WO2005000281A3 - Derives de pyrazolidinedione - Google Patents

Derives de pyrazolidinedione Download PDF

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Publication number
WO2005000281A3
WO2005000281A3 PCT/EP2004/006471 EP2004006471W WO2005000281A3 WO 2005000281 A3 WO2005000281 A3 WO 2005000281A3 EP 2004006471 W EP2004006471 W EP 2004006471W WO 2005000281 A3 WO2005000281 A3 WO 2005000281A3
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WO
WIPO (PCT)
Prior art keywords
compounds
tautomers
pharmaceutically acceptable
geometric isomers
heteroaryl
Prior art date
Application number
PCT/EP2004/006471
Other languages
English (en)
Other versions
WO2005000281A2 (fr
Inventor
Olivier Houille
Heinz Fretz
Kurt Hilpert
Markus Riederer
Thomas Giller
Oliver Valdenaire
Original Assignee
Actelion Pharmaceuticals Ltd
Olivier Houille
Heinz Fretz
Kurt Hilpert
Markus Riederer
Thomas Giller
Oliver Valdenaire
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 Actelion Pharmaceuticals Ltd, Olivier Houille, Heinz Fretz, Kurt Hilpert, Markus Riederer, Thomas Giller, Oliver Valdenaire filed Critical Actelion Pharmaceuticals Ltd
Priority to CA002529436A priority Critical patent/CA2529436A1/fr
Priority to JP2006515947A priority patent/JP2007506661A/ja
Priority to US10/562,623 priority patent/US20070037846A1/en
Priority to EP04739938A priority patent/EP1638540A2/fr
Publication of WO2005000281A2 publication Critical patent/WO2005000281A2/fr
Publication of WO2005000281A3 publication Critical patent/WO2005000281A3/fr

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic 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
    • C07D401/02—Heterocyclic 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
    • C07D401/04—Heterocyclic 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 directly linked by a ring-member-to-ring-member bond
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/415—1,2-Diazoles
    • A61K31/4152—1,2-Diazoles having oxo groups directly attached to the heterocyclic ring, e.g. antipyrine, phenylbutazone, sulfinpyrazone
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/415—1,2-Diazoles
    • A61K31/4155—1,2-Diazoles non condensed and containing further heterocyclic rings
    • 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
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/04—Antihaemorrhagics; Procoagulants; Haemostatic agents; Antifibrinolytic agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C309/00—Sulfonic acids; Halides, esters, or anhydrides thereof
    • C07C309/63—Esters of sulfonic acids
    • C07C309/64—Esters of sulfonic acids having sulfur atoms of esterified sulfo groups bound to acyclic carbon atoms
    • C07C309/65—Esters of sulfonic acids having sulfur atoms of esterified sulfo groups bound to acyclic carbon atoms of a saturated carbon skeleton
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C45/00—Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C45/00—Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds
    • C07C45/61—Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds by reactions not involving the formation of >C = O groups
    • C07C45/62—Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds by reactions not involving the formation of >C = O groups by hydrogenation of carbon-to-carbon double or triple bonds
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C45/00—Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds
    • C07C45/61—Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds by reactions not involving the formation of >C = O groups
    • C07C45/67—Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds by reactions not involving the formation of >C = O groups by isomerisation; by change of size of the carbon skeleton
    • C07C45/673—Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds by reactions not involving the formation of >C = O groups by isomerisation; by change of size of the carbon skeleton by change of size of the carbon skeleton
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C45/00—Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds
    • C07C45/61—Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds by reactions not involving the formation of >C = O groups
    • C07C45/67—Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds by reactions not involving the formation of >C = O groups by isomerisation; by change of size of the carbon skeleton
    • C07C45/68—Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds by reactions not involving the formation of >C = O groups by isomerisation; by change of size of the carbon skeleton by increase in the number of carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C45/00—Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds
    • C07C45/61—Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds by reactions not involving the formation of >C = O groups
    • C07C45/67—Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds by reactions not involving the formation of >C = O groups by isomerisation; by change of size of the carbon skeleton
    • C07C45/68—Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds by reactions not involving the formation of >C = O groups by isomerisation; by change of size of the carbon skeleton by increase in the number of carbon atoms
    • C07C45/70—Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds by reactions not involving the formation of >C = O groups by isomerisation; by change of size of the carbon skeleton by increase in the number of carbon atoms by reaction with functional groups containing oxygen only in singly bound form
    • C07C45/71—Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds by reactions not involving the formation of >C = O groups by isomerisation; by change of size of the carbon skeleton by increase in the number of carbon atoms by reaction with functional groups containing oxygen only in singly bound form being hydroxy groups
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C47/00—Compounds having —CHO groups
    • C07C47/52—Compounds having —CHO groups bound to carbon atoms of six—membered aromatic rings
    • C07C47/542—Alkylated benzaldehydes
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C47/00—Compounds having —CHO groups
    • C07C47/52—Compounds having —CHO groups bound to carbon atoms of six—membered aromatic rings
    • C07C47/548—Compounds having —CHO groups bound to carbon atoms of six—membered aromatic rings having unsaturation outside the six-membered aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C47/00—Compounds having —CHO groups
    • C07C47/52—Compounds having —CHO groups bound to carbon atoms of six—membered aromatic rings
    • C07C47/56—Compounds having —CHO groups bound to carbon atoms of six—membered aromatic rings containing hydroxy groups
    • C07C47/565—Compounds having —CHO groups bound to carbon atoms of six—membered aromatic rings containing hydroxy groups all hydroxy groups bound to the ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C47/00—Compounds having —CHO groups
    • C07C47/52—Compounds having —CHO groups bound to carbon atoms of six—membered aromatic rings
    • C07C47/575—Compounds having —CHO groups bound to carbon atoms of six—membered aromatic rings containing ether groups, groups, groups, or groups
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/14—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings 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
    • C07D231/28—Two oxygen or sulfur atoms
    • C07D231/30—Two oxygen or sulfur atoms attached in positions 3 and 5
    • C07D231/32—Oxygen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2601/00—Systems containing only non-condensed rings
    • C07C2601/06—Systems containing only non-condensed rings with a five-membered ring
    • C07C2601/08—Systems containing only non-condensed rings with a five-membered ring the ring being saturated

Abstract

L'invention concerne des dérivés de pyrazolidinédione de formule générale (I), dans laquelle R1 désigne un hydrogène, un alkyle éventuellement substitué, un cycloalkyle, un aryle, un arylalkyle, un hétéroaryle, un hétéroarylalkyle ou un alkanoyle; et R2 représente un aryle ou un hétéroaryle; des tautomères de ceux-ci; des isomères géométriques de ceux-ci et des tautomères de ces isomères géométriques, notamment des mélanges de composés individuels de formule (I), ou des tautomères de ceux-ci, et des isomères géométriques de ceux-ci ou des tautomères de ceux-ci, des sels d'ajout acides acceptables sur le plan pharmaceutique des composés qui sont basiques; des sels acceptables sur le plan pharmaceutique de composés renfermant des groupes acides avec des bases; des esters acceptables sur le plan pharmaceutique des composés renfermant des groupes hydroxy ou carboxy; des promédicaments de composés dans lesquels un groupe formant un promédicament est présent; ainsi que des hydrates ou solvates de ceux-ci; lesdits dérivés sont actifs comme antagonistes du récepteur de l'adénosine diphosphate des plaquettes et peuvent être utilisés pour la prévention et/ou le traitement de maladies vasculaires périphériques, vasculaires viscérales, hépatiques et rénales, cardio-vasculaires et cérébro-vasculaires ou d'états associés à l'agrégation plaquettaire, notamment la thrombose et, respectivement, pour la fabrication des médicaments correspondants. Quelques composés, mais pas tous, de la formule (I) susmentionnée sont nouveaux.
PCT/EP2004/006471 2003-06-24 2004-06-16 Derives de pyrazolidinedione WO2005000281A2 (fr)

Priority Applications (4)

Application Number Priority Date Filing Date Title
CA002529436A CA2529436A1 (fr) 2003-06-24 2004-06-16 Derives de pyrazolidinedione
JP2006515947A JP2007506661A (ja) 2003-06-24 2004-06-16 ピラゾリジンジオン誘導体
US10/562,623 US20070037846A1 (en) 2003-06-24 2004-06-16 Pyrazolidinedione derivatives
EP04739938A EP1638540A2 (fr) 2003-06-24 2004-06-16 Dérivés de pyrazolidinedione et leur utilisation comme inhibiteurs d'agrégation plaquettaire

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EPPCT/EP03/006616 2003-06-24
PCT/EP2003/006616 WO2005002574A1 (fr) 2003-06-24 2003-06-24 Derives de pyrazolidinedione et leur utilisation en tant qu'inhibiteurs de l'agregation des plaquettes

Publications (2)

Publication Number Publication Date
WO2005000281A2 WO2005000281A2 (fr) 2005-01-06
WO2005000281A3 true WO2005000281A3 (fr) 2005-04-14

Family

ID=33547562

Family Applications (2)

Application Number Title Priority Date Filing Date
PCT/EP2003/006616 WO2005002574A1 (fr) 2003-06-24 2003-06-24 Derives de pyrazolidinedione et leur utilisation en tant qu'inhibiteurs de l'agregation des plaquettes
PCT/EP2004/006471 WO2005000281A2 (fr) 2003-06-24 2004-06-16 Derives de pyrazolidinedione

Family Applications Before (1)

Application Number Title Priority Date Filing Date
PCT/EP2003/006616 WO2005002574A1 (fr) 2003-06-24 2003-06-24 Derives de pyrazolidinedione et leur utilisation en tant qu'inhibiteurs de l'agregation des plaquettes

Country Status (6)

Country Link
EP (1) EP1638540A2 (fr)
JP (1) JP2007506661A (fr)
CN (1) CN1812782A (fr)
AU (1) AU2003249865A1 (fr)
CA (1) CA2529436A1 (fr)
WO (2) WO2005002574A1 (fr)

Families Citing this family (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2005026127A1 (fr) * 2003-09-11 2005-03-24 Institute Of Medicinal Molecular Design. Inc. Inhibiteur d'inhibiteur-1 activateur de plasmogene
WO2007020935A1 (fr) * 2005-08-17 2007-02-22 Ono Pharmaceutical Co., Ltd. Agent thérapeutique pour soulager la douleur, comprenant un récepteur p2y12 et/ou un bloqueur de récepteur p2y14
TWI391378B (zh) 2006-03-16 2013-04-01 Astellas Pharma Inc 喹啉酮衍生物或其製藥學上可被容許之鹽
EP2238128B1 (fr) 2007-12-26 2012-08-22 Sanofi Pyrazole-carboxamides hétérocycliques utilisés en tant qu'antagonistes du récepteur p2y12
EP2238127B1 (fr) 2007-12-26 2012-08-15 Sanofi Dérivés de pyrazole-carboxamide utiles en tant qu'antagonistes de p2y12
JP6016788B2 (ja) * 2011-05-16 2016-10-26 国立大学法人九州大学 ＤＯＣＫ−Ａサブファミリー分子によるＲａｃ活性化を制御する低分子化合物及びその用途
US10822357B2 (en) 2015-08-28 2020-11-03 Sekisui Medical Co., Ltd. Benzyl compound
WO2017131149A1 (fr) * 2016-01-29 2017-08-03 小野薬品工業株式会社 Dérivé de tétrahydronaphtalène
MA49887A (fr) * 2017-03-15 2020-06-24 Idorsia Pharmaceuticals Ltd Administration sous-cutanée d'un antagoniste du récepteur p2y12
EP3661912B9 (fr) 2017-07-31 2024-02-28 Horitzonts Tecnologics Hungary Korlátolt Felelosségu Társaság Composés destinés au traitement d'infections

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2012634A1 (fr) * 1990-03-20 1991-09-20 Hassan Salari Tyrphostines pour le traitement des allergies et des affections inflammatoires et cardiovasculaires
WO2001009121A2 (fr) * 1999-07-30 2001-02-08 Basf Aktiengesellschaft 2-pyrazolin-5-ones
WO2002102359A2 (fr) * 2001-06-18 2002-12-27 Applied Research Systems Ars Holding N.V. Derives d'alkylidene pyrazolidinedione
WO2003074550A2 (fr) * 2002-03-01 2003-09-12 Pintex Pharmaceuticals, Inc. Composes de modulation de pin1 et procedes d'utilisation correspondant

Family Cites Families (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1404682B1 (fr) * 2001-06-29 2005-09-14 Novo Nordisk A/S Procede permettant d'inhiber ptp1b et / ou ptp de lymphocyteet et / ou d'autres ptpases a reste asp en position 48

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2012634A1 (fr) * 1990-03-20 1991-09-20 Hassan Salari Tyrphostines pour le traitement des allergies et des affections inflammatoires et cardiovasculaires
WO2001009121A2 (fr) * 1999-07-30 2001-02-08 Basf Aktiengesellschaft 2-pyrazolin-5-ones
WO2002102359A2 (fr) * 2001-06-18 2002-12-27 Applied Research Systems Ars Holding N.V. Derives d'alkylidene pyrazolidinedione
WO2003074550A2 (fr) * 2002-03-01 2003-09-12 Pintex Pharmaceuticals, Inc. Composes de modulation de pin1 et procedes d'utilisation correspondant

Also Published As

Publication number Publication date
AU2003249865A1 (en) 2005-01-21
JP2007506661A (ja) 2007-03-22
CN1812782A (zh) 2006-08-02
CA2529436A1 (fr) 2005-01-16
WO2005000281A2 (fr) 2005-01-06
EP1638540A2 (fr) 2006-03-29
WO2005002574A1 (fr) 2005-01-13

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