公开(公告)号：US5814631A

公开(公告)日：1998-09-29

申请号：US849114

申请日：1997-05-28

申请人： Harukazu Fukami ,  Akiko Ito ,  Shinjiro Niwata ,  Saki Kakutani ,  Motoo Sumida ,  Yoshinobu Kiso

发明人： Harukazu Fukami ,  Akiko Ito ,  Shinjiro Niwata ,  Saki Kakutani ,  Motoo Sumida ,  Yoshinobu Kiso

IPC分类号： C07D239/96 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07F9/6512 ,  A61K31/495 ,  A61K31/505 ,  C07D239/72 ,  C07D403/02

CPC分类号： C07D401/06 ,  C07D239/96 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07F9/65128

摘要： A chymase inhibitor containing as its effective ingredient a quinazoline derivative, or a pharmaceutically acceptable salt thereof, having the formula (1): ##STR1## and a pharmaceutical preparation for the prevention of cardiac and circulatory system diseases derived from abnormal exacerbation of Ang II production containing the same as its effective ingredient.

摘要翻译： PCT No.PCT / JP96 / 02830 Sec。 371日期：1997年5月8日 102（e）日期1997年5月8日PCT提交1996年9月27日PCT公布。 公开号WO97 / 11941 日期1997年3月4日含有具有式（1）的喹唑啉衍生物或其药学上可接受的盐作为其有效成分的胃促胰酶抑制剂：（1）和用于预防心脏和循环系统疾病的药物制剂 衍生自与其有效成分相同的Ang II产生异常恶化。

公开(公告)号：US5691335A

公开(公告)日：1997-11-25

申请号：US615277

申请日：1996-03-28

申请人： Harukazu Fukami ,  Motoo Sumida ,  Shinjiro Niwata ,  Saki Kakutani ,  Saitoh Masayuki ,  Shibata Hiroshi ,  Kiso Yoshinobu

发明人： Harukazu Fukami ,  Motoo Sumida ,  Shinjiro Niwata ,  Saki Kakutani ,  Saitoh Masayuki ,  Shibata Hiroshi ,  Kiso Yoshinobu

IPC分类号： C07D233/80 ,  C07D233/84 ,  C07D233/86 ,  C07D401/04 ,  C07D403/04 ,  C07D405/12 ,  A61K31/415 ,  A61K31/495

CPC分类号： C07D401/04 ,  C07D233/80 ,  C07D233/86 ,  C07D403/04 ,  C07D405/12

摘要： The invention relates to an imidazolidine derivative represented by the following general formula (1): ##STR1## wherein A and B mean individually an aromatic hydrocarbon group which may be substituted by 1-3 substituents selected from halogen atoms, C.sub.1-4 alkyl groups, C.sub.1-4 alkoxy groups, C.sub.1-4 alkylenedioxy groups, a phenoxy group, a nitro group, a cyano group, a phenyl group, C.sub.2-5 alkanoylamino groups, a carboxyl group which may be esterified with a C.sub.1-4 alkyl or alkenyl group, carboxyalkyl groups which may be esterified with a C.sub.1-4 alkyl or alkenyl group, carboxyalkyloxy groups which may be esterified with a C.sub.1-4 alkyl or alkenyl group, N-alkylpiperazinylcarbonyl groups, N-alkylpiperazinylcarbonylalkyl groups, N-alkylpiperazinylcarbonylalkyloxy groups, and a morpholinocarbonyl group; X denotes a sulfonyl or carbonyl group; and Y stands for an oxygen or sulfur atom, a chymase inhibitor comprising the same as an active ingredient, and a medicine comprising the same as an active ingredient, typified by a prophylactic and therapeutic agent for a disease of the heart or circulatory system, which is caused by the abnormal acceleration of production of angiotensin II.

摘要翻译： PCT No.PCT / JP95 / 01485第 371日期：1996年3月28日 102（e）1996年3月28日PCT PCT 1995年7月26日PCT公布。 出版物WO96 / 04248 日期：1996年2月15日本发明涉及由以下通式（1）表示的咪唑烷衍生物：其中A和B分别表示可被1-3个选自以下的取代基取代的芳族烃基：卤素 原子，C 1-4烷基，C 1-4烷氧基，C 1-4亚烷基二氧基，苯氧基，硝基，氰基，苯基，C 2-5烷酰基氨基，可被酯化的羧基 可以被C 1-4烷基或链烯基酯化的羧基烷基，可被C 1-4烷基或链烯基酯化的羧基烷氧基，N-烷基哌嗪基羰基，N-烷基哌嗪基羰基烷基， ，N-烷基哌嗪基羰基烷氧基和吗啉代羰基; X表示磺酰基或羰基; Y表示氧或硫原子，包含与活性成分相同的胃促胰酶抑制剂和包含其作为活性成分的药物，以心脏或循环系统疾病的预防和治疗剂为代表，其中 是由血管紧张素II的异常加速引起的。

公开(公告)号：US5424310A

公开(公告)日：1995-06-13

申请号：US79925

申请日：1993-06-23

申请人： Harukazu Fukami ,  Masaki Hashimoto ,  Shinjiro Niwata ,  Jun Imose ,  Harumoto Kawaguchi ,  Toshio Takahashi

发明人： Harukazu Fukami ,  Masaki Hashimoto ,  Shinjiro Niwata ,  Jun Imose ,  Harumoto Kawaguchi ,  Toshio Takahashi

IPC分类号： A61K31/53 ,  A61P33/02 ,  C07D401/12 ,  C07D403/12 ,  C07D413/12 ,  C07D417/12 ,  C07D253/075

CPC分类号： C07D401/12 ,  C07D403/12 ,  C07D413/12 ,  C07D417/12

摘要： A substituted 1,2,4-triazine-3,5-dione derivative having the formula (I) or a salt thereof: ##STR1## wherein R represents a 5- or 6-membered heterocyclic group which may have at least one substituent selected from the group consisting of a halogen, a lower alkyl group and a halogenated lower alkyl group, and an anticoccidial drug composition containing the same as an active component.

摘要翻译： 具有式（I）的取代的1,2,4-三嗪-3,5-二酮衍生物或其盐：其中R表示可以具有至少5或6元杂环基 选自卤素，低级烷基和卤代低级烷基的一个取代基和含有它们作为活性组分的抗球虫药物组合物。

公开(公告)号：US5039696A

公开(公告)日：1991-08-13

申请号：US473632

申请日：1990-02-01

申请人： Shinjiro Niwata ,  Harukazu Fukami ,  Masaki Hashimoto ,  Norio Ohtsuka ,  Fumio Fujita

发明人： Shinjiro Niwata ,  Harukazu Fukami ,  Masaki Hashimoto ,  Norio Ohtsuka ,  Fumio Fujita

IPC分类号： C07D207/452 ,  A01N37/46 ,  C07D207/44 ,  C07D207/456

CPC分类号： C07D207/456 ,  A01N37/46

摘要： A maleimide derivative useful as an active agent for a fungicide for agriculture and horticulture, having the formula (I): ##STR1## wherein X and Y each independently represent a hydrogen atom, a halogen atom, a hydroxyl group, a lower alkyl group, a lower alkoxy group, an aralkyloxy group or a trifluoromethyl group,Z represents a chlorine atom or bromine atom,and R represents a straight or branched alkyl group having 1 to 15 carbon atoms, an alkenyl group having 2 to 5 carbon atoms, an alkynyl group having 2 to 5 carbon atoms, an alkoxyalkyl group having 2 to 5 carbon atoms, an oxoalkyl group having 3 to 6 carbon atoms or a phenyl group or a phenyl alkyl group which may be substituted.

公开(公告)号：US5141551A

公开(公告)日：1992-08-25

申请号：US631978

申请日：1990-12-21

申请人： Naoko Kawaguchi ,  Harukazu Fukami ,  Shinjiro Niwata ,  Ryuichi Sago ,  Fumio Fujita

发明人： Naoko Kawaguchi ,  Harukazu Fukami ,  Shinjiro Niwata ,  Ryuichi Sago ,  Fumio Fujita

IPC分类号： A01N43/84 ,  C07D265/36 ,  C07D279/16 ,  C07D413/12 ,  C07D417/12

CPC分类号： C07D413/10 ,  A01N43/84 ,  C07D265/36 ,  C07D279/16 ,  C07D417/12

摘要： A benzoxazine derivative and a benzothiazine derivative having the formula (I): ##STR1## wherein A is N or a CH group;B is O, S, and SO group or an SO.sub.2 group;W is O, S, a CR.sup.4 R.sup.5 group or an NR.sup.4 group wherein R.sup.4 and R.sup.5 are each independently a hydrogen atom, a CN group or an NO.sub.2 group;X, Y and Z are each independently a hydrogen atom, a halogen atom or a lower haloalkyl group having 1 to 3 carbon atoms;R.sup.1 is a hydrogen atom, a lower alkyl group having 1 to 5 carbon atoms, a lower alkenyl group having 2 to 5 carbon atoms, a lower alkynyl group having 2 to 5 carbon atoms, a lower hydroxyalkyl group having 1 to 5 carbon atoms or a lower haloalkyl group having 1 to 3 carbon atoms; andR.sup.2 and R.sup.3 are each independently a hydrogen atom, a lower alkyl group having 1 to 5 carbon atoms or an aryl group having 6 to 10 carbon atoms and a herbicidal composition containing the compound of the formula (I) as an active ingredient.

公开(公告)号：US4945104A

公开(公告)日：1990-07-31

申请号：US370800

申请日：1989-06-23

申请人： Harukazu Fukami ,  Masaki Hashimoto ,  Shinjiro Niwata ,  Norio Ohtsuka ,  Fumio Fujita

发明人： Harukazu Fukami ,  Masaki Hashimoto ,  Shinjiro Niwata ,  Norio Ohtsuka ,  Fumio Fujita

IPC分类号： C07D207/452 ,  A01N37/32 ,  A01N39/00 ,  A01N43/36 ,  C07D207/44 ,  C07D207/456

CPC分类号： C07D207/456 ,  A01N39/00

摘要： A maleimide derivative having the formula (I): ##STR1## wherein R.sub.1 represents a lower alkyl group having 1 to 4 carbon atoms, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 independently represent a hydrogen atom, a lower alkyl group having 1 to 4 carbon atoms, a phenyl group which may be substituted, or an aralkyl group having 7 to 10 carbon atoms, and X.sub.1 and X.sub.2 independently represent a hydrogen atom or a halogen atom, and a production process thereof as well as a agricultural and horticultural fungicide containing, as an active ingredient, the maleimide derivative.

公开(公告)号：US5399743A

公开(公告)日：1995-03-21

申请号：US121461

申请日：1993-09-16

申请人： Naoki Higuchi ,  Masayuki Saitoh ,  Shinjiro Niwata ,  Yoshinobu Kiso ,  Yasuhiro Hayashi

发明人： Naoki Higuchi ,  Masayuki Saitoh ,  Shinjiro Niwata ,  Yoshinobu Kiso ,  Yasuhiro Hayashi

IPC分类号： A61K31/16 ,  A61K31/27 ,  A61P3/00 ,  A61P3/14 ,  A61P19/10 ,  A61P43/00 ,  C07C237/22 ,  C07C271/22 ,  C07C261/00 ,  C07C233/00

CPC分类号： C07C271/22 ,  C07C237/22

摘要： A dipeptide derivative having the formula (I):R.sup.1 NH--CH(R.sup.2)--CO--NH--CH(R.sup.3)--COCH.sub.2 F (I)wherein, R.sup.1 is an aliphatic acyl group having 2 to 8 carbon atoms or a benzyloxycarbonyl group; andR.sup.2 and R.sup.3 are independently a hydrogen atom or a straight or branched alkyl group having 1 to 4 carbon atoms and a prophylactic or therapeutic agent containing the same as an active ingredient.

摘要翻译： 具有式（I）的二肽衍生物：R1NH-CH（R2）-CO-NH-CH（R3）-COCH2F（Ⅰ）其中，R1是碳原子数2〜8的脂肪族酰基或苄氧羰基; R2和R3独立地为氢原子或碳原子数为1〜4的直链或支链状的烷基以及含有该活性成分的预防或治疗剂。

公开(公告)号：US5395824A

公开(公告)日：1995-03-07

申请号：US969453

申请日：1992-10-30

申请人： Naoki Higuchi ,  Masayuki Saitoh ,  Shinjiro Niwata ,  Yoshinobu Kiso ,  Yasuhiro Hayashi

发明人： Naoki Higuchi ,  Masayuki Saitoh ,  Shinjiro Niwata ,  Yoshinobu Kiso ,  Yasuhiro Hayashi

IPC分类号： A61K31/335 ,  A61K31/357 ,  A61K38/00 ,  A61P3/02 ,  A61P3/14 ,  A61P19/10 ,  A61P43/00 ,  C07C237/12 ,  C07C237/22 ,  C07C251/38 ,  C07C271/22 ,  C07C281/10 ,  C07C323/41 ,  C07D235/14 ,  C07D277/04 ,  C07D317/28 ,  C07D327/04 ,  C07D339/06 ,  C07D339/08 ,  A61K37/02

CPC分类号： C07D327/04 ,  C07C237/22 ,  C07C251/38 ,  C07C271/22 ,  C07C281/10 ,  C07C323/41 ,  C07D235/14 ,  C07D277/04 ,  C07D317/28 ,  C07D339/06 ,  C07D339/08

摘要： A prophylactic or therapeutic agent for malignant hypercalcemia, bone Paget's disease and osteoporosis is disclosed, which contains as an active ingredient a dipeptide derivative represented by formula:R.sup.1 NH--CH(R.sup.2)--CO--NH--CH(R.sup.3)--R.sup.4 (I)wherein R.sup.1 represents an aliphatic acyl group, a halogen-substituted aliphatic acyl group, or benzyloxycarbonyl group; R.sup.2 represents a lower alkyl group or an aralkyl group; R.sup.3 represents a lower alkyl group, an aralkyl group, or methylthioethyl group; R.sup.4 represents formyl group, an aliphatic acyl group, an aliphatic acyl group substituted with a halogen atom or a lower alkoxycarbonyl group, a di-lower alkoxymethyl group, a diacyloxymethyl group, a lower alkoxalyl group, a 1-hydroxy-2-lower alkoxycarbonylethyl group, a halogen-substituted 1-hydroxy-2-lower alkoxycarbonylethyl group, hydroxyiminomethyl group, ureidoiminomethyl group, benzimidazol-2-yl group, or a group: ##STR1## wherein A and B, which may be the same or different, each represents O, S, NH; and n represents 2 or 3; provided that R.sup.4 is not a formyl group when R.sup.3 is an n-butyl group.

摘要翻译： 公开了用于恶性高钙血症，骨佩吉特氏病和骨质疏松症的预防或治疗剂，其包含作为活性成分的由式：R1NH-CH（R2）-CO-NH-CH（R3）-R4（I）表示的二肽衍生物， 其中R1表示脂族酰基，卤素取代的脂族酰基或苄氧基羰基; R2表示低级烷基或芳烷基; R3表示低级烷基，芳烷基或甲硫基乙基; R4表示甲酰基，脂肪族酰基，被卤素原子或低级烷氧基羰基取代的脂族酰基，二低级烷氧基甲基，二酰氧基甲基，低级烷氧基，1-羟基-2-低级烷氧基羰基乙基 基团，卤素取代的1-羟基-2-低级烷氧基羰基乙基，羟基亚氨基甲基，脲基亚氨基甲基，苯并咪唑-2-基或基团：其中A和B各自可以相同或不同 表示O，S，NH; n表示2或3; 条件是当R 3为正丁基时，R 4不是甲酰基。