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1. CN111574422 - Phenyl difluoromethyl substituted prolinamide compound

Office
China
Application Number 202010529596.X
Application Date 23.01.2018
Publication Number 111574422
Publication Date 25.08.2020
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
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 nitrogen atoms as the only ring hetero atoms, e.g. piperazine
496Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene
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 37/08
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
37Drugs for immunological or allergic disorders
08Antiallergic agents
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
CPC
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
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 37/08
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
37Drugs for immunological or allergic disorders
08Antiallergic agents
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 13/12
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
13Drugs for disorders of the urinary system
12of the kidneys
C07D 401/10
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
401Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
02containing two hetero rings
10linked by a carbon chain containing aromatic rings
Applicants ASTELLAS PHARMA INC
安斯泰来制药株式会社
Inventors NAKAJIMA YUTAKA
中岛丰
IMADA SUNAO
今田直
YAMAMOTO ERIKO
山本永利子
TSUCHIYA KAZUYUKI
土屋和之
HARAYAMA YU
原山悠
MATSUMOTO SHUNICHIRO
松本俊一郎
Agents 北京天昊联合知识产权代理有限公司 11112
北京天昊联合知识产权代理有限公司 11112
Priority Data 2017-010321 24.01.2017 JP
Title
(EN) Phenyl difluoromethyl substituted prolinamide compound
(ZH) 苯基二氟甲基取代脯氨酰胺化合物
Abstract
(EN) Provided is a compound useful as a cathepsin S inhibitor. The present inventors have studied a compound having a cathepsin S inhibitory activity and useful as an active ingredient of a pharmaceuticalcomposition for the prevention and/or treatment of autoimmune diseases including systemic lupus erythematosus (SLE) and lupus nephritis, allergy, or graft rejection of organs, bone marrow, or tissue.It is confirmed that the phenyl difluoromethyl-substituted prolinamide compound according to the present invention has a cathepsin S inhibitory effect. The phenyl difluoromethyl-substituted prolinamide compound according to the present invention has a cathepsin S inhibitory activity, and can be used as a prophylactic and/or therapeutic agent for autoimmune diseases including SLE and nephritis, allergies, or graft rejection of organs, bone marrow, or tissues.
(ZH) 提供了一种用作组织蛋白酶S抑制剂的化合物。本发明人研究了具有组织蛋白酶S抑制作用且可作为用于预防和/或治疗包括系统性红斑狼疮(SLE)和狼疮性肾炎的自身免疫性疾病、过敏症、或者器官、骨髓或组织的移植物排斥的医药组合物的有效成分的化合物,确认本发明的苯基二氟甲基取代脯氨酰胺化合物具有组织蛋白酶S抑制作用,从而完成了本发明。本发明的苯基二氟甲基取代脯氨酰胺化合物具有组织蛋白酶S抑制作用,可以用作包括SLE和肾炎的自身免疫性疾病、过敏症、或者器官、骨髓或组织的移植物排斥的预防和/或治疗剂。