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1. 发明授权

US06994872B2 Monolayer sugar-coated tablet and process for preparation thereof 有权
标题翻译：单层糖衣片及其制备方法
公开(公告)号：US06994872B2
公开(公告)日：2006-02-07
申请号：US09795083
申请日：2001-03-01
申请人： Toshio Takeuchi
发明人： Toshio Takeuchi
IPC分类号： A61K9/36 , A61K9/00 , A61K9/20 , A61K9/28
CPC分类号： A61K9/2826
摘要： This invention relates to a monolayer sugar-coated tablet which is coated with a sugar-coating liquid containing 30–54% by weight of saccharide, 2–10% by weight of polyethylene glycol and 0.2–2% by weight of polyvinylpyrrolidone, and a process for preparing the same.According to the invention, a monolayer sugar-coated tablet and a process for preparation thereof are provided with very great economical advantages that the skill required for conventional sugar-coating processing is unnecessary and furthermore consumption of sugar-coating material can be reduced and the processing time can be shortened.
摘要翻译：本发明涉及一种单层糖衣片剂，其包被含有30-54重量％糖，2-10重量％聚乙二醇和0.2-2重量％聚乙烯吡咯烷酮的糖衣液，以及制备方法

2. 发明授权

US5472962A Benzothiophene derivative 失效
标题翻译：苯并噻吩衍生物
公开(公告)号：US5472962A
公开(公告)日：1995-12-05
申请号：US244049
申请日：1994-05-13
申请人： Naoyuki Koizumi , Shigehiro Takegawa , Shigeki Iwashita , Tomoko Kawachi , Teruaki Matsui , Mamoru Mieda , Hiroo Takahashi , Tomoyuki Saito , Kenyu Shibata
发明人： Naoyuki Koizumi , Shigehiro Takegawa , Shigeki Iwashita , Tomoko Kawachi , Teruaki Matsui , Mamoru Mieda , Hiroo Takahashi , Tomoyuki Saito , Kenyu Shibata
IPC分类号： A61K31/38 , A61K31/381 , A61K31/4025 , A61K31/4433 , A61K31/445 , A61K31/4535 , A61K31/47 , A61K31/4725 , A61P5/32 , A61P13/02 , A61P15/00 , A61P35/00 , C07D333/54 , C07D333/56 , C07D333/58 , C07D333/62 , C07D409/12 , C07D333/64 , C07D409/10
CPC分类号： C07D333/54 , C07D333/56 , C07D333/62
摘要： A benzothiophene derivative represented by the formula ##STR1## or a salt thereof has an excellent antiestrogenic activity, and is useful as a therapeutic agent of breast cancer, endometrial cancer, endometriosis, mastopathy, etc.This compound is characterized in that the 2-position (the substituent R.sup.2) of the benzothiophene nucleus is substituted by a halogen atom; a lower alkyl group; or a cycloalkyl or cycloalkenyl group optionally substituted by a lower alkyl group, a hydroxyl group, acyloxy group or an oxo group.
摘要翻译： PCT No.PCT / JP92 / 01465 Sec。 371日期1994年5月13日 102（e）日期1994年5月13日PCT提交1992年11月11日PCT公布。公开号WO93 / 10113 日本专利公开说明书1日本公报昭和5月27日公开。一种式IMA表示的苯并噻吩衍生物或其盐具有优异的抗雌激素活性，可用作乳腺癌，子宫内膜癌，子宫内膜异位症，乳腺病等的治疗剂。因为苯并噻吩核的2位（取代基R2）被卤素原子取代; 低级烷基; 或任选被低级烷基，羟基，酰氧基或氧代基取代的环烷基或环烯基。

3. 发明授权

US5082844A Pyridazinone derivatives 失效
标题翻译：吡咯烷酮衍生物
公开(公告)号：US5082844A
公开(公告)日：1992-01-21
申请号：US539741
申请日：1990-06-18
申请人： Kikuo Yasuda , Kenyu Shibata , Nobuyoshi Minami , Toshimi Seki , Masafumi Shiraiwa , Tomio Nakao , Katsuhiko Miyasaka , Tsutomu Ishimori , Kotaro Gotanda , Takako Sasaki
发明人： Kikuo Yasuda , Kenyu Shibata , Nobuyoshi Minami , Toshimi Seki , Masafumi Shiraiwa , Tomio Nakao , Katsuhiko Miyasaka , Tsutomu Ishimori , Kotaro Gotanda , Takako Sasaki
IPC分类号： C07D237/04 , C07D401/12 , C07D403/12
CPC分类号： C07D401/12 , C07D237/04 , C07D403/12
摘要： A pyridazinone compound represented by the general formula ##STR1## wherein Ar is ##STR2## in which R.sup.1, R.sup.2 and R.sup.3 may be identical or different, and each represents a hydrogen atom, a lower alkyl group, a trifluoromethyl group, a halogen atom, a cyano group or a nitro group, and R.sup.4 represents a hydrogen atom, a lower alkoxy group, or a lower alkyl group substituted by a lower alkoxy group or a carbamoyl group, and C* is an asymmetric carbon atom, or a salt thereof. This compound is useful for the treatment of diseases of the circulatory system.

4. 发明授权

US4914106A Compositions and methods employing 2-oxa- or -aza-pregnan compounds for inhibiting androgen or supplying progestin in mammals 失效
标题翻译：使用2-氧杂 - 或-aza-孕烷化合物抑制哺乳动物雄激素或供应孕激素的组合物和方法
公开(公告)号：US4914106A
公开(公告)日：1990-04-03
申请号：US228316
申请日：1988-08-04
申请人： Kenyu Shibata , Nobuaki Yamakoshi , Naoyuki Koizumi , Shigehiro Takegawa , Eiichiro Shimazawa , Mamoru Mieda
发明人： Kenyu Shibata , Nobuaki Yamakoshi , Naoyuki Koizumi , Shigehiro Takegawa , Eiichiro Shimazawa , Mamoru Mieda
IPC分类号： C07J73/00
CPC分类号： C07J73/005 , C07J73/003 , C07C2103/16
摘要： A compound represented by the following formula ##STR1## wherein A represents a hydrogen atom or a lower alkanoyl group, Z represents an oxygen atom or the group ##STR2## in which R represents a hydrogen atom or a lower alkyl group, and X represents a halogen atom, the compound being useful for controlling androgen-dependent diseases, particularly for preventing abortion or for contraception.

5. 发明授权

US4695581A 2-(3,5-dialkyl-4-hydroxyphenyl)indole derivatives 失效
标题翻译： 2-（3,5-二烷基-4-羟基苯基）吲哚衍生物
公开(公告)号：US4695581A
公开(公告)日：1987-09-22
申请号：US770773
申请日：1985-08-29
申请人： Yasushi Suzuki , Yukio Hasegawa , Michitaka Sato , Morinobu Saito , Norio Yamamoto , Katsuhiko Miyasaka , Takashi Mikami , Katsuhiko Miyazawa
发明人： Yasushi Suzuki , Yukio Hasegawa , Michitaka Sato , Morinobu Saito , Norio Yamamoto , Katsuhiko Miyasaka , Takashi Mikami , Katsuhiko Miyazawa
IPC分类号： A61K31/40 , A61K31/403 , A61K31/404 , A61P37/08 , A61P43/00 , C07D209/12 , C07D491/04 , C07D491/056
CPC分类号： C07D491/04 , C07D209/12
摘要： A compound represented by the formula ##STR1## wherein R.sub.1 represents a lower alkyl group; each of R.sub.2 and R.sub.3 represents an alkyl group having 1 to 3 carbon atoms; and each of R.sub.4, R.sub.5 and R.sub.6 represents a hydrogen atom, a halogen atom, a lower alkyl group, a lower alkoxy group, a lower alkanoyloxy group, an aralkyloxy group, a lower alkylthio group, a lower haloalkyl group, a hydroxyl group, a cyano group, a nitro group, an amino group, a mono- or di-(lower alkyl or aralkyl)amino group or a group of the formula ##STR2## in which R.sub.7 represents a lower alkylene group having at least 2 carbon atoms, one of R.sub.8 and R.sub.9 represents a hydrogen atom or a lower alkyl group and the other represents a lower alkyl group, and R.sub.10 represents a hydrogen atom or a lower alkyl group; or any two of R.sub.4, R.sub.5 and R.sub.6 which are adjacent to each other, together, represent a lower alkylenedioxy group, and a salt thereof; and a process for production thereof. This compound has 5-lipoxygenase inhibiting activity and is useful as a medicament.
摘要翻译：由式（I）表示的化合物，其中R 1表示低级烷基; R 2和R 3各自表示具有1至3个碳原子的烷基; R4，R5和R6各自表示氢原子，卤素原子，低级烷基，低级烷氧基，低级烷酰氧基，芳烷氧基，低级烷硫基，低级卤代烷基，羟基，氰基，硝基，氨基，单 - 或二 - （低级烷基或芳烷基）氨基或式“IMAGE”的基团，其中R 7表示具有至少2个碳原子的低级亚烷基， R8和R9中的一个表示氢原子或低级烷基，另一个表示低级烷基，R 10表示氢原子或低级烷基; 或彼此相邻的R 4，R 5和R 6中的任何两个一起代表低级亚烷基二氧基及其盐; 及其制造方法。该化合物具有5-脂氧合酶抑制活性，可用作药物。

6. 发明授权

US4018824A 1-Aryloxy-3-aminopropane derivatives 失效
标题翻译： 1-芳氧基-3-氨基丙烷衍生物
公开(公告)号：US4018824A
公开(公告)日：1977-04-19
申请号：US507793
申请日：1974-09-20
申请人： Kunio Tsukamoto , Yasushi Suzuki , Akihiro Izumi , Yoshio Hiramatsu
发明人： Kunio Tsukamoto , Yasushi Suzuki , Akihiro Izumi , Yoshio Hiramatsu
IPC分类号： C07D209/08 , C07C93/06
CPC分类号： C07D209/08
摘要： A process for the preparation of 1-aryloxy-3-aminopropane derivatives and acid addition salts thereof and such products per se, the process comprising ring opening of tertiary azetidinol derivatives. They possess .beta.-adrenegic block activity and an activity of controlling secretion of gastric juice and are therefore useful antiulcerative medicines for peptic ulcer and duodenal ulcer.
摘要翻译：一种制备1-芳氧基-3-氨基丙烷衍生物及其酸加成盐的方法及其制备方法，该方法包括开环三氮杂环丁醇衍生物。它们具有β-adrengic阻滞活性和控制胃液分泌的活性，因此是消化性溃疡和十二指肠溃疡的有用的抗溃疡药物。

7. 发明授权

US3872093A Naphthisoxazolyl alkanoic acids and their derivatives 失效
标题翻译：萘四唑类碱性酸及其衍生物
公开(公告)号：US3872093A
公开(公告)日：1975-03-18
申请号：US22300972
申请日：1972-02-02
申请人： TEIKOKU HORMONE MFG CO LTD
发明人： SUZUKI YASUSHI , ITAYA TOSHIHISA , MINAMI NOBUYOSHI , TARUTANI MASAAKI , MIKI TOKUTARO , MYASAKA KATSUHIKO
IPC分类号： C07D261/20 , C07D263/60 , C07D85/22
CPC分类号： C07D263/60 , C07D261/20
摘要： Naphthisoxazolyl alkanoic acids and their derivatives expressed by the general formula

WHEREIN RING A may be optionally substituted, ring B may have a double bond between the positions of C-4 and C-5, R1 represents a methylene group, and R is a hydroxyl group, a group of the formula -O(M)1/m (wherein M is a base having a valence of 1,2 or 3 and m is the valence of M), an alkoxy group, an amino group, an aminoalkoxy group or an aminoalkyl amino group. These compounds have analgesic, anti-inflammatory and antipyretic properties.
摘要翻译：萘并噻唑基链烷酸及其衍生物由通式为A可以任选取代，环B可以在C-4和C-5的位置之间具有双键，R1表示亚甲基，R是羟基，式-O（M）1 / m的基团（其中M为化合价为1,2或3的基，m为M的化合价），烷氧基，氨基，氨基烷氧基或氨基烷基氨基。这些化合物具有止痛，消炎和解热特性。

8. 发明授权

US3872087A Process for production of 1,3-disubstituted azetidine derivatives 失效
标题翻译：生产1,3-取代的AZETIDINE衍生物的方法
公开(公告)号：US3872087A
公开(公告)日：1975-03-18
申请号：US29837172
申请日：1972-10-17
申请人： TEIKOKU HORMONE MFG CO LTD
发明人： TSUKAMOTO KUNIO , SUZUKI YASUSHI , IZUMI AKIHIRO , HIRAMATSU YOSHIO
IPC分类号： C07D209/08 , C07D25/00
CPC分类号： C07D209/08
摘要： This invention relates to the production of a pharmaceutical intermediate which is a 1,3-disubstituted azetidine derivative expressed by the general formula

WHEREIN Z represents a hydrogen atom or a group

IN WHICH R'' represents a hydrogen atom or an electron-donor group and n is a number of 1 to 3, and R represents an alkyl or aralkyl group.
摘要翻译：本发明涉及药物中间体的制备，该药物中间体是由通式为WHEREIN Z表示氢原子的表示的1,3-二取代的氮杂环丁烷衍生物或其中R'表示氢原子的基团或电子给体基团，n 是1〜3的数，R表示烷基或芳烷基。

9. 发明授权

US3864398A Process for the preparation of acylamino alkanol derivatives 失效
标题翻译：制备酰氨基链烷醇衍生物的方法
公开(公告)号：US3864398A
公开(公告)日：1975-02-04
申请号：US24919672
申请日：1972-05-01
申请人： TEIKOKU HORMONE MFG CO LTD
发明人： SUZUKI YASUSHI , TSUKAMOTO KUNIO
IPC分类号： C07C233/16 , C07C103/38
CPC分类号： C07C233/16 , Y02P20/55
摘要： A novel process for the production of 1-(acylamino-aryloxy)-3amino-propanol derivative having an excellent Beta -adrenergic blocking effect. The process comprises basically reacting a compound of the formula

WHEREIN Z is a hydrogen atom or a protective group bonded to the oxygen atom by an aliphatic ether linkage, and R stands for an alkyl or aralkyl group, with a compound of the formula

WHEREIN Ar stands for a substituted or unsubstituted benzene or naphthalene ring, Ac indicates an organic acid residue, and Y represents a hydrogen atom, a monovalent hydrocarbon radical having up to 12 carbon atoms or an organic acid residue, or Y may be bonded to the group Ac to form a diacyl group.
摘要翻译：一种制备具有优异的β-肾上腺素能阻断作用的1-（酰氨基 - 芳氧基）-3-氨基 - 丙醇衍生物的新方法。该方法基本上使式WHEREIN Z为氢原子的化合物或通过脂族醚键与氧原子键合的保护基团，R表示烷基或芳烷基，与式WHEREIN Ar表示的化合物对于取代或未取代的苯或萘环，Ac表示有机酸残基，Y表示氢原子，具有至多12个碳原子的一价烃基或有机酸残基，或Y可以键合到基团Ac至形成二酰基。

10. 发明授权

US3689633A Preparation of test sample for immunological assay of pregnancy of mares 失效
标题翻译：制定玛氏怀孕免疫测定试验样品
公开(公告)号：US3689633A
公开(公告)日：1972-09-05
申请号：US3689633D
申请日：1969-01-13
申请人： TEIKOKU HORMONE MFG CO LTD
发明人： SANAE MATSUSHIMA , TEZUKA TADASHI , NAKANOWATARI KAMEO
IPC分类号： G01N33/76 , A23J1/06 , C07G7/00 , G01N33/16
CPC分类号： G01N33/76 , Y10S436/814 , Y10S436/818 , Y10S436/825 , Y10S436/826 , Y10S530/829 , Y10S530/83
摘要： A process for the preparation of a sample to be tested by immunological assay for detecting serum gonadotrophin in blood of mares, for the purpose of diagnosing the mares pregnancy, which comprises adding an acid selected from the group consisting of sulfosalicyclic, perchloric, and metaphosphoric acids, to the blood, plasma, or serum of the mare to be diagnosed, at a concentration of at least 0.15 m-mol based on 1 ml of serum but below the saturation concentration, separating the resultant precipitate and recovering the supernatnat liquid, and a method diagnosis of pregnancy of a mare using such test sample.
摘要翻译：用于通过免疫测定法检测母体血液中血清促性腺激素测试的样品的方法，用于诊断母马怀孕，其包括加入选自磺基脂环，高氯酸和偏磷酸的酸对待诊断的母体的血液，血浆或血清，浓度为基于1ml血清至少0.15m mol，但低于饱和浓度，分离所得沉淀并回收上清液，并且使用这种测试样品的母马怀孕的方法诊断。

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