AR083003A1 - Lactamas sustituidas por piperidinilo como moduladores de gpr119 - Google Patents
Lactamas sustituidas por piperidinilo como moduladores de gpr119Info
- Publication number
- AR083003A1 AR083003A1 ARP110103373A ARP110103373A AR083003A1 AR 083003 A1 AR083003 A1 AR 083003A1 AR P110103373 A ARP110103373 A AR P110103373A AR P110103373 A ARP110103373 A AR P110103373A AR 083003 A1 AR083003 A1 AR 083003A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- optionally substituted
- alkoxy
- halogen
- independently selected
- Prior art date
Links
Classifications
-
- 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
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
-
- 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/445—Non condensed piperidines, e.g. piperocaine
- A61K31/4468—Non condensed piperidines, e.g. piperocaine having a nitrogen directly attached in position 4, e.g. clebopride, fentanyl
-
- 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/445—Non condensed piperidines, e.g. piperocaine
- A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
- A61K31/454—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic 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
-
- 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
- A61P3/06—Antihyperlipidemics
-
- 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
- A61P9/00—Drugs for disorders of the cardiovascular system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/12—Antihypertensives
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
- C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D211/68—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member
- C07D211/72—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member with hetero atoms or with carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, directly attached to ring carbon atoms
- C07D211/74—Oxygen atoms
- C07D211/76—Oxygen atoms attached in position 2 or 6
-
- 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
- C07D401/04—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 directly linked by a ring-member-to-ring-member bond
-
- 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
- C07D401/14—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 three or more hetero rings
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Diabetes (AREA)
- Epidemiology (AREA)
- Obesity (AREA)
- Hematology (AREA)
- Biomedical Technology (AREA)
- Cardiology (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Heart & Thoracic Surgery (AREA)
- Psychiatry (AREA)
- Endocrinology (AREA)
- Emergency Medicine (AREA)
- Vascular Medicine (AREA)
- Child & Adolescent Psychology (AREA)
- Urology & Nephrology (AREA)
- Hospice & Palliative Care (AREA)
- Ophthalmology & Optometry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Hydrogenated Pyridines (AREA)
Abstract
Son moduladores de GPR119 y son útiles en el tratamiento o prevención de enfermedades tales como pero sin limitación a, diabetes tipo 2, complicaciones diabéticas, síntomas de diabetes, síndrome metabólico, obesidad, dislipidemia y afecciones relacionadas.Reivindicación 1: Un compuesto que tiene la fórmula general (1) o una sal farmacéuticamente aceptable del mismo, donde: L es O ó NRx; Rx es H o alquilo C1-3; X1 es N o CR1 y X2 es N o CR2, donde solo uno de X1 y X2 puede ser N; R1, R2, R3 y R4 se seleccionan independientemente de H, halógeno, CF3, alquilo C1-6 y alcoxi C1-6; R5 es (alquil C1-3)sulfonilo, (cicloalquil C3-6)sulfonilo, (ciclopropilmetil)sulfonilo, fenilsulfonilo, CN, Br, CF3 o tetrazolilo opcionalmente sustituido por alquilo C1-3; R7 se selecciona de los compuestos de fórmula (2) ó (3); R8 es alquilo C1-6, fluoroalquilo C1-6, difluoroalquilo C1-6, trifluoroalquilo C1-6, tricloroalquilo C1-6, Cyc1, Ar1, hetCyc1 o hetAr1; Cyc1 es cicloalquilo C3-6 opcionalmente sustituido por CF3; Ar1 es fenilo opcionalmente sustituido por uno o más grupos seleccionados independientemente de halógeno, CF3, alquilo C1-4 y alcoxi C1-4; hetCyc1 es un heterociclo de 5 - 6 miembros que tienen un átomo de nitrógeno en el anillo y que está opcionalmente sustituido por uno o más grupos seleccionados independientemente de halógeno, CF3, alquilo C1-4 y alcoxi C1-4; hetAr1 es un heteroarilo de 6 miembros que tiene un átomo de nitrógeno en el anillo y que está opcionalmente sustituido con uno o más grupos seleccionados independientemente de halógeno, CF3, alquilo C1-6 y alcoxi C1-4; y n es 1, 2 ó 3.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US38379910P | 2010-09-17 | 2010-09-17 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR083003A1 true AR083003A1 (es) | 2013-01-23 |
Family
ID=44736053
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP110103373A AR083003A1 (es) | 2010-09-17 | 2011-09-16 | Lactamas sustituidas por piperidinilo como moduladores de gpr119 |
Country Status (19)
| Country | Link |
|---|---|
| US (1) | US20130184257A1 (es) |
| EP (1) | EP2616074A1 (es) |
| JP (1) | JP2013537234A (es) |
| KR (1) | KR20130099970A (es) |
| CN (1) | CN103221046A (es) |
| AR (1) | AR083003A1 (es) |
| AU (1) | AU2011301934A1 (es) |
| BR (1) | BR112013006344A2 (es) |
| CA (1) | CA2811525A1 (es) |
| CL (1) | CL2013000714A1 (es) |
| CR (1) | CR20130173A (es) |
| IL (1) | IL225214A0 (es) |
| MX (1) | MX2013003034A (es) |
| PH (1) | PH12013500472A1 (es) |
| RU (1) | RU2013117403A (es) |
| SG (1) | SG188985A1 (es) |
| TW (1) | TW201213322A (es) |
| UY (1) | UY33614A (es) |
| WO (1) | WO2012037393A1 (es) |
Families Citing this family (25)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| SG185615A1 (en) | 2010-05-17 | 2012-12-28 | Array Biopharma Inc | Piperidinyl-substituted lactams as gpr119 modulators |
| AU2012267556B9 (en) | 2011-06-09 | 2017-05-11 | Rhizen Pharmaceuticals Sa | Novel compounds as modulators of GPR-119 |
| CN104039321B (zh) | 2011-11-18 | 2017-02-22 | 赫普泰雅治疗有限公司 | 药物化合物 |
| HK1210825A1 (en) | 2012-07-11 | 2016-05-06 | Elcelyx Therapeutics, Inc. | Compositions comprising statins, biguanides and further agents for reducing cardiometabolic risk |
| AR092924A1 (es) | 2012-10-09 | 2015-05-06 | Sanofi Sa | Derivados de pirrolidinona como moduladores de gpr119 para el tratamiento de diabetes, obesidad, dislipidemia y trastornos relacionados |
| GB201404922D0 (en) | 2014-03-19 | 2014-04-30 | Heptares Therapeutics Ltd | Pharmaceutical compounds |
| TW201625605A (zh) | 2014-04-04 | 2016-07-16 | 賽諾菲公司 | 用於治療糖尿病、肥胖、血脂異常及相關病症之作為ｇｐｒ１１９調節劑的經取代之稠合雜環類 |
| CN106132949A (zh) | 2014-04-04 | 2016-11-16 | 赛诺菲 | 作为治疗糖尿病、肥胖、血脂障碍及相关病症的gpr119调节剂的取代的茚满酮化合物 |
| AR099937A1 (es) | 2014-04-04 | 2016-08-31 | Sanofi Sa | Compuestos de isoindolinona como moduladores de gpr119 para el tratamiento de diabetes, obesidad, dislipidemia y trastornos relacionados |
| CN104672116B (zh) * | 2015-02-13 | 2016-06-01 | 佛山市赛维斯医药科技有限公司 | 一种含苯磺酰肼和腈基苯结构gpr119激动剂及其用途 |
| CN104610151A (zh) * | 2015-02-13 | 2015-05-13 | 佛山市赛维斯医药科技有限公司 | 含酰肼和烷氧苯类结构的化合物、其制备方法及用途 |
| CN104892517A (zh) * | 2015-02-13 | 2015-09-09 | 佛山市赛维斯医药科技有限公司 | 酰肼类化合物、其制备方法及用途 |
| UY36586A (es) | 2015-03-26 | 2016-10-31 | Bayer Pharma AG | Heterociclilmetiltienouracilos y uso de los mismos |
| GB201513743D0 (en) | 2015-08-03 | 2015-09-16 | Heptares Therapeutics Ltd | Muscarinic agonists |
| GB201519352D0 (en) | 2015-11-02 | 2015-12-16 | Heptares Therapeutics Ltd | Pharmaceutical compounds |
| GB201617454D0 (en) | 2016-10-14 | 2016-11-30 | Heptares Therapeutics Limited | Pharmaceutical compounds |
| AR110988A1 (es) | 2017-02-21 | 2019-05-22 | Sanofi Sa | Compuestos de azetidina como moduladores de gpr119 para el tratamiento de la diabetes, la obesidad, la dislipidemia y trastornos relacionados |
| GB201810245D0 (en) | 2018-06-22 | 2018-08-08 | Heptares Therapeutics Ltd | Pharmaceutical compounds |
| GB201810239D0 (en) | 2018-06-22 | 2018-08-08 | Heptares Therapeutics Ltd | Pharmaceutical compounds |
| GB201819960D0 (en) | 2018-12-07 | 2019-01-23 | Heptares Therapeutics Ltd | Pharmaceutical compounds |
| GB201819961D0 (en) | 2018-12-07 | 2019-01-23 | Heptares Therapeutics Ltd | Pharmaceutical compounds |
| GB202020191D0 (en) | 2020-12-18 | 2021-02-03 | Heptares Therapeutics Ltd | Pharmaceutical compounds |
| CA3173731A1 (en) | 2020-02-28 | 2021-09-02 | Kallyope, Inc. | Gpr40 agonists |
| CN116323608A (zh) | 2020-05-19 | 2023-06-23 | 卡尔优普公司 | Ampk活化剂 |
| EP4172162A4 (en) | 2020-06-26 | 2024-08-07 | Kallyope, Inc. | AMPK ACTIVATORS |
Family Cites Families (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5543523A (en) | 1994-11-15 | 1996-08-06 | Regents Of The University Of Minnesota | Method and intermediates for the synthesis of korupensamines |
| CA2661371A1 (en) * | 2006-08-30 | 2008-03-06 | Biovitrum Ab (Publ) | Pyrimidine compounds for treating gpr119 related disorders |
| ES2387865T3 (es) * | 2008-07-10 | 2012-10-03 | Prosidion Ltd | Agonistas de GPCR de piperidina |
-
2011
- 2011-09-15 BR BR112013006344A patent/BR112013006344A2/pt not_active Application Discontinuation
- 2011-09-15 CA CA2811525A patent/CA2811525A1/en not_active Abandoned
- 2011-09-15 US US13/823,041 patent/US20130184257A1/en not_active Abandoned
- 2011-09-15 CN CN2011800554986A patent/CN103221046A/zh active Pending
- 2011-09-15 EP EP11764392.4A patent/EP2616074A1/en not_active Withdrawn
- 2011-09-15 WO PCT/US2011/051821 patent/WO2012037393A1/en not_active Ceased
- 2011-09-15 JP JP2013529341A patent/JP2013537234A/ja not_active Withdrawn
- 2011-09-15 KR KR1020137009752A patent/KR20130099970A/ko not_active Withdrawn
- 2011-09-15 MX MX2013003034A patent/MX2013003034A/es not_active Application Discontinuation
- 2011-09-15 SG SG2013018551A patent/SG188985A1/en unknown
- 2011-09-15 AU AU2011301934A patent/AU2011301934A1/en not_active Abandoned
- 2011-09-15 PH PH1/2013/500472A patent/PH12013500472A1/en unknown
- 2011-09-15 RU RU2013117403/04A patent/RU2013117403A/ru not_active Application Discontinuation
- 2011-09-16 UY UY0001033614A patent/UY33614A/es not_active Application Discontinuation
- 2011-09-16 TW TW100133495A patent/TW201213322A/zh unknown
- 2011-09-16 AR ARP110103373A patent/AR083003A1/es not_active Application Discontinuation
-
2013
- 2013-03-14 IL IL225214A patent/IL225214A0/en unknown
- 2013-03-15 CL CL2013000714A patent/CL2013000714A1/es unknown
- 2013-04-17 CR CR20130173A patent/CR20130173A/es unknown
Also Published As
| Publication number | Publication date |
|---|---|
| US20130184257A1 (en) | 2013-07-18 |
| CN103221046A (zh) | 2013-07-24 |
| EP2616074A1 (en) | 2013-07-24 |
| TW201213322A (en) | 2012-04-01 |
| BR112013006344A2 (pt) | 2016-06-21 |
| AU2011301934A1 (en) | 2013-05-16 |
| RU2013117403A (ru) | 2014-10-27 |
| IL225214A0 (en) | 2013-06-27 |
| WO2012037393A1 (en) | 2012-03-22 |
| JP2013537234A (ja) | 2013-09-30 |
| KR20130099970A (ko) | 2013-09-06 |
| CL2013000714A1 (es) | 2013-10-11 |
| MX2013003034A (es) | 2013-08-15 |
| SG188985A1 (en) | 2013-05-31 |
| UY33614A (es) | 2013-04-05 |
| CA2811525A1 (en) | 2012-03-22 |
| CR20130173A (es) | 2013-05-15 |
| PH12013500472A1 (en) | 2013-04-29 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FA | Abandonment or withdrawal |