AR084455A1 - Polimorfos de 3-cloro-4-[(2r)-2-(4-clorofenil)-4-[(1r)-1-(4-cianofenil)etil]-1-piperazinil]-benzonitrilo, composiciones farmaceuticas y metodo de uso que comprende dichos polimorfos, y un proceso para su preparacion - Google Patents

Polimorfos de 3-cloro-4-[(2r)-2-(4-clorofenil)-4-[(1r)-1-(4-cianofenil)etil]-1-piperazinil]-benzonitrilo, composiciones farmaceuticas y metodo de uso que comprende dichos polimorfos, y un proceso para su preparacion

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Publication number
AR084455A1
AR084455A1 ARP110104842A ARP110104842A AR084455A1 AR 084455 A1 AR084455 A1 AR 084455A1 AR P110104842 A ARP110104842 A AR P110104842A AR P110104842 A ARP110104842 A AR P110104842A AR 084455 A1 AR084455 A1 AR 084455A1
Authority
AR
Argentina
Prior art keywords
cyanophenyl
benzonitrile
piperazinyl
chlorophenyl
chloro
Prior art date
Application number
ARP110104842A
Other languages
English (en)
Original Assignee
Intervet Int Bv
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 Intervet Int Bv filed Critical Intervet Int Bv
Publication of AR084455A1 publication Critical patent/AR084455A1/es

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C253/00Preparation of carboxylic acid nitriles
    • C07C253/30Preparation of carboxylic acid nitriles by reactions not involving the formation of cyano groups
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D295/00Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/04Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
    • C07D295/14Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D295/155Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with the ring nitrogen atoms and the carbon atoms with three bonds to hetero atoms separated by carbocyclic rings or by carbon chains interrupted by carbocyclic rings
    • 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
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/04Anorexiants; Antiobesity agents
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C255/00Carboxylic acid nitriles
    • C07C255/49Carboxylic acid nitriles having cyano groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
    • C07C255/58Carboxylic acid nitriles having cyano groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton containing cyano groups and singly-bound nitrogen atoms, not being further bound to other hetero atoms, bound to the carbon skeleton
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C303/00Preparation of esters or amides of sulfuric acids; Preparation of sulfonic acids or of their esters, halides, anhydrides or amides
    • C07C303/26Preparation of esters or amides of sulfuric acids; Preparation of sulfonic acids or of their esters, halides, anhydrides or amides of esters of sulfonic acids
    • C07C303/28Preparation of esters or amides of sulfuric acids; Preparation of sulfonic acids or of their esters, halides, anhydrides or amides of esters of sulfonic acids by reaction of hydroxy compounds with sulfonic acids or derivatives thereof
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C309/00Sulfonic acids; Halides, esters, or anhydrides thereof
    • C07C309/63Esters of sulfonic acids
    • C07C309/64Esters of sulfonic acids having sulfur atoms of esterified sulfo groups bound to acyclic carbon atoms
    • C07C309/65Esters of sulfonic acids having sulfur atoms of esterified sulfo groups bound to acyclic carbon atoms of a saturated carbon skeleton
    • C07C309/66Methanesulfonates
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D241/00Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
    • C07D241/02Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
    • C07D241/04Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D309/00Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings
    • C07D309/02Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
    • C07D309/08Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings having no double bonds between ring members or between ring members and non-ring members 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
    • C07D309/10Oxygen atoms
    • C07D309/12Oxygen atoms only hydrogen atoms and one oxygen atom directly attached to ring carbon atoms, e.g. tetrahydropyranyl ethers

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Epidemiology (AREA)
  • Hematology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Diabetes (AREA)
  • Obesity (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Child & Adolescent Psychology (AREA)
  • Engineering & Computer Science (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Pyrane Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)

Abstract

Se describen polimorfos de 3-cloro-4[(2R)-2-(4-clorofenil)-4-[(1R)-1-(4-cianofenil)etil]-1-piperazinil]-benzonitrilo de fórmula (1) e intermediarios. Útil como antagonista del receptor 1 cannabinoide para tratar la obesidad. Patrón de difracción de Rayos X: Forma I: 13,4; 20,2; 23,0; y 24,1 grados 2q; Forma II: 12,9; 15,8; 18,5 y 24,2 grados 2q; y Forma III: 17,9; 21,9; 24,5 y 26,8 grados 2q.Reivindicación 34: Un compuesto seleccionado del grupo que consiste de las fórmulas (2) a (7). Reivindicación 35: Un compuesto seleccionado del grupo que consiste de las fórmulas (4) y (7).
ARP110104842A 2010-12-23 2011-12-21 Polimorfos de 3-cloro-4-[(2r)-2-(4-clorofenil)-4-[(1r)-1-(4-cianofenil)etil]-1-piperazinil]-benzonitrilo, composiciones farmaceuticas y metodo de uso que comprende dichos polimorfos, y un proceso para su preparacion AR084455A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201061426592P 2010-12-23 2010-12-23
EP11155049 2011-02-18

Publications (1)

Publication Number Publication Date
AR084455A1 true AR084455A1 (es) 2013-05-15

Family

ID=44041600

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP110104842A AR084455A1 (es) 2010-12-23 2011-12-21 Polimorfos de 3-cloro-4-[(2r)-2-(4-clorofenil)-4-[(1r)-1-(4-cianofenil)etil]-1-piperazinil]-benzonitrilo, composiciones farmaceuticas y metodo de uso que comprende dichos polimorfos, y un proceso para su preparacion

Country Status (8)

Country Link
US (1) US20130274270A1 (es)
EP (1) EP2655343A1 (es)
JP (1) JP2014501753A (es)
AR (1) AR084455A1 (es)
AU (1) AU2011346746A1 (es)
BR (1) BR112013015903A2 (es)
CA (1) CA2822767A1 (es)
WO (1) WO2012085645A1 (es)

Families Citing this family (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US10117430B2 (en) 2012-12-14 2018-11-06 Basf Se Malononitrile compounds for controlling animal pests
US10857121B2 (en) 2014-04-17 2020-12-08 Merial Inc. Use of malononitrile compounds for protecting animals from parasites

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ES2435790T3 (es) * 2004-12-03 2013-12-23 Intervet International B.V. Piperazinas sustituidas como antagonistas de CB1
BRPI0814806A2 (pt) * 2007-06-28 2015-02-03 Intervet Int Bv Pirazinas substituídas como antagonistas de cb1

Also Published As

Publication number Publication date
JP2014501753A (ja) 2014-01-23
US20130274270A1 (en) 2013-10-17
EP2655343A1 (en) 2013-10-30
WO2012085645A1 (en) 2012-06-28
CA2822767A1 (en) 2012-06-28
AU2011346746A1 (en) 2013-07-11
BR112013015903A2 (pt) 2018-06-05

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