Takeda Pharmaceutical Company Limited

Takeda Chemical Industries, Inc.

Jun Terauchi

Kaneyoshi Kato

Mitsuru Kakihana

Hiroaki Fukumoto

Nobuhiro Suzuki

Hiroshi Nara

Kenjiro Sato

Shiro Takekawa

Hideyuki Oki

Yuji Ishihara

Masaaki Mori

Kazuyoshi Aso

Satoshi Endo

Yukio Shimomura

Akira Kaieda

Yasuo Nagai

Nobuhiro Inatomi

Fumihiko Sato

Haruhiko Kuno

The present invention provides a novel amide derivative having a matrix metalloproteinase inhibitory activity, and useful as a pharmaceutical agent, which is a compound represented by the formula (I) wherein ring A is an optionally substituted, nitrogen containing heterocycle, ring B is an optionally substituted monocyclic homocycle or an optionally substituted monocyclic heterocycle, Z is N or NR(Ris a hydrogen atom or an optionally substituted hydrocarbon group), is a single bond or a double bond, Ris a hydrogen atom or an optionally substituted hydrocarbon group, X is an optionally substituted spacer having 1 to 6 atoms, ring C is (1) an optionally substituted homocycle or (2) an optionally substituted heterocycle other than a ring represented by (II) (X' is S, O, SO, or CH), and at least one of ring B and ring C has substituent(s), provided that N-{(1S,2R)-1-(3,5-difluorobenzyl)-3-[(3-ethylbenzyl)amino]2 hydroxypropyl} 5,6 dimethyl 4 oxo 1,4 dihydrothieno[2,3-d]pyrimidine-2-carboxamide is excluded, or a salt thereof. 

Substituted 2- amidoquinazol-4-ones as matrix metalloproteinase-13 inhibitors

The present invention provides a novel amide derivative having a matrix metalloproteinase inhibitory activity, and useful as a pharmaceutical agent, which is a compound represented by the formula (I) wherein ring A is an optionally substituted, nitrogen-containing heterocycle, ring B is an optionally substituted monocyclic homocycle or an optionally substituted monocyclic heterocycle, Z is N or NR(Ris a hydrogen atom or an optionally substituted hydrocarbon group),is a single bond or a double bond, Ris a hydrogen atom or an optionally substituted hydrocarbon group, X is an optionally substituted spacer having 1 to 6 atoms, ring C is (1) an optionally substituted homocycle or (2) an optionally substituted heterocycle other than a ring represented by (II) (X' is S, O, SO, or CH), and at least one of ring B and ring C has substituent(s), provided that N-{(1S,2R)-1-(3,5-difluorobenzyl)-3-[(3-ethylbenzyl)amino]-2-hydroxypropyl}-5,6-dimethyl-4-oxo-1,4-dihadrothieno[2,3-d]pyrimidine-2-carboxamide is excluded, or a salt thereof. 

Substituted 2-amidoquinazol-4-ones as matrix metalloproteinase-13 inhibitors

The present invention provides a therapeutic agent and methods thereof for the treatment for irritable bowel syndrome. The agent comprises a compound represented by formula (I): wherein, Rrepresents an optionally substituted hydrocarbon group, etc., Rrepresents a hydrogen atom or an optionally substituted hydrocarbon group, Rrepresents a hydrogen atom, an optionally substituted hydrocarbon group, etc., X represents CHR, NR, CO, O or S (wherein, Rrepresents a hydrogen atom, an optionally substituted hydrocarbon group, etc.), Y represents C, CH or N, represents a single bond or double bond, ring A represents an optionally substituted 5- to 7-membered oxygen-containing heterocyclic ring, ring B represents an optionally substituted benzene ring, and m represents an integer of 1 to 4, or a salt thereof, wherein the compound represented by formula (I) or a salt thereof is (S)&#x2014;N-[2-(1,6,7,8-tetrahydro-2H-indeno[5,4-b]furan-8-yl)ethyl]propionamide.

Therapeutic agent for irritable bowel syndrome and methods thereof

The present invention provides a novel amide compound represented by the following formula, which has a matrix metalloproteinase inhibitory activity and is useful as a pharmaceutical agent. wherein each symbol is as defined in the specification.

Heterocyclic amide compound and use thereof

A compound of the formula: wherein Ar is an aromatic ring assembly group which may be substituted or a fused aromatic group which may be substituted; X is (i) a bond, (ii) &#x2014;S&#x2014;, &#x2014;SO&#x2014; or &#x2014;SO&#x2014;, (iii) Calkylene, Calkenylene or Calkynylene, etc., (iv) &#x2014;CO&#x2014;O&#x2014; or (v) &#x2014;(CH)p-X&#x2014;, &#x2014;(CH)p-X&#x2014;CH)q-, &#x2014;(CH)r-CO&#x2014;X&#x2014;, &#x2014;SO&#x2014;NR&#x2014; or &#x2014;(CH)r-SO&#x2014;NR&#x2014; wherein Xis O or NR, Ris H, a hydrocarbon group which may be substituted or an acyl, p is 0 to 5, q is 1 to 5, p+q is 1 to 5, and r is 1 to 4; Y is a divalent Caliphatic hydrocarbon group optionally containing O or S, which may be substituted; Rand Reach is H or a lower alkyl which may be substituted, or Rand Rform a N-containing heterocyclic ring which may be substituted; Ring A is a benzene ring which may be further substituted; and Ring B is a 4- to 8-membered ring which may be further substituted, or a salt thereof has the effect of inhibiting amyloid-&#x3b2; protein production and/or secretion and is useful as a pharmaceutical composition for preventing and/or treating the neurodegenerative disease, etc.

Amine compounds, their production and use

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

A melanin-concentrating hormone antagonist which comprises a compound of the formula: wherein Aris a cyclic group which may have substituents;

Melanin concentrating hormone antagonist

&bgr;-amyloid protein production/secretion inhibitors

The present invention provides a compound of the formula:

Amine compounds, their production and use as amyloid-&bgr; production inhibitors

A spiro compound represented by the formula: ##STR1## wherein ring A represents an optionally substituted aromatic ring; T represents an optionally substituted hydrogen atom or an optionally substituted hydrocarbon group; X represents --CH.sub.2 --, --CO-- or --CH(OH)--; D represents --CH.sub.2 --, --O-- or --NR-- wherein R is a hydrogen atom or an optionally substituted hydrocarbon group and m, e and f independently represent an integer from 1 to 3, or a salt thereof. The spiro compound inhibits monoamine uptake, monoamine oxidase B and/or Ca ion uptake, and is a prophylactic and therapeutic drug for a central nervous diseases.

Growing community of inventors

Ikeda, Japan

Jun Terauchi