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 (https=) | 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 (https=) |
| EP (1) | EP2470012B1 (https=) |
| JP (1) | JP5671538B2 (https=) |
| CN (1) | CN102573471B (https=) |
| AU (1) | AU2010286694B2 (https=) |
| BR (1) | BR112012004333A2 (https=) |
| CA (1) | CA2770475C (https=) |
| IN (1) | IN2012DN00971A (https=) |
| MX (1) | MX2012002366A (https=) |
| WO (1) | WO2011025774A1 (https=) |
Families Citing this family (26)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU2011279845B8 (en) | 2010-07-23 | 2014-11-20 | Merck Sharp & Dohme Corp. | Novel pyrrolidine derived beta 3 adrenergic receptor agonists |
| BR112013002511A2 (pt) | 2010-08-03 | 2017-06-27 | Altherx Inc | combinações de agonistas de receptores adrenérgicos beta - 3 e antagonistas receptores muscarínicos para tratamento da bexica hiperativa |
| US9522129B2 (en) | 2010-08-03 | 2016-12-20 | Velicept Therapeutics, Inc. | Pharmaceutical Combination |
| US9907767B2 (en) | 2010-08-03 | 2018-03-06 | Velicept Therapeutics, Inc. | Pharmaceutical compositions and the treatment of overactive bladder |
| 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 |
| MX2021012208A (es) | 2013-10-04 | 2023-01-19 | Infinity Pharmaceuticals Inc | Compuestos heterocíclicos y usos de los mismos. |
| WO2015051241A1 (en) | 2013-10-04 | 2015-04-09 | Infinity Pharmaceuticals, Inc. | Heterocyclic compounds and uses thereof |
| NZ724368A (en) | 2014-03-19 | 2023-07-28 | Infinity Pharmaceuticals Inc | Heterocyclic compounds for use in the treatment of pi3k-gamma mediated disorders |
| WO2016054491A1 (en) | 2014-10-03 | 2016-04-07 | Infinity Pharmaceuticals, Inc. | Heterocyclic compounds and uses thereof |
| CN107205964A (zh) | 2014-12-03 | 2017-09-26 | 威力塞帕特治疗股份有限公司 | 使用调节释放索拉贝隆用于下尿路症状的组合物和方法 |
| EP3317258A4 (en) * | 2015-07-01 | 2019-06-26 | Pharmakea, Inc. | LYSYL OXIDASE LIKE 2 INHIBITORS AND USES THEREOF |
| EP4585268A3 (en) | 2015-09-14 | 2025-10-15 | Twelve Therapeutics, Inc. | Solid forms of isoquinolinone derivatives, process of making, compositions comprising, and methods of using the same |
| 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 |
| JP7114076B2 (ja) | 2015-12-22 | 2022-08-08 | シャイ・セラピューティクス・エルエルシー | がん及び炎症性疾患の処置のための化合物 |
| US10759806B2 (en) | 2016-03-17 | 2020-09-01 | 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 |
| JP7514005B2 (ja) | 2017-06-21 | 2024-07-10 | シャイ・セラピューティクス・エルエルシー | がん、炎症性疾患、ラソパシー、及び線維性疾患の治療のためのｒａｓスーパーファミリーと相互作用する化合物 |
| 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 |
| JP7407461B2 (ja) | 2018-12-19 | 2024-01-04 | シャイ・セラピューティクス・エルエルシー | がん、炎症性疾患、ｒａｓ病、及び線維性疾患の処置のためのｒａｓスーパーファミリーと相互作用する化合物 |
| 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 |
|---|---|---|---|---|
| EP0071399A3 (en) * | 1981-07-22 | 1983-12-07 | Syntex (U.S.A.) Inc. | Substituted pyrrolidine cardiovascular system regulators and antihypertensives, their preparation and use |
| 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 |
| PE20091825A1 (es) * | 2008-04-04 | 2009-12-04 | Merck & Co Inc | Hidroximetil pirrolidinas como agonistas del receptor adrenergico beta 3 |
| AU2009231967B2 (en) * | 2008-04-04 | 2013-02-07 | Merck Sharp & Dohme Corp. | Hydroxymethyl pyrrolidines as beta 3 adrenergic receptor agonists |
| US8354403B2 (en) * | 2009-08-27 | 2013-01-15 | Merck Sharp & Dohme Corp. | Pyrrolidine derived beta 3 adrenergic receptor agonists |
-
2010
- 2010-08-24 MX MX2012002366A patent/MX2012002366A/es active IP Right Grant
- 2010-08-24 WO PCT/US2010/046468 patent/WO2011025774A1/en not_active Ceased
- 2010-08-24 IN IN971DEN2012 patent/IN2012DN00971A/en unknown
- 2010-08-24 JP JP2012526908A patent/JP5671538B2/ja not_active Expired - Fee Related
- 2010-08-24 AU AU2010286694A patent/AU2010286694B2/en not_active Ceased
- 2010-08-24 BR BR112012004333A patent/BR112012004333A2/pt not_active Application Discontinuation
- 2010-08-24 CA CA2770475A patent/CA2770475C/en not_active Expired - Fee Related
- 2010-08-24 US US13/392,282 patent/US8604038B2/en active Active
- 2010-08-24 EP EP10812548.5A patent/EP2470012B1/en not_active Not-in-force
- 2010-08-24 CN CN201080037958.8A patent/CN102573471B/zh not_active Expired - Fee Related
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