[go: up one dir, main page]

AR065858A1 - METHOD FOR PREPARING THE TRIPTASE INHIBITOR [4- (5-AMINOETIL-2-FLUORO-PHENYL) -PIPERIDIN-1-IL] - (4-BROMO-3-METHYL-5-PROPOXI-TIOFEN-2-IL) -METANONE . - Google Patents

METHOD FOR PREPARING THE TRIPTASE INHIBITOR [4- (5-AMINOETIL-2-FLUORO-PHENYL) -PIPERIDIN-1-IL] - (4-BROMO-3-METHYL-5-PROPOXI-TIOFEN-2-IL) -METANONE .

Info

Publication number
AR065858A1
AR065858A1 ARP080101260A ARP080101260A AR065858A1 AR 065858 A1 AR065858 A1 AR 065858A1 AR P080101260 A ARP080101260 A AR P080101260A AR P080101260 A ARP080101260 A AR P080101260A AR 065858 A1 AR065858 A1 AR 065858A1
Authority
AR
Argentina
Prior art keywords
piperidin
bromo
methyl
fluoro
phenyl
Prior art date
Application number
ARP080101260A
Other languages
Spanish (es)
Original Assignee
Sanofi Aventis
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 Sanofi Aventis filed Critical Sanofi Aventis
Publication of AR065858A1 publication Critical patent/AR065858A1/en

Links

Classifications

    • 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
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • 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
    • A61P11/08—Bronchodilators

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Pulmonology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

Reivindicacion 1: Procedimiento para preparar [4-(5-aminometil-2-fluoro-fenil)-piperidin-1il]-(4-bromo-3-metil-5-propoxi-tiofen-2-il)-meta nona que comprende acoplar por imitacion el éster de2,5-dioxo-pirrolidin-1-ilo de ácido 4-bromo-3-metil-5-propoxitiofeno-2-carboxílico con hidrocloruro de 2,2,2-trifluoro-N-(4-fluoro-3-piperidin-4-il-bencil)-acetamida y una base fuerte o una base amina terciaria en un disolvente alcoholico para producir 2,2,2-trifluoro-N-{3-[1-(4-Bromo-3-metil-5-propoxi-tiofeno-2-carbonil)-piperidin-4-il]-4-fluoro-bencil}-acetamida y desproteger la 2,2,2-trifluoro-N-{3-[1-(4-Bromo-3-metil-5-propoxi-tiofeno-2-carbonil)-piperidin-4-il]-4-fluro-bencil}-acetamida con una base para producir [4-(5-aminometil-2-fluoro-fenil)-piperidin-1-il]-(4-bromo -3-metil-5-propoxy-thiophen-2-il)-metanonaClaim 1: Process for preparing [4- (5-aminomethyl-2-fluoro-phenyl) -piperidin-1yl] - (4-bromo-3-methyl-5-propoxy-thiophene-2-yl) -meta nona comprising Coupling by imitation the 2,5-dioxo-pyrrolidin-1-yl ester of 4-bromo-3-methyl-5-propoxythiophene-2-carboxylic acid with 2,2,2-trifluoro-N- (4-fluoro) hydrochloride -3-piperidin-4-yl-benzyl) -acetamide and a strong base or a tertiary amine base in an alcohol solvent to produce 2,2,2-trifluoro-N- {3- [1- (4-Bromo-3 -methyl-5-propoxy-thiophene-2-carbonyl) -piperidin-4-yl] -4-fluoro-benzyl} -acetamide and deprotect 2,2,2-trifluoro-N- {3- [1- (4 -Bromo-3-methyl-5-propoxy-thiophene-2-carbonyl) -piperidin-4-yl] -4-fluro-benzyl} -acetamide with a base to produce [4- (5-aminomethyl-2-fluoro- phenyl) -piperidin-1-yl] - (4-bromo -3-methyl-5-propoxy-thiophen-2-yl) -methanone

ARP080101260A 2007-03-29 2008-03-27 METHOD FOR PREPARING THE TRIPTASE INHIBITOR [4- (5-AMINOETIL-2-FLUORO-PHENYL) -PIPERIDIN-1-IL] - (4-BROMO-3-METHYL-5-PROPOXI-TIOFEN-2-IL) -METANONE . AR065858A1 (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US90884407P 2007-03-29 2007-03-29

Publications (1)

Publication Number Publication Date
AR065858A1 true AR065858A1 (en) 2009-07-08

Family

ID=39535396

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP080101260A AR065858A1 (en) 2007-03-29 2008-03-27 METHOD FOR PREPARING THE TRIPTASE INHIBITOR [4- (5-AMINOETIL-2-FLUORO-PHENYL) -PIPERIDIN-1-IL] - (4-BROMO-3-METHYL-5-PROPOXI-TIOFEN-2-IL) -METANONE .

Country Status (3)

Country Link
AR (1) AR065858A1 (en)
TW (1) TW200904811A (en)
WO (1) WO2008121666A1 (en)

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2010022196A2 (en) * 2008-08-22 2010-02-25 Sanofi-Aventis [4-(5-aminomethyl-2-fluoro-phenyl)-piperidin-1-yl]-[7-fluoro-1-(2-methoxy-ethyl)-4-trifluoromethoxy-1h-indol-3-yl]-methanone as an inhibitor of mast cell tryptase
GB0905955D0 (en) 2009-04-06 2009-05-20 Respivert Ltd Novel compounds
JP5787977B2 (en) 2010-04-08 2015-09-30 レスピバート・リミテツド P38 MAP kinase inhibitor
WO2011158044A2 (en) 2010-06-17 2011-12-22 Respivert Limited Respiratory formulations and compounds for use therein

Family Cites Families (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DOP2005000039A (en) * 2004-03-26 2005-10-31 Aventis Pharma Inc HYDROCHLORIDE OF [4- (5-AMINOMETIL-2-FLUORO-PHENYL) - PIPERIDIN-1-IL] - (4-BOMO-3-METHYL-5-PROPOXI-TIOFEN-2-IL) -METANONE AS AN INHIBITOR OF THE MASTOCYT TRIPTASE

Also Published As

Publication number Publication date
WO2008121666A1 (en) 2008-10-09
TW200904811A (en) 2009-02-01

Similar Documents

Publication Publication Date Title
ECSP18063798A (en) AN AMORPHOUS FORM AND A GENZ 112638 HEMITARTRATE CRYSTALLINE AS A GLUCOSYLCERAMIDE SYNTHASE INHIBITOR
BRPI0911273A2 (en) dpp-iv inhibitor combined with another antidiabetic agent, tablets comprising such formulations, their use and process for their preparation
CR9875A (en) DIPEPTIDYL PEPTIDASE INHIBITORS TO TREAT DIABETES
BRPI0513199A (en) organic compounds
AR060648A1 (en) CRYSTAL FORMS OF A CARBAMOIL ETIL PIPERIDINE DIMETHYLENE COMPOUND
ECSP11010825A (en) DABIGATRAN FOR PERCUTANEOUS INTERVENTIONAL CARDIAC CATHETERING.
CL2010001588A1 (en) Process for preparing nodules comprising polymorph i of dabigatran etexilate prothrombin methanesulfonate inhibitor; process for preparing a suspension comprising dabigatran ethtexilate methanesulfonate used in the preparation of the nodules.
CO6290644A2 (en) KAPPA SELECTIVE OPIOID RECEIVER ANTAGONIST.
HUE038158T2 (en) Deuterated benzoquinolizine derivatives as vesicular monoamine transporter-2 inhibitors
BRPI0513864A (en) compounds, process for their manufacture, pharmaceutical compositions comprising them, their use and method for the treatment and / or prophylaxis of diseases
ATE448217T1 (en) SUBSTITUTED PIPERIDINES AS RENIN INHIBITORS
CL2007001584A1 (en) Pharmaceutical composition comprising: a nucleus with phenylephrine in the form of immediate release and an erodible layer comprising phenylephrine and a sustained-release matrix; Useful to treat symptoms of cold, influenza, allergies or non-allergic rhinitis.
CL2009000256A1 (en) Substituted phenyl imidazolines, pharmaceutical composition containing these compounds and their use in metabolic syndrome, obesity, diabetes, stein-leventhal syndrome, CNS disorders, schizophrenia, Alzheimer's, alcohol dependence and nicotine dependence.
AR053336A1 (en) CRYSTAL FORMS OF A BIFENYL COMPOUND
AR065858A1 (en) METHOD FOR PREPARING THE TRIPTASE INHIBITOR [4- (5-AMINOETIL-2-FLUORO-PHENYL) -PIPERIDIN-1-IL] - (4-BROMO-3-METHYL-5-PROPOXI-TIOFEN-2-IL) -METANONE .
AR067813A1 (en) PHENILENDIAMINS REPLACED AS INHIBITORS OF L AINTERACTION BETWEEN MDM2 AND P53
CO6361993A2 (en) COMPOUNDS OF 4- [2- (2-FLUOROPHENOXIMETHYL) PHENYL] PIPERIDINE
ECSP088138A (en) NEW PROCEDURE TO PREPARE TIOTROPE SALTS
HUE048798T2 (en) Method for preparing 1-(4-(4-(3,4-dichloro-2-fluorophenylamino)-7-methoxyquinazolin-6-yloxy)piperidin-1-yl)-prop-2-en-1-one hydrochloride and intermediates used therein
DK1811957T3 (en) Solid pharmaceutical composition comprising donepezil hydrochloride
EP2004190A4 (en) METHOD AND FORMULATIONS USING OPIOID ANALGESICS OTHER THAN CODEIN
BR112012013319A8 (en) azacyclic spiro derivatives
DK1982190T3 (en) Pharmaceutical composition book methods for vaccination against disseminated candidiasis and other infectious agents
SMT201400033B (en) Cxcr1 / 2 inhibitors as adjuvants in pancreatic islet transplantation
TW200604173A (en) Novel compounds

Legal Events

Date Code Title Description
FA Abandonment or withdrawal