Takeda Chemical Industries, Inc.

Takeda Pharmaceutical Company Limited

Satoru Oi

Yoshihiro Banno

Chitoshi Hatanaka

Koji Ikedou

Takashi Sohda

Hiroyuki Tawada

Nobuhiro Suzuki

Yukio Fujisawa

Masaki Ogino

Hironobu Maezaki

Kazuyoshi Aso

Hidefumi Yukimasa

Junji Mizoguchi

Masafumi Nakao

Hideaki Nagaya

Nobuhiro Inatomi

Taihei Yamane

Sigel Nuwa

Koji Takeuchi

A compound represented by the formula wherein ring A is an optionally substituted 5- to 10-membered aromatic ring; Rand Rare the same or different and each is an optionally substituted hydrocarbon group or an optionally substituted heterocyclic group; X and Y are the same or different and each is a bound, &#x2014;O&#x2014;, &#x2014;S&#x2014;, &#x2014;SO&#x2014;, &#x2014;SO?2#191- or &#x2014;NR&#x2014; (Ris a hydrogen atom or an optionally substituted hydrocarbon group); and L is a divalent hydrocarbon group, or a salt thereof shows a superior peptidase-inhibitory activity and is useful as a prophylactic or therapeutic agent of diabetes and the like. 

Fused heterocyclic compounds as peptidase inhibitors

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

The present invention provides a compound of the formula: wherein ring A is an optionally substituted 5 to 10-membered aromatic ring; Rand Rare the same or different and each is an optionally substituted hydrocarbon group or an optionally substituted heterocyclic group; X is a bond and the like; and L is a divalent hydrocarbon group, and a salt thereof, except 3-(aminomethyl)-2,6,7-trimethyl-4-phenyl-1(2H)-isoquinolinone, 3-(aminomethyl)-2-methyl-4-phenyl-1(2H)-isoquinolinone, 3-(aminomethyl)-6-chloro-2-methyl-4-phenyl-1(2H)-isoquinolinone and 3-(aminomethyl)-2-isopropyl-4-phenyl-1(2H)-isoquinolinone. The compound shows a superior peptidase-inhibitory activity and is useful as an agent for the prophylaxis or treatment of diabetes and the like.

Fused heterocyclic compounds

Phosphorylamides, their preparation and use

The present invention provides novel compound of the formulas (Ia) or (I): ##STR1## wherein Q is one or two amino acid residues which may be substituted; R.sup.3 is a carboxyl group which may be esterified or an acyl group; A is an alkylene group; B is hydrogen or an alkyl group which may be substituted or an acyl group; or a salt thereof; ##STR2## wherein R.sup.1 and R.sup.2 may be the same or different and each is hydrogen or a hydrocarbon residue which may be substituted; R.sup.3, A and B have the same definitions as those shown above; m and n each is 0 or 1; provided that where both m and n are both equal to 0, R.sup.3 is a carboxyl group which may be esterified or an acyl group having not less than 7 carbon atoms; or a salt thereof. The compound (Ia) or (I) shows cathepsin L inhibitory and bone resorption inhibitory activities and are useful as a prophylactic/therapeutic agent for osteoporosis.

Lactol derivatives, their production and use

There is disclosed an improved process for substitution of the hydroxy group at 2-position of an ascorbic acid derivative according to the following reaction scheme: ##STR1## wherein R.sup.0 is hydrogen, alkyl having 1 to 6 carbon atoms, phenyl or a group of the formula ##STR2## (wherein X is two hydrogen atoms, or acetal or ketal residue); R.sup.1 is an alkyl or alkenyl group having up to 22 carbon atoms which may be substituted with phenyl or alkoxy having 1 to 22 carbon atoms; Y is halogen or optionally substituted sulfonyloxy; R is hydrogen, or primary, secondary or tertiary alkyl having 1 to 10 carbon atoms; and Z is an alkali metal or an alkali earth metal. There is also disclosed hydrolysis of the following scheme: ##STR3## wherein R.sup.1 is as defined above; and X is acetal or ketal residue.

Selective etherification

An improved process for producing a substituted vinyl pyridine compound of the general formula: ##STR1## wherein R.sup.1 is pyridyl group; R.sup.2 is an optionally substituted aromatic or heterocyclic group; R.sup.3 is a lower alkyl group, hydroxymethyl group, nitroxymethyl group, a nitrogen containing 5 membered ring-methyl group, an acetal-methyl group, a trialkylsilyloxymethyl group, an alkyl- or aryl-sulfonyloxymethyl group, an alkyl- or aryl-sulfonylaminocarbonyloxymethyl group, an acyloxymethyl group, an alkoxycarbonyloxymethyl group, a halogenomethyl group, an alkoxymethyl group, an aryl-oxymethyl group, cyano group, an optionally substituted carbamoyl group, an optionally substituted carbamoyloxymethyl group, an optionally substituted thiocarbamoyloxymethyl group, carboxyl group or an alkoxycarbonyl group; and n is an integer of 1 to 22, which comprises reacting a compound of the general formula: ##STR2## wherein R.sup.1 and R.sup.2 are as defined above, with a compound of the general formula:

Process for producing substituted vinyl pyridine derivatives

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Nara, Japan

Satoru Oi