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1. 发明申请

US20050171185A1 Indole derivatives 审中-公开
标题翻译：吲哚衍生物
公开(公告)号：US20050171185A1
公开(公告)日：2005-08-04
申请号：US11092398
申请日：2005-03-29
申请人： Noritsugu Yamasaki , Takafumi Imoto , Teruo Oku , Noriko Oku , Chikako Oku , Tomohito Oku , Hiroshi Kayakiri , Osamu Onomura , Takahiro Hiramura
发明人： Noritsugu Yamasaki , Takafumi Imoto , Teruo Oku , Noriko Oku , Chikako Oku , Tomohito Oku , Hiroshi Kayakiri , Osamu Onomura , Takahiro Hiramura
IPC分类号： C07D209/10 , C07D209/12 , C07D405/10 , C07D409/10 , C07D409/12 , A61K31/405 , C07D209/02 , C07D43/02
CPC分类号： C07D405/10 , C07D209/10 , C07D209/12 , C07D409/10 , C07D409/12
摘要： A novel indole derivative or a salt thereof is provided, which is represented by the formula: wherein R1 represents an aryl lower alkyl group, said aryl group may be substituted with one or more groups selected from the group consisting of a halogen atom, an aryl group, a heterocyclic group, an aryl lower alkyl group, an aryl lower alkenyl group, a halo-lower alkyl group, a lower cycloalkyl-lower alkoxy group, a lower cycloalkoxy-lower alkyl group, an aryl lower alkynyl group, an aryloxy lower alkyl group, an aryl lower alkoxy group, a lower alkylthio group, a lower alkoxy group, and an alkenyl group; and R2 represents a lower alkyl group, a lower alkenyl group, an aryl group, or a heterocyclic group, each of which may be substituted with a hydrogen atom, a lower alkyl group, a lower alkenyl group, or an aryl group. The compound of the present invention has blood sugar level-depressing activity and PDE5-inhibiting activity, and is useful as medicine.
摘要翻译：提供了一种新的吲哚衍生物或其盐，其由下式表示：其中R 1表示芳基低级烷基，所述芳基可以被一个或多个选自下组的基团取代：由卤素原子，芳基，杂环基，芳基低级烷基，芳基低级烯基，卤代低级烷基，低级环烷基 - 低级烷氧基，低级环烷氧基 - 低级烷基，芳基低级炔基，芳氧基低级烷基，芳基低级烷氧基，低级烷硫基，低级烷氧基和烯基; R 2表示低级烷基，低级烯基，芳基或杂环基，它们各自可以被氢原子，低级烷基，低级烯基，或芳基。本发明的化合物具有血糖降低活性和PDE5抑制活性，作为药物有用。

2. 发明申请

US20140012010A1 METHOD FOR PRODUCING OPTICALLY ACTIVE COMPOUND OR SALT THEREOF 有权
标题翻译：用于生产光学活性化合物或其盐的方法
公开(公告)号：US20140012010A1
公开(公告)日：2014-01-09
申请号：US13982707
申请日：2012-01-31
申请人： Osamu Onomura , Yutaro Tsuda , Masami Kuriyama , Toshiharu Yanagi , Kazuya Kodama
发明人： Osamu Onomura , Yutaro Tsuda , Masami Kuriyama , Toshiharu Yanagi , Kazuya Kodama
IPC分类号： C07D263/14 , C07D413/04
CPC分类号： C07D263/14 , C07B53/00 , C07D413/04 , C07D417/04
摘要： Provided is a process for producing an optically active compound represented by Formula (3): (wherein R1 is an alkyl group, an alkynyl group, an alkenyl group, an aliphatic heterocyclic group, a cycloalkyl group, an aryl group, an aralkyl group, or an aromatic heterocyclic group, and any hydrogen atom of R1 may be replaced with a substituent; R2 is a hydrogen atom or a group which is not reactive in the reaction below; and * represents a chiral center) or a salt thereof by subjecting a compound represented by Formula (1): (wherein R1 and R2 have the same meanings as defined in Formula (3)) to a ring closure reaction in the presence of a chiral ligand having 1 or more coordination sites, a Lewis acid represented by Formula (2): MmZn (2) (wherein M is a metal ion, Z is a counter anion of M, and m and n are integers of 1 to 4), and a sulfonyl halide having an optionally substituted alkyl or phenyl group
摘要翻译：提供一种制备由式（3）表示的光学活性化合物的方法：（其中R1是烷基，炔基，烯基，脂族杂环基，环烷基，芳基，芳烷基，或芳族杂环基，R 1的任何氢原子可以被取代基取代; R2是氢原子或下述反应中不具有反应性的基团;和*表示手性中心）或其盐，通过使由式（1）表示的化合物：其中R1和R2与式（3）中定义相同）在具有1个或多个配位点的手性配位体存在下进行闭环反应，式（2）：MmZn（2）（其中M是金属离子，Z是M的抗衡阴离子，m和n是1〜4的整数）和具有任选取代的烷基或苯基的磺酰卤

3. 发明申请

US20070276156A1 PROCESS FOR PRODUCING ALIPHATIC DICARBOXYLIC ACID COMPOUND 失效
标题翻译：生产二氯二羧酸化合物的方法
公开(公告)号：US20070276156A1
公开(公告)日：2007-11-29
申请号：US10599171
申请日：2005-03-23
申请人： Yoshihiro Matsumura , Osamu Onomura , Fumiaki Iwasaki
发明人： Yoshihiro Matsumura , Osamu Onomura , Fumiaki Iwasaki
IPC分类号： C07C51/31
CPC分类号： C07C51/316 , C07C55/02
摘要： The present invention discloses a process for producing an aliphatic dicarboxylic acid compound, which comprises oxidizing, with a nitrite or a nitrate in the presence of trifluoroacetic acid, an alicyclic secondary alcohol compound or an alicyclic ketone compound, in each of which at least one methylene group is bonded to the carbon atom having hydroxyl group bonded thereto or the carbon atom as a member of carbonyl group, wherein the reaction is conducted in the presence of water of 5 mass % or less relative to 100 mass % of the total of the trifluoroacetic acid and the water.
摘要翻译：本发明公开了一种生产脂肪族二羧酸化合物的方法，其包括在三氟乙酸存在下，用亚硝酸盐或硝酸盐，脂环族仲醇化合物或脂环酮化合物氧化至少一种亚甲基基团与键合有羟基的碳原子或作为羰基成员的碳原子结合，其中反应在相对于三氟乙酸总量的100质量％为5质量％以下的水的存在下进行酸和水。

4. 发明授权

US08969585B2 Method for producing optically active compound or salt thereof 有权
标题翻译：光学活性化合物或其盐的制备方法
公开(公告)号：US08969585B2
公开(公告)日：2015-03-03
申请号：US13982707
申请日：2012-01-31
申请人： Osamu Onomura , Yutaro Tsuda , Masami Kuriyama , Toshiharu Yanagi , Kazuya Kodama
发明人： Osamu Onomura , Yutaro Tsuda , Masami Kuriyama , Toshiharu Yanagi , Kazuya Kodama
IPC分类号： C07D263/14 , C07D413/04 , C07B53/00 , C07D417/04
CPC分类号： C07D263/14 , C07B53/00 , C07D413/04 , C07D417/04
摘要： Provided is a process for producing an optically active compound represented by Formula (3): (wherein R1 is an alkyl group, an alkynyl group, an alkenyl group, an aliphatic heterocyclic group, a cycloalkyl group, an aryl group, an aralkyl group, or an aromatic heterocyclic group, and any hydrogen atom of R1 may be replaced with a substituent; R2 is a hydrogen atom or a group which is not reactive in the reaction below; and * represents a chiral center) or a salt thereof by subjecting a compound represented by Formula (1): (wherein R1 and R2 have the same meanings as defined in Formula (3)) to a ring closure reaction in the presence of a chiral ligand having 1 or more coordination sites, a Lewis acid represented by Formula (2): MmZn (2) (wherein M is a metal ion, Z is a counter anion of M, and m and n are integers of 1 to 4), and a sulfonyl halide having an optionally substituted alkyl or phenyl group.
摘要翻译：提供一种制备由式（3）表示的光学活性化合物的方法：（其中R1是烷基，炔基，烯基，脂族杂环基，环烷基，芳基，芳烷基，或芳族杂环基，R 1的任何氢原子可以被取代基取代; R2是氢原子或下述反应中不具有反应性的基团;和*表示手性中心）或其盐，通过使由式（1）表示的化合物：其中R1和R2与式（3）中定义相同）在具有1个或多个配位点的手性配位体存在下进行闭环反应，式（2）：MmZn（2）（其中M是金属离子，Z是M的抗衡阴离子，m和n是1〜4的整数）和具有任选取代的烷基或苯基的磺酰卤。

5. 发明授权

US07312357B2 Process for producing aliphatic dicarboxylic acid compound 失效
标题翻译：脂肪族二羧酸化合物的制造方法
公开(公告)号：US07312357B2
公开(公告)日：2007-12-25
申请号：US10599171
申请日：2005-03-23
申请人： Yoshihiro Matsumura , Osamu Onomura , Fumiaki Iwasaki
发明人： Yoshihiro Matsumura , Osamu Onomura , Fumiaki Iwasaki
IPC分类号： C07C51/245 , C07C51/27
CPC分类号： C07C51/316 , C07C55/02
摘要： The present invention discloses a process for producing an aliphatic dicarboxylic acid compound, which comprises oxidizing, with a nitrite or a nitrate in the presence of trifluoroacetic acid, an alicyclic secondary alcohol compound or an alicyclic ketone compound, in each of which at least one methylene group is bonded to the carbon atom having hydroxyl group bonded thereto or the carbon atom as a member of carbonyl group, wherein the reaction is conducted in the presence of water of 5 mass % or less relative to 100 mass % of the total of the trifluoroacetic acid and the water.
摘要翻译：本发明公开了一种生产脂肪族二羧酸化合物的方法，其包括在三氟乙酸存在下，用亚硝酸盐或硝酸盐，脂环族仲醇化合物或脂环酮化合物氧化至少一种亚甲基基团与键合有羟基的碳原子或作为羰基成员的碳原子结合，其中反应在相对于三氟乙酸总量的100质量％为5质量％以下的水的存在下进行酸和水。

6. 发明授权

US06911469B2 Sulfonamide compounds and pharmaceutical use thereof 失效
标题翻译：磺酰胺化合物及其药物用途
公开(公告)号：US06911469B2
公开(公告)日：2005-06-28
申请号：US10047093
申请日：2002-01-17
申请人： Hiroshi Kayakiri , Yoshito Abe , Hitoshi Hamashima , Hitoshi Sawada , Tsuyoshi Mizutani , Teruo Oku , Noritsugu Yamasaki , Osamu Onomura , Masahiro Nishikawa , Takahiro Hiramura , Takafumi Imoto
发明人： Hiroshi Kayakiri , Yoshito Abe , Hitoshi Hamashima , Hitoshi Sawada , Tsuyoshi Mizutani , Teruo Oku , Noritsugu Yamasaki , Osamu Onomura , Masahiro Nishikawa , Takahiro Hiramura , Takafumi Imoto
IPC分类号： G06Q50/10 , A61K20060101 , A61K31/381 , A63B69/36 , C07D20060101 , C07D215/48 , C07D231/56 , C07D239/96 , C07D241/52 , C07D249/18 , C07D307/79 , C07D333/54 , C07D333/56 , C07D333/62 , C07D405/12 , C07D409/12 , C07D471/04 , C07D487/04 , C07D495/04 , C07F20060101 , A61K31/34
CPC分类号： C07D241/52 , C07D215/48 , C07D231/56 , C07D239/96 , C07D249/18 , C07D307/79 , C07D333/54 , C07D333/62 , C07D405/12 , C07D409/12 , C07D471/04 , C07D487/04 , C07D495/04
摘要： A sulfonamide compound of the formula (I): R1—SO2NHCO—A—X—R2 (I) wherein R1 is alky, alkenyl, alkynyl and the like; A is an optionally substitutedheteropolycyclic group except benzimidazolyl, indolyl, 4,7-dihydrobenzimidazolyland 2,3-dihydrobenzoxazinyl; X is alkylene, oxa, oxa(lower)alkylene and the like; and R2 is optionally substituted aryl, substituted biphenylyl and the like, a salt thereof and a pharmaceutical composition comprising the same. The sulfonamide compound is effective for the diseases treatable based on their blood sugar level-depressing activity, cGMP-PDE (especially PDE-V)-inhibiting activity, smooth muscle relaxing activity, bronchodilating activity, vasodilating activity, smooth muscle cell suppressing activity, and antiallergic activity.
摘要翻译：式（I）的磺酰胺化合物：<？in-line-formula description =“In-line Formulas”end =“lead”→> R 2 NHCO-AXR 2（I）<？in-line-formula description =“In-line Formulas”end =“tail”？>其中R 1是烷基，烯基，炔基等; A是任选取代的杂多环基团，除了苯并咪唑基，吲哚基，4,7-二氢苯并咪唑啉-2,3-二氢苯并恶嗪基; X是亚烷基，氧杂，氧杂（低级）亚烷基等; 和R 2是任选取代的芳基，取代的联苯基等，其盐和包含它们的药物组合物。磺胺类化合物可以基于其血糖降低活性，cGMP-PDE（特别是PDE-V）抑制活性，平滑肌松弛活性，支气管扩张活性，血管舒张活性，平滑肌细胞抑制活性，以及抗过敏活性。

7. 发明授权

US06420613B1 Process for preparing reductants of unsaturated organic compounds by the use of trichlorosilane and reducing agents 失效
标题翻译：通过使用三氯硅烷和还原剂制备不饱和有机化合物的还原剂的方法
公开(公告)号：US06420613B1
公开(公告)日：2002-07-16
申请号：US09674960
申请日：2000-12-11
申请人： Fumiaki Iwasaki , Yoshihiro Matsumura , Osamu Onomura , Kenji Tanaka
发明人： Fumiaki Iwasaki , Yoshihiro Matsumura , Osamu Onomura , Kenji Tanaka
IPC分类号： C07C3700
CPC分类号： C07C29/143 , C07B2200/07 , C07B2200/09 , C07C29/14 , C07C209/52 , C07C2601/14 , C07C2601/16 , C07C2601/18 , C07C211/17 , C07C211/27 , C07C211/45 , C07C211/52 , C07C31/12 , C07C31/125 , C07C35/08 , C07C35/20 , C07C33/46 , C07C33/22 , C07C33/24 , C07C33/18 , C07C33/20 , C07C35/21 , C07C35/18
摘要： A method of preparing a reduced product by efficiently reducing an unsaturated organic compound by using, as a reducing agent, a trichlorosilane which is industrially cheaply available and is easy to handle, and a reducing agent therefor. A reduced product of an unsaturated organic compound is obtained by mixing the unsaturated organic compound and a trichlorosilane together to reduce the unsaturated organic compound in the presence of a compound that forms a silicon complex having five coordinations upon acting on the trichlorosilane such as an N-formylated product of a secondary amine having not less than 3 carbon atoms. The invention further provides a reducing agent comprising a particular silicon complex.
摘要翻译：通过使用工业上廉价可利用并易于处理的三氯硅烷作为还原剂，有效还原不饱和有机化合物及其还原剂，制备还原产物的方法。不饱和有机化合物的还原产物是通过将不饱和有机化合物和三氯硅烷混合在一起，在作用于三氯硅烷上的形成具有五个配位的硅配合物的化合物的存在下将不饱和有机化合物混合在一起，具有不少于3个碳原子的仲胺的甲酰化产物。本发明还提供了包含特定硅复合物的还原剂。

8. 发明授权

US06348474B1 Sulfonamide compounds and medicinal use thereof 失效
标题翻译：磺酰胺类化合物及其医药用途
公开(公告)号：US06348474B1
公开(公告)日：2002-02-19
申请号：US09446110
申请日：2000-02-14
申请人： Hiroshi Kayakiri , Yoshito Abe , Hitoshi Hamashima , Hitoshi Sawada , Tsuyoshi Mizutani , Teruo Oku , Noritsugu Yamasaki , Osamu Onomura , Masahiro Nishikawa , Takahiro Hiramura , Takafumi Imoto
发明人： Hiroshi Kayakiri , Yoshito Abe , Hitoshi Hamashima , Hitoshi Sawada , Tsuyoshi Mizutani , Teruo Oku , Noritsugu Yamasaki , Osamu Onomura , Masahiro Nishikawa , Takahiro Hiramura , Takafumi Imoto
IPC分类号： A61K31435
CPC分类号： C07D241/52 , C07D215/48 , C07D231/56 , C07D239/96 , C07D249/18 , C07D307/79 , C07D333/54 , C07D333/62 , C07D405/12 , C07D409/12 , C07D471/04 , C07D487/04 , C07D495/04
摘要： A sulfonamide compound of the formula (I): R1—SO2NHCO—A—R2 (I) wherein R1 is alkyl, alkenyl, alkynyl and the like; A is an optionally substituted heteropolycyclic group except benzimidazolyl, indolyl, 4,7-dihydrobenzimidazolyl and 2,3-dihydrobenzoxazinyl; X is alkylene, oxa, oxa(lower)alkylene and the like; and R2 is optionally substituted aryl, substituted biphenylyl and the like, a salt thereof and a pharmaceutical composition comprising the same. The sulfonamide compound is effective for the diseases treatable based on their blood sugar level-depressing activity, cGMP-PDE (especially PDE-V)-inhibiting activity, smooth muscle relaxing activity, bronchodilating activity, vasodilating activity, smooth muscle cell suppressing activity, and antiallergic activity.
摘要翻译：式（I）的磺酰胺化合物：其中R1是烷基，烯基，炔基等; A是任选取代的杂多环基团，除了苯并咪唑基，吲哚基，4,7-二氢苯并咪唑基和2,3-二氢苯并恶嗪基; X是亚烷基，氧杂，氧杂（低级）亚烷基等; 并且R 2是任选取代的芳基，取代的联苯基等，其盐和包含它们的药物组合物。磺胺类化合物可以基于其血糖降低活性，cGMP-PDE（特别是PDE-V）抑制活性，平滑肌松弛活性，支气管扩张活性，血管舒张活性，平滑肌细胞抑制活性，以及抗过敏活性。

9. 发明授权

US06242474B1 Aromatic ring derivatives 失效
标题翻译：芳香环衍生物
公开(公告)号：US06242474B1
公开(公告)日：2001-06-05
申请号：US09446619
申请日：2000-03-21
申请人： Noritsugu Yamasaki , Takafumi Imoto , Takahiro Hiramura , Osamu Onomura , Masahiro Nishikawa , Hiroshi Kayakiri , Yoshito Abe , Hitoshi Hamashima , Hitoshi Sawada
发明人： Noritsugu Yamasaki , Takafumi Imoto , Takahiro Hiramura , Osamu Onomura , Masahiro Nishikawa , Hiroshi Kayakiri , Yoshito Abe , Hitoshi Hamashima , Hitoshi Sawada
IPC分类号： A61K314164
CPC分类号： C07D213/78 , C07C311/51 , C07D213/81 , C07D233/64 , C07D233/68 , C07D409/06
摘要： Novel aromatic ring derivatives represented by formula (I) or their pharmaceutical acceptable salts are provided. wherein Nu represents a 5- or 6-membered aromatic ring; ch1 and ch2 each represents a cross-linking group; and A represents an aromatic ring. These compounds have blood sugar-depressing activity or PDE 5 inhibitory activity and are useful as medicines for treating impaired glucose tolerance, diabetes, diabetic complications, syndrome of insulin-resistance, polycystic ovary syndrome, hyperlipidemia, atherosclerosis, cardiovascular disorders, hyperglycemia, hypertension, stenocardia, pulmonary hypertension, congestive heart failure, glomerulopathy, tubulointerstitial disorders, renal failure, angiostenosis, distal angiopathy, cerebral apoplexy, chronic reversible obstructions, autoimmune diseases, allergic rhinitis, urticaria, glaucoma, diseases characterized by enteromotility disorders, impotence, nephritis, cachexia, pancreatitis, restenosis after PTCA, etc.
摘要翻译：提供由式（I）表示的新颖芳环衍生物或其药学上可接受的盐。其中Nu表示5-或6-元芳环; ch1和ch2各自表示交联基团; 并且A代表芳香环。这些化合物具有抑制血糖的活性或PDE 5抑制活性，可用作治疗糖耐量异常，糖尿病，糖尿病并发症，胰岛素抵抗综合征，多囊卵巢综合症，高脂血症，动脉粥样硬化，心血管疾病，高血糖症，高血压，心律失常，肺动脉高压，充血性心力衰竭，肾小球病，肾小管间质性疾病，肾衰竭，血管狭窄，远端血管病，脑中风，慢性可逆障碍，自身免疫性疾病，过敏性鼻炎，荨麻疹，青光眼，以肠蠕动为特征的疾病疾病，阳ence，肾炎，恶病质，胰腺炎，PTCA后再狭窄等。

10. 发明授权

US5962692A 2-isoxazoline derivative and process for producing the same, and process for producing related derivatives from the same 失效
标题翻译： 2-异恶唑啉衍生物及其制备方法，以及由其制备相关衍生物的方法
公开(公告)号：US5962692A
公开(公告)日：1999-10-05
申请号：US976482
申请日：1997-11-24
申请人： Yoichiro Ueda , Osamu Onomura
发明人： Yoichiro Ueda , Osamu Onomura
IPC分类号： C07C213/00 , C07C213/10 , C07C215/28 , C07C269/06 , C07C273/18 , C07D261/04
CPC分类号： C07C269/06 , C07C213/00 , C07C213/10 , C07C273/1854 , C07D261/04
摘要： The present invention provides useful intermediates for the synthesis of 2,5-diamino-1,6-diphenyl-3-hydroxyhexane derivatives which serve as intermediates in the synthesis of medicines such as retrovirus protease inhibitors including human immunodeficiency virus (HIV) protease inhibitors, and a method for preparing these intermediates using the former intermediates.More particularly, the invention provides methods for preparing a 2-isoxazoline derivative represented by formula �1! and a 2,5-diamino-1,6-diphenyl-3-hydroxyhexane derivative obtainable by reducing the 2-isoxazoline derivative and represented by formula �6!: ##STR1## (wherein Ph is phenyl; and each of R.sup.1 and R.sup.2 independently represents hydrogen, acyl, alkyloxycarbonyl, arylalkyloxycarbonyl, aryloxycarbonyl, alkylaminocarbonyl, arylalkylaminocarbonyl, arylaminocarbonyl, alkyl, arylalkyl, aryl, alkylsulfonyl, arylalkylsulfonyl, or arylsulfonyl, or R.sup.1 and R.sup.2 are linked to each other to represent divalent acyl).
摘要翻译：本发明提供了用于合成作为药物合成中间体的2,5-二氨基-1,6-二苯基-3-羟基己烷衍生物的有用的中间体，所述药物例如包括人免疫缺陷病毒（HIV）蛋白酶抑制剂的逆转录病毒蛋白酶抑制剂，以及使用前述中间体制备这些中间体的方法。更具体地说，本发明提供了制备由式[1]表示的2-异恶唑啉衍生物和通过还原2-异恶唑啉衍生物而得到的2,5-二氨基-1,6-二苯基-3-羟基己烷衍生物的方法， [6]：（其中Ph为苯基; R 1和R 2各自独立地表示氢，酰基，烷氧基羰基，芳基烷氧基羰基，芳氧基羰基，烷基氨基羰基，芳基烷基氨基羰基，芳基氨基羰基，烷基，芳基烷基，芳基，烷基磺酰基，芳基烷基磺酰基或芳基磺酰基， R2彼此连接以表示二价酰基）。

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