公开(公告)号：US5063222A

公开(公告)日：1991-11-05

申请号：US508686

申请日：1990-04-13

申请人： Teruo Komoto ,  Junji Okawa ,  Yoichiro Ogawa ,  Susumu Sato ,  Naokata Taido ,  Tadayuki Kuraishi

发明人： Teruo Komoto ,  Junji Okawa ,  Yoichiro Ogawa ,  Susumu Sato ,  Naokata Taido ,  Tadayuki Kuraishi

IPC分类号： A61K31/57 ,  A61P29/00 ,  C07J5/00 ,  C07J7/00

CPC分类号： C07J7/0055 ,  C07J5/0076 ,  C07J7/0085

摘要： Steroid derivatives represented by formula (I) are disclosed. ##STR1## wherein R is a hydrogen atom, a halogen atom, a hydroxy group, or a group --OCOR.sub.1, wherein R.sub.1 is a linear or branched alkyl group which may be substituted by a halogen atom or a cycloalkyl group, a cycloalkyl group, or an aryl group. The compounds are useful for curing or alleviating inflammation or rheumatism.

公开(公告)号：US5190951A

公开(公告)日：1993-03-02

申请号：US773432

申请日：1991-10-09

申请人： Hiroshi Hasegawa ,  Kazuo Isomae ,  Takeshi Kotsugai ,  Noriaki Shioiri ,  Kumiko Sekine ,  Naokata Taido ,  Susumu Sato ,  Tadayuki Kuraishi

发明人： Hiroshi Hasegawa ,  Kazuo Isomae ,  Takeshi Kotsugai ,  Noriaki Shioiri ,  Kumiko Sekine ,  Naokata Taido ,  Susumu Sato ,  Tadayuki Kuraishi

IPC分类号： C07D219/06 ,  C07D221/16 ,  C07D401/06 ,  C07D471/04

CPC分类号： C07D401/06 ,  C07D219/06 ,  C07D221/16 ,  C07D471/04

摘要： Quinoline derivatives of the formula, ##STR1## wherein > A represents a group >N--(CH.sub.2).sub.n --, >C.dbd., >C.dbd.CH(CH.sub.2).sub.n --, or >CH(CH.sub.2).sub.n --, wherein n is an integer of 0-7; Y represents a group >C.dbd.O or >CHOH, R.sup.1 is a hydrogen atom, a halogen atom, an alkyl group, an alkoxy group, or an alkylthio group, R.sup.2 is a hydrogen atom, a halogen atom, an alkyl group, a hydroxy group, an alkoxy group, a phenyl group which may have a substituent, a phenoxy group, an alkanoyloxy group, or an amino group which may have a substituent, R.sup.3 is a hydrogen atom, a halogen atom, an alkyl group, or an alkoxy group, and m is an integer of 1-3. The compounds and their salts exhibit a superior antiacetylcholinesterase activity with no side effects and are effective for the prevention or cure of senile dementia or memory disturbance.

公开(公告)号：US5159091A

公开(公告)日：1992-10-27

申请号：US596323

申请日：1990-10-12

申请人： Tadatoshi Kuriyama ,  Masaki Ogawa ,  Susumu Sato ,  Naokata Taido ,  Tadayuki Kuraishi

发明人： Tadatoshi Kuriyama ,  Masaki Ogawa ,  Susumu Sato ,  Naokata Taido ,  Tadayuki Kuraishi

IPC分类号： C07J5/00 ,  C07J7/00 ,  C07J21/00 ,  C07J31/00 ,  C07J75/00

CPC分类号： C07J7/0045 ,  C07J21/00 ,  C07J31/006 ,  C07J5/0053

摘要： A process for preparing 21-desoxyprednisolone 17-esters of formula (IV) is disclosed. ##STR1## The process comprises reacting a prednisolone 17.alpha.,21-cyclic orthoester with an acid in a 40-60% lower alcohol solution to produce a prednisolone 17-ester, sulfonylating the prednisolone 17-ester into a prednisolone 17-ester 21-sulfonate, and reacting the sulfonate with an alkali metal iodide in methyl ethyl ketone in the presence of a lower fatty acid to produce the compound of formula (IV). The process ensures economical industrial production of high purity 21-desoxyprednisolone 17-esters, an excellent local anti-inflammatory medicine, in a high yield by simple procedures.

公开(公告)号：US5231101A

公开(公告)日：1993-07-27

申请号：US821803

申请日：1992-01-17

申请人： Haruyoshi Honda ,  Hiroyuki Mizuno ,  Kinichi Mogi ,  Yoshikuni Ito ,  Yasushi Kaneko ,  Naokata Taido ,  Susumu Sato ,  Tadayuki Kuraishi

发明人： Haruyoshi Honda ,  Hiroyuki Mizuno ,  Kinichi Mogi ,  Yoshikuni Ito ,  Yasushi Kaneko ,  Naokata Taido ,  Susumu Sato ,  Tadayuki Kuraishi

IPC分类号： A61K31/445 ,  A61K31/4427 ,  A61P37/08 ,  A61P43/00 ,  C07D401/04 ,  C07D401/14

CPC分类号： C07D401/04

摘要： Benzo[5,6]cyclohepta[1,2-b]pyridine derivatives of the following formula: ##STR1## wherein R.sup.1 represents a cyano, carbamoyl, alkylsulfoxy, alkylsulfonyl, tetrazolyl or sulfonic acid group, and R.sup.2 represents a hydrogen atom, a cyano, phenyl, aralkyl, alkoxycarbonylalkyl, aminoalkylcarbamoylalkyl or lower alkyl group, or a group ##STR2## or --X--R.sub.4, X being an oxygen or sulfur atom, R.sup.3 standing for a hydrogen atom or a substituted or unsubstituted lower alkyl, phenyl or aralkyl group, and R.sup.4 being a substituted or unsubstituted lower alkyl, phenyl or aralkyl group or an aminoalkyl group, and salts thereof. Antiallergic and antihistamic agents containing one of the above derivatives or salts as an active ingredient are also described.

公开(公告)号：US5300517A

公开(公告)日：1994-04-05

申请号：US53202

申请日：1993-04-28

申请人： Hiroshi Hasegawa ,  Kazuo Isomae ,  Takeshi Kotsugai ,  Noriaki Shioiri ,  Kumiko Sekine ,  Naokata Taido ,  Susumu Sato ,  Tadayuki Kuraishi

发明人： Hiroshi Hasegawa ,  Kazuo Isomae ,  Takeshi Kotsugai ,  Noriaki Shioiri ,  Kumiko Sekine ,  Naokata Taido ,  Susumu Sato ,  Tadayuki Kuraishi

IPC分类号： C07D219/06 ,  C07D221/16 ,  C07D401/06 ,  C07D471/04 ,  A61K31/445 ,  C07D401/04

CPC分类号： C07D401/06 ,  C07D219/06 ,  C07D221/16 ,  C07D471/04

摘要： Piperidine compounds of formula II: ##STR1## that exhibit anticholinesterase activity and are effective in treating dementia.

摘要翻译： 具有抗胆碱酯酶活性并有效治疗痴呆的式II的哌啶化合物：IMAGE（II）。

公开(公告)号：US5240934A

公开(公告)日：1993-08-31

申请号：US946620

申请日：1992-09-18

申请人： Hiroshi Hasegawa ,  Kazuo Isomae ,  Takeshi Kotsugai ,  Noriaki Shioiri ,  Kumiko Sekine ,  Naokata Taido ,  Susumu Sato ,  Tadayuki Kuraishi

发明人： Hiroshi Hasegawa ,  Kazuo Isomae ,  Takeshi Kotsugai ,  Noriaki Shioiri ,  Kumiko Sekine ,  Naokata Taido ,  Susumu Sato ,  Tadayuki Kuraishi

IPC分类号： C07D219/06 ,  C07D221/16 ,  C07D401/06 ,  C07D471/04

CPC分类号： C07D401/06 ,  C07D219/06 ,  C07D221/16 ,  C07D471/04

摘要： Quinoline derivatives of the formula, ##STR1## wherein >A represents a group >N--(CH.sub.2).sub.n --, >C.dbd., >C.dbd.CH(CH.sub.2).sub.n --, or >CH(CH.sub.2).sub.n --, wherein n is an integer of 0-7; Y represents a group >C.dbd.O or >CHOH, R.sup.1 is a hydrogen atom, a halogen atom, an alkyl group, an alkoxy group, or an alkylthio group, R.sup.2 is a hydrogen atom, a halogen atom, an alkyl group, a hydroxy group, an alkoxy group, a phenyl group which may have a substituent, a phenoxy group, an alkanoyloxy group, or an amino group which may have a substituent, R.sup.3 is a hydrogen atom, a halogen atom, an alkyl group, or an alkoxy group, and m is an integer of 1-3. The compounds and their salts exhibit a superior anti-acetylcholinesterase activity with no side effects and are effective for the prevention or cure of senile dementia or memory disturbance.

摘要翻译： 其中> A表示基团> N-（CH 2）n - ，> C = C = CH（CH 2）n - 或> CH（CH 2）n - ，其中n为 0-7的整数; Y表示C = O或> CHOH基团，R1表示氢原子，卤素原子，烷基，烷氧基或烷硫基，R2表示氢原子，卤原子，烷基， 羟基，烷氧基，可以具有取代基的苯基，苯氧基，烷酰氧基或可以具有取代基的氨基，R3是氢原子，卤素原子，烷基或 烷氧基，m为1-3的整数。 化合物及其盐具有优异的抗乙酰胆碱酯酶活性，无副作用，对预防或治愈老年痴呆或记忆障碍有效。

公开(公告)号：US5532371A

公开(公告)日：1996-07-02

申请号：US377965

申请日：1995-01-25

申请人： Teruo Komoto ,  Hiroyuki Hirota ,  Susumu Sato ,  Mari Ohtsuka ,  Hidehiko Koya ,  Hiroyuki Mizuno ,  Tadayuki Kuraishi

发明人： Teruo Komoto ,  Hiroyuki Hirota ,  Susumu Sato ,  Mari Ohtsuka ,  Hidehiko Koya ,  Hiroyuki Mizuno ,  Tadayuki Kuraishi

IPC分类号： C07D211/22 ,  C07D211/52 ,  C07D211/70 ,  C07D213/82 ,  C07D295/192 ,  C07D333/38 ,  C07D401/06 ,  C07D405/06 ,  C07D409/06 ,  C07D401/10

CPC分类号： C07D213/82 ,  C07D211/22 ,  C07D211/52 ,  C07D211/70 ,  C07D295/192 ,  C07D333/38 ,  C07D401/06 ,  C07D405/06 ,  C07D409/06

摘要： An arylamide derivative of formula (1), a salt thereof and a therapeutic agent for hyperlipemia which comprises the derivative or salt: ##STR1## wherein Ar represents a group ##STR2## a naphthyl group, a pyridinyl group, a furyl group, a thienyl group, a quinolyl group or an indolyl group; Y represents a group ##STR3## and Q represents --O-- or a single bond, Z represents an alkylene group, and R.sup.4 represents a hydroxyl group, an alkoxy group or a group --NH(CH.sub.2).sub.m COOH.

摘要翻译： 式（1）的芳基酰胺衍生物，其盐和含有该衍生物或盐的高脂血症治疗剂：其中Ar表示基团，萘基，吡啶基，呋喃基 噻吩基，喹啉基或吲哚基; Y表示基团，Q表示-O-或单键，Z表示亚烷基，R4表示羟基，烷氧基或基团-NH（CH2）mCOOH。

公开(公告)号：US5411972A

公开(公告)日：1995-05-02

申请号：US158398

申请日：1993-11-29

申请人： Teruo Komoto ,  Hiroyuki Hirota ,  Susumu Sato ,  Mari Ohtsuka ,  Hidehiko Koya ,  Hiroyuki Mizuno ,  Tadayuki Kuraishi

发明人： Teruo Komoto ,  Hiroyuki Hirota ,  Susumu Sato ,  Mari Ohtsuka ,  Hidehiko Koya ,  Hiroyuki Mizuno ,  Tadayuki Kuraishi

IPC分类号： C07D211/22 ,  C07D211/52 ,  C07D211/70 ,  C07D213/82 ,  C07D295/192 ,  C07D333/38 ,  C07D401/06 ,  C07D405/06 ,  C07D409/06 ,  A61K31/445 ,  C07D211/40 ,  C07D211/74 ,  C07D295/10

CPC分类号： C07D213/82 ,  C07D211/22 ,  C07D211/52 ,  C07D211/70 ,  C07D295/192 ,  C07D333/38 ,  C07D401/06 ,  C07D405/06 ,  C07D409/06

摘要： An arylamide derivative of formula (1), a salt thereof and a therapeutic agent for hyperlipemia which comprises the derivative or salt: ##STR1## wherein Ar represents a group ##STR2## a naphthyl group, a pyridinyl group, a furyl group, a thienyl group, a quinolyl group or an indolyl group; Y represents a group ##STR3## and Q represents --O-- or a single bond, Z represents an alkylene group, and R.sup.4 represents a hydroxyl group, an alkoxy group or a group --NH(CH.sub.2).sub.m COOH, useful for the treatment and prevention of hyperlipemia due to their excellent cholesterol reducing action, triglyceride reducing action and high safety.

摘要翻译： 式（1）的芳基酰胺衍生物，其盐和含有该衍生物或盐的高脂血症治疗剂：其中Ar表示基团，萘基，吡啶基，呋喃基 噻吩基，喹啉基或吲哚基; Y表示 ，Q表示-O-或单键，Z表示亚烷基，R4表示羟基，烷氧基或-NH（CH2）mCOOH基团，可用于 治疗和预防高脂血症由于其优异的胆固醇降低作用，甘油三酯降低作用和高安全性。

公开(公告)号：US4690924A

公开(公告)日：1987-09-01

申请号：US939808

申请日：1986-12-09

申请人： Susumu Sato ,  Haruyoshi Honda ,  Teruo Koumoto ,  Kazuo Isomae ,  Tadayuki Kuraishi ,  Tatsuhiko Katori

发明人： Susumu Sato ,  Haruyoshi Honda ,  Teruo Koumoto ,  Kazuo Isomae ,  Tadayuki Kuraishi ,  Tatsuhiko Katori

IPC分类号： A61K31/435 ,  A61K31/44 ,  A61K31/445 ,  A61K31/495 ,  A61P7/10 ,  A61P9/00 ,  A61P9/04 ,  A61P9/06 ,  A61P9/12 ,  A61P11/00 ,  A61P11/08 ,  A61P25/02 ,  A61P25/04 ,  A61P29/00 ,  C07D471/04 ,  A61K31/535

CPC分类号： C07D471/04

摘要： Certain 1,7-naphthyridine derivatives and their acid addition salts have strong anticholinergic effects, cardiotonic effects, diuretic effects, bronchodilation effects, anti-acetylocholine effects, anti-inflammatory effects, analgesic effects and the like and are hence useful for various diseases such as heart diseases, hypertension, asthma, arthritis, lumbago, toothache, etc.

公开(公告)号：US4659710A

公开(公告)日：1987-04-21

申请号：US850820

申请日：1986-04-11

申请人： Susumu Sato ,  Haruyoshi Honda ,  Teruo Koumoto ,  Kazuo Isomae ,  Tadayuki Kuraishi ,  Tatsuhiko Katori

发明人： Susumu Sato ,  Haruyoshi Honda ,  Teruo Koumoto ,  Kazuo Isomae ,  Tadayuki Kuraishi ,  Tatsuhiko Katori

IPC分类号： A61K31/435 ,  A61K31/44 ,  A61K31/445 ,  A61K31/495 ,  A61P7/10 ,  A61P9/00 ,  A61P9/04 ,  A61P9/06 ,  A61P9/12 ,  A61P11/00 ,  A61P11/08 ,  A61P25/02 ,  A61P25/04 ,  A61P29/00 ,  C07D471/04 ,  A61K31/535 ,  C07D221/00 ,  C07D413/14

CPC分类号： C07D471/04

摘要： Certain 1,7-naphthyridine derivatives and their acid addition salts have strong antiarrhythmic effects, cardiotonic effects, diuretic effects, bronchodilation effects, anti-acetylcholine effects, anti-inflammatory effects, analgesic effects and the like and are hence useful for various diseases such as heart diseases, hypertension, asthma, arthritis, lumbago, toothache, etc.

摘要翻译： 某些1,7-萘啶衍生物及其酸加成盐具有强烈的抗心律失常作用，强心作用，利尿作用，支气管扩张作用，抗乙酰胆碱作用，抗炎作用，镇痛作用等，因此可用于各种疾病如 心脏病，高血压，哮喘，关节炎，腰痛，牙痛等。