AR034271A1 - Compuestos derivados de benzo[d]isotiazol y benzo[b]tiofeno, su uso, un proceso para su elaboracion y composiciones farmaceuticas que los comprenden - Google Patents

Compuestos derivados de benzo[d]isotiazol y benzo[b]tiofeno, su uso, un proceso para su elaboracion y composiciones farmaceuticas que los comprenden

Info

Publication number
AR034271A1
AR034271A1 ARP010105115A ARP010105115A AR034271A1 AR 034271 A1 AR034271 A1 AR 034271A1 AR P010105115 A ARP010105115 A AR P010105115A AR P010105115 A ARP010105115 A AR P010105115A AR 034271 A1 AR034271 A1 AR 034271A1
Authority
AR
Argentina
Prior art keywords
lower alkyl
hydrogen
optionally substituted
alkyl
benzo
Prior art date
Application number
ARP010105115A
Other languages
English (en)
Inventor
Johannes Aebi
Jean Ackermann
Henrietta Dehmlow
Hans-Peter Maerki
Olivier Morand
Original Assignee
Hoffmann La Roche
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Hoffmann La Roche filed Critical Hoffmann La Roche
Publication of AR034271A1 publication Critical patent/AR034271A1/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • 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
    • A61P3/06—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
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/10—Antimycotics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00—Antiparasitic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/12—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D233/56—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D249/00—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
    • C07D249/02—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
    • C07D249/08—1,2,4-Triazoles; Hydrogenated 1,2,4-triazoles
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D275/00—Heterocyclic compounds containing 1,2-thiazole or hydrogenated 1,2-thiazole rings
    • C07D275/04—Heterocyclic compounds containing 1,2-thiazole or hydrogenated 1,2-thiazole rings condensed with carbocyclic rings or ring systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D275/00—Heterocyclic compounds containing 1,2-thiazole or hydrogenated 1,2-thiazole rings
    • C07D275/04—Heterocyclic compounds containing 1,2-thiazole or hydrogenated 1,2-thiazole rings condensed with carbocyclic rings or ring systems
    • C07D275/06—Heterocyclic compounds containing 1,2-thiazole or hydrogenated 1,2-thiazole rings condensed with carbocyclic rings or ring systems with hetero atoms directly attached to the ring sulfur atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D333/00—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
    • C07D333/50—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom condensed with carbocyclic rings or ring systems
    • C07D333/52—Benzo[b]thiophenes; Hydrogenated benzo[b]thiophenes
    • C07D333/54—Benzo[b]thiophenes; Hydrogenated benzo[b]thiophenes with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to carbon atoms of the hetero ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur 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)
  • Veterinary Medicine (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Diabetes (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Urology & Nephrology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Vascular Medicine (AREA)
  • Emergency Medicine (AREA)
  • Endocrinology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Thiazole And Isothizaole Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Steroid Compounds (AREA)

Abstract

Compuestos derivados de benzo[d]isotiazol y benzo[b]tiofeno de fórmula (1) en donde: U es O ó un par sólo; Y es N ó CR1; Z es S ó S(O)2; V es (a) -CH=CH-, y m y n son 0, ó (b) -CH2-, y m + n <= 2, ó (c) O ó NR2, y m es de 1 a 6, n es de 1 a 6, m + n <= 7, o m es de 1 a 3, n es 0, ó (d) S, y m es de 1 a 7, n es de 0 a 6, m + n <= 7, ó (e) -C:::C-, y m es de 0 a 7, n es de 0 a 7, m + n <= 7; Q es cicloalquilo, cicloalquil-alquilo inferior, fenilo opcionalmente sustituido por 1-3 sustituyentes seleccionados independientemente del grupo R3, o un grupo alquilo, alquenilo o alcadienilo opcionalmente sustituido por OH; A1 es hidrógeno, alquenilo inferior, o alquilo inferior opcionalmente sustituido con hidroxilo, alcoxilo inferior o tio-alcoxilo inferior; A2 es cicloalquilo, cicloalquil-alquilo inferior, alquenilo inferior, alquinilo inferior, heteroarilo o alquilo inferior opcionalmente sustituido con halógeno, hidroxilo, alcoxilo inferior, o tio-alcoxilo inferior; o A1 y A2 están unidos uno al otro formando un anillo y -A1-A2- es alquileno inferior, o alquenileno inferior, opcionalmente sustituido por R4, en el que un grupo -CH2- de -A1-A2- puede estar opcionalmente reemplazado por un NR5, S, u O, ó -A1-A2- es -CH=N=CH=CH- que puede estar opcionalmente sustituido por alquilo inferior; A3 y A4 independientemente uno del otro son hidrógeno o alquilo inferior, o A3 y A4 están unidos uno al otro para formar un anillo junto con el átomo de C al que están unidos y A3 y A4 es -(CH2)2-5- que pueden estar mono- o multi-sustituidos por alquilo inferior; X es hidrógeno o uno o más halógenos opcionales y/o sustituyentes alquilo inferior; R1 es hidrógeno o alquilo inferior; R2 es hidrógeno o alquilo inferior; R3 es halógeno, N(R6, R7), piperidilo, piperazinilo, piperazinil-etanona, morfolinilo, CONH2, CN, NO2, CF3, OH, alcoxilo inferior, tio-alcoxilo inferior, o es alquilo inferior, alquenilo inferior, o alquinilo inferior, opcionalmente sustituido con OH, SH o N(R8, R9); R4 es hidroxilo, alquilo inferior, alcoxilo inferior, o tio-alcoxilo inferior; R5 es hidrógeno, alquilo inferior, o alquil-carbonilo inferior; R6 y R7 independientemente uno del otro se seleccionan del grupo consistente en hidrógeno, alquilo inferior, fenilo y bencilo; R8 y R9 independientemente uno del otro se seleccionan del grupo consistente en hidrógeno y alquilo inferior; y sales farmacéuticamente aceptables y/o ésteres farmacéuticamente aceptables de los mismos. Los compuestos son útiles para el tratamiento y/o prevención de enfermedades que están asociadas con 2,3-oxidoescualeno-lanosterol ciclasa tales como hipercolesterolemia, hiperlipemia, arteriosclerosis, enfermedades vasculares, micosis, cálculos biliares, tumores y/o trastornos hiperproliferativos, y tratamiento y/o prevención de la disminución de la tolerancia a la glucosa y diabetes. Proceso para su elaboración y composiciones farmacéuticas que los comprenden.
ARP010105115A 2000-11-02 2001-11-01 Compuestos derivados de benzo[d]isotiazol y benzo[b]tiofeno, su uso, un proceso para su elaboracion y composiciones farmaceuticas que los comprenden AR034271A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP00123826 2000-11-02

Publications (1)

Publication Number Publication Date
AR034271A1 true AR034271A1 (es) 2004-02-18

Family

ID=8170270

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP010105115A AR034271A1 (es) 2000-11-02 2001-11-01 Compuestos derivados de benzo[d]isotiazol y benzo[b]tiofeno, su uso, un proceso para su elaboracion y composiciones farmaceuticas que los comprenden

Country Status (21)

Country Link
US (3) US6951879B2 (es)
EP (1) EP1334094B1 (es)
JP (1) JP4012064B2 (es)
KR (1) KR100545430B1 (es)
CN (1) CN1261429C (es)
AR (1) AR034271A1 (es)
AT (1) ATE286042T1 (es)
AU (2) AU2002214029B2 (es)
BR (1) BR0115075A (es)
CA (1) CA2426009C (es)
DE (1) DE60108164T2 (es)
DK (1) DK1334094T3 (es)
ES (1) ES2233703T3 (es)
GT (1) GT200100220A (es)
MX (1) MXPA03003845A (es)
PA (1) PA8531601A1 (es)
PE (1) PE20020600A1 (es)
PT (1) PT1334094E (es)
UY (1) UY27009A1 (es)
WO (1) WO2002036584A1 (es)
ZA (1) ZA200302742B (es)

Families Citing this family (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
RU2225393C1 (ru) 2000-08-16 2004-03-10 Ф.Хоффманн-Ля Рош Аг Новые производные аминоциклогексана
US7012077B2 (en) * 2001-12-20 2006-03-14 Hoffmann-La Roche Inc. Substituted cyclohexane derivatives
EP1647549A1 (en) * 2004-10-14 2006-04-19 Laboratoire Theramex Indazoles, benzisoxazoles and benzisothiazoles as estrogenic agents
JP4912314B2 (ja) * 2004-10-26 2012-04-11 ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプ 因子Ｘａ化合物
EP1902023A4 (en) * 2005-06-30 2009-08-12 Bayer Cropscience Ag IMPROVED PROCESS FOR PREPARING PHENYLALKYL SUBSTITUTED INSECTICIDE HETEROCYCLES (DISUBSTITUTED PROPENYL)
FR2913019A1 (fr) * 2007-02-23 2008-08-29 Cerep Sa Composes heterocycliques comme agents anti-neoplasiques ou inhibiteurs de proliferation cellulaire
BRPI0820224A2 (pt) * 2007-11-29 2015-06-16 Ranbaxy Lab Ltd Composto de fórmula iii ou seus estereoisômeros; processo para sua preparação e seu uso; uso de um composto de formula iii(a) ou iii(b) em um processo para a preparação de lamivudina de fórmula i(a) ou um composto de fórmula i(c); processo para preparação de lamivudina de fórmula i(a)
SI2225232T1 (sl) * 2007-11-29 2012-12-31 Ranbaxy Laboratories Limited Postopek za pripravo substituiranih 1,3-oksatiolanov
WO2012092114A2 (en) 2010-12-27 2012-07-05 The Curators Of The University Of Missouri Oxidosqualene cyclase as a protein target for anticancer therapeutics

Family Cites Families (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3598839A (en) * 1969-06-30 1971-08-10 Parke Davis & Co Phenylbenzothiophene compounds
GR75101B (es) * 1980-10-23 1984-07-13 Pfizer
GB8417559D0 (en) * 1984-07-10 1984-08-15 Pfizer Ltd Anti-diarrhoeal agents
DE3905364A1 (de) 1989-02-22 1990-08-23 Hoechst Ag Substituierte pyrimidin-derivate, verfahren zu ihrer herstellung und ihre verwendung als tool
EP0530149A1 (de) * 1991-08-30 1993-03-03 Ciba-Geigy Ag Schädlingsbekämpfungsmittel
US5482949A (en) * 1993-03-19 1996-01-09 Eli Lilly And Company Sulfonate derivatives of 3-aroylbenzo[b]thiophenes
CA2190699A1 (en) * 1995-12-08 1997-06-09 Johannes Aebi Tertiary amines
CA2190708A1 (en) * 1995-12-08 1997-06-09 Johannes Aebi Aminoalkyl substituted benzo-heterocyclic compounds
UA56197C2 (uk) 1996-11-08 2003-05-15 Зенека Лімітед Гетероциклічні похідні

Also Published As

Publication number Publication date
PA8531601A1 (es) 2003-02-14
KR100545430B1 (ko) 2006-01-24
KR20030045166A (ko) 2003-06-09
ZA200302742B (en) 2004-07-08
MXPA03003845A (es) 2003-07-28
PE20020600A1 (es) 2002-07-08
DK1334094T3 (da) 2005-05-02
AU2002214029B2 (en) 2004-12-23
EP1334094B1 (en) 2004-12-29
ATE286042T1 (de) 2005-01-15
CN1261429C (zh) 2006-06-28
UY27009A1 (es) 2002-06-20
CN1471522A (zh) 2004-01-28
US7173043B2 (en) 2007-02-06
CA2426009A1 (en) 2002-05-10
GT200100220A (es) 2002-07-04
US20070099985A1 (en) 2007-05-03
DE60108164D1 (de) 2005-02-03
CA2426009C (en) 2008-10-07
US20050267200A1 (en) 2005-12-01
WO2002036584A1 (en) 2002-05-10
US20020086891A1 (en) 2002-07-04
US7449483B2 (en) 2008-11-11
JP4012064B2 (ja) 2007-11-21
AU1402902A (en) 2002-05-15
EP1334094A1 (en) 2003-08-13
US6951879B2 (en) 2005-10-04
ES2233703T3 (es) 2005-06-16
JP2004513124A (ja) 2004-04-30
PT1334094E (pt) 2005-05-31
BR0115075A (pt) 2003-07-29
DE60108164T2 (de) 2006-03-02

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