AR062744A1 - Derivados de tartrato como inhibidores del factor de coagulacion ixa - Google Patents

Derivados de tartrato como inhibidores del factor de coagulacion ixa

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Publication number
AR062744A1
AR062744A1 ARP070104011A ARP070104011A AR062744A1 AR 062744 A1 AR062744 A1 AR 062744A1 AR P070104011 A ARP070104011 A AR P070104011A AR P070104011 A ARP070104011 A AR P070104011A AR 062744 A1 AR062744 A1 AR 062744A1
Authority
AR
Argentina
Prior art keywords
alkyl
aryl
het
trisubstituted
mono
Prior art date
Application number
ARP070104011A
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English (en)
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Sanofi Aventis
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Publication date
Application filed by Sanofi Aventis filed Critical Sanofi Aventis
Publication of AR062744A1 publication Critical patent/AR062744A1/es

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D307/00—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
    • C07D307/02—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings
    • C07D307/34—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D307/56—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members 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
    • C07D307/60—Two oxygen atoms, e.g. succinic anhydride
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D217/00—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems
    • C07D217/22—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems 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 carbon atoms of the nitrogen-containing ring
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • 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
    • A61P3/00—Drugs for disorders of the metabolism
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04—Antibacterial agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/04—Antineoplastic agents specific for metastasis
    • 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
    • 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
    • A61P9/06—Antiarrhythmics
    • 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
    • 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
    • A61P9/14—Vasoprotectives; Antihaemorrhoidals; Drugs for varicose therapy; Capillary stabilisers
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C235/00—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms
    • C07C235/02—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to acyclic carbon atoms and singly-bound oxygen atoms bound to the same carbon skeleton
    • C07C235/04—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to acyclic carbon atoms and singly-bound oxygen atoms bound to the same carbon skeleton the carbon skeleton being acyclic and saturated
    • C07C235/16—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to acyclic carbon atoms and singly-bound oxygen atoms bound to the same carbon skeleton the carbon skeleton being acyclic and saturated having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a six-membered aromatic ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C257/00—Compounds containing carboxyl groups, the doubly-bound oxygen atom of a carboxyl group being replaced by a doubly-bound nitrogen atom, this nitrogen atom not being further bound to an oxygen atom, e.g. imino-ethers, amidines
    • C07C257/10—Compounds containing carboxyl groups, the doubly-bound oxygen atom of a carboxyl group being replaced by a doubly-bound nitrogen atom, this nitrogen atom not being further bound to an oxygen atom, e.g. imino-ethers, amidines with replacement of the other oxygen atom of the carboxyl group by nitrogen atoms, e.g. amidines
    • C07C257/18—Compounds containing carboxyl groups, the doubly-bound oxygen atom of a carboxyl group being replaced by a doubly-bound nitrogen atom, this nitrogen atom not being further bound to an oxygen atom, e.g. imino-ethers, amidines with replacement of the other oxygen atom of the carboxyl group by nitrogen atoms, e.g. amidines having carbon atoms of amidino groups bound to carbon atoms of six-membered aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D235/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
    • C07D235/02—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
    • C07D235/04—Benzimidazoles; Hydrogenated benzimidazoles
    • C07D235/24—Benzimidazoles; Hydrogenated benzimidazoles 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 in position 2
    • C07D235/30—Nitrogen atoms not forming part of a nitro radical
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D307/00—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
    • C07D307/02—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings
    • C07D307/34—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D307/56—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members 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
    • C07D307/58—One oxygen atom, e.g. butenolide

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (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)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Diabetes (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Hematology (AREA)
  • Rheumatology (AREA)
  • Vascular Medicine (AREA)
  • Oncology (AREA)
  • Obesity (AREA)
  • Urology & Nephrology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Emergency Medicine (AREA)
  • Pain & Pain Management (AREA)
  • Pulmonology (AREA)
  • Dermatology (AREA)
  • Immunology (AREA)
  • Endocrinology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Ophthalmology & Optometry (AREA)
  • Communicable Diseases (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Other In-Based Heterocyclic Compounds (AREA)

Abstract

Tienen actividad antitrombotica, que en particular inhiben el factor de coagulacion de la sangre IXa, a procedimientos para su preparacion y a su uso como medicamentos. Reivindicacion 1: Un compuesto de la formula (1) y/o todas las formas estereoisomeras del compuesto de la formula (1) y/o las mezclas de estas formas en cualquier relacion, y/o una sal fisiologicamente tolerable del compuesto de la formula (1), en la que R1 es 1) -aril C6-14-Z, donde Z es un grupo que contiene nitrogeno básico y donde el arilo no está sustituido o está mono-, di- o trisustituido con T, 2) -cicloalquil C3-12-Z, donde Z es un grupo que contiene nitrogeno básico y donde el cicloalquilo no está sustituido o está mono-, di- o trisustituido con T, 3) un Het-Z de cuatro a quince miembros, donde Z es un grupo que contiene nitrogeno básico y donde Het no está sustituido o está adicionalmente mono-, di- o trisustituido con T, R2 y R4 son idénticos o diferentes y son, independientemente uno del otro un átomo de hidrogeno o alquilo C1-4, R3 es 1) -alquilen C0-5-arilo C6-14, donde el arilo no está sustituido o está mono-, di- o trisustituido con T; 2) alquileno C0-4-Het, donde Het no está sustituido o está mono-, di- o trisustituido con T, 3) -alquilen C0-4-aril 6-14-Q-arilo C6-14, donde los dos arilos, en cada caso independientemente uno del otro, no están sustituidos o están mono-, di- o trisustituidos con T, 4) -alquilen C0-4-aril C6-14-Q-cicloalquilo C3-12, donde arilo y cicloalquilo, en cada caso independientemente uno del otro, no están sustituidos o están mono-, di- o trisustituidos con T, 5) -alquilen C0-4-aril C6-14-Q-Het, donde arilo y Het, en cada caso independientemente uno del otro, no están sustituidos o están mono-, di- o trisustituidos con T, 6) -alquilen C0-4-Het-Q-arilo C6-14, donde arilo y Het, en cada caso independientemente uno del otro, no están sustituidos o están mono-, di- o trisustituidos con T, o 7) -alquilen C0-4-Het-Q-Het, donde los dos radicales Het en cada caso, independientemente uno del otro, no están sustituidos o están mono-, di- o trisustituidos con T, Q es un enlace covalente, -alquileno C1-4, -NH-, -N(alquilo C1-4)-, -O-, -SO2- o -S-, T es 1) halogeno, 2) -alquilo C1- 6, donde el alquilo no está sustituido o está mono-, di- o trisustituido con fluoroalquilo C1-3, -N-C(O)-OH o -N-C(O)-alquilo C1-4, 3) -fluoroalquilo C1-3, 4) -cicloalquilo C3-8, 5) -OH, 6) -O-alquilo C1-4, 7) -O-fluoroalquilo C1-3, 8) -NO2, 9) -CN, 10) -N(R10)(R11), donde R10 y R11, independientemente uno del otro, son un átomo de hidrogeno, -cicloalquilo C3-8, halogeno o alquilo C1-6, 11) -C(O)-NH-R10, 12) -NH-C(O)-R10, 13) -NH-SO2-R10, 14) -SO2-alquilo C1-4, 15) -SO2-NH-R10, 16) -SO2- fluoroalquilo C1-3, 17) -S-alquilo C1-4 o 18) -S-fluoroalquilo C1-3, R5 y R6 son idénticos o diferentes y son, independientemente uno del otro, un átomo de hidrogeno, -C(O)-R12, -C(O)-O-R12, -C(O)-NH-R12 o -alquilo C1-4, donde R12 es alquilo C1-6, - cicloalquilo C3-8, -arilo C6-14 o Het.
ARP070104011A 2006-09-13 2007-09-11 Derivados de tartrato como inhibidores del factor de coagulacion ixa AR062744A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
DE102006042927 2006-09-13

Publications (1)

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AR062744A1 true AR062744A1 (es) 2008-12-03

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ID=38720737

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Application Number Title Priority Date Filing Date
ARP070104011A AR062744A1 (es) 2006-09-13 2007-09-11 Derivados de tartrato como inhibidores del factor de coagulacion ixa

Country Status (23)

Country Link
US (1) US8263621B2 (es)
EP (1) EP2069288B1 (es)
JP (1) JP5249225B2 (es)
KR (1) KR20090053813A (es)
CN (1) CN101516833B (es)
AR (1) AR062744A1 (es)
AU (1) AU2007297012B2 (es)
BR (1) BRPI0716778A2 (es)
CA (1) CA2663543A1 (es)
CL (1) CL2007002651A1 (es)
CO (1) CO6220943A2 (es)
HK (1) HK1137419A1 (es)
IL (1) IL197505A0 (es)
MA (1) MA30706B1 (es)
MX (1) MX2009001990A (es)
MY (1) MY148254A (es)
NO (1) NO20091106L (es)
NZ (1) NZ575604A (es)
RU (1) RU2446160C2 (es)
TW (1) TWI406852B (es)
UY (1) UY30586A1 (es)
WO (1) WO2008031508A1 (es)
ZA (1) ZA200900806B (es)

Families Citing this family (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101209976B (zh) * 2006-12-29 2012-01-11 中国人民解放军军事医学科学院毒物药物研究所 取代的酒石酸衍生物及其用于制备β-分泌酶抑制剂的用途
TW201033184A (en) 2008-12-05 2010-09-16 Mochida Pharm Co Ltd Morpholinone compounds as factor IXa inhibitors
US8987242B2 (en) 2008-12-05 2015-03-24 Merck Sharp & Dohme Corp. Morpholinone compounds as factor IXA inhibitors
JP5841547B2 (ja) * 2010-02-11 2016-01-13 ブリストル−マイヤーズ スクイブ カンパニーＢｒｉｓｔｏｌ−Ｍｙｅｒｓ Ｓｑｕｉｂｂ Ｃｏｍｐａｎｙ 第ｘｉａ因子阻害剤としてのマクロ環
EP3131897B8 (en) 2014-04-16 2022-08-03 Merck Sharp & Dohme LLC Factor ixa inhibitors

Family Cites Families (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE3731542A1 (de) 1987-09-17 1989-03-30 Schering Ag Neue dicarbonsaeure-bis(3,5-dicarbamoyl-2,4,6-triiod-anilide), verfahren zu deren herstellung sowie diese enthaltende roentgenkontrastmittel
RU2043344C1 (ru) * 1991-05-20 1995-09-10 Курский Государственный Медицинский Институт N-2-(1- r1-5-r2-6-r3- бензимидазолил)сукцинаминовые кислоты, проявляющие нейролептическую, антигипоксическую и антиаритмическую активность
WO1994022885A1 (en) 1993-03-29 1994-10-13 Queen's University At Kingston Anticoagulant compounds
EP1332131A2 (en) 2000-11-07 2003-08-06 Bristol-Myers Squibb Company Acid derivatives useful as serine protease inhibitors
DE10104598A1 (de) 2001-02-02 2002-08-08 Boehringer Ingelheim Pharma Carbonsäureamide, deren Herstellung und deren Verwendung als Arzneimittel
US20020151595A1 (en) 2001-02-02 2002-10-17 Ries Uwe Joerg Carboxylic acid amides having antithrombotic activity
US7122559B2 (en) 2003-02-11 2006-10-17 Bristol-Myers Squibb Company Phenylglycine derivatives useful as serine protease inhibitors
US7638513B2 (en) * 2004-06-02 2009-12-29 Schering Corporation Compounds for the treatment of inflammatory disorders

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JP5249225B2 (ja) 2013-07-31
TWI406852B (zh) 2013-09-01
BRPI0716778A2 (pt) 2014-04-22
AU2007297012B2 (en) 2011-12-22
NO20091106L (no) 2009-06-09
ZA200900806B (en) 2009-12-30
KR20090053813A (ko) 2009-05-27
TW200829557A (en) 2008-07-16
EP2069288A1 (de) 2009-06-17
CA2663543A1 (en) 2008-03-20
JP2010503624A (ja) 2010-02-04
MA30706B1 (fr) 2009-09-01
CL2007002651A1 (es) 2008-02-08
RU2446160C2 (ru) 2012-03-27
EP2069288B1 (de) 2014-03-26
RU2009113616A (ru) 2010-10-20
HK1137419A1 (en) 2010-07-30
US8263621B2 (en) 2012-09-11
US20090233961A1 (en) 2009-09-17
UY30586A1 (es) 2008-05-02
NZ575604A (en) 2011-12-22
MY148254A (en) 2013-03-29
WO2008031508A1 (de) 2008-03-20
CN101516833A (zh) 2009-08-26
MX2009001990A (es) 2009-03-06
AU2007297012A1 (en) 2008-03-20
IL197505A0 (en) 2009-12-24
CN101516833B (zh) 2013-04-03
CO6220943A2 (es) 2010-11-19

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