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1. 发明授权

US5728841A Process for preparing 1-amino-1,2,3-triazole 失效
标题翻译： 1-氨基-1,2,3-三唑的制备方法
公开(公告)号：US5728841A
公开(公告)日：1998-03-17
申请号：US637718
申请日：1996-04-30
申请人： Kazuhiko Shigeno , Tomoyasu Ono , Motoaki Tanaka , Shozo Yamada , Tetsuji Asao
发明人： Kazuhiko Shigeno , Tomoyasu Ono , Motoaki Tanaka , Shozo Yamada , Tetsuji Asao
IPC分类号： C07D249/04
CPC分类号： C07D249/04
摘要： This invention is to provide a process for preparing 1-amino-1,2,3-triazole represented by formula (III): ##STR1## comprising cyclizing glyoxal bishydrazone represented by formula (I): ##STR2## by reaction with an aqueous hydrogen peroxide solution in the presence of a catalytic amount of a transition metal oxide represented by formula (II): M.sub.m O.sub.n wherein M represents a transition metal atom; and m and n, which may be the same or different, each represent an integer of 1 to 5.
摘要翻译： PCT No.PCT / JP95 / 01727 Sec。 371日期：1996年04月30日 102（e）日期1996年4月30日PCT提交1995年8月30日PCT公布。出版物WO96 / 06835 日本特开1996年3月7日本发明提供一种制备由式（III）表示的1-氨基-1,2,3-三唑的方法：包含使由式（I）表示的乙二醛双腙环化：在催化量的由式（II）表示的过渡金属氧化物存在下，过氧化物溶液：MmOn其中M表示过渡金属原子; m和n可相同或不同，分别表示1〜5的整数。

2. 发明授权

US06818764B2 Process for preparing substance GM-95 失效
标题翻译：制造物质GM-95的方法
公开(公告)号：US06818764B2
公开(公告)日：2004-11-16
申请号：US10433500
申请日：2003-06-03
申请人： Shozo Yamada , Kazuhiko Shigeno , Kazuhiro Kitagawa , Shigeo Okajima , Tetsuji Asao
发明人： Shozo Yamada , Kazuhiko Shigeno , Kazuhiro Kitagawa , Shigeo Okajima , Tetsuji Asao
IPC分类号： C07D51322
CPC分类号： C07D498/22 , C07D513/22 , Y02P20/55
摘要： A method of manufacturing substance GM-95 having general formula [I], comprising (a) deprotecting a macrocyclic compound having general formula [II] (wherein, R1's are the same or different and each represents a lower alkyl group, and R2 represents a thiol protecting group) by removing acetal protecting groups (the R1's) thereof, and forming an oxazole ring through an intramolecular cyclization reaction between produced formyl group and an amide group, and (b) deprotecting a resulting macrocyclic compound having general formula [III] (wherein, R2 is as mentioned above) by removing the thiol protecting group (R2) thereof, and forming a thiazoline ring through an intramolecular cyclization reaction between a thiol group thus produced and an amide group.
摘要翻译：制备具有通式[I]的物质GM-95的方法，包括（a）使通式[II]的大环化合物脱保护（其中，R 1相同或不同，各自表示低级烷基，R 2表示硫醇保护基），除去缩醛保护基（R 1），通过产生的甲酰基和酰胺基之间的分子内环化反应形成恶唑环，（b ）通过除去其中的硫醇保护基（R 2），使所得的具有通式[III]（其中R 2如上所述）的大环化合物脱保护，并通过分子内环化反应形成噻唑啉环由此产生的硫醇基团和酰胺基团。

3. 发明授权

US6110967A Epoxysuccinamide derivative or salt thereof 失效
标题翻译：环氧琥珀酰胺衍生物或其盐
公开(公告)号：US6110967A
公开(公告)日：2000-08-29
申请号：US202607
申请日：1998-12-17
申请人： Tetsuji Asao , Tomohiro Yamashita , Yoshimitsu Suda , Shigeo Okajima , Yukio Tada , Nobuhiko Katsunuma , Shozo Yamada , Kazuhiko Shigeno , Atsuhiko Uemura
发明人： Tetsuji Asao , Tomohiro Yamashita , Yoshimitsu Suda , Shigeo Okajima , Yukio Tada , Nobuhiko Katsunuma , Shozo Yamada , Kazuhiko Shigeno , Atsuhiko Uemura
IPC分类号： C07D303/40 , C07D303/48 , A61K31/495 , A61K31/41 , A61K31/435
CPC分类号： C07D303/48
摘要： The invention relates an epoxysuccinamide derivative represented by a formula (I): ##STR1## wherein R.sup.1 represents a hydrogen atom, an alkyl or aminoalkyl group, R.sup.2 represents an aminoalkyl group which May be substituted, an aryl group which may be substituted, a heterocyclic group which may be substituted, an aralkyl group which may be substituted, or an alkyl group substituted by a heterocyclic ring which may be substituted, or R.sup.1 and R.sup.2 may form a nitrogen-containing heterocyclic ring, which may be substituted, together with the adjacent nitrogen atoms, and R.sup.3 and R.sup.4 are the same or different from each other and independently represent a hydrogen atom, or an alkyl or aralkyl group, or a salt thereof, a preparation process thereof, and a medicine comprising such a derivative or salt as an active ingredient. This compound has a specific inhibitory activity for cathepsin L and family enzymes thereof, and is useful as an agent for preventing and treating metabolic osteopathy such as osteoporosis and hypercalcemia.
摘要翻译： PCT No.PCT / JP98 / 01778 Sec。 371日期1998年12月17日第 102（e）1998年12月17日日期PCT提交1998年4月17日PCT公布。第WO98 / 47887号公报日期：1998年10月29日本发明涉及由式（I）表示的环氧琥珀酰胺衍生物：其中R1表示氢原子，烷基或氨基烷基，R2表示可以被取代的氨基烷基，可以被取代的芳基，可以被取代的杂环基，可以被取代的芳烷基或被可被取代的杂环取代的烷基，或者可以被R 1和R 2形成可以被取代的含氮杂环，和相邻的氮原子和R3和R4彼此相同或不同，并且独立地表示氢原子或烷基或芳烷基或其盐，其制备方法和包含这种衍生物或盐的药物作为活性成分。该化合物对组织蛋白酶L及其家族酶具有特异性抑制活性，可用作预防和治疗代谢性骨病如骨质疏松症和高钙血症的药剂。

4. 发明申请

US20110319413A1 PIPERAZINE COMPOUND CAPABLE OF INHIBITING PROSTAGLANDIN D SYNTHASE 有权
标题翻译： PIPERAZINE化合物可抑制PROSTAGLANDIN D合成酶
公开(公告)号：US20110319413A1
公开(公告)日：2011-12-29
申请号：US13255134
申请日：2010-03-08
申请人： Yoshihiro Urade , Makoto Kitade , Kazuhiko Shigeno , Keiko Yamane , Katsunao Tanaka
发明人： Yoshihiro Urade , Makoto Kitade , Kazuhiko Shigeno , Keiko Yamane , Katsunao Tanaka
IPC分类号： A61K31/496 , C07D413/14 , A61P21/00 , A61K31/5377 , A61P37/08 , A61P29/00 , C07D401/14 , C07D403/14
CPC分类号： C07D401/14 , A61K31/496 , A61K31/5377 , C07D207/34 , C07D213/81 , C07D277/82 , C07D401/12 , C07D403/12 , C07D403/14 , C07D405/12 , C07D409/12 , C07D413/12 , C07D413/14
摘要： This invention relates to a piperazine compound represented by Formula (I), wherein R1 is C1-6 alkyl; R2 is hydroxy, C1-6 alkyl that may have one or more substituents, —(C═O)—N(R3)(R4), or —(C═O)—OR5; R3 and R4 are the same or different, and each represents hydrogen or C1-6 alkyl that may have one or more substituents, or R3 and R4, taken together with a nitrogen atom to which R3 and R4 are attached, may form a saturated heterocyclic group; R5 is hydrogen or C1-6 alkyl that may have one or more substituents; and n is 1 or 2; or a salt thereof.
摘要翻译：本发明涉及由式（I）表示的哌嗪化合物，其中R 1是C 1-6烷基; R 2是羟基，可具有一个或多个取代基的C 1-6烷基， - （C = O）-N（R 3）（R 4）或 - （C = O） R 3和R 4相同或不同，各自表示氢或可具有一个或多个取代基的C 1-6烷基，或者R 3和R 4与R 3和R 4连接的氮原子一起可以形成饱和杂环组; R5是氢或可具有一个或多个取代基的C 1-6烷基; n为1或2; 或其盐。

5. 发明授权

US6046186A Estrone sulfamate inhibitors of estrone sulfatase, and associated pharmaceutical compositions and methods of use 失效
标题翻译：雌酮硫酸酯酶的氨基磺酸盐抑制剂及其相关药物组合物和使用方法
公开(公告)号：US6046186A
公开(公告)日：2000-04-04
申请号：US997416
申请日：1997-12-24
申请人： Masato Tanabe , Richard H. Peters , Wan-Ru Chao , Kazuhiko Shigeno
发明人： Masato Tanabe , Richard H. Peters , Wan-Ru Chao , Kazuhiko Shigeno
IPC分类号： A61K31/565 , A61K31/57 , A61K31/575 , A61P35/00 , A61P43/00 , C07J41/00 , A61K31/56 , A61K31/58 , C07J9/00 , C07J43/00
CPC分类号： C07J41/0072 , C07J41/0005 , C07J41/0094
摘要： Novel compounds useful as inhibitors of estrone sulfatase are provided. The compounds have the structural formula (I) wherein r1 is an optional double bond, R.sup.1 and R.sup.2 are selected from the group consisting of hydrogen and lower alky, or together form a cyclic substituent (II) ##STR1## wherein Q is NH, O or CH.sub.2, and the other various substituents are as defined herein. Pharmaceutical compositions and methods for using the compounds of formula (I) to treat estrogen-dependent disorders are provided as well.
摘要翻译：提供了可用作雌酮硫酸酯酶抑制剂的新型化合物。化合物具有结构式（I），其中r1是任选的双键，R 1和R 2选自氢和低级烷基，或一起形成其中Q是NH，O或CH 2的环状取代基（II）而其它各种取代基如本文所定义。还提供了使用式（I）化合物治疗雌激素依赖性疾病的药物组合物和方法。

6. 发明授权

US08865714B2 Piperazine compound capable of inhibiting prostaglandin D synthase 有权
标题翻译：能够抑制前列腺素D合成酶的哌嗪化合物
公开(公告)号：US08865714B2
公开(公告)日：2014-10-21
申请号：US13255134
申请日：2010-03-08
申请人： Yoshihiro Urade , Makoto Kitade , Kazuhiko Shigeno , Keiko Yamane , Katsunao Tanaka
发明人： Yoshihiro Urade , Makoto Kitade , Kazuhiko Shigeno , Keiko Yamane , Katsunao Tanaka
IPC分类号： A61K31/496 , A61K31/5377 , C07D401/12 , C07D403/14 , C07D413/14 , C07D405/12 , C07D413/12 , C07D409/12 , C07D277/82 , C07D207/34 , C07D401/14 , C07D213/81
CPC分类号： C07D401/14 , A61K31/496 , A61K31/5377 , C07D207/34 , C07D213/81 , C07D277/82 , C07D401/12 , C07D403/12 , C07D403/14 , C07D405/12 , C07D409/12 , C07D413/12 , C07D413/14
摘要： This invention relates to a piperazine compound represented by Formula (I), wherein R1 is C1-6 alkyl; R2 is hydroxy, C1-6 alkyl that may have one or more substituents, —(C═O)—N(R3)(R4), or —(C═O)—OR5; R3 and R4 are the same or different, and each represents hydrogen or C1-6 alkyl that may have one or more substituents, or R3 and R4, taken together with a nitrogen atom to which R3 and R4 are attached, may form a saturated heterocyclic group; R5 is hydrogen or C1-6 alkyl that may have one or more substituents; and n is 1 or 2; or a salt thereof.
摘要翻译：本发明涉及由式（I）表示的哌嗪化合物，其中R 1是C 1-6烷基; R 2是羟基，可具有一个或多个取代基的C 1-6烷基， - （C = O）-N（R 3）（R 4）或 - （C = O） R 3和R 4相同或不同，各自表示氢或可具有一个或多个取代基的C 1-6烷基，或者R 3和R 4与R 3和R 4连接的氮原子一起可以形成饱和杂环组; R5是氢或可具有一个或多个取代基的C 1-6烷基; n为1或2; 或其盐。

7. 发明授权

US08765750B2 Piperazine compound having a PGDS inhibitory effect 有权
标题翻译：具有PGDS抑制作用的哌嗪化合物
公开(公告)号：US08765750B2
公开(公告)日：2014-07-01
申请号：US13522605
申请日：2011-01-19
申请人： Yoshihiro Urade , Makoto Kitade , Kazuhiko Shigeno , Keiko Yamane , Katsunao Tanaka
发明人： Yoshihiro Urade , Makoto Kitade , Kazuhiko Shigeno , Keiko Yamane , Katsunao Tanaka
IPC分类号： A61K31/496 , A61K31/5377 , C07D401/14 , C07D413/14 , C07D403/14
CPC分类号： C07D403/14 , A61K31/496 , A61K31/5377 , C07D211/58 , C07D213/81 , C07D277/82 , C07D401/12 , C07D401/14 , C07D405/12 , C07D409/12 , C07D413/12
摘要： The present invention provides a piperazine compound represented by Formula (I) or a salt thereof, wherein X represents CH or an N atom; R1 represents C1-6 alkyl; R2 represents C1-6 alkyl that may have one or more substituents, C2-6 alkenyl that may have one or more substituents, —(C═O)—N(R3)(R4), or —(C═O)—OR5, R3 and R4 are the same or different, and each represents hydrogen or C1-6 alkyl that may have one or more substituents; or R3 and R4, taken together with a nitrogen atom to which R3 and R4 are attached, may form a saturated heterocyclic group; and R5 represents hydrogen or C1-6 alkyl that may have one or more substituents or aralkyl.
摘要翻译：本发明提供由式（I）表示的哌嗪化合物或其盐，其中X表示CH或N原子; R1表示C1-6烷基; R 2表示可具有一个或多个取代基的C 1-6烷基，可具有一个或多个取代基的C 2-6烯基， - （C = O）-N（R 3）（R 4）或 - （C = O） R 3和R 4相同或不同，各自表示氢或可具有一个或多个取代基的C 1-6烷基; 或者R3和R4与R3和R4连接的氮原子一起形成饱和杂环基; 并且R 5表示氢或可以具有一个或多个取代基或芳烷基的C 1-6烷基。

8. 发明申请

US20120309760A1 PIPERAZINE COMPOUND HAVING A PGDS INHIBITORY EFFECT 有权
标题翻译：具有PGDS抑制作用的哌嗪化合物
公开(公告)号：US20120309760A1
公开(公告)日：2012-12-06
申请号：US13522605
申请日：2011-01-19
申请人： Yoshihiro Urade , Makoto Kitade , Kazuhiko Shigeno , Keiko Yamane , Katsunao Tanaka
发明人： Yoshihiro Urade , Makoto Kitade , Kazuhiko Shigeno , Keiko Yamane , Katsunao Tanaka
IPC分类号： A61K31/496 , A61P29/00 , A61K31/5377 , A61P37/08 , C07D401/14 , C07D413/14
CPC分类号： C07D403/14 , A61K31/496 , A61K31/5377 , C07D211/58 , C07D213/81 , C07D277/82 , C07D401/12 , C07D401/14 , C07D405/12 , C07D409/12 , C07D413/12
摘要： The present invention provides a piperazine compound represented by Formula (I) or a salt thereof, wherein X represents CH or an N atom; R1 represents C1-6 alkyl; R2 represents C1-6 alkyl that may have one or more substituents, C2-6 alkenyl that may have one or more substituents, —(C═O)—N(R3)(R4), or —(C═O)—OR5, R3 and R4 are the same or different, and each represents hydrogen or C1-6 alkyl that may have one or more substituents; or R3 and R4, taken together with a nitrogen atom to which R3 and R4 are attached, may form a saturated heterocyclic group; and R5 represents hydrogen or C1-6 alkyl that may have one or more substituents or aralkyl.
摘要翻译：本发明提供由式（I）表示的哌嗪化合物或其盐，其中X表示CH或N原子; R1表示C1-6烷基; R 2表示可具有一个或多个取代基的C 1-6烷基，可具有一个或多个取代基的C 2-6烯基， - （C = O）-N（R 3）（R 4）或 - （C = O） R 3和R 4相同或不同，各自表示氢或可具有一个或多个取代基的C 1-6烷基; 或者R3和R4与R3和R4连接的氮原子一起形成饱和杂环基; 并且R 5表示氢或可以具有一个或多个取代基或芳烷基的C 1-6烷基。

9. 发明授权

US5861388A Steroid inhibitors of estrone sulfatase and associated pharmaceutical compositions and methods of use 失效
标题翻译：甾体硫酸酯酶的类固醇抑制剂及其相关药物组合物和使用方法
公开(公告)号：US5861388A
公开(公告)日：1999-01-19
申请号：US1601
申请日：1997-12-31
申请人： Masato Tanabe , Richard H. Peters , Wan-Ru Chao , Kazuhiko Shigeno
发明人： Masato Tanabe , Richard H. Peters , Wan-Ru Chao , Kazuhiko Shigeno
IPC分类号： C07J71/00 , A61K31/58
CPC分类号： C07J71/0094
摘要： Novel compounds useful as inhibitors of estrone sulfatase are provided. The compounds have the structural formula (I) ##STR1## wherein X and Y, or Y and Z, form an oxathiazine dioxide ring or a dihydro-oxathiazine dioxide ring, and the other various substituents are as defined herein. Pharmaceutical compositions and methods for using the compounds of formula (I) to treat estrogen-dependent disorders are provided as well.
摘要翻译：提供了可用作雌酮硫酸酯酶抑制剂的新型化合物。化合物具有结构式（I）其中X和Y或Y和Z形成氧噻嗪二氧化物环或二氢 - 噻吩二氧化物环，其它各种取代基如本文所定义。还提供了使用式（I）化合物治疗雌激素依赖性疾病的药物组合物和方法。

10. 发明授权

US5763432A Steriod inhibitors of estrone sulfatase and associated pharmaceutical compositions and methods of use 失效
标题翻译：雌酮硫酸酯酶的Steriod抑制剂及其相关药物组合物和使用方法
公开(公告)号：US5763432A
公开(公告)日：1998-06-09
申请号：US794229
申请日：1997-01-29
申请人： Masato Tanabe , Richard H. Peters , Wan-Ru Chao , Kazuhiko Shigeno
发明人： Masato Tanabe , Richard H. Peters , Wan-Ru Chao , Kazuhiko Shigeno
IPC分类号： C07J71/00 , A61K31/58
CPC分类号： C07J71/0094
摘要： Novel compounds useful as inhibitors of estrone sulfatase are provided. The compounds have the structural formula (I) ##STR1## wherein X and Y, or Y and Z, form an oxathiazine dioxide ring or a dihydro-oxathiazine dioxide ring, and the other various substituents are as defined herein. Pharmaceutical compositions and methods for using the compounds of formula (I) to treat estrogen-dependent disorders are provided as well.
摘要翻译：提供了可用作雌酮硫酸酯酶抑制剂的新型化合物。化合物具有结构式（I）其中X和Y或Y和Z形成氧噻嗪二氧化物环或二氢 - 噻吩二氧化物环，其它各种取代基如本文所定义。还提供了使用式（I）化合物治疗雌激素依赖性疾病的药物组合物和方法。

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