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1. 发明申请

US20060293641A1 Housing body for deglutition of solid molding for oral ingestion, container for the housing body, and deglutition method 审中-公开
标题翻译：用于口腔摄入的固体成型用于脱脂的壳体，用于壳体的容器和脱脂方法
公开(公告)号：US20060293641A1
公开(公告)日：2006-12-28
申请号：US10556592
申请日：2004-05-14
申请人： Fuyuhiko Nishijima , Saichi Ono , Tadahiko Chiba , Yukio Iwase , Yoshiaki Osaka , Koichi Niimura
发明人： Fuyuhiko Nishijima , Saichi Ono , Tadahiko Chiba , Yukio Iwase , Yoshiaki Osaka , Koichi Niimura
IPC分类号： A61M31/00
CPC分类号： A61J7/0038 , A47G21/183
摘要： A housing body (10) for deglutition of a shaped solid (5) for oral ingestion which is stored therein, comprising a generally tubular water-resistant envelope (1); an opening-side end part (A) at one end of the envelope, having an unsealable structure part (2), and capable of forming an opening part (22) by removing the unsealable structure part; a shielding-side end part (B) at the other end of the envelope, having a means for preventing the shaped solid for oral ingestion from release, the means allowing liquid to pass therethrough but not allowing the shaped solid for oral ingestion to pass therethrough; and a storage chamber (6) storing the shaped solid for oral ingestion between the opening-side end part and the shielding-side end part is disclosed. A method for swallowing a shaped solid for oral ingestion, wherein an unsealable structure part installed at an opening-side end part of the housing body is removed; the shielding-side end part of the housing body is immersed into liquid in a vessel while the shaped solid for oral ingestion is stored in the storage chamber in the tubular envelope; and an opening part formed at the opening-side end part is held between the lips so that the shaped solid for oral ingestion is sucked in together with the liquid in the vessel is also disclosed.
摘要翻译：一种用于口腔成形固体（5）脱水的壳体（10），其用于口腔摄取，其存储在其中，包括大致管状的防水外壳（1）; 在封套的一端处的开口侧端部（A），具有可开封结构部分（2），并且能够通过移除开封结构部分形成开口部分（22）; 在封套的另一端处的屏蔽侧端部（B）具有用于防止成形固体口服摄取的装置，允许液体通过但不允许用于口服摄取的成形固体通过的装置 ; 公开了一种在开口侧端部和屏蔽侧端部之间存储用于口腔摄取的成形固体的储存室（6）。一种吞咽用于口服摄取的成形固体的方法，其中移除安装在所述壳体的开口侧端部的开封结构部分; 将壳体的屏蔽侧端部浸入容器中的液体中，同时将用于口腔摄取的成形固体储存在管状外壳中的储存室中; 并且形成在开口侧端部处的开口部分保持在唇缘之间，使得用于口服摄取的成形固体与容器中的液体一起被吸入。

2. 发明授权

US5736522A Esculetin derivatives and method for manufacture thereof, use thereof, and pharmaceutical composition 失效
标题翻译： Esculetin衍生物及其制备方法，其用途和药物组合物
公开(公告)号：US5736522A
公开(公告)日：1998-04-07
申请号：US340421
申请日：1994-11-15
申请人： Koju Watanabe , Koichi Niimura , Junko Miyagawa
发明人： Koju Watanabe , Koichi Niimura , Junko Miyagawa
IPC分类号： A61K31/70 , A61K31/7042 , A61K31/7048 , A61P29/00 , A61P43/00 , C07H17/075 , C07H1/00 , C07H15/00
CPC分类号： C07H17/075 , Y02P20/55
摘要： A compound of the formula (I): ##STR1## wherein R.sup.1 and R.sup.2 are, independently, a hydrogen atom, a monosaccharide residue, a protected monosaccharide residue, or a protecting group for hydroxyl group, but at least one of R.sup.1 and R.sup.2 is a monosaccharide residue or a protected monosaccharide residue, and R.sup.3 is a hydrogen atom, a hydroxyl group, an alkyl group, an aryl group, or an aralkyl group, with the proviso that (1) when R.sup.1 and R.sup.2 are glucose residues at the same time, R.sup.3 is not a hydrogen atom, (2) when R.sup.1 is a hydrogen atom, an acetyl group or a benzyl group and R.sup.2 is a glucose residue, an acetylated glucose residue, or acetalized glucose residue, R.sup.3 is not a hydrogen atom, or (3) when R.sup.1 is a glucose residue and R.sup.2 is a hydrogen atom, R.sup.3 is not a hydrogen atom or a salt thereof is disclosed.
摘要翻译：式（I）的化合物：其中R 1和R 2独立地为氢原子，单糖残基，被保护的单糖残基或羟基的保护基，但R 1和R 2中的至少一个为且R2为单糖残基或被保护的单糖残基，R3为氢原子，羟基，烷基，芳基或芳烷基，条件是（1）R1和R2为葡萄糖残基时同时，R3不是氢原子，（2）当R1是氢原子，乙酰基或苄基，R2是葡萄糖残基，乙酰化葡萄糖残基或缩醛化葡萄糖残基时，R3不是氢原子，或（3）当R1是葡萄糖残基且R2是氢原子时，R3不是氢原子或其盐。

3. 发明授权

US5731293A Esculetin derivatives, method for manufacture thereof, and pharmaceutical composition 失效
标题翻译： Esculetin衍生物，其制备方法和药物组合物
公开(公告)号：US5731293A
公开(公告)日：1998-03-24
申请号：US580364
申请日：1995-12-28
申请人： Koju Watanabe , Koichi Niimura , Toru Yamazaki , Hiroshi Maruoka
发明人： Koju Watanabe , Koichi Niimura , Toru Yamazaki , Hiroshi Maruoka
IPC分类号： C12N9/99 , A61K31/365 , A61K31/535 , A61K31/70 , A61K31/7042 , A61K31/7048 , A61P1/02 , A61P11/00 , A61P13/02 , A61P15/00 , A61P17/00 , A61P27/02 , A61P29/00 , A61P43/00 , C07D311/16 , C07H1/00 , C07H17/075 , A61K31/35 , C07D313/06 , C07H15/24
CPC分类号： C07H17/075 , C07D311/16
摘要： A compound of the formula (I): ##STR1## wherein R.sup.1 and R.sup.2 are, independently, --CON(R.sup.4)R.sup.5, or a monosaccharide, or acylated monosaccharide group, with the proviso that at least one of R.sup.1 and R.sup.2 is --CON(R.sup.4)R.sup.5, and R.sup.4 and R.sup.5 are, independently, a hydrogen atom, or a hydroxyl, alkyl, aryl, or aralkyl group, or R.sup.4 and R.sup.5 together with the nitrogen atom attached thereto form a 3- to 7-membered saturated cycloaliphatic amino group, and R.sup.3 is a hydrogen atom, or a hydroxyl, alkyl, aryl, aralkyl, or --COOR.sup.8 group, and R.sup.3 is at 3- or 4-position, and R.sup.8 is a hydrogen atom or an alkyl group, or a salt thereof is disclosed. The compound has a function to inhibit a matrix metalloproteinase.
摘要翻译：式（I）的化合物：其中R 1和R 2独立地为-CON（R 4）R 5，或单糖或酰化单糖基团，条件是R 1和R 2中的至少一个是-CON（R4）R5，R4和R5独立地是氢原子或羟基，烷基，芳基或芳烷基，或R4和R5与连接的氮原子一起形成3-至7- R 3为氢原子或羟基，烷基，芳基，芳烷基或-COOR 8基，R 3为3-或4-位，R 8为氢原子或烷基，或其盐。该化合物具有抑制基质金属蛋白酶的功能。

4. 发明授权

US5561125A Estradiol derivative and growth inhibiting composition thereof 失效
标题翻译：雌二醇衍生物及其生长抑制组合物
公开(公告)号：US5561125A
公开(公告)日：1996-10-01
申请号：US408381
申请日：1995-03-22
申请人： Koichi Niimura , Takako Kawabe , Tsutomu Wada , Tsuyoshi Saitoh , Kenji Bannai
发明人： Koichi Niimura , Takako Kawabe , Tsutomu Wada , Tsuyoshi Saitoh , Kenji Bannai
IPC分类号： A61K31/565 , A61P35/00 , C07J1/00 , C07J41/00
CPC分类号： C07J41/0072 , C07J1/0077
摘要： Estradiol derivatives of the formula: ##STR1## wherein R.sup.1 is C.sub.1-4 alky or C.sub.1-4 alkoxy; R.sup.2 is acyl or benzyl; m is an integer of 1 to 3; n is an integer of 1 to 3; and X is hydroxy or halogen are useful as tumor growth inhibiting agents.
摘要翻译：下式的雌二醇衍生物：其中R 1是C 1-4烷基或C 1-4烷氧基; R2是酰基或苄基; m为1〜3的整数。 n为1〜3的整数。 X是羟基或卤素可用作肿瘤生长抑制剂。

5. 发明授权

US5480878A Method for treating prostatic hypertrophy with estradiol derivatives 失效
标题翻译：用雌二醇衍生物治疗前列腺肥大的方法
公开(公告)号：US5480878A
公开(公告)日：1996-01-02
申请号：US408389
申请日：1995-03-22
申请人： Koichi Niimura , Takako Kawabe , Tsutomu Wada , Tsuyoshi Saitoh , Kenji Bannai
发明人： Koichi Niimura , Takako Kawabe , Tsutomu Wada , Tsuyoshi Saitoh , Kenji Bannai
IPC分类号： A61K31/565 , A61P35/00 , C07J1/00 , C07J41/00
CPC分类号： C07J41/0072 , C07J1/0077
摘要： Disclosed is a method for treating prostatic hypertrophy with an estradiol derivative-alkylating agent conjugate of the formula (1'): ##STR1## wherein R.sup.1 is C.sub.1-4 alkyl or C.sub.1-4 alkoxy; R.sup.2 is acyl or benzyl; m is an integer of 1 to 3; and n is an integer of 0 to 3. Also disclosed is the treatment of prostatic hypertrophy with an estradiol derivative of the formula (II): ##STR2## wherein R.sup.1 is C.sub.1-4 alkyl or C.sub.1-4 alkoxy; R.sup.2 is acyl or benzyl; m is an integer of 1 to 3; and n is an integer of 0 to 3; and X is hydroxy or halogen.
摘要翻译：公开了一种用式（1'）的雌二醇衍生物 - 烷化剂缀合物治疗前列腺肥大的方法：其中R 1是C 1-4烷基或C 1-4烷氧基; R2为酰基或苄基; m为1〜3的整数。并且n是0至3的整数。还公开了用式（II）的雌二醇衍生物治疗前列腺肥大：其中R 1是C 1-4烷基或C 1-4烷氧基; R2是酰基或苄基; m为1〜3的整数。 n为0〜3的整数。 X是羟基或卤素。

6. 发明授权

US5726196A Aromatase-inhibiting composition containing azole derivative 失效
标题翻译：含有唑衍生物的芳香酶抑制组合物
公开(公告)号：US5726196A
公开(公告)日：1998-03-10
申请号：US623914
申请日：1996-03-28
申请人： Koichi Niimura , Akira Kato , Junko Miyagawa , Yuko Ikeda
发明人： Koichi Niimura , Akira Kato , Junko Miyagawa , Yuko Ikeda
IPC分类号： C07D249/08 , A61K31/41 , A61K31/415 , A61K31/4164 , A61K31/4174 , A61K31/4178 , A61K31/4196 , A61P13/02 , A61P15/00 , A61P35/00 , A61P43/00 , C07D233/56 , C07D233/60 , C07D405/06 , C07D521/00
CPC分类号： C07D231/12 , A61K31/41 , A61K31/415 , A61K31/4164 , A61K31/4174 , A61K31/4178 , A61K31/4196 , C07D233/56 , C07D249/08
摘要： The disclosure describes a pharmaceutical composition comprising an aromatase-inhibiting effective amount of a compound selected from the group consisting of compounds of the formula (I): ##STR1## including their stereoisomers and salts thereof, wherein R.sup.1 is halogen or phenyl; m is 0, 1, 2 or 3; k and n each are independently 0, 1 or 2; R.sup.2 and R.sup.3 each are independently H or OH; R.sup.6 and R.sup.7 each are independently H or C.sub.1-4 alkyl; R.sup.8 and R.sup.9 each are H or R.sup.8 and R.sup.9 form --C(R.sup.4) (R.sup.5)--C(R.sup.11) (R12)-- bond wherein R.sup.4, R.sup.5, R.sup.11 and R.sup.12 each are independently H or C.sub.1-4 alkyl; Y is N or CH; and R.sup.10 is H or halogen, or R.sup.10 combines with R.sup.2 to form --O-- bond, with proviso that if R.sup.8 and R.sup.9 form --C (R.sup.4) (R.sup.5)--C(R.sup.11) (R.sup.12)-- bond R.sup.3, R.sup.6 and R.sup.7 each are H, and k and n each are 1, then R.sup.2 and R.sup.10 form --O-- bond, and a pharmaceutically acceptable carrier or diluent.
摘要翻译：本公开描述了一种药物组合物，其包含芳香酶抑制有效量的选自式（I）的化合物的化合物：包括其立体异构体和盐的其中R 1是卤素或苯基; m为0,1,2或3; k和n各自独立地为0,1或2; R2和R3各自独立地为H或OH; R6和R7各自独立地为H或C1-4烷基; R8和R9各自为H或R8，R9为-C（R4）（R5）-C（R11）（R12） - 键，其中R4，R5，R11和R12各自独立地为H或C1-4烷基; Y为N或CH; R 10为H或卤素，或R 10与R 2结合形成-O-键，条件是如果R 8和R 9形成-C（R 4）（R 5）-C（R 11）（R 12） - 键R 3，R 6和R 7 各自为H，并且k和n各自为1，则R 2和R 10形成-O-键，以及药学上可接受的载体或稀释剂。

7. 发明授权

US5633393A Estradiol derivative-alkylating agent conjugate with reduced hormonal activity, process for preparing the same, compounds useful for the preparation thereof, and growth inhibiting compositon containing the conjugate or estradiol derivative. 失效
标题翻译：具有降低的激素活性的雌二醇衍生物 - 烷化剂，其制备方法，可用于其制备的化合物和含有缀合物或雌二醇衍生物的生长抑制性组合物。
公开(公告)号：US5633393A
公开(公告)日：1997-05-27
申请号：US692154
申请日：1996-08-05
申请人： Koichi Niimura , Takako Kawabe , Tsutomu Wada , Tsuyoshi Saitoh , Kenji Bannai
发明人： Koichi Niimura , Takako Kawabe , Tsutomu Wada , Tsuyoshi Saitoh , Kenji Bannai
IPC分类号： A61K31/565 , A61P35/00 , C07J1/00 , C07J41/00 , C07J75/00
CPC分类号： C07J41/0072 , C07J1/0077
摘要： Conjugates of the formula ##STR1## are prepared by reacting an estradiol derivative with a compound of the formula: ##STR2## in the presence of thionyl chloride or a metal hydride at -30.degree. to 150.degree. C. for 3 minutes to 48 hours and then recovering and purifying the product.
摘要翻译：通过在-30℃〜150℃下，在亚硫酰氯或金属氢化物的存在下使雌二醇衍生物与下式化合物反应来制备式（I）的缀合物： 3分钟至48小时，然后回收和纯化产物。

8. 发明授权

US5633356A 3-deoxyglucosone derivatives 失效
标题翻译： 3-脱氧葡萄糖醛衍生物
公开(公告)号：US5633356A
公开(公告)日：1997-05-27
申请号：US314687
申请日：1994-09-29
申请人： Toshimitsu Niwa , Koichi Niimura , Minoru Ohara , Sigemi Tomiyama
发明人： Toshimitsu Niwa , Koichi Niimura , Minoru Ohara , Sigemi Tomiyama
IPC分类号： G01N33/60 , C07H23/00 , G01N1/28 , G01N30/72 , G01N33/64 , G01N33/66 , C07H3/00 , C07H3/02
CPC分类号： G01N33/60 , G01N1/28 , G01N33/64 , G01N33/66 , G01N2001/2893 , G01N30/7206 , Y10T436/10 , Y10T436/104998 , Y10T436/13 , Y10T436/143333 , Y10T436/144444 , Y10T436/200833 , Y10T436/24 , Y10T436/25 , Y10T436/25375
摘要： For determining 3-deoxyglucosone derivatives which are intermediate metabolites of the Maillard reaction in body fluids such as blood, urine, serum, plasma and the like in gas chromatography/mass spectrometry, .sup.13 C-labelled compounds or .sup.14 C-labelled compounds are useful as an internal standard substance. More specifically, 3-deoxyglucosone derivatives having the formula (I): ##STR1## wherein *C is .sup.13 C or .sup.14 C, X is O or N--OR wherein R is Me, Et or H, and Y is SiMe.sub.3 or SiMe.sub.2 tBu, and their production are provided. The measurement of 3-deoxyglucosone derivatives is useful in diagnosing diseases such as diabetes and diseases complicated with diabetes, including diabetic nephrosis, various renal disorders, renal insufficiency, metabolic diseases of carbohydrate and the like.
摘要翻译：为了测定作为气相色谱/质谱法中体液如血液，尿液，血清，血浆等的美拉德反应的中间代谢物的3-脱氧葡萄糖苷衍生物，13C标记的化合物或14C标记的化合物可用作内部标准物质。更具体地，具有式（I）的3-脱氧葡萄糖醛衍生物：其中* C为13C或14C，X为O或N-OR，其中R为Me，Et或H，Y为SiMe3或SiMe2tBu ，并提供其生产。 3-脱氧葡萄糖苷衍生物的测定可用于诊断糖尿病和糖尿病并发糖尿病等疾病，包括糖尿病肾病，各种肾功能衰竭，肾功能不全，糖类代谢疾病等。

9. 发明授权

US5618734A Method for measuring 3-deoxyglucosone derivatives in a sample 失效
标题翻译：测定样品中3-脱氧葡萄糖醛衍生物的方法
公开(公告)号：US5618734A
公开(公告)日：1997-04-08
申请号：US406704
申请日：1995-03-20
申请人： Toshimitsu Niwa , Koichi Niimura , Minoru Ohara , Sigemi Tomiyama
发明人： Toshimitsu Niwa , Koichi Niimura , Minoru Ohara , Sigemi Tomiyama
IPC分类号： G01N33/60 , C07H23/00 , G01N1/28 , G01N30/72 , G01N33/64 , G01N33/66 , G01N30/06 , G01N30/14
CPC分类号： G01N33/60 , G01N1/28 , G01N33/64 , G01N33/66 , G01N2001/2893 , G01N30/7206 , Y10T436/10 , Y10T436/104998 , Y10T436/13 , Y10T436/143333 , Y10T436/144444 , Y10T436/200833 , Y10T436/24 , Y10T436/25 , Y10T436/25375
摘要： For determining 3-deoxyglucosone derivatives which are intermediate metabolites of the Maillard reaction in body fluids such as blood, urine, serum, plasma and the like in gas chromatography/mass spectrometry, .sup.13 C-labelled compounds or .sup.14 C-labelled compounds are useful as an internal standard substance. More specifically, 3-deoxyglucosone derivatives having the formula (I): ##STR1## wherein *C is .sup.13 C or .sup.14 C, X is O or N--OR wherein R is Me, Et or H, and Y is SiMe.sub.3 or SiMe.sub.2 tBu, and their production are provided. The measurement of 3-deoxyglucosone derivatives is useful in diagnosing diseases such as diabetes and diseases complicated with diabetes, including diabetic nephrosis, various renal disorders, renal insufficiency, metabolic diseases of carbohydrate and the like.
摘要翻译：为了测定作为气相色谱/质谱法中体液如血液，尿液，血清，血浆等的美拉德反应的中间代谢物的3-脱氧葡萄糖苷衍生物，13C标记的化合物或14C标记的化合物可用作内部标准物质。更具体地，具有式（I）的3-脱氧葡萄糖醛衍生物：其中* C为13C或14C，X为O或N-OR，其中R为Me，Et或H，Y为SiMe3或SiMe2tBu ，并提供其生产。 3-脱氧葡萄糖苷衍生物的测定可用于诊断糖尿病和糖尿病并发糖尿病等疾病，包括糖尿病肾病，各种肾功能衰竭，肾功能不全，糖类代谢疾病等。

10. 发明授权

US5508298A Azole derivative and pharmaceutical composition 失效
标题翻译：唑衍生物和药物组合物
公开(公告)号：US5508298A
公开(公告)日：1996-04-16
申请号：US444027
申请日：1995-05-18
申请人： Koichi Niimura , Takao Ando , Toyohiko Nitta , Yuko Ikeda
发明人： Koichi Niimura , Takao Ando , Toyohiko Nitta , Yuko Ikeda
IPC分类号： C07C45/62 , C07C45/68 , C07C49/657 , C07C49/683 , C07C49/697 , C07C49/747 , C07C255/56 , C07D233/60 , C07D249/08 , C07D303/04 , C07D303/08 , C07D303/14 , C07D303/46 , C07D521/00 , A61K31/41
CPC分类号： C07D231/12 , C07C255/56 , C07C45/62 , C07C45/68 , C07C49/657 , C07C49/683 , C07C49/697 , C07C49/747 , C07D233/56 , C07D249/08 , C07D303/04 , C07D303/08 , C07D303/14 , C07D303/46 , C07C2101/14 , C07C2101/16
摘要： A novel azole derivative of the general formula (I): ##STR1## wherein R.sub.1 and R.sub.2 are, independently from each other, a hydrogen atom or an alkyl group having 1 to 4 carbon atoms, x.sub.1 and x.sub.2 are, independently from each other, a hydrogen or halogen atom, or hydroxyl, cyano, or trifluoromethyl group, and Y is CH or a nitrogen atom, a process for the production thereof, and a pharmaceutical composition containing the same as the active ingredient.
摘要翻译：通式（I）的新型唑衍生物：其中R 1和R 2彼此独立地为氢原子或具有1至4个碳原子的烷基，其中x 1和x 2独立地为氢或卤素原子，或羟基，氰基或三氟甲基，Y为CH或氮原子，其制备方法和含有该活性成分的药物组合物。

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