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CL2012002259A1 - Forma cristalina de 4-{(1s,2s)-2-[84-ciclobutilpiperazin-1-il-carbonil]ciclopropil}benzamida; composicion farmacéutica; y su uso para tratar enfermedades tales como esquizofrenia, narcolepsia, somnolencia diurna excesiva, obesidad, trastornos por deficit de atencion con hiperactividad, dolor, entre otras. - Google Patents

Forma cristalina de 4-{(1s,2s)-2-[84-ciclobutilpiperazin-1-il-carbonil]ciclopropil}benzamida; composicion farmacéutica; y su uso para tratar enfermedades tales como esquizofrenia, narcolepsia, somnolencia diurna excesiva, obesidad, trastornos por deficit de atencion con hiperactividad, dolor, entre otras.

Info

Publication number
CL2012002259A1
CL2012002259A1 CL2012002259A CL2012002259A CL2012002259A1 CL 2012002259 A1 CL2012002259 A1 CL 2012002259A1 CL 2012002259 A CL2012002259 A CL 2012002259A CL 2012002259 A CL2012002259 A CL 2012002259A CL 2012002259 A1 CL2012002259 A1 CL 2012002259A1
Authority
CL
Chile
Prior art keywords
crystalline form
cyclobutylpiperazin
narcolepsy
schizophrenia
benzamide
Prior art date
Application number
CL2012002259A
Other languages
English (en)
Inventor
Michael A Uczynski
Original Assignee
Astrazeneca Ab
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=44370080&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=CL2012002259(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Astrazeneca Ab filed Critical Astrazeneca Ab
Publication of CL2012002259A1 publication Critical patent/CL2012002259A1/es

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C233/00Carboxylic acid amides
    • C07C233/64Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings
    • C07C233/65Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atoms of the carboxamide groups bound to hydrogen atoms or to carbon atoms of unsubstituted hydrocarbon radicals
    • 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
    • C07D295/16Heterocyclic 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 acylated on ring nitrogen atoms
    • C07D295/18Heterocyclic 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 acylated on ring nitrogen atoms by radicals derived from carboxylic acids, or sulfur or nitrogen analogues thereof
    • C07D295/182Radicals derived from carboxylic acids
    • C07D295/192Radicals derived from carboxylic acids from aromatic carboxylic acids
    • 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
    • A61K31/4965Non-condensed pyrazines
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/04Centrally acting analgesics, e.g. opioids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/18Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/20Hypnotics; Sedatives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/30Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/36Opioid-abuse
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C231/00Preparation of carboxylic acid amides
    • C07C231/06Preparation of carboxylic acid amides from nitriles by transformation of cyano groups into carboxamide groups
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C231/00Preparation of carboxylic acid amides
    • C07C231/14Preparation of carboxylic acid amides by formation of carboxamide groups together with reactions not involving the carboxamide groups
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C235/00Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms
    • C07C235/70Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups and doubly-bound oxygen atoms bound to the same carbon skeleton
    • C07C235/84Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups and doubly-bound oxygen atoms bound to the same carbon skeleton with the carbon atom of at least one of the carboxamide groups bound to a carbon atom of a six-membered aromatic ring
    • 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
    • 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
    • C07D295/16Heterocyclic 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 acylated on ring nitrogen atoms
    • C07D295/18Heterocyclic 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 acylated on ring nitrogen atoms by radicals derived from carboxylic acids, or sulfur or nitrogen analogues thereof
    • C07D295/182Radicals derived from carboxylic acids
    • 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
    • C07D295/16Heterocyclic 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 acylated on ring nitrogen atoms
    • C07D295/18Heterocyclic 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 acylated on ring nitrogen atoms by radicals derived from carboxylic acids, or sulfur or nitrogen analogues thereof
    • C07D295/182Radicals derived from carboxylic acids
    • C07D295/185Radicals derived from carboxylic acids from aliphatic carboxylic acids

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Psychiatry (AREA)
  • Epidemiology (AREA)
  • Pain & Pain Management (AREA)
  • Addiction (AREA)
  • Anesthesiology (AREA)
  • Hospice & Palliative Care (AREA)
  • Hematology (AREA)
  • Rheumatology (AREA)
  • Psychology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Obesity (AREA)
  • Diabetes (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Hydrogenated Pyridines (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Epoxy Compounds (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

Forma cristalina de 4-{(1S,2S)-2-[(4-ciclobutilpiperazin-1-il-carbonil]ciclopropil}benzamida (fórmula I); formulación farmacéutica que comprende la forma cristalina del compuesto de fórmula (I); y su uso para el tratamiento de la esquizofrenia, narcolepsia, obesidad, TDAH, dolor, enfermedad de Alzheimer, entre otros.
CL2012002259A 2010-02-18 2012-08-16 Forma cristalina de 4-{(1s,2s)-2-[84-ciclobutilpiperazin-1-il-carbonil]ciclopropil}benzamida; composicion farmacéutica; y su uso para tratar enfermedades tales como esquizofrenia, narcolepsia, somnolencia diurna excesiva, obesidad, trastornos por deficit de atencion con hiperactividad, dolor, entre otras. CL2012002259A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US30558310P 2010-02-18 2010-02-18

Publications (1)

Publication Number Publication Date
CL2012002259A1 true CL2012002259A1 (es) 2012-11-30

Family

ID=44370080

Family Applications (2)

Application Number Title Priority Date Filing Date
CL2012002259A CL2012002259A1 (es) 2010-02-18 2012-08-16 Forma cristalina de 4-{(1s,2s)-2-[84-ciclobutilpiperazin-1-il-carbonil]ciclopropil}benzamida; composicion farmacéutica; y su uso para tratar enfermedades tales como esquizofrenia, narcolepsia, somnolencia diurna excesiva, obesidad, trastornos por deficit de atencion con hiperactividad, dolor, entre otras.
CL2012002286A CL2012002286A1 (es) 2010-02-18 2012-08-17 Procesos para preparar cde 4-{(1s,2s)-2-[((r)-4-ciclobutil-2-(sustituidas) piperazin-1-il)carbonil]ciclopropil}benzamida; uno de los compuestos intermediarios considerados; y el procedimiento de preparacion del intermediario.

Family Applications After (1)

Application Number Title Priority Date Filing Date
CL2012002286A CL2012002286A1 (es) 2010-02-18 2012-08-17 Procesos para preparar cde 4-{(1s,2s)-2-[((r)-4-ciclobutil-2-(sustituidas) piperazin-1-il)carbonil]ciclopropil}benzamida; uno de los compuestos intermediarios considerados; y el procedimiento de preparacion del intermediario.

Country Status (19)

Country Link
US (2) US9012452B2 (es)
EP (2) EP2536685B1 (es)
JP (3) JP2013520413A (es)
KR (2) KR20130002316A (es)
CN (2) CN103168027B (es)
AR (2) AR080205A1 (es)
AU (2) AU2011218492B2 (es)
BR (2) BR112012020782A2 (es)
CA (2) CA2790040A1 (es)
CL (2) CL2012002259A1 (es)
CO (1) CO6592109A2 (es)
ES (1) ES2541857T3 (es)
IL (1) IL221431A (es)
MX (2) MX2012009473A (es)
NZ (2) NZ601920A (es)
RU (2) RU2012139082A (es)
SG (3) SG183274A1 (es)
TW (2) TWI520945B (es)
WO (2) WO2011102794A1 (es)

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TW201039825A (en) 2009-02-20 2010-11-16 Astrazeneca Ab Cyclopropyl amide derivatives 983
AU2011218490B9 (en) * 2010-02-18 2014-12-18 Astrazeneca Ab Solid forms comprising a cyclopropyl amide derivative
RU2012139082A (ru) * 2010-02-18 2014-03-27 Астразенека Аб Способы получения производных циклопропиламида и связанных с ними промежуточных соединений
FR3003466B1 (fr) * 2013-03-22 2015-08-07 Servier Lab Utilisation du 4-{3-[cis-hexahydrocyclopenta[c]pyrrol-2(1h)-yl]propoxy}benzamide pour le traitement des douleurs neuropathiques
WO2014146750A1 (de) * 2013-03-22 2014-09-25 Merck Patent Gmbh Synthesebausteine für die herstellung von materialien für organische elektrolumineszenzvorrichtungen
CN103342655A (zh) * 2013-07-02 2013-10-09 扬州大学 取代乙二酮双苯胺希夫碱合成取代酰胺的新方法
JP2026000886A (ja) 2024-06-18 2026-01-06 イーライ リリー アンド カンパニー Gip受容体アゴニスト化合物

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