AR020124A1 - DERIVATIVES OF PIPERAZINONE, A PROCEDURE FOR THEIR PREPARATION, THE PHARMACEUTICAL COMPOSITIONS THAT CONTAIN THEM AND THE USE OF THE SAME TO PREPARE A MEDICINAL PRODUCT - Google Patents

DERIVATIVES OF PIPERAZINONE, A PROCEDURE FOR THEIR PREPARATION, THE PHARMACEUTICAL COMPOSITIONS THAT CONTAIN THEM AND THE USE OF THE SAME TO PREPARE A MEDICINAL PRODUCT

Info

Publication number
AR020124A1
AR020124A1 ARP990103925A ARP990103925A AR020124A1 AR 020124 A1 AR020124 A1 AR 020124A1 AR P990103925 A ARP990103925 A AR P990103925A AR P990103925 A ARP990103925 A AR P990103925A AR 020124 A1 AR020124 A1 AR 020124A1
Authority
AR
Argentina
Prior art keywords
formula
derivatives
piperazinone
cooa
hal
Prior art date
Application number
ARP990103925A
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 AR020124A1 publication Critical patent/AR020124A1/en

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/10—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing aromatic rings
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D241/00—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
    • C07D241/02—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
    • C07D241/06—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having one or two double bonds between ring members or between ring members and non-ring members
    • C07D241/08—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having one or two double bonds between ring members or between ring members and non-ring members with oxygen atoms directly attached to ring carbon atoms

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Health & Medical Sciences (AREA)
  • Urology & Nephrology (AREA)
  • Vascular Medicine (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

Los nuevos derivados de la piperazinona de la formula (1), en donde: R1, R2 representan independientemente A, fenilo, naftilo o bifenilo nosustituido o mono, di- o trisustituido con R8, A, Ar, OH, OA, O(C(R3)2)n-Ar,-OAr,NH2, NHA, NA2, NO2, CN, Hal,N HCOA, NHCOAr, NHSO2A, NHSO2Ar, COOH,COOA, CONH2, CONHA, CONA2, CONHAr, COA, COAr, S(O)nA, S(O)nAr, SO2NH2, SO2NHA o SO2NA2, o un heterociclo saturado, insaturado o aromático de uno o dosnucleos que contiene de 1 a 4 átomos de N, O y/o S, que seencue ntra unido a través del N o C y que puede estar no sustituido o mono, di o trisustituidocon R8, A, Ar, OH, OA, OAr, NH2, NHA, NA2, NO2, CN, Hal, NHCOA, NHCOAr, NHSO2A, NHSO2Ar, COOH, COOA, CONH2, CONHA, CONA2, CONHAr, COA, COAr,S(O)nA,S(O)nAr, SO2NH 2, SO2NHA o SO2NA2 o carboniloxi, con la condicion de que el resto R8 debe estar presente al menos una vez en R1 o en R2, o también puedeaparecer una vez en cada uno de los restos R1 y R2; R3 representa H o A; representanindependientemente H, A, C(R 3)2)n-Ar, (C(R3)2)n-Het, (C(R3)2)n-COOR3,representa C(=NH)-NH2 no sustituido o también monosustituido con COA, CO-[C(R3)2]n-Ar, COOA, OH o con un grupo protector de amino convencional, orepresenta un grupo no sustituidode NH-C(=NH)-NH2, CON=C(NH2)2, formula (2); W representa -CO, -C(R3)2, X representa -(C(R3)2)n,-SO2, -CO-, -COO-, -CONR4-,y A, Ar, Ar, Het, Hal y n tienen los significados indicados en la reivindicacion 1, y también sus sales y solvatos, actuan comoinhibidores del factor decoagu lacion Xa y pueden ser empleados para la profilaxis y/o terapia de las enfermedades tromboembolicas. Un procedimiento para preparar losderivados de la piperazinona de formula (1), en el cual: a) se libera loscompuestos de uno de sus derivados funcio nales por tratamiento con un agentede solvolisis o hidrogenolisis, o b) se hace reaccionar un compuestos de formula (3), en donde: R1, R3, R4, R5, R6, R7 y W tienen los significadosindicados en lareivindicacion 1 y R8 representa formula (4) con un c ompuesto de formula (5): R2-X-L en donde: R2 y X tienen el significado indicado en laThe new piperazinone derivatives of the formula (1), wherein: R1, R2 independently represent A, phenyl, naphthyl or biphenyl substituted or mono, di- or trisubstituted with R8, A, Ar, OH, OA, O (C (R3) 2) n-Ar, -OAr, NH2, NHA, NA2, NO2, CN, Hal, N HCOA, NHCOAr, NHSO2A, NHSO2Ar, COOH, COOA, CONH2, CONHA, CONA2, CONHAr, COA, COAr, S (O) nA, S (O) nAr, SO2NH2, SO2NHA or SO2NA2, or a saturated, unsaturated or aromatic heterocycle of one or two nuclei containing from 1 to 4 atoms of N, O and / or S, which is attached to through N or C and which may be unsubstituted or mono, di or trisubstituted with R8, A, Ar, OH, OA, OAr, NH2, NHA, NA2, NO2, CN, Hal, NHCOA, NHCOAr, NHSO2A, NHSO2Ar, COOH , COOA, CONH2, CONHA, CONA2, CONHAr, COA, COAr, S (O) nA, S (O) nAr, SO2NH 2, SO2NHA or SO2NA2 or carbonyloxy, with the proviso that the rest R8 must be present at least one once in R1 or R2, or it can also appear once in each of the remains R1 and R2; R3 represents H or A; independently represent H, A, C (R 3) 2) n-Ar, (C (R3) 2) n-Het, (C (R3) 2) n-COOR3, represents C (= NH) -NH2 unsubstituted or also monosubstituted with COA, CO- [C (R3) 2] n-Ar, COOA, OH or with a conventional amino protecting group, or represents an unsubstituted group of NH-C (= NH) -NH2, CON = C (NH2) 2, formula (2); W represents -CO, -C (R3) 2, X represents - (C (R3) 2) n, -SO2, -CO-, -COO-, -CONR4-, and A, Ar, Ar, Het, Hal and n they have the meanings indicated in claim 1, and also their salts and solvates, act as inhibitors of decoding factor Xa and can be used for the prophylaxis and / or therapy of thromboembolic diseases. A process for preparing the derivatives of the piperazinone of formula (1), in which: a) the compounds of one of its functional derivatives are released by treatment with a solvolysis or hydrogenolysis agent, or b) a compound of formula (3) is reacted ), wherein: R1, R3, R4, R5, R6, R7 and W have the meanings indicated in claim 1 and R8 represents formula (4) with a formula c (5): R2-XL where: R2 and X they have the meaning indicated in the

ARP990103925A 1998-08-08 1999-08-06 DERIVATIVES OF PIPERAZINONE, A PROCEDURE FOR THEIR PREPARATION, THE PHARMACEUTICAL COMPOSITIONS THAT CONTAIN THEM AND THE USE OF THE SAME TO PREPARE A MEDICINAL PRODUCT AR020124A1 (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
DE19835950A DE19835950A1 (en) 1998-08-08 1998-08-08 Piperazinone derivatives

Publications (1)

Publication Number Publication Date
AR020124A1 true AR020124A1 (en) 2002-04-10

Family

ID=7876912

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP990103925A AR020124A1 (en) 1998-08-08 1999-08-06 DERIVATIVES OF PIPERAZINONE, A PROCEDURE FOR THEIR PREPARATION, THE PHARMACEUTICAL COMPOSITIONS THAT CONTAIN THEM AND THE USE OF THE SAME TO PREPARE A MEDICINAL PRODUCT

Country Status (4)

Country Link
AR (1) AR020124A1 (en)
AU (1) AU5411499A (en)
DE (1) DE19835950A1 (en)
WO (1) WO2000008005A2 (en)

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ATE346050T1 (en) * 1998-01-27 2006-12-15 Aventis Pharma Inc SUBSTITUTED OXOAZAHETEROCYCLYL FACTOR XA INHIBITORS
CA2422873A1 (en) * 2000-09-29 2002-04-04 Wenhao Li Piperazin-2-one amides as inhibitors of factor xa
AU2003282566A1 (en) * 2002-10-09 2004-05-04 Millennium Pharmaceuticals, Inc. Piperazine and piperazinone inhibitors of factor xa
CN100513398C (en) 2002-12-03 2009-07-15 Axys药物公司 2-(2-hydroxybiphenyl-3-yl)-1h-benzoimidazole-5-carboxamidine derivatives as factor VIIA inhibitors

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE4302485A1 (en) * 1993-01-29 1994-08-04 Merck Patent Gmbh Piperazine derivatives
EP0623615B1 (en) * 1993-05-01 1999-06-30 MERCK PATENT GmbH Substituted 1-phenyl-oxazolidin-2-one derivatives, their preparation and their use as adhesion-receptor antagonists
IL115420A0 (en) * 1994-09-26 1995-12-31 Zeneca Ltd Aminoheterocyclic derivatives
DE19530996A1 (en) * 1995-08-23 1997-02-27 Boehringer Mannheim Gmbh Cyclic guanidines, process for their preparation and pharmaceuticals
EP0765660A3 (en) * 1995-09-28 1998-09-23 Takeda Chemical Industries, Ltd. Microcapsules comprising 2-piperazinone-1-acetic acid compounds
AU4172397A (en) * 1996-09-06 1998-03-26 Biochem Pharma Inc. Lactam inhibitors of thrombin

Also Published As

Publication number Publication date
WO2000008005A3 (en) 2000-05-18
DE19835950A1 (en) 2000-02-10
AU5411499A (en) 2000-02-28
WO2000008005A2 (en) 2000-02-17

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