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1. 发明授权

US5550138A Condensed thiadiazole derivative, method of its production, and use thereof 失效
标题翻译：缩合噻二唑衍生物，其制备方法及其用途
公开(公告)号：US5550138A
公开(公告)日：1996-08-27
申请号：US039579
申请日：1993-03-23
申请人： Takashi Sohda , Zen-ichi Terashita , Yu Momose , Yukio Fujisawa , Junji Mizoguchi
发明人： Takashi Sohda , Zen-ichi Terashita , Yu Momose , Yukio Fujisawa , Junji Mizoguchi
IPC分类号： C07D513/04 , A61K31/435
CPC分类号： C07D513/04
摘要： (1) a compound represented by the following formula (I): ##STR1## wherein R represents a hydrocarbon group or heterocyclic group which may be substituted; the ring A represents a pyridine ring having a substituent or a thiazole ring which may be substituted; or a pharmaceutically acceptable salt thereof, and a method of its production, and(2) an endothelin receptor antagonist, an cathepsin B inhibitor or a bone resorption suppressor having as an active ingredient a compound represented by the following formula (I'): ##STR2## wherein R has the same definition as in term (1); the ring A' represents a pyridine ring or thiazole ring which may be substituted; or a pharmaceutically acceptable salt thereof.
摘要翻译：（1）由下式（I）表示的化合物：其中R表示可被取代的烃基或杂环基; 环A表示具有取代基的吡啶环或可被取代的噻唑环; 或其药学上可接受的盐及其制备方法，和（2）作为活性成分的下式（I'）表示的化合物的内皮素受体拮抗剂，组织蛋白酶B抑制剂或骨吸收抑制剂：（I'）其中R与术语（1）具有相同的定义; 环A'表示可被取代的吡啶环或噻唑环; 或其药学上可接受的盐。

2. 发明授权

US5614544A Oxazolidinedione derivatives and their use 失效
标题翻译：恶唑二酮衍生物及其用途
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

3. 发明授权

US5371098A Use of oxazole compounds to treat osteoporosis 失效
标题翻译：使用恶唑化合物治疗骨质疏松症
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。

4. 发明授权

US06552058B1 Oxazolidinedione derivatives and their use 失效
标题翻译：恶唑二酮衍生物及其用途
公开(公告)号：US06552058B1
公开(公告)日：2003-04-22
申请号：US09667247
申请日：2000-09-22
申请人： Takashi Sohda , Hitoshi Ikeda , Yu Momose , Sachiko Imai
发明人： Takashi Sohda , Hitoshi Ikeda , Yu Momose , Sachiko Imai
IPC分类号： C07D26318
CPC分类号： C07D263/44 , C07D413/12 , C07D413/14 , C07D417/12
摘要： Novel 2,4-oxazolidinedione compounds of the formula: wherein R is a hydrocarbon residue or a heterocyclic group each of which may be substituted; Y is —CO—, —CH(OH)— or —NR3— (wherein R3 is an alkyl group which may be substituted); m is 0 or 1; n is 0, 1 or 2; X is CH or N; A is bivalent straight or branched hydrocarbon chain residue having 1 to 7 carbon atoms; R1 and R2 each are hydrogen or an alkyl group, or R1 and R2 are combined with each other to form a 5- to 6-membered heterocyclic group optionally containing nitrogen; L and M each are hydrogen, or L and M are combined with each other to form a bond, or pharmaceutically acceptable salts thereof, having excellent hypoglycemic and hypolipidemic activities and are useful as anti-diabetics or hypolipidemic agents.
摘要翻译：下式的新型2,4-恶唑烷二酮化合物：其中R是可以被取代的烃残基或杂环基; Y是-CO - ， - CH（OH） - 或-NR 3 - （其中R 3是可被取代的烷基）; m为0或1; n为0,1或2; X是CH或N; A是具有1至7个碳原子的二价直链或支链烃链残基; R 1和R 2各自为氢或烷基，或者R 1和R 2彼此结合形成任选含有氮的5至6元杂环基; L和M各自为氢，或L和M彼此结合以形成具有优异的降血糖和降血脂活性的键或其药学上可接受的盐，并且可用作抗糖尿病药或降血脂药。

5. 发明授权

US06365607B1 Anticachectic composition 失效
标题翻译：防寒组成
公开(公告)号：US06365607B1
公开(公告)日：2002-04-02
申请号：US09605628
申请日：2000-06-28
申请人： Yu Momose , Etsuya Matsutani , Takashi Sohda
发明人： Yu Momose , Etsuya Matsutani , Takashi Sohda
IPC分类号： A61K3144
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: 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— (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 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 bond, provided that when m and n are 0, X represents CH, A represents a bond, Q represents sulfur, R1, 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：一种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。

6. 发明授权

US6147099A Oxazolidinedione derivatives, their production and use 失效
标题翻译：恶唑二酮衍生物，其生产和使用
公开(公告)号：US6147099A
公开(公告)日：2000-11-14
申请号：US292748
申请日：1999-04-16
申请人： Takashi Sohda , Hitoshi Ikeda , Yu Momose , Sachiko Imai
发明人： Takashi Sohda , Hitoshi Ikeda , Yu Momose , Sachiko Imai
IPC分类号： C07D491/048 , A61K31/42 , A61K31/421 , A61K31/422 , A61K31/425 , A61K31/427 , A61K31/435 , A61K31/44 , A61K31/4439 , A61K31/47 , A61K31/4709 , A61K31/535 , A61K31/5377 , A61P3/06 , A61P3/08 , A61P3/10 , A61P9/12 , A61P43/00 , C07D263/44 , C07D277/22 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D491/052 , C07D498/04
CPC分类号： C07D263/44 , C07D413/12 , C07D413/14 , C07D417/12
摘要： Novel 2,4-oxazolidinedione compounds of the formula: ##STR1## wherein R is a hydrocarbon residue or a heterocyclic group each of which may be substituted; Y is --CO--, --CH(OH)-- or --NR.sup.3 -- (wherein R.sup.3 is an alkyl group which may be substituted); m is 0 or 1; n is 0, 1 or 2; X is CH or N; A is bivalent straight or branched hydrocarbon chain residue having 1 to 7 carbon atoms; R.sup.1 and R.sup.2 each are hydrogen or an alkyl group, or R and R are combined with each other to form a 5- to 6-membered heterocyclic group optionally containing nitrogen; L and M each are hydrogen, or L and M are combined with each other to form a bond, or pharmaceutically acceptable salts thereof, having excellent hypoglycemic and hypolipidemic activities and are useful as anti-diabetics or hypolipidemic agents.
摘要翻译：下式的新型2,4-恶唑烷二酮化合物：其中R是可以被取代的烃残基或杂环基; Y是-CO - ， - CH（OH） - 或-NR 3 - （其中R 3是可被取代的烷基）; m为0或1; n为0,1或2; X是CH或N; A是具有1至7个碳原子的二价直链或支链烃链残基; R 1和R 2各自为氢或烷基，或R和R彼此结合形成任选含有氮的5至6元杂环基; L和M各自为氢，或L和M彼此结合以形成具有优异的降血糖和降血脂活性的键或其药学上可接受的盐，并且可用作抗糖尿病药或降血脂药。

7. 发明授权

US6110948A Anticachectic composition 失效
标题翻译：防寒组成
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。

8. 发明授权

US5239080A Oxazole compounds and their use as antidiabetic and bone-reduction inhibitory agents 失效
标题翻译：恶唑化合物及其作为抗糖尿病和骨抑制剂的用途
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。

9. 发明授权

US5965589A Thiazolidinedione derivatives, their production and use 失效
标题翻译：噻唑烷二酮衍生物，其生产和使用
公开(公告)号：US5965589A
公开(公告)日：1999-10-12
申请号：US530115
申请日：1995-10-05
申请人： Takashi Sohda , Hiroyuki Odaka , Yu Momose
发明人： Takashi Sohda , Hiroyuki Odaka , Yu Momose
IPC分类号： C07D277/34 , C07D417/12 , C07D413/12 , A61K31/42
CPC分类号： C07D417/12 , C07D277/34
摘要： A 2,4-thiazolidinedione derivative of the formula (I): ##STR1## wherein R is an optionally substituted hydrocarbon group or heterocyclic group which may be attached through a hydrocarbon chain; n is 0 or 1; X is CH or N; Y is a bivalent hydrocarbon group; R.sup.1 and R.sup.2 are the same or different and are a hydrogen atom, a halogen atom, an optionally substituted hydroxyl group or an optionally substituted hydrocarbon group, and either R.sup.1 or R.sup.2 and a part of Y may be linked together to form a ring; and L and M are a hydrogen atom, or L and M are linked together to form a bond; or a salt thereof. A pharmaceutical composition comprising the compound (I) and a process for producing the compound (I) are also provided.
摘要翻译： PCT No.PCT / JP95 / 01579 Sec。 371日期1995年10月5日第 102（e）日期1995年10月5日PCT 1995年8月9日PCT PCT。公开号WO96 / 05186 日期：1996年2月22日A式（I）的2,4-噻唑烷二酮衍生物：其中R是可通过烃链连接的任选取代的烃基或杂环基; n为0或1; X是CH或N; Y为二价烃基; R 1和R 2相同或不同，为氢原子，卤素原子，任选取代的羟基或任选取代的烃基，R 1或R 2和Y的一部分可以连接在一起形成环; L和M是氢原子，或L和M连接在一起形成键; 或其盐。还提供了包含化合物（I）和制备化合物（I）的方法的药物组合物。

10. 发明授权

US5932601A Oxazolidinedione derivatives, their production and use 失效
标题翻译：恶唑二酮衍生物，其生产和使用
公开(公告)号：US5932601A
公开(公告)日：1999-08-03
申请号：US550289
申请日：1995-10-30
申请人： Takashi Sohda , Hiroyuki Odaka , Yu Momose , Mitsuru Kawada
发明人： Takashi Sohda , Hiroyuki Odaka , Yu Momose , Mitsuru Kawada
IPC分类号： A61K31/42 , C07D263/32 , C07D263/44 , C07D277/22 , C07D277/24 , C07D413/04 , C07D413/12 , C07D413/14 , C07D417/12
CPC分类号： C07D277/22 , C07D263/32 , C07D263/44 , C07D277/24 , C07D413/04 , C07D413/12 , C07D413/14 , C07D417/12
摘要： 2,4-Oxazolidinedione derivative represented by the formula: ##STR1## wherein R stands for an optionally substituted hydrocarbon residue or heterocyclic group; Y stands for a group represented by --CO--, --CH(OH)-- or --NR.sup.3 -- (wherein R.sup.3 stands for an optionally substituted alkyl group); m is 0 or 1; n is 0, 1 or 2; A stands for a C.sub.1-7 divalent aliphatic hydrocarbon group; R.sup.1 stands for hydrogen or an alkyl group; ring E stands for a benzene ring having 1 or 2 substituents; L and M respectively stand for hydrogen, or L and M may optionally be combined with each other to form a bond; with a proviso that the partial formula: ##STR2## does not include the formula: ##STR3## wherein R' stands for an alkyl group; or a salt thereof, which has excellent actions of lowering blood sugar and lipid in blood.
摘要翻译：由下式表示的2,4-恶唑烷二酮衍生物：其中R表示任选取代的烃残基或杂环基; Y表示由-CO-，-CH（OH） - 或-NR 3 - （其中R 3表示任选取代的烷基）表示的基团; m为0或1; n为0,1或2; A代表C 1-7二价脂族烃基; R1代表氢或烷基; 环E代表具有1或2个取代基的苯环; L和M分别代表氢，或者L和M可以任选地彼此结合形成键; 条件是部分式：不包括下式：其中R'代表烷基; 或其盐，其具有降低血液中血糖和血脂的优异作用。

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