JP2012533546A5 - - Google Patents
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- Publication number
- JP2012533546A5 JP2012533546A5 JP2012520691A JP2012520691A JP2012533546A5 JP 2012533546 A5 JP2012533546 A5 JP 2012533546A5 JP 2012520691 A JP2012520691 A JP 2012520691A JP 2012520691 A JP2012520691 A JP 2012520691A JP 2012533546 A5 JP2012533546 A5 JP 2012533546A5
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- JP
- Japan
- Prior art keywords
- acceptable salt
- pharmaceutically acceptable
- compound according
- methyl
- pharmaceutical composition
- 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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- 150000003839 salts Chemical class 0.000 claims 9
- 239000011780 sodium chloride Substances 0.000 claims 9
- 150000001875 compounds Chemical class 0.000 claims 8
- 239000008194 pharmaceutical composition Substances 0.000 claims 6
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 4
- 206010012601 Diabetes mellitus Diseases 0.000 claims 2
- 125000000753 cycloalkyl group Chemical group 0.000 claims 2
- 239000004615 ingredient Substances 0.000 claims 2
- 230000001225 therapeutic Effects 0.000 claims 2
- 125000006555 (C3-C5) cycloalkyl group Chemical group 0.000 claims 1
- RDTBTUCYZYOHAM-UHFFFAOYSA-N 1-methylsulfonyl-4-[4-[[1-[[1-(trifluoromethyl)cyclopropyl]methyl]piperidin-4-yl]methoxy]phenyl]-3,6-dihydro-2H-pyridine Chemical compound C1N(S(=O)(=O)C)CCC(C=2C=CC(OCC3CCN(CC4(CC4)C(F)(F)F)CC3)=CC=2)=C1 RDTBTUCYZYOHAM-UHFFFAOYSA-N 0.000 claims 1
- -1 2-Fluoro-2-methyl-propyl Chemical group 0.000 claims 1
- KZGNFYYDTXHWCN-UHFFFAOYSA-N 3-methyl-2-(1,2,3,6-tetrahydropyridin-4-yl)pyridine Chemical group CC1=CC=CN=C1C1=CCNCC1 KZGNFYYDTXHWCN-UHFFFAOYSA-N 0.000 claims 1
- 208000008589 Obesity Diseases 0.000 claims 1
- MFFMDFFZMYYVKS-SECBINFHSA-N Sitagliptin Chemical compound C([C@H](CC(=O)N1CC=2N(C(=NN=2)C(F)(F)F)CC1)N)C1=CC(F)=C(F)C=C1F MFFMDFFZMYYVKS-SECBINFHSA-N 0.000 claims 1
- 239000000969 carrier Substances 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 235000020824 obesity Nutrition 0.000 claims 1
- 229960004034 sitagliptin Drugs 0.000 claims 1
- 238000002560 therapeutic procedure Methods 0.000 claims 1
Claims (12)
- RbおよびRcは、Fおよびメチルから独立して選択されるか、もしくは結合してC3シクロアルキルを形成する、請求項1に記載の化合物、またはその薬学的に受容可能な塩。
- RbおよびRcは、メチルであるか、もしくは結合してC3シクロアルキルを形成する、請求項1もしくは2のいずれか一項に記載の化合物、またはその薬学的に受容可能な塩。
- Raは、CF3である、請求項1〜3のいずれか一項に記載の化合物、またはその薬学的に受容可能な塩。
- R2は、Hである、請求項1〜4のいずれか一項に記載の化合物、またはその薬学的に受容可能な塩。
- 5−[1−(2−フルオロ−2−メチル−プロピル)−ピペリジン−4−イルメトキシ]−1’−メタンスルホニル−1’,2’,3’,6’−テトラヒドロ−[2,4’]ビピリジニル、および1−メタンスルホニル−4−{4−[1−(1−トリフルオロメチル−シクロプロピルメチル)−ピペリジン−4−イルメトキシ]−フェニル}−1,2,3,6−テトラヒドロ−ピリジンから選択される、請求項1に記載の化合物、またはその薬学的に受容可能な塩。
- 請求項1〜6のいずれか一項に記載の化合物、またはその薬学的に受容可能な塩、および薬学的に受容可能な希釈剤もしくは担体を含む医薬組成物。
- 1つ以上の他の治療成分をさらに含む、請求項7に記載の医薬組成物。
- シタグリプチンがさらなる治療成分である、請求項8に記載の医薬組成物。
- 請求項1〜6のいずれか一項に記載の化合物、またはその薬学的に受容可能な塩を含む、治療に使用するための医薬組成物。
- 請求項1〜6のいずれか一項に記載の化合物、またはその薬学的に受容可能な塩を含む、糖尿病または肥満の治療に使用するための医薬組成物。
- II型糖尿病の治療に使用するための請求項11に記載の医薬組成物。
Applications Claiming Priority (5)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
EP09382114.8 | 2009-07-15 | ||
EP09382114 | 2009-07-15 | ||
US24544509P | 2009-09-24 | 2009-09-24 | |
US61/245,445 | 2009-09-24 | ||
PCT/US2010/041645 WO2011008663A1 (en) | 2009-07-15 | 2010-07-12 | Gpr119 agonists |
Publications (3)
Publication Number | Publication Date |
---|---|
JP2012533546A JP2012533546A (ja) | 2012-12-27 |
JP2012533546A5 true JP2012533546A5 (ja) | 2013-08-08 |
JP5715127B2 JP5715127B2 (ja) | 2015-05-07 |
Family
ID=43449712
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP2012520691A Expired - Fee Related JP5715127B2 (ja) | 2009-07-15 | 2010-07-12 | Gpr119アゴニスト |
Country Status (24)
Country | Link |
---|---|
US (1) | US8207344B2 (ja) |
EP (1) | EP2454251A1 (ja) |
JP (1) | JP5715127B2 (ja) |
KR (1) | KR101365854B1 (ja) |
CN (1) | CN102471313B (ja) |
AR (1) | AR077638A1 (ja) |
AU (1) | AU2010273642B2 (ja) |
BR (1) | BRPI1015921A2 (ja) |
CA (1) | CA2764906C (ja) |
CO (1) | CO6480977A2 (ja) |
CR (1) | CR20120012A (ja) |
DO (1) | DOP2012000006A (ja) |
EA (1) | EA020540B1 (ja) |
EC (1) | ECSP12011606A (ja) |
IL (1) | IL216776A0 (ja) |
MA (1) | MA33428B1 (ja) |
MX (1) | MX2012000704A (ja) |
NZ (1) | NZ597125A (ja) |
PE (1) | PE20121045A1 (ja) |
SG (1) | SG177646A1 (ja) |
TN (1) | TN2012000002A1 (ja) |
TW (1) | TWI429634B (ja) |
WO (1) | WO2011008663A1 (ja) |
ZA (1) | ZA201200227B (ja) |
Families Citing this family (23)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US8293751B2 (en) | 2003-01-14 | 2012-10-23 | Arena Pharmaceuticals, Inc. | 1,2,3-trisubstituted aryl and heteroaryl derivatives as modulators of metabolism and the prophylaxis and treatment of disorders related thereto such as diabetes and hyperglycemia |
EP2108960A1 (en) | 2008-04-07 | 2009-10-14 | Arena Pharmaceuticals, Inc. | Methods of using A G protein-coupled receptor to identify peptide YY (PYY) secretagogues and compounds useful in the treatment of conditons modulated by PYY |
US20130109703A1 (en) | 2010-03-18 | 2013-05-02 | Boehringer Ingelheim International Gmbh | Combination of a GPR119 Agonist and the DPP-IV Inhibitor Linagliptin for Use in the Treatment of Diabetes and Related Conditions |
EP2619198A1 (en) | 2010-09-22 | 2013-07-31 | Arena Pharmaceuticals, Inc. | Modulators of the gpr119 receptor and the treatment of disorders related thereto |
US20140018371A1 (en) * | 2011-04-01 | 2014-01-16 | Arena Pharmaceuticals, Inc. | Modulators Of The GPR119 Receptor And The Treatment Of Disorders Related Thereto |
WO2012138845A1 (en) | 2011-04-08 | 2012-10-11 | Merck Sharp & Dohme Corp. | Substituted cyclopropyl compounds, compositions containing such compounds and methods of treatment |
WO2012170702A1 (en) * | 2011-06-08 | 2012-12-13 | Arena Pharmaceuticals, Inc. | Modulators of the gpr119 receptor and the treatment of disorders related thereto |
US9181214B2 (en) | 2011-06-09 | 2015-11-10 | Rhizen Pharmaceuticals Sa | Bicyclic compounds as modulators of GPR-119 |
US9006228B2 (en) | 2011-06-16 | 2015-04-14 | Merck Sharp & Dohme Corp. | Substituted cyclopropyl compounds, compositions containing such compounds, and methods of treatment |
EP2760855B1 (en) | 2011-09-30 | 2017-03-15 | Merck Sharp & Dohme Corp. | Substituted cyclopropyl compounds, compositions containing such compounds as well as their use in treating type-2 diabetes |
US9018200B2 (en) | 2011-10-24 | 2015-04-28 | Merck Sharp & Dohme Corp. | Substituted piperidinyl compounds useful as GPR119 agonists |
WO2013062835A1 (en) * | 2011-10-24 | 2013-05-02 | Merck Sharp & Dohme Corp. | Substituted piperidinyl compounds useful as gpr119 agonists |
EP2780337B1 (en) | 2011-11-15 | 2017-12-20 | Merck Sharp & Dohme Corp. | Substituted cyclopropyl compounds useful as gpr119 agonists |
US9944600B2 (en) * | 2012-06-12 | 2018-04-17 | Chong Kun Dang Pharmaceutical Corp. | Piperidine derivatives for GPR119 agonist |
CN104780915A (zh) | 2012-07-11 | 2015-07-15 | 埃尔舍利克斯治疗公司 | 包含他汀、双胍和用于减小心脏代谢风险的其它药剂的组合物 |
WO2014052619A1 (en) * | 2012-09-27 | 2014-04-03 | Irm Llc | Piperidine derivatives and compositions as modulators of gpr119 activity |
WO2015080446A1 (en) * | 2013-11-26 | 2015-06-04 | Chong Kun Dang Pharmaceutical Corp. | Amide derivatives for gpr119 agonist |
KR101651505B1 (ko) * | 2014-05-02 | 2016-08-29 | 현대약품 주식회사 | 싸이클로 헥센 유도체, 이의 제조방법 및 이를 유효성분으로 함유하는 대사성 질환의 예방 또는 치료용 약학적 조성물 |
AU2016205361C1 (en) | 2015-01-06 | 2021-04-08 | Arena Pharmaceuticals, Inc. | Methods of treating conditions related to the S1P1 receptor |
DK3310760T3 (da) | 2015-06-22 | 2022-10-24 | Arena Pharm Inc | Krystallinsk L-argininsalt af (R)-2-(7-(4-cyclopentyl-3-(trifluormethyl)benzyloxy)-1,2,3,4-tetrahydrocyclopenta[b]indol-3- yl)eddikesyre til anvendelse ved S1P1-receptor-associerede lidelser |
CA3053418A1 (en) | 2017-02-16 | 2018-08-23 | Arena Pharmaceuticals, Inc. | Compounds and methods for treatment of primary biliary cholangitis |
WO2021236617A1 (en) | 2020-05-19 | 2021-11-25 | Kallyope, Inc. | Ampk activators |
AU2021297323A1 (en) | 2020-06-26 | 2023-02-16 | Kallyope, Inc. | AMPK activators |
Family Cites Families (4)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US8293751B2 (en) * | 2003-01-14 | 2012-10-23 | Arena Pharmaceuticals, Inc. | 1,2,3-trisubstituted aryl and heteroaryl derivatives as modulators of metabolism and the prophylaxis and treatment of disorders related thereto such as diabetes and hyperglycemia |
WO2008025798A1 (en) * | 2006-08-30 | 2008-03-06 | Biovitrum Ab (Publ) | Pyridine compounds for treating gpr119 related disorders |
US7638541B2 (en) * | 2006-12-28 | 2009-12-29 | Metabolex Inc. | 5-ethyl-2-{4-[4-(4-tetrazol-1-yl-phenoxymethyl)-thiazol-2-yl]-piperidin-1-yl}-pyrimidine |
AU2008302570B2 (en) * | 2007-09-20 | 2012-05-31 | Irm Llc | Compounds and compositions as modulators of GPR119 activity |
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2010
- 2010-07-06 AR ARP100102424A patent/AR077638A1/es not_active Application Discontinuation
- 2010-07-08 TW TW099122534A patent/TWI429634B/zh not_active IP Right Cessation
- 2010-07-12 NZ NZ597125A patent/NZ597125A/xx not_active IP Right Cessation
- 2010-07-12 PE PE2012000041A patent/PE20121045A1/es not_active Application Discontinuation
- 2010-07-12 US US12/834,054 patent/US8207344B2/en not_active Expired - Fee Related
- 2010-07-12 MX MX2012000704A patent/MX2012000704A/es active IP Right Grant
- 2010-07-12 CA CA2764906A patent/CA2764906C/en not_active Expired - Fee Related
- 2010-07-12 CN CN201080031375.4A patent/CN102471313B/zh not_active Expired - Fee Related
- 2010-07-12 EA EA201270169A patent/EA020540B1/ru not_active IP Right Cessation
- 2010-07-12 SG SG2012002523A patent/SG177646A1/en unknown
- 2010-07-12 BR BRPI1015921A patent/BRPI1015921A2/pt not_active IP Right Cessation
- 2010-07-12 JP JP2012520691A patent/JP5715127B2/ja not_active Expired - Fee Related
- 2010-07-12 WO PCT/US2010/041645 patent/WO2011008663A1/en active Application Filing
- 2010-07-12 AU AU2010273642A patent/AU2010273642B2/en not_active Ceased
- 2010-07-12 MA MA34531A patent/MA33428B1/fr unknown
- 2010-07-12 KR KR1020127000996A patent/KR101365854B1/ko not_active IP Right Cessation
- 2010-07-12 EP EP10734412A patent/EP2454251A1/en not_active Withdrawn
-
2011
- 2011-12-05 IL IL216776A patent/IL216776A0/en unknown
- 2011-12-29 CO CO11181048A patent/CO6480977A2/es active IP Right Grant
-
2012
- 2012-01-02 TN TNP2012000002A patent/TN2012000002A1/en unknown
- 2012-01-09 CR CR20120012A patent/CR20120012A/es unknown
- 2012-01-11 DO DO2012000006A patent/DOP2012000006A/es unknown
- 2012-01-11 ZA ZA2012/00227A patent/ZA201200227B/en unknown
- 2012-01-13 EC EC2012011606A patent/ECSP12011606A/es unknown