AR078542A1 - Moduladores de gpr40 de pirrolidina - Google Patents
Moduladores de gpr40 de pirrolidinaInfo
- Publication number
- AR078542A1 AR078542A1 ARP100103635A ARP100103635A AR078542A1 AR 078542 A1 AR078542 A1 AR 078542A1 AR P100103635 A ARP100103635 A AR P100103635A AR P100103635 A ARP100103635 A AR P100103635A AR 078542 A1 AR078542 A1 AR 078542A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- group
- occurrence
- substituted
- halo
- Prior art date
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D207/04—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
- C07D207/06—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with radicals, containing only hydrogen and carbon atoms, attached to ring carbon atoms
-
- 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
- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
-
- 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
- C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D207/04—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
- C07D207/08—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon radicals, substituted by hetero atoms, attached to ring carbon atoms
Abstract
Estos compuestos son moduladores de receptor acoplados a proteínas G GPR40 que se pueden usar como medicamentos. Composiciones farmacéuticas. Reivindicacion 1: Un compuesto caracterizado porque tiene la formula (1), o un estereoisomero, un tautomero, o una sal farmacéuticamente aceptable del mismo, en el que: X se selecciona entre el grupo constituido por: O, S, CH2, CH(alquilo C1-4), CH(alquilo C1-4)2, CH(alcoxi C1-4-fenilo) y C(O); el anillo A es fenilo sustituido con 0 - 2 R5, piridinilo sustituido con 0 - 2 R5 o pirimidilo sustituido con 0 - 2 R5; R1 es -(CH2)n-fenilo sustituido con 0 - 3 R2, -(CH2)n-naftilo sustituido con 0 - 3 R2 o -(CH2)n-heteroarilo de 5 a 6 miembros que contiene átomos de carbono y 1 - 4 heteroátomos seleccionados del grupo constituido por N, O y S(O)p; en el que dicho heteroarilo está sustituido con 0 - 3 R2; R2, en cada aparicion, se selecciona independientemente del grupo constituido por: halo, CF3, CN, NO2, OCF3, SCF3, alquilo C1-6, alcoxi C1-6, alquiltio C1-6, NH2, NH(alquilo C1-4), N(alquilo C1-4)2, -(CH2)n-carbociclo C3-10, -(CH2)n-O-carbociclo C3-10 y-(CH2)n-heterociclo de 3 a 10 miembros que contiene átomos de carbono y 1 - 4 heteroátomos seleccionados del grupo constituido por N, O y S(O)p; en el que dichos carbociclo y heterociclo están sustituidos con 0 - 3 R6; R3 y R4, en cada aparicion, se seleccionan independientemente del grupo constituido por: H, OH, halo, CF3, alquilo C1-4 y alcoxi C1-4; R5, en cada aparicion, se selecciona independientemente del grupo constituido por: halo y alquilo C1-4; R6, en cada aparicion, se selecciona independientemente del grupo constituido por: halo, CF3, alquilo C1-4 y alcoxi C1-4; n, en cada aparicion, es independientemente 0, 1, 2 o 3; y p, en cada aparicion, es independientemente 0, 1 o 2.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US24889609P | 2009-10-06 | 2009-10-06 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR078542A1 true AR078542A1 (es) | 2011-11-16 |
Family
ID=43242297
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP100103635A AR078542A1 (es) | 2009-10-06 | 2010-10-06 | Moduladores de gpr40 de pirrolidina |
Country Status (13)
| Country | Link |
|---|---|
| US (1) | US8288404B2 (es) |
| EP (1) | EP2486005B1 (es) |
| JP (1) | JP2013506714A (es) |
| KR (1) | KR20120104534A (es) |
| CN (1) | CN102639495A (es) |
| AR (1) | AR078542A1 (es) |
| AU (1) | AU2010303670A1 (es) |
| BR (1) | BR112012007979A2 (es) |
| CA (1) | CA2777041A1 (es) |
| MX (1) | MX2012003389A (es) |
| RU (1) | RU2012118504A (es) |
| TW (1) | TW201116510A (es) |
| WO (1) | WO2011044073A1 (es) |
Families Citing this family (24)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103402986A (zh) * | 2010-11-24 | 2013-11-20 | 阿勒根公司 | S1p受体的调节剂 |
| 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 |
| KR101942752B1 (ko) * | 2012-11-05 | 2019-01-28 | 주식회사 엘지화학 | Ｇｐｒ120 효능제로서의 티오아릴 유도체 |
| CA2891551A1 (en) | 2012-11-16 | 2014-05-22 | Bristol-Myers Squibb Company | Dihydropyrazole gpr40 modulators |
| SG11201503559TA (en) * | 2012-11-16 | 2015-06-29 | Bristol Myers Squibb Co | Pyrrolidine gpr40 modulators |
| SI2920165T1 (sl) * | 2012-11-16 | 2017-02-28 | Bristol-Myers Squibb Company | Modulatorji dihidropirazola GPR40 |
| BR112015010791A2 (pt) * | 2012-11-16 | 2017-07-11 | Bristol Myers Squibb Co | moduladores de gpr40 de di-hidropirazol |
| US8962660B2 (en) | 2013-03-14 | 2015-02-24 | Bristol-Myers Squibb Company | Oxabicyclo [2.2.2] acid GPR120 modulators |
| CA2914132A1 (en) | 2013-06-21 | 2014-12-24 | Lupin Limited | Substituted heterocyclic compounds as crac modulators |
| EP3013810A1 (en) | 2013-06-24 | 2016-05-04 | Lupin Limited | Chromane and chromene derivatives and their use as crac modulators |
| AU2014372114A1 (en) | 2013-11-14 | 2016-06-09 | Cadila Healthcare Limited | Novel heterocyclic compounds |
| CN105814035B (zh) | 2013-12-13 | 2018-02-02 | 豪夫迈·罗氏有限公司 | 布鲁顿氏酪氨酸激酶抑制剂 |
| EP3140294A1 (en) * | 2014-05-07 | 2017-03-15 | Bristol-Myers Squibb Company | Pyrrolidine gpr40 modulators |
| SG11201609167RA (en) * | 2014-05-07 | 2016-12-29 | Bristol Myers Squibb Co | Pyrrolidine gpr40 modulators for the treatment of diseases such as diabetes |
| RS57170B1 (sr) | 2014-05-07 | 2018-07-31 | Bristol Myers Squibb Co | Pirolidinski gpr40 modulatori za lečenje bolesti kao što je dijabetes |
| WO2018095344A1 (en) * | 2016-11-24 | 2018-05-31 | Shanghai Meton Pharmaceutical Co., Ltd | Isocitrate dehydrogenase (idh) inhibitor |
| TWI796596B (zh) | 2018-02-13 | 2023-03-21 | 美商基利科學股份有限公司 | Pd‐1/pd‐l1抑制劑 |
| IL277071B1 (en) | 2018-03-08 | 2024-03-01 | Incyte Corp | Aminopyrizine diol compounds as PI3K–y inhibitors |
| CA3093130C (en) | 2018-04-19 | 2023-10-17 | Gilead Sciences, Inc. | Pd-1/pd-l1 inhibitors |
| US11046658B2 (en) | 2018-07-02 | 2021-06-29 | Incyte Corporation | Aminopyrazine derivatives as PI3K-γ inhibitors |
| KR20230159715A (ko) | 2018-07-13 | 2023-11-21 | 길리애드 사이언시즈, 인코포레이티드 | Pd-1/pd-l1 억제제 |
| KR102635333B1 (ko) | 2018-10-24 | 2024-02-15 | 길리애드 사이언시즈, 인코포레이티드 | Pd-1/pd-l1 억제제 |
| CN110041269A (zh) * | 2019-05-16 | 2019-07-23 | 海门瑞一医药科技有限公司 | 一种2-氯-5-羟基嘧啶的制备方法 |
| CN111253223A (zh) * | 2020-03-20 | 2020-06-09 | 重庆医科大学 | 一类大位阻三芳基甲烷衍生物及其合成方法 |
Family Cites Families (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| PL374860A1 (en) * | 2002-07-09 | 2005-11-14 | Bristol-Myers Squibb Company | Substituted heterocyclic derivatives useful as antidiabetic and antiobesity agents and method |
| DE10309929B4 (de) * | 2003-03-07 | 2006-02-23 | Sanofi-Aventis Deutschland Gmbh | Substituierte Benzoylureidopyridyl-piperidin- und -pyrrolidin-carbonsäurederivate, Verfahren zu deren Herstellung und deren Verwendung |
| US7501440B2 (en) * | 2003-03-07 | 2009-03-10 | Sanofi-Aventis Deutschland Gmbh | Substituted benzoylureidopyridylpiperidine-and-pyrrolidinecarboxylic acid derivatives, processes for preparing them and their use |
| US7714008B2 (en) * | 2006-09-07 | 2010-05-11 | Amgen Inc. | Heterocyclic GPR40 modulators |
-
2010
- 2010-10-05 BR BR112012007979A patent/BR112012007979A2/pt not_active Application Discontinuation
- 2010-10-05 CN CN2010800552581A patent/CN102639495A/zh active Pending
- 2010-10-05 AU AU2010303670A patent/AU2010303670A1/en not_active Abandoned
- 2010-10-05 RU RU2012118504/04A patent/RU2012118504A/ru unknown
- 2010-10-05 WO PCT/US2010/051389 patent/WO2011044073A1/en active Application Filing
- 2010-10-05 US US12/897,913 patent/US8288404B2/en active Active
- 2010-10-05 KR KR1020127011617A patent/KR20120104534A/ko not_active Application Discontinuation
- 2010-10-05 EP EP10763955.1A patent/EP2486005B1/en not_active Not-in-force
- 2010-10-05 MX MX2012003389A patent/MX2012003389A/es not_active Application Discontinuation
- 2010-10-05 CA CA2777041A patent/CA2777041A1/en not_active Abandoned
- 2010-10-05 JP JP2012533240A patent/JP2013506714A/ja active Pending
- 2010-10-06 AR ARP100103635A patent/AR078542A1/es not_active Application Discontinuation
- 2010-10-06 TW TW099134095A patent/TW201116510A/zh unknown
Also Published As
| Publication number | Publication date |
|---|---|
| KR20120104534A (ko) | 2012-09-21 |
| WO2011044073A1 (en) | 2011-04-14 |
| TW201116510A (en) | 2011-05-16 |
| US20110082165A1 (en) | 2011-04-07 |
| BR112012007979A2 (pt) | 2016-03-29 |
| JP2013506714A (ja) | 2013-02-28 |
| US8288404B2 (en) | 2012-10-16 |
| CN102639495A (zh) | 2012-08-15 |
| AU2010303670A1 (en) | 2012-03-29 |
| EP2486005A1 (en) | 2012-08-15 |
| CA2777041A1 (en) | 2011-04-14 |
| MX2012003389A (es) | 2012-04-10 |
| RU2012118504A (ru) | 2013-11-20 |
| EP2486005B1 (en) | 2014-06-18 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FA | Abandonment or withdrawal |