NITROGEN-CONTAINING SPIROCYCLIC COMPOUND AND ITS APPLICATION IN MEDICINE Russian patent published in 2017 - IPC C07D487/04 A61K31/519 A61P35/00 A61P37/06 A61P37/02 A61P37/08 A61P17/06 A61P19/02 A61P27/04 A61P27/16 A61P27/00 A61P27/14 

Abstract RU 2630694 C2

FIELD: pharmacology.

SUBSTANCE: compounds can be used to prepare a medicament for treatment or prevention of a disease selected from the group consisting of organ transplant rejection, graft versus host transplantation, autoimmune disease, allergic diseases and chronic myeloproliferative disease. The disease can be selected from rheumatoid arthritis, psoriasis, atopic dermatitis or a disease caused by dry eyes. In the general formula

Ra is the same or different and each represents (1) C1-6 alkyl or (2) a halogen atom, n1 is an integer selected from the integers from 0 to 2, Rb are the same or different and each represents (1) C1-6 alkyl or (2) halogen atom, n2 is an integer selected from the integers from 0 to 2, m1 is an integer selected from the integers from 0 to 3, m2 is an integer selected from the integers from 1 to 4, Xa=Xb is (1) CH=CH, (2) N=CH or (3) CH=N, X is (1) a nitrogen atom or (2) C-Rd, where Rd is a hydrogen atom or halogen atom, Rc is a group selected from the following groups (1)-(6): (1) a hydrogen atom, (2) C1-6 alkyl, optionally substituted with 1-5 same or different substituents selected from the following group A, (3) -C(=O)-Rc1, (4) -C(=O)-O-Rc2, (5) -C(=O)-NRc3Rc4, where Rc1, Rc2, Rc3, Rc4 are the same or different and each represents (i) a hydrogen atom or (ii) C1-6 alkyl, optionally substituted with 1-5 same or different substituents selected from the following group A, or (6) a group of the following formula

in which Ya is a group selected from the following groups (i) to(iii) (i) C1-6 alkylene, (ii) -C(=O)- or (iii) -S(=O)-O-, ring T is (i) a phenyl, (ii) C3-10 cycloalkyl or (iii) a saturated monoheterocyclyl, which contains 1 nitrogen atom and carbon atoms, and the number of atoms, constituting the ring, is 3-7, Rc5 is the same or different and each represents (i) cyano, or (ii) a nitro group, p is an integer selected from the integers from 0 to 1, group A is a group, consisting of (a) a hydroxyl, (b) C1-6 alkoxy, (c) a cyano, (d) C1-6 alkoxycarbonyl, (e) C1-6 alkylcarboxylic and (f) C2-6 alkenylacyl.

EFFECT: increased efficiency of treatment.

60 cl, 33 tbl, 8 ex

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RU 2 630 694 C2

Authors

Nodzi Satoru

Siodzaki Makoto

Miura Tomoya

Khara Esinori

Yamanaka Khirosi

Maeda Katsuya

Khori Akimi

Inoe Masafumi

Khase Yasunori

Dates

2017-09-12Published

2010-07-30Filed