BRPI0509245A - cloridrato [4-(5-aminoetil-2-flúor-fenil)-piperidina-1-il](4-bromo-3 -metil-5-propóxi-tiofeno-2-il)-metanona como um inibidor de triptase de mastócito - Google Patents

cloridrato [4-(5-aminoetil-2-flúor-fenil)-piperidina-1-il](4-bromo-3 -metil-5-propóxi-tiofeno-2-il)-metanona como um inibidor de triptase de mastócito

Info

Publication number
BRPI0509245A
BRPI0509245A BRPI0509245-0A BRPI0509245A BRPI0509245A BR PI0509245 A BRPI0509245 A BR PI0509245A BR PI0509245 A BRPI0509245 A BR PI0509245A BR PI0509245 A BRPI0509245 A BR PI0509245A
Authority
BR
Brazil
Prior art keywords
compound
formula
relates
present
aminoethyl
Prior art date
Application number
BRPI0509245-0A
Other languages
English (en)
Inventor
Zhongli Gao
Larry Davis
Julian Levell
Mark Czekaj
Adam W Sledeski
El-Bdaouil Haddad
Original Assignee
Aventis Pharma Inc
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 Aventis Pharma Inc filed Critical Aventis Pharma Inc
Publication of BRPI0509245A publication Critical patent/BRPI0509245A/pt

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    • 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
    • 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
    • A61P1/04—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
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • 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
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • 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
    • 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
    • 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
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic 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
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic 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
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis

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  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Pulmonology (AREA)
  • Diabetes (AREA)
  • Rheumatology (AREA)
  • Immunology (AREA)
  • Cardiology (AREA)
  • Neurosurgery (AREA)
  • Vascular Medicine (AREA)
  • Obesity (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Virology (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Hematology (AREA)
  • Endocrinology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Urology & Nephrology (AREA)
  • Pain & Pain Management (AREA)
  • Emergency Medicine (AREA)
  • Dermatology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

"CLORIDRATO ¢4-(5-AMINOETIL-2-FLúOR-FENIL)-PIPERIDINA-1-IL!-(4-BROMO- 3-METIL-5-PROPóXI-TIOFENO-2-IL)-METANONA COMO UM INIBIDOR DE TRIPTASE DE MASTóCITO". A presente invenção refere-se ao composto de fórmula 1, ou um pró-fármaco, um sal farmaceuticamente aceitável, ou solvato do dito composto. Ademais, a presente invenção refere-se a uma composição farmacêutica que compreende uma quantidade farmaceuticamente aceitável do composto de fórmula 1, e um veículo farmaceuticamente aceitável. Ademais, a presente invenção refere-se ao uso de um composto de fórmula l como um inibidor de triptase, que compreende introduzir o composto dentro de uma composição que compreende triptase. Ademais, a presente invenção referese ao uso de um composto de fórmula 1 para tratar um paciente que sofre de, ou está submetido a, uma condição fisiológica necessitada de melhora de um inibidor de triptase que compreende administrar ao paciente uma quantidade terapeuticamente eficaz do composto da reivindicação 1. A presente invenção refere-se à preparação de um composto de fórmula 1.
BRPI0509245-0A 2004-03-26 2005-03-24 cloridrato [4-(5-aminoetil-2-flúor-fenil)-piperidina-1-il](4-bromo-3 -metil-5-propóxi-tiofeno-2-il)-metanona como um inibidor de triptase de mastócito BRPI0509245A (pt)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US55692704P 2004-03-26 2004-03-26
PCT/US2005/009899 WO2005097780A1 (en) 2004-03-26 2005-03-24 [4-(5-aminomethyl-2-fluoro-phenyl)-piperidin-1-yl]-(4-bromo-3-methyl-5-propoxy-thiophen-2-yl)-methanone hydrochloride as an inhibitor of mast cell tryptase

Publications (1)

Publication Number Publication Date
BRPI0509245A true BRPI0509245A (pt) 2007-09-11

Family

ID=34964263

Family Applications (1)

Application Number Title Priority Date Filing Date
BRPI0509245-0A BRPI0509245A (pt) 2004-03-26 2005-03-24 cloridrato [4-(5-aminoetil-2-flúor-fenil)-piperidina-1-il](4-bromo-3 -metil-5-propóxi-tiofeno-2-il)-metanona como um inibidor de triptase de mastócito

Country Status (25)

Country Link
US (1) US20070142435A1 (pt)
EP (1) EP1737848A1 (pt)
JP (1) JP2007530580A (pt)
KR (1) KR20060130682A (pt)
CN (1) CN1956978A (pt)
AR (1) AR048336A1 (pt)
AU (1) AU2005230934A1 (pt)
BR (1) BRPI0509245A (pt)
CA (1) CA2560649A1 (pt)
CR (1) CR8603A (pt)
DO (1) DOP2005000039A (pt)
EC (1) ECSP066878A (pt)
IL (1) IL178031A0 (pt)
MA (1) MA28547B1 (pt)
MX (1) MXPA06010610A (pt)
NO (1) NO20064811L (pt)
PA (1) PA8627601A1 (pt)
PE (1) PE20060084A1 (pt)
RU (1) RU2330034C1 (pt)
TN (1) TNSN06278A1 (pt)
TW (1) TW200602035A (pt)
UA (1) UA83738C2 (pt)
UY (1) UY28821A1 (pt)
WO (1) WO2005097780A1 (pt)
ZA (1) ZA200607752B (pt)

Families Citing this family (17)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PE20071148A1 (es) * 2006-03-29 2007-12-10 Sanofi Aventis Mejoras en la preparacion de intermedios que conducen a hidrocloruro de [4-(5-aminometil-2-fluoro-fenil)-piperidin-1-il]-(4-bromo-3-metil-5-propoxi-tiofen-2-il)-metanona
AR065616A1 (es) * 2007-03-07 2009-06-17 Sanofi Aventis Sintesis regioselectiva de ullmann de acido 4- bromo-3- metil-5- propoxi- tiofeno-2- carboxilico
WO2008115912A1 (en) * 2007-03-21 2008-09-25 Sanofi-Aventis Regio-specific synthesis of 4-bromo-3-methyl-5-propoxy-thiophene-2-carboxylic acid
WO2008121666A1 (en) * 2007-03-29 2008-10-09 Sanofi-Aventis Use of 4-bromo-3-methyl-5-propoxythiophene-2-carboxylic acid 2,5-dioxo-pyrrolidin-1-yl ester for preparing the tryptase inhibitor [4-(5-aminomethyl-2-fluoro-phenyl)-piperidin-1-yl]-(4-bromo-3-methyl-5-propoxy-thiophen-2-yl)-methanone
AR065859A1 (es) * 2007-03-29 2009-07-08 Sanofi Aventis Ester de 2,5-dioxo-pirrolidin-1-ilo de acido 4-bromo-3-metil-5-propoxitiofen-2- carboxilico ,su sintesis regioespecifica y un intermedio del mismo
ES2469824T3 (es) 2007-11-21 2014-06-20 Janssen Pharmaceutica N.V. Espiropiperidinas para su uso como inhibidores de la triptasa
NZ587119A (en) * 2008-01-24 2013-01-25 Soligenix Inc Use of beclomethasone dipropionate in the treatment of an interstitial lung disease
BRPI0916920A2 (pt) * 2008-08-22 2015-11-24 Sanofi Aventis 4-(5-aminometil-2-fluoro-fenil)-piperidin-1-il]-[7-fluoro-1-(2-metóxi-etil)-4-trifluorometóxi-1h-indol-3-il]-metanona como inibidor de triptase de mastócito, seu uso e método de preparação, bem como forma cristalina
AR074776A1 (es) 2008-12-18 2011-02-09 Sanofi Aventis Metodo para tratar la degeneracion macular; modulando el sistema inmunitario del paciente
FR2955324A1 (fr) * 2010-01-15 2011-07-22 Sanofi Aventis [4-(5-aminomethyl-phenyl)-piperidin-1-yl]-1h-indol-3-yl]-methanones disubstituees
MX2012003023A (es) * 2009-09-24 2012-04-10 Sanofi Aventis Us Llc Sintesis del ester terc-butilico del acido (4-fluoro-3-piperidin-4 -il-bencil)-carbamico y sus productos intermedios.
KR20120107999A (ko) * 2009-12-23 2012-10-04 사노피 염증성 장 질환의 치료
AU2010333779A1 (en) * 2009-12-23 2012-07-12 Sanofi Indolyl-piperidinyl benzylamines as beta-tryptase inhibitors
EP2516428A1 (en) * 2009-12-23 2012-10-31 Sanofi Tropinone benzylamines as beta-tryptase inhibitors
AR080255A1 (es) * 2010-02-24 2012-03-21 Sanofi Aventis Tratamiento de afecciones alergicas dermatologicas. composicion farmaceutica
CA2851087C (en) 2011-10-07 2019-09-24 Takeda Pharmaceutical Company Limited 1-arylcarbonyl-4-oxy-piperidine compounds useful for the treatment of neurodegenerative diseases
BR112019016595A2 (pt) * 2017-02-10 2020-03-31 Genentech, Inc. Anticorpos isolados, métodos de produção do anticorpo e de tratamento de um distúrbio, ácido nucleico isolado, vetor ou conjunto de vetores, célula hospedeira, composições farmacêuticas e uso

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
OA12274A (en) * 2000-05-22 2006-05-09 Aventis Pharma Inc Arylmethylamine derivatives for use as tryptase inhibitors.
GB0012362D0 (en) * 2000-05-22 2000-07-12 Aventis Pharma Ltd Chemical compounds

Also Published As

Publication number Publication date
DOP2005000039A (es) 2005-10-31
EP1737848A1 (en) 2007-01-03
US20070142435A1 (en) 2007-06-21
MXPA06010610A (es) 2006-12-15
RU2006137717A (ru) 2008-05-10
AR048336A1 (es) 2006-04-19
CA2560649A1 (en) 2005-10-20
RU2330034C1 (ru) 2008-07-27
UA83738C2 (en) 2008-08-11
WO2005097780A1 (en) 2005-10-20
CN1956978A (zh) 2007-05-02
CR8603A (es) 2007-06-08
MA28547B1 (fr) 2007-04-03
TNSN06278A1 (en) 2007-12-03
AU2005230934A1 (en) 2005-10-20
JP2007530580A (ja) 2007-11-01
ECSP066878A (es) 2006-11-24
TW200602035A (en) 2006-01-16
KR20060130682A (ko) 2006-12-19
IL178031A0 (en) 2006-12-31
PA8627601A1 (es) 2006-01-23
NO20064811L (no) 2006-10-23
PE20060084A1 (es) 2006-03-09
UY28821A1 (es) 2005-10-31
ZA200607752B (en) 2008-05-28

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Legal Events

Date Code Title Description
B25G Requested change of headquarter approved

Owner name: AVENTIS PHARMACEUTICALS, INC. (US)

Free format text: SEDE ALTERADA CONFORME SOLICITADO NA PETICAO NO 020070165509/RJ DE 23/11/2007.

B08F Application dismissed because of non-payment of annual fees [chapter 8.6 patent gazette]

Free format text: REFERENTE AS 5A, 6A E 7A ANUIDADES.

B08K Patent lapsed as no evidence of payment of the annual fee has been furnished to inpi [chapter 8.11 patent gazette]

Free format text: REFERENTE AO DESPACHO 8.6 PUBLICADO NA RPI 2158 DE 15/05/2012.