PE20130007A1 - Procedimiento para la preparacion de 2-(ciclohexilmetil)-n-{2-[(2s)-1-metilpirrolidin-2-il]etil}-1,2,3,4-tetrahidroisoquinolin-7-sulfonamida - Google Patents

Procedimiento para la preparacion de 2-(ciclohexilmetil)-n-{2-[(2s)-1-metilpirrolidin-2-il]etil}-1,2,3,4-tetrahidroisoquinolin-7-sulfonamida

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Publication number
PE20130007A1
PE20130007A1 PE2012001391A PE2012001391A PE20130007A1 PE 20130007 A1 PE20130007 A1 PE 20130007A1 PE 2012001391 A PE2012001391 A PE 2012001391A PE 2012001391 A PE2012001391 A PE 2012001391A PE 20130007 A1 PE20130007 A1 PE 20130007A1
Authority
PE
Peru
Prior art keywords
tetrahydroisoquinolin
methylpyrrolidin
ethyl
sulfonamide
cyclohexylmethyl
Prior art date
Application number
PE2012001391A
Other languages
English (en)
Inventor
Steven Elenbaas
Robert Allan Farr
John Michael Kane
Original Assignee
Sanofi Sa
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
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First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=44012569&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=PE20130007(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Sanofi Sa filed Critical Sanofi Sa
Publication of PE20130007A1 publication Critical patent/PE20130007A1/es

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    • 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
    • C07D401/12—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 linked by a chain containing hetero atoms as chain links
    • 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
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/472—Non-condensed isoquinolines, e.g. papaverine
    • A61K31/4725—Non-condensed isoquinolines, e.g. papaverine containing further heterocyclic rings
    • 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
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • 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
    • A61P25/08—Antiepileptics; Anticonvulsants
    • 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
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • 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
    • A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • 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
    • A61P25/22—Anxiolytics
    • 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
    • A61P25/24—Antidepressants
    • 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
    • A61P25/28—Drugs 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
    • 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
    • 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
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/18—Drugs for disorders of the endocrine system of the parathyroid hormones
    • A61P5/20—Drugs for disorders of the endocrine system of the parathyroid hormones for decreasing, blocking or antagonising the activity of PTH
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C51/00—Preparation of carboxylic acids or their salts, halides or anhydrides
    • C07C51/41—Preparation of salts of carboxylic acids
    • C07C51/412—Preparation of salts of carboxylic acids by conversion of the acids, their salts, esters or anhydrides with the same carboxylic acid part
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D217/00—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems
    • C07D217/02—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with only hydrogen atoms or radicals containing only carbon and hydrogen atoms, directly attached to carbon atoms of the nitrogen-containing ring; Alkylene-bis-isoquinolines
    • C07D217/04—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with only hydrogen atoms or radicals containing only carbon and hydrogen atoms, directly attached to carbon atoms of the nitrogen-containing ring; Alkylene-bis-isoquinolines with hydrocarbon or substituted hydrocarbon radicals attached to the ring nitrogen atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Psychiatry (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Diabetes (AREA)
  • Pain & Pain Management (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Hospice & Palliative Care (AREA)
  • Cardiology (AREA)
  • Psychology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Epidemiology (AREA)
  • Endocrinology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)

Abstract

SE REFIERE A UN PROCESO DE PREPARACION DEL COMPUESTO 2-(CICLOHEXILMETIL)-N-{2-[(2S)-1-METILPIRROLIDIN-2-IL]ETIL}-1,2,3,4-TETRAHIDROISOQUINOLIN-7-SULFONAMIDA QUE COMPRENDE: A) ACOPLAR (-)-2-(2-AMINOETIL)-1-METILPIRROLIDINA CON EL CLORURO DE 2-(2,2,2-TRIFLUOROACETIL)-1,2,3,4-TETRAHIDROISOQUINOLIN-7-SULFONILO PARA OBTENER 2-(2,2,2-TRIFLUOROACETIL)-N-{2-[(2S)-1-METILPIRROLIDIN-2-IL]ETIL}-1,2,3,4-TETRAHIDROISOQUINOLIN-7-SULFONAMIDA EN PRESENCIA DE UNA BASE ORGANICA O INORGANICA TAL COMO HIDROXIDO DE SODIO, TRIETILAMINA, ENTRE OTROS, Y UN DISOLVENTE INERTE; B) DESPROTEGER LA 2-(2,2,2-TRIFLUOROACETIL)-N-{2-[(2S)-1-METILPIRROLIDIN-2-IL]ETIL}-1,2,3,4-TETRAHIDROISOQUINOLIN-7-SULFONAMIDA PARA DAR N-{2-[(2S)-1-METILPIRROLIDIN-2-IL]ETIL}-1,2,3,4-TETRAHIDROISOQUINOLIN-7-SULFONAMIDA EN CONDICIONES BASICAS Y EN UN ALCOHOL; C) AMINAR DE MANERA REDUCTORA N-{2-[(2S)-1-METILPIRROLIDIN-2-IL]ETIL}-1,2,3,4-TETRAHIDROISOQUINOLIN-7-SULFONAMIDA CON CICLOHEXANOCARBOXALDEHIDO PARA FORMAR 2-(CICLOHEXILMETIL)-N-{2-[(2S)-1-METILPIRROLIDIN-2-IL]ETIL}-1,2,3,4-TETRAHIDROISOQUINOLIN-7-SULFONAMIDA EN UN DISOLVENTE ORGANICO Y EN PRESENCIA DE UN AGENTE REDUCTOR TAL COMO ACIDO FORMICO; Y D) HACER REACCIONAR 2-(CICLOHEXILMETIL)-N-{2-[(2S)-1-METILPIRROLIDIN-2-IL]ETIL}-1,2,3,4-TETRAHIDROISOQUINOLIN-7-SULFONAMIDA CON ACIDO FUMARICO PARA FORMAR EL DIFUMARATO DEL COMPUESTO. TAMBIEN SE REFIERE A UNA COMPOSICION FARMACEUTICA
PE2012001391A 2010-03-05 2011-03-04 Procedimiento para la preparacion de 2-(ciclohexilmetil)-n-{2-[(2s)-1-metilpirrolidin-2-il]etil}-1,2,3,4-tetrahidroisoquinolin-7-sulfonamida PE20130007A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US31106910P 2010-03-05 2010-03-05
FR1059750 2010-11-25

Publications (1)

Publication Number Publication Date
PE20130007A1 true PE20130007A1 (es) 2013-02-01

Family

ID=44012569

Family Applications (1)

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PE2012001391A PE20130007A1 (es) 2010-03-05 2011-03-04 Procedimiento para la preparacion de 2-(ciclohexilmetil)-n-{2-[(2s)-1-metilpirrolidin-2-il]etil}-1,2,3,4-tetrahidroisoquinolin-7-sulfonamida

Country Status (27)

Country Link
US (2) US8748615B2 (es)
EP (2) EP2556064B1 (es)
JP (2) JP2013521308A (es)
KR (2) KR20130047685A (es)
CN (2) CN103221394A (es)
AR (2) AR080374A1 (es)
AU (2) AU2011223560A1 (es)
BR (2) BR112012022234A2 (es)
CA (2) CA2789669A1 (es)
CL (2) CL2012002452A1 (es)
CO (2) CO6630129A2 (es)
CR (1) CR20120467A (es)
DO (1) DOP2012000228A (es)
EC (1) ECSP12012207A (es)
GT (1) GT201200228A (es)
IL (2) IL221341A (es)
MA (2) MA34144B1 (es)
MX (2) MX2012008422A (es)
NZ (2) NZ602009A (es)
PE (1) PE20130007A1 (es)
RU (2) RU2012142338A (es)
SG (2) SG182576A1 (es)
TN (1) TN2012000361A1 (es)
TW (2) TW201144284A (es)
UY (2) UY33263A (es)
WO (2) WO2011109680A2 (es)
ZA (1) ZA201205311B (es)

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CN102816101A (zh) * 2012-08-21 2012-12-12 江苏恒祥化工有限责任公司 一种(s)-n-甲基-2氯乙基吡咯烷的合成方法
SG11201601306QA (en) * 2013-09-09 2016-03-30 Sanofi Sa An h3 receptor antagonist combined with a cholinesterase inhibitor for use in the treatment of alzheimer's disease
WO2019070827A1 (en) * 2017-10-04 2019-04-11 Celgene Corporation PROCESSES FOR THE PREPARATION OF CIS-4 [2 - {(3S, 4R) -3-FLUOROOXAN-4-YL] AMINO) -8- (2,4,6-TRICHLOROANILINO) -9H-PURIN-9-YL] -1 -MÉTHYLCYCLOHEXANE-1-carboxamide

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JP2013521308A (ja) 2013-06-10
ZA201205311B (en) 2013-03-27
CR20120467A (es) 2012-10-05
MX2012008422A (es) 2012-08-15
NZ601498A (en) 2014-12-24
CA2787427C (en) 2017-10-10
JP2013521309A (ja) 2013-06-10
IL221341A (en) 2014-05-28
CN103221394A (zh) 2013-07-24
EP2556064A2 (en) 2013-02-13
EP2556064B1 (en) 2014-10-15
IL221341A0 (en) 2012-10-31
AU2011222588A1 (en) 2012-08-23
UY33263A (es) 2011-09-30
WO2011109680A2 (en) 2011-09-09
CL2012002452A1 (es) 2012-11-30
MX2012009413A (es) 2012-09-07
US20130137718A1 (en) 2013-05-30
KR20130038186A (ko) 2013-04-17
AU2011223560A1 (en) 2012-09-13
RU2012142338A (ru) 2014-04-10
CA2787427A1 (en) 2011-09-09
TN2012000361A1 (en) 2014-01-30
US20130123302A1 (en) 2013-05-16
WO2011109675A3 (en) 2012-11-22
CL2012002451A1 (es) 2012-11-30
UY33262A (es) 2011-09-30
BR112012022356A2 (pt) 2016-08-30
US8779145B2 (en) 2014-07-15
DOP2012000228A (es) 2013-01-15
BR112012022234A2 (pt) 2015-12-15
CO6630099A2 (es) 2013-03-01
AR080374A1 (es) 2012-04-04
GT201200228A (es) 2013-11-21
ECSP12012207A (es) 2013-03-28
CN103068815A (zh) 2013-04-24
SG183256A1 (en) 2012-09-27
CA2789669A1 (en) 2011-09-09
AR080375A1 (es) 2012-04-04
WO2011109680A3 (en) 2012-12-20
RU2012142310A (ru) 2014-04-10
IL221339A0 (en) 2012-10-31
NZ602009A (en) 2015-01-30
JP5927126B2 (ja) 2016-05-25
MA34144B1 (fr) 2013-04-03
KR101783679B1 (ko) 2017-10-10
EP2542530A2 (en) 2013-01-09
US8748615B2 (en) 2014-06-10
SG182576A1 (en) 2012-08-30
AU2011222588B2 (en) 2016-09-08
KR20130047685A (ko) 2013-05-08
TW201144285A (en) 2011-12-16
CO6630129A2 (es) 2013-03-01
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WO2011109675A2 (en) 2011-09-09
TW201144284A (en) 2011-12-16

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