AR021782A1 - DERIVATIVES OF 2-OXO-2H-QUINOLEINA, A PROCEDURE FOR THEIR PREPARATION, THE USE OF THE SAME TO PREPARE A MEDICINAL PRODUCT, THE PHARMACEUTICAL COMPOSITIONS THAT CONTAIN THEM AND A PROCEDURE TO PREPARE THESE PHARMACEUTICAL COMPOSITIONS. - Google Patents

DERIVATIVES OF 2-OXO-2H-QUINOLEINA, A PROCEDURE FOR THEIR PREPARATION, THE USE OF THE SAME TO PREPARE A MEDICINAL PRODUCT, THE PHARMACEUTICAL COMPOSITIONS THAT CONTAIN THEM AND A PROCEDURE TO PREPARE THESE PHARMACEUTICAL COMPOSITIONS.

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Publication number
AR021782A1
AR021782A1 ARP990104301A ARP990104301A AR021782A1 AR 021782 A1 AR021782 A1 AR 021782A1 AR P990104301 A ARP990104301 A AR P990104301A AR P990104301 A ARP990104301 A AR P990104301A AR 021782 A1 AR021782 A1 AR 021782A1
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AR
Argentina
Prior art keywords
group
procedure
formula
derivatives
prepare
Prior art date
Application number
ARP990104301A
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 AR021782A1 publication Critical patent/AR021782A1/en

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D215/20—Oxygen atoms
    • C07D215/22—Oxygen atoms attached in position 2 or 4
    • C07D215/227—Oxygen atoms attached in position 2 or 4 only one oxygen atom which is attached in position 2
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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
    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D215/48—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
    • C07D215/50—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen attached in position 4
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D215/48—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
    • C07D215/54—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen attached in position 3
    • 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
    • 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
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings

Abstract

Nuevos derivados de la 2-oxo-2H-quinoleína, de formula 1 en donde R, R1 representan independientemente H, A, -(CH2)m-R4, -(CH2)m-OA o -(CH2)m -Ar, R2representa Ar, 2 o 3,R3 representa Ar,R4 representa CN, COOH, COOA, CONH2, CONHA, CONA2 o C(=NH)-NH2,representa -C(=NH)-NH2, -NH-C(=NH)-NH2 o -C(=O)-N=C(NH2)2no sustituido o monosustituido con -COA, COOA, -OH con un grupo protector de amino convencional 4 o 5, R6 representa H, A o NH2, Ar representa fenilo, naftilo,o bifenilo no sustituido o mono,di, o trisustituido con A, cicloalquilo C3-6, OH, OA, Hal, CN, NO2, CF3, NH2, NHA, NA2, pirrolidin-1-ilo, piperidin-1-ilo,benciloxi, SO2NH2,SO2NHA,SO2NA2,-(CH2)n-NH2,-(CH2)n-NHA,-(CH2)n-NA2,-O-(CH2)n-NH2,-O-(CH2)n-NHA,-O-(CH2)n-,NA2,-O-(CH2)m-O-o R5,A representa alquilo C1-6, Xestá ausente o representa alquileno C1-4 o carbonilo, Y está ausente o representa NH, O o S, Hal representa F, Cl, Br o I, m es 0, 1 o 2, n es 0, 1, 2 o 3.Estos compuestos actuan como inhibidores del factor de coagulacionXa y pueden ser empleados para la profilaxis y/o terapia de las enfermedades tromboembolicasUn procedimiento para preparar los derivados de la 2-oxo-2H-quinolina, de formula 1, en el cual a) se los libera de uno de sus derivados funcionales portratamiento con un agente de solvolisis o hidrogenolisis, ya sea i)liberando por hidrogenolisis o solvolisis un grupo de amidino de su derivado de oxadiazol ode su derivado de oxazolidinona, ii)reemplazando un grupo protector de amino convencional por hidrogeno al tratarlo con un agente de solvolisis ohidrogenolisis o liberando un grupo de amino que se encuentra protegido con un grupo protector convencional, porque en un compuesto de formula 1 setransforma(n) uno o varios restos R, R1, R2 y/ R3 en uno o varios restos R, R1, R2 y/o R3 diferentes ya sea, por ejemplo, i)hidrolizando un grupo éster a ungrupo de carboxilo, ii)reduciendo un grupo nitro, iii)acilando un grupo de amino, iv)transformando un grupo ciano en un grupo de amidino y/o C)se transformauna base o un ácido de formula 1 en una de sus sales.New derivatives of 2-oxo-2H-quinoline, of formula 1 wherein R, R1 independently represent H, A, - (CH2) m-R4, - (CH2) m-OA or - (CH2) m -Ar, R2 represents Ar, 2 or 3, R3 represents Ar, R4 represents CN, COOH, COOA, CONH2, CONHA, CONA2 or C (= NH) -NH2, represents -C (= NH) -NH2, -NH-C (= NH ) -NH2 or -C (= O) -N = C (NH2) 2 unsubstituted or monosubstituted with -COA, COOA, -OH with a conventional amino protecting group 4 or 5, R6 represents H, A or NH2, Ar represents phenyl, naphthyl, or unsubstituted or mono, di, or trisubstituted biphenyl with A, C3-6 cycloalkyl, OH, OA, Hal, CN, NO2, CF3, NH2, NHA, NA2, pyrrolidin-1-yl, piperidin-1 -yl, benzyloxy, SO2NH2, SO2NHA, SO2NA2, - (CH2) n-NH2, - (CH2) n-NHA, - (CH2) n-NA2, -O- (CH2) n-NH2, -O- (CH2 ) n-NHA, -O- (CH2) n-, NA2, -O- (CH2) mOo R5, A represents C1-6 alkyl, X is absent or represents C1-4 alkylene or carbonyl, Y is absent or represents NH, O or S, Hal represents F, Cl, Br or I, m is 0, 1 or 2, n is 0, 1, 2 or 3. These compounds act as clotting factor inhibitors Xa and can be used for the prophylaxis and / or therapy of thromboembolic diseases A procedure for preparing the derivatives of 2-oxo-2H-quinoline, of formula 1, in which a) is released from one of its functional derivatives with a solvolysis or hydrogenolysis agent, either i) releasing an amidine group from its oxadiazole derivative or from its oxazolidinone derivative by hydrogenolysis or solvolysis, ii) replacing a conventional amino protecting group with hydrogen by treating it with a solvolysis agent ohydrogenolysis or releasing an amino group that is protected with a conventional protective group, because in a compound of formula 1 one or more R, R1, R2 and / R3 residues are transformed into one or more R, R1, R2 moieties and / or different R3 either, for example, i) hydrolyzing an ester group to a carboxyl group, ii) reducing a nitro group, iii) acylating an amino group, iv) transforming a cyano group into an amidino group and / or C) it is It forms a base or an acid of formula 1 in one of its salts.

ARP990104301A 1998-08-29 1999-08-27 DERIVATIVES OF 2-OXO-2H-QUINOLEINA, A PROCEDURE FOR THEIR PREPARATION, THE USE OF THE SAME TO PREPARE A MEDICINAL PRODUCT, THE PHARMACEUTICAL COMPOSITIONS THAT CONTAIN THEM AND A PROCEDURE TO PREPARE THESE PHARMACEUTICAL COMPOSITIONS. AR021782A1 (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
DE19839499A DE19839499A1 (en) 1998-08-29 1998-08-29 2-oxo-2H-quinoline derivatives

Publications (1)

Publication Number Publication Date
AR021782A1 true AR021782A1 (en) 2002-08-07

Family

ID=7879227

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP990104301A AR021782A1 (en) 1998-08-29 1999-08-27 DERIVATIVES OF 2-OXO-2H-QUINOLEINA, A PROCEDURE FOR THEIR PREPARATION, THE USE OF THE SAME TO PREPARE A MEDICINAL PRODUCT, THE PHARMACEUTICAL COMPOSITIONS THAT CONTAIN THEM AND A PROCEDURE TO PREPARE THESE PHARMACEUTICAL COMPOSITIONS.

Country Status (17)

Country Link
EP (1) EP1107954A1 (en)
JP (1) JP2002523494A (en)
KR (1) KR20010072862A (en)
CN (1) CN1315942A (en)
AR (1) AR021782A1 (en)
AU (1) AU5164199A (en)
BR (1) BR9913140A (en)
CA (1) CA2342230A1 (en)
DE (1) DE19839499A1 (en)
HK (1) HK1042478A1 (en)
HU (1) HUP0103212A3 (en)
ID (1) ID27863A (en)
NO (1) NO20010996L (en)
PL (1) PL346045A1 (en)
SK (1) SK2652001A3 (en)
WO (1) WO2000012479A1 (en)
ZA (1) ZA200102565B (en)

Families Citing this family (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DK1569912T3 (en) 2002-12-03 2015-06-29 Pharmacyclics Inc 2- (2-hydroxybiphenyl-3-yl) -1h-benzoimidazole-5-carboxamidine derivatives as factor VIIa inhibitors.
DK3174868T3 (en) 2014-08-01 2021-11-08 Nuevolution As COMPOUNDS ACTIVE AGAINST BROMODOMAINS

Family Cites Families (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4070470A (en) * 1974-06-24 1978-01-24 Otsuka Pharmaceutical Co., Ltd. Platelet aggregation inhibiting carbostyrils, their compositions and method of use
IE43079B1 (en) * 1975-03-20 1980-12-17 Ici Ltd Quinolone derivatives
JPS596858B2 (en) * 1975-04-30 1984-02-15 オオツカセイヤク カブシキガイシヤ Method for producing 3,4-dihydrocarbostyryl derivative
AT347956B (en) * 1976-03-18 1979-01-25 Ici Ltd Process for the preparation of new quinol-2-on-4-yl-alkanoic acids and their base addition salts
DE2651581A1 (en) * 1976-11-12 1978-05-18 Merck Patent Gmbh CHINOLONE DERIVATIVES AND METHOD FOR THE PRODUCTION THEREOF
CA2091173A1 (en) * 1990-09-07 1992-03-08 Adriano Afonso Antiviral compounds and antihypertensive compounds
CA2091172C (en) * 1990-09-07 1997-05-20 Adriano Afonso Antiviral compounds and antihypertensive compounds
ZA928276B (en) * 1991-10-31 1993-05-06 Daiichi Seiyaku Co Aromatic amidine derivates and salts thereof.
DE4208304A1 (en) * 1992-03-16 1993-09-23 Merck Patent Gmbh 2-OXOCHINOLINDERIVATE
IL115420A0 (en) * 1994-09-26 1995-12-31 Zeneca Ltd Aminoheterocyclic derivatives
US5612353A (en) * 1995-06-07 1997-03-18 Rhone-Poulenc Rorer Pharmaceuticals Inc. Substituted (sulfinic acid, sulfonic acid, sulfonylamino or sulfinylamino) N-[(aminoiminomethyl)phenylalkyl]-azaheterocyclylamide compounds
DE19528418A1 (en) * 1995-08-02 1997-02-06 Merck Patent Gmbh Endothelin receptor antagonists
DE19530996A1 (en) * 1995-08-23 1997-02-27 Boehringer Mannheim Gmbh Cyclic guanidines, process for their preparation and pharmaceuticals
US5968959A (en) * 1997-12-12 1999-10-19 Orion Corporation Method for the prevention and treatment of stunned myocardium

Also Published As

Publication number Publication date
NO20010996D0 (en) 2001-02-27
EP1107954A1 (en) 2001-06-20
HUP0103212A3 (en) 2002-06-28
KR20010072862A (en) 2001-07-31
HUP0103212A2 (en) 2002-05-29
SK2652001A3 (en) 2001-09-11
CN1315942A (en) 2001-10-03
WO2000012479A1 (en) 2000-03-09
PL346045A1 (en) 2002-01-14
DE19839499A1 (en) 2000-03-02
HK1042478A1 (en) 2002-08-16
ID27863A (en) 2001-04-26
AU5164199A (en) 2000-03-21
NO20010996L (en) 2001-02-27
CA2342230A1 (en) 2000-03-09
BR9913140A (en) 2001-05-08
ZA200102565B (en) 2002-06-28
JP2002523494A (en) 2002-07-30

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