AR083542A1 - PIPERIDIN-4-IL-AZETIDIN DIAMIDS AS INHIBITORS OF MONOACILGLICEROL LIPASA - Google Patents

PIPERIDIN-4-IL-AZETIDIN DIAMIDS AS INHIBITORS OF MONOACILGLICEROL LIPASA

Info

Publication number
AR083542A1
AR083542A1 ARP110103927A ARP110103927A AR083542A1 AR 083542 A1 AR083542 A1 AR 083542A1 AR P110103927 A ARP110103927 A AR P110103927A AR P110103927 A ARP110103927 A AR P110103927A AR 083542 A1 AR083542 A1 AR 083542A1
Authority
AR
Argentina
Prior art keywords
group
unsubstituted
trifluoromethyl
fluorine
phenyl
Prior art date
Application number
ARP110103927A
Other languages
Spanish (es)
Original Assignee
Janssen Pharmaceutica Nv
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 Janssen Pharmaceutica Nv filed Critical Janssen Pharmaceutica Nv
Publication of AR083542A1 publication Critical patent/AR083542A1/en

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    • 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
    • C07D417/14—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 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
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • 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
    • 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
    • A61P1/02—Stomatological preparations, e.g. drugs for caries, aphtae, periodontitis
    • 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
    • A61P11/00—Drugs for disorders of the respiratory system
    • 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
    • A61P13/02—Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
    • 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
    • A61P13/10—Drugs for disorders of the urinary system of the bladder
    • 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
    • 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
    • A61P17/04—Antipruritics
    • 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
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • 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
    • 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
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • 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
    • A61P25/06—Antimigraine 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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
    • 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
    • C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Neurology (AREA)
  • Pain & Pain Management (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Dermatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Rheumatology (AREA)
  • Pulmonology (AREA)
  • Endocrinology (AREA)
  • Reproductive Health (AREA)
  • Immunology (AREA)
  • Epidemiology (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

Se describen los compuestos, composiciones y métodos para la manufactura de medicamentos que son útiles para tratar trastornos que incluyen el dolor.Reivindicación 1: Un compuesto de fórmula (1) en donde Y y Z están seleccionados independientemente del Grupo a) o el Grupo b), de manera que uno de Y y Z es el Grupo a) y el otro es el Grupo b); el Grupo a) es i) arilo C6-10 no sustituido o sustituido con un sustituyente seleccionado del grupo que consiste en flúor, cloro, alquilo C1-4, alcoxi C1-4, ciano y trifluorometilo; o ii) un heteroarilo no sustituido seleccionado del grupo que consiste en tiazolilo, isotiazolilo y 1H-pirrolilo; el Grupo b) es i) arilo C6-10; ii) un heteroarilo seleccionado del grupo que consiste en benzoxazolilo, benzotiazolilo, benzimidazolilo, benzotienilo, indazolilo, e indolilo; iii) fenilmetil-fenilo, en donde el grupo fenilo del fenilmetilo es no sustituido o sustituido con trifluorometilo o flúor; o iv) 1,3-dihidro-H-benzimidazol-2-on-ilo; en donde el Grupo b) que no es fenilmetil-fenilo es no sustituido o sustituido con uno o dos sustituyentes seleccionados independientemente del grupo que consiste en bromo, cloro, flúor, yodo, alquilo C1-4, alcoxi C1-4 y Rb; siempre que no más que un sustituyente sea Rb; y Rb está seleccionado del grupo que consiste en trifluorometilo, 2,2,2-trifluoroetilo, 3,3,3-trifluoropropilo, 4,4-difluorociclohexilo, tienilo, piridinilo y fenilo; en donde dichos tienilo, piridinilo y fenilo de Rb son no sustituidos o sustituidos con uno o dos sustituyentes seleccionados independientemente del grupo que consiste en trifluorometilo, metilo, cloro, ciano y flúor; R es hidrógeno o hidroxi; y enantiómeros, diastereómeros y sales farmacéuticamente aceptables de estos.Compounds, compositions and methods for the manufacture of medicaments that are useful for treating disorders including pain are described. Claim 1: A compound of formula (1) wherein Y and Z are independently selected from Group a) or Group b ), so that one of Y and Z is Group a) and the other is Group b); Group a) is i) C6-10 aryl unsubstituted or substituted with a substituent selected from the group consisting of fluorine, chlorine, C1-4 alkyl, C1-4 alkoxy, cyano and trifluoromethyl; or ii) an unsubstituted heteroaryl selected from the group consisting of thiazolyl, isothiazolyl and 1H-pyrrolyl; Group b) is i) C6-10 aryl; ii) a heteroaryl selected from the group consisting of benzoxazolyl, benzothiazolyl, benzimidazolyl, benzothienyl, indazolyl, and indolyl; iii) phenylmethyl-phenyl, wherein the phenylmethyl group is unsubstituted or substituted with trifluoromethyl or fluorine; or iv) 1,3-dihydro-H-benzimidazol-2-on-yl; wherein Group b) which is not phenylmethyl-phenyl is unsubstituted or substituted with one or two substituents independently selected from the group consisting of bromine, chlorine, fluorine, iodine, C1-4 alkyl, C1-4 alkoxy and Rb; provided that no more than one substituent is Rb; and Rb is selected from the group consisting of trifluoromethyl, 2,2,2-trifluoroethyl, 3,3,3-trifluoropropyl, 4,4-difluorocyclohexyl, thienyl, pyridinyl and phenyl; wherein said thienyl, pyridinyl and Rb phenyl are unsubstituted or substituted with one or two substituents independently selected from the group consisting of trifluoromethyl, methyl, chlorine, cyano and fluorine; R is hydrogen or hydroxy; and enantiomers, diastereomers and pharmaceutically acceptable salts thereof.

ARP110103927A 2010-10-22 2011-10-24 PIPERIDIN-4-IL-AZETIDIN DIAMIDS AS INHIBITORS OF MONOACILGLICEROL LIPASA AR083542A1 (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US40587610P 2010-10-22 2010-10-22

Publications (1)

Publication Number Publication Date
AR083542A1 true AR083542A1 (en) 2013-03-06

Family

ID=44993878

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP110103927A AR083542A1 (en) 2010-10-22 2011-10-24 PIPERIDIN-4-IL-AZETIDIN DIAMIDS AS INHIBITORS OF MONOACILGLICEROL LIPASA

Country Status (12)

Country Link
EP (1) EP2629851A1 (en)
JP (1) JP2013540159A (en)
KR (1) KR20130142137A (en)
CN (1) CN103260703A (en)
AR (1) AR083542A1 (en)
AU (1) AU2011316970A1 (en)
BR (1) BR112013009858A2 (en)
CA (1) CA2815350A1 (en)
IL (1) IL225769A0 (en)
RU (1) RU2013123275A (en)
TW (1) TW201305136A (en)
WO (1) WO2012054716A1 (en)

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WO2018140514A1 (en) 2017-01-26 2018-08-02 Araxes Pharma Llc 1-(6-(3-hydroxynaphthalen-1-yl)quinazolin-2-yl)azetidin-1-yl)prop-2-en-1-one derivatives and similar compounds as kras g12c inhibitors for the treatment of cancer
WO2018140512A1 (en) 2017-01-26 2018-08-02 Araxes Pharma Llc Fused bicyclic benzoheteroaromatic compounds and methods of use thereof
JP7327802B2 (en) 2017-01-26 2023-08-16 アラクセス ファーマ エルエルシー Fused hetero-heterobicyclic compounds and methods of use thereof
EP3573971A1 (en) 2017-01-26 2019-12-04 Araxes Pharma LLC 1-(3-(6-(3-hydroxynaphthalen-1-yl)benzofuran-2-yl)azetidin-1yl)prop-2-en-1-one derivatives and similar compounds as kras g12c modulators for treating cancer
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Also Published As

Publication number Publication date
CN103260703A (en) 2013-08-21
WO2012054716A1 (en) 2012-04-26
AU2011316970A1 (en) 2013-05-09
CA2815350A1 (en) 2012-04-26
RU2013123275A (en) 2014-11-27
TW201305136A (en) 2013-02-01
KR20130142137A (en) 2013-12-27
EP2629851A1 (en) 2013-08-28
BR112013009858A2 (en) 2016-07-26
IL225769A0 (en) 2013-06-27
JP2013540159A (en) 2013-10-31

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