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 mastócitoInfo
- 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
Links
- 229940122598 Tryptase inhibitor Drugs 0.000 title abstract 3
- 239000002750 tryptase inhibitor Substances 0.000 title abstract 3
- 102000001400 Tryptase Human genes 0.000 title abstract 2
- 108060005989 Tryptase Proteins 0.000 title abstract 2
- -1 [4- (5-Aminoethyl-2-fluoro-phenyl) -piperidin-1-yl] (4-bromo-3-methyl-5-propoxy-thiophen-2-yl) -methanone hydrochloride Chemical compound 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 8
- 239000003937 drug carrier Substances 0.000 abstract 1
- 210000003630 histaminocyte Anatomy 0.000 abstract 1
- 239000003112 inhibitor Substances 0.000 abstract 1
- 239000000203 mixture Substances 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 230000004962 physiological condition Effects 0.000 abstract 1
- 239000000651 prodrug Substances 0.000 abstract 1
- 229940002612 prodrug Drugs 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 239000012453 solvate Substances 0.000 abstract 1
Classifications
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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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Pulmonology (AREA)
- Diabetes (AREA)
- Rheumatology (AREA)
- Immunology (AREA)
- Neurology (AREA)
- Dermatology (AREA)
- Virology (AREA)
- Communicable Diseases (AREA)
- Oncology (AREA)
- Vascular Medicine (AREA)
- Emergency Medicine (AREA)
- Endocrinology (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Biomedical Technology (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Pain & Pain Management (AREA)
- Neurosurgery (AREA)
- Ophthalmology & Optometry (AREA)
- Gastroenterology & Hepatology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Physical Education & Sports Medicine (AREA)
- Urology & Nephrology (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.
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)
| 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 |
| 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 |
| US8158792B2 (en) | 2007-11-21 | 2012-04-17 | Janssen Pharmaceutica N.V. | Spiropiperidines for use as tryptase inhibitors |
| NZ587119A (en) * | 2008-01-24 | 2013-01-25 | Soligenix Inc | Use of beclomethasone dipropionate in the treatment of an interstitial lung disease |
| RS54413B1 (sr) * | 2008-08-22 | 2016-04-28 | Sanofi | [4-(5-aminometil-2-fluoro-fenil)-piperidin-1-il]-[7-fluoro-1-(2-metoksi-etil)-4trifluorometoksi-1h-indol-3-il]metanon kao inhibitor triptaze iz mastocita |
| TW201034675A (en) | 2008-12-18 | 2010-10-01 | Sanofi Aventis | Method for treating macular degeneration |
| FR2955324A1 (fr) * | 2010-01-15 | 2011-07-22 | Sanofi Aventis | [4-(5-aminomethyl-phenyl)-piperidin-1-yl]-1h-indol-3-yl]-methanones disubstituees |
| SG179201A1 (en) | 2009-09-24 | 2012-05-30 | Sanofi Aventis Us Llc | Synthesis of (4-fluoro-3-piperidin-4-yl-benzyl)-carbamic acid tert-butyl ester and intermediates thereof |
| JP2013515733A (ja) * | 2009-12-23 | 2013-05-09 | サノフイ | β−トリプターゼインヒビターとしてのインドリル−ピペリジニルベンジルアミン |
| 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 |
| KR20120107999A (ko) * | 2009-12-23 | 2012-10-04 | 사노피 | 염증성 장 질환의 치료 |
| TW201141478A (en) * | 2010-02-24 | 2011-12-01 | Sanofi Aventis | Treatment of dermatological allergic conditions |
| 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. |
| EP3580240A1 (en) * | 2017-02-10 | 2019-12-18 | H. Hoffnabb-La Roche Ag | Anti-tryptase antibodies, compositions thereof, and uses thereof |
Family Cites Families (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| IL152830A0 (en) * | 2000-05-22 | 2003-06-24 | Aventis Pharma Inc | Arylmethylamine derivatives for use as tryptase inhibitors |
| GB0012362D0 (en) * | 2000-05-22 | 2000-07-12 | Aventis Pharma Ltd | Chemical compounds |
-
2005
- 2005-03-21 DO DO2005000039A patent/DOP2005000039A/es unknown
- 2005-03-22 PE PE2005000325A patent/PE20060084A1/es not_active Application Discontinuation
- 2005-03-23 UY UY28821A patent/UY28821A1/es unknown
- 2005-03-23 AR ARP050101170A patent/AR048336A1/es not_active Application Discontinuation
- 2005-03-24 MX MXPA06010610A patent/MXPA06010610A/es not_active Application Discontinuation
- 2005-03-24 JP JP2007505191A patent/JP2007530580A/ja not_active Abandoned
- 2005-03-24 UA UAA200611261A patent/UA83738C2/ru unknown
- 2005-03-24 CN CNA2005800164250A patent/CN1956978A/zh active Pending
- 2005-03-24 BR BRPI0509245-0A patent/BRPI0509245A/pt not_active IP Right Cessation
- 2005-03-24 AU AU2005230934A patent/AU2005230934A1/en not_active Abandoned
- 2005-03-24 WO PCT/US2005/009899 patent/WO2005097780A1/en not_active Ceased
- 2005-03-24 CA CA002560649A patent/CA2560649A1/en not_active Abandoned
- 2005-03-24 EP EP05731154A patent/EP1737848A1/en not_active Withdrawn
- 2005-03-24 KR KR1020067019886A patent/KR20060130682A/ko not_active Withdrawn
- 2005-03-24 RU RU2006137717/04A patent/RU2330034C1/ru not_active IP Right Cessation
- 2005-03-25 TW TW094109209A patent/TW200602035A/zh unknown
- 2005-03-28 PA PA20058627601A patent/PA8627601A1/es unknown
-
2006
- 2006-09-07 CR CR8603A patent/CR8603A/es not_active Application Discontinuation
- 2006-09-12 IL IL178031A patent/IL178031A0/en unknown
- 2006-09-12 TN TNP2006000278A patent/TNSN06278A1/en unknown
- 2006-09-14 US US11/520,998 patent/US20070142435A1/en active Granted
- 2006-09-15 ZA ZA200607752A patent/ZA200607752B/en unknown
- 2006-09-22 EC EC2006006878A patent/ECSP066878A/es unknown
- 2006-10-20 MA MA29405A patent/MA28547B1/fr unknown
- 2006-10-23 NO NO20064811A patent/NO20064811L/no not_active Application Discontinuation
Also Published As
| Publication number | Publication date |
|---|---|
| PE20060084A1 (es) | 2006-03-09 |
| NO20064811L (no) | 2006-10-23 |
| RU2330034C1 (ru) | 2008-07-27 |
| MA28547B1 (fr) | 2007-04-03 |
| CA2560649A1 (en) | 2005-10-20 |
| AU2005230934A1 (en) | 2005-10-20 |
| RU2006137717A (ru) | 2008-05-10 |
| DOP2005000039A (es) | 2005-10-31 |
| EP1737848A1 (en) | 2007-01-03 |
| AR048336A1 (es) | 2006-04-19 |
| PA8627601A1 (es) | 2006-01-23 |
| ECSP066878A (es) | 2006-11-24 |
| WO2005097780A1 (en) | 2005-10-20 |
| MXPA06010610A (es) | 2006-12-15 |
| UY28821A1 (es) | 2005-10-31 |
| CN1956978A (zh) | 2007-05-02 |
| TW200602035A (en) | 2006-01-16 |
| IL178031A0 (en) | 2006-12-31 |
| US20070142435A1 (en) | 2007-06-21 |
| KR20060130682A (ko) | 2006-12-19 |
| UA83738C2 (en) | 2008-08-11 |
| TNSN06278A1 (en) | 2007-12-03 |
| CR8603A (es) | 2007-06-08 |
| JP2007530580A (ja) | 2007-11-01 |
| 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. |