AR022220A1 - DERIVATIVES OF THE IMIDAZO [4,5-C] -PIRIDIN-4-ONA, A PROCEDURE FOR THEIR PREPARATION, THE USE OF THE SAME TO PREPARE A MEDICINAL PRODUCT, THE MEDICINAL BASE OF THESE COMPOUNDS, THE PHARMACEUTICAL COMPOSITIONS CONTAINING THESE COMPOUNDS AND ONE PROCEDURE TO PREPARE THESE FA COMPOSITIONS - Google Patents
DERIVATIVES OF THE IMIDAZO [4,5-C] -PIRIDIN-4-ONA, A PROCEDURE FOR THEIR PREPARATION, THE USE OF THE SAME TO PREPARE A MEDICINAL PRODUCT, THE MEDICINAL BASE OF THESE COMPOUNDS, THE PHARMACEUTICAL COMPOSITIONS CONTAINING THESE COMPOUNDS AND ONE PROCEDURE TO PREPARE THESE FA COMPOSITIONSInfo
- Publication number
- AR022220A1 AR022220A1 ARP000100062A ARP000100062A AR022220A1 AR 022220 A1 AR022220 A1 AR 022220A1 AR P000100062 A ARP000100062 A AR P000100062A AR P000100062 A ARP000100062 A AR P000100062A AR 022220 A1 AR022220 A1 AR 022220A1
- Authority
- AR
- Argentina
- Prior art keywords
- formula
- compounds
- prepare
- procedure
- derivatives
- Prior art date
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Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/12—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains three hetero rings
- C07D471/14—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
-
- 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
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
- A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
-
- 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)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Public Health (AREA)
- Engineering & Computer Science (AREA)
- Rheumatology (AREA)
- Pain & Pain Management (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Urology & Nephrology (AREA)
- Vascular Medicine (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Abstract
Los derivados de la imidazo[4,5-c]-piridin-4-ona, de formula (1), en donde: R representa H, alquilo C1-6 de cadena recta o ramificada o cicloalquilo C3-6;R1 representa Ar; R2 representa Ar; R3 representa H, R, R4, Hal, CN, COOH, COOA o CONH2; Ar yAr representan independientemente fenilo, naftilo o bifenilo nosustituido o mono, di o trisustituido con R, OH, Hal, CN, NO2, CF3, NH2, NHR, NR2, pirrolidin-1-ilo, piperidin-1-ilo, benciloxi, SO2NH2, SO2NHR, SO2NR2,-CONHR, -CONR2, -(CH2)n-NH2,-(CH2)n- NHR, -(CH2)n-NR2, -O-(CH2)n-NH2, -O-(CH2)n-NHR, -O-(CH2)n-NR2, R4 o sustituido en forma conjunta con -O-(CH2)m-O-, oisoquinoleinilo sustituido con NH2; R4 representa -C(=NH)-NH2, -NH-C(=NH)-NH2 o -C(=O)-N=C(NH2)2 no sustituido omonosustituido con -C OR, -COOR, -OH o con ungrupo protector de amino convencional, un compuesto de formula (2) o formula (3); A representa alquilo C1-4; Hal representa F, Cl, Br o I; m es 1 o 2; y n es 0o 1. Un procedimiento para preparar losderivados de la imidazo[4,5- c]-piridin-4-ona, de formula (1), en la cual: a) se los libera de uno de sus derivadosfuncionales por tratamiento con un agente de sovolisis o hidrogenolisis, o b) en un compuesto de formula (1) se transforma(n) uno ovarios restos R, R1, R2 y/oR3 en uno o varios restos R, R1, R2 y/o R3 diferentes, y/o c) se transforma una base o un ácido de formula (1) en una de sus sales. El empleo de los compuestosde formula (1) y/o de una de sus sales aceptables desde elpunto de vista patologico para prepar ar un medicamento destinado a la profilaxis y/o terapia de lasenfermedades tromboembolicas. Los compuestos de formula (1) son inhibidores del factor de coagulacion Xa.Derivatives of the imidazo [4,5-c] -pyridin-4-one, of formula (1), wherein: R represents H, straight or branched C1-6 alkyl or C3-6 cycloalkyl; R1 represents Ar ; R2 represents Ar; R3 represents H, R, R4, Hal, CN, COOH, COOA or CONH2; Ar and Ar independently represent phenyl, naphthyl or biphenyl substituted or mono, di or trisubstituted with R, OH, Hal, CN, NO2, CF3, NH2, NHR, NR2, pyrrolidin-1-yl, piperidin-1-yl, benzyloxy, SO2NH2 , SO2NHR, SO2NR2, -CONHR, -CONR2, - (CH2) n-NH2, - (CH2) n- NHR, - (CH2) n-NR2, -O- (CH2) n-NH2, -O- (CH2 ) n-NHR, -O- (CH2) n-NR2, R4 or jointly substituted with -O- (CH2) mO-, oisoquinoline substituted with NH2; R4 represents -C (= NH) -NH2, -NH-C (= NH) -NH2 or -C (= O) -N = C (NH2) 2 unsubstituted or substituted with -C OR, -COOR, -OH or with a conventional amino protecting group, a compound of formula (2) or formula (3); A represents C1-4 alkyl; Hal represents F, Cl, Br or I; m is 1 or 2; and n is 0o 1. A process for preparing the imidazo [4,5- c] -pyridin-4-one derivatives of formula (1), in which: a) they are released from one of their functional derivatives by treatment with a sovolysis or hydrogenolysis agent, or b) in a compound of formula (1) is transformed (n) one ovarian R, R1, R2 and / or R3 moieties into one or more different R, R1, R2 and / or R3 moieties, and / oc) a base or an acid of formula (1) is transformed into one of its salts. The use of the compounds of formula (1) and / or one of its acceptable salts from the pathological point of view to prepare a medicament for the prophylaxis and / or therapy of thromboembolic diseases. The compounds of formula (1) are inhibitors of coagulation factor Xa.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| DE19900471A DE19900471A1 (en) | 1999-01-08 | 1999-01-08 | Imidazo [4,5c] pyridin-4-one derivatives |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR022220A1 true AR022220A1 (en) | 2002-09-04 |
Family
ID=7893790
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP000100062A AR022220A1 (en) | 1999-01-08 | 2000-01-07 | DERIVATIVES OF THE IMIDAZO [4,5-C] -PIRIDIN-4-ONA, A PROCEDURE FOR THEIR PREPARATION, THE USE OF THE SAME TO PREPARE A MEDICINAL PRODUCT, THE MEDICINAL BASE OF THESE COMPOUNDS, THE PHARMACEUTICAL COMPOSITIONS CONTAINING THESE COMPOUNDS AND ONE PROCEDURE TO PREPARE THESE FA COMPOSITIONS |
Country Status (16)
| Country | Link |
|---|---|
| EP (1) | EP1149099A2 (en) |
| JP (1) | JP2002534429A (en) |
| KR (1) | KR20010086085A (en) |
| CN (1) | CN1333772A (en) |
| AR (1) | AR022220A1 (en) |
| AU (1) | AU3041700A (en) |
| BR (1) | BR9916774A (en) |
| CA (1) | CA2357771A1 (en) |
| CZ (1) | CZ20012407A3 (en) |
| DE (1) | DE19900471A1 (en) |
| HU (1) | HUP0105054A3 (en) |
| NO (1) | NO20013384L (en) |
| PL (1) | PL349341A1 (en) |
| SK (1) | SK9442001A3 (en) |
| WO (1) | WO2000040583A2 (en) |
| ZA (1) | ZA200106454B (en) |
Families Citing this family (16)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| SI1140941T1 (en) | 1998-12-23 | 2005-04-30 | Bristol-Myers Squibb Pharma Company | Nitrogen containing heterobicycles as factor xa inhibitors |
| NZ523184A (en) * | 2000-06-23 | 2004-06-25 | Bristol Myers Squibb Pharma Co | 1 - (heteroaryl-phenyl) - condensed pyrazol derivatives as factor Xa inhibitors |
| CA2447488A1 (en) | 2001-05-22 | 2002-11-28 | Irina Jacobson | Bicyclic inhibitors of factor xa |
| GB0215293D0 (en) | 2002-07-03 | 2002-08-14 | Rega Foundation | Viral inhibitors |
| GB0225399D0 (en) * | 2002-10-31 | 2002-12-11 | Merck Sharp & Dohme | Therapeutic agents |
| PT1569912E (en) | 2002-12-03 | 2015-09-15 | Pharmacyclics Llc | 2-(2-hydroxybiphenyl-3-yl)-1h-benzoimidazole-5-carboxamidine derivatives as factor viia inhibitors |
| US20050222198A1 (en) | 2003-12-22 | 2005-10-06 | K.U. Leuven Research & Development, Gerhard Puerstinger And Gilead Sciences, Inc. | Imidazo[4,5-c]pyridine compounds and methods of antiviral treatment |
| EP1841765B1 (en) | 2004-12-21 | 2009-03-25 | Gilead Sciences, Inc. | Imidazo[4,5-c]pyridine compound and method of antiviral treatment |
| WO2007009883A1 (en) | 2005-07-15 | 2007-01-25 | F. Hoffmann-La Roche Ag | Novel heteroaryl fused cyclic amines |
| ZA200802857B (en) | 2005-09-14 | 2009-09-30 | Takeda Pharmaceutical | Dipeptidyl peptidase inhibitors for treating diabetes |
| KR101368988B1 (en) | 2005-09-16 | 2014-02-28 | 다케다 야쿠힌 고교 가부시키가이샤 | Dipeptidyl peptidase inhibitors |
| WO2007112347A1 (en) | 2006-03-28 | 2007-10-04 | Takeda Pharmaceutical Company Limited | Dipeptidyl peptidase inhibitors |
| US7754720B2 (en) | 2006-07-07 | 2010-07-13 | Gilead Sciences, Inc. | Pyridazine compound and use thereof |
| TW200838536A (en) | 2006-11-29 | 2008-10-01 | Takeda Pharmaceutical | Polymorphs of succinate salt of 2-[6-(3-amino-piperidin-1-yl)-3-methyl-2,4-dioxo-3,4-dihydro-2H-pyrimidin-1-ylmethy]-4-fluor-benzonitrile and methods of use therefor |
| UA99466C2 (en) | 2007-07-06 | 2012-08-27 | Гилиад Сайенсиз, Инк. | Crystalline pyridazine compound |
| CN107074846B (en) * | 2014-08-12 | 2020-05-19 | 先正达参股股份有限公司 | Pesticidally active heterocyclic derivatives with sulphur containing substituents |
Family Cites Families (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TW219935B (en) * | 1991-12-25 | 1994-02-01 | Mitsubishi Chemicals Co Ltd | |
| CA2309347A1 (en) * | 1997-12-01 | 1999-06-10 | Merck & Co., Inc. | Thrombin inhibitors |
-
1999
- 1999-01-08 DE DE19900471A patent/DE19900471A1/en not_active Withdrawn
- 1999-12-21 SK SK944-2001A patent/SK9442001A3/en unknown
- 1999-12-21 HU HU0105054A patent/HUP0105054A3/en unknown
- 1999-12-21 BR BR9916774-3A patent/BR9916774A/en not_active Application Discontinuation
- 1999-12-21 KR KR1020017007074A patent/KR20010086085A/en not_active Application Discontinuation
- 1999-12-21 AU AU30417/00A patent/AU3041700A/en not_active Abandoned
- 1999-12-21 CZ CZ20012407A patent/CZ20012407A3/en unknown
- 1999-12-21 EP EP99964639A patent/EP1149099A2/en not_active Withdrawn
- 1999-12-21 CN CN99815465A patent/CN1333772A/en active Pending
- 1999-12-21 CA CA002357771A patent/CA2357771A1/en not_active Abandoned
- 1999-12-21 PL PL99349341A patent/PL349341A1/en unknown
- 1999-12-21 WO PCT/EP1999/010236 patent/WO2000040583A2/en not_active Application Discontinuation
- 1999-12-21 JP JP2000592291A patent/JP2002534429A/en active Pending
-
2000
- 2000-01-07 AR ARP000100062A patent/AR022220A1/en unknown
-
2001
- 2001-07-06 NO NO20013384A patent/NO20013384L/en not_active Application Discontinuation
- 2001-08-06 ZA ZA200106454A patent/ZA200106454B/en unknown
Also Published As
| Publication number | Publication date |
|---|---|
| SK9442001A3 (en) | 2002-05-09 |
| NO20013384D0 (en) | 2001-07-06 |
| WO2000040583A2 (en) | 2000-07-13 |
| NO20013384L (en) | 2001-07-06 |
| CZ20012407A3 (en) | 2001-12-12 |
| PL349341A1 (en) | 2002-07-15 |
| HUP0105054A2 (en) | 2002-05-29 |
| CN1333772A (en) | 2002-01-30 |
| ZA200106454B (en) | 2002-11-06 |
| BR9916774A (en) | 2001-10-30 |
| KR20010086085A (en) | 2001-09-07 |
| AU3041700A (en) | 2000-07-24 |
| EP1149099A2 (en) | 2001-10-31 |
| DE19900471A1 (en) | 2000-07-13 |
| JP2002534429A (en) | 2002-10-15 |
| CA2357771A1 (en) | 2000-07-13 |
| WO2000040583A3 (en) | 2000-09-21 |
| HUP0105054A3 (en) | 2002-12-28 |
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