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PE20090521A1 - Malonamidas como antagonistas de orexina - Google Patents

Malonamidas como antagonistas de orexina

Info

Publication number
PE20090521A1
PE20090521A1 PE2008000482A PE2008000482A PE20090521A1 PE 20090521 A1 PE20090521 A1 PE 20090521A1 PE 2008000482 A PE2008000482 A PE 2008000482A PE 2008000482 A PE2008000482 A PE 2008000482A PE 20090521 A1 PE20090521 A1 PE 20090521A1
Authority
PE
Peru
Prior art keywords
phenyl
malonamide
halogen
dimetoxy
trifluormethyl
Prior art date
Application number
PE2008000482A
Other languages
English (en)
Inventor
Luca Gobbi
Henner Knust
Parichehr Malherbe
Matthias Heinrich Nettekoven
Emmanuel Pinard
Olivier Roche
Mark Roger-Evans
Original Assignee
Hoffmann La Roche
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 Hoffmann La Roche filed Critical Hoffmann La Roche
Publication of PE20090521A1 publication Critical patent/PE20090521A1/es

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    • C07C233/01—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
    • C07C233/16—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by singly-bound oxygen atoms
    • C07C233/24—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by singly-bound oxygen atoms with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by a carbon atom of a six-membered aromatic ring
    • C07C233/29—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by singly-bound oxygen atoms with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by a carbon atom of a six-membered aromatic ring having the carbon atom of the carboxamide group bound to an acyclic carbon atom of a carbon skeleton containing six-membered aromatic rings
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    • C07C233/12—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by halogen atoms or by nitro or nitroso groups
    • C07C233/15—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by halogen atoms or by nitro or nitroso groups with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by a carbon atom of a six-membered aromatic ring
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    • C07C233/32—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by doubly-bound oxygen atoms with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by a carbon atom of a ring other than a six-membered aromatic ring
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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06—Heterocyclic 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
    • C07D211/08—Heterocyclic 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
    • C07D211/10—Heterocyclic 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 radicals containing only carbon and hydrogen atoms attached to ring carbon atoms
    • C07D211/16—Heterocyclic 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 radicals containing only carbon and hydrogen atoms attached to ring carbon atoms with acylated ring nitrogen atom
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    • C07D211/40—Oxygen atoms
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    • C07D213/24—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D213/36—Radicals substituted by singly-bound nitrogen atoms
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    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen 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
    • C07D213/72—Nitrogen atoms
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    • C07D295/00—Heterocyclic 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
    • C07D295/16—Heterocyclic 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
    • C07D295/18—Heterocyclic 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
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    • C07C2601/08—Systems containing only non-condensed rings with a five-membered ring the ring being saturated

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  • Hydrogenated Pyridines (AREA)
  • Pyridine Compounds (AREA)
  • Pyrane Compounds (AREA)

Abstract

REFERIDO A COMPUESTOS DERIVADOS DE MALONAMIDA DE FORMULA (I) DONDE Ar1 Y Ar2 SON CADA UNO ARILO O HETEROARILO; R1 Y R2 SON CADA UNO H, ALQUILO INFERIOR OPCIONALMENTE SUSTITUIDO CON HALOGENO, -(CH2)o-O-ALQUILO INFERIOR, ENTRE OTROS, EN DONDE o ES DE 1 A 3; R ES HALOGENO, ALQUILO INFERIOR OPCIONALMENTE SUSTITUIDO CON HALOGENO O ALCOXI INFERIOR OPCIONALMENTE SUSTITUIDO CON HALOGENO; R3 ES H O ALQUILO INFERIOR; n ES DE 0 A 4. SON COMPUESTOS PREFERIDOS: N-(3,4-DIMETOXI-FENIL)-N'-METIL-2-FENIL-N-[2-(4-TRIFLUORMETIL-FENIL)-ETIL]-MALONAMIDA, N-BUTIL-N'-(3,4-DIMETOXI-FENIL)-2-FENIL-N'-[2-(4-TRIFLUORMETIL-FENIL)-ETIL]-MALONAMIDA, N-CICLOPROPIL-N'-(3,4-DIMETOXI-FENIL)-2-FENIL-N'-[2-(4-TRIFLUORMETIL-FENIL)-ETIL]-MALONAMIDA, ENTRE OTROS. SE REFIERE TAMBIEN A UN PROCESO DE PREPARACION Y A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS SON ANTAGONISTAS DEL RECEPTOR DE LA OREXINA SIENDO UTILES EN EL TRATAMIENTO DE INSOMNIO, DEPRESION, ANSIEDAD
PE2008000482A 2007-03-15 2008-03-14 Malonamidas como antagonistas de orexina PE20090521A1 (es)

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EP07104232 2007-03-15

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US (1) US7501541B2 (es)
EP (1) EP2121579B1 (es)
JP (1) JP5148636B2 (es)
CN (1) CN101636378A (es)
AR (1) AR071925A1 (es)
AT (1) ATE506343T1 (es)
AU (1) AU2008225922B2 (es)
BR (1) BRPI0808737A2 (es)
CA (1) CA2679985A1 (es)
CL (1) CL2008000738A1 (es)
DE (1) DE602008006368D1 (es)
ES (1) ES2361453T3 (es)
IL (1) IL200438A0 (es)
MX (1) MX2009009384A (es)
PE (1) PE20090521A1 (es)
TW (1) TW200843727A (es)
WO (1) WO2008110488A1 (es)

Families Citing this family (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2008225766B2 (en) 2007-03-15 2012-06-07 Novartis Ag Organic compounds and their uses
CN102066325A (zh) * 2008-06-16 2011-05-18 弗·哈夫曼-拉罗切有限公司 作为食欲肽受体拮抗剂的杂芳族单酰胺类
US20100041663A1 (en) 2008-07-18 2010-02-18 Novartis Ag Organic Compounds as Smo Inhibitors
JP5785045B2 (ja) * 2011-10-06 2015-09-24 エヌ・イーケムキャット株式会社 選択的脱ベンジル化方法およびこれに用いる選択水素化触媒
US9029364B2 (en) 2011-10-21 2015-05-12 Merck Sharp & Dohme Corp. 2,5-disubstituted thiomorpholine orexin receptor antagonists
US9440982B2 (en) 2012-02-07 2016-09-13 Eolas Therapeutics, Inc. Substituted prolines/piperidines as orexin receptor antagonists
SG11201404738QA (en) 2012-02-07 2014-10-30 Eolas Therapeutics Inc Substituted prolines / piperidines as orexin receptor antagonists
MA40249A (fr) * 2014-06-27 2017-05-03 Nogra Pharma Ltd Modulateurs des récepteurs d'aryle, et leurs procédés de fabrication et méthodes d'utilisation
UY36272A (es) 2014-08-13 2016-02-29 Eolas Therapeutics Inc Difluoropirrolidinas como moduladores de los receptores de orexinas
JP6883045B2 (ja) 2016-02-12 2021-06-02 アストラゼネカ・アクチエボラーグＡｓｔｒａｚｅｎｅｃａ Ａｋｔｉｅｂｏｌａｇ オレキシン受容体調節因子としてのハロ置換ピペリジン
EP3454857A1 (en) 2016-05-10 2019-03-20 INSERM (Institut National de la Santé et de la Recherche Médicale) Methods and pharmaceutical compositions for the treatment of autoimmune inflammatory diseases
NO345530B1 (en) * 2020-03-20 2021-03-29 Axichem As Synthesis of capsaicin derivatives

Family Cites Families (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3622596A (en) * 1960-10-14 1971-11-23 A Wander Sa Dr Carbanilide compounds
US3529012A (en) * 1966-02-11 1970-09-15 Smithkline Corp Methyl alpha-ethyl-alpha-phenyl-malonamidates
DE3013906A1 (de) * 1980-04-11 1981-10-15 C.H. Boehringer Sohn, 6507 Ingelheim Substituierte (alpha) -aminocarbonyl-l-benzyl-3,4-dihydro-isochinoline, verfahren zu deren herstellung und deren verwendung
AU6659090A (en) * 1989-11-16 1991-06-13 Warner-Lambert Company Acat inhibitors
DE4041482A1 (de) * 1990-12-22 1992-06-25 Boehringer Ingelheim Kg Neue pharmazeutische verwendung carbocyclisch und heterocyclisch annelierter dihydropyridine
EP1661564A1 (fr) * 1999-11-05 2006-05-31 Société de Conseils de Recherches et d'Applications Scientifiques ( S.C.R.A.S.) Nouveaux composés hétérocycliques et leur application à titre de médicaments
EP1193248A1 (en) * 2000-09-30 2002-04-03 Aventis Pharma Deutschland GmbH Malonamid and malonamic ester derivatives with antithrombotic activity, their preparation and their use
ES2297413T3 (es) * 2003-04-28 2008-05-01 Actelion Pharmaceuticals Ltd. Derivados de quinoxalinona-3-ona utilizados como antagonistas del receptor de orexina.
DE602004020680D1 (de) * 2003-09-09 2009-05-28 Hoffmann La Roche Die aktivität von gamma-secretase blockierende malonamidderivate
US20070043076A1 (en) * 2003-10-06 2007-02-22 Cai Sui X Substituted 2-arylmethylene-n-aryl-n'aryl-malonamides and analogs as activators of caspases and inducers of apoptosis
RU2342930C2 (ru) * 2003-10-09 2009-01-10 Уорнер-Ламберт Компани Ллс Фармацевтические композиции, содержащие малонамидные производные для уменьшения продукции кожного сала

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AU2008225922B2 (en) 2012-04-26
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AU2008225922A1 (en) 2008-09-18
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