JP2013503167A5 - - Google Patents
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- Publication number
- JP2013503167A5 JP2013503167A5 JP2012526908A JP2012526908A JP2013503167A5 JP 2013503167 A5 JP2013503167 A5 JP 2013503167A5 JP 2012526908 A JP2012526908 A JP 2012526908A JP 2012526908 A JP2012526908 A JP 2012526908A JP 2013503167 A5 JP2013503167 A5 JP 2013503167A5
- Authority
- JP
- Japan
- Prior art keywords
- halogen
- optionally substituted
- independently
- nitrogen
- group
- 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
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- 229910052736 halogen Inorganic materials 0.000 claims description 19
- 150000002367 halogens Chemical class 0.000 claims description 19
- 125000005843 halogen group Chemical group 0.000 claims description 15
- 229910052739 hydrogen Inorganic materials 0.000 claims description 9
- 239000001257 hydrogen Substances 0.000 claims description 9
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 5
- 125000000217 alkyl group Chemical group 0.000 claims description 5
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical group N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 32
- 229910052757 nitrogen Chemical group 0.000 claims 20
- 125000005842 heteroatom Chemical group 0.000 claims 19
- 229910052760 oxygen Inorganic materials 0.000 claims 19
- 229910052717 sulfur Inorganic materials 0.000 claims 19
- 239000001301 oxygen Substances 0.000 claims 17
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical group [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims 16
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical group [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims 15
- 239000011593 sulfur Chemical group 0.000 claims 15
- 150000001875 compounds Chemical class 0.000 claims 13
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 11
- 125000002373 5 membered heterocyclic group Chemical group 0.000 claims 9
- 125000004070 6 membered heterocyclic group Chemical group 0.000 claims 9
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 6
- 125000002837 carbocyclic group Chemical group 0.000 claims 6
- 125000004093 cyano group Chemical group *C#N 0.000 claims 5
- 125000000623 heterocyclic group Chemical group 0.000 claims 5
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 5
- 150000002431 hydrogen Chemical class 0.000 claims 4
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 4
- 150000003839 salts Chemical class 0.000 claims 4
- -1 OR a Chemical group 0.000 claims 3
- 239000008194 pharmaceutical composition Substances 0.000 claims 3
- 125000004076 pyridyl group Chemical group 0.000 claims 3
- 125000004485 2-pyrrolidinyl group Chemical group [H]N1C([H])([H])C([H])([H])C([H])([H])C1([H])* 0.000 claims 2
- KXDAEFPNCMNJSK-UHFFFAOYSA-N Benzamide Chemical compound NC(=O)C1=CC=CC=C1 KXDAEFPNCMNJSK-UHFFFAOYSA-N 0.000 claims 2
- 150000001204 N-oxides Chemical class 0.000 claims 2
- 229910052799 carbon Inorganic materials 0.000 claims 2
- 125000000753 cycloalkyl group Chemical group 0.000 claims 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 2
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 2
- 125000004434 sulfur atom Chemical group 0.000 claims 2
- MOWXJLUYGFNTAL-DEOSSOPVSA-N (s)-[2-chloro-4-fluoro-5-(7-morpholin-4-ylquinazolin-4-yl)phenyl]-(6-methoxypyridazin-3-yl)methanol Chemical compound N1=NC(OC)=CC=C1[C@@H](O)C1=CC(C=2C3=CC=C(C=C3N=CN=2)N2CCOCC2)=C(F)C=C1Cl MOWXJLUYGFNTAL-DEOSSOPVSA-N 0.000 claims 1
- MHCVCKDNQYMGEX-UHFFFAOYSA-N 1,1'-biphenyl;phenoxybenzene Chemical group C1=CC=CC=C1C1=CC=CC=C1.C=1C=CC=CC=1OC1=CC=CC=C1 MHCVCKDNQYMGEX-UHFFFAOYSA-N 0.000 claims 1
- 125000001399 1,2,3-triazolyl group Chemical group N1N=NC(=C1)* 0.000 claims 1
- 125000004504 1,2,4-oxadiazolyl group Chemical group 0.000 claims 1
- 125000001376 1,2,4-triazolyl group Chemical group N1N=C(N=C1)* 0.000 claims 1
- 125000004506 1,2,5-oxadiazolyl group Chemical group 0.000 claims 1
- NCZMLHHWWPHDGU-ISJGIBHGSA-N 4-[[(2s,5r)-5-[(r)-hydroxy(phenyl)methyl]pyrrolidin-2-yl]methyl]-n-methyl-n-(pyridin-3-ylmethyl)benzamide Chemical compound C=1C=C(C[C@H]2N[C@H](CC2)[C@H](O)C=2C=CC=CC=2)C=CC=1C(=O)N(C)CC1=CC=CN=C1 NCZMLHHWWPHDGU-ISJGIBHGSA-N 0.000 claims 1
- MYMOFIZGZYHOMD-UHFFFAOYSA-N Dioxygen Chemical compound O=O MYMOFIZGZYHOMD-UHFFFAOYSA-N 0.000 claims 1
- 206010020853 Hypertonic bladder Diseases 0.000 claims 1
- JCXJVPUVTGWSNB-UHFFFAOYSA-N Nitrogen dioxide Chemical class O=[N]=O JCXJVPUVTGWSNB-UHFFFAOYSA-N 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
- LXRZVMYMQHNYJB-UNXOBOICSA-N [(1R,2S,4R)-4-[[5-[4-[(1R)-7-chloro-1,2,3,4-tetrahydroisoquinolin-1-yl]-5-methylthiophene-2-carbonyl]pyrimidin-4-yl]amino]-2-hydroxycyclopentyl]methyl sulfamate Chemical compound CC1=C(C=C(S1)C(=O)C1=C(N[C@H]2C[C@H](O)[C@@H](COS(N)(=O)=O)C2)N=CN=C1)[C@@H]1NCCC2=C1C=C(Cl)C=C2 LXRZVMYMQHNYJB-UNXOBOICSA-N 0.000 claims 1
- 239000013543 active substance Substances 0.000 claims 1
- 125000004122 cyclic group Chemical group 0.000 claims 1
- 125000005051 dihydropyrazinyl group Chemical group N1(CC=NC=C1)* 0.000 claims 1
- 125000004925 dihydropyridyl group Chemical group N1(CC=CC=C1)* 0.000 claims 1
- 125000005053 dihydropyrimidinyl group Chemical group N1(CN=CC=C1)* 0.000 claims 1
- 201000010099 disease Diseases 0.000 claims 1
- 208000035475 disorder Diseases 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 1
- 125000002883 imidazolyl group Chemical group 0.000 claims 1
- LOFXRNVLYKTYJZ-SKBVVQJISA-N n-[(2-fluorophenyl)methyl]-4-[[(2s,5r)-5-[(r)-hydroxy(phenyl)methyl]pyrrolidin-2-yl]methyl]-n-methylbenzamide Chemical compound C=1C=C(C[C@H]2N[C@H](CC2)[C@H](O)C=2C=CC=CC=2)C=CC=1C(=O)N(C)CC1=CC=CC=C1F LOFXRNVLYKTYJZ-SKBVVQJISA-N 0.000 claims 1
- XJCJGIGCUIJOJY-QQKQFIJSSA-N n-[(6-aminopyridin-2-yl)methyl]-4-[[(2s,5r)-5-[(r)-hydroxy(phenyl)methyl]pyrrolidin-2-yl]methyl]-n-methylbenzamide Chemical compound C=1C=C(C[C@H]2N[C@H](CC2)[C@H](O)C=2C=CC=CC=2)C=CC=1C(=O)N(C)CC1=CC=CC(N)=N1 XJCJGIGCUIJOJY-QQKQFIJSSA-N 0.000 claims 1
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims 1
- 208000020629 overactive bladder Diseases 0.000 claims 1
- 125000002971 oxazolyl group Chemical group 0.000 claims 1
- 230000002265 prevention Effects 0.000 claims 1
- 125000003373 pyrazinyl group Chemical group 0.000 claims 1
- 125000003226 pyrazolyl group Chemical group 0.000 claims 1
- 125000002098 pyridazinyl group Chemical group 0.000 claims 1
- 125000000714 pyrimidinyl group Chemical group 0.000 claims 1
- 125000000719 pyrrolidinyl group Chemical group 0.000 claims 1
- 125000003831 tetrazolyl group Chemical group 0.000 claims 1
- 125000000335 thiazolyl group Chemical group 0.000 claims 1
- 206010046494 urge incontinence Diseases 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US23748709P | 2009-08-27 | 2009-08-27 | |
| US61/237,487 | 2009-08-27 | ||
| PCT/US2010/046468 WO2011025774A1 (en) | 2009-08-27 | 2010-08-24 | Novel pyrrolidine derived beta 3 adrenergic receptor agonists |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2013503167A JP2013503167A (ja) | 2013-01-31 |
| JP2013503167A5 true JP2013503167A5 (enExample) | 2014-12-18 |
| JP5671538B2 JP5671538B2 (ja) | 2015-02-18 |
Family
ID=43628346
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2012526908A Expired - Fee Related JP5671538B2 (ja) | 2009-08-27 | 2010-08-24 | 新規なピロリジン誘導体型β３−アドレナリン作動性受容体アゴニスト |
Country Status (10)
| Country | Link |
|---|---|
| US (1) | US8604038B2 (enExample) |
| EP (1) | EP2470012B1 (enExample) |
| JP (1) | JP5671538B2 (enExample) |
| CN (1) | CN102573471B (enExample) |
| AU (1) | AU2010286694B2 (enExample) |
| BR (1) | BR112012004333A2 (enExample) |
| CA (1) | CA2770475C (enExample) |
| IN (1) | IN2012DN00971A (enExample) |
| MX (1) | MX2012002366A (enExample) |
| WO (1) | WO2011025774A1 (enExample) |
Families Citing this family (26)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US9186354B2 (en) | 2010-07-23 | 2015-11-17 | Merck Sharp & Dohme Corp. | Pyrrolidine derived β3 adrenergic receptor agonists |
| 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 |
| US8940742B2 (en) | 2012-04-10 | 2015-01-27 | Infinity Pharmaceuticals, Inc. | Heterocyclic compounds and uses thereof |
| US9486448B2 (en) | 2013-10-03 | 2016-11-08 | Merck Sharp & Dohme Corp. | Pyrrolidine derived beta 3 adrenergic receptor agonists |
| PE20160685A1 (es) | 2013-10-04 | 2016-07-23 | Infinity Pharmaceuticals Inc | Compuestos heterociclicos y usos de los mismos |
| WO2015051241A1 (en) | 2013-10-04 | 2015-04-09 | Infinity Pharmaceuticals, Inc. | Heterocyclic compounds and uses thereof |
| CN113620958A (zh) | 2014-03-19 | 2021-11-09 | 无限药品股份有限公司 | 用于治疗PI3K-γ介导的障碍的杂环化合物 |
| US9708348B2 (en) | 2014-10-03 | 2017-07-18 | Infinity Pharmaceuticals, Inc. | Trisubstituted bicyclic heterocyclic compounds with kinase activities and uses thereof |
| KR20170086659A (ko) | 2014-12-03 | 2017-07-26 | 벨리셉트 테라퓨틱스, 인크. | 하부 요로 증상을 위한 변형 방출형 솔라베그론을 이용한 조성물 및 방법 |
| US20180186755A1 (en) * | 2015-07-01 | 2018-07-05 | Pharmakea, Inc. | Lysyl oxidase-like 2 inhibitors and uses thereof |
| PH12018500554B1 (en) | 2015-09-14 | 2024-01-24 | Infinity Pharmaceuticals Inc | Solid forms of isoquinolinone derivatives, process of making, compositions comprising, and methods of using the same |
| PL3365321T3 (pl) | 2015-10-23 | 2024-03-25 | B3Ar Therapeutics, Inc. | Jon obojnaczy solabegronu i jego zastosowania |
| SG11201804901WA (en) | 2015-12-22 | 2018-07-30 | SHY Therapeutics LLC | Compounds for the treatment of cancer and inflammatory disease |
| WO2017161116A1 (en) | 2016-03-17 | 2017-09-21 | Infinity Pharmaceuticals, Inc. | Isotopologues of isoquinolinone and quinazolinone compounds and uses thereof as pi3k kinase inhibitors |
| WO2017214269A1 (en) | 2016-06-08 | 2017-12-14 | Infinity Pharmaceuticals, Inc. | Heterocyclic compounds and uses thereof |
| US10408983B2 (en) | 2016-08-16 | 2019-09-10 | Moxtek, Inc. | Durable, high performance wire grid polarizer having permeable junction between top protection layer |
| CN106831601A (zh) * | 2017-01-13 | 2017-06-13 | 河北博伦特药业有限公司 | 一种2‑氨基甲基嘧啶盐酸盐及其衍生物的合成方法 |
| CA3066939A1 (en) | 2017-06-21 | 2018-12-27 | SHY Therapeutics LLC | Compounds that interact with the ras superfamily for the treatment of cancers, inflammatory diseases, rasopathies, and fibrotic disease |
| GB201714734D0 (en) | 2017-09-13 | 2017-10-25 | Atrogi Ab | New compounds and uses |
| EP3893892A4 (en) * | 2018-12-12 | 2022-09-14 | Rutgers, the State University of New Jersey | Organic compounds |
| WO2020132071A1 (en) | 2018-12-19 | 2020-06-25 | Shy Therapeutics. Llc | Compounds that interact with the ras superfamily for the treatment of cancers, inflammatory diseases, rasopathies, and f1brotic disease |
| GB201903832D0 (en) | 2019-03-20 | 2019-05-01 | Atrogi Ab | New compounds and methods |
| GB202113588D0 (en) | 2021-09-23 | 2021-11-10 | Atrogi Ab | New compounds and methods |
| CN113816917B (zh) * | 2021-11-19 | 2022-02-18 | 奥锐特药业(天津)有限公司 | 一种维贝格龙中间体的制备方法 |
Family Cites Families (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DK328382A (da) * | 1981-07-22 | 1983-01-23 | Syntex Inc | Fremgangsmaade til fremstilling af antihypertensive midler |
| US6015824A (en) * | 1998-02-10 | 2000-01-18 | Hoffmann-La Roche Ag | Pyrrolidine and piperidine derivatives and treatment of neurodegenerative disorders |
| GB2356197A (en) | 1999-10-12 | 2001-05-16 | Merck & Co Inc | Amide derivatives as beta 3 agonists |
| US6864268B2 (en) | 2002-02-27 | 2005-03-08 | Pfizer Inc. | β3 adrenergic receptor agonists |
| JP2011516482A (ja) * | 2008-04-04 | 2011-05-26 | メルク・シャープ・エンド・ドーム・コーポレイション | β３アドレナリン作動性受容体アゴニストとしてのヒドロキシメチルピロリジン |
| PE20091825A1 (es) * | 2008-04-04 | 2009-12-04 | Merck & Co Inc | Hidroximetil pirrolidinas como agonistas del receptor adrenergico beta 3 |
| EP2470021B1 (en) * | 2009-08-27 | 2014-10-22 | Merck Sharp & Dohme Corp. | Novel pyrrolidine derived beta 3 adrenergic receptor agonists |
-
2010
- 2010-08-24 EP EP10812548.5A patent/EP2470012B1/en not_active Not-in-force
- 2010-08-24 BR BR112012004333A patent/BR112012004333A2/pt not_active Application Discontinuation
- 2010-08-24 CN CN201080037958.8A patent/CN102573471B/zh not_active Expired - Fee Related
- 2010-08-24 US US13/392,282 patent/US8604038B2/en active Active
- 2010-08-24 IN IN971DEN2012 patent/IN2012DN00971A/en unknown
- 2010-08-24 MX MX2012002366A patent/MX2012002366A/es active IP Right Grant
- 2010-08-24 CA CA2770475A patent/CA2770475C/en not_active Expired - Fee Related
- 2010-08-24 JP JP2012526908A patent/JP5671538B2/ja not_active Expired - Fee Related
- 2010-08-24 WO PCT/US2010/046468 patent/WO2011025774A1/en not_active Ceased
- 2010-08-24 AU AU2010286694A patent/AU2010286694B2/en not_active Ceased
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