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PE20081349A1 - DERIVADOS DE UREA Y DERIVADOS DE SULFAMIDA EN CALIDAD DE INHIBIDORES DE TAFIa - Google Patents

DERIVADOS DE UREA Y DERIVADOS DE SULFAMIDA EN CALIDAD DE INHIBIDORES DE TAFIa

Info

Publication number
PE20081349A1
PE20081349A1 PE2007001712A PE2007001712A PE20081349A1 PE 20081349 A1 PE20081349 A1 PE 20081349A1 PE 2007001712 A PE2007001712 A PE 2007001712A PE 2007001712 A PE2007001712 A PE 2007001712A PE 20081349 A1 PE20081349 A1 PE 20081349A1
Authority
PE
Peru
Prior art keywords
alkyl
amino
derivatives
sulfamidyl
ethyl
Prior art date
Application number
PE2007001712A
Other languages
English (en)
Inventor
Christopher Kallus
Mark Broenstrup
Werngard Czechtizky
Andreas Evers
Markus Follmann
Nis Halland
Herman Schreuder
Original Assignee
Sanofi Aventis
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 Sanofi Aventis filed Critical Sanofi Aventis
Publication of PE20081349A1 publication Critical patent/PE20081349A1/es

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    • A—HUMAN NECESSITIES
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    • 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
    • A61K31/4164—1,3-Diazoles
    • A—HUMAN NECESSITIES
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    • A61K31/16—Amides, e.g. hydroxamic acids
    • A61K31/17—Amides, e.g. hydroxamic acids having the group >N—C(O)—N< or >N—C(S)—N<, e.g. urea, thiourea, carmustine
    • A—HUMAN NECESSITIES
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    • A61K31/16—Amides, e.g. hydroxamic acids
    • A61K31/18—Sulfonamides
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    • A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/19—Carboxylic acids, e.g. valproic acid
    • A61K31/195—Carboxylic acids, e.g. valproic acid having an amino group
    • A61K31/197—Carboxylic acids, e.g. valproic acid having an amino group the amino and the carboxyl groups being attached to the same acyclic carbon chain, e.g. gamma-aminobutyric acid [GABA], beta-alanine, epsilon-aminocaproic acid or pantothenic acid
    • A61K31/198—Alpha-amino acids, e.g. alanine or edetic acid [EDTA]
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    • A61K31/215—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids
    • A61K31/22—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin
    • A61K31/223—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin of alpha-aminoacids
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    • A61K31/445—Non condensed piperidines, e.g. piperocaine
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Abstract

REFERIDA UN DERIVADO DE SULFAMIDA DE FORMULA (I), DONDE X ES SO2; R1 ES H, ALQUILO C1-C6, ALQUILENO C0-C4-CICLOALQUILO C3-C12, ENTRE OTROS; R2 ES -(A1)m-A2; m ES 0 O 1; A1 ES (CH2)n, NH-(CH2)n, NH(ALQUILO C1-C6)-(CH2)n, ENTRE OTROS; n ES 1, 2 O 3; A2 ES ALQUILEN C0-C6-NH2, ALQUILEN C1-C6-NH-C(=NH)-NH2, ALQUILEN C1-C6-NH-C(=NH)-ALQUILO C1-C4, ENTRE OTROS; R3 ES ALQUILO C1-C6, ALQUILEN C0-C4-CICLOALQUILO C3-C12, ALQUILEN C0-C8-O-PG, ENTRE OTROS; R4 ES ALQUILO C1-C6, H, ALQUILEN C0-C8-O-PG, ENTRE OTROS; PG ES UN GRUPO PROTECTOR PARA LA FUNCION AMINO, CARBOXILO, HIDROXI; R7 ES H O ALQUILO C1-C6; R9 ES H O ALQUILO C1-C6. SON COMPUESTOS PREFERIDOS: ACIDO (S)-6-AMINO-2-(3-{(S)-1-[(S)-1-((S)-1-METOXICARBONIL-2-METIL-PROPILCARBAMOIL)-2-METIL-PROPILCARBAMOIL]-2-FENIL-ETIL}-SULFAMIDIL)-HEXANOICO, ACIDO (S)-6-AMINO-2-{3--[(R)-1-(BICICLO[2.2.1]HEPT-2-ILCARBAMOIL)-2-CICLOHEXIL-ETIL-SULFAMIDIL}-HEXANOICO, ACIDO (S)-6-AMINO-2-[3-((S)-1-CICLOHEXILCARBAMOIL-2-FENIL-ETIL)-SULFAMIDIL]-HEXANOICO, ENTRE OTROS. TAMBIEN ESTA REFERIDA A UN PROCEDIMIENTO DE PREPARACION. DICHOS COMPUESTOS SON INHIBIDORES DE LA ENZIMA TAFIa (INHIBIDOR DE LA FIBRINOLISIS ACTIVABLE POR TROMBINA ACTIVADO) Y SON UTILES EN EL TRATAMIENTO DE TRASTORNOS ASOCIADOS A TROMBOSIS, EMBOLISMOS, CAMBIOS FIBROTICOS, ENTRE OTROS
PE2007001712A 2006-12-06 2007-12-04 DERIVADOS DE UREA Y DERIVADOS DE SULFAMIDA EN CALIDAD DE INHIBIDORES DE TAFIa PE20081349A1 (es)

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US8580777B2 (en) 2008-06-06 2013-11-12 Sanofi Macrocyclic urea and sulfamide derivatives as inhibitors of TAFIa
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CA2741783A1 (en) * 2008-10-29 2010-05-06 Taisho Pharmaceutical Co., Ltd. Compounds having tafia inhibitory activity
SG11201509144YA (en) * 2013-06-10 2015-12-30 Sanofi Sa MACROCYCLIC UREA DERIVATIVES AS INHIBITORS OF TAFI<sb>A</sb>, THEIR PREPARATION AND THEIR USE AS PHARMACEUTICALS
CN104529859B (zh) * 2015-01-13 2016-08-17 佛山市赛维斯医药科技有限公司 含苯胺和二烯氟代金刚烷结构的化合物、其制备方法和用途
RU2687254C1 (ru) * 2018-10-03 2019-05-08 Федеральное государственное бюджетное учреждение науки Новосибирский институт органической химии им. Н.Н. Ворожцова Сибирского отделения Российской академии наук (НИОХ СО РАН) N-гетероциклические производные борниламина в качестве ингибиторов ортопоксвирусов

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