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1. MX2019008756 - COMPUESTO DE PROLINAMIDA SUSTITUIDA POR FENILDIFLUROMETILO.

Office
Mexico
Application Number 2019008756
Application Date 23.07.2019
Publication Number 2019008756
Publication Date 11.09.2019
Publication Kind A
IPC
C07D 207/16
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
207Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
02with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
04having no double bonds between ring members or between ring members and non-ring members
10with 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
16Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
CPC
A61P 37/02
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
37Drugs for immunological or allergic disorders
02Immunomodulators
A61P 37/06
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
37Drugs for immunological or allergic disorders
02Immunomodulators
06Immunosuppressants, e.g. drugs for graft rejection
A61P 37/08
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
37Drugs for immunological or allergic disorders
08Antiallergic agents
C07D 207/16
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
207Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
02with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
04having no double bonds between ring members or between ring members and non-ring members
10with hetero atoms or with carbon atoms having three bonds to hetero atoms, with at the most one to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
16Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
A61K 31/4439
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
435having six-membered rings with one nitrogen as the only ring hetero atom
44Non condensed pyridines; Hydrogenated derivatives thereof
4427containing further heterocyclic ring systems
4439containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
A61K 31/496
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
495having six-membered rings with two ; or more; nitrogen atoms as the only ring heteroatoms, e.g. piperazine ; or tetrazines
496Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene
Applicants ASTELLAS PHARMA INC.
Inventors Yutaka NAKAJIMA
Yu Harayama
Sunao IMADA
Kazuyuki TSUCHIYA
Eriko YAMAMOTO
Shunichiro MATSUMOTO
Priority Data 2017-010321 24.01.2017 JP
Title
(EN) COMPUESTO DE PROLINAMIDA SUSTITUIDA POR FENILDIFLUROMETILO.
(ES) COMPUESTO DE PROLINAMIDA SUSTITUIDA POR FENILDIFLUROMETILO.
Abstract
(EN) [Problem] To provide a compound useful as a cathepsin S inhibitor. [Solution] The present inventors have studied on a compound which has a cathepsin S-inhibiting activity and can be used as an active ingredient for a pharmaceutical composition for preventing and/or treating an autoimmune disease such as systemic lupus erythematosus (SLE) and lupus nephritis, an allergy, or organ, bone marrow or tissue graft rejection. As a result, it has been confirmed that a phenyldifluoromethyl-substituted prolineamide compound according to the present invention has a cathepsin S-inhibiting activity. This confirmation leads to the accomplishment of the present invention. The phenyldifluoromethyl-substituted prolineamide compound according to the present invention has a cathepsin S-inhibiting activity, and can be used as a prophylactic and/or therapeutic agent for an autoimmune disease such as SLE and nephritis, an allergy, or organ, bone marrow or tissue graft rejection.
(ES) Problema Proporcionar un compuesto útil como inhibidor de la catepsina S. Medios para la solución Los presentes inventores han examinado un compuesto que tiene un efecto inhibidor de la catepsina S y puede utilizarse como un principio activo de una composición farmacéutica para prevenir y/o tratar enfermedades autoinmunes que incluyen lupus eritematoso sistémico (SLE) y nefritis lúpica, alergias, o rechazo de injertos de un órgano, médula ósea o tejido, y han hallado que un compuesto de prolinamida sustituida por fenildifluorometilo de la presente invención tiene el efecto inhibidor de la catepsina S, y de ese modo completa la presente invención. El compuesto de prolinamida sustituida por fenildifluorometilo de la presente invención tiene el efecto inhibidor de la catepsina S, y es útil como un agente para prevenir y/o tratar enfermedades autoinmunes que incluyen SLE y nefritis, alergias, o rechazo de injertos de un órgano, médula ósea o tejido.
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