AR054198A1 - Derivados de benzotiazol-2-ona como inhibidores de lipasas y fosflipasas - Google Patents

Derivados de benzotiazol-2-ona como inhibidores de lipasas y fosflipasas

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Publication number
AR054198A1
AR054198A1 ARP060102371A ARP060102371A AR054198A1 AR 054198 A1 AR054198 A1 AR 054198A1 AR P060102371 A ARP060102371 A AR P060102371A AR P060102371 A ARP060102371 A AR P060102371A AR 054198 A1 AR054198 A1 AR 054198A1
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AR
Argentina
Prior art keywords
alkylene
alkyl
nr9r10
alkylamino
heteroaryl
Prior art date
Application number
ARP060102371A
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English (en)
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Sanofi Aventis Deutschland
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Application filed by Sanofi Aventis Deutschland filed Critical Sanofi Aventis Deutschland
Publication of AR054198A1 publication Critical patent/AR054198A1/es

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D277/00Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/60Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings condensed with carbocyclic rings or ring systems
    • C07D277/62Benzothiazoles
    • C07D277/68Benzothiazoles 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 in position 2
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic 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
    • A61K31/425Thiazoles
    • A61K31/428Thiazoles condensed with carbocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/18Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/06Antiasthmatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/02Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P17/00Drugs for dermatological disorders
    • A61P17/06Antipsoriatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/08Antiseborrheics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/10Anti-acne agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/12Keratolytics, e.g. wart or anti-corn preparations
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
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    • A61P25/00Drugs for disorders of the nervous system
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    • A61P3/06Antihyperlipidemics
    • AHUMAN NECESSITIES
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
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    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
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    • A61P9/12Antihypertensives

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Dermatology (AREA)
  • Neurology (AREA)
  • Obesity (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Immunology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pulmonology (AREA)
  • Rheumatology (AREA)
  • Pain & Pain Management (AREA)
  • Emergency Medicine (AREA)
  • Hospice & Palliative Care (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Oncology (AREA)
  • Endocrinology (AREA)
  • Psychiatry (AREA)
  • Urology & Nephrology (AREA)
  • Psychology (AREA)
  • Communicable Diseases (AREA)
  • Vascular Medicine (AREA)
  • Child & Adolescent Psychology (AREA)
  • Ophthalmology & Optometry (AREA)

Abstract

Composiciones farmacéuticas que los contienen, método d preparacion y usos en la prevencion de trastornos de metabolismo de ácidos grasos y trastornos de utilizacion de glucosa. Reivindicacion 1: Un compuesto de formula (1) en la que los significados son R1 es alquilo C5-16, alquileno C1-4-arilo C6-10, alquileno C1-4-heteroarilo C5-12, alquileno C1-4-cicloalquilo C4-12, biciclo C8-14, donde el arilo, heteroarilo, cicloalquilo o biciclo pueden estar sustituidos una o más veces con halogeno, alquilo C1-6, alquiloxi C1-3, alquilmercapto C1-6, amino, alquilamino C1-6, di-alquilamino C2-12, mono-alquilaminocarbonilo C1-6, di-alquilaminocarbonilo C2-8, alcoxicarbonilo C1-6, alquilcarbonilo C1-6, ciano, trifluorometilo, trifluorometoxi, alquilsulfonilo C1-6 o aminosulfonilo; R2 es H, alquilo C1-6; o R1 y R2 forman junto con el átomo de N que los tiene un sistema de anillos monocíclico, saturado o parcialmente insaturado, de 4 a 7 miembros o un sistema de anillos bicíclico, saturado o parcialmente insaturado, de 8 a 14 miembros, donde los miembros individuales de los sistemas de anillos pueden reemplazarse con uno a tres átomos o grupos atomicos de la serie -CHR8-, -CR8R8a-, -(C=R8)-, -NR9-, -C(=O)-, -O-, -S- , -SO-, -SO2-, con la condicion de que dos unidades de la serie -O-, -S-, -SO-, -SO2- no pueden ser adyacentes; R3 es H; R4, R5 son iguales o diferentes y son hidrogeno, halogeno, alquilo C1-6, alquiloxi C1-3-alquileno C1-3, hidroxi, alquilmercapto C1-6, amino, alquilamino C1-6, di-alquilamino C2-12, -alquilcarbonilo C1-6, CO-OR7, trifluorometilo, alquilsulfonilo C1-6, alquilsulfinilo C1-6, aminosulfonilo, pentafluorosulfanilo, arilo C6-10, heteroarilo C5-12, CO-NR9R10, O-CO-NR9R10, O-CO- alquileno C1-8-CO-O-alquilo C1-6, O-CO-alquileno C1-6-CO-OH, O-CO-alquileno C1-6-CO-NR9R10 o alquiloxi C1-6 sin sustituir o mono- o poli-F-sustituido; R6 es hidrogeno, alquiloxi C1-3-alquileno C1-3, hidroxi, alquilmercapto C1-6, amino, alquilamino C1-6, di-alquilamino C2-12, pentafluorosulfanilo, arilo C6-10, heteroarilo C5-12, CO-NR9R10, O-CO-NR9R10, O-CO-alquileno C1-6-CO-O-alquilo C1-6, O-CO-alquileno C1-6-CO-OH, O-CO-alquileno C1-6-CO-NR9R10 o alquiloxi C1-6 sin sustituir o mono- o poli-F- sustituido; con la condicion de que no más de uno de los sustituyentes R3, R4, R5 sea halogeno, trifluorometilo o alquilo C1-6; R7 es hidrogeno, alquilo C1-6, bencilo; R8, R8a son iguales o diferentes y son alquilo C1-6, halogeno, trifluorometilo, CO-OR7, ciclopropilo, ciclopropileno; R9, R10 son iguales o diferentes y son hidrogeno, alquilo C1-6, -arilo C6-10, -heteroarilo C5-12, cicloalquilo C3-12, alquileno C1-4-arilo C6-10, alquileno C1-C4-heteroarilo C5-12, alquileno C1-4-cicloalquilo C3- 12, biciclo C8-14; las formas tautoméricas de los compuestos y sales fisiologicamente toleradas de los mismos.
ARP060102371A 2005-06-09 2006-06-07 Derivados de benzotiazol-2-ona como inhibidores de lipasas y fosflipasas AR054198A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
DE102005026809A DE102005026809A1 (de) 2005-06-09 2005-06-09 Benzothiazol-2-on-derivate als Inhibitoren von Lipasen und Phospholipasen

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AR054198A1 true AR054198A1 (es) 2007-06-06

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Application Number Title Priority Date Filing Date
ARP060102371A AR054198A1 (es) 2005-06-09 2006-06-07 Derivados de benzotiazol-2-ona como inhibidores de lipasas y fosflipasas

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US (1) US8008331B2 (es)
EP (1) EP1896435B1 (es)
JP (1) JP2008542411A (es)
KR (1) KR20080014020A (es)
CN (1) CN101189218A (es)
AR (1) AR054198A1 (es)
AT (1) ATE495163T1 (es)
AU (1) AU2006257023A1 (es)
BR (1) BRPI0611918A2 (es)
CA (1) CA2609560A1 (es)
DE (2) DE102005026809A1 (es)
IL (1) IL187729A0 (es)
MA (1) MA29482B1 (es)
MX (1) MX2007015269A (es)
MY (1) MY146803A (es)
NO (1) NO20080034L (es)
NZ (1) NZ564061A (es)
RU (1) RU2007145476A (es)
TW (1) TW200716581A (es)
UY (1) UY29594A1 (es)
WO (1) WO2006131232A1 (es)

Families Citing this family (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE102005026808A1 (de) * 2005-06-09 2006-12-14 Sanofi-Aventis Deutschland Gmbh Benzooxazol-2-on-derivate als Inhibitoren von Lipasen und Phospholipasen
EP2025674A1 (de) 2007-08-15 2009-02-18 sanofi-aventis Substituierte Tetrahydronaphthaline, Verfahren zu ihrer Herstellung und ihre Verwendung als Arzneimittel
US8470841B2 (en) 2008-07-09 2013-06-25 Sanofi Heterocyclic compounds, processes for their preparation, medicaments comprising these compounds, and the use thereof
JP5605844B2 (ja) 2008-10-17 2014-10-15 塩野義製薬株式会社 血管内皮リパーゼ阻害活性を有する酢酸アミド誘導体
CA2784710A1 (en) 2009-12-15 2011-06-23 Shionogi & Co., Ltd. Oxadiazole derivative having endothelial lipase inhibitory activity
CN101845027B (zh) * 2010-05-28 2012-11-21 浙江工业大学 一种n-取代苯基-苯并噻唑酮-3-甲酰胺衍生物
US8933024B2 (en) 2010-06-18 2015-01-13 Sanofi Azolopyridin-3-one derivatives as inhibitors of lipases and phospholipases

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE2101150A1 (de) * 1971-01-12 1972-08-03 Farbenfabriken Bayer Ag, 5090 Leverkusen Substituierte Benzthiazolone, Verfahren zu ihrer Herstellung sowie ihre Verwendung als Akarizide und Insektizide
JPS60105671A (ja) * 1983-11-14 1985-06-11 Idemitsu Kosan Co Ltd ベンゾチアゾロン誘導体、その製造方法およびそれを有効成分とする農園芸用殺菌剤
JPS61155376A (ja) * 1984-12-28 1986-07-15 Idemitsu Kosan Co Ltd ベンゾチアゾロン誘導体,その製造方法およびそれを有効成分とする農園芸用殺菌剤
DE3835576A1 (de) * 1988-03-25 1989-10-12 Bayer Ag 3,7-disubstituierte benzthiazolone
JP2005518376A (ja) * 2001-12-14 2005-06-23 ノボ ノルディスク アクティーゼルスカブ 化合物およびホルモン感受性リパーゼの活性を低下させるためのその使用
DE10247680B4 (de) * 2002-10-12 2005-09-01 Aventis Pharma Deutschland Gmbh Neue bicyclische Inhibitoren der Hormon Sensitiven Lipase

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Publication number Publication date
AU2006257023A1 (en) 2006-12-14
CA2609560A1 (en) 2006-12-14
MY146803A (en) 2012-09-28
BRPI0611918A2 (pt) 2010-10-05
ATE495163T1 (de) 2011-01-15
CN101189218A (zh) 2008-05-28
TW200716581A (en) 2007-05-01
MX2007015269A (es) 2008-02-21
EP1896435B1 (de) 2011-01-12
WO2006131232A1 (de) 2006-12-14
IL187729A0 (en) 2008-08-07
US20080161370A1 (en) 2008-07-03
DE102005026809A1 (de) 2006-12-14
UY29594A1 (es) 2007-01-31
JP2008542411A (ja) 2008-11-27
US8008331B2 (en) 2011-08-30
EP1896435A1 (de) 2008-03-12
NZ564061A (en) 2010-07-30
RU2007145476A (ru) 2009-06-20
DE502006008717D1 (de) 2011-02-24
KR20080014020A (ko) 2008-02-13
MA29482B1 (fr) 2008-05-02
NO20080034L (no) 2008-03-10

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