N-Phenpropylclopentyl-substituted glutaramide derivatives as NEP inhibitors for FSAD.

The invention relates to compounds of formula (I) for treating for example sexual dysfunction, wherein R1 is optionally substituted C1-6alkyl, optionally substituted carbocyclyl, optionally substituted heterocyclyl, hydrogen, C1-6alkoxy, -NR2R3 or -NR4SO2R5; X is the linkage -(CH2)n-or-(CH2)q-O-(wherein y is attached to the oxygen); wherein in one or more hydrogen atoms in linkage X may be replaced independently by C1-4alkoxy; hydroxy; hydroxy(C1-3alkyl); C3-7cycloalkyl; carbocyclyl; heterocyclyl; or by C1-4alkyl optionally substituted by one or more fluoro or phenyl groups; n is 3, 4, 5, 6 or 7; and q is 2, 3, 4, 5 or 6; and Y is phenyl or pyridyl, each of which may be substituted; or two R8 groups on adjacent carbon atoms together with the interconnnecting carbon atoms may form a fused optionally substituted 5- or 6-membered carbocyclic or heterocyclyic ring.

Piperazine derivatives

The present invention relates to a crystalline form of 5-{(1S)-2-[(2R)-4-benzoyl-2-methyl-piperazin-1-yl]-1-methyl-2-oxo-ethoxy}-4-methoxy-pyridine-2-carboxylic acid methylamide, processes for the preparation thereof, compositions containing the crystalline form, and uses of the crystalline form. 5-{(1S)-2-[(2R)-4-Benzoyl-2-methyl-piperazin-1-yl]-1-methyl-2-oxo-ethoxy}-4-methoxy-pyridine-2-carboxylic acid methylamide is particularly suitable as a drug substance and inhibits the interaction of gp120 with CD4 and is therefore of use in the treatment of HIV, a retroviral infection genetically related to HIV, or AIDS.

N-PHENPROPYLCYCLOPENTYL-SUBSTITUTED GLUTARAMIDE DERIVATIVES AS NEP INHIBITORS FOR FSAD

The invention relates to compounds of formula (I) for treating for example sexual dysfunction, wherein R1 is optionally substituted C1-6alkyl, optionally substituted carbocyclyl, optionally substituted heterocyclyl, hydrogen, C1-6alkoxy, -NR2 R3 or - NR4SO2R5; X is the linkage - (CH2)n- or -(CH2)q-O- (wherein Y is attached to the oxygen); wherein one or more hydrogen atoms in linkage X may be replaced independently by C1-4alkoxy; hydroxy; hydroxy(C1-3alkyl); C3-7cycloalkyl; carbocyclyl; heterocyclyl; or by C1-4alkyl optionally substituted by one or more fluoro or phenyl groups; n is 3, 4, 5, 6, or 7; and q is 2, 3, 4, 5 or 6; and Y is phenyl or pyridyl, each of which may be substituted; or two R8 groups on adjacent carbon atoms together with the interconnecting carbon atoms may form a fused optionally substituted 5- or 6-membered carbocyclic or heterocyclyic ring. © KIPO & WIPO 2007 ...

N-phenpropylcyclopentyl-substituted glutaramide derivatives as inhibitors of neutral endopeptidase

The invention relates to compounds of formula (I) for treating for example sexual dysfunction, wherein R<1 >is optionally substituted C1-6alkyl, optionally substituted carbocyclyl, optionally substituted heterocyclyl, hydrogen, C1-6alkoxy, -NR<2>R<3 >or -NR<4>SO2R<5>; X is the linkage -(CH2)n- or -(CH2)q-O- (wherein Y is attached to the oxygen); wherein one or more hydrogen atoms in linkage X may be replaced independently by C1-4alkoxy; hydroxy; hydroxy(C1-3alkyl); C3-7cycloalkyl; carbocyclyl; heterocyclyl; or by C1-4alkyl optionally substituted by one or more fluoro or phenyl groups; n is 3, 4, 5, 6 or 7; and q is 2, 3, 4, 5 or 6; and Y is phenyl or pyridyl, each of which may be substituted; or two R<8 >groups on adjacent carbon atoms together with the interconnecting carbon atoms may form a fused optionally substituted 5- or 6-membered carbocyclic or heterocyclyic ring.

N-phenpropylcyclopentyl-substituted glutaramide derivatives as inhibitors of neutral endopeptidase

The invention relates to compounds of formula (I) for treating for example sexual dysfunction, wherein R<1 >is optionally substituted C1-6alkyl, optionally substituted carbocyclyl, optionally substituted heterocyclyl, hydrogen, C1-6alkoxy, -NR<2 >R<3 >or -NR<4>SO2R<5>; X is the linkage -(CH2)n- or -(CH2)q-O- (wherein Y is attached to the oxygen); wherein one or more hydrogen atoms in linkage X may be replaced independently by C1-4alkoxy; hydroxy; hydroxy(C1-3alkyl); C3-7cycloalkyl; carbocyclyl; heterocyclyl; or by C1-4alkyl optionally substituted by one or more fluoro or phenyl groups; n is 3, 4, 5, 6 or 7; and q is 2, 3, 4, 5 or 6; and Y is phenyl or pyridyl, each of which may be substituted; or two R<8 >groups on adjacent carbon atoms together with the interconnecting carbon atoms may form a fused optionally substituted 5- or 6-membered carbocyclic or heterocyclyic ring.

PIPERAZINE DERIVATIVE

PROBLEM TO BE SOLVED: To provide the crystal form of 5-{(1S)-2-[(2R)-4-benzoyl-2-methyl-piperazin-1-yl]-1-methyl-2-oxo-ethoxy}-4-methoxy-pyridine-2-carboxylic acid methyl amide, to provide a method for producing the same, to provide a medicinal composition containing the crystal form, and to provide the employment of the crystal form. SOLUTION: The 5-{(1S)-2-[(2R)-4-benzoyl-2-methyl-piperazin-1-yl]-1-methyl-2-oxo-ethoxy}-4-methoxy-pyridine-2-carboxylic acid methyl amide is especially suitable as a substance for medicines, inhibits the interaction of gp120 with CD4, and is therefore used for treating HIV, the infection of a retrovirus genetically related to HIV, or AIDS. COPYRIGHT: (C)2006,JPO&NCIPI ...

DERIVATIVES OF GLUTARAMIDA REPLACED WITH N-FENPROPILCICLOPENTILO LIKE INHIBITORS OF NEP FOR FSAD REF.PCS10967

LA INVENCION SE REFIERE A COMPUESTOS DE FORMULA (I)PARA TRATAR, POR EJEMPLO, DISFUNCIOPN SEXUAL, EN LA QUE R1 ES ALQUILO C1-6 OPCIONALMENTE SUSTITUIDO, CARBOCICLICO OPCIONALMENTE SUSTITUIDO, HETEROCICLILO OPCIONALMENTE SUSTITUIDO, HIDROGENO, ALCOXI C1-6, -NR2R3 O -NR4SO2R5, X ES EL ENLACE -(CH2)N O-(C2)Q-O-(DONDE Y ESTA UNIDO AL OXIGENO); DONDE UNO O MAS ATOMOSD E HIDROGENO EN EL ENLACE X SE PUEDEN REEMPLAZAR INDEPENDIENTEMENTE POR ALCOXI C1-4; HIDROXI; HIDROXI(ALQUILO C1-3); CICLOALQUILO C3-7; CARBOCICLILO; HETEROCICLILO; O POR ALQUILO C1-4 OPCIONALMENTE SUSTITUIDO CON UNO O MAS GRUPOS FLUORO O FENILO; N ES 3,4,5,6 O 7; Y Q ES 2,3,4,5 O 6; Y ES FENILO O PIRIDILO, CADA UNO DE LOS CUALES PUEDE ESTAR SUSTITUIDO; O DOS GRUPOS R8 EN LOS TOMOS DE CARBONO ADYACENTES JUNTO CON LOS ATOMOS DE CARONO QUE LE INTERCONECTAN PUEDEN FORMAR UN ANILLO CARBOCICLICO O HETEROCICLICO, CONDENSADO DE 5 O 6 MIEMBROS, OPCIONALMENTE SUSTITUIDO, VER FORMULAS.

N-Phenylpropylcyclopentyl- substituted glutaramide derivatives as NEP inhibitors for FSAD

The invention relates to compounds of formula (I) for treating for example sexual dysfunction, wherein R<1> is optionally substituted C1-6alkyl, optionally substituted carbocyclyl, optionally substituted heterocyclyl, hydrogen, C1-6alkoxy, -NR2 R<3> or - NR<4>SO2R<5>; X is the linkage -(CH2)n- or -(CH2)q-O- (wherein Y is attached to the oxygen); wherein one or more hydrogen atoms in linkage X may be replaced independently by C1-4alkoxy; hydroxy; hydroxy(C1-3alkyl); C3-7cycloalkyl; carbocyclyl; heterocyclyl; or by C1-4alkyl optionally substituted by one or more fluoro or phenyl groups; n is 3, 4, 5, 6, or 7; and q is 2, 3, 4, 5 or 6; and Y is phenyl or pyridyl, each of which may be substituted; or two R<8> groups on adjacent carbon atoms together with the interconnecting carbon atoms may form a fused optionally substituted 5- or 6-membered carbocyclic or heterocyclyic ring.

N-Phenpropylcyclopentyl-Substituted Glutaramide Derivatives as Inhibitors of Neutral Endopeptidase Enzyme (NEP) for Treating Female Sexual Dysfunction (FSAD)

1. Technical Result Increase in treatment efficiency. 2. Essence N-phenpropylcyclopentyl -substituted glutara- mide derivatives of formula 1 wherein R1, X, Y are provided in the description, pharmaceutically acceptable salts thereof, solvates, polymorphs or prodrugs thereof as inhibitors of neutral endopeptidase (NEP) for treatment of the disorders of Female Sexual Dysfunction (FSAD), methods for its production and pharmaceutical compositions on its basis. 3. Field of Application Medicine, pharmacology.

N-phenpropylcyclopentyl-substituted glutaramide derivatives as NEP inhibitors for FSAD

N-phenpropylcyclopentyl-substituted glutaramide derivatives as NEP inhibitors for FSAD

Compounds of formula (I) that are suitable for treating for example sexual dysfunction are disclosed, wherein R1 is optionally substituted C1-6alkyl, optionally substituted carbocyclyl, optionally substituted heterocyclyl, hydrogen, C1- 6alkoxy, -NR2R3 or - NR4SO2R5; X is the linkage -(CH2)n- or -(CH2)q-O- (wherein Y is attached to the oxygen); wherein one or more hydrogen atoms in linkage X may be replaced independently by C1-4alkoxy; hydroxy; hydroxy(C1- 3alkyl); C3-7cycloalkyl; carbocyclyl; heterocyclyl; or by C1-4alkyl optionally substituted by one or more fluoro or phenyl groups; n is 3, 4, 5, 6, or 7; and q is 2, 3, 4, 5 or 6; and Y is phenyl or pyridyl, each of which may be substituted; or two R8 groups on adjacent carbon atoms together with the interconnecting carbon atoms may form a fused optionally substituted 5- or 6-membered carbocyclic or heterocyclic ring.

N-phenpropylcyclopentyl-substituted glutaramide derivatives as NEP inhibitors of FSAD

GLUTARAMIDE DERIVATIVES REPLACED WITH N-FENPROPILCICLOPENTILO AS NEP INHIBITORS FOR FSAD

LA INVENCION SE REFIERE A COMPUESTOS DE FORMULA (I) PARA TRATAR, POR EJEMPLO, DISFUNCION SEXUAL, EN LA QUE R1 ES ALQUILO C1-6 OPCIONALMENTE SUSTITUIDO, CARBOCICLILO OPCIONALMENTE SUSTITUIDO, HETEROCICLILO OPCIONALMENTE SUSTITUIDO, HIDROGENO, ALCOXI C1-6, -NR2R3 O -NR4SO2R5, X ES EL ENLACE -(CH2)n- o -(CH2)q-O- (DONDE Y ESTA UNIDO AL OXIGENO); DONDE UNO O MAS ATOMOS DE HIDROGENO EN EL ENLACE X SE PUEDEN REEMPLAZAR, INDEPENDIENTEMENTE, POR ALCOXI C1-4; HIDROXI; HIDROXI(ALQUILO C1-3); CICLOALQUILO C3-7; CARBOCICLILO; HETEROCICLILO; O POR ALQUILO C1-4 OPCIONALMENTE SUSTITUIDO CON UNO O MAS GRUPOS FLUORO O FENILO; n ES 3, 4, 5, 6 ó 7; Y q ES 2, 3, 4, 5 ó 6; E Y ES FENILO O PIRIDILO, CADA UNO DE LOS CUALES PUEDE ESTAR SUSTITUIDO; O DOS GRUPOS R8 EN LOS ATOMOS DE CARBONO ADYACENTES JUNTO CON LOS ATOMOS DE CARBONO QUE LOS INTERCONECTAN PUEDEN FORMAR UN ANILLO CARBOCICLICO O HETEROCICLICO, CONDENSADO, DE 5 ó 6 MIEMBROS, OPCIONALMENTE SUSTITUIDO.

N-phenpropylcyclopentyl-substituted glutaramide derivatives as nep inhibitors for fsad

Derivatives of n-fenpropylcyclopentylsubstituted glutamide as nep inhibitors for treatment of sexual dysfunction

Derivados de glutaramida sustituida con n-fenpropilciclopentilo como inhibidores de nep para fsad

LA INVENCION SE REFIERE A COMPUESTO DE LA FORMULA II PARA TRATAR POR EJEMPLO DISFUNCION SEXUAL, EN LA QUE R1 ES ALQUILO C1-6 OPCIONALMENTE SUSTITUIDO, CARBOCICLILO OPCIONALMENTE SUSTITUIDO, HETEROCICLILO OPCIONALMENTE SUSTITUIDO,HIDROGENO, ALCOXI C1-6, NR2 R3 O -NR4SO2R5, X ES EL ENLACE -(CH2)N, O (CH2)q-0- DONDE Y ESTA UNIDO AL OXIGENO, DONDE UNO O MAS ATAMOS DE HIDROGENO EN EL ENLACE X SE PUEDEN REEMPLAZAR, INDEPENDIENTEMENTE, POR ALCOXI C1-4, HIDROXI, HIDROXI(ALQUILO C1-3) CICLOALQUILO C3-7, CARBOCICLILO, HETEROCICLILO O POR ALQUILO C1-4 OPCIONALMENTE SUSTITUIDO CON UNO O MAS GRUPOS FLUORO O FENILO.

N-phenpropylcyclopentyl-substituted glutaramide derivatives as NEP inhibitors for FSAD.

Derivados de glutaramida sustituida con n-fenpropilciclopentilo como inhibidores de nep para fsad

LA PRESENTE INVENCION SE REFIERE A INHIBIDORES DE LA ENZIMA ENDOPEPTIDASA NEUTRA (NEP) PARA EL TRASTORNO DE LA EXCITACION SEXUAL FEMENINA (FSAD) DE FORMULA GENERAL (I) EN DONDE R1,Y,X, SON GRUPOS FUNCIONALES DESCRITOS EN EL EXPEDIENTE. ESTOS COMPUESTOS PROPORCIONAN UN MEDIO PARA RECUPERAR UNA RESPUESTA DE EXCITACION SEXUAL NORMAL AL INCREMENTAR EL FLUJO DE SANGRE A NIVEL GENITAL QUE CONDUCE A CONGESTION VAGINAL, CLITORAL Y LABIAL MEJORANDO LA LUBRICACION, ELASTICIDAD Y SENSIBILIDAD GENITAL.