MX2016010771A - Compuestos que se une al receptor gamma activado por el proliferador de peroxisoma (pparg) pero que no actua como promotor y composicion farmaceutica para tratar enfermedades relacionadas con pparg que contienen el mismo como ingrediente activo. - Google Patents
Compuestos que se une al receptor gamma activado por el proliferador de peroxisoma (pparg) pero que no actua como promotor y composicion farmaceutica para tratar enfermedades relacionadas con pparg que contienen el mismo como ingrediente activo.Info
- Publication number
- MX2016010771A MX2016010771A MX2016010771A MX2016010771A MX2016010771A MX 2016010771 A MX2016010771 A MX 2016010771A MX 2016010771 A MX2016010771 A MX 2016010771A MX 2016010771 A MX2016010771 A MX 2016010771A MX 2016010771 A MX2016010771 A MX 2016010771A
- Authority
- MX
- Mexico
- Prior art keywords
- pparg
- related diseases
- pharmaceutical composition
- treating
- active ingredient
- Prior art date
Links
- 201000010099 disease Diseases 0.000 title abstract 4
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 title abstract 4
- 150000001875 compounds Chemical class 0.000 title abstract 3
- 239000008194 pharmaceutical composition Substances 0.000 title abstract 3
- 239000004480 active ingredient Substances 0.000 title abstract 2
- 101150023417 PPARG gene Proteins 0.000 title 2
- 101000741790 Homo sapiens Peroxisome proliferator-activated receptor gamma Proteins 0.000 abstract 6
- 102100038825 Peroxisome proliferator-activated receptor gamma Human genes 0.000 abstract 6
- 102000013717 Cyclin-Dependent Kinase 5 Human genes 0.000 abstract 2
- 108010025454 Cyclin-Dependent Kinase 5 Proteins 0.000 abstract 2
- 230000026731 phosphorylation Effects 0.000 abstract 2
- 238000006366 phosphorylation reaction Methods 0.000 abstract 2
- 239000000556 agonist Substances 0.000 abstract 1
- 230000003178 anti-diabetic effect Effects 0.000 abstract 1
- 239000003814 drug Substances 0.000 abstract 1
- 229940079593 drug Drugs 0.000 abstract 1
- 230000000694 effects Effects 0.000 abstract 1
- 230000001939 inductive effect Effects 0.000 abstract 1
- 230000002401 inhibitory effect Effects 0.000 abstract 1
- 230000001404 mediated effect Effects 0.000 abstract 1
- 231100000957 no side effect Toxicity 0.000 abstract 1
- 230000003287 optical effect Effects 0.000 abstract 1
- 230000000144 pharmacologic effect Effects 0.000 abstract 1
- 108090000623 proteins and genes Proteins 0.000 abstract 1
- 239000000126 substance Substances 0.000 abstract 1
- 230000035897 transcription Effects 0.000 abstract 1
- 238000013518 transcription Methods 0.000 abstract 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
- C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
- C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D215/48—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
-
- 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
- A61P3/04—Anorexiants; Antiobesity agents
-
- 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
-
- 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
- A61P5/00—Drugs for disorders of the endocrine system
- A61P5/48—Drugs for disorders of the endocrine system of the pancreatic hormones
- A61P5/50—Drugs for disorders of the endocrine system of the pancreatic hormones for increasing or potentiating the activity of insulin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
- A61P7/10—Antioedematous agents; Diuretics
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D265/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom and one oxygen atom as the only ring hetero atoms
- C07D265/28—1,4-Oxazines; Hydrogenated 1,4-oxazines
- C07D265/34—1,4-Oxazines; Hydrogenated 1,4-oxazines condensed with carbocyclic rings
- C07D265/36—1,4-Oxazines; Hydrogenated 1,4-oxazines condensed with carbocyclic rings condensed with one six-membered ring
-
- 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
- C07D401/02—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 two hetero rings
- C07D401/12—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 two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
- C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Diabetes (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Engineering & Computer Science (AREA)
- Public Health (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Endocrinology (AREA)
- Physical Education & Sports Medicine (AREA)
- Emergency Medicine (AREA)
- Rheumatology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Child & Adolescent Psychology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Hydrogenated Pyridines (AREA)
- Quinoline Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
La presente invención se refiere a un compuesto que inhibe la fosforilación de PPARG mediada por CDK5 y una composición farmacéutica para tratar enfermedades relacionadas con PPARG que contienen el mismo como un ingrediente activo. Un compuesto representado por la fórmula 1 o un isómero óptico del mismo de conformidad con la presente invención se une a PPARG a un nivel de alta afinidad, pero no actúa como un agonista, de este modo no induciendo transcripción del gen; bloquea a CDK5, la cual es una causa de fosforilación de PPARG, de este modo no causando efectos secundarios de anti-diabéticos existentes; puede ser formulado en fármacos debido a las propiedades farmacológicas mejoradas del mismo; y puede ser usado favorablemente como una composición farmacéutica para tratar enfermedades relacionadas con PPARG debido a un excelente efecto de tratamiento en enfermedades relacionadas con PPARG.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| KR1020140033041A KR101585605B1 (ko) | 2014-03-20 | 2014-03-20 | Pparg에 결합하되 증진제로 작용하지 않는 화합물 및 이를 유효성분으로 함유하는 pparg 관련 질병의 치료용 약학적 조성물 |
| PCT/KR2015/001941 WO2015141958A1 (ko) | 2014-03-20 | 2015-02-27 | Pparg에 결합하되 증진제로 작용하지 않는 화합물 및 이를 유효성분으로 함유하는 pparg 관련 질병의 치료용 약학적 조성물 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| MX2016010771A true MX2016010771A (es) | 2016-11-08 |
Family
ID=54144878
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| MX2016010771A MX2016010771A (es) | 2014-03-20 | 2015-02-27 | Compuestos que se une al receptor gamma activado por el proliferador de peroxisoma (pparg) pero que no actua como promotor y composicion farmaceutica para tratar enfermedades relacionadas con pparg que contienen el mismo como ingrediente activo. |
Country Status (9)
| Country | Link |
|---|---|
| US (1) | US20160355483A1 (es) |
| EP (1) | EP3121167A4 (es) |
| JP (1) | JP2017506654A (es) |
| KR (1) | KR101585605B1 (es) |
| CN (1) | CN106061953A (es) |
| AU (1) | AU2015232269A1 (es) |
| CA (1) | CA2938762A1 (es) |
| MX (1) | MX2016010771A (es) |
| WO (1) | WO2015141958A1 (es) |
Families Citing this family (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2018030550A1 (en) | 2016-08-09 | 2018-02-15 | Takeda Pharmaceutical Company Limited | Heterocyclic compounds with an ror(gamma)t modulating activity |
| KR101934197B1 (ko) * | 2017-06-12 | 2018-12-31 | 아주대학교산학협력단 | PPARα/γ 이중 작용 활성을 갖는 신규 화합물 및 이를 유효성분으로 함유하는 대사질환 예방 또는 치료용 조성물 |
Family Cites Families (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB9919411D0 (en) * | 1999-08-18 | 1999-10-20 | Zeneca Ltd | Chemical compounds |
| AU2003296960A1 (en) * | 2002-12-11 | 2004-06-30 | Smithkline Beecham Corporation | Peptide deformylase inhibitors |
| US7129264B2 (en) * | 2003-04-16 | 2006-10-31 | Bristol-Myers Squibb Company | Biarylmethyl indolines and indoles as antithromboembolic agents |
| SG165362A1 (en) * | 2005-09-07 | 2010-10-28 | Plexxikon Inc | Ppar active compounds |
| ZA200806983B (en) * | 2006-02-20 | 2009-11-25 | Astellas Pharma Inc | Amide derivative or salt thereof |
| KR20090118958A (ko) * | 2007-03-08 | 2009-11-18 | 플렉시콘, 인코퍼레이티드 | Ｐｐａｒ 활성 화합물 |
| RU2479576C9 (ru) * | 2008-05-14 | 2014-03-10 | Астеллас Фарма Инк. | Амидное соединение |
| WO2012170554A1 (en) * | 2011-06-06 | 2012-12-13 | Theodore Mark Kamenecka | N-biphenylmethylindole modulators of pparg |
-
2014
- 2014-03-20 KR KR1020140033041A patent/KR101585605B1/ko not_active Expired - Fee Related
-
2015
- 2015-02-27 CA CA2938762A patent/CA2938762A1/en not_active Abandoned
- 2015-02-27 WO PCT/KR2015/001941 patent/WO2015141958A1/ko not_active Ceased
- 2015-02-27 AU AU2015232269A patent/AU2015232269A1/en not_active Abandoned
- 2015-02-27 JP JP2016554276A patent/JP2017506654A/ja active Pending
- 2015-02-27 MX MX2016010771A patent/MX2016010771A/es unknown
- 2015-02-27 CN CN201580011038.1A patent/CN106061953A/zh active Pending
- 2015-02-27 EP EP15764627.4A patent/EP3121167A4/en not_active Withdrawn
-
2016
- 2016-08-23 US US15/244,821 patent/US20160355483A1/en not_active Abandoned
Also Published As
| Publication number | Publication date |
|---|---|
| KR101585605B1 (ko) | 2016-01-21 |
| AU2015232269A1 (en) | 2016-08-25 |
| EP3121167A1 (en) | 2017-01-25 |
| WO2015141958A1 (ko) | 2015-09-24 |
| JP2017506654A (ja) | 2017-03-09 |
| EP3121167A4 (en) | 2017-09-27 |
| CN106061953A (zh) | 2016-10-26 |
| KR20150110901A (ko) | 2015-10-05 |
| CA2938762A1 (en) | 2015-09-24 |
| US20160355483A1 (en) | 2016-12-08 |
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