公开(公告)号：US4912135A

公开(公告)日：1990-03-27

申请号：US263345

申请日：1988-10-27

申请人： Hiroaki Taguchi ,  Takeo Katsushima ,  Masakazu Ban ,  Akihiko Watanabe

发明人： Hiroaki Taguchi ,  Takeo Katsushima ,  Masakazu Ban ,  Akihiko Watanabe

IPC分类号： C07C255/59 ,  A61K31/165 ,  A61K31/275 ,  A61P11/00 ,  A61P17/00 ,  A61P27/16 ,  A61P37/08 ,  C07C67/00 ,  C07C231/00 ,  C07C233/44 ,  C07C235/16 ,  C07C235/56 ,  C07C235/64 ,  C07C237/30 ,  C07C237/42 ,  C07C255/60 ,  C07C311/29 ,  C07C311/39 ,  C07C311/48 ,  C07C323/59 ,  C07C323/63

CPC分类号： C07C255/60

摘要： Novel amide compounds of the formula: ##STR1## wherein R.sup.1 is hydrogen, lower alkyl, acetyl, or propionyl; R.sup.2 is hydrogen or chlorine; R.sup.3 is hydrogen or a group of the formula: --CO.sub.2 R.sup.6 (wherein R.sup.6 is hydrogen, lower alkyl or alkali metal); R.sup.4 is hydrogen, trifluoromethyl, cyano, aminocarbonyl, or a group of the formula: --CO.sub.2 R.sup.7 (wherein R.sup.7 is hydrogen, lower alkyl, or alkali metal); R.sup.5 is hydrogen, or a group of the formula: --CO.sub.2 R.sup.8 (wherein R.sup.8 is hydrogen, lower alkyl, or alkali metal), which have excellent anti-allergic activity and are useful for the prophylaxis and treatment of various allergic diseases, and a pharmaceutical composition containing the amide compound as set forth above as an active ingredient.

公开(公告)号：US5036086A

公开(公告)日：1991-07-30

申请号：US501727

申请日：1990-03-30

申请人： Hiroaki Taguchi ,  Takeo Katsushima ,  Masakazu Ban ,  Mitsuru Takahashi ,  Kiyotaka Shinoda ,  Akihiko Watanabe

发明人： Hiroaki Taguchi ,  Takeo Katsushima ,  Masakazu Ban ,  Mitsuru Takahashi ,  Kiyotaka Shinoda ,  Akihiko Watanabe

IPC分类号： A61K31/425 ,  A61K31/428 ,  A61P37/08 ,  C07D277/82

CPC分类号： C07D277/82

摘要： Novel benzothiazole derivatives of the formula (I): ##STR1## wherein R.sup.1 is hydrogen atom, a lower alkyl group or a lower acyl group; X and Y are the same or different and are each hydrogen atom, a halogen atom, a lower alkyl group, a lower alkoxy group, nitro group, amino group, cyano group, trifluoromethyl group, a group of the formula: --COOR.sup.2 (wherein R.sup.2 is hydrogen atom, a lower alkyl group, an alkali metal, an alkaline earth metal, or a cation of amine), or a group of the formula: --CONR.sup.3 R.sup.4 (wherein R.sup.3 and R.sup.4 are the same or different and are each hydrogen atom or a lower alkyl group) or a pharmaceutically acceptable acid addition salt thereof, which have excellent anti-allergic activity and are useful for the prophylaxis and treatment of various allergic diseases, and a pharmaceutical composition containing the compound as set forth above as an active ingredient.

公开(公告)号：US20050107448A1

公开(公告)日：2005-05-19

申请号：US10986296

申请日：2004-11-12

申请人： Yuko Shinagawa ,  Takeo Katsushima ,  Takashi Nakagawa

发明人： Yuko Shinagawa ,  Takeo Katsushima ,  Takashi Nakagawa

IPC分类号： C07C217/28 ,  C07C217/60 ,  C07C217/76 ,  C07C229/38 ,  C07C233/25 ,  C07C235/42 ,  C07C235/60 ,  C07C237/30 ,  C07C255/54 ,  C07C311/21 ,  C07C311/29 ,  C07D213/30 ,  C07D277/24 ,  C07D307/42 ,  C07D317/58 ,  C07D333/16 ,  C07D333/56 ,  A61K31/44 ,  A61K31/138 ,  A61K31/18 ,  A61K31/195 ,  A61K31/277

CPC分类号： C07D213/30 ,  C07B2200/07 ,  C07C217/28 ,  C07C217/60 ,  C07C217/76 ,  C07C229/38 ,  C07C233/25 ,  C07C235/42 ,  C07C235/60 ,  C07C237/30 ,  C07C255/54 ,  C07C311/21 ,  C07C311/29 ,  C07C2601/02 ,  C07C2601/04 ,  C07C2601/08 ,  C07D277/24 ,  C07D307/42 ,  C07D317/58 ,  C07D333/16 ,  C07D333/56

摘要： A compound of the formula [I] wherein R1 is optionally substituted aryl group or optionally substituted heteroaryl group; R2 is optionally substituted C1-6 alkyl group, C3-7 cycloalkyl group and the like; R3 is hydrogen atom, C1-6 alkyl group, hydroxyl group and the like; R4 is hydrogen atom, C1-6 alkyl group and the like; R5 and R6 are each C1-6 alkyl group and the like; R7 is optionally substituted aryl group or optionally substituted heteroaryl group; X1, X2 and X3 are each C1-6 alkylene group and the like; and X4 and X5 are each a single bond, methylene group and the like, a salt thereof, a solvate thereof or a prodrug thereof, and a pharmaceutical composition containing the compound, particularly a calcium receptor antagonist and a therapeutic agent for osteoporosis, are provided. The compound of the present invention is useful as a therapeutic drug of diseases accompanied by abnormal calcium homeostasis, or osteoporosis, hypoparathyreosis, osteosarcoma, periodontal disease, bone fracture, steoarthrosis, chronic rheumatoid arthritis, Paget's disease, humoral hypercalcemia, autosomal dominant hypocalcemia and the like. In addition, an intermediate for the compound is provided.

摘要翻译： 其中R 1为式（I）的化合物为任选取代的芳基或任选取代的杂芳基; R 2是任选取代的C 1-6烷基，C 3-7环烷基等; R 3是氢原子，C 1-6烷基，羟基等; R 4是氢原子，C 1-6烷基等; R 5和R 6各自为C 1-6烷基等; R 7是任选取代的芳基或任选取代的杂芳基; X 1，X 2和X 3各自为C 1-6亚烷基等; 和X 4和X 5各自为单键，亚甲基等，其盐，其溶剂合物或其前药，以及含有 化合物，特别是钙受体拮抗剂和骨质疏松症的治疗剂。 本发明的化合物可用作伴有异常钙稳态或骨质疏松症，hypoparathyreosis，骨肉瘤，牙周病，骨折，骨关节炎，慢性类风湿性关节炎，佩吉特氏病，体液性高钙血症，常染色体显性低钙血症的疾病的治疗药物 喜欢。 此外，还提供了化合物的中间体。

公开(公告)号：US5624961A

公开(公告)日：1997-04-29

申请号：US535077

申请日：1995-12-11

申请人： Masakazu Ban ,  Kiyotaka Shinoda ,  Mitsuru Takahashi ,  Shuhei Deguchi ,  Hiroaki Taguchi ,  Takeo Katsushima

发明人： Masakazu Ban ,  Kiyotaka Shinoda ,  Mitsuru Takahashi ,  Shuhei Deguchi ,  Hiroaki Taguchi ,  Takeo Katsushima

IPC分类号： A61K31/135 ,  A61K31/165 ,  A61K31/22 ,  A61P9/00 ,  C07C213/02 ,  C07C213/04 ,  C07C217/18 ,  C07C217/58 ,  C07C217/84 ,  C07C219/28 ,  C07C231/12 ,  C07C233/18 ,  C07C233/25 ,  C07C303/32 ,  C07C309/30

CPC分类号： C07C217/84 ,  C07C217/18 ,  C07C217/58 ,  C07C219/28 ,  C07C233/18 ,  C07C233/25

摘要： Novel benzylaminoethoxybenzene derivatives of the formula (I) ##STR1## wherein R.sup.1 is a hydrogen atom, a lower alkyl, a lower hydroxyalkyl, a lower alkoxyalkyl, an allyl or a benzyl; R.sup.2 is a hydrogen atom, a lower alkyl, a lower acyl, an allyl or a benzyl; R.sup.3 is a hydrogen atom, a lower alkyl, a lower alkoxyalkyl, a lower dialkylaminoalkyl or a lower acyl; and R.sup.4 is a hydrogen atom, a halogen atom, a lower alkoxy, an amino, a lower acylamino, a hydroxy, a lower acyloxy, a lower acyl, a carboxy or a lower alkoxycarbonyl, salts thereof and solvates thereof. An .alpha..sub.1 -adrenoceptor blocker obtained from this compound has a strong .alpha..sub.1 -adrenoceptor blocking effect and causes less side effects such as orthostatic hypotension.

摘要翻译： PCT No.PCT / JP95 / 00187 Sec。 371 1995年12月11日第 102（e）日期1995年12月11日PCT提交1995年2月10日PCT公布。 出版物WO95 / 21811 日期：1995年8月17日式（I）的新型苄基氨基乙氧基苯衍生物其中R 1为氢原子，低级烷基，低级羟烷基，低级烷氧基烷基，烯丙基或苄基; R2是氢原子，低级烷基，低级酰基，烯丙基或苄基; R3是氢原子，低级烷基，低级烷氧基烷基，低级二烷基氨基烷基或低级酰基; R4为氢原子，卤素原子，低级烷氧基，氨基，低级酰基氨基，羟基，低级酰氧基，低级酰基，羧基或低级烷氧基羰基，其盐及其溶剂合物。 从该化合物获得的α1-肾上腺素受体阻滞剂具有强α1-肾上腺素能受体阻断效应并且引起较少的副作用，例如直立性低血压。

公开(公告)号：US5041462A

公开(公告)日：1991-08-20

申请号：US476515

申请日：1990-02-07

申请人： Hiroaki Taguchi ,  Takeo Katsushima ,  Masakazu Ban ,  Mitsuru Takahashi ,  Kiyotaka Shinoda ,  Akihiko Watanabe

发明人： Hiroaki Taguchi ,  Takeo Katsushima ,  Masakazu Ban ,  Mitsuru Takahashi ,  Kiyotaka Shinoda ,  Akihiko Watanabe

IPC分类号： A61K31/165 ,  A61K31/275 ,  A61P37/08 ,  C07C237/30 ,  C07C237/42 ,  C07C237/44 ,  C07C255/60 ,  C07D295/155

CPC分类号： C07D295/155 ,  C07C237/42 ,  C07C237/44 ,  C07C255/60

摘要： Novel substituted acetamide compounds of the formula ##STR1## wherein R.sup.1 is hydrogen atom, a lower alkyl group, a lower acyl group, or an aryl group; R.sup.2 is cyano group or aminocarbonyl group; R.sup.3 is a halogen atom, nitro group, a lower alkoxy group, a group of the formula: --NR.sup.4 R.sup.5 (wherein R.sup.4 is hydrogen atom, a lower alkyl group or a group of the formula: --COCH.sub.2 OR.sup.1 ; R.sup.5 is hydrogen atom or a lower alkyl group), or a cyclic amino group of the formula: ##STR2## (wherein R.sup.6 and R.sup.7 are each an alkylene group having 1 to 3 carbon atoms, and X is oxygen atom or methylene), or a pharmaceutically acceptable acid addition salt thereof, which have excellent anti-allergic activity and are useful for the prophylaxis and treatment of various allergic diseases, and a pharmaceutical composition containing the amide compound as set forth above as an active ingredient.

公开(公告)号：US07211685B2

公开(公告)日：2007-05-01

申请号：US10986296

申请日：2004-11-12

申请人： Yuko Shinagawa ,  Takeo Katsushima ,  Takashi Nakagawa

发明人： Yuko Shinagawa ,  Takeo Katsushima ,  Takashi Nakagawa

IPC分类号： C07C63/36 ,  C07C205/04 ,  C07C271/10

CPC分类号： C07D213/30 ,  C07B2200/07 ,  C07C217/28 ,  C07C217/60 ,  C07C217/76 ,  C07C229/38 ,  C07C233/25 ,  C07C235/42 ,  C07C235/60 ,  C07C237/30 ,  C07C255/54 ,  C07C311/21 ,  C07C311/29 ,  C07C2601/02 ,  C07C2601/04 ,  C07C2601/08 ,  C07D277/24 ,  C07D307/42 ,  C07D317/58 ,  C07D333/16 ,  C07D333/56

摘要： A compound of the formula [I] wherein R1 is optionally substituted aryl group or optionally substituted heteroaryl group; R2 is optionally substituted C1-6 alkyl group, C3-7 cycloalkyl group and the like; R3 is hydrogen atom, C1-6 alkyl group, hydroxyl group and the like; R4 is hydrogen atom, C1-6 alkyl group and the like; R5 and R6 are each C1-6 alkyl group and the like; R7 is optionally substituted aryl group or optionally substituted heteroaryl group; X1, X2 and X3 are each C1-6 alkylene group and the like; and X4 and X5 are each a single bond, methylene group and the like, a salt thereof, a solvate thereof or a prodrug thereof, and a pharmaceutical composition containing the compound, particularly a calcium receptor antagonist and a therapeutic agent for osteoporosis, are provided. The compound of the present invention is useful as a therapeutic drug of diseases accompanied by abnormal calcium homeostasis, or osteoporosis, hypoparathyreosis, osteosarcoma, periodontal disease, bone fracture, steoarthrosis, chronic rheumatoid arthritis, Paget's disease, humoral hypercalcemia, autosomal dominant hypocalcemia and the like. In addition, an intermediate for the compound is provided.

摘要翻译： 其中R 1为式（I）的化合物为任选取代的芳基或任选取代的杂芳基; R 2是任选取代的C 1-6烷基，C 3-7环烷基等; R 3是氢原子，C 1-6烷基，羟基等; R 4是氢原子，C 1-6烷基等; R 5和R 6各自为C 1-6烷基等; R 7是任选取代的芳基或任选取代的杂芳基; X 1，X 2和X 3各自为C 1-6亚烷基等; 和X 4和X 5各自为单键，亚甲基等，其盐，其溶剂合物或其前药，以及含有 化合物，特别是钙受体拮抗剂和骨质疏松症的治疗剂。 本发明的化合物可用作伴有异常钙稳态或骨质疏松症，hypoparathyreosis，骨肉瘤，牙周病，骨折，骨关节炎，慢性类风湿性关节炎，佩吉特氏病，体液性高钙血症，常染色体显性低钙血症的疾病的治疗药物 喜欢。 此外，还提供了化合物的中间体。

公开(公告)号：US06916956B2

公开(公告)日：2005-07-12

申请号：US10344157

申请日：2001-08-10

申请人： Yuko Shinagawa ,  Takeo Katsushima ,  Takashi Nakagawa

发明人： Yuko Shinagawa ,  Takeo Katsushima ,  Takashi Nakagawa

IPC分类号： C07C217/28 ,  C07C217/60 ,  C07C217/76 ,  C07C229/38 ,  C07C233/25 ,  C07C235/42 ,  C07C235/60 ,  C07C237/30 ,  C07C255/54 ,  C07C311/21 ,  C07C311/29 ,  C07D213/30 ,  C07D277/24 ,  C07D307/42 ,  C07D317/58 ,  C07D333/16 ,  C07D333/56 ,  C07C217/10 ,  C07D33/16

CPC分类号： C07D213/30 ,  C07B2200/07 ,  C07C217/28 ,  C07C217/60 ,  C07C217/76 ,  C07C229/38 ,  C07C233/25 ,  C07C235/42 ,  C07C235/60 ,  C07C237/30 ,  C07C255/54 ,  C07C311/21 ,  C07C311/29 ,  C07C2601/02 ,  C07C2601/04 ,  C07C2601/08 ,  C07D277/24 ,  C07D307/42 ,  C07D317/58 ,  C07D333/16 ,  C07D333/56

摘要： A compound of the formula [I] wherein R1 is optionally substituted aryl group or optionally substituted heteroaryl group; R2 is optionally substituted C1-6 alkyl group, C3-7 cycloalkyl group and the like; R3 is hydrogen atom, C1-6 alkyl group, hydroxyl group and the like; R4 is hydrogen atom, C1-6 alkyl group and the like; R5 and R6 are each C1-6 alkyl group and the like; R7 is optionally substituted aryl group or optionally substituted heteroaryl group; X1, X2 and X3 are each C1-6 alkylene group and the like; and X4 and X5 are each a single bond, methylene group and the like, a salt thereof, a solvate thereof or a prodrug thereof, and a pharmaceutical composition containing the compound, particularly a calcium receptor antagonist and a therapeutic agent for osteoporosis, are provided. The compound of the present invention is useful as a therapeutic drug of diseases accompanied by abnormal calcium homeostasis, or osteoporosis, hypoparathyreosis, osteosarcoma, periodontal disease, bone fracture, steoarthrosis, chronic rheumatoid arthritis, Paget's disease, humoral hypercalcemia, autosomal dominant hypocalcemia and the like. In addition, an intermediate for the compound is provided.

摘要翻译： 其中R 1为式（I）的化合物为任选取代的芳基或任选取代的杂芳基; R 2是任选取代的C 1-6烷基，C 3-7环烷基等; R 3是氢原子，C 1-6烷基，羟基等; R 4是氢原子，C 1-6烷基等; R 5和R 6各自为C 1-6烷基等; R 7是任选取代的芳基或任选取代的杂芳基; X 1，X 2和X 3各自为C 1-6亚烷基等; 和X 4和X 5各自为单键，亚甲基等，其盐，其溶剂合物或其前药，以及含有 化合物，特别是钙受体拮抗剂和骨质疏松症的治疗剂。 本发明的化合物可用作伴有异常钙稳态或骨质疏松症，hypoparathyreosis，骨肉瘤，牙周病，骨折，骨关节炎，慢性类风湿性关节炎，佩吉特氏病，体液性高钙血症，常染色体显性低钙血症的疾病的治疗药物 喜欢。 此外，还提供了化合物的中间体。

公开(公告)号：US06235730B1

公开(公告)日：2001-05-22

申请号：US09367242

申请日：1999-10-26

申请人： Motohide Sato ,  Takeo Katsushima ,  Hajime Kinoshita

发明人： Motohide Sato ,  Takeo Katsushima ,  Hajime Kinoshita

IPC分类号： C07D40104

CPC分类号： C07D401/04 ,  C07D401/14 ,  C07D409/14 ,  C07D417/14

摘要： 3-piperidyl-4-oxoquinazoline derivatives are provided, which is represented by the formula (I): wherein R represents an amino group or a cyclic amino group such as dibenzoazepine, each of which is substituted with a substituted or unsubstituted aryl group, a substituted or unsubstituted heteroaryl group, or the like, n is an integer of 1 to 3, R3 and R4 independently represents a hydrogen atom, a lower alkyl group, or the like, or a pharmaceutically acceptable salt thereof. Compounds (I) of the present invention have excellent MTP-inhibitory activity. Thus, these compounds not only inhibit formation of LDL that is a cause of arteriosclerotic diseases but also regulate TG, cholesterol, and lipoproteins such as LDL in the blood and regulate cellular lipids through regulation of MTP activity. They can also be used as a new type of preventive or therapeutic agents for hyperlipemia or arteriosclerotic diseases. Furthermore, they can be used as therapeutic or preventive agents for pancreatitis, obesity, hypercholesterolemia, and hypertriglyceridemia.

摘要翻译： 提供了由式（I）表示的3-哌啶基-4-氧代喹唑啉衍生物：其中R表示氨基或环状氨基，例如二苯并氮杂，其各自被取代或未取代的芳基取代， 取代或未取代的杂芳基等，n为1〜3的整数，R3和R4分别独立地表示氢原子，低级烷基等，或其药学上可接受的盐。 本发明的化合物（I）具有优异的MTP抑制活性。 因此，这些化合物不仅抑制作为动脉硬化疾病的原因的LDL的形成，而且通过调节MTP活性来调节血液中的TG，胆固醇和脂蛋白如LDL，并调节细胞脂质。 它们也可以用作高脂血症或动脉硬化性疾病的新型预防或治疗剂。 此外，它们可以用作胰腺炎，肥胖症，高胆固醇血症和高甘油三酯血症的治疗或预防剂。

公开(公告)号：US4729995A

公开(公告)日：1988-03-08

申请号：US033734

申请日：1987-04-03

申请人： Hiroaki Taguchi ,  Takeo Katsushima ,  Masakazu Ban ,  Shoichi Aoki ,  Akihiko Watanabe

发明人： Hiroaki Taguchi ,  Takeo Katsushima ,  Masakazu Ban ,  Shoichi Aoki ,  Akihiko Watanabe

IPC分类号： C07D239/48 ,  C07D239/50 ,  A61K31/505 ,  A61K31/535 ,  C07D413/04

CPC分类号： C07D239/48 ,  C07D239/50

摘要： Novel pyrimidine compounds of the formula: ##STR1## wherein R.sub.1 and R.sub.1 ' are each hydrogen atom, a lower alkyl, benzyl, an alkali metal, or ammonium; R.sub.2 is hydrogen atom, a halogen atom, a lower alkyl, a lower alkoxy, an aryl, a group of the formula: ##STR2## (wherein R.sub.3 and R.sub.4 are each hydrogen atom, a lower alkyl, or an aryl), or a group of the formula: ##STR3## [wherein R.sub.5 and R.sub.6 are each an alkylene having 1 to 3 carbon atoms, and X is oxygen atom, methylene, or a group of the formula: >N-Y (wherein Y is hydrogen atom, a lower alkyl, benzyl, or an aryl)], which have excellent antiallergic activities and are useful for the prophylaxis and treatment of various allergic diseases, and a pharmaceutical composition containing said pyrimidine compound as an active ingredient.