公开(公告)号：US07939536B2

公开(公告)日：2011-05-10

申请号：US11794180

申请日：2005-12-27

申请人： Koichi Hasumi ,  Shuji Ohta ,  Takahisa Saito ,  Shuichiro Sato ,  Jun-ya Kato ,  Jun Sato ,  Hiroyuki Suzuki ,  Hajime Asano ,  Mami Okada ,  Yasuhiro Matsumoto ,  Kazuhiko Shirota

发明人： Koichi Hasumi ,  Shuji Ohta ,  Takahisa Saito ,  Shuichiro Sato ,  Jun-ya Kato ,  Jun Sato ,  Hiroyuki Suzuki ,  Hajime Asano ,  Mami Okada ,  Yasuhiro Matsumoto ,  Kazuhiko Shirota

IPC分类号： C07D413/04 ,  A61K31/506

CPC分类号： C07D413/04 ,  C07D413/14

摘要： The invention discloses isoxazole derivatives represented by a formula, in which R1 stands for hydrogen, lower alkyl, amino, halogen, lower alkoxy and the like, R2 stands for substituted or unsubstituted aryl and the like, R3 stands for hydrogen or lower alkyl, R4 stands for substituted or unsubstituted phenyl and the like, and Y stands for —CH2—, —CO—, —CH(CH3)—, —O—, —NH— and the like, or pharmaceutically acceptable salts thereof, which have excellent p38MAPkinase inhibitory action.

摘要翻译： 本发明公开了由式表示的异恶唑衍生物，其中R1代表氢，低级烷基，氨基，卤素，低级烷氧基等，R2代表取代或未取代的芳基等，R3代表氢或低级烷基，R4代表 代表取代或未取代的苯基等，Y代表具有优异p38MAP激酶的-CH 2 - ， - CO - ， - CH（CH 3） - ， - O-，-NH-等或其药学上可接受的盐 抑制作用。

公开(公告)号：US20090192164A1

公开(公告)日：2009-07-30

申请号：US12308750

申请日：2007-06-26

申请人： Koichi Hasumi ,  Shuji Ohta ,  Takahisa Saito ,  Shuichiro Sato ,  Jun-ya Kato ,  Jun Sato ,  Hiroyuki Suzuki ,  Hajime Asano ,  Mami Okada ,  Yasuhiro Matsumoto ,  Kazuhiko Shirota

发明人： Koichi Hasumi ,  Shuji Ohta ,  Takahisa Saito ,  Shuichiro Sato ,  Jun-ya Kato ,  Jun Sato ,  Hiroyuki Suzuki ,  Hajime Asano ,  Mami Okada ,  Yasuhiro Matsumoto ,  Kazuhiko Shirota

IPC分类号： A61K31/4439 ,  C07D401/04 ,  C07D401/14 ,  C07D413/04 ,  C07D403/04 ,  A61K31/444 ,  A61K31/506 ,  A61K31/53 ,  A61P1/00

CPC分类号： C07D401/04 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/506 ,  C07D401/14 ,  C07D413/04

摘要： The invention discloses treating agents of inflammatory bowel disease, which contain p38MAPkinase inhibitor having properties of antedrug as the active ingredient.

摘要翻译： 本发明公开了含有作为活性成分的具有特性的p38MAP激酶抑制剂的炎症性肠病治疗剂。

公开(公告)号：US08207203B2

公开(公告)日：2012-06-26

申请号：US12308875

申请日：2007-06-26

申请人： Koichi Hasumi ,  Shuji Ohta ,  Takahisa Saito ,  Shuichiro Sato ,  Jun-ya Kato ,  Jun Sato ,  Hiroyuki Suzuki ,  Hajime Asano ,  Mami Okada ,  Yasuhiro Matsumoto ,  Kazuhiko Shirota

发明人： Koichi Hasumi ,  Shuji Ohta ,  Takahisa Saito ,  Shuichiro Sato ,  Jun-ya Kato ,  Jun Sato ,  Hiroyuki Suzuki ,  Hajime Asano ,  Mami Okada ,  Yasuhiro Matsumoto ,  Kazuhiko Shirota

IPC分类号： A61K31/4439 ,  C07D413/04

CPC分类号： C07D413/04 ,  C07D413/14

摘要： This invention offers isoxazole derivatives represented by the following formula (I) in which R1 and R2 each stands for hydrogen, lower alkyl, amino and the like; R3 stands for substituted or unsubstituted aryl or hetero aryl; R4 stands for hydrogen or lower alkyl; R5 stands for substituted or unsubstituted phenyl, furyl and the like; and Y stands for —CH2—, —CO—, —O—, —NH— and the like, or pharmaceutically acceptable salts thereof which exhibit excellent p38MAPkinase-inhibiting action with reduced side-effects, and are useful for treating such diseases as chronic rheumatoid arthritis, ulcerative colitis and the like.

摘要翻译： 本发明提供由下式（I）表示的异恶唑衍生物，其中R 1和R 2各自代表氢，低级烷基，氨基等; R3代表取代或未取代的芳基或杂芳基; R4代表氢或低级烷基; R5代表取代或未取代的苯基，呋喃基等; Y表示具有优异的p38MAP激酶抑制作用的副产物-CH 2 - ， - CO - ， - O-，-NH-等或其药学上可接受的盐，可用于治疗慢性 类风湿性关节炎，溃疡性结肠炎等。

公开(公告)号：US20090306145A1

公开(公告)日：2009-12-10

申请号：US12308875

申请日：2007-06-26

申请人： Koichi Hasumi ,  Shuji Ohta ,  Takahisa Saito ,  Shuichiro Sato ,  Jun-ya Kato ,  Jun Sato ,  Hiroyuki Suzuki ,  Hajime Asano ,  Mami Okada ,  Yasuhiro Matsumoto ,  Kazuhiko Shirota

发明人： Koichi Hasumi ,  Shuji Ohta ,  Takahisa Saito ,  Shuichiro Sato ,  Jun-ya Kato ,  Jun Sato ,  Hiroyuki Suzuki ,  Hajime Asano ,  Mami Okada ,  Yasuhiro Matsumoto ,  Kazuhiko Shirota

IPC分类号： A61K31/4439 ,  C07D413/04 ,  A61P35/00

CPC分类号： C07D413/04 ,  C07D413/14

摘要： This invention offers isoxazole derivatives represented by the following formula (I) in which R1 and R2 each stands for hydrogen, lower alkyl, amino and the like; R3 stands for substituted or unsubstituted aryl or hetero aryl; R4 stands for hydrogen or lower alkyl; R5 stands for substituted or unsubstituted phenyl, furyl and the like; and Y stands for —CH2—, —CO—, —O—, —NH— and the like, or pharmaceutically acceptable salts thereof which exhibit excellent p38MAPkinase-inhibiting action with reduced side-effects, and are useful for treating such diseases as chronic rheumatoid arthritis, ulcerative colitis and the like.

摘要翻译： 本发明提供由下式（I）表示的异恶唑衍生物，其中R 1和R 2各自代表氢，低级烷基，氨基等; R3代表取代或未取代的芳基或杂芳基; R4代表氢或低级烷基; R5代表取代或未取代的苯基，呋喃基等; Y表示具有优异的p38MAP激酶抑制作用的副产物-CH 2 - ， - CO - ， - O-，-NH-等或其药学上可接受的盐，可用于治疗慢性 类风湿性关节炎，溃疡性结肠炎等。

公开(公告)号：US20080114003A1

公开(公告)日：2008-05-15

申请号：US11794180

申请日：2005-12-27

申请人： Koichi Hasumi ,  Shuji Ohta ,  Takahisa Saito ,  Shuichiro Sato ,  Junya Kato ,  Jun Sato ,  Hiroyuki Suzuki ,  Hajime Asano ,  Mami Okada ,  Yasuhiro Matsumoto ,  Kazuhiko Shirota

发明人： Koichi Hasumi ,  Shuji Ohta ,  Takahisa Saito ,  Shuichiro Sato ,  Junya Kato ,  Jun Sato ,  Hiroyuki Suzuki ,  Hajime Asano ,  Mami Okada ,  Yasuhiro Matsumoto ,  Kazuhiko Shirota

IPC分类号： A61K31/506 ,  C07D413/04 ,  A61P29/00 ,  A61P11/00 ,  A61P35/00 ,  A61P9/00 ,  A61P25/00

CPC分类号： C07D413/04 ,  C07D413/14

摘要： The invention discloses isoxazole derivatives represented by a formula, in which R1 stands for hydrogen, lower alkyl, amino, halogen, lower alkoxy and the like, R2 stands for substituted or unsubstituted aryl and the like, R3 stands for hydrogen or lower alkyl, R4 stands for substituted or unsubstituted phenyl and the like, and Y stands for —CH2—, —CO—, —CH(CH3)—, —O—, —NH— and the like, or pharmaceutically acceptable salts thereof, which have excellent p38MAPkinase inhibitory action.

摘要翻译： 本发明公开了由式表示的异恶唑衍生物，其中R 1代表氢，低级烷基，氨基，卤素，低级烷氧基等，R 2代表取代的 或未取代的芳基等，R 3代表氢或低级烷基，R 4代表取代或未取代的苯基等，Y代表-CH

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

IPC分类号： A61K31/44 ,  C07D40/00

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

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。

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。

公开(公告)号：US06291485B1

公开(公告)日：2001-09-18

申请号：US09462413

申请日：2000-01-10

申请人： Hiroshi Azuma ,  Haruo Yamashita ,  Katsuyuki Keino ,  Shuji Ota ,  Takahisa Saito ,  Shuichiro Sato ,  Hidehisa Hamasaki ,  Katsura Suzuki ,  Akiko Sugimoto

发明人： Hiroshi Azuma ,  Haruo Yamashita ,  Katsuyuki Keino ,  Shuji Ota ,  Takahisa Saito ,  Shuichiro Sato ,  Hidehisa Hamasaki ,  Katsura Suzuki ,  Akiko Sugimoto

IPC分类号： A01N4340

CPC分类号： C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D405/14

摘要： 4,5-Dihydro-[1H]-benz[g]indazole-3-carboxylic acid derivatives represented by the following formula, or their salts, have excellent antagonism to endothelin receptors and are useful as preventives or remedies for diseases such as hypertension, angina pectoris, myocardial infarction, brain infarction, cerebrovascular contraction, renal insufficiency, hepatic dysfunction, arteriosclerosis and post-PTCA restenosis. wherein Ar represents an optionally substituted aryl group, and R1 represents a hydrogen atom, an optionally substituted lower alkyl group, an optionally substituted aryl group, an optionally substituted cycloalkyl group or an optionally substituted heterocyclic group.

摘要翻译： 由下式表示的4,5-二氢 - [1H] - 苯并[g]吲唑-3-羧酸衍生物或其盐对内皮素受体具有优异的拮抗作用，可用作疾病如高血压， 心绞痛，心肌梗塞，脑梗塞，脑血管收缩，肾功能不全，肝功能障碍，动脉硬化和PTCA后再狭窄。其中Ar表示任选取代的芳基，R 1表示氢原子，任选取代的低级烷基，任选地 取代的芳基，任选取代的环烷基或任选取代的杂环基。

公开(公告)号：US08101624B2

公开(公告)日：2012-01-24

申请号：US12310025

申请日：2007-07-24

申请人： Akira Asagarasu ,  Shuichiro Sato ,  Makoto Okada

发明人： Akira Asagarasu ,  Shuichiro Sato ,  Makoto Okada

IPC分类号： A61K31/517 ,  C07D401/06 ,  C07D239/88

CPC分类号： C07D239/91 ,  C07D401/06 ,  C07D409/06

摘要： The invention discloses quinazoline derivatives or salts thereof, which possess PDE9-inhibiting activity and are useful as treating agents of dysuria and the like, the derivatives being represented by the formula (I) in the formula, R1 stands for phenyl or aromatic heterocyclic group which are optionally substituted with 1-3 substituents selected from halogen, C1-6 alkyl, C1-6 haloalkyl containing 1-6 halogen atoms and C1-6 alkoxy; and n is an integer of 1-3.

摘要翻译： 本发明公开了具有PDE9抑制活性的喹唑啉衍生物或其盐，可用作排尿困难等的治疗剂，该衍生物由式中的式（I）表示，R 1表示苯基或芳族杂环基， 任选被1-3个选自卤素，C 1-6烷基，含有1-6个卤原子的C 1-6卤代烷基和C 1-6烷氧基取代的取代基取代; n为1-3的整数。