BRPI0916920A2 - 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 - Google Patents
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 cristalinaInfo
- Publication number
- BRPI0916920A2 BRPI0916920A2 BRPI0916920A BRPI0916920A BRPI0916920A2 BR PI0916920 A2 BRPI0916920 A2 BR PI0916920A2 BR PI0916920 A BRPI0916920 A BR PI0916920A BR PI0916920 A BRPI0916920 A BR PI0916920A BR PI0916920 A2 BRPI0916920 A2 BR PI0916920A2
- Authority
- BR
- Brazil
- Prior art keywords
- fluoro
- methanone
- indol
- piperidin
- trifluoromethoxy
- Prior art date
Links
- -1 5-Aminomethyl-2-fluoro-phenyl Chemical group 0.000 title 1
- 102000001400 Tryptase Human genes 0.000 title 1
- 108060005989 Tryptase Proteins 0.000 title 1
- 229940122598 Tryptase inhibitor Drugs 0.000 title 1
- 239000002750 tryptase inhibitor Substances 0.000 title 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
- C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
- C07D211/08—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms
- C07D211/18—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms
- C07D211/26—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by nitrogen atoms
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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
- C07D401/06—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 carbon chain containing only aliphatic carbon atoms
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- 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
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/445—Non condensed piperidines, e.g. piperocaine
- A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
- A61K31/454—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
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- C—CHEMISTRY; METALLURGY
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- C07C271/06—Esters of carbamic acids
- C07C271/08—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms
- C07C271/26—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atom of at least one of the carbamate groups bound to a carbon atom of a six-membered aromatic ring
- C07C271/28—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atom of at least one of the carbamate groups bound to a carbon atom of a six-membered aromatic ring to a carbon atom of a non-condensed six-membered aromatic ring
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
- C07D209/04—Indoles; Hydrogenated indoles
- C07D209/08—Indoles; Hydrogenated indoles with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to carbon atoms of the hetero ring
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- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
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- C07D209/10—Indoles; Hydrogenated indoles with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
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- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
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- C07D209/04—Indoles; Hydrogenated indoles
- C07D209/30—Indoles; Hydrogenated indoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to carbon atoms of the hetero ring
- C07D209/42—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
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- C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D213/24—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
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- C07D213/38—Radicals substituted by singly-bound nitrogen atoms having only hydrogen or hydrocarbon radicals attached to the substituent nitrogen atom
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- C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
- C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
- C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D213/24—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
- C07D213/36—Radicals substituted by singly-bound nitrogen atoms
- C07D213/40—Acylated substituent nitrogen atom
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F7/00—Compounds containing elements of Groups 4 or 14 of the Periodic Table
- C07F7/02—Silicon compounds
- C07F7/08—Compounds having one or more C—Si linkages
- C07F7/10—Compounds having one or more C—Si linkages containing nitrogen having a Si-N linkage
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Pulmonology (AREA)
- Physical Education & Sports Medicine (AREA)
- Rheumatology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Neurology (AREA)
- Dermatology (AREA)
- Immunology (AREA)
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- Ophthalmology & Optometry (AREA)
- Biomedical Technology (AREA)
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- Heart & Thoracic Surgery (AREA)
- Oncology (AREA)
- Gastroenterology & Hepatology (AREA)
- Pain & Pain Management (AREA)
- Cardiology (AREA)
- Otolaryngology (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Plural Heterocyclic Compounds (AREA)
- Indole Compounds (AREA)
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US9101808P | 2008-08-22 | 2008-08-22 | |
US9101108P | 2008-08-22 | 2008-08-22 | |
PCT/US2009/054381 WO2010022196A2 (en) | 2008-08-22 | 2009-08-20 | [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 |
Publications (1)
Publication Number | Publication Date |
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BRPI0916920A2 true BRPI0916920A2 (pt) | 2015-11-24 |
Family
ID=41198646
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
BRPI0916920A BRPI0916920A2 (pt) | 2008-08-22 | 2009-08-20 | 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 |
Country Status (37)
Country | Link |
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US (2) | US8217178B2 (pt) |
EP (1) | EP2367812B1 (pt) |
JP (1) | JP5656834B2 (pt) |
KR (1) | KR101630217B1 (pt) |
CN (2) | CN103508936A (pt) |
AR (1) | AR073117A1 (pt) |
AU (1) | AU2009282884B8 (pt) |
BR (1) | BRPI0916920A2 (pt) |
CA (1) | CA2734877C (pt) |
CL (1) | CL2009001759A1 (pt) |
CO (1) | CO6341624A2 (pt) |
CR (1) | CR20110093A (pt) |
CY (1) | CY1117261T1 (pt) |
DK (1) | DK2367812T3 (pt) |
DO (1) | DOP2011000055A (pt) |
EC (1) | ECSP11010841A (pt) |
ES (1) | ES2556764T3 (pt) |
HK (1) | HK1156598A1 (pt) |
HR (1) | HRP20151338T1 (pt) |
HU (1) | HUE026331T2 (pt) |
IL (2) | IL211265A (pt) |
MA (1) | MA32639B1 (pt) |
MX (1) | MX2011001135A (pt) |
MY (1) | MY150599A (pt) |
NI (1) | NI201100024A (pt) |
NZ (1) | NZ591234A (pt) |
PE (1) | PE20100235A1 (pt) |
PL (1) | PL2367812T3 (pt) |
PT (1) | PT2367812E (pt) |
RS (1) | RS54413B1 (pt) |
RU (1) | RU2509766C2 (pt) |
SI (1) | SI2367812T1 (pt) |
TW (1) | TWI473613B (pt) |
UA (1) | UA104148C2 (pt) |
UY (1) | UY32069A (pt) |
WO (1) | WO2010022196A2 (pt) |
ZA (1) | ZA201100597B (pt) |
Families Citing this family (9)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
EP2367812B1 (en) | 2008-08-22 | 2015-09-16 | Sanofi | [4-(5-aminomethyl-2-fluoro-phenyl)-piperidin-1-yl]-[7-fluoro-1-(2-methoxy-ethyl)-4trifluoromethoxy-1h-indol-3-yl]methanone as an inhibitor of mast cell tryptase |
FR2955324A1 (fr) * | 2010-01-15 | 2011-07-22 | Sanofi Aventis | [4-(5-aminomethyl-phenyl)-piperidin-1-yl]-1h-indol-3-yl]-methanones disubstituees |
EP2516428A1 (en) * | 2009-12-23 | 2012-10-31 | Sanofi | Tropinone benzylamines as beta-tryptase inhibitors |
WO2011079102A1 (en) * | 2009-12-23 | 2011-06-30 | Sanofi | Indolyl-piperidinyl benzylamines as beta-tryptase inhibitors |
EP2516418B1 (en) | 2009-12-23 | 2014-05-14 | Sanofi | Prodrugs of [4[4-(5-aminomethyl-2-fluoro-phenyl)-piperidin-1-yl]-(1h-pyrrolo-pyridin-yl)-methanones and synthesis thereof |
WO2011078983A1 (en) * | 2009-12-23 | 2011-06-30 | Sanofi | Treatment for inflammatory bowel disease |
AU2011220909A1 (en) * | 2010-02-24 | 2012-09-13 | Sanofi | Treatment of dermatological allergic conditions |
EP2397074B1 (en) | 2010-06-19 | 2012-10-24 | M Stenqvist AB | A system and computer readable medium for determination of transpulmonary pressure in a patient connected to a breathing apparatus |
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. |
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US5087240A (en) * | 1983-08-18 | 1992-02-11 | Drug Delivery Systems Inc. | Transdermal drug patch with conductive fibers |
US4921475A (en) * | 1983-08-18 | 1990-05-01 | Drug Delivery Systems Inc. | Transdermal drug patch with microtubes |
US4879119A (en) * | 1984-02-21 | 1989-11-07 | Yamanouchi Pharmaceutical Co., Ltd. | Patch |
NL8720442A (nl) * | 1986-08-18 | 1989-04-03 | Clinical Technologies Ass | Afgeefsystemen voor farmacologische agentia. |
US5163899A (en) * | 1987-03-20 | 1992-11-17 | Drug Delivery Systems Inc. | Transdermal drug delivery system |
US5312325A (en) * | 1987-05-28 | 1994-05-17 | Drug Delivery Systems Inc | Pulsating transdermal drug delivery system |
GB8804164D0 (en) * | 1988-02-23 | 1988-03-23 | Tucker J M | Bandage for administering physiologically active compound |
US5008110A (en) * | 1988-11-10 | 1991-04-16 | The Procter & Gamble Company | Storage-stable transdermal patch |
US5088977A (en) * | 1988-12-21 | 1992-02-18 | Drug Delivery Systems Inc. | Electrical transdermal drug applicator with counteractor and method of drug delivery |
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EP2367812B1 (en) | 2008-08-22 | 2015-09-16 | Sanofi | [4-(5-aminomethyl-2-fluoro-phenyl)-piperidin-1-yl]-[7-fluoro-1-(2-methoxy-ethyl)-4trifluoromethoxy-1h-indol-3-yl]methanone as an inhibitor of mast cell tryptase |
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