公开(公告)号：US20050054668A1

公开(公告)日：2005-03-10

申请号：US10969440

申请日：2004-10-19

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

IPC分类号： A61K31/357 ,  A61K31/41 ,  A61K31/427 ,  A61K31/4433 ,  A61K31/47 ,  A61K31/498 ,  A61K31/538 ,  A61K45/00 ,  A61P1/04 ,  A61P1/18 ,  A61P3/10 ,  A61P9/00 ,  A61P9/10 ,  A61P11/00 ,  A61P11/06 ,  A61P13/12 ,  A61P29/00 ,  A61P37/00 ,  A61P37/02 ,  A61P37/08 ,  A61P43/00 ,  C07D215/48 ,  C07D241/42 ,  C07D241/44 ,  C07D265/36 ,  C07D319/18 ,  C07D401/12 ,  C07D405/12 ,  C07D407/12 ,  C07D409/12 ,  C07D417/12 ,  C07D491/02 ,  A61K31/4745 ,  C07D471/02 ,  C07D498/02

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。

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。

公开(公告)号：US06670364B2

公开(公告)日：2003-12-30

申请号：US10060967

申请日：2002-01-29

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： A61P2900

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.

摘要翻译： 本发明涉及化合物，包含所述化合物的药物组合物，所述化合物和组合物的用途，使用所述化合物和组合物的治疗方法，以及制备所述化合物的方法。 具体而言，本发明涉及作为MCP-1功能的拮抗剂的新化合物，其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，例如关节炎，哮喘，动脉粥样硬化， 糖尿病肾病，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。 更具体地，本发明涉及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：US06962926B2

公开(公告)日：2005-11-08

申请号：US10637746

申请日：2003-08-08

申请人： Edgardo Laborde ,  Louise Robinson ,  Fanying Meng ,  Brian T. Peterson ,  Hugo O. Villar ,  Steven E. Anuskiewicz ,  Wenli Ma ,  Yukiharu Matsumoto ,  Kunihisa Baba ,  Hideaki Inagaki ,  Katsumasa Tanaka ,  Yoshiro Ishiwata ,  Shoji Yokochi ,  Masayuki Okamoto ,  Takashi Nakamura ,  Atsushi Miyachi ,  Mitsuaki Takeuchi ,  Kouji Matsushima

发明人： Edgardo Laborde ,  Louise Robinson ,  Fanying Meng ,  Brian T. Peterson ,  Hugo O. Villar ,  Steven E. Anuskiewicz ,  Wenli Ma ,  Yukiharu Matsumoto ,  Kunihisa Baba ,  Hideaki Inagaki ,  Katsumasa Tanaka ,  Yoshiro Ishiwata ,  Shoji Yokochi ,  Masayuki Okamoto ,  Takashi Nakamura ,  Atsushi Miyachi ,  Mitsuaki Takeuchi ,  Kouji Matsushima

IPC分类号： A61K31/437 ,  A61K31/496 ,  A61K31/5377 ,  A61K31/5513 ,  A61K45/06 ,  A61P29/00 ,  C07D471/04 ,  C07D498/04 ,  C07D519/00 ,  C61K31/5377

CPC分类号： A61K31/437 ,  A61K9/0019 ,  A61K9/2054 ,  A61K9/4866 ,  A61K31/496 ,  A61K31/5377 ,  A61K31/5513 ,  A61K45/06 ,  C07D231/56 ,  C07D471/04 ,  A61K2300/00

摘要： Compounds of formula A and formula B: and their pharmaceutically acceptable salts, compositions comprising them, methods for their use, and their use in the preparation of medicaments. The compounds are antagonists of MCP-1 function, and are useful in the prevention and treatment of chronic or acute inflammatory or autoimmune diseases, such as multiple sclerosis, and in the prevention and treatment of allergic hypersensitivity disorders.

摘要翻译： 式A和式B化合物及其药学上可接受的盐，包含它们的组合物，其使用方法及其在制备药物中的用途。 该化合物是MCP-1功能的拮抗剂，可用于预防和治疗慢性或急性炎性或自身免疫性疾病如多发性硬化，以及预防和治疗过敏性超敏反应性疾病。

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：US06251689B1

公开(公告)日：2001-06-26

申请号：US09313568

申请日：1999-05-14

申请人： Edgardo Laborde ,  Yukiharu Matsumoto

发明人： Edgardo Laborde ,  Yukiharu Matsumoto

IPC分类号： G01N33543

CPC分类号： C07D277/66 ,  C07B2200/11 ,  C07D235/18 ,  C07D235/30 ,  C07D263/57 ,  C07D263/58 ,  C40B40/00

摘要： The present invention provides an efficient and versatile method for the synthesis and screening of combinatorial libraries of benzimidazoles, benzoxazoles, benzothiazoles, and derivatives thereof. In order to expedite the synthesis of large arrays of compounds possessing these core structures, a general methodology for solid phase synthesis of these derivatives is provided. Arrays of benzimidazoles, benzoxazoles, benzothiazoles, and derivatives thereof useful as peptidomimetics and for the identification of agents having antifungal, antiviral, antimicrobial, anticoagulant, and antiulcer activity, or use in the treatment of inflammation, hypertension, cancer, and other conditions can be prepared by this method.

摘要翻译： 本发明提供了用于合成和筛选苯并咪唑，苯并恶唑，苯并噻唑及其衍生物的组合文库的有效且通用的方法。 为了加速具有这些核心结构的大阵列化合物的合成，提供了这些衍生物的固相合成的一般方法。 可用作肽模拟物和用于鉴定具有抗真菌，抗病毒，抗微生物，抗凝血和抗溃疡活性的药物的苯并咪唑，苯并恶唑，苯并噻唑及其衍生物的阵列，或用于治疗炎症，高血压，癌症和其它病症的阵列可以是 通过这种方法准备。