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1. MYPI 2019004186 - PHENYLDIFLUOROMETHYL-SUBSTITUTED PROLINEAMIDE COMPOUND

Office
Malaysia
Application Number PI 2019004186
Application Date 23.01.2018
Publication Number PI 2019004186
Publication Date 24.07.2018
Publication Kind A
IPC
C07D 403/10
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
403Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/167
02containing two hetero rings
10linked by a carbon chain containing aromatic rings
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
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
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
Applicants Astellas Pharma Inc.
Inventors MATSUMOTO, Shunichiro
HARAYAMA, Yu
TSUCHIYA, Kazuyuki
YAMAMOTO, Eriko
IMADA, Sunao
NAKAJIMA, Yutaka
Agents ZARAIHAN BT SHAARI
Priority Data 2017-010321 24.01.2017 JP
Title
(EN) PHENYLDIFLUOROMETHYL-SUBSTITUTED PROLINEAMIDE COMPOUND
Abstract
(EN) [PROBLEM] TO PROVIDE A COMPOUND USEFUL AS A CATHEPSIN S INHIBITOR. [MEANS FOR SOLUTION] THE PRESENT INVENTORS HAVE EXAMINED A COMPOUND THAT HAS A CATHEPSIN S INHIBITORY EFFECT AND IS USABLE AS AN ACTIVE INGREDIENT OF A PHARMACEUTICAL COMPOSITION FOR PREVENTING AND/OR TREATING AUTOIMMUNE DISEASE INCLUDING SYSTEMIC LUPUS ERYTHEMATOSUS (SLE) AND LUPUS NEPHRITIS. ALLERGIES, OR GRAFT REJECTION OF AN ORGAN, BONE MARROW OR TISSUE, AND HAVE FOUND THAT A PHENYLDIFLUOROMETHYL-SUBSTITUTED PROLINAMIDE COMPOUND OF THE PRESENT INVENTION HAS THE CATHEPSIN S INHIBITORY EFFECT, THEREBY COMPLETING THE PRESENT INVENTION. THE PHENYLDIFLUOROMETHYL-SUBSTITUTED PROLINAMIDE COMPOUND OF THE PRESENT INVENTION HAS THE CATHEPSIN S INHIBITORY EFFECT AND IS USEFUL AS AN AGENT FOR PREVENTING AND/OR TREATING AUTOIMMUNE DISEASE INCLUDING SLE AND NEPHRITIS, ALLERGIES, OR GRAFT REJECTION OF AN ORGAN. BONE MARROW OR TISSUE. [SELECTED FIGURE] NIL