公开(公告)号：US5614544A

公开(公告)日：1997-03-25

申请号：US303209

申请日：1994-09-08

申请人： Takashi Sohda ,  Hitoshi Ikeda ,  Yu Momose

发明人： Takashi Sohda ,  Hitoshi Ikeda ,  Yu Momose

IPC分类号： C07D263/44 ,  C07D413/14 ,  C07D417/10 ,  A61K31/42

CPC分类号： C07D263/44 ,  C07D413/14 ,  C07D417/10

摘要： [Object]To provide a new 2,4-oxazolidinedione derivative possessing excellent hypoglycemic and hypolipidemic activities.[Constituent]A 2,4-oxazolidinedione derivative represented by the general formula: ##STR1## wherein X represents --CH.sub.2 --, --C(.dbd.O)--, --CH(OH)--, --C(.dbd.NOH)-- or --CH.dbd.CH--; R represents a hydrocarbon residue or heterocyclic group which may be substituted; n represents an integer from 0 to 5, and m represents an integer from 1 to 3; ....... represents a single or double bond; provided that n is an integer from 1 to 5 when X is --C(.dbd.O)--, or a pharmacologically acceptable salt thereof.[Drawings selected]None

摘要翻译： [目的]提供具有优异的降血糖和降血脂活性的新的2,4-恶唑烷二酮衍生物。 [组成成分]下列通式表示的2,4-恶唑烷二酮衍生物：其中X代表-CH2-，-C（= O） - ， - CH（OH） - ， - C（= NOH） CH = CH-; R表示可以被取代的烃残基或杂环基; n表示0〜5的整数，m表示1〜3的整数， + E，uns ....... + EE表示单键或双键; 条件是当X为-C（= O） - 时，n为1至5的整数，或其药理学上可接受的盐。 [已选图纸]无

公开(公告)号：US5371098A

公开(公告)日：1994-12-06

申请号：US929097

申请日：1992-08-13

申请人： Takashi Sohda ,  Iwao Yamazaki ,  Yu Momose

发明人： Takashi Sohda ,  Iwao Yamazaki ,  Yu Momose

IPC分类号： A61K31/42 ,  A61K31/421 ,  A61K31/422 ,  A61P3/00 ,  A61P3/02 ,  A61P19/08 ,  A61P19/10 ,  A61P43/00 ,  C07D263/32 ,  C07D263/34 ,  C07D413/12 ,  C07D417/12 ,  C07D263/30

CPC分类号： C07D263/32

摘要： An oxazole compound having the formula (I): ##STR1## in which A is a group of the formula --CH.sub.2 OR.sup.2 (wherein R.sup.2 is a hydrogen atom, an optionally substituted hydrocarbon residue, an optionally substituted heterocyclic group or an acyl group) or an aldehyde group, B is an optionally substituted phenyl group, R.sup.1 is a hydrogen atom or an optionally substituted alkyl group, and n is an integer of 0 to 6, provided that when n is 2, R.sup.1 is an optionally substituted alkyl group, or its salt, which is useful as a therapeutic agent for metabolic bone diseases including osteoporosis.

摘要翻译： 具有式（I）的恶唑化合物：其中A是式-CH 2 OR 2的基团（其中R 2是氢原子，任选取代的烃残基，任选取代的杂环基或酰基） ）或醛基，B为任选取代的苯基，R 1为氢原子或任选取代的烷基，n为0〜6的整数，条件是当n为2时，R 1为任选取代的烷基 或其盐，其可用作包括骨质疏松症在内的代谢性骨疾病的治疗剂。

公开(公告)号：US06399639B1

公开(公告)日：2002-06-04

申请号：US09519274

申请日：2000-03-07

申请人： Junji Matsui ,  Naoki Tarui ,  Yu Momose ,  Ken-ichi Naruo

发明人： Junji Matsui ,  Naoki Tarui ,  Yu Momose ,  Ken-ichi Naruo

IPC分类号： A61K31427

CPC分类号： A61K31/427 ,  A61K31/422 ,  A61K31/425 ,  A61K31/4439

摘要： An apoptosis inhibitor which comprises a compound of the formula: wherein R represents a hydrocarbon group that may be substituted or a heterocyclic group that may be substituted; Y represents a group of the formula: —CO—, —CH(OH)— or —NR3— where R3 represents an alkyl group that may be substituted; m is 0 or 1; n is 0, 1 or 2; X represents CH or N; A represents a chemical bond or a bivalent aliphatic hydrocarbon group having 1 to 7 carbon atoms; Q represents oxygen or sulfur; R1 represents hydrogen or an alkyl group; ring E may have further 1 to 4 substituents, which may form a ring in combination with R1; L and M respectively represent hydrogen or may be combined with each other to form a chemical bond; or a salt thereof, or a compound having an insulin sensitivity enhancing activity.

摘要翻译： 一种凋亡抑制剂，其包含下式化合物：其中R表示可被取代的烃基或可被取代的杂环基; Y表示式-CO-，-CH（OH） - 或-NR 3 - ，其中R 3表示可被取代的烷基; m为0或1; n为0,1或2; X表示CH或N; A表示化学键或碳原子数为1〜7的二价脂肪族烃基; Q表示氧或硫; R1表示氢或烷基; 环E可以具有另外1至4个取代基，其可以与R 1组合形成环; L和M分别表示氢或可以相互结合形成化学键; 或其盐，或具有胰岛素敏感性增强活性的化合物。

公开(公告)号：US06251926B1

公开(公告)日：2001-06-26

申请号：US09423854

申请日：1999-11-15

申请人： Yu Momose ,  Hiroyuki Odaka ,  Hiroshi Imoto ,  Hiroyuki Kimura ,  Junichi Sakamoto

发明人： Yu Momose ,  Hiroyuki Odaka ,  Hiroshi Imoto ,  Hiroyuki Kimura ,  Junichi Sakamoto

IPC分类号： A61K314245

CPC分类号： C07D213/74 ,  A61K31/42 ,  A61K31/421 ,  A61K31/4245 ,  A61K31/426 ,  A61K31/427 ,  A61K31/44 ,  A61K31/4439 ,  A61K31/47 ,  A61K31/4745 ,  A61K31/505 ,  C07D215/14 ,  C07D239/42 ,  C07D261/08 ,  C07D263/32 ,  C07D271/06 ,  C07D277/24 ,  C07D413/12 ,  C07D471/04

摘要： This invention provides a novel oxyiminoalkanoic acid derivative which has excellent hypoglycemic and hypolipidemic actions and which is used for the treatment of diabetes mellitus, hyperlipemia, insulin insensitivity, insulin resistance and impaired glucose tolerance.

摘要翻译： 本发明提供一种具有优异的降血糖和降血脂作用的新型氧亚氨基链烷酸衍生物，其用于治疗糖尿病，高脂血症，胰岛素不敏感，胰岛素抵抗和葡萄糖耐量异常。

公开(公告)号：US6110948A

公开(公告)日：2000-08-29

申请号：US155593

申请日：1998-09-30

申请人： Yu Momose ,  Etsuya Matsutani ,  Takashi Sohda

发明人： Yu Momose ,  Etsuya Matsutani ,  Takashi Sohda

IPC分类号： C07D277/20 ,  A61K31/42 ,  A61K31/421 ,  A61K31/422 ,  A61K31/425 ,  A61K31/426 ,  A61K31/427 ,  A61K31/44 ,  A61K31/4439 ,  A61P3/00 ,  A61P3/08 ,  A61P3/10 ,  A61P43/00 ,  C07D263/44 ,  C07D277/34 ,  C07D413/06 ,  C07D413/14 ,  C07D417/06 ,  C07D417/12 ,  C07D417/14 ,  A61K31/40

CPC分类号： A61K31/4439 ,  A61K31/422 ,  A61K31/427

摘要： A medicinal composition for the prophylaxis and treatment of cachexia which comprises a compound of the formula: ##STR1## wherein R represents a hydrocarbon group that may be substituted or a heterocyclic group that may be substituted; Y represents a group of the formula --CO--, --CH(OH)--, or --NR.sup.3 -- (R.sup.3 represents an alkyl group that may be substituted); m is 0 or 1; n is 0, 1 or 2; X represents CH or N; A represents a bond or a bivalent aliphatic hydrocarbon group having 1 to 7 carbon atoms; Q represents oxygen or sulfur; R.sup.1 represents hydrogen or an alkyl group; ring E may have further 1 to 4 substituents, which may form a ring in combination with R.sup.1 ; L and M respectively represent hydrogen or may be combined with each other to form a bond, provided that when m and n are 0, X represents CH, A represents a bond, Q represents sulfur, R.sup.1, L and M respectively represent hydrogen, and ring E does not have further substituents, R does not represent dihydrobenzopyranyl; or a salt thereof.

摘要翻译： PCT No.PCT / JP97 / 01148 Sec。 371日期：1998年9月30日 102（e）1998年9月30日PCT PCT 1997年4月3日提交PCT公布。 公开号WO97 / 37656 日期1997年10月16日用于预防和治疗恶病质的药物组合物，其包含下式化合物：其中R表示可被取代的烃基或可被取代的杂环基; Y表示式-CO-，-CH（OH） - 或-NR 3 - （R 3表示可被取代的烷基）的基团; m为0或1; n为0,1或2; X表示CH或N; A表示碳原子数1〜7的键或2价脂肪族烃基， Q表示氧或硫; R1表示氢或烷基; 环E可以具有另外1至4个取代基，其可以与R 1组合形成环; L和M分别表示氢或可以彼此结合形成键，条件是当m和n为0时，X表示CH，A表示键，Q表示硫，R 1，L和M表示氢， 环E不具有其它取代基，R不表示二氢苯并吡喃基; 或其盐。

公开(公告)号：US5239080A

公开(公告)日：1993-08-24

申请号：US723675

申请日：1991-06-27

申请人： Takashi Sohda ,  Hitoshi Ikeda ,  Yu Momose

发明人： Takashi Sohda ,  Hitoshi Ikeda ,  Yu Momose

IPC分类号： C07D263/32

CPC分类号： C07D263/32

摘要： Oxazole compounds having the formula: ##STR1## in which A is a group of the formula --CH.sub.2 OR.sup.3 (R.sup.3 is a hydrogen atom, an optionally substituted hydrocarbon residue, an optionally substituted heterocyclic group or an acyl group), or an aldehyde group and B is an optionally substituted phenyl group, or their salts, which are useful as antidiabetic agents.

摘要翻译： 具有下式的恶唑化合物：其中A是式-CH 2OR 3的基团（R 3是氢原子，任选取代的烃残基，任选取代的杂环基或酰基）或醛 基团，B是任选取代的苯基或其盐，其可用作抗糖尿病剂。

公开(公告)号：US20080269219A1

公开(公告)日：2008-10-30

申请号：US12080461

申请日：2008-04-03

申请人： Yu Momose ,  Katsuhito Murase

发明人： Yu Momose ,  Katsuhito Murase

IPC分类号： A61K31/5377 ,  A61K31/421 ,  A61K31/426 ,  A61K31/4525 ,  A61P25/00 ,  A61P1/00 ,  A61P29/00 ,  A61K31/496 ,  A61K31/443 ,  A61K31/506

CPC分类号： C07D263/34 ,  C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D263/38 ,  C07D263/46 ,  C07D263/48 ,  C07D277/32 ,  C07D277/40 ,  C07D277/54 ,  C07D413/04 ,  C07D413/12 ,  C07D417/04 ,  C07D417/14

摘要： A neurotrophin production/secretion promoting agent which comprises an azole derivative of the formula: wherein R1 represents a halogen atom, a heterocyclic group which may optionally be substituted, a hydroxy group which may optionally be substituted, a thiol group which may optionally be substituted, or an amino group which may optionally be substituted; A represents an acyl group which may optionally be substituted, a heterocyclic group which may optionally be substituted, a hydroxy group which may optionally be substituted, or a carboxyl group which may optionally be esterified or amidated; B represents an aromatic group which may optionally be substituted; X represents oxygen atom, sulfur atom, or nitrogen atom which may optionally be substituted; and Y represents a divalent hydrocarbon group or heterocyclic group, or a salt thereof; which is useful as an agent for preventing or treating neuropathy.

摘要翻译： 神经营养蛋白产生/分泌促进剂，其包含下式的唑衍生物：其中R 1表示卤素原子，可任选被取代的杂环基，可任选被取代的羟基， 可以任选被取代的硫醇基，或可任意被取代的氨基; A表示可任选被取代的酰基，可任选被取代的杂环基，可任意取代的羟基或可任意被酯化或酰胺化的羧基; B表示可任选被取代的芳族基团; X表示可任选被取代的氧原子，硫原子或氮原子; Y表示二价烃基或杂环基，或其盐; 其可用作预防或治疗神经病的药剂。

公开(公告)号：US06924300B2

公开(公告)日：2005-08-02

申请号：US10331056

申请日：2002-12-27

申请人： Yu Momose ,  Hiroyuki Odaka ,  Hiroshi Imoto ,  Hiroyuki Kimura ,  Junichi Sakamoto

发明人： Yu Momose ,  Hiroyuki Odaka ,  Hiroshi Imoto ,  Hiroyuki Kimura ,  Junichi Sakamoto

IPC分类号： A61K31/195 ,  A61K31/235 ,  A61K31/42 ,  A61K31/421 ,  A61K31/422 ,  A61K31/4245 ,  A61K31/426 ,  A61K31/427 ,  A61K31/437 ,  A61K31/44 ,  A61K31/4402 ,  A61K31/4439 ,  A61K31/47 ,  A61K31/4704 ,  A61K31/4745 ,  A61K31/496 ,  A61K31/505 ,  A61P3/06 ,  A61P3/10 ,  A61P9/10 ,  A61P29/00 ,  A61P43/00 ,  C07D213/74 ,  C07D215/14 ,  C07D239/42 ,  C07D261/08 ,  C07D263/32 ,  C07D271/06 ,  C07D277/24 ,  C07D413/04 ,  C07D413/12 ,  C07D471/04 ,  C07D263/30 ,  C07D277/20

CPC分类号： C07D213/74 ,  A61K31/42 ,  A61K31/421 ,  A61K31/4245 ,  A61K31/426 ,  A61K31/427 ,  A61K31/44 ,  A61K31/4439 ,  A61K31/47 ,  A61K31/4745 ,  A61K31/505 ,  C07D215/14 ,  C07D239/42 ,  C07D261/08 ,  C07D263/32 ,  C07D271/06 ,  C07D277/24 ,  C07D413/12 ,  C07D471/04

摘要： To provide a novel oxyiminoalkanoic acid derivative which has excellent hypoglycemic and hypolipidemic actions and which is used for the prevention or treatment of diabetes mellitus, hyperlipemia, insulin insensitivity, insulin resistance and impaired glucose tolerance.A compound represented by the formula: wherein R1 is an optionally substituted hydrocarbon group or an optionally substituted heterocyclic group; X is a bond, —CO—, —CH(OH)— or a group represented by —NR6— wherein R6 is a hydrogen atom or an optionally substituted alkyl group; n is an integer of 1 to 3; Y is an oxygen atom, a sulfur atom, —SO—, —SO2— or a group represented by —NR7— wherein R7 is a hydrogen atom or an optionally alkyl group; ring A is a benzene ring optionally having additional one to three substituents; p is an integer of 1 to 8; R2 is a hydrogen atom, an optionally substituted hydrocarbon group or an optionally substituted heterocyclic group; q is an integer of 0 to 6; m is 0 or 1; R3 is a hydroxy group, OR8 (R8 is an optionally substituted hydrocarbon group.) or NR9R10 (R9 and R10 are the same or different groups which are selected from a hydrogen atom, an optionally substituted hydrocarbon group, an optionally substituted heterocyclic group or an optionally substituted acyl group or R9 and R10 combine together to form a ring); R4 and R5 are the same or different groups which are selected from a hydrogen atom or an optionally substituted hydrocarbon group wherein R4 may form a ring with R2; provided that when R1 is a ethoxymethyl, a C1-3 alkyl, phenyl or p-methoxyphenyl and q=m=0, R3 is NR9R10; and provided that O-[2-chloro-4-(2-quinolylmethoxy)phenylmethyl]oxime and a methyl pyruvate of [2-chloro-4-(2-quinolylmethoxy)phenylmethyl]-2-iminoxypropionic acid are excluded; or a salt thereof.

公开(公告)号：US06605629B1

公开(公告)日：2003-08-12

申请号：US09868304

申请日：2001-06-29

申请人： Yu Momose ,  Katsuhito Murase

发明人： Yu Momose ,  Katsuhito Murase

IPC分类号： C07D41312

CPC分类号： C07D263/34 ,  C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D263/38 ,  C07D263/46 ,  C07D263/48 ,  C07D277/32 ,  C07D277/40 ,  C07D277/54 ,  C07D413/04 ,  C07D413/12 ,  C07D417/04 ,  C07D417/14

摘要： A neurotrophin production/secretion promoting agent which comprises an azole derivative of the formula: wherein R1 represents a halogen atom, a heterocyclic group which may optionally be substituted, a hydroxy group which may optionally be substituted, a thiol group which may optionally be substituted, or an amino group which may optionally be substituted; A represents an acyl group which may optionally be substituted, a heterocyclic group which may optionally be substituted, a hydroxy group which may optionally be substituted, or a carboxyl group which may optionally be esterified or amidated; B represents an aromatic group which may optionally be substituted; X represents oxygen atom, sulfur atom, or nitrogen atom which may optionally be substituted; and Y represents a divalent hydrocarbon group or heterocyclic group, or a salt thereof; which is useful as an agent for preventing or treating neuropathy.

摘要翻译： 一种神经营养因子产生/分泌促进剂，其包含下式的唑衍生物：其中R1表示卤素原子，可任意取代的杂环基，可任选被取代的羟基，可任选被取代的硫醇基， 或可任选被取代的氨基; A表示可任选被取代的酰基，可任选被取代的杂环基，可任意取代的羟基或可任意被酯化或酰胺化的羧基; B表示可任选被取代的芳族基团; X表示可任选被取代的氧原子，硫原子或氮原子; Y表示二价烃基或杂环基，或其盐; 其可用作预防或治疗神经病的药剂。

公开(公告)号：US06495581B1

公开(公告)日：2002-12-17

申请号：US09714699

申请日：2000-11-16

申请人： Yu Momose ,  Hiroyuki Odaka ,  Hiroshi Imoto ,  Hiroyuki Kimura ,  Junichi Sakamoto

发明人： Yu Momose ,  Hiroyuki Odaka ,  Hiroshi Imoto ,  Hiroyuki Kimura ,  Junichi Sakamoto

IPC分类号： A61K31425

CPC分类号： C07D213/74 ,  A61K31/42 ,  A61K31/421 ,  A61K31/4245 ,  A61K31/426 ,  A61K31/427 ,  A61K31/44 ,  A61K31/4439 ,  A61K31/47 ,  A61K31/4745 ,  A61K31/505 ,  C07D215/14 ,  C07D239/42 ,  C07D261/08 ,  C07D263/32 ,  C07D271/06 ,  C07D277/24 ,  C07D413/12 ,  C07D471/04

摘要： A compound represented by the formula: wherein R1 is an optionally substituted hydrocarbon group or an optionally substituted heterocyclic group; X is a bond, —CO—, —CH(OH)— or a group represented by —NR6— wherein R6 is a hydrogen atom or an optionally substituted alkyl group; n is an integer of 1 to 3; Y is an oxygen atom, a sulfur atom, —SO—, —SO2— or a group represented by —NR7— wherein R7 is a hydrogen atom or an optionally alkyl group; ring A is a benzene ring optionally having additional one to three substituents; p is an integer of 1 to 8; R2 is a hydrogen atom, an optionally substituted hydrocarbon group or an optionally substituted heterocyclic group; q is an integer of 0 to 6; m is 0 or 1; R3 is a hydroxy group, OR8 (R8 is an optionally substituted hydrocarbon group.) or NR9R10 (R9 and R10 are the same or different groups which are selected from a hydrogen atom, an optionally substituted hydrocarbon group, an optionally substituted heterocyclic group or an optionally substituted acyl group or R9 and R10 combine together to form a ring); R4 and R5 are the same or different groups which are selected from a hydrogen atom or an optionally substituted hydrocarbon group wherein R4 may form a ring with R2; provided that when R1 is a ethoxymethyl, a C1-3 alkyl, phenyl or p-methoxyphenyl and q=m=0, R3 is NR9R10; and provided that O-[2-chloro-4-(2-quinolylmethoxy)phenylmethyl]oxime and a methyl pyruvate of [2-chloro-4-(2-quinolylmethoxy)phenylmethyl]-2-iminoxypropionic acid are excluded; or a salt thereof which has excellent hypoglycemic and hypolipidemic actions.

摘要翻译： 由下式表示的化合物：其中R1是任选取代的烃基或任选取代的杂环基; X是键，-CO - ， - CH（OH） - 或-NR 6 - 表示的基团，其中R 6是氢原子或任选取代的烷基; n为1〜3的整数。 Y是氧原子，硫原子，-SO-，-SO 2 - 或-NR 7 - 表示的基团，其中R 7是氢原子或任意烷基; 环A是任选具有另外一个至三个取代基的苯环; p为1〜8的整数， R2是氢原子，任选取代的烃基或任选取代的杂环基; q为0〜6的整数; m为0或1; R3是羟基，OR8（R8是任选取代的烃基）或NR9R10（R9和R10是相同或不同的基团，其选自氢原子，任选取代的烃基，任选取代的杂环基或 任选取代的酰基或R 9和R 10结合在一起形成环）; R4和R5是选自氢原子或任选取代的烃基的相同或不同的基团，其中R 4可以与R 2形成环; 条件是当R1是乙氧基甲基，C1-3烷基，苯基或对甲氧基苯基且q = m = 0时，R3是NR9R10; 并且排除了[2-氯-4-（2-喹啉基甲氧基）苯基甲基] -2-亚氨基丙酸的O- [2-氯-4-（2-喹啉基甲氧基）苯甲基]肟和丙酮酸甲酯。 或其盐，其具有优异的降血糖和降血脂作用。