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1. 发明授权

US06391905B1 Condensed 4,5,6,7-tetrahydrobenzo[C]thiopenes as enhancer for cell differentiation induction factor action 失效
标题翻译：缩合的4,5,6,7-四氢苯并[C]噻吩作为细胞分化诱导因子作用的增强剂
公开(公告)号：US06391905B1
公开(公告)日：2002-05-21
申请号：US09847416
申请日：2001-05-03
申请人： Tsuneo Yasuma , Tsuneo Oda , Masatoshi Hazama , Shigehisa Taketomi
发明人： Tsuneo Yasuma , Tsuneo Oda , Masatoshi Hazama , Shigehisa Taketomi
IPC分类号： A61K314162
CPC分类号： C07D495/04 , C07D513/04 , C07F9/6561
摘要： A compound represented by the formula: wherein X represents a sulfur atom or an oxygen atom; Y represents an optionally oxidized sulfur atom or an oxygen atom; Z represents a bond or a divalent hydrocarbon group; R1 represents an optionally substituted hydrocarbon group; R2 represents an optionally amidated or esterified carboxyl group; ring A represents an optionally substituted aromatic 5-membered heterocyclic ring; or a salt thereof. A compound of the above formula possesses cell differentiation inducing factor action-enhancing activity and anti-matrix metalloprotease activity and that is useful in the prevention and treatment of bone diseases such as osteoporosis, bone fractures, osteoarthritis and rheumatoid arthritis, arteriosclerosis, cancer metastasis, and diseases based on nerve degeneration.
摘要翻译：由下式表示的化合物：其中X表示硫原子或氧原子; Y表示任选氧化的硫原子或氧原子; Z表示键或二价烃基; R1表示任选取代的烃基; R 2表示任选的酰胺化或酯化的羧基; 环A表示任选取代的芳族5元杂环; 或其盐。上述化合物具有细胞分化诱导因子作用增强活性和抗基质金属蛋白酶活性，并且其可用于预防和治疗骨疾病如骨质疏松症，骨折，骨关节炎和类风湿性关节炎，动脉硬化，癌转移以及基于神经变性的疾病。

2. 发明授权

US6066658A Condensed 4,5,6,7-tetrahydrobenzo[C]thiophenes as enhancer for cell differentiation induction factor action 失效
标题翻译：缩合的4,5,6,7-四氢苯并[C]噻吩作为细胞分化诱导因子作用的增强子
公开(公告)号：US6066658A
公开(公告)日：2000-05-23
申请号：US252913
申请日：1999-02-19
申请人： Tsuneo Yasuma , Tsuneo Oda , Masatoshi Hazama , Shigehisa Taketomi
发明人： Tsuneo Yasuma , Tsuneo Oda , Masatoshi Hazama , Shigehisa Taketomi
IPC分类号： C07D495/04 , C07D498/04 , C07D513/04 , C07F9/6561 , A61K31/4439 , A61K31/429
CPC分类号： C07D495/04 , C07D513/04 , C07F9/6561
摘要： A compound represented by the formula: ##STR1## wherein X represents a sulfur atom or an oxygen atom; Y represents an optionally oxidized sulfur atom or an oxygen atom; Z represents a bond or a divalent hydrocarbon group; R.sup.1 represents an optionally substituted hydrocarbon group; R.sup.2 represents an optionally amidated or esterified carboxyl group; ring A represents an optionally substituted aromatic 5-membered heterocyclic ring; or a salt thereof. A compound of the above formula possesses cell differentiation inducing factor action-enhancing activity and anti-matrix metalloprotease activity and that is useful in the prevention and treatment of bone diseases such as osteoporosis, bone fractures, osteoarthritis and rheumatoid arthritis, arteriosclerosis, cancer metastasis, and diseases based on nerve degeneration.
摘要翻译：由下式表示的化合物：其中X表示硫原子或氧原子; Y表示任选氧化的硫原子或氧原子; Z表示键或二价烃基; R1表示任选取代的烃基; R 2表示任选的酰胺化或酯化的羧基; 环A表示任选取代的芳族5元杂环; 或其盐。上述化合物具有细胞分化诱导因子作用增强活性和抗基质金属蛋白酶活性，可用于预防和治疗骨质疏松症，骨折，骨关节炎和类风湿性关节炎，动脉硬化，癌症转移等骨疾病，和基于神经变性的疾病。

3. 发明授权

US06489351B1 Condensed 4,5,6,7-tetrahydrobenzo[C]thiophenes as enhancer for cell differentation induction factor action 失效
标题翻译：缩合的4,5,6,7-四氢苯并[C]噻吩作为细胞分化诱导因子作用的增强剂
公开(公告)号：US06489351B1
公开(公告)日：2002-12-03
申请号：US10105333
申请日：2002-03-26
申请人： Tsuneo Yasuma , Tsuneo Oda , Masatoshi Hazama , Shigehisa Taketomi
发明人： Tsuneo Yasuma , Tsuneo Oda , Masatoshi Hazama , Shigehisa Taketomi
IPC分类号： A61K311424
CPC分类号： C07D495/04 , C07D513/04 , C07F9/6561
摘要： A compound represented by the formula: wherein X represents a sulfur atom or an oxygen atom; Y represents an optionally oxidized sulfur atom or an oxygen atom; Z represents a bond or a divalent hydrocarbon group; R1 represents an optionally substituted hydrocarbon group; R2 represents an optionally amidated or esterified carboxyl group; ring A represents an optionally substituted aromatic 5-membered heterocyclic ring; or a salt thereof. A compound of the above formula possesses cell differentiation inducing factor action-enhancing activity and anti-matrix metalloprotease activity and that is useful in the prevention and treatment of bone diseases such as osteoporosis, bone fractures, osteoarthritis and rheumatoid arthritis, arteriosclerosis, cancer metastasis, and diseases based on nerve degeneration.
摘要翻译：由下式表示的化合物：其中X表示硫原子或氧原子; Y表示任选氧化的硫原子或氧原子; Z表示键或二价烃基; R1表示任选取代的烃基; R 2表示任选的酰胺化或酯化的羧基; 环A表示任选取代的芳族五元杂环; 或其盐。上述化合物具有细胞分化诱导因子作用增强活性和抗基质金属蛋白酶活性，并且其可用于预防和治疗骨疾病如骨质疏松症，骨折，骨关节炎和类风湿性关节炎，动脉硬化，癌转移以及基于神经变性的疾病。

4. 发明授权

US06242471B1 Condensed 4,5,6,7-tetrahydrobenzo[C]thiophenes as enhancer for cell differentiation induction factor action 失效
标题翻译：缩合的4,5,6,7-四氢苯并[C]噻吩作为细胞分化诱导因子作用的增强子
公开(公告)号：US06242471B1
公开(公告)日：2001-06-05
申请号：US09559453
申请日：2000-04-28
申请人： Tsuneo Yasuma , Tsuneo Oda , Masatoshi Hazama , Shigehisa Taketomi
发明人： Tsuneo Yasuma , Tsuneo Oda , Masatoshi Hazama , Shigehisa Taketomi
IPC分类号： A61K31424
CPC分类号： C07D495/04 , C07D513/04 , C07F9/6561
摘要： A compound represented by the formula: wherein X represents a sulfur atom or an oxygen atom; Y represents an optionally oxidized sulfur atom or an oxygen atom; Z represents a bond or a divalent hydrocarbon group; R1 represents an optionally substituted hydrocarbon group; R2 represents an optionally amidated or esterified carboxyl group; ring A represents an optionally substituted aromatic 5-membered heterocyclic ring; or a salt thereof. A compound of the above formula possesses cell differentiation inducing factor action-enhancing activity and anti-matrix metalloprotease activity and that is useful in the prevention and treatment of bone diseases such as osteoporosis, bone fractures, osteoarthritis and rheumatoid arthritis, arteriosclerosis, cancer metastasis, and diseases based on nerve degeneration.
摘要翻译：由下式表示的化合物：其中X表示硫原子或氧原子; Y表示任选氧化的硫原子或氧原子; Z表示键或二价烃基; R1表示任选取代的烃基; R 2表示任选的酰胺化或酯化的羧基; 环A表示任选取代的芳族5元杂环; 或其盐。上述化合物具有细胞分化诱导因子作用增强活性和抗基质金属蛋白酶活性，并且其可用于预防和治疗骨疾病如骨质疏松症，骨折，骨关节炎和类风湿性关节炎，动脉硬化，癌转移以及基于神经变性的疾病。

5. 发明申请

US20080131370A1 Screening Method 审中-公开
标题翻译：筛选方法
公开(公告)号：US20080131370A1
公开(公告)日：2008-06-05
申请号：US11579104
申请日：2005-04-26
申请人： Masatoshi Hazama , Yasushi Fujitani , Hidenori Ichijo
发明人： Masatoshi Hazama , Yasushi Fujitani , Hidenori Ichijo
IPC分类号： A61K39/395 , G01N33/00 , A61P3/10 , A61K31/70 , C07H21/00 , A61K38/45 , G01N33/53 , A61K49/00 , C12Q1/68 , A61K38/00 , C07K16/18 , A61P11/00 , C12Q1/02
CPC分类号： C12Q1/485 , A61K38/16 , G01N2500/00 , G01N2510/00
摘要： The present invention provides a method for screening for a prophylactic or therapeutic drug for apoptosis or an inflammation-associated disease, diabetes and complications thereof or a chronic obstructive pulmonary disease (COPD), namely, a method for screening for a prophylactic or therapeutic drug for apoptosis or an inflammation-associated disease, diabetes and complications thereof or COPD, which includes (1) comparing the activities of a protein having an amino acid sequence the same as or substantially the same as the amino acid sequence shown by SEQ ID NO: 2 or a partial peptide thereof or a salt thereof, between in the presence of a test substance and in the absence of the test substance, or (2) comparing the expressions of a protein having an amino acid sequence the same as or substantially the same as the amino acid sequence shown by SEQ ID NO: 2, a partial peptide thereof and a salt thereof in the cells having the ability to produce the protein, the partial peptide thereof and the salt thereof, between in the presence of a test substance and in the absence of the test substance.
摘要翻译：本发明提供了用于筛选用于凋亡或炎症相关疾病，糖尿病及其并发症或慢性阻塞性肺病（COPD）的预防或治疗药物的方法，即用于预防或治疗药物的预防或治疗药物的筛选方法凋亡或炎症相关疾病，糖尿病及其并发症或COPD，其包括（1）比较具有与SEQ ID NO：2所示氨基酸序列相同或基本相同的氨基酸序列的蛋白质的活性或其部分肽或其盐，在测试物质的存在下和不存在测试物质之间，或（2）比较具有与或不相同的氨基酸序列的蛋白质的表达在具有产生蛋白质的能力的细胞中SEQ ID NO：2所示的氨基酸序列，其部分肽及其盐，其部分肽在测试物质的存在下和不存在测试物质之间。

6. 发明申请

US20050234116A1 Vdac regulator 失效
标题翻译： Vdac调节器
公开(公告)号：US20050234116A1
公开(公告)日：2005-10-20
申请号：US10507731
申请日：2003-03-13
申请人： Yasuo Sugiyama , Masatoshi Hazama , Norihisa Iwakami
发明人： Yasuo Sugiyama , Masatoshi Hazama , Norihisa Iwakami
IPC分类号： A61K31/422 , A61P1/00 , A61P1/16 , A61P3/04 , A61P3/06 , A61P3/10 , A61P7/06 , A61P9/00 , A61P9/10 , A61P9/12 , A61P19/02 , A61P21/00 , A61P25/00 , A61P25/04 , A61P25/08 , A61P25/14 , A61P25/16 , A61P25/18 , A61P25/22 , A61P25/24 , A61P25/28 , A61P27/02 , A61P31/18 , A61P31/20 , A61P43/00 , C07D263/34 , C07D413/04 , C07D413/14 , A61K31/4178 , A61K31/427
CPC分类号： A61K31/422 , C07D263/34 , C07D413/04 , C07D413/14 , G01N2500/04
摘要： The present invention provides a VDAC regulator comprising a compound represented by the formula (I): wherein R1 is a halogen atom, an optionally substituted heterocyclic group, an optionally substituted hydroxy group, an optionally substituted thiol group or an optionally substituted amino group; A is an optionally substituted acyl group, an optionally substituted heterocyclic group, an optionally substituted hydroxy group or an optionally esterified or amidated carboxyl group; B is an optionally substituted aromatic group; X is an oxygen atom, a sulfur atom or an optionally substituted nitrogen atom; and Y is a divalent hydrocarbon group or heterocyclic group, a salt thereof or a prodrug thereof, which is useful as an agent for the prophylaxis or treatment of Down's syndrome and the like, and the like.
摘要翻译：本发明提供一种VDAC调节剂，其包含由式（I）表示的化合物：其中R 1是卤素原子，任选取代的杂环基，任选取代的羟基，任选取代的硫醇基或任选取代的氨基; A是任选取代的酰基，任选取代的杂环基，任选取代的羟基或任选酯化或酰胺化的羧基; B是任选取代的芳基; X是氧原子，硫原子或任选取代的氮原子; Y是可用作预防或治疗唐氏综合征等的二价烃基或杂环基，其盐或前体药物等。

7. 发明申请

US20050090534A1 Azole compounds 失效
标题翻译：唑类化合物
公开(公告)号：US20050090534A1
公开(公告)日：2005-04-28
申请号：US10505742
申请日：2003-02-27
申请人： Nozomu Sakai , Yu Momose , Katsuhito Murase , Masatoshi Hazama
发明人： Nozomu Sakai , Yu Momose , Katsuhito Murase , Masatoshi Hazama
IPC分类号： A61P3/10 , A61P25/00 , A61P25/24 , A61P43/00 , C07D263/32 , C07D263/38 , C07D263/46 , C07D263/48 , C07D277/28 , C07D277/30 , C07D277/40 , C07D277/46 , C07D413/04 , C07D413/06 , C07D413/12 , C07D413/14 , C07D417/04 , C07D417/14 , C07F9/653 , C07F9/6539 , C07D417/02 , A61K31/4178 , A61K31/422 , A61K31/427 , C07D413/02 , C07D43/02
CPC分类号： C07D413/04 , C07D263/32 , C07D263/38 , C07D263/46 , C07D263/48 , C07D277/30 , C07D277/40 , C07D277/46 , C07D413/06 , C07D413/12 , C07D413/14 , C07D417/04 , C07D417/14 , C07F9/653 , C07F9/6539
摘要： The present invention provides a compound represented by the formula (I) wherein R1 is a hydrogen atom, a halogen atom, an optionally substituted hydrocarbon group, an optionally substituted heterocyclic group, an optionally substituted hydroxy group, an optionally substituted thiol group or an optionally substituted amino group, A is an optionally substituted cyclic amino group or —NR2—W-D wherein R2 is a hydrogen atom or an alkyl group, W is a bond or a divalent acyclic hydrocarbon group, and D is an optionally substituted cyclic group, an optionally substituted amino group or an optionally substituted acyl group, B is an optionally substituted hydrocarbon group or an optionally substituted heterocyclic group, X is an oxygen atom, a sulfur atom or an optionally substituted nitrogen atom, and Y is a bond or a divalent acyclic hydrocarbon group, or a salt thereof, which is useful for the prophylaxis or treatment of diabetic neuropathy and the like.
摘要翻译：本发明提供由式（I）表示的化合物，其中R 1为氢原子，卤素原子，任选取代的烃基，任选取代的杂环基，任选取代的羟基，任选取代的硫醇基或任选取代的氨基，A是任选取代的环氨基或-NR 2 -WD，其中R 2是氢原子或烷基基团，W是键或二价无环烃基，D是任选取代的环状基团，任选取代的氨基或任选取代的酰基，B是任选取代的烃基或任选取代的杂环基，X是氧原子，硫原子或任选取代的氮原子，Y是可用于预防或治疗糖尿病性神经病变等的键或二价无环烃基或其盐。

8. 发明授权

US07498352B2 TGF-β superfamily production/secretion promoter 失效
标题翻译： TGF-β超家族生产/分泌启动子
公开(公告)号：US07498352B2
公开(公告)日：2009-03-03
申请号：US10480849
申请日：2002-06-25
申请人： Yasuo Sugiyama , Masatoshi Hazama , Asae Shintani
发明人： Yasuo Sugiyama , Masatoshi Hazama , Asae Shintani
IPC分类号： A61K31/42 , C07D263/30
CPC分类号： A61K31/422
摘要： The present invention provides a TGF-β superfamily production/secretion promoter comprising a compound represented by the formula wherein R1 is a halogen atom, an optionally substituted heterocyclic group, an optionally substituted hydroxy group, an optionally substituted thiol group or an optionally substituted amino group; A is an optionally substituted acyl group, an optionally substituted heterocyclic group, an optionally substituted hydroxy group or an optionally esterified or amidated carboxyl group; B is an optionally substituted aromatic group; X is an oxygen atom, a sulfur atom or an optionally substituted nitrogen atom; and Y is a divalent hydrocarbon group or heterocyclic group, or a salt thereof or a prodrug thereof, which is useful as an agent for the prophylaxis or treatment of dysautonomia, bladder dysfunction, hearing impairment, bone disease and the like.
摘要翻译：本发明提供了包含下式表示的化合物的TGF-β超家族产生/分泌促进剂，其中R1是卤素原子，任选取代的杂环基，任选取代的羟基，任选取代的硫醇基或任选取代的氨基 ; A是任选取代的酰基，任选取代的杂环基，任选取代的羟基或任选酯化或酰胺化的羧基; B是任选取代的芳基; X是氧原子，硫原子或任选取代的氮原子; Y是二价烃基或杂环基，或其盐或其前药，其可用作预防或治疗自主神经功能障碍，膀胱功能障碍，听力障碍，骨病等。

9. 发明授权

US07462635B2 Thiazole and oxazole VDAC regulator 失效
标题翻译：噻唑和恶唑VDAC调节剂
公开(公告)号：US07462635B2
公开(公告)日：2008-12-09
申请号：US10507731
申请日：2003-03-13
申请人： Yasuo Sugiyama , Masatoshi Hazama , Norihisa Iwakami
发明人： Yasuo Sugiyama , Masatoshi Hazama , Norihisa Iwakami
IPC分类号： A61K31/422 , A61K31/427 , A61K31/4178
CPC分类号： A61K31/422 , C07D263/34 , C07D413/04 , C07D413/14 , G01N2500/04
摘要： The present invention provides a VDAC regulator comprising a compound represented by the formula (I): wherein R1 is a halogen atom, an optionally substituted heterocyclic group, an optionally substituted hydroxyl group, an optionally substituted thiol group or an optionally substituted amino group; A is an optionally substituted acyl group, an optionally substituted heterocyclic group, an optionally substituted hydroxyl group or an optionally esterified or amidated carboxyl group; B is an optionally substituted aromatic group; X is an oxygen atom, a sulfur atom or an optionally substituted nitrogen atom; and Y is a divalent hydrocarbon group or heterocyclic group; a salt thereof or a prodrug thereof, which is useful as an agent for the prophylaxis or treatment of Down's syndrome and the like.
摘要翻译：本发明提供一种VDAC调节剂，其包含由式（I）表示的化合物：其中R1是卤素原子，任选取代的杂环基，任选取代的羟基，任选取代的硫醇基或任选取代的氨基; A是任选取代的酰基，任选取代的杂环基，任选取代的羟基或任选酯化或酰胺化的羧基; B是任选取代的芳基; X是氧原子，硫原子或任选取代的氮原子; Y为二价烃基或杂环基; 其盐或其前药，其可用作预防或治疗唐氏综合征等的药剂。

10. 发明授权

US07183276B2 Azole compounds 失效
标题翻译：唑类化合物
公开(公告)号：US07183276B2
公开(公告)日：2007-02-27
申请号：US10505742
申请日：2003-02-27
申请人： Nozomu Sakai , Yu Momose , Katsuhito Murase , Masatoshi Hazama
发明人： Nozomu Sakai , Yu Momose , Katsuhito Murase , Masatoshi Hazama
IPC分类号： A61K31/5377 , A61K31/421 , A61K31/454 , A61K31/541 , C07D413/04 , C07D279/12 , C07F9/653 , C07D211/46
CPC分类号： C07D413/04 , C07D263/32 , C07D263/38 , C07D263/46 , C07D263/48 , C07D277/30 , C07D277/40 , C07D277/46 , C07D413/06 , C07D413/12 , C07D413/14 , C07D417/04 , C07D417/14 , C07F9/653 , C07F9/6539
摘要： The present invention provides a compound represented by the formula (I) wherein R1 is a hydrogen atom, a halogen atom, an optionally substituted hydrocarbon group, an optionally substituted heterocyclic group, an optionally substituted hydroxy group, an optionally substituted thiol group or an optionally substituted amino group, A is an optionally substituted cyclic amino group or —NR2—W—D wherein R2 is a hydrogen atom or an alkyl group, W is a bond or a divalent acyclic hydrocarbon group, and D is an optionally substituted cyclic group, an optionally substituted amino group or an optionally substituted acyl group, B is an optionally substituted hydrocarbon group or an optionally substituted heterocyclic group, X is an oxygen atom, a sulfur atom or an optionally substituted nitrogen atom, and Y is a bond or a divalent acyclic hydrocarbon group, or a salt thereof, which is useful for the prophylaxis or treatment of diabetic neuropathy and the like.
摘要翻译：本发明提供由式（I）表示的化合物，其中R 1为氢原子，卤素原子，任选取代的烃基，任选取代的杂环基，任选取代的羟基，任选取代的硫醇基或任选取代的氨基，A是任选取代的环氨基或-NR 2 -WD，其中R 2是氢原子或烷基基团，W是键或二价无环烃基，D是任选取代的环状基团，任选取代的氨基或任选取代的酰基，B是任选取代的烃基或任选取代的杂环基，X是氧原子，硫原子或任选取代的氮原子，Y是可用于预防或治疗糖尿病性神经病变等的键或二价无环烃基或其盐。

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