公开(公告)号：US4082780A

公开(公告)日：1978-04-04

申请号：US744185

申请日：1976-11-22

申请人： Takuichi Miki ,  Kentaro Hiraga ,  Giichi Goto

发明人： Takuichi Miki ,  Kentaro Hiraga ,  Giichi Goto

IPC分类号： A61K31/565 ,  C07J1/00

CPC分类号： C07J1/007 ,  C07J1/0059

摘要： Novel estradiol derivatives of the formula ##STR1## wherein R.sup.1 means an alkyl group of two or more carbon atoms, and R.sup.2 is hydrogen or an acyl group, have antiestrogen activity and are useful as antiestrogen drugs.

公开(公告)号：US3953483A

公开(公告)日：1976-04-27

申请号：US479676

申请日：1974-06-13

申请人： Kentaro Hiraga ,  Kouichi Yoshioka ,  Giichi Goto ,  Ryo Nakayama ,  Michio Masuoka

发明人： Kentaro Hiraga ,  Kouichi Yoshioka ,  Giichi Goto ,  Ryo Nakayama ,  Michio Masuoka

IPC分类号： C07J1/00 ,  A61K20060101 ,  A61K31/565 ,  C07C20060101 ,  C07J20060101

CPC分类号： C07J75/00

摘要： Novel steroid compounds are provided represented by the formula: ##SPC1##Wherein each of R.sup.1 and R.sup.2 represents hydrogen or methyl group or R.sup.1 and R.sup.2 may be combined with each other to represent methylene group, n is 2 or 3 and the dotted line means a double bond at 6-exo-position when n is 2 or between 6- and 7-position when n is 3.These novel compounds show a strong anti-androgenic activity, especially by oral administration, and can be used as a remedy for the prostatomegaly.

摘要翻译： 新型类固醇化合物由下式表示：

公开(公告)号：US4879293A

公开(公告)日：1989-11-07

申请号：US241851

申请日：1988-09-08

申请人： Kentaro Hiraga ,  Yoshiaki Saji

发明人： Kentaro Hiraga ,  Yoshiaki Saji

IPC分类号： C07D209/44 ,  C07D209/46 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D417/06 ,  C07D417/12 ,  C07D471/04 ,  C07D487/04 ,  C07D495/04 ,  C07F9/553 ,  C07F9/572 ,  C07F9/59

CPC分类号： C07D401/04 ,  C07D209/46 ,  C07D401/12 ,  C07D417/06 ,  C07D417/12 ,  C07D471/04 ,  C07D487/04 ,  C07D495/04 ,  C07F9/5532 ,  C07F9/5721 ,  C07F9/591

摘要： The compound of the formula ##STR1## wherein X is a cyclic group which may optionally be substituted; Y is a carboxyl group which may optionally be esterified or amidated; Z is --CH.dbd.CH--CH.dbd.CH--, --S--(CH.sub.2).sub.l --S-- is an integer of 1 to 3), --N.dbd.CH--CH.dbd.N-- or --(CH.sub.2).sub.m --(m is an integer of 3 to 5); ring A may optionally be substituted with halogen, nitro, amino, alkanoylamino, alkoxycarbonyl, carboxyl or carbamoyl; and n is an integer of 1 to 3, and salts thereof. The compounds display a strong antianxiety effect to mammalian animals and are useful for the prevention or treatment of a disease such as psychoromatic disease and anxiety neurosis.

公开(公告)号：US4590189A

公开(公告)日：1986-05-20

申请号：US478478

申请日：1983-03-24

申请人： Kentaro Hiraga ,  Yoshiaki Saji

发明人： Kentaro Hiraga ,  Yoshiaki Saji

IPC分类号： C07D209/44 ,  C07D209/46 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D417/06 ,  C07D417/12 ,  C07D471/04 ,  C07D487/04 ,  C07D495/04 ,  C07F9/553 ,  C07F9/572 ,  C07F9/59 ,  C07D413/02 ,  C07D403/04 ,  C07D401/02 ,  C07D209/02 ,  A61K31/535 ,  A61K31/505 ,  A61K31/495 ,  A61K31/47 ,  A61K31/40

CPC分类号： C07D401/04 ,  C07D209/46 ,  C07D401/12 ,  C07D417/06 ,  C07D417/12 ,  C07D471/04 ,  C07D487/04 ,  C07D495/04 ,  C07F9/5532 ,  C07F9/5721 ,  C07F9/591

摘要： The compound of the formula ##STR1## wherein X is a cyclic group which may optionally be substituted; Y is a carboxyl group which may optionally be esterified or amidated; Z is --CH.dbd.CH--CH.dbd.CH--, --S--(CH.sub.2).sub.l --S--(l is an integer of 1 to 3), --N.dbd.CH--CH.dbd.N-- or --(CH.sub.2).sub.m --(m is an integer of 3 to 5); ring A may optionally be substituted with halogen, nitro, amino, alkanoylamino, alkoxycarbonyl, carboxyl or carbamoyl; and n is an integer of 1 to 3, and salts thereof. The compounds display a strong antianxiety effect to mammalian animals and are useful for the prevention or treatment of a disease such as psychosomatic disease and anxiety neurosis.

摘要翻译： 其中X是可任选被取代的环状基团的式“IMAGE”的化合物; Y是任选被酯化或酰胺化的羧基; Z是-CH = CH-CH = CH-，-S-（CH 2）l S-（I是1至3的整数），-N = CH-CH = N-或 - （CH 2）m - （m是 3〜5的整数）; 环A可以任选被卤素，硝基，氨基，烷酰基氨基，烷氧基羰基，羧基或氨基甲酰基取代; n为1〜3的整数，及其盐。 这些化合物对哺乳动物具有强烈的抗焦虑作用，可用于预防或治疗诸如心身疾病和焦虑性神经症等疾病。

公开(公告)号：US4029883A

公开(公告)日：1977-06-14

申请号：US426693

申请日：1973-12-20

申请人： Kentaro Hiraga ,  Tetsuya Okutani ,  Kouichi Yoshioka ,  Tsunehiko Asako

发明人： Kentaro Hiraga ,  Tetsuya Okutani ,  Kouichi Yoshioka ,  Tsunehiko Asako

IPC分类号： C07H15/00 ,  C07H15/222 ,  C07H15/23 ,  C07H17/00

CPC分类号： C07H15/222 ,  C07H15/23 ,  Y02P20/55

摘要： Dehydroxylation of aminoglycoside antibiotics is carried out by halogenation of phosphorylated aminoglycoside antibiotics followed by reduction of thus halogenated antibiotics. The dehydroxylation process is entirely new and gives the final product in a high yield. The resulting deoxyaminoglycoside antibiotics are effective against microorganisms including aminoglycoside antiobiotics-resistant microorganisms.

摘要翻译： 氨基糖苷类抗生素的脱羟基化是通过卤化磷酸化的氨基糖苷类抗生素进行的，随后还原如此卤化的抗生素。 脱羟基化过程是全新的，并以高产率给出最终产品。 所得脱氧氨基糖苷类抗生素对抗微生物有效，包括抗氨基糖苷类抗生素的微生物。

公开(公告)号：US4020269A

公开(公告)日：1977-04-26

申请号：US566519

申请日：1975-04-08

申请人： Kentaro Hiraga ,  Tetsuya Okutani ,  Tsunehiko Asako ,  Kouichi Yoshioka

发明人： Kentaro Hiraga ,  Tetsuya Okutani ,  Tsunehiko Asako ,  Kouichi Yoshioka

IPC分类号： C07H15/23 ,  C07H15/232 ,  C07H15/236 ,  C07H15/22

CPC分类号： C07H15/234 ,  C07H15/23 ,  C07H15/232

摘要： Deoxyaminoglycoside antibiotics are prepared in a high yield from phosphorylated aminoglycosides by reacting a phosphorylated aminoglycoside (a) with a silylating agent, or (b) successively with (i) a silylating or acylating agent and (ii) a halogenating agent; then subjecting thus obtained intermediate to reduction. Deoxyaminoglycoside antibiotics are useful for treating infections caused by microorganisms which are resistant or non-resistant to the corresponding aminoglycoside antibiotics.

摘要翻译： 通过使磷酸化氨基糖苷（a）与甲硅烷基化剂反应，或（b）依次与（i）甲硅烷基化或酰化剂和（ii）卤化剂反应，从磷酸化氨基糖苷类制备高脱离氨基糖苷类抗生素; 然后对由此得到的中间体进行还原。 脱氧氨基糖苷类抗生素可用于治疗由相应的氨基糖苷类抗生素耐药或不耐药的微生物引起的感染。

公开(公告)号：US4788191A

公开(公告)日：1988-11-29

申请号：US832138

申请日：1986-04-23

申请人： Kentaro Hiraga ,  Yoshiaki Saji

发明人： Kentaro Hiraga ,  Yoshiaki Saji

IPC分类号： C07D209/44 ,  C07D209/46 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D417/06 ,  C07D417/12 ,  C07D471/04 ,  C07D487/04 ,  C07D495/04 ,  C07F9/553 ,  C07F9/572 ,  C07F9/59 ,  A61K31/33 ,  A61K31/495 ,  A61K31/50 ,  A61K31/505 ,  C07D413/14 ,  C07D403/14 ,  C07D409/14

CPC分类号： C07D401/04 ,  C07D209/46 ,  C07D401/12 ,  C07D417/06 ,  C07D417/12 ,  C07D471/04 ,  C07D487/04 ,  C07D495/04 ,  C07F9/5532 ,  C07F9/5721 ,  C07F9/591

摘要： The compound of the formula ##STR1## wherein X is a cyclic group which may optionally be substituted; Y is a carboxyl group which may optionally be esterified or amidated; Z is --CH.dbd.CH--CH.dbd.CH--, --S--(CH.sub.2).sub.l --S-- (l is an integer of 1 to 3), --N.dbd.CH--CH.dbd.N-- or --(CH.sub.2).sub.m -- (m is an integer of 3 to 5); ring A may optionally be substituted with halogen, nitro, amino, alkanoylamino, alkoxycarbonyl, carboxyl or carbamoyl; and n is an integer of 1 to 3, and salts thereof. The compounds display a strong antianxiety effect to mammalian animals and are useful for the prevention or treatment of a disease such as psychoromatic disease and anxiety neurosis.

公开(公告)号：US4324795A

公开(公告)日：1982-04-13

申请号：US190412

申请日：1980-09-24

申请人： Tetsuo Okauchi ,  Kentaro Hiraga ,  Yasuo Sato

发明人： Tetsuo Okauchi ,  Kentaro Hiraga ,  Yasuo Sato

IPC分类号： A01N43/36 ,  C07D207/22

CPC分类号： A01N43/36 ,  C07D207/22

摘要： Novel acaricidal agents which contains, as an active ingredient, a pyrroline derivative of the formula: ##STR1## wherein R.sup.1 and R.sup.2 are each hydrogen, halogen or lower alkyl;R.sup.3 is hydrogen or phenyl which may be substituted with halogen;R.sup.4 is hydrogen or lower alkanoyl and R.sup.5 is hydrogen or phenyl or its acid addition salt and a carrier, vehicle or diluent thereof, can effectively eradicate ticks and mites.

摘要翻译： 含有作为活性成分的下式的吡咯啉衍生物的新型杀螨剂：其中R 1和R 2各自为氢，卤素或低级烷基; R3是氢或可被卤素取代的苯基; R4是氢或低级烷酰基，R5是氢或苯基或其酸加成盐及其载体，载体或稀释剂，可以有效地根除蜱和螨。