AR051090A1 - Derivados heterociclicos y su uso como inhibidores de la estearoil-coa desaturasa - Google Patents

Derivados heterociclicos y su uso como inhibidores de la estearoil-coa desaturasa

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Publication number
AR051090A1
AR051090A1 ARP050103904A ARP050103904A AR051090A1 AR 051090 A1 AR051090 A1 AR 051090A1 AR P050103904 A ARP050103904 A AR P050103904A AR P050103904 A ARP050103904 A AR P050103904A AR 051090 A1 AR051090 A1 AR 051090A1
Authority
AR
Argentina
Prior art keywords
alkyl
independently selected
group
rings
heteroaryl
Prior art date
Application number
ARP050103904A
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English (en)
Original Assignee
Xenon Pharmaceuticals Inc
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.)
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Publication date
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=35759135&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=AR051090(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Xenon Pharmaceuticals Inc filed Critical Xenon Pharmaceuticals Inc
Publication of AR051090A1 publication Critical patent/AR051090A1/es

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen 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
    • C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/81—Amides; Imides
    • C07D213/82—Amides; Imides in position 3
    • 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
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • 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
    • A61P1/18—Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/08—Drugs for genital or sexual disorders; Contraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
    • 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
    • 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
    • A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • 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
    • 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
    • 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
    • A61P19/06—Antigout agents, e.g. antihyperuricemic or uricosuric agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • 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
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/04—Antineoplastic agents specific for metastasis
    • 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
    • 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
    • A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • 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

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  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Rheumatology (AREA)
  • Dermatology (AREA)
  • Reproductive Health (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Endocrinology (AREA)
  • Pain & Pain Management (AREA)
  • Child & Adolescent Psychology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Oncology (AREA)
  • Emergency Medicine (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Immunology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Gynecology & Obstetrics (AREA)
  • Pregnancy & Childbirth (AREA)
  • Cardiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

Métodos para tratar una enfermedad o afeccion mediada por la SCD en un mamífero, preferentemente un ser humano. Los métodos comprenden administrar a un mamífero que lo necesita un compuesto de formula (1). También se revelan composiciones farmacéuticas que comprenden los compuestos de formula (1). Reivindicacion 10: Un compuesto de formula (1) caracterizado porque: y es 0, 1, 2 o 3; G es -N(R4)-, -O-, -S(O)t- (donde t es 0, 1 o 2), -C(R4)= o -C(R4)=C(R4)-; K es N o C(R10); L y M son cada uno en forma independiente -N= o -C(R4)=, con la salvedad de que cuando G es -C(R4)= o -C(R4)=C(R4)-, L y M no pueden ser ambos -C(R4)=; V es -N(R1)-, -O-, -C(R10)2-, -C(O)-, -C(O)O-, -C(S)-, -C(O)N(R1), -S(O)t- (donde t es 0, 1 o 2) o - S(O)pN(R1)- (donde p es 1 o 2), con la salvedad de que cuando K es N, V no puede ser -S-; W es un enlace directo, -N(R1)C(O)-, -C(O)N(R1)-, -OC(O)N(R1)-, -N(R1)C(O)N(R1)-, -O-, -N(R1)-, -S(O)t- (donde t es 0, 1 o 2), -N(R1)S(O)p- (donde p es 1 o 2), -S(O)pN(R1)- (donde p es 1 o 2), -C(O)-, -OS(O)2N(R1)-, -OC(O)-, -C(O)O-, o -N(R1)C(O)O-; cada R1 se selecciona en forma independiente el grupo formado por H, C1-12 alquilo, C2-12 hidroxialquilo, C4-12 cicloalquilalquilo y C7-19 aralquilo; R2 se selecciona el grupo formado por C1-12 alquilo, C2-12 alquenilo, C2-12 hidroxialquilo, C2-12 hidroxialquenilo, C2-12 alcoxialquilo, C3-12 cicloalquilo, C4-12 cicloalquilalquilo, arilo, C7-19 aralquilo, C3-12 heterociclilo, C3-12 heterociclilalquilo, C1-12 heteroarilo, y C3-12 heteroarilalquilo; o R2 es una estructura de anillos multiples que tiene entre 2 y 4 anillos en donde los anillos se seleccionan en forma independiente del grupo formado por cicloalquilo, heterociclilo, arilo y heteroarilo y, donde algunos o todos los anillos pueden estar fusionados entre sí, R3 se selecciona del grupo formado por H, C1-12 alquilo, C2-12 alquenilo, C2-12 hidroxialquilo, C2-12 hidroxialquenilo, C2-12 alcoxialquilo, C3-12 cicloalquilo, C4-12 cicloalquilalquilo, arilo, C7-19 aralquilo, C3-12 heterociclilo, C3-12 heterociclilalquilo, C1-12 heteroarilo, y C3-12 heteroarilalquilo; o R3 es una estructura de anillos multiples que tiene entre 2 y 4 anillos en donde los anillos se seleccionan en forma independiente del grupo formado por cicloalquilo, heterociclilo, arilo y heteroarilo y, donde algunos o todos los anillos pueden estar fusionados entre sí; cada R4 se selecciona en forma independiente entre H, F, Cl, C1-12 alquilo, C1-12 alcoxi, haloalquilo, ciano, nitro o -N(R9)2; o dos grupos R4 contiguos, junto con los átomos de C a los cuales están unidos, pueden formar un sistema de anillos arilo, heteroarilo o heterocíclico; R4a es H, F, Cl, C1-12 alquilo, C1-12 alcoxi, haloalquilo, ciano, nitro o -N(R9)2; o R4a es un enlace directo con un C contiguo; R6, R6a, R7, R7a, R8 y R8a se seleccionan cada uno en forma independiente entre H o C1-3 alquilo; o R6 y R6a juntos, o R7 y R7a juntos, o R8 y R8a juntos constituyen un grupo oxo, con la salvedad de que cuando V es -C(O)-, R6 y R6a juntos o R8 y R8a juntos no formen un grupo oxo, mientras los restantes R6, R6a, R7, R7a, R8 y R8a se seleccionan cada uno en forma independiente entre H o C1-3 alquilo; o uno de R6 y R6a junto con uno de R7, R7a, R8 y R8a forma un enlace directo o un puente alquileno, mientras los restantes R6, R6a, R7, R7a, R8 y R8a se seleccionan cada uno en forma independiente entre H o C1-3 alquilo; cada R9 se selecciona en forma independiente entre H o C1-6 alquilo; y R10 se selecciona en forma independiente entre H, F, Cl, C1-12 alquilo o C1-12 alcoxi; en forma de uno sus estereoisomeros, enantiomeros o tautomeros, en forma de mezcla de estereoisomeros, en forma de sal aceptable para uso farmacéutico, o como prodroga del mismo.
ARP050103904A 2004-09-20 2005-09-20 Derivados heterociclicos y su uso como inhibidores de la estearoil-coa desaturasa AR051090A1 (es)

Applications Claiming Priority (1)

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US61150804P 2004-09-20 2004-09-20

Publications (1)

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AR051090A1 true AR051090A1 (es) 2006-12-20

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ID=35759135

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US (1) US7777036B2 (es)
EP (1) EP1799667B1 (es)
JP (1) JP5043668B2 (es)
CN (1) CN101084211A (es)
AR (1) AR051090A1 (es)
AU (1) AU2005286846A1 (es)
BR (1) BRPI0515488A (es)
CA (1) CA2580762A1 (es)
MX (1) MX2007003321A (es)
TW (1) TW200626138A (es)
WO (1) WO2006034279A1 (es)

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US7777036B2 (en) 2010-08-17
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