AR073117A1 - Derivado de aminometil-fenil-piperidin-1-il-indolil-metanona, inhibidores de la triptasa de mastocitos, composiciones farmaceuticas que lo contienen, metodo de preparacion, compuestos intermediarios y uso del compuesto en el tratamiento de procesos inflamatorios. - Google Patents
Derivado de aminometil-fenil-piperidin-1-il-indolil-metanona, inhibidores de la triptasa de mastocitos, composiciones farmaceuticas que lo contienen, metodo de preparacion, compuestos intermediarios y uso del compuesto en el tratamiento de procesos inflamatorios.Info
- Publication number
- AR073117A1 AR073117A1 ARP090103234A ARP090103234A AR073117A1 AR 073117 A1 AR073117 A1 AR 073117A1 AR P090103234 A ARP090103234 A AR P090103234A AR P090103234 A ARP090103234 A AR P090103234A AR 073117 A1 AR073117 A1 AR 073117A1
- Authority
- AR
- Argentina
- Prior art keywords
- mastocyt
- triptase
- aminometil
- indolil
- metanone
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 title abstract 7
- 239000003112 inhibitor Substances 0.000 title 1
- 238000000034 method Methods 0.000 title 1
- 239000008194 pharmaceutical composition Substances 0.000 title 1
- 238000002360 preparation method Methods 0.000 title 1
- 150000003839 salts Chemical class 0.000 abstract 3
- WPYMKLBDIGXBTP-UHFFFAOYSA-N benzoic acid Chemical group OC(=O)C1=CC=CC=C1 WPYMKLBDIGXBTP-UHFFFAOYSA-N 0.000 abstract 1
- 238000000634 powder X-ray diffraction Methods 0.000 abstract 1
- 229940002612 prodrug Drugs 0.000 abstract 1
- 239000000651 prodrug Substances 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
- 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
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- 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
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C271/00—Derivatives of carbamic acids, i.e. compounds containing any of the groups, the nitrogen atom not being part of nitro or nitroso groups
- 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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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
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- 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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- C07D213/02—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
- C07D213/38—Radicals substituted by singly-bound nitrogen atoms having only hydrogen or hydrocarbon radicals attached to the substituent nitrogen atom
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- C07D213/02—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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- 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pulmonology (AREA)
- Physical Education & Sports Medicine (AREA)
- Rheumatology (AREA)
- Dermatology (AREA)
- Ophthalmology & Optometry (AREA)
- Immunology (AREA)
- Biomedical Technology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Communicable Diseases (AREA)
- Gastroenterology & Hepatology (AREA)
- Pain & Pain Management (AREA)
- Cardiology (AREA)
- Oncology (AREA)
- Hospice & Palliative Care (AREA)
- Heart & Thoracic Surgery (AREA)
- Otolaryngology (AREA)
- Virology (AREA)
- Psychiatry (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Indole Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Abstract
Reivindicacion 1: Un compuesto de formula 1: o un profármaco, sal farmacéuticamente aceptable o solvato del mismo. Reivindicacion 2: El compuesto de la reivindicacion 1 en forma de una sal farmacéuticamente aceptable del mismo. Reivindicacion 14: El compuesto de acuerdo con la reivindicacion 3, en el que la sal es benzoato. Reivindicacion 15: Una forma cristalina A del compuesto de acuerdo con la reivindicacion 14. Reivindicacion 16: Una forma cristalina del compuesto de acuerdo con la reivindicacion 14, donde la forma cristalina tiene picos de XRPD a al menos dos de los siguientes ángulos 2 theta: 7,75, 10,13, 17,03, 17,16, 18,39, 21,33, y 21,88.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US9101808P | 2008-08-22 | 2008-08-22 | |
US9101108P | 2008-08-22 | 2008-08-22 |
Publications (1)
Publication Number | Publication Date |
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AR073117A1 true AR073117A1 (es) | 2010-10-13 |
Family
ID=41198646
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
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ARP090103234A AR073117A1 (es) | 2008-08-22 | 2009-08-21 | Derivado de aminometil-fenil-piperidin-1-il-indolil-metanona, inhibidores de la triptasa de mastocitos, composiciones farmaceuticas que lo contienen, metodo de preparacion, compuestos intermediarios y uso del compuesto en el tratamiento de procesos inflamatorios. |
Country Status (37)
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US (2) | US8217178B2 (es) |
EP (1) | EP2367812B1 (es) |
JP (1) | JP5656834B2 (es) |
KR (1) | KR101630217B1 (es) |
CN (2) | CN103508936A (es) |
AR (1) | AR073117A1 (es) |
AU (1) | AU2009282884B8 (es) |
BR (1) | BRPI0916920A2 (es) |
CA (1) | CA2734877C (es) |
CL (1) | CL2009001759A1 (es) |
CO (1) | CO6341624A2 (es) |
CR (1) | CR20110093A (es) |
CY (1) | CY1117261T1 (es) |
DK (1) | DK2367812T3 (es) |
DO (1) | DOP2011000055A (es) |
EC (1) | ECSP11010841A (es) |
ES (1) | ES2556764T3 (es) |
HK (1) | HK1156598A1 (es) |
HR (1) | HRP20151338T1 (es) |
HU (1) | HUE026331T2 (es) |
IL (2) | IL211265A (es) |
MA (1) | MA32639B1 (es) |
MX (1) | MX2011001135A (es) |
MY (1) | MY150599A (es) |
NI (1) | NI201100024A (es) |
NZ (1) | NZ591234A (es) |
PE (1) | PE20100235A1 (es) |
PL (1) | PL2367812T3 (es) |
PT (1) | PT2367812E (es) |
RS (1) | RS54413B1 (es) |
RU (1) | RU2509766C2 (es) |
SI (1) | SI2367812T1 (es) |
TW (1) | TWI473613B (es) |
UA (1) | UA104148C2 (es) |
UY (1) | UY32069A (es) |
WO (1) | WO2010022196A2 (es) |
ZA (1) | ZA201100597B (es) |
Families Citing this family (9)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
MY150599A (en) | 2008-08-22 | 2014-01-30 | 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 |
FR2955324A1 (fr) * | 2010-01-15 | 2011-07-22 | Sanofi Aventis | [4-(5-aminomethyl-phenyl)-piperidin-1-yl]-1h-indol-3-yl]-methanones disubstituees |
MX2012006805A (es) * | 2009-12-23 | 2012-07-10 | Sanofi Sa | Indolil-piperidinil bencilaminas como inhibidores de beta-triptasa. |
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 |
ES2481790T3 (es) * | 2009-12-23 | 2014-07-31 | Sanofi | Profármacos de [4[4-(5-aminometil-2-fluoro-fenil)-piperidin-1-il]-(1H-pirrolo-piridin-il)-metanonas y síntesis de los mismos |
JP2013515723A (ja) * | 2009-12-23 | 2013-05-09 | サノフイ | 炎症性腸疾患の処置 |
KR20130009769A (ko) * | 2010-02-24 | 2013-01-23 | 사노피 | 피부과 알레르기성 병태의 치료 |
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 |
US9193709B2 (en) | 2011-10-07 | 2015-11-24 | Takeda Pharmaceutical Company Limited | 1-arylcarbonyl-4-oxy-piperidine compounds useful for the treatment of neurodegenerative diseases |
Family Cites Families (23)
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US4921475A (en) * | 1983-08-18 | 1990-05-01 | Drug Delivery Systems Inc. | Transdermal drug patch with microtubes |
US5087240A (en) * | 1983-08-18 | 1992-02-11 | Drug Delivery Systems Inc. | Transdermal drug patch with conductive fibers |
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