JP5812500B2 - 新規なβ３アドレナリン作動性受容体アゴニスト - Google Patents
新規なβ３アドレナリン作動性受容体アゴニスト Download PDFInfo
- Publication number
- JP5812500B2 JP5812500B2 JP2013508120A JP2013508120A JP5812500B2 JP 5812500 B2 JP5812500 B2 JP 5812500B2 JP 2013508120 A JP2013508120 A JP 2013508120A JP 2013508120 A JP2013508120 A JP 2013508120A JP 5812500 B2 JP5812500 B2 JP 5812500B2
- Authority
- JP
- Japan
- Prior art keywords
- ring
- membered heterocyclic
- independently
- 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.)
- Expired - Fee Related
Links
- 0 CC(N)=C(CC*)NN Chemical compound CC(N)=C(CC*)NN 0.000 description 3
- TUVBJSPUCMUOSD-UHFFFAOYSA-N C(C1)Cc2c1cn[nH]2 Chemical compound C(C1)Cc2c1cn[nH]2 TUVBJSPUCMUOSD-UHFFFAOYSA-N 0.000 description 1
- WQCDCCSBNXFASP-UHFFFAOYSA-N C(C1)Cc2c1nc[o]2 Chemical compound C(C1)Cc2c1nc[o]2 WQCDCCSBNXFASP-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
- ZFJKWGRCVBGSQD-UHFFFAOYSA-N C(C=C1)c2c1[nH]cn2 Chemical compound C(C=C1)c2c1[nH]cn2 ZFJKWGRCVBGSQD-UHFFFAOYSA-N 0.000 description 1
- ARTURBRGMUCSCZ-HZBCCHQASA-N C/C=N\C(CCC1)[C@@H]1[I]=C Chemical compound C/C=N\C(CCC1)[C@@H]1[I]=C ARTURBRGMUCSCZ-HZBCCHQASA-N 0.000 description 1
- PKORYTIUMAOPED-UHFFFAOYSA-N C1NCNc2c1cccc2 Chemical compound C1NCNc2c1cccc2 PKORYTIUMAOPED-UHFFFAOYSA-N 0.000 description 1
- STIWEDICJHIFJT-UHFFFAOYSA-N C1NNCc2ccccc12 Chemical compound C1NNCc2ccccc12 STIWEDICJHIFJT-UHFFFAOYSA-N 0.000 description 1
- WQCOCIJDFQQMSI-FPLPWBNLSA-N CC/C(/N)=C(\CC)/NCNC Chemical compound CC/C(/N)=C(\CC)/NCNC WQCOCIJDFQQMSI-FPLPWBNLSA-N 0.000 description 1
- ATQUFXWBVZUTKO-UHFFFAOYSA-N CC1=CCCC1 Chemical compound CC1=CCCC1 ATQUFXWBVZUTKO-UHFFFAOYSA-N 0.000 description 1
- WOJMLUPYKCMJNC-CHWSQXEVSA-N COC([C@H](CCC#C)[C@@H](c1ccccc1)N=O)=O Chemical compound COC([C@H](CCC#C)[C@@H](c1ccccc1)N=O)=O WOJMLUPYKCMJNC-CHWSQXEVSA-N 0.000 description 1
- LLFHHFFVWTZQSU-UHFFFAOYSA-N NNc1ccccc1S Chemical compound NNc1ccccc1S LLFHHFFVWTZQSU-UHFFFAOYSA-N 0.000 description 1
- BAXOFTOLAUCFNW-UHFFFAOYSA-N c1c(cccc2)c2n[nH]1 Chemical compound c1c(cccc2)c2n[nH]1 BAXOFTOLAUCFNW-UHFFFAOYSA-N 0.000 description 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/4164—1,3-Diazoles
- A61K31/4184—1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/4196—1,2,4-Triazoles
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/425—Thiazoles
- A61K31/427—Thiazoles not condensed and containing further heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/425—Thiazoles
- A61K31/428—Thiazoles condensed with carbocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/10—Laxatives
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/10—Drugs for disorders of the urinary system of the bladder
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
Landscapes
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Epidemiology (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Engineering & Computer Science (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Urology & Nephrology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Plural Heterocyclic Compounds (AREA)
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 JP2013527847A5 (enExample) | 2014-06-19 |
| JP5812500B2 true 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 |
| US9522129B2 (en) | 2010-08-03 | 2016-12-20 | Velicept Therapeutics, Inc. | Pharmaceutical Combination |
| 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 |
| ES2584427T3 (es) | 2011-10-27 | 2016-09-27 | Merck Sharp & Dohme Corp. | Proceso para la preparación de agonistas beta 3 y productos intermedios |
| EP2770996B1 (en) | 2011-10-27 | 2016-09-28 | Merck Sharp & Dohme Corp. | Process for making beta 3 agonists and intermediates |
| LT2968269T (lt) | 2013-03-15 | 2019-10-25 | Merck Sharp & Dohme | Beta 3 agonistų ir tarpinių junginių gamybos būdas |
| KR20170086659A (ko) | 2014-12-03 | 2017-07-26 | 벨리셉트 테라퓨틱스, 인크. | 하부 요로 증상을 위한 변형 방출형 솔라베그론을 이용한 조성물 및 방법 |
| PL3365321T3 (pl) | 2015-10-23 | 2024-03-25 | B3Ar Therapeutics, Inc. | Jon obojnaczy solabegronu i jego zastosowania |
| AU2018282104B2 (en) | 2017-06-06 | 2024-07-11 | Urovant Sciences Gmbh | Use of vibegron to treat overactive bladder |
| 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 |
| EP3890743A1 (en) | 2018-12-05 | 2021-10-13 | Urovant Sciences GmbH | Vibegron for the treatment of overactive bladder symptoms |
| 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 |
|---|---|---|---|---|
| NL267508A (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 |
| WO1994029290A1 (en) * | 1993-06-14 | 1994-12-22 | Pfizer Inc. | Secondary amines as antidiabetic and antiobesity agents |
| 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 |
| US6028052A (en) | 1995-09-18 | 2000-02-22 | Ligand Pharmaceuticals Incorporated | Treating NIDDM with RXR agonists |
| WO1997020820A1 (en) | 1995-12-01 | 1997-06-12 | Novartis Ag | Heteroaryl compounds |
| WO1997019682A1 (en) | 1995-12-01 | 1997-06-05 | Synaptic Pharmaceutical Corporation | Aryl sulfonamide and sulfamide derivatives and uses thereof |
| WO1997020821A1 (en) | 1995-12-01 | 1997-06-12 | Novartis Ag | Heteroaryl derivatives |
| AU7692996A (en) | 1995-12-01 | 1997-06-27 | Ciba-Geigy Ag | Receptor antagonists |
| WO1997020822A1 (en) | 1995-12-01 | 1997-06-12 | Novartis Ag | Quinazolin-2,4-diazirines as npy receptor antagonist |
| EP0904079B1 (en) | 1996-02-02 | 2004-03-24 | Merck & Co., Inc. | Antidiabetic agents |
| EP0882029B1 (en) | 1996-02-02 | 2003-04-02 | Merck & Co., Inc. | Heterocyclic derivatives as antidiabetic and antiobesity agents |
| CA2244831A1 (en) | 1996-02-02 | 1997-08-07 | John T. Olson | Method of treating diabetes and related disease states |
| WO1997028115A1 (en) | 1996-02-02 | 1997-08-07 | Merck & Co., Inc. | Antidiabetic agents |
| WO1997028149A1 (en) | 1996-02-02 | 1997-08-07 | 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 |
| GEP20043354B (en) | 1998-08-27 | 2004-04-13 | Pharmacia & Upjohn Ab | Therapeutic Formulation for Administering Tolterodine with Controlled Release |
| SE9803871D0 (sv) | 1998-11-11 | 1998-11-11 | Pharmacia & Upjohn Ab | Therapeutic method and formulation |
| GB2356197A (en) * | 1999-10-12 | 2001-05-16 | Merck & Co Inc | Amide derivatives as beta 3 agonists |
| HK1054196B (zh) | 1999-11-11 | 2008-08-01 | 法马西雅公司 | 含托特罗定的药物制剂及其应用 |
| DE29923134U1 (de) | 1999-11-16 | 2000-06-29 | Schwarz Pharma Ag, 40789 Monheim | Stabile Salze neuartiger Derviate von 3,3-Diphenylpropylaminen |
| DK1280486T3 (da) | 2000-04-26 | 2011-02-14 | Watson Pharmaceuticals Inc | Minimering af bivirkning forbundet med oxybutinin-terapi |
| DK1277736T3 (da) * | 2000-04-28 | 2007-10-01 | Asahi Kasei Pharma Corp | Hidtil ukendte bicykliske forbindelser |
| BR0112297A (pt) | 2000-06-27 | 2003-05-06 | S A L V A T Lab Sa | Compostos carbamatos derivados de arilalquilaminas |
| 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 |
| WO2003035620A1 (en) * | 2001-10-25 | 2003-05-01 | Asahi Kasei Pharma Corporation | Bicyclic compound |
| AU2002368152A1 (en) | 2002-07-31 | 2004-02-25 | Ranbaxy Laboratories Limited | 3,6-disubstituted azabicyclo (3.1.0)hexane derivatives useful as muscarinic receptor antagonists |
| US7468437B2 (en) | 2003-09-30 | 2008-12-23 | Merck & Co., Inc. | Phenyl pyrrolidine ether tachykinin receptor antagonists |
| 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 JP JP2013508120A patent/JP5812500B2/ja not_active Expired - Fee Related
- 2011-04-25 EP EP11775471.3A patent/EP2563123B1/en active Active
- 2011-04-25 US US13/643,361 patent/US8748433B2/en active Active
- 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
Also Published As
| Publication number | Publication date |
|---|---|
| AU2011245499A1 (en) | 2012-09-20 |
| AU2011245499B2 (en) | 2014-09-25 |
| US8748433B2 (en) | 2014-06-10 |
| EP2563123A1 (en) | 2013-03-06 |
| JP2013527847A (ja) | 2013-07-04 |
| EP2563123B1 (en) | 2018-04-25 |
| EP2563123A4 (en) | 2013-10-23 |
| US20130053403A1 (en) | 2013-02-28 |
| CA2796877A1 (en) | 2011-11-03 |
| WO2011137054A1 (en) | 2011-11-03 |
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