AR051842A1 - Derivados de oxadiazol como inhibidores de dgat - Google Patents
Derivados de oxadiazol como inhibidores de dgatInfo
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- AR051842A1 AR051842A1 ARP050105216A ARP050105216A AR051842A1 AR 051842 A1 AR051842 A1 AR 051842A1 AR P050105216 A ARP050105216 A AR P050105216A AR P050105216 A ARP050105216 A AR P050105216A AR 051842 A1 AR051842 A1 AR 051842A1
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D271/00—Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms
- C07D271/02—Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms not condensed with other rings
- C07D271/10—1,3,4-Oxadiazoles; Hydrogenated 1,3,4-oxadiazoles
- C07D271/113—1,3,4-Oxadiazoles; Hydrogenated 1,3,4-oxadiazoles with oxygen, sulfur or nitrogen atoms, directly attached to ring carbon atoms, the nitrogen atoms not forming part of a nitro radical
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- 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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/4245—Oxadiazoles
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
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- A—HUMAN NECESSITIES
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- A61P13/00—Drugs for disorders of the urinary system
- A61P13/12—Drugs for disorders of the urinary system of the kidneys
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- A61P15/08—Drugs for genital or sexual disorders; Contraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/06—Antipsoriatics
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- 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
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
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- 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
- A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P21/00—Drugs for disorders of the muscular or neuromuscular system
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- 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
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- 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
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- 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
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- 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
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- 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
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- 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
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- 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
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- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
- A61P31/14—Antivirals for RNA viruses
- A61P31/18—Antivirals for RNA viruses for HIV
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- 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
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- 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
- A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
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- 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
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- 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
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- Orthopedic Medicine & Surgery (AREA)
- Obesity (AREA)
- Hematology (AREA)
- Biomedical Technology (AREA)
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- Rheumatology (AREA)
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- Heart & Thoracic Surgery (AREA)
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- Dermatology (AREA)
- Urology & Nephrology (AREA)
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Abstract
La presente se refiere a derivados de oxadiasol como inhibidores de DGAT. También se describen procesos para preparar tales compuestos y su uso como inhibidores de DGAT, por ejemplo en el tratamiento de la obesidad. Reivindicacion 1: Un compuesto de formula (1) o su sal aceptable para uso farmacéutico o su profármaco, donde: R1 es un arilo opcionalmente sustituido o un grupo heteroarilo opcionalmente sustituido, donde lo sustituyentes opcionales son uno o más grupos seleccionados de un grupo -Za, un grupo -X2-(CR52R53)w-Za, un grupo -X2-(CR52R53)a-X3-Za, un grupo -(CR52R53)aX3-Za o un grupo funcional (el cual es diferente de un grupo -X2-(CR52R53)w-Za o de un grupo -X2-(CR52R53)a-X3-Za); Y e un enlace directo, o un grupo (CR40R41)s o - X6(CR40R41)t- donde cada R40 y R41 se seleccionan independientemente de H, alquilo C1-4, hidroxi, halo, haloalquilo C1-4, amino, ciano, alcoxi C1-4, haloalcoxi C1-4 o (alquilo C1-3)CONH-; s es un numero entero de 1 a 6 y t es un numero entero de 1 a 6, con la condicion de que el átomo X6 del grupo -X6(CR40R41)t- esté unido al grupo R2 y que un unico C hibridado sp3 no sea portador de dos o más enlaces a un heteroátomo a menos que el heteroátomo sea un halo; R2 es un arilo opcionalmente sustituido, un cicloalquilo opcionalmente sustituido o un grupo heterocíclico opcionalmente sustituido, donde los sustituyentes opcionales son uno o más grupos seleccionados de un grupo -Z, un grupo -X-(CR42R43)u-Z, un grupo -X-(CR42R43)v-X1-Z o un grupo -(CR42R43)vX1-Z o un grupo funcional (el cual es diferente de un grupo -X-(CR42R43)u-Z o un grupo -X-(CR42R43)v-X1-Z); donde Z y Za se seleccionan independientemente de un grupo hidrocarbilo o un grupo heterocíclico o su combinacion, donde el grupo Z y Za está opcionalmente sustituido en cualquier átomo disponible con uno o más grupos funcionales, o con un grupo -X7-(CR62R63)bR64; X, X1, X2, X3, X6 y X7 son grupos conectores seleccionados independientemente de -C(O)x-, -O-, -S(O)y-, - NR44, -C(O)R44-, -OC(O)NR44-, -CH=NO-, -NR44C(O)x-, -NR44CONR45-, -S(O)2NR44- o -NR44S(O)2-, donde x es un numero entero de 1 o 2, y es 0, 1 o 2, y R44 y R45 se seleccionan independientemente de H o alquilo C1-6, u y w se seleccionan independientemente de 0 o un numero entero de 1 a 6; v, a y b se seleccionan independientemente de un numero entero de 1 a 6; cada R42, R43, R52, R53, R62 y R63 se selecciona independientemente de H, alquilo C1-4, hidroxi, halo, haloalquilo C1-4, amino, ciano, alcoxi C1-4, haloalcoxi C1-4, alquilo (C1-3)CONH-, carboxi o un mimético de ácido carboxílico o bioisostero del mismo, y R64 es un grupo funcional.
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
GB0427328A GB0427328D0 (en) | 2004-12-14 | 2004-12-14 | Chemical compounds |
GB0507403A GB0507403D0 (en) | 2005-04-13 | 2005-04-13 | Chemical compounds |
GB0520383A GB0520383D0 (en) | 2005-10-07 | 2005-10-07 | Chemical compounds |
Publications (1)
Publication Number | Publication Date |
---|---|
AR051842A1 true AR051842A1 (es) | 2007-02-14 |
Family
ID=35999598
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
ARP050105216A AR051842A1 (es) | 2004-12-14 | 2005-12-13 | Derivados de oxadiazol como inhibidores de dgat |
Country Status (15)
Country | Link |
---|---|
US (2) | US7795283B2 (es) |
EP (1) | EP1833806A1 (es) |
JP (1) | JP2008523133A (es) |
KR (1) | KR20070087096A (es) |
AR (1) | AR051842A1 (es) |
AU (2) | AU2005315430B2 (es) |
BR (1) | BRPI0519058A2 (es) |
CA (1) | CA2588162A1 (es) |
IL (1) | IL183279A0 (es) |
MX (1) | MX2007007101A (es) |
NO (1) | NO20072632L (es) |
NZ (2) | NZ555683A (es) |
SA (1) | SA05260407B1 (es) |
TW (1) | TW200633991A (es) |
WO (1) | WO2006064189A1 (es) |
Families Citing this family (62)
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BRPI0610850A2 (pt) * | 2005-04-19 | 2008-12-02 | Bayer Pharmaceuticals Corp | derivados de Ácido aril alquila, composiÇço farmacÊutica, medicamento, bem como uso dos referidos derivados |
AR058562A1 (es) | 2005-12-22 | 2008-02-13 | Astrazeneca Ab | Derivados de pirimido [4,5 b] (1,4) oxazinas , procedimientos de obtencion y su uso como inhibidores de acetil coa y dgat 1 |
CA2651663A1 (en) * | 2006-05-30 | 2007-12-06 | Astrazeneca Ab | Chemical compounds |
US8084478B2 (en) * | 2006-05-30 | 2011-12-27 | Asstrazeneca Ab | Substituted 5- phenylamino- 1, 3, 4-oxadiazol-2-ylcarbonylamino-4-phenoxy-cyclohexane carboxylic acid as inhibitors of acetyl coenzyme A diacylglycerol acyltransferase |
US20090209602A1 (en) * | 2006-06-06 | 2009-08-20 | Roger John Butlin | Chemical compounds |
CN101460492A (zh) * | 2006-06-08 | 2009-06-17 | 阿斯利康(瑞典)有限公司 | 苯并咪唑及其治疗糖尿病的用途 |
GB0611507D0 (en) * | 2006-06-10 | 2006-07-19 | Astrazeneca Ab | Chemical compounds |
GB0611552D0 (en) * | 2006-06-12 | 2006-07-19 | Astrazeneca Ab | Chemical compounds |
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US8828995B2 (en) | 2011-03-08 | 2014-09-09 | Sanofi | Branched oxathiazine derivatives, method for the production thereof, use thereof as medicine and drug containing said derivatives and use thereof |
US8901114B2 (en) | 2011-03-08 | 2014-12-02 | Sanofi | Oxathiazine derivatives substituted with carbocycles or heterocycles, method for producing same, drugs containing said compounds, and use thereof |
EP2683698B1 (de) | 2011-03-08 | 2017-10-04 | Sanofi | Mit adamantan- oder noradamantan substituierte benzyl-oxathiazinderivate, diese verbindungen enthaltende arzneimittel und deren verwendung |
WO2012120050A1 (de) | 2011-03-08 | 2012-09-13 | Sanofi | Neue substituierte phenyl-oxathiazinderivate, verfahren zu deren herstellung, diese verbindungen enthaltende arzneimittel und deren verwendung |
EP2683700B1 (de) | 2011-03-08 | 2015-02-18 | Sanofi | Tetrasubstituierte oxathiazinderivate, verfahren zu deren herstellung, ihre verwendung als medikament sowie sie enthaltendes arzneimittel und deren verwendung |
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2005
- 2005-12-09 MX MX2007007101A patent/MX2007007101A/es active IP Right Grant
- 2005-12-09 AU AU2005315430A patent/AU2005315430B2/en not_active Ceased
- 2005-12-09 BR BRPI0519058-4A patent/BRPI0519058A2/pt not_active IP Right Cessation
- 2005-12-09 WO PCT/GB2005/004726 patent/WO2006064189A1/en active Application Filing
- 2005-12-09 NZ NZ555683A patent/NZ555683A/en not_active IP Right Cessation
- 2005-12-09 NZ NZ587106A patent/NZ587106A/en not_active IP Right Cessation
- 2005-12-09 KR KR1020077016200A patent/KR20070087096A/ko not_active Application Discontinuation
- 2005-12-09 JP JP2007546161A patent/JP2008523133A/ja not_active Withdrawn
- 2005-12-09 EP EP05818139A patent/EP1833806A1/en not_active Withdrawn
- 2005-12-09 CA CA002588162A patent/CA2588162A1/en not_active Abandoned
- 2005-12-09 US US11/792,922 patent/US7795283B2/en not_active Expired - Fee Related
- 2005-12-13 AR ARP050105216A patent/AR051842A1/es not_active Application Discontinuation
- 2005-12-14 TW TW094144264A patent/TW200633991A/zh unknown
- 2005-12-14 SA SA5260407A patent/SA05260407B1/ar unknown
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- 2007-05-24 NO NO20072632A patent/NO20072632L/no not_active Application Discontinuation
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- 2010-07-28 AU AU2010206031A patent/AU2010206031A1/en not_active Abandoned
- 2010-08-03 US US12/849,158 patent/US20100317653A1/en not_active Abandoned
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CA2588162A1 (en) | 2006-06-22 |
MX2007007101A (es) | 2007-08-21 |
AU2005315430B2 (en) | 2010-05-27 |
US20080096874A1 (en) | 2008-04-24 |
US20100317653A1 (en) | 2010-12-16 |
KR20070087096A (ko) | 2007-08-27 |
SA05260407B1 (ar) | 2009-11-15 |
BRPI0519058A2 (pt) | 2008-12-23 |
WO2006064189A1 (en) | 2006-06-22 |
NZ555683A (en) | 2010-09-30 |
NO20072632L (no) | 2007-08-31 |
NZ587106A (en) | 2012-03-30 |
TW200633991A (en) | 2006-10-01 |
AU2010206031A1 (en) | 2010-08-19 |
JP2008523133A (ja) | 2008-07-03 |
AU2005315430A1 (en) | 2006-06-22 |
IL183279A0 (en) | 2007-09-20 |
US7795283B2 (en) | 2010-09-14 |
EP1833806A1 (en) | 2007-09-19 |
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