公开(公告)号：US4870062A

公开(公告)日：1989-09-26

申请号：US183575

申请日：1988-04-19

申请人： Masayasu Kurono ,  Ryoichi Unno ,  Yukiharu Matsumoto ,  Yasuaki Kondo ,  Takahiko Mitani ,  Takahito Jomori ,  Hisashi Michishita ,  Kiichi Sawai

发明人： Masayasu Kurono ,  Ryoichi Unno ,  Yukiharu Matsumoto ,  Yasuaki Kondo ,  Takahiko Mitani ,  Takahito Jomori ,  Hisashi Michishita ,  Kiichi Sawai

IPC分类号： A61K31/28 ,  A61K31/282 ,  A61K31/55 ,  A61P35/00 ,  C07F15/00

CPC分类号： C07F15/0093

摘要： A removable rating plug for a circuit breaker provides an active variable impedance in series with a reference resistor between the sensing terminals of the circuit breaker trip circuit to adjust the sensing voltage produced in response to the input current received from current monitors in the protected circuit. The active variable impedance, which is energized by the input current, includes a high gain transistor amplifier, preferably a Darlington transistor, controlled by an operational amplifier. A control circuit includes a pair of reference diodes which match the forward drop across the Darlington transistor when full on, in series with a reference voltage selection circuit which applies a reference voltage to the non-inverting input of the operational amplifier. The voltage at the connection between the Darlington transistor and the reference resistor is fed back to the inverting input of the operational amplifier so that the gain of the amplifier, and therefore the variable impedance in series with the reference resistor, varies with the reference voltage.

公开(公告)号：US4897495A

公开(公告)日：1990-01-30

申请号：US351006

申请日：1989-05-12

申请人： Masayasu Kurono ,  Yasuaki Kondo ,  Ryoichi Unno ,  Yukiharu Matsumoto ,  Hiromoto Kimura ,  Mitsuru Oka ,  Kiichi Sawai

发明人： Masayasu Kurono ,  Yasuaki Kondo ,  Ryoichi Unno ,  Yukiharu Matsumoto ,  Hiromoto Kimura ,  Mitsuru Oka ,  Kiichi Sawai

IPC分类号： C07D487/04

CPC分类号： C07D487/04

摘要： A process for the preparation of pyrrolizine derivatives of the formula ##STR1## wherein R is --CN or --CH.sub.2 NH.sub.2, and salts thereof.

公开(公告)号：US4985569A

公开(公告)日：1991-01-15

申请号：US350990

申请日：1989-05-12

申请人： Masayasu Kurono ,  Yasuaki Kondo ,  Ryoichi Unno ,  Yukiharu Matsumoto ,  Hiromoto Kimura ,  Mitsuru Oka ,  Kiichi Sawai

发明人： Masayasu Kurono ,  Yasuaki Kondo ,  Ryoichi Unno ,  Yukiharu Matsumoto ,  Hiromoto Kimura ,  Mitsuru Oka ,  Kiichi Sawai

IPC分类号： C07D487/04

CPC分类号： C07D487/04

摘要： 7a-Nitromethyl-2,3,5,6,7,7a-hexahydro-1H-pyrrolizine of the formula ##STR1## and salts thereof, as well as processes for the preparation of the compound and 7a-aminomethyl-2,3,5,6,7,7a-hexahydro-1H-pyrrolizine and salts thereof.

公开(公告)号：US5110945A

公开(公告)日：1992-05-05

申请号：US776039

申请日：1991-10-15

申请人： Masayasu Kurono ,  Yasuaki Kondo ,  Yukiharu Matsumoto ,  Mitsuru Oka ,  Kiichi Sawai

发明人： Masayasu Kurono ,  Yasuaki Kondo ,  Yukiharu Matsumoto ,  Mitsuru Oka ,  Kiichi Sawai

IPC分类号： C07D487/04

CPC分类号： C07D487/04

摘要： There are described 1-azoniabicyclo[3.3.0]oct-1(5)-ene salt derivatives inclusive of 1-azonia-4,6-dimethylbicyclo[3.3.0]oct-1(5)-ene perchlorate, and a process for the preparation of the same. The derivatives can be prepared by heating dicyclopropylmethanimine salt derivative in a solvent, in the presence or absence of an ammonium salt. Each of the derivatives is employed as an intermediate for preparing various medicines and agricultural chemicals.

公开(公告)号：US4939126A

公开(公告)日：1990-07-03

申请号：US217523

申请日：1988-07-11

申请人： Masayasu Kurono ,  Tsunemasa Suzuki ,  Tomoo Suzuki ,  Kiyotaka Hirooka ,  Yukiharu Matsumoto ,  Hiroshi Ozawa ,  Kiichi Sawai

发明人： Masayasu Kurono ,  Tsunemasa Suzuki ,  Tomoo Suzuki ,  Kiyotaka Hirooka ,  Yukiharu Matsumoto ,  Hiroshi Ozawa ,  Kiichi Sawai

IPC分类号： C07F7/10 ,  A61K31/695 ,  A61P25/28 ,  C07F7/08

CPC分类号： C07F7/0812

摘要： 1-Pyrrolidineacetamide derivatives of the formula ##STR1## wherein R.sub.1 is hydrogen atom or a trialkylsilyl group, R.sub.2 and R.sub.3 are hydrogen atom, respectively, when R.sub.1 is hydrogen atom, R.sub.4 is an alkyl group, R.sub.5 is a radical of ##STR2## in which R.sub.6 and R.sub.7 are an alkyl group, respectively, m and n are an integer of 1 to 3, respectively,or R.sub.4 represents together with R.sub.5 a hetero cyclic ring having nitrogen and silicon atoms or piperazine ring having a substituent of ##STR3## in which R.sub.6 and n have the meanings as referred to, and R.sub.2 and R.sub.4 as well as R.sub.3 and R.sub.5 form a hetero cyclic ring, respectively, connected with an alkylene chain, where R.sub.1 is the trialkylsilyl group, salts thereof, a process for the preparation thereof, as well as use thereof as for a medicine.

公开(公告)号：US06809113B2

公开(公告)日：2004-10-26

申请号：US10087208

申请日：2002-02-27

申请人： Edgardo Laborde ,  Louise Robinson ,  Fanying Meng ,  Brian T. Peterson ,  Hugo O. Villar ,  Steven E. Anuskiewicz ,  Yoshiro Ishiwata ,  Shoji Yokochi ,  Yukiharu Matsumoto ,  Takuji Kakigami ,  Hideaki Inagaki ,  Takahito Jomori ,  Kouji Matsushima

发明人： Edgardo Laborde ,  Louise Robinson ,  Fanying Meng ,  Brian T. Peterson ,  Hugo O. Villar ,  Steven E. Anuskiewicz ,  Yoshiro Ishiwata ,  Shoji Yokochi ,  Yukiharu Matsumoto ,  Takuji Kakigami ,  Hideaki Inagaki ,  Takahito Jomori ,  Kouji Matsushima

IPC分类号： A61K3135

CPC分类号： C07D401/12 ,  C07D215/48 ,  C07D241/42 ,  C07D265/36 ,  C07D319/18 ,  C07D405/12 ,  C07D407/12 ,  C07D409/12 ,  C07D417/12

摘要： Compounds which are antagonists of MCP-1 function and are useful in the prevention or treatment of chronic or acute inflammatory or autoimmune diseases, especially those associated with aberrant lymphocyte or monocyte accumulation such as arthritis, asthma, atherosclerosis, diabetic nephropathy, inflammatory bowel disease, Crohn's disease, multiple sclerosis, nephritis, pancreatitis, pulmonary fibrosis, psoriasis, restenosis, and transplant rejection; pharmaceutical compositions comprising these compounds; and the use of these compounds and compositions in the prevention or treatment of such diseases.

摘要翻译： 作为MCP-1拮抗剂的化合物起作用，可用于预防或治疗慢性或急性炎性或自身免疫性疾病，特别是与异常淋巴细胞或单核细胞积累相关的疾病如关节炎，哮喘，动脉粥样硬化，糖尿病性肾病，炎性肠病， 克罗恩病，多发性硬化，肾炎，胰腺炎，肺纤维化，牛皮癣，再狭窄和移植排斥反应; 包含这些化合物的药物组合物; 以及这些化合物和组合物在预防或治疗这些疾病中的用途。

公开(公告)号：US06998407B2

公开(公告)日：2006-02-14

申请号：US10716652

申请日：2003-11-18

申请人： Edgardo Laborde ,  Louise Robinson ,  Fanying Meng ,  Brian T. Peterson ,  Hugo O. Villar ,  Steven E. Anuskiewicz ,  Yoshiro Ishiwata ,  Shoji Yokochi ,  Yukiharu Matsumoto ,  Takuji Kakigami ,  Hideaki Inagaki ,  Takahito Jomori ,  Kouji Matsushima

发明人： Edgardo Laborde ,  Louise Robinson ,  Fanying Meng ,  Brian T. Peterson ,  Hugo O. Villar ,  Steven E. Anuskiewicz ,  Yoshiro Ishiwata ,  Shoji Yokochi ,  Yukiharu Matsumoto ,  Takuji Kakigami ,  Hideaki Inagaki ,  Takahito Jomori ,  Kouji Matsushima

IPC分类号： A61K31/36 ,  A61K31/343 ,  C07D307/79 ,  C07D317/60

CPC分类号： C07D235/06 ,  C07D209/08 ,  C07D249/18 ,  C07D263/56 ,  C07D307/79 ,  C07D317/68 ,  C07D405/12 ,  C07D407/12 ,  C07D409/12 ,  C07D417/12

摘要： Chemical compounds which are antagonists of Monocyte Chemoattractant Protein-1 (MCP-1) function, pharmaceutical compositions comprising these compounds, methods of treatment employing these compounds and compositions, and processes for preparing these compounds. The compounds are useful in the prevention or treatment of chronic or acute inflammatory or autoimmune diseases, especially those associated with aberrant lymphocyte or monocyte accumulation such as arthritis, asthma, atherosclerosis, diabetic nephropathy, inflammatory bowel disease, Crohn's disease, multiple sclerosis, nephritis, pancreatitis, pulmonary fibrosis, psoriasis, restenosis, and transplant rejection.

摘要翻译： 作为单核细胞趋化蛋白-1（MCP-1）功能拮抗剂的化合物，包含这些化合物的药物组合物，使用这些化合物和组合物的治疗方法，以及制备这些化合物的方法。 该化合物可用于预防或治疗慢性或急性炎性或自身免疫疾病，特别是与异常淋巴细胞或单核细胞积累相关的疾病，如关节炎，哮喘，动脉粥样硬化，糖尿病性肾病，炎性肠病，克罗恩病，多发性硬化，肾炎， 胰腺炎，肺纤维化，牛皮癣，再狭窄和移植排斥。

公开(公告)号：US06992086B2

公开(公告)日：2006-01-31

申请号：US10716363

申请日：2003-11-17

申请人： Edgardo Laborde ,  Louise Robinson ,  Fanying Meng ,  Brian T. Peterson ,  Hugo O. Villar ,  Steven E. Anuskiewicz ,  Yoshiro Ishiwata ,  Shoji Yokochi ,  Yukiharu Matsumoto ,  Takuji Kakigami ,  Hideaki Inagaki ,  Takahito Jomori ,  Kouji Matsushima

发明人： Edgardo Laborde ,  Louise Robinson ,  Fanying Meng ,  Brian T. Peterson ,  Hugo O. Villar ,  Steven E. Anuskiewicz ,  Yoshiro Ishiwata ,  Shoji Yokochi ,  Yukiharu Matsumoto ,  Takuji Kakigami ,  Hideaki Inagaki ,  Takahito Jomori ,  Kouji Matsushima

IPC分类号： A61K31/496 ,  A61K31/437 ,  C07D498/04 ,  C07D471/04 ,  A61P37/00

CPC分类号： C07D471/04 ,  A61K31/437 ,  A61K31/496 ,  A61K31/5377 ,  A61K31/5513 ,  A61K45/06 ,  A61K2300/00

摘要： The present invention relates to chemical compounds, pharmaceutical compositions comprising said compounds, uses of said compounds and compositions, methods of treatment employing said compounds and compositions, and processes for preparing said compounds. Specifically, this invention relates to novel compounds which are antagonists of MCP-1 function and are useful in the prevention or treatment of chronic or acute inflammatory or autoimmune diseases, especially those associated with aberrant lymphocyte or monocyte accumulation such as arthritis, asthma, atherosclerosis, diabetic nephropathy, inflammatory bowel disease, Crohn's disease, multiple sclerosis, nephritis, pancreatitis, pulmonary fibrosis, psoriasis, restenosis, and transplant rejection. More specifically, the invention is related to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases.

公开(公告)号：US06677365B2

公开(公告)日：2004-01-13

申请号：US10106881

申请日：2002-03-25

申请人： Edgardo Laborde ,  Louise Robinson ,  Fanying Meng ,  Brian T. Peterson ,  Hugo O. Villar ,  Steven E. Anuskiewicz ,  Yoshiro Ishiwata ,  Shoji Yokochi ,  Yukiharu Matsumoto ,  Takuji Kakigami ,  Hideaki Inagaki ,  Takahito Jomori ,  Kouji Matsushima

发明人： Edgardo Laborde ,  Louise Robinson ,  Fanying Meng ,  Brian T. Peterson ,  Hugo O. Villar ,  Steven E. Anuskiewicz ,  Yoshiro Ishiwata ,  Shoji Yokochi ,  Yukiharu Matsumoto ,  Takuji Kakigami ,  Hideaki Inagaki ,  Takahito Jomori ,  Kouji Matsushima

IPC分类号： A61K3142

CPC分类号： C07D235/06 ,  C07D209/08 ,  C07D249/18 ,  C07D263/56 ,  C07D307/79 ,  C07D317/68 ,  C07D405/12 ,  C07D407/12 ,  C07D409/12 ,  C07D417/12

摘要： Chemical compounds which are antagonists of Monocyte Chemoattractant Protein-1 (MCP-1) function, pharmaceutical compositions comprising these compounds, methods of treatment employing these compounds and compositions, and processes for preparing these compounds. The compounds are useful in the prevention or treatment of chronic or acute inflammatory or autoimmune diseases, especially those associated with aberrant lymphocyte or monocyte accumulation such as arthritis, asthma, atherosclerosis, diabetic nephropathy, inflammatory bowel disease, Crohn's disease, multiple sclerosis, nephritis, pancreatitis, pulmonary fibrosis, psoriasis, restenosis, and transplant rejection.

公开(公告)号：US07297696B2

公开(公告)日：2007-11-20

申请号：US10969440

申请日：2004-10-19

申请人： Edgardo Laborde ,  Louise Robinson ,  Fanying Meng ,  Brian T. Peterson ,  Hugo O. Villar ,  Steven E. Anuskiewicz ,  Yoshiro Ishiwata ,  Shoji Yokochi ,  Yukiharu Matsumoto ,  Takuji Kakigami ,  Hideaki Inagaki ,  Takahito Jomori ,  Kouji Matsushima

发明人： Edgardo Laborde ,  Louise Robinson ,  Fanying Meng ,  Brian T. Peterson ,  Hugo O. Villar ,  Steven E. Anuskiewicz ,  Yoshiro Ishiwata ,  Shoji Yokochi ,  Yukiharu Matsumoto ,  Takuji Kakigami ,  Hideaki Inagaki ,  Takahito Jomori ,  Kouji Matsushima

IPC分类号： A61K31/498 ,  C07D241/36

CPC分类号： C07D401/12 ,  C07D215/48 ,  C07D241/42 ,  C07D265/36 ,  C07D319/18 ,  C07D405/12 ,  C07D407/12 ,  C07D409/12 ,  C07D417/12

摘要： Compounds which are antagonists of MCP-1 function and are useful in the prevention or treatment of chronic or acute inflammatory or autoimmune diseases, especially those associated with aberrant lymphocyte or monocyte accumulation such as arthritis, asthma, atherosclerosis, diabetic nephropathy, inflammatory bowel disease, Crohn's disease, multiple sclerosis, nephrtitis, pancreatitis, pulmonary fibrosis, psoriasis, restenosis, and transplant rejection; pharmaceutical compositions comprising these compounds; and the use of these compounds and compositions in the prevention or treatment of such diseases.

摘要翻译： 作为MCP-1拮抗剂的化合物起作用，可用于预防或治疗慢性或急性炎性或自身免疫性疾病，特别是与异常淋巴细胞或单核细胞积累相关的疾病如关节炎，哮喘，动脉粥样硬化，糖尿病性肾病，炎性肠病， 克罗恩病，多发性硬化，肾炎，胰腺炎，肺纤维化，牛皮癣，再狭窄和移植排斥反应; 包含这些化合物的药物组合物; 以及这些化合物和组合物在预防或治疗这些疾病中的用途。