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公开(公告)号：US07087624B2
公开(公告)日：2006-08-08
申请号：US10693461
申请日：2003-10-27
申请人： Nobuyoshi Minami , Michitaka Sato , Koichi Hasumi , Norio Yamamoto , Katsuyuki Keino , Teruaki Matsui , Arihiro Kanada , Shuji Ohta , Takahisa Saito , Shuichiro Sato , Akira Asagarasu , Satoshi Doi , Motohiro Kobayashi , Jun Sato , Hajime Asano
发明人： Nobuyoshi Minami , Michitaka Sato , Koichi Hasumi , Norio Yamamoto , Katsuyuki Keino , Teruaki Matsui , Arihiro Kanada , Shuji Ohta , Takahisa Saito , Shuichiro Sato , Akira Asagarasu , Satoshi Doi , Motohiro Kobayashi , Jun Sato , Hajime Asano
CPC分类号： C07D231/12 , A61K31/4439 , A61K31/4709 , A61K31/4725 , C07D233/56 , C07D249/08 , C07D401/04 , C07D401/14 , C07D405/14 , Y02A50/411
摘要： Substituted pyrazole compounds represented by formula (I), or salts thereof are disclosed, wherein R1 is —CH(OH)—CH(R4)-(A)n-Y, —CH2—CH(R4)-(A)n-Y, —CO-B1-A-Y or the like (wherein A is a lower alkylene; Y is an aryl group which may be substituted, for example, by halogen, or the like; R4 is a hydrogen atom or a lower alkyl group; B1 is —CH(R4)— or —N(R4)—; and n is 0 or 1); R2 is a hydrogen atom, a lower alkyl group which may be substituted by hydroxyl or the like, or an aralkyl group; R3 is a phenyl group which may be substituted by halogen or the like, or a pyridyl group; and Q is a pyridyl or quinolyl group. These substituted pyrazole compounds or their salts have an excellent p38MAP kinase inhibiting effect and are hence useful in the prevention or treatment of tumor necrosis factor α-related diseases, interleukin 1-related diseases, interleukin 6-related diseases or cyclooxygenase II-related diseases
摘要翻译： 公开了由式（I）表示的取代的吡唑化合物或其盐，其中R 1是-CH（OH）-CH（R 4） - （A） -CH（R 4） - （A）n -Y， - CO（CH 2） -B 1 -I 1等（其中A是低级亚烷基; Y是可以被卤素取代的芳基等）; R 4， SUP>是氢原子或低级烷基; B 1是-CH（R 4） - 或-N（R 4） - ;和n为0或1）; R 2是氢原子，可以被羟基等取代的低级烷基或芳烷基; R 3是可以被卤素等取代的苯基或吡啶基; Q为吡啶基或喹啉基。 这些取代的吡唑化合物或其盐具有优异的p38MAP激酶抑制作用，因此可用于预防或治疗肿瘤坏死因子α相关疾病，白细胞介素1相关疾病，白细胞介素6相关疾病或环氧合酶II相关疾病
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公开(公告)号：US06667325B1
公开(公告)日：2003-12-23
申请号：US09980579
申请日：2001-12-03
申请人： Nobuyoshi Minami , Michitaka Sato , Koichi Hasumi , Norio Yamamoto , Katsuyuki Keino , Teruaki Matsui , Arihiro Kanada , Shuji Ohta , Takahisa Saito , Shuichiro Sato , Akira Asagarasu , Satoshi Doi , Motohiro Kobayashi , Jun Sato , Hajime Asano
发明人： Nobuyoshi Minami , Michitaka Sato , Koichi Hasumi , Norio Yamamoto , Katsuyuki Keino , Teruaki Matsui , Arihiro Kanada , Shuji Ohta , Takahisa Saito , Shuichiro Sato , Akira Asagarasu , Satoshi Doi , Motohiro Kobayashi , Jun Sato , Hajime Asano
IPC分类号： C07D40104
CPC分类号： C07D231/12 , A61K31/4439 , A61K31/4709 , A61K31/4725 , C07D233/56 , C07D249/08 , C07D401/04 , C07D401/14 , C07D405/14 , Y02A50/411
摘要： Substituted pyrazole compounds represented by formula (I), or salts thereof are disclosed, wherein R1 is —CH(OH)—CH(R4)—(A)n—Y, —CH2—CH(R4)—(A)n—Y, —CO—B1—A—Y or the like (wherein A is a lower alkylene; Y is an aryl group which may be substituted, for example, by halogen, or the like; R4 is a hydrogen atom or a lower alkyl group; B1 is —CH(R4)— or —N(R4)—; and n is 0 or 1); R2 is a hydrogen atom, a lower alkyl group which may be substituted by hydroxyl or the like, or an aralkyl group; R3 is a phenyl group which may be substituted by halogen or the like, or a pyridyl group; and Q is a pyridyl or quinolyl group. These substituted pyrazole compounds or their salts have an excellent p38MAP kinase inhibiting effect and are hence useful in the prevention or treatment of tumor necrosis factor &agr;-related diseases, interleukin 1-related diseases, interleukin 6-related diseases or cyclooxygenase II-related diseases.
摘要翻译： 公开了由式（I）表示的取代的吡唑化合物或其盐，其中R 1是-CH（OH）-CH（R 4） - （A）n Y，-CH 2 -CH（R 4） ） - （A）nY，-CO-B 1 -AY等（其中A是低级亚烷基; Y是可以被卤素取代的芳基等; R 4 >是氢原子或低级烷基; B 1是-CH（R 4） - 或-N（R 4） - ，n是0或1）; R 2是氢原子，可以被羟基等取代的低级烷基或芳烷基; R 3是可被卤素等取代的苯基或吡啶基; Q为吡啶基或喹啉基。 这些取代的吡唑化合物或其盐具有优异的p38MAP激酶抑制作用，因此可用于预防或治疗肿瘤坏死因子α相关疾病，白细胞介素1相关疾病，白介素6相关疾病或环加氧酶II相关疾病。
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公开(公告)号：US06511997B1
公开(公告)日：2003-01-28
申请号：US09869051
申请日：2001-06-22
申请人： Nobuyoshi Minami , Michitaka Sato , Koichi Hasumi , Norio Yamamoto , Katsuyuki Keino , Teruaki Matsui , Arihiro Kanada , Shuji Ohta , Takahisa Saito , Shuichiro Sato , Akira Asagarasu , Satoshi Doi , Motohiro Kobayashi , Jun Sato , Hajime Asano
发明人： Nobuyoshi Minami , Michitaka Sato , Koichi Hasumi , Norio Yamamoto , Katsuyuki Keino , Teruaki Matsui , Arihiro Kanada , Shuji Ohta , Takahisa Saito , Shuichiro Sato , Akira Asagarasu , Satoshi Doi , Motohiro Kobayashi , Jun Sato , Hajime Asano
IPC分类号： A61K314409
CPC分类号： C07D401/04 , C07D405/14
摘要： Aminopyrazole derivatives represented by formula (I), or salts thereof, wherein X1 and X2 are each a hydrogen atom or a halogen atom, or X1 and X2 may be united together to form a lower alkylenedioxy group, Q is a pyridyl group or a quinolyl group, R1 is a hydrogen atom, a substituted or unsubstituted lower alkyl or aryl group, R2 is a hydrogen atom, a lower alkyl group, or an aralkyl group, and R3 represents a hydrogen atom, an organic sulfonyl group, or —C(═Y)—R4 in which R4 is a hydrogen atom or an organic residue and Y is an oxygen or sulfur atom, provided that, when R3 is a hydrogen atom, R1 is a group other than a hydrogen atom and R2 is a hydrogen atom. These amimopyrazole derivatives or their salts have excellent p38MAP kinase inhibiting activities and are hence useful in the prevention or treatment of diseases associated with tumor necrosis sis factor &agr;, interleukin 1, interleukin 6 or cyclooxygenase II.
摘要翻译： 式（I）表示的氨基吡唑衍生物或其盐，其中X 1和X 2各自为氢原子或卤素原子，或者X 1和X 2可以一起结合形成低级亚烷基二氧基，Q是吡啶基或喹啉基 基团，R 1是氢原子，取代或未取代的低级烷基或芳基，R 2是氢原子，低级烷基或芳烷基，R 3表示氢原子，有机磺酰基或-C（ = Y）-R4，其中R4为氢原子或有机残基，Y为氧或硫原子，条件是当R3为氢原子时，R1为氢原子以外的基团，R2为氢原子 。 这些酰胺吡唑衍生物或其盐具有优异的p38MAP激酶抑制活性，因此可用于预防或治疗与肿瘤坏死因子α，白细胞介素1，白介素6或环加氧酶II相关的疾病。
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公开(公告)号：US07385029B2
公开(公告)日：2008-06-10
申请号：US11180582
申请日：2005-07-14
CPC分类号： C07K5/101 , A61K38/00 , C07K5/0205
摘要： The invention provides crystals of N2-(N,N-dimethyl-L-valyl)-N-[(1S,2R)-2-methoxy-4-[(2S)-2-[(1R,2R)-1-methoxy-2-methyl-3-oxo-3-[(2-phenylethyl)amino]propyl]-1-pyrrolidinyl]-1-[(S)-1-methylpropyl]-4-oxobutyl]-N-methyl-L-valinamide or salts thereof which possess potent antitumor activity and methods for their preparation.
摘要翻译： 本发明提供N 2 - （N，N-二甲基-L-缬氨酰基）-N - [（1S，2R）-2-甲氧基-4 - [（2S）-2- [ （1R，2R）-1-甲氧基-2-甲基-3-氧代-3 - [（2-苯基乙基）氨基]丙基] -1-吡咯烷基] -1 - [（S）-1-甲基丙基] 氧代丁基] -N-甲基-L-缬氨酰胺或其盐，其具有有效的抗肿瘤活性及其制备方法。
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公开(公告)号：US20050267041A1
公开(公告)日：2005-12-01
申请号：US11180582
申请日：2005-07-14
CPC分类号： C07K5/101 , A61K38/00 , C07K5/0205
摘要： The invention provides crystals of N2-(N,N-dimethyl-L-valyl)-N-[(1S, 2R)-2-methoxy-4-[(2S)-2-[(1R,2R)-1-methoxy-2-methyl-3-oxo-3-[(2-phenylethyl)amino]propyl]-1-pyrrolidinyl]-1-[(S)-1-methylpropyl]-4-oxobutyl]-N-methyl-L-valinamide or salts thereof which possess potent antitumor activity and methods for their preparation.
摘要翻译： 本发明提供N 2 - （N，N-二甲基-L-缬氨酰基）-N - [（1S，2R）-2-甲氧基-4 - [（2S）-2- [ （1R，2R）-1-甲氧基-2-甲基-3-氧代-3 - [（2-苯基乙基）氨基]丙基] -1-吡咯烷基] -1 - [（S）-1-甲基丙基] 氧代丁基] -N-甲基-L-缬氨酰胺或其盐，其具有有效的抗肿瘤活性及其制备方法。
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公开(公告)号：US07008928B2
公开(公告)日：2006-03-07
申请号：US10490340
申请日：2002-09-19
CPC分类号： C07K5/101 , A61K38/00 , C07K5/0205
摘要： The invention provides crystals of N2-(N,N-dimethyl-L-valyl)-N-[(1S,2R)-2-methoxy-4-[(2S)-2-[(1R,2R)-1-methoxy-2-methyl-3-oxo-3-[(2-phenylethyl)amino]propyl]-1-pyrrolidinyl]-1-[(S)-1-methylpropyl]-4-oxobutyl]-N-methyl-L-valinamide or salts thereof which possess potent antitumor activity and methods for their preparation.
摘要翻译： 本发明提供N 2 - （N，N-二甲基-L-缬氨酰基）-N - [（1S，2R）-2-甲氧基-4 - [（2S）-2- [ （1R，2R）-1-甲氧基-2-甲基-3-氧代-3 - [（2-苯基乙基）氨基]丙基] -1-吡咯烷基] -1 - [（S）-1-甲基丙基] 氧代丁基] -N-甲基-L-缬氨酰胺或其盐，其具有有效的抗肿瘤活性及其制备方法。
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公开(公告)号：US06750315B2
公开(公告)日：2004-06-15
申请号：US10264542
申请日：2002-10-04
申请人： Arihiro Kanada
发明人： Arihiro Kanada
IPC分类号： C08G216
CPC分类号： C08L71/00 , C08G2650/40 , C08K3/01 , C08K7/00
摘要： The present invention is envisioned to improve sliding characteristics of polyether aromatic ketone resins and to provide their molded articles which are themselves resistant to damage and abrasion, cause no such damage or abrasion to their partner parts and can be easily molded. Thus, the present invention pertains to a polyether aromatic ketone resin composition comprising a polyether aromatic ketone resin and a high-hardness filler having a Mohs hardness of 6 or higher, the content of said filler being 1 to 100 parts by weight per 100 parts by weight of said ketone resin, and furthermore to a film or sheet made of the resin composition. The high-hardness filler having a Mohs hardness of 6 or higher is preferably particulate or spherical in particle shape. Also, the maximal particle size of said high-hardness filler is preferably not larger than 100 &mgr;m.
摘要翻译： 本发明旨在改善聚醚芳族酮树脂的滑动特性并提供它们本身对损伤和磨损有抵抗力的模塑制品，不会对其配合部件造成这种损伤或磨损，并且可以容易地模塑。 因此，本发明涉及一种聚醚芳族酮树脂组合物，其包含聚醚芳族酮树脂和莫氏硬度为6以上的高硬度填料，所述填料的含量为每100重量份1〜100重量份 所述酮树脂的重量，以及由所述树脂组合物制成的膜或片。 莫氏硬度为6以上的高硬度填料优选为粒状或球状。 此外，所述高硬度填料的最大粒径优选为100μm以下。
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