Corporation | Aryl sulfonamide and sulfamide derivatives and uses thereof |
| WO1997020822A1 (en) | 1995-12-01 | 1997-06-12 | Novartis Ag | Quinazolin-2,4-diazirines as npy receptor antagonist |
| AU7626496A (en) | 1995-12-01 | 1997-06-27 | Ciba-Geigy Ag | Heteroaryl compounds |
| WO1997020821A1 (en) | 1995-12-01 | 1997-06-12 | Novartis Ag | Heteroaryl derivatives |
| ATE236137T1 (de) | 1996-02-02 | 2003-04-15 | Merck & Co Inc | Heterocyclische verbindungen als antidiabetische mittel und für die behandlung von fettleibigkeit |
| CA2244831A1 (en) | 1996-02-02 | 1997-08-07 | John T. Olson | Method of treating diabetes and related disease states |
| JP2002503202A (ja) | 1996-02-02 | 2002-01-29 | メルク エンド カンパニー インコーポレーテッド | 抗糖尿病薬 |
| CA2245524A1 (en) | 1996-02-02 | 1997-08-07 | Wei Han | Antidiabetic agents |
| AU1856997A (en) | 1996-02-02 | 1997-08-22 | Merck & Co., Inc. | Method for raising hdl cholesterol levels |
| GB9606805D0 (en) | 1996-03-30 | 1996-06-05 | Glaxo Wellcome Inc | Medicaments |
| EP0957073A1 (en) | 1998-05-12 | 1999-11-17 | Schwarz Pharma Ag | Novel derivatives of 3,3-diphenylpropylamines |
| SE9803871D0 (sv) | 1998-11-11 | 1998-11-11 | Pharmacia & Upjohn Ab | Therapeutic method and formulation |
| SK287111B6 (sk) | 1998-08-27 | 2009-12-07 | Pharmacia & Upjohn Ab | Farmaceutický prípravok obsahujúci tolterodin s regulovaným uvoľňovaním |
| GB2356197A (en) * | 1999-10-12 | 2001-05-16 | Merck & Co Inc | Amide derivatives as beta 3 agonists |
| DK1227806T3 (da) | 1999-11-11 | 2005-10-31 | Pfizer Health Ab | Farmaceutisk præparat indeholdende tolterodin og dets anvendelse |
| DE19955190A1 (de) | 1999-11-16 | 2001-06-21 | Sanol Arznei Schwarz Gmbh | Stabile Salze neuartiger Derivate von 3,3-Diphenylpropylaminen |
| AU5378201A (en) | 2000-04-26 | 2001-11-07 | Watson Pharmaceuticals Inc | Minimizing adverse experience associated with oxybutynin therapy |
| WO2001083451A1 (en) * | 2000-04-28 | 2001-11-08 | Asahi Kasei Kabushiki Kaisha | Novel bicyclic compounds |
| AU2001266100B9 (en) | 2000-06-27 | 2005-10-06 | Laboratorios S.A.L.V.A.T., S.A. | Carbamates derived from arylalkylamines |
| US6506901B2 (en) * | 2000-07-17 | 2003-01-14 | Wyeth | Substituted 2-(S)-hydroxy-3-(piperidin-4-yl-methylamino)-propyl ethers and substituted 2-aryl-2-(R)-hydroxy-1-(piperidin-4-yl-methyl)-ethylamine β-3 adrenergic receptor agonists |
| EP1447400B1 (en) * | 2001-10-25 | 2008-09-17 | Asahi Kasei Pharma Corporation | Bicyclic compound |
| EP1546098B1 (en) | 2002-07-31 | 2008-05-28 | Ranbaxy Laboratories Limited | 3,6-disubstituted azabicyclo [3.1.0]hexane derivatives useful as muscarinic receptor antagonists |
| JP2007507504A (ja) | 2003-09-30 | 2007-03-29 | メルク エンド カムパニー インコーポレーテッド | フェニルピロリジンエーテル系タキキニン受容体拮抗薬 |
| TWI341198B (en) | 2004-01-27 | 2011-05-01 | Merck Sharp & Dohme | Hydroisoindoline tachykinin receptor antagonists |
| PE20091825A1 (es) * | 2008-04-04 | 2009-12-04 | Merck & Co Inc | Hidroximetil pirrolidinas como agonistas del receptor adrenergico beta 3 |
-
2011
- 2011-04-25 CA CA2796877A patent/CA2796877A1/en active Pending
- 2011-04-25 WO PCT/US2011/033741 patent/WO2011137054A1/en not_active Ceased
- 2011-04-25 AU AU2011245499A patent/AU2011245499B2/en not_active Ceased
- 2011-04-25 EP EP11775471.3A patent/EP2563123B1/en not_active Not-in-force
- 2011-04-25 US US13/643,361 patent/US8748433B2/en not_active Expired - Fee Related
- 2011-04-25 JP JP2013508120A patent/JP5812500B2/ja not_active Expired - Fee Related