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 COMPOSITIONS

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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
Application number
ARP000100062A
Other languages
Spanish (es)
Original Assignee
Merck Patent Gmbh
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 Merck Patent Gmbh filed Critical Merck Patent Gmbh
Publication of AR022220A1 publication Critical patent/AR022220A1/en

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Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/12Heterocyclic 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
    • C07D471/14Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/02Heterocyclic 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
    • C07D471/04Ortho-condensed systems
    • 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
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • 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

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.

ARP000100062A 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 AR022220A1 (en)

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) NO20013384D0 (en)
PL (1) PL349341A1 (en)
SK (1) SK9442001A3 (en)
WO (1) WO2000040583A2 (en)
ZA (1) ZA200106454B (en)

Families Citing this family (16)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
IL142959A0 (en) 1998-12-23 2002-04-21 Du Pont Pharm Co 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
AU2002310070A1 (en) 2001-05-22 2002-12-03 Bristol-Myers Squibb Company 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
DK1569912T3 (en) 2002-12-03 2015-06-29 Pharmacyclics Inc 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
CA2592388C (en) 2004-12-21 2013-04-02 Steven S. Bondy Imidazo[4,5-c]pyridine compound and method of antiviral treatment
CA2614401A1 (en) 2005-07-15 2007-01-25 F. Hoffmann-La Roche Ag Novel heteroaryl fused cyclic amines
EA015169B1 (en) 2005-09-14 2011-06-30 Такеда Фармасьютикал Компани Лимитед Use of dipeptidyl peptidase inhibitors
EP1924567B1 (en) 2005-09-16 2012-08-22 Takeda Pharmaceutical Company Limited Process for the preparation of pyrimidinedione derivatives
WO2007112347A1 (en) 2006-03-28 2007-10-04 Takeda Pharmaceutical Company Limited Dipeptidyl peptidase inhibitors
AU2007269614B2 (en) 2006-07-07 2011-09-08 Gilead Sciences, Inc. Novel 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
JP6689821B2 (en) * 2014-08-12 2020-04-28 シンジェンタ パーティシペーションズ アーゲー Pesticidally Active Heterocyclic Derivatives Bearing Sulfur-Containing Substituents

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TW219935B (en) * 1991-12-25 1994-02-01 Mitsubishi Chemicals Co Ltd
JP2001524522A (en) * 1997-12-01 2001-12-04 メルク エンド カムパニー インコーポレーテッド Thrombin inhibitor

Also Published As

Publication number Publication date
CA2357771A1 (en) 2000-07-13
NO20013384L (en) 2001-07-06
AU3041700A (en) 2000-07-24
KR20010086085A (en) 2001-09-07
WO2000040583A3 (en) 2000-09-21
CZ20012407A3 (en) 2001-12-12
ZA200106454B (en) 2002-11-06
EP1149099A2 (en) 2001-10-31
CN1333772A (en) 2002-01-30
SK9442001A3 (en) 2002-05-09
WO2000040583A2 (en) 2000-07-13
BR9916774A (en) 2001-10-30
DE19900471A1 (en) 2000-07-13
NO20013384D0 (en) 2001-07-06
HUP0105054A2 (en) 2002-05-29
PL349341A1 (en) 2002-07-15
HUP0105054A3 (en) 2002-12-28
JP2002534429A (en) 2002-10-15

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