Takeda Pharmaceutical Company Limited

Takeda Chemical Industries, Inc.

Kazuyoshi Aso

Michiyo Mochizuki

Albert Charles Gyorkos

Christopher Peter Corrette

Suk Young Cho

Katsumi Kobayashi

Satoshi Sasaki

Hiroshi Akimoto

Nobuhiro Suzuki

Takuto Kojima

Masakuni Kori

Takafumi Takai

Shiro Takekawa

Koichiro Ootsu

Scott Alan Pratt

Christopher Stephen Siedem

Kazuyuki Tokumaru

Timothy Mark Turner

Steven Armen Boyd

Masaki Seto

Kevin Ronald Condroski

Naoyuki Kanzaki

Yasutaka Hoashi

Masato Yoshida

Norihito Tokunaga

Hiroyuki Watanabe

Yuji Ishihara

Tetsuo Miwa

Jun Terauchi

Naoki Tarui

Satoshi Endo

Yoshihiro Banno

Nobuo Cho

Satoru Oi

Takatoshi Yogo

Yusuke Ohba

Hiroyuki Nagamiya

Michiyo Gyoten

Takashi Santo

Provided is a compound or a salt thereof, which has an excellent JAK inhibitory action, and is useful as a prophylactic or therapeutic agent for autoimmune diseases (rheumatoid arthritis, psoriasis, inflammatory bowel disease, Sjogren's syndrome, Behcet's syndrome, multiple sclerosis, systemic lupus erythematosus, etc.), cancer (leukemia, uterine leiomyosarcoma, prostate cancer, multiple myeloma, cachexia, myelofibrosis, etc.) and the like. The present invention relates to a compound represented by the formula (I) wherein each symbol is as defined in the present specification, or a salt thereof.

Heterocyclic compound

There is provided a compound of the formula (I'): wherein X is a nitrogen or CRx, Rx is a hydrogen, etc., Ris an optionally substituted hydrocarbon group, etc., Ris an optionally substituted hydrocarbon group, etc., ring A is 5- to -8-membered heterocyclic ring, etc., and each of Y, Yand Yis an optionally substituted carbon or a nitrogen, etc.; or 'a salt thereof or a prodrug thereof, which have CRF receptor antagonistic activity and use thereof. 

Tricyclic compounds having corticotropin-releasing factor antagonistic activity and pharmaceutical compositions containing them

There is provided a compound of the formula (I'): wherein x is a nitrogen or CRx, Rx is a hydrogen, etc., Ris an optionally substituted hydrocarbon group, etc., Ris an optionally substituted hydrocarbon group, etc., ring A is 5- to 8-membered heterocyclic ring, etc., and each of Y, Yand Yis an optionally substituted carbon or a nitrogen, etc.; or a salt thereof or a prodrug thereof, which have CRF receptor antagonistic activity and use thereof.

Tricyclic compounds and use thereof

There is provided a CRF receptor antagonist comprising a compound of the formula (I): wherein Ris an optionally substituted hydrocarbyl, an optionally substituted C-linked heterocyclic group, an optionally substituted N-linked heteroaryl group, a cyano or an acyl; Ris an optionally substituted cyclic hydrocarbyl or an optionally substituted heterocyclic group; X is oxygen, sulfur or &#x2014;NR&#x2014; (wherein Ris a hydrogen, an optionally substituted hydrocarbyl or an acyl); Y, Yand Yare each an optionally substituted carbon or a nitrogen, provided that one or less of Y, Yand Yis nitrogen; and Z is a bond, &#x2014;CO&#x2014;, oxygen, sulfur, &#x2014;SO&#x2014;, &#x2014;SO&#x2014;, &#x2014;NR&#x2014;, &#x2014;NR-alk-, &#x2014;CONR&#x2014; or &#x2014;NRCO&#x2014; (wherein alk is an optionally substituted Calkylene and Ris a hydrogen, an optionally substituted hydrocarbyl or an acyl); or a salt thereof or a prodrug thereof.

Fused heterocyclic compounds

There is provided a compound of the formula: wherein Ris an optionally substituted hydrocarbyl, a substituted amino, etc.; Ris an aromatic group substituted with one or two substituents at the positions adjacent to the position bonded to Z, and said aromatic group may have additional substituent(s); X is &#x2014;NR&#x2014; wherein Ris a hydrogen, an optionally substituted hydrocarbyl or an acyl, or sulfur; Y, Yand Yare an optionally substituted methine or a nitrogen, etc.; and Z is an optionally substituted methylene, provided that carbonyl is excluded; or a salt thereof or a prodrug thereof, which have CRF receptor antagonist activity and use thereof.

There is provided a CRF receptor antagonist comprising a compound of the formula (I):A-W&#x2014;Ar&#x2003;&#x2003;(I) 

Cyclic compounds

There is provided a CRF receptor antagonist comprising a compound of the formula (I): wherein, ring A is a 5-membered ring represented by the formula (A'): wherein X is a carbon and Xis an oxygen, a sulfur or &#x2014;NR&#x2014;, or formula (A&#x2033;): wherein X is a nitrogen and Ris an optionally substituted hydrocarbyl, Ris an amino substituted by two optionally substituted hydrocarbyl groups, Ris an phenyl, Yis CRor a nitrogen, Yis CRor a nitrogen and Yis CRor a nitrogen, provided that one or less of Y, Y, and Yis nitrogen, W is a bond, &#x2014;(CH)n-, and Z is a bond, &#x2014;NR&#x2014;, etc.; or a salt thereof or a prodrug thereof.

Nitrogen-containing fused heterocyclic compounds

The present invention provides a compound having melanocortin receptor agonist activity or antagonist activity, which is a novel biaryl compound represented by the formula (I): 

Biaryl compound and use thereof

A melanin-concentrating hormone antagonist comprising a compound of the formula: wherein R is hydrogen atom or a cyclic group which may be substituted; X is a bond or a spacer having a main chain of 1 to 10 atoms; Y is a spacer having a main chain of 1 to 6 atoms; ring A is benzene ring which may be further substituted; ring B is a 5- to 9-membered nitrogen-containing non-aromatic heterocyclic ring which may be further substituted; Rand Rare the same or different and are hydrogen atom, a hydrocarbon group which may be substituted or a heterocyclic group which may be substituted; or Rand R, together with the adjacent nitrogen atom, may form a nitrogen-containing heterocyclic ring which may be substituted; or R, together with the adjacent nitrogen atom and Y, may form a nitrogen-containing heterocyclic ring which may be substituted; or a salt thereof is useful as a preventive or therapeutic agent for obesity, etc.

Melanin-concentrating hormone antagonist

Compounds of a formula: wherein Ring A represents an optionally-substituted aromatic ring; Ring B represents an optionally-substituted cyclic hydrocarbon group; Z represents an optionally-substituted cyclic group; Rrepresents a hydrogen atom, an optionally-substituted hydrocarbon group, an optionally-substituted heterocyclic group, or an acyl group; Rrepresents an optionally-substituted amino group; D represents a chemical bond or a divalent group; E represents &#x2014;CO&#x2014;, &#x2014;CON(R)&#x2014;, COO&#x2014;, N(R)CON(R)&#x2014;, &#x2014;N(R)COO&#x2014;, &#x2014;N(R)SO&#x2014;, N(R)&#x2014;, &#x2014;O&#x2014;, &#x2014;S&#x2014;, &#x2014;SO&#x2014; or &#x2014;SO&#x2014; (in which Rand Reach independently represent a hydrogen atom or an optionally-substituted hydrocarbon group); G represents a chemical bond or a divalent group; L represents (1) a chemical bond or (2) a divalent hydrocarbon group optionally having from 1 to 5 substituents selected from;

Aromatic amine derivatives, their production and use

A novel biphenyl compound having GPR 14 antagonistic activity. It is a compound represented by the formula (I): wherein Rrepresents hydrogen, etc.; X represents 1 to 12 spacers; A represents amino, etc., Rand Reach represents a hydrocarbon group, etc.; and rings B and C each represents an optionally further substituted benzene ring, or a salt thereof.

Biphenyl compound

A novel compound of the formula: ##STR1## wherein a ring A stands for an optionally substituted 5-membered ring; B stands for an optionally substituted divalent cyclic or chain group; either one of Q.sup.1 and Q.sup.2 stands for N and the other stands for N or CH; X stands for an amino group, hydroxyl group or mercapto group; Y stands for H, halogen atom or a group bonded through C, N, 0 or S; Z stands for a straight-chain divalent group having 2 to 5 atoms constituted of optionally substituted carbon atoms or constituted of optionally substituted carbon atoms and one optionally substituted hetero-atom; COOR.sup.1 and COOR.sup.2 independently stand for an optionally esterified carboxyl group; n denotes an integer of 2 to 6; and R.sup.1 may be different in each of n repeating units, or their salts and it is useful as a therapeutic drug for tumor in mammals.

Condensed heterocyclic compounds, their production and use

A novel compound of the formula: ##STR1## wherein a ring A stands for an optionally substituted 5-membered ring; B stands for an optionally substituted divalent cyclic or chain group; either one of Q.sup.1 and Q.sup.2 stands for N and the other stands for N or CH; X stands for an amino group, hydroxyl group or mercapto group; Y stands for H, halogen atom or a group bonded through C, N, O or S; Z stands for a straight-chain divalent group having 2 to 5 atoms constituted of optionally substituted carbon atoms or constituted of optionally substituted carbon atoms and one optionally substituted hetero-atom; COOR.sup.1 and COOR.sup.2 independently stand for an optionally esterified carboxyl group; n denotes an integer of 2 to 6; and R.sup.1 may be different in each of n repeating units, or their salts and it is useful as a therapeutic drug for tumor in mammals.

Growing community of inventors

Osaka, Japan

Kazuyoshi Aso