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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Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/06Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/02Stomatological preparations, e.g. drugs for caries, aphtae, periodontitis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/06Antiasthmatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • 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
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • 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
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/08Antiallergic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs 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

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
AR065858A1 (es) * 2007-03-29 2009-07-08 Sanofi Aventis Metodo para preparar el inhibidor de triptasa [ 4-(5-aminoetil-2-fluoro-fenil)-piperidin-1-il]-(4-bromo-3-metil-5-propoxi-tiofen-2-il)-metanona.
WO2008121669A1 (en) * 2007-03-29 2008-10-09 Sanofi-Aventis 4-bromo-3-methyl-5-propoxythiophene-2-carboxylic acid 2,5-dioxo-pyrrolidin-1-yl ester, its regio-specific synthesis and intermediate thereto
EP2224803B1 (en) * 2007-11-21 2014-04-02 Janssen Pharmaceutica N.V. Spiropiperidines for use as tryptase inhibitors
WO2009094641A2 (en) 2008-01-24 2009-07-30 Dor Biopharma, Inc. Topically active steroids for use in interstitial pulmonary fibrosis
PT2367812E (pt) * 2008-08-22 2016-01-20 Sanofi Sa [4-(5-aminometil-2-fluoro-fenil)-piperidin-1-il]-[7-fluoro-1-(2-metoxi-etil)-4-trifluorometoxi-1h-indol-3-il]metanona como um inibidor da triptase de mastócitos
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
JP2013505935A (ja) 2009-09-24 2013-02-21 サノフィ−アベンティス・ユー・エス・エルエルシー (4−フルオロ−3−ピペリジン−4−イル−ベンジル)−カルバミン酸tert−ブチルエステルの合成及びその中間体
MX2012006741A (es) * 2009-12-23 2012-07-04 Sanofi Sa Tratamiento para la enfermedad inflamatoria del intestino.
JP2013515724A (ja) * 2009-12-23 2013-05-09 サノフイ ベータ−トリプターゼ阻害剤としてのトロピノンベンジルアミン類
CN102770425A (zh) * 2009-12-23 2012-11-07 赛诺菲 用作β-类胰蛋白酶抑制剂的吲哚基-哌啶基苄胺类化合物
JP2013520506A (ja) * 2010-02-24 2013-06-06 サノフイ 皮膚科学的なアレルギー状態の治療
MX360706B (es) 2011-10-07 2018-11-14 Takeda Pharmaceuticals Co Compuestos de 1-arilcarbonil-4-oxi-piperidina utiles para el tratamiento de enfermedades neurodegenerativas.
RU2771485C2 (ru) * 2017-02-10 2022-05-04 Дженентек, Инк. Антитела против триптазы, их композиции и применения

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB0012362D0 (en) * 2000-05-22 2000-07-12 Aventis Pharma Ltd Chemical compounds
CA2409827C (en) * 2000-05-22 2010-06-01 Aventis Pharmaceuticals Products Inc. Arylmethylamine derivatives for use as tryptase inhibitors

Also Published As

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

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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.