公开(公告)号：US5922767A

公开(公告)日：1999-07-13

申请号：US946098

申请日：1997-10-07

申请人： Yoshihiko Kanamaru ,  Hiroyuki Hirota ,  Akihiro Shibata ,  Teruo Komoto ,  Hiroyuki Naito ,  Koichi Tachibana ,  Mari Ohtsuka ,  Fumio Ishii ,  Susumu Sato

发明人： Yoshihiko Kanamaru ,  Hiroyuki Hirota ,  Akihiro Shibata ,  Teruo Komoto ,  Hiroyuki Naito ,  Koichi Tachibana ,  Mari Ohtsuka ,  Fumio Ishii ,  Susumu Sato

IPC分类号： C07C275/28 ,  C07D213/30 ,  C07D307/42 ,  C07D333/16 ,  A61K31/17 ,  C07C275/06

CPC分类号： C07D213/30 ,  C07C275/28 ,  C07D307/42 ,  C07D333/16

摘要： Disclosed herein are substituted benzylurea derivatives represented by the following general formula (1): ##STR1## wherein R.sup.1 and R.sup.2 are independently H, a halogen atom, or an alkyl or alkoxyl group, R.sup.3 is a phenyl or heterocyclic group which may be substituted, n is an integer of 1-6, and R.sup.4 is a phenyl group which may be substituted, or salts thereof, and medicines comprising such a derivative as an active ingredient. The derivatives or salts thereof strongly inhibit only ACAT in macrophages and are hence useful as prophylactic and therapeutic agents for arteriosclerosis.

摘要翻译： 本文公开了由以下通式（1）表示的取代的苄基脲衍生物：其中R 1和R 2独立地为H，卤素原子或烷基或烷氧基，R 3为可被取代的苯基或杂环基，n为 1-6的整数，R4是可被取代的苯基或其盐，以及包含这种衍生物作为活性成分的药物。 其衍生物或盐在巨噬细胞中仅强烈地抑制ACAT，因此可用作动脉硬化的预防和治疗剂。

公开(公告)号：US5866609A

公开(公告)日：1999-02-02

申请号：US899647

申请日：1997-07-24

申请人： Yoshihiko Kanamaru ,  Hiroyuki Hirota ,  Akihiro Shibata ,  Teruo Komoto ,  Hiroyuki Naito ,  Koichi Tachibana ,  Mari Ohtsuka ,  Fumio Ishii ,  Susumu Sato

发明人： Yoshihiko Kanamaru ,  Hiroyuki Hirota ,  Akihiro Shibata ,  Teruo Komoto ,  Hiroyuki Naito ,  Koichi Tachibana ,  Mari Ohtsuka ,  Fumio Ishii ,  Susumu Sato

IPC分类号： C07C275/28 ,  C07C275/30 ,  C07C275/34 ,  C07C275/40 ,  C07C275/42 ,  C07C317/42 ,  C07C323/44 ,  C07D211/58 ,  C07D317/58 ,  C07D317/66 ,  A61K31/17 ,  C07C275/04

CPC分类号： C07C317/42 ,  C07C275/28 ,  C07C275/30 ,  C07C275/34 ,  C07C275/40 ,  C07C275/42 ,  C07C323/44 ,  C07D211/58 ,  C07D317/58 ,  C07D317/66 ,  C07C2101/14

摘要： Disclosed herein are substituted vinylurea derivatives represented by the following general formula (1): ##STR1## wherein R.sup.1 and R.sup.3 are independently a phenyl group which may be substituted, R.sup.2 is a phenyl group which may be substituted, or a cycloalkyl group, and wave lines mean that the bonding state may be either E or Z, with the proviso that the cases where R.sup.1, R.sup.2 and R.sup.3 are unsubstituted phenyl groups, and where R.sup.1 and R.sup.2 are unsubstituted phenyl groups and R.sup.3 is a 4-ethoxyphenyl group are excluded, or salt thereof, and medicines comprising such a derivative as an active ingredient as well as a method of preventing and treating arteriosclerosis with such a medicine. The derivatives or salts thereof selectively and strongly inhibit ACAT in macrophages and are hence useful as prophylactic and therapeutic agents for arteriosclerosis.

摘要翻译： 本文公开了由以下通式（1）表示的取代的乙烯基脲衍生物：其中R 1和R 3独立地为可被取代的苯基，R 2为可被取代的苯基或环烷基 并且波线意味着键合状态可以是E或Z，条件是其中R1，R2和R3是未取代的苯基，R1和R2是未取代的苯基，R3是4-乙氧基苯基的情况 或其盐，以及包含这样的衍生物作为活性成分的药物，以及用这种药物预防和治疗动脉硬化的方法。 其衍生物或其盐在巨噬细胞中选择性且强烈地抑制ACAT，因此可用作动脉硬化的预防和治疗剂。

公开(公告)号：US06362203B1

公开(公告)日：2002-03-26

申请号：US09698041

申请日：2000-10-30

申请人： Kinichi Mogi ,  Yoshihiko Kanamaru ,  Noriyuki Kawamoto ,  Teruo Komoto ,  Norimitsu Umehara ,  Susumu Sato ,  Tetsuo Oka

发明人： Kinichi Mogi ,  Yoshihiko Kanamaru ,  Noriyuki Kawamoto ,  Teruo Komoto ,  Norimitsu Umehara ,  Susumu Sato ,  Tetsuo Oka

IPC分类号： C07D21152

CPC分类号： C07D211/52

摘要： Described is a 4-hydroxy-4-phenylpiperidine derivative represented by the following formula (1): [wherein, R1 and R2 are the same or different and each independently represents a hydrogen atom, a lower alkyl, or the like, R3 represents a hydrogen atom or a group —(CR4R5)n—Y (in which, R4 and R5 each represents a hydrogen atom or a lower alkyl group, Y represents a group —COOR6, —CONR7R8, —OR9 or —OCOR10 (in which R6, R9 and R10 each independently represents a hydrogen atom, a lower alkyl group, or the like, R7 and R8 are the same or different and each independently represents a hydrogen atom, a lower alkyl group, or the like), and n stands for 1 to 6)], or salt thereof. The compound exhibits excellent peripheral analgesic action.

摘要翻译： 描述了由下式（1）表示的4-羟基-4-苯基哌啶衍生物：[其中，R 1和R 2相同或不同，各自独立地表示氢原子，低级烷基等，R 3表示 氢原子或基团 - （CR 4 R 5）n Y（其中，R 4和R 5各自表示氢原子或低级烷基，Y表示-COOR 6，-CONR 7 R 8，-OR 9或-OCOR 10（其中R 6，R 9和 R 10各自独立地表示氢原子，低级烷基等，R 7和R 8相同或不同，各自独立地表示氢原子，低级烷基等），n表示1〜6 ）]或其盐。该化合物表现出优异的外周镇痛作用。

公开(公告)号：US5147886A

公开(公告)日：1992-09-15

申请号：US626545

申请日：1990-12-12

申请人： Minoru Tokizawa ,  Yoshihiko Kanamaru ,  Masaru Matsumoto ,  Takemitsu Asaoka ,  Hideaki Matsuda ,  Tadayuki Kuraishi ,  Kazunori Maebashi ,  Naokata Taido ,  Ryuichi Kawahara

发明人： Minoru Tokizawa ,  Yoshihiko Kanamaru ,  Masaru Matsumoto ,  Takemitsu Asaoka ,  Hideaki Matsuda ,  Tadayuki Kuraishi ,  Kazunori Maebashi ,  Naokata Taido ,  Ryuichi Kawahara

IPC分类号： C07D249/08 ,  C07D521/00

CPC分类号： C07D231/12 ,  C07D233/56 ,  C07D249/08

摘要： A triazole derivative is disclosed. The compound have a general formula, ##STR1## wherein R.sup.1 and R.sup.2 represent a hydrogen atom or a lower alkyl group, or R.sup.1 and R.sup.2 together form a lower alkylene group, R.sup.3 represents a lower alkyl group, and n denotes an integer of 0 to 2, provided that not both R.sup.1 and R.sup.2 are a hydrogen atom at the same time. The triazole derivatives and their salts are effective for curing or preventing deep-seated mycoses, e.g. mycotic meningitis, mycotic infectious diseases of respiratory organs, fungemia, and urinary tract mycosis.

公开(公告)号：US4987144A

公开(公告)日：1991-01-22

申请号：US412152

申请日：1989-09-25

申请人： Yoshihiko Kanamaru ,  Minoru Tokizawa ,  Masaru Matsumoto ,  Takemitsu Asaoka ,  Hideaki Matsuda ,  Tadayuki Kuraishi

发明人： Yoshihiko Kanamaru ,  Minoru Tokizawa ,  Masaru Matsumoto ,  Takemitsu Asaoka ,  Hideaki Matsuda ,  Tadayuki Kuraishi

IPC分类号： A61K31/41 ,  A61P31/04 ,  A61P31/10 ,  C07D249/08 ,  C07D521/00

CPC分类号： C07D249/08 ,  C07D231/12 ,  C07D233/56

摘要： Disclosed herein is 1,3-bis(1,2,4-triazol-1-yl)-2-(4-trifluoromethylphenyl)propan-2-ol represented by the following formula (I): ##STR1## An antimycotic preparation containing the triazole compound (I) is also disclosed. Also disclosed is a method for the prevention and/treatment of a deep-seated mycosis of a human or mammal, which comprises administering an effective dose of the triazole compound (I) to the human or mammal.