AR052197A1 - COMPOSITION CONTAINING DERIVATIVES OF CYANOPIRROLIDINE FOR SOLID PHARMACEUTICAL PREPARATIONS, SOLID PHARMACEUTICAL PREPARATION CONTAINING COMPOSITION, AND PROCESS TO PRODUCE SOLID PHARMACEUTICAL PREPARATION - Google Patents

COMPOSITION CONTAINING DERIVATIVES OF CYANOPIRROLIDINE FOR SOLID PHARMACEUTICAL PREPARATIONS, SOLID PHARMACEUTICAL PREPARATION CONTAINING COMPOSITION, AND PROCESS TO PRODUCE SOLID PHARMACEUTICAL PREPARATION

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AR052197A1
AR052197A1 ARP060100263A ARP060100263A AR052197A1 AR 052197 A1 AR052197 A1 AR 052197A1 AR P060100263 A ARP060100263 A AR P060100263A AR P060100263 A ARP060100263 A AR P060100263A AR 052197 A1 AR052197 A1 AR 052197A1
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Argentina
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group
substituted
represented
hydrogen atom
atom
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ARP060100263A
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Spanish (es)
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Hiroaki Yazaki
Hiroshi Ikuta
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Taisho Pharmaceutical Co Ltd
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Publication of AR052197A1 publication Critical patent/AR052197A1/en

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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2013Organic compounds, e.g. phospholipids, fats
    • A61K9/2018Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2022Organic macromolecular compounds
    • A61K9/205Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2054Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Diabetes (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Organic Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Endocrinology (AREA)
  • Emergency Medicine (AREA)
  • Biophysics (AREA)
  • Molecular Biology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)

Abstract

La presente se refiere al tratamiento de diabetes. Reivindicacion 1: Una composicion para preparaciones farmacéuticas solidas, caracterizada porque consiste esencialmente en un derivado de cianopirrolidina representado por la formula general (1) o una de sus sales farmacéuticamente aceptables, y por lo menos un ingrediente estabilizante seleccionado del grupo que consiste en azucares y alcoholes de azucar; [en donde R1 representa un átomo de halogeno, grupo hidroxilo, grupo alcoxi C1-5 o grupo alquilo C1-5, R2 representa un átomo de hidrogeno, átomo de halogeno, grupo hidroxilo, grupo alcoxi C1-5, o grupo alquilo C1-5, o R1 y R2 enlazados para formar grupo oxo, grupo hidroxiimino, grupo alcoxiimino C1-5 o grupo alquilideno C1-5; R3 y R4 pueden ser iguales o diferentes, representando cada uno un átomo de hidrogeno, un átomo de halogeno, grupo hidroxilo, grupo alcoxi C1-5 o grupo alquilo C1-5, o R3 y R4 enlazados para formar grupo oxo, grupo hidroxiimino, grupo alcoxiimino C1-5 o grupo alquilideno C1-5; X representa un átomo de oxígeno o un átomo de azufre; Y representa grupo representado por -CR5R6- [en donde R5 y R6 pueden ser iguales o diferentes, representando cada uno un átomo de hidrogeno; un átomo de halogeno; grupo alquilo C1-10 que puede ser sustituido con uno o más grupos seleccionados del grupo que consiste en un átomo de halogeno, grupo hidroxilo, grupo hidroxialquilo C1-5, grupo carboxilo, grupo mercapto, grupo alquiltio C1-5, grupo guanidilo, grupo fenilo que puede ser sustituido, grupo imidazolilo, grupo indolilo, grupo representado por -NHR11 (en donde R11 representa un átomo de hidrogeno, grupo fenilo que puede ser sustituido, grupo piridilo que puede ser sustituido, grupo tert- butoxicarbonilo o grupo benciloxicarbonilo), grupo representado por -CONHR12 (en donde R12 representa un átomo de hidrogeno o grupo representado por -(CH2)m-R13 (en donde m representa un entero de 1 a 5, y R13 representa átomo de hidrogeno, grupo metoxicarbonilo, grupo etoxicarbonilo o grupo benciloxicarbonilo) y grupo representado por -OR14 (en donde R14 representa grupo alquilo de cadena C1-5 o grupo bencilo); o grupo alquenilo C2-10 que puede ser sustituido con uno o más grupos seleccionados del grupo que consiste en un átomo de halogeno, grupo hidroxilo, grupo carboxilo, grupo amino, grupo aminocarbonilo y grupo alcoxi de cadena C1-5], o grupo representado por -CR7R8-CR9R10- (en donde R7, R8, R9 y R10 pueden ser iguales o diferentes, representando cada uno un átomo de hidrogeno; un átomo de halogeno; o grupo alquilo C1-10 que puede ser sustituido con uno o más grupos seleccionados del grupo que consiste en un átomo de halogeno, grupo hidroxilo, grupo hidroxialquilo C1-5, grupo carboxilo, grupo mercapto, grupo alquiltio C1-5, grupo guanidilo, grupo fenilo que puede ser sustituido, grupo imidazolilo, grupo indolilo, grupo representado por -NHR11 (en donde R11 representa un átomo de hidrogeno, grupo fenilo que puede ser sustituido, grupo piridilo que puede ser sustituido, grupo tert- butoxicarbonilo o grupo benciloxicarbonilo), grupo representado por -CONHR12 (en donde R12 representa un átomo de hidrogeno o grupo representado por -(CH2)m-R13 (en donde m representa un entero de 1 a 5, y R13 representa un átomo de hidrogeno, grupo metoxicarbonilo, grupo etoxicarbonilo o grupo benciloxicarbonilo) y grupo representado por -OR14 (en donde R14 representa grupo alquilo de cadena C1-5 o grupo bencilo); o R7, R9 y un átomo de carbono adyacente enlazados para formar: los grupos representados cada uno con cicloalquilo C3-8, cicloalquenilo C4-8, bicicloalquilo C5-10, o bicicloalquenilo C5-10 que pueden ser sustituidos con uno o más grupos seleccionados del grupo que consiste en un átomo de halogeno, grupo hidroxilo, grupo carboxilo, grupo amino, grupo aminocarbonilo, grupo alquilo de cadena C1-5 y grupo alcoxi de cadena C1-5); W representa un átomo de hidrogeno, grupo acilo derivado de aminoácidos que ocurren naturalmente, grupo representado por la formula general (2), [en donde W1 representa grupo alcanoilo C1-5, grupo arilcarbonilo que puede ser sustituido o grupo alquilo C1-5, y W2 representa un átomo de hidrogeno o grupo alquilo C1-5]; o grupo representado por la formula general (3), [en donde W3 y W4 pueden ser iguales o diferentes, representando cada uno un átomo de hidrogeno o grupo alquilo C1-5]; Z representa un átomo de hidrogeno; grupo alquilo C1-10 que puede ser sustituido con uno o más grupos seleccionados del grupo que consiste en un átomo de halogeno, grupo hidroxilo, grupo hidroxialquilo C1-5, grupo carboxilo, grupo mercapto, grupo alquiltio C1-5, grupo guanidilo, grupo fenilo que puede ser sustituido, grupo imidazolilo, grupo indolilo, grupo representado por -NHR11 (en donde R11 representa átomo de hidrogeno, grupo fenilo que puede ser sustituido, grupo piridilo que puede ser sustituido, grupo tert-butoxicarbonilo o grupo benciloxicarbonilo), grupo representado por -CONHR12 (en donde R12 representa átomo de hidrogeno o grupo representado por -(CH2)m-R13 (en donde m representa un entero de 1 a 5, y R13 representa un átomo de hidrogeno, grupo metoxicarbonilo, grupo etoxicarbonilo o grupo benciloxicarbonilo)) y grupo representado por -OR14 (en donde R14 representa grupo alquilo de cadena C1-5 o grupo bencilo); o grupo representado por la formula general (4), [en donde R15 y R16 pueden ser iguales o diferentes, representando cada uno un átomo de hidrogeno; grupo alquilo C1-6 que puede ser sustituido con uno o más sustituyentes seleccionados del siguiente grupo sustituyente Y1; los grupos representados cada uno con cicloalquilo C3-6, cicloalquilo C4-9, alquenilo C2-6, cicloalquenilo C3-6 y cicloalquenilo C4-9 que pueden ser sustituidos con uno o más sustituyentes seleccionados del siguiente grupo sustituyente Y2; o R15, R16 y un átomo de carbono adyacente enlazados para formar grupo cicloalquilo C3-10 que puede ser sustituido con uno o más sustituyentes seleccionados del siguiente grupo sustituyente Y2; A representa un enlace simple o grupo alquileno C1-3; R17 representa grupo representado por -N(R18)COR19, -N(R18)SO2R19, -NR18R20, -SO2R19, -SO2NR18R19, - OCONR18R19, -CH=CH-R21 o -C:::C-R21; o grupo heteroarilo seleccionado de grupos heteroarilo que tienen por lo menos un átomo de oxígeno y/o un átomo de azufre y puede tener también un átomo de nitrogeno, anillos aromáticos de 6 miembros conteniendo nitrogeno, y anillos condensados de 9 a 11 miembros de ellos (aquí, los grupos heteroarilo pueden ser sustituidos con uno o más sustituyentes seleccionados del siguiente sustituyente Y3), (en donde R18 y R20 pueden ser iguales o diferentes, representando cada uno: un átomo de hidrogeno; grupo alquilo C1-10 que puede ser sustituido con uno o más sustituyentes seleccionados del siguiente grupo sustituyente Y4; los grupos representados cada uno con cicloalquilo C3-6, cicloalquilo C4-9 que puede ser sustituido con uno o más sustituyentes seleccionados del siguiente grupo sustituyente Y2; o grupo arilalquilo que puede ser sustituido con uno o más sustituyentes seleccionados del siguiente grupo sustituyente Y3; R19 representa: grupo alquilo C1-10 que puede ser sustituido con uno o más sustituyentes seleccionados del siguiente grupo sustituyente Y4; la siguiente Q; o -alquilenoC1-3-Q, el alquileno C1-3 puede ser sustituido con uno o más sustituyentes seleccionados de un átomo de halogeno y grupo hidroxilo, el Q representa hidrocarburo alifático o aromático seleccionado del grupo que consiste en los grupos representados cada uno con cicloalquilo C3-10, alquilo cíclico de puente C4-10, alquenilo C2-10, cicloalquenilo C3-10, grupo alquenilo cíclico de puente C4-10 y arilo que pueden ser sustituidos con uno o más sustituyentes seleccionados del siguiente grupo sustituyente Y3; o anillo heterocíclico que puede ser sustituido con uno o más sustituyentes seleccionados del siguiente grupo sustituyente Y5; en R19 que representa un grupo arilo o anillo heterocíclico puede formar un anillo de 5 a 8 miembros combinando un sustituyente adyacente al átomo que constituye su anillo, y puede contener uno o más heteroátomos en el anillo; R18, R19 o R20 pueden enlazarse a un heteroátomo adyacente a R18 y R19, R18 y R20, o R19 y R20 para formar un anillo heterocíclico de 4 a 10 miembros que puede ser sustituido con uno o más sustituyentes seleccionados del siguiente grupo sustituyente Y5; y R21 representa un átomo de hidrogeno; grupo alquilo C1-6 que puede ser sustituido con uno o más sustituyentes seleccionados del siguiente grupo sustituyente Y1; y los grupos represetados cada uno con arilo, o heteroarilo que pueden ser sustituidos con uno o más sustituyentes seleccionados del siguiente grupo sustituyente Y3)]; o Y, Z y un átomo adyacentes de nitrogeno enlazados para formar un grupo amino cíclico C2-10 que puede ser sustituido con uno o más grupos seleccionados del grupo que consiste en un átomo de halogeno, grupo hidroxilo, grupo amino, grupo alquilo de cadena C1-5 y grupo representado por -OR22 (en donde R22 representa grupo alquilo de cadena C1-5, grupo aminocarbonilmetilo o grupo bencilo)]; (grupo sustituyente Y1): grupo que consiste en un átomo de halogeno, grupo hidroxilo, grupo carboxilo, grupo ciano, grupo amino, grupo aminocarbonilo, grupo cicloalquiloxi C3-5 y grupo alcoxi C1-6; (grupo sustituyente Y2): grupo que consiste en un átomo de halogeno, grupo hidroxilo, grupo carboxilo, grupo ciano, grupo amino, grupo aminocarbonilo, grupo cicloalquiloxi C3-5, grupo alcoxi C1-6 y grupo alquilo C1-6; (grupo sustituyente Y3): grupo que consiste en un átomo de halogeno, grupo hidroxilo, grupo ciano, grupo nitro, grupo amino, grupos representados por -OR30, - COR30, -CO2R30, -CONR30R31, -N(R30)COR31, -N(R30)CONR31R32, -N(R30)SO2R31, -NR30R31, -SO2R30, -SO2NR30R31, -SO2N= CHNR30R31 y -OCONR30R31 (en donde R30, R31, y R32 pueden ser iguales o diferentes, representando cada uno un átomo de hidrogeno; grupo alquilo C1-6 que puede ser sustituido con uno oThis refers to the treatment of diabetes. Claim 1: A composition for solid pharmaceutical preparations, characterized in that it consists essentially of a cyanopyrrolidine derivative represented by the general formula (1) or a pharmaceutically acceptable salt thereof, and at least one stabilizing ingredient selected from the group consisting of sugars and sugar alcohols; [wherein R1 represents a halogen atom, hydroxyl group, C1-5 alkoxy group or C1-5 alkyl group, R2 represents a hydrogen atom, halogen atom, hydroxyl group, C1-5 alkoxy group, or C1- alkyl group 5, or R1 and R2 linked to form oxo group, hydroxyimino group, C1-5 alkoxyimino group or C1-5 alkylidene group; R3 and R4 may be the same or different, each representing a hydrogen atom, a halogen atom, hydroxyl group, C1-5 alkoxy group or C1-5 alkyl group, or R3 and R4 linked to form oxo group, hydroxyimino group, C1-5 alkoxyimino group or C1-5 alkylidene group; X represents an oxygen atom or a sulfur atom; Y represents a group represented by -CR5R6- [where R5 and R6 can be the same or different, each representing a hydrogen atom; a halogen atom; C1-10 alkyl group which can be substituted with one or more groups selected from the group consisting of a halogen atom, hydroxyl group, C1-5 hydroxyalkyl group, carboxyl group, mercapto group, C1-5 alkylthio group, guanidyl group, group phenyl that can be substituted, imidazolyl group, indolyl group, group represented by -NHR11 (where R11 represents a hydrogen atom, phenyl group that can be substituted, pyridyl group that can be substituted, tert-butoxycarbonyl group or benzyloxycarbonyl group), group represented by -CONHR12 (where R12 represents a hydrogen atom or group represented by - (CH2) m-R13 (where m represents an integer from 1 to 5, and R13 represents hydrogen atom, methoxycarbonyl group, ethoxycarbonyl group or benzyloxycarbonyl group) and group represented by -OR14 (where R14 represents C1-5 alkyl group or benzyl group); or C2-10 alkenyl group which can be substituted with one or more groups selected from the gr upo consisting of a halogen atom, hydroxyl group, carboxyl group, amino group, aminocarbonyl group and C1-5 alkoxy group], or group represented by -CR7R8-CR9R10- (where R7, R8, R9 and R10 can be the same or different, each representing a hydrogen atom; a halogen atom; or C1-10 alkyl group which can be substituted with one or more groups selected from the group consisting of a halogen atom, hydroxyl group, C1-5 hydroxyalkyl group, carboxyl group, mercapto group, C1-5 alkylthio group, guanidyl group, phenyl group that can be substituted, imidazolyl group, indolyl group, group represented by -NHR11 (where R11 represents a hydrogen atom, phenyl group that can be substituted, pyridyl group that can be substituted, tert-butoxycarbonyl group or benzyloxycarbonyl group) , group represented by -CONHR12 (where R12 represents a hydrogen atom or group represented by - (CH2) m-R13 (where m represents an integer from 1 to 5, and R13 represents a hydrogen atom, methoxycarbonyl group, group ethoxycarbonyl or benzyloxycarbonyl group) and group represented by -OR14 (where R14 represents C1-5 alkyl group or benzyl group); or R7, R9 and an adjacent carbon atom linked to form: the groups represents two each with C3-8 cycloalkyl, C4-8 cycloalkenyl, C5-10 bicycloalkyl, or C5-10 bicycloalkenyl which may be substituted with one or more groups selected from the group consisting of a halogen atom, hydroxyl group, carboxyl group, amino group, aminocarbonyl group, C1-5 chain alkyl group and C1-5 chain alkoxy group); W represents a hydrogen atom, acyl group derived from naturally occurring amino acids, group represented by the general formula (2), [wherein W1 represents C1-5 alkanoyl group, arylcarbonyl group that can be substituted or C1-5 alkyl group, and W2 represents a hydrogen atom or C1-5 alkyl group]; or group represented by the general formula (3), [wherein W3 and W4 can be the same or different, each representing a hydrogen atom or C1-5 alkyl group]; Z represents a hydrogen atom; C1-10 alkyl group which can be substituted with one or more groups selected from the group consisting of a halogen atom, hydroxyl group, C1-5 hydroxyalkyl group, carboxyl group, mercapto group, C1-5 alkylthio group, guanidyl group, group phenyl that can be substituted, imidazolyl group, indolyl group, group represented by -NHR11 (where R11 represents hydrogen atom, phenyl group that can be substituted, pyridyl group that can be substituted, tert-butoxycarbonyl group or benzyloxycarbonyl group), group represented by -CONHR12 (where R12 represents hydrogen atom or group represented by - (CH2) m-R13 (where m represents an integer from 1 to 5, and R13 represents a hydrogen atom, methoxycarbonyl group, ethoxycarbonyl group or group benzyloxycarbonyl)) and group represented by -OR14 (wherein R14 represents C1-5 alkyl group or benzyl group); or group represented by the general formula (4), [wherein R15 and R16 may be the same or different, each representing a hydrogen atom; C1-6 alkyl group which can be substituted with one or more substituents selected from the following substituent group Y1; the groups each represented with C3-6 cycloalkyl, C4-9 cycloalkyl, C2-6 alkenyl, C3-6 cycloalkenyl and C4-9 cycloalkenyl which may be substituted with one or more substituents selected from the following substituent group Y2; or R15, R16 and an adjacent carbon atom linked to form C3-10 cycloalkyl group which can be substituted with one or more substituents selected from the following substituent group Y2; A represents a single bond or C1-3 alkylene group; R17 represents group represented by -N (R18) COR19, -N (R18) SO2R19, -NR18R20, -SO2R19, -SO2NR18R19, - OCONR18R19, -CH = CH-R21 or -C ::: C-R21; or heteroaryl group selected from heteroaryl groups having at least one oxygen atom and / or one sulfur atom and may also have a nitrogen atom, 6-membered aromatic rings containing nitrogen, and condensed rings of 9 to 11 members thereof (Here, the heteroaryl groups can be substituted with one or more substituents selected from the following substituent Y3), (wherein R18 and R20 may be the same or different, each representing: a hydrogen atom; C1-10 alkyl group which may be substituted with one or more substituents selected from the following substituent group Y4; the groups each represented with C3-6 cycloalkyl, C4-9 cycloalkyl which may be substituted with one or more substituents selected from the following substituent group Y2; or arylalkyl group which may be substituted with one or more substituents selected from the following substituent group Y3; R19 represents: C1-10 alkyl group which can be substituted with one or more substituents selected from the following substituent group Y4; the following Q; or -C1-3-Q alkylene, C1-3 alkylene can be substituted with one or more substituents selected from a halogen atom and hydroxyl group, the Q represents aliphatic or aromatic hydrocarbon selected from the group consisting of the groups represented each with C3-10 cycloalkyl, C4-10 bridge cyclic alkyl, C2-10 alkenyl, C3-10 cycloalkenyl, C4-10 bridge cyclic alkenyl group and aryl which may be substituted with one or more substituents selected from the following substituent group Y3; or heterocyclic ring that can be substituted with one or more substituents selected from the following substituent group Y5; in R19 representing an aryl group or heterocyclic ring it can form a 5- to 8-membered ring by combining a substituent adjacent to the atom that constitutes its ring, and can contain one or more heteroatoms in the ring; R18, R19 or R20 can be linked to a heteroatom adjacent to R18 and R19, R18 and R20, or R19 and R20 to form a 4- to 10-membered heterocyclic ring that can be substituted with one or more substituents selected from the following substituent group Y5; and R21 represents a hydrogen atom; C1-6 alkyl group which can be substituted with one or more substituents selected from the following substituent group Y1; and the groups each represented with aryl, or heteroaryl which may be substituted with one or more substituents selected from the following substituent group Y3)]; or Y, Z and an adjacent nitrogen atom linked to form a C2-10 cyclic amino group that can be substituted with one or more groups selected from the group consisting of a halogen atom, hydroxyl group, amino group, chain alkyl group C1-5 and group represented by -OR22 (wherein R22 represents C1-5 alkyl group, aminocarbonylmethyl group or benzyl group)]; (substituent group Y1): group consisting of a halogen atom, hydroxyl group, carboxyl group, cyano group, amino group, aminocarbonyl group, C3-5 cycloalkyloxy group and C1-6 alkoxy group; (substituent group Y2): group consisting of a halogen atom, hydroxyl group, carboxyl group, cyano group, amino group, aminocarbonyl group, C3-5 cycloalkyloxy group, C1-6 alkoxy group and C1-6 alkyl group; (substituent group Y3): group consisting of a halogen atom, hydroxyl group, cyano group, nitro group, amino group, groups represented by -OR30, - COR30, -CO2R30, -CONR30R31, -N (R30) COR31, - N (R30) CONR31R32, -N (R30) SO2R31, -NR30R31, -SO2R30, -SO2NR30R31, -SO2N = CHNR30R31 and -OCONR30R31 (where R30, R31, and R32 can be the same or different, each representing an atom of hydrogen; C1-6 alkyl group which can be substituted with one or

ARP060100263A 2005-01-28 2006-01-24 COMPOSITION CONTAINING DERIVATIVES OF CYANOPIRROLIDINE FOR SOLID PHARMACEUTICAL PREPARATIONS, SOLID PHARMACEUTICAL PREPARATION CONTAINING COMPOSITION, AND PROCESS TO PRODUCE SOLID PHARMACEUTICAL PREPARATION AR052197A1 (en)

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Family Cites Families (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4743450A (en) * 1987-02-24 1988-05-10 Warner-Lambert Company Stabilized compositions
CO5150173A1 (en) * 1998-12-10 2002-04-29 Novartis Ag COMPOUNDS N- (REPLACED GLYCLE) -2-DIPEPTIDYL-IV PEPTIDASE INHIBITING CYANOPIRROLIDINS (DPP-IV) WHICH ARE EFFECTIVE IN THE TREATMENT OF CONDITIONS MEDIATED BY DPP-IV INHIBITION
US6395767B2 (en) * 2000-03-10 2002-05-28 Bristol-Myers Squibb Company Cyclopropyl-fused pyrrolidine-based inhibitors of dipeptidyl peptidase IV and method
TW583185B (en) * 2000-06-13 2004-04-11 Novartis Ag N-(substituted glycyl)-2-cyanopyrrolidines and pharmaceutical composition for inhibiting dipeptidyl peptidase-IV (DPP-IV) or for the prevention or treatment of diseases or conditions associated with elevated levels of DPP-IV comprising the same
TWI243162B (en) * 2000-11-10 2005-11-11 Taisho Pharmaceutical Co Ltd Cyanopyrrolidine derivatives
GB0115517D0 (en) * 2001-06-25 2001-08-15 Ferring Bv Novel antidiabetic agents
AU2002360732A1 (en) * 2001-12-26 2003-07-24 Guilford Pharmaceuticals Change inhibitors of dipeptidyl peptidase iv
HUP0200849A2 (en) * 2002-03-06 2004-08-30 Sanofi-Synthelabo N-aminoacetyl-pyrrolidine-2-carbonitrile derivatives, pharmaceutical compositions containing them and process for producing them
TW200401635A (en) * 2002-07-23 2004-02-01 Yamanouchi Pharma Co Ltd 2-Cyano-4-fluoropyrrolidine derivative or salt thereof
US7304166B2 (en) * 2002-08-29 2007-12-04 Taisho Pharmaceutical Co., Ltd. Benzenesulfonate salt of 4-fluoro-2-cyanopyrrolidine derivatives
HU227684B1 (en) * 2003-08-29 2011-11-28 Sanofi Aventis Adamantane and azabicyclo-octane and nonane derivatives and their use as dpp-iv inhibitors
ES2684325T5 (en) * 2004-01-20 2024-06-10 Novartis Ag Formulation and direct compression process

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WO2006080412A3 (en) 2006-09-21
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WO2006080412A2 (en) 2006-08-03
DOP2006000019A (en) 2006-07-15

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