AR001801A1 - Nuevos compuestos que tienen actividad como inhibidores de la tripsina y la trombina procedimientos e intermediarios para prepararlos y las composiciones farmacéuticas que contienen dichos compuestos - Google Patents

Nuevos compuestos que tienen actividad como inhibidores de la tripsina y la trombina procedimientos e intermediarios para prepararlos y las composiciones farmacéuticas que contienen dichos compuestos

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Publication number
AR001801A1
AR001801A1 AR33579096A AR33579096A AR001801A1 AR 001801 A1 AR001801 A1 AR 001801A1 AR 33579096 A AR33579096 A AR 33579096A AR 33579096 A AR33579096 A AR 33579096A AR 001801 A1 AR001801 A1 AR 001801A1
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AR
Argentina
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residue
compounds
integer
cqh2q
alkyl
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AR33579096A
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English (en)
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Ciba Geigy
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D207/00Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/04Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom 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
    • C07D207/08Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom 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 radicals, substituted by hetero atoms, attached to ring carbon atoms
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • 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
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    • C07D211/00Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06Heterocyclic 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
    • C07D211/08Heterocyclic 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
    • C07D211/18Heterocyclic 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
    • C07D211/20Heterocyclic 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 singly bound oxygen or sulphur atoms
    • C07D211/22Heterocyclic 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 singly bound oxygen or sulphur atoms by oxygen atoms
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    • C07D211/00Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06Heterocyclic 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
    • C07D211/08Heterocyclic 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
    • C07D211/18Heterocyclic 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
    • C07D211/26Heterocyclic 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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    • C07D211/00Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
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    • C07D211/06Heterocyclic 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
    • C07D211/08Heterocyclic 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
    • C07D211/18Heterocyclic 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
    • C07D211/34Heterocyclic 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 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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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D215/00Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02Heterocyclic 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
    • C07D215/16Heterocyclic 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
    • C07D215/36Sulfur atoms
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    • C07D217/00Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems
    • C07D217/12Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with radicals, substituted by hetero atoms, attached to carbon atoms of the nitrogen-containing ring
    • C07D217/14Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with radicals, substituted by hetero atoms, attached to carbon atoms of the nitrogen-containing ring other than aralkyl radicals
    • C07D217/16Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with radicals, substituted by hetero atoms, attached to carbon atoms of the nitrogen-containing ring other than aralkyl radicals substituted by oxygen atoms
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    • C07D295/00Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/16Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms
    • C07D295/18Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms by radicals derived from carboxylic acids, or sulfur or nitrogen analogues thereof
    • C07D295/182Radicals derived from carboxylic acids
    • C07D295/185Radicals derived from carboxylic acids from aliphatic carboxylic acids
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    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/12Heterocyclic 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 chain containing hetero atoms as chain links
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    • C07D417/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
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    • C07D417/12Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
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    • C07D513/02Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
    • C07D513/04Ortho-condensed systems
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    • C07F9/00Compounds containing elements of Groups 5 or 15 of the Periodic Table
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    • C07F9/547Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
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    • C07F9/00Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02Phosphorus compounds
    • C07F9/547Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
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    • C07F9/65583Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system each of the hetero rings containing nitrogen as ring hetero atom

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  • Diabetes (AREA)
  • Hematology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Peptides Or Proteins (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

Se describen compuestos de la fórmula general (I), en el cual Ar es un residuo de arilo o heterocíclico substituido o no substituido; Aa es unresiduo de aminoácido usualmente de configuración L y (II) es un residuo de la fórmula (IV) o fórmula(V) en la cual los grupos variables tienen lossignificados senalados, en donde X es hidrógeno o alquilo; Y es a) a SO3H, PO(OR14)2, OH, SH, NR15R16 o grupo halógeno o b) un residuo -(CqH2q)-Qdonde Q es H, COR14, CO2R14, CONR15R16, SO3H, OR14, OCOR14, PO(OR14)2, NR15R16, SR14 o Hal en donde R14, R15 y R16 son hidrógeno, alquilo, C5-C8 cicloalquilo oC7-C11 aralquilo o R15 y R16 juntos con el átomo de nitrógeno forman un azacicloalquilo o oxazacicloalquilo de 5 o 6 miembros;q es cero oun entero de1 a 8 y el residuo (CqH2q) puede ser substituido por OH o interrumpido por oxígeno, sulfuro, oxicarbonilo O.CO, carboniloxi CO.O, aminocarboniloNHCO, sulfonamido, NHSO2 o carboxamido CONH; o c) un residuo (Cw-H2w+1-y-z)FyOHz en el cual w es un entero de 1 a 8, y es un entero de 1 a17 y z es 0 ó 1, o X e Y juntos son = O,Z es un enlace directo, oxígeno o nitrógeno substituido o nó por X o Y, m = 2 a 4, n = 2 a 4 y m + n = 4,j = 0 a 2, k = 0 a 2 y j + k =2 ó 3 donde Y es un residuo (CqH2q), y las sales de los mismos, siempre que cuando Aa es arginina X e Y no son alquilo y cuandoQ es COR4, Q es un entero de 1 a 8. Los compuestos (I) tienen actividad como inhibidores de la tripsina y la trombina.Se describen además losprocedimientos e intermediarios para obtener dichos compuestos y las composiciones farmacéuticas que los contienen.
AR33579096A 1995-03-18 1996-03-18 Nuevos compuestos que tienen actividad como inhibidores de la tripsina y la trombina procedimientos e intermediarios para prepararlos y las composiciones farmacéuticas que contienen dichos compuestos AR001801A1 (es)

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Application Number Priority Date Filing Date Title
GBGB9505538.0A GB9505538D0 (en) 1995-03-18 1995-03-18 New compounds

Publications (1)

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AR001801A1 true AR001801A1 (es) 1997-12-10

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AR33579096A AR001801A1 (es) 1995-03-18 1996-03-18 Nuevos compuestos que tienen actividad como inhibidores de la tripsina y la trombina procedimientos e intermediarios para prepararlos y las composiciones farmacéuticas que contienen dichos compuestos

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EP (1) EP0815103A1 (es)
JP (1) JPH11502219A (es)
AR (1) AR001801A1 (es)
AU (1) AU4887296A (es)
GB (1) GB9505538D0 (es)
IL (1) IL117437A0 (es)
WO (1) WO1996029327A1 (es)
ZA (1) ZA962112B (es)

Families Citing this family (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0823430B1 (en) * 1996-08-07 2001-10-24 Mitsubishi Chemical Corporation Method for preparing n2-arylsulfonyl-l-argininamides
FR2761065B1 (fr) * 1997-03-20 2000-03-03 Synthelabo Derives de n-(arginyle)benzenesulfonamide, leur preparation et leur application en therapeutique
FR2825705B1 (fr) 2001-06-08 2005-05-20 Aventis Pharma Sa Nouveaux composes heterocycliques, leur preparation et leur utilisation comme medicaments, notamment comme anti-bacteriens
FR2835186B1 (fr) 2002-01-28 2006-10-20 Aventis Pharma Sa Nouveaux composes heterocycliques, actifs comme inhibiteurs de beta-lactamases
FR2844273B1 (fr) 2002-09-05 2008-04-04 Aventis Pharma Sa Nouveaux composes heterocycliques, procede et intermediaires de preparation et utilisation comme medicament, notamment comme inhibiteurs de beta-lactamases et anti-bacteriens.
GB0507577D0 (en) 2005-04-14 2005-05-18 Novartis Ag Organic compounds
KR101846029B1 (ko) * 2008-08-06 2018-04-06 메디베이션 테크놀로지즈 엘엘씨 폴리(adp-리보오스)폴리머라아제 (parp)의 디히드로피리도프탈라지논 억제제
CN102869258A (zh) 2010-02-03 2013-01-09 生物马林药物股份有限公司 用于pten基因缺失相关疾病的治疗的聚(adp-核糖)聚合酶(parp)的二氢吡啶并酞嗪酮抑制剂
EP2533640B1 (en) 2010-02-08 2016-09-28 Medivation Technologies, Inc. Processes of synthesizing dihydropyridophthalazinone derivatives
CN103282365B (zh) 2010-10-21 2017-12-29 麦迪韦逊科技有限公司 结晶的(8S,9R)‑5‑氟‑8‑(4‑氟苯基)‑9‑(1‑甲基‑1H‑1,2,4‑三唑‑5‑基)‑8,9‑二氢‑2H‑吡啶并[4,3,2‑de]酞嗪‑3(7H)‑酮甲苯磺酸盐

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
IE48623B1 (en) * 1978-08-31 1985-03-20 Mitsubishi Chem Ind Alpha-(n-arylsulfonyl-l-argininamides,processes for their preparation and pharmaceutical compositions containing these substances
JPH0681722B2 (ja) * 1984-02-06 1994-10-19 三菱化成株式会社 抗トリプシン剤
PH31294A (en) * 1992-02-13 1998-07-06 Thomae Gmbh Dr K Benzimidazolyl derivatives, pharmaceutical compositions containing these compounds and process for preparing them.
FR2689130B1 (fr) * 1992-03-30 1994-05-27 Synthelabo Derives de 1-[2 (arylsulfonylamino)ethyl-1-oxo] piperidine, leur preparation et leur application en therapeutique.
GB9209032D0 (en) * 1992-04-25 1992-06-10 Ciba Geigy Ag New peptide derivatives
US5371091A (en) * 1992-08-31 1994-12-06 Bristol-Myers Squibb Company Heteroaromatic amine thrombin inhibitors

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EP0815103A1 (en) 1998-01-07
AU4887296A (en) 1996-10-08
JPH11502219A (ja) 1999-02-23
ZA962112B (en) 1996-09-18
WO1996029327A1 (en) 1996-09-26
GB9505538D0 (en) 1995-05-03
IL117437A0 (en) 1996-10-16

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