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1. 发明申请

US20050222146A1 N-substituted-n-sulfonylaminocyclopropane compounds and pharmaceutical use thereof 审中-公开
标题翻译： N-取代的n-磺酰氨基环丙烷化合物及其药物用途
公开(公告)号：US20050222146A1
公开(公告)日：2005-10-06
申请号：US11011781
申请日：2004-12-15
申请人： Andrew Fryer , Makoto Shiozaki , Nicole Littmann , Takashi Inaba , Steven Andrews , Katsutaka Yasue , Ellen Laird , Masahiro Yokota , Julia Haas , Hiroto Imai , Katsuya Maeda , Yuichi Shinozaki , Yoshikazu Hori
发明人： Andrew Fryer , Makoto Shiozaki , Nicole Littmann , Takashi Inaba , Steven Andrews , Katsutaka Yasue , Ellen Laird , Masahiro Yokota , Julia Haas , Hiroto Imai , Katsuya Maeda , Yuichi Shinozaki , Yoshikazu Hori
IPC分类号： A61K31/18 , A61K31/33 , A61K31/381 , A61K31/496 , A61K31/5377 , C07C311/20 , C07C311/51 , C07C381/06 , C07C381/08 , C07D207/34 , C07D209/52 , C07D211/46 , C07D211/60 , C07D213/42 , C07D213/65 , C07D213/74 , C07D213/79 , C07D213/80 , C07D231/14 , C07D231/20 , C07D233/90 , C07D235/10 , C07D235/14 , C07D249/10 , C07D257/04 , C07D257/06 , C07D261/18 , C07D271/06 , C07D271/07 , C07D277/56 , C07D285/06 , C07D285/08 , C07D295/088 , C07D295/092 , C07D295/13 , C07D295/15 , C07D295/185 , C07D307/68 , C07D333/18 , C07D333/34 , C07D409/12 , C07D413/02 , C07D413/04 , C07D413/12 , C07D49/02
CPC分类号： C07C311/20 , C07C311/51 , C07C381/06 , C07C381/08 , C07C2601/02 , C07C2601/14 , C07D207/34 , C07D209/52 , C07D211/46 , C07D211/60 , C07D213/42 , C07D213/65 , C07D213/74 , C07D213/79 , C07D213/80 , C07D231/14 , C07D231/20 , C07D233/90 , C07D235/14 , C07D249/10 , C07D257/04 , C07D257/06 , C07D261/18 , C07D271/07 , C07D277/56 , C07D285/06 , C07D285/08 , C07D295/088 , C07D295/13 , C07D295/15 , C07D295/185 , C07D307/68 , C07D333/18 , C07D333/34 , C07D409/12 , C07D413/04 , C07D413/12
摘要： The present invention provides a compound having aggrecanase inhibitory activity and MMP-13 inhibitory activity, and useful as a therapeutic agent for osteoarthritis, rheumatoid arthritis and the like, more specifically, a N-substituted-N-sulfonylaminocyclopropane compound of formula (1): wherein R1 is —W-A1—W1-A2, W is —(CH2)m—X—(CH2)n—, wherein W1 is —(CH2)m1—X1—(CH2)n1—, m, m1, n and n1 are the same or different and each is 0 to 6, X and X1 are the same or different and each is a single bond, etc., A1 is an optionally substituted C3-14 hydrocarbon ring group, etc. and A2 is a substituted C3-14 hydrocarbon ring group etc.; R2 is —(CH2)r—CO—R8, etc., wherein r is 0 to 6 and R8 is a C1-6 alkoxy group, etc.; R3 and R4 are the same or different and each is a hydrogen atom, a C1-6 alkyl group, etc.; and R5 is —CO2R21 etc.; R30 and R31 are the same or different and each is a hydrogen atom, etc.; or a prodrug thereof or a pharmaceutically acceptable salt thereof.
摘要翻译：本发明提供具有聚集蛋白聚糖蛋白聚糖酶抑制活性和MMP-13抑制活性的化合物，可用作骨关节炎，类风湿性关节炎等的治疗剂，更具体而言，可以使用式（1）所示的N-取代-N-磺酰氨基环丙烷化合物：其中R 1是-WA 1 -W 1 -A 2，W是 - （CH 3）其中W 1是 - （CH 2）n - 其中W 1是 - （CH 2）n1 - （CH 2）n1 - （CH 2）n1 - ，m，m1，n和n1相同或不同，各自为0〜6，X和X 1相同或不同，均为单键等。 1是任选取代的C 3-14烃环基等，而A 2是取代的C 3-14烃基，烃环组等; R 2是 - （CH 2 CH 2）n -CO-R 8等，其中r是0 至6和R 8是C 1-6烷氧基等; R 3和R 4相同或不同，各自为氢原子，C 1-6烷基等; 和R 5是-CO 2 R 21等; R 30和R 31相同或不同，各自为氢原子等; 或其前药或其药学上可接受的盐。

2. 发明申请

US20060199826A1 Cyclopropane compounds and pharmaceutical use thereof 失效
标题翻译：环丙烷化合物及其药物用途
公开(公告)号：US20060199826A1
公开(公告)日：2006-09-07
申请号：US11011773
申请日：2004-12-15
申请人： Takashi Inaba , Julia Haas , Makoto Shiozaki , Nicole Littmann , Katsutaka Yasue , Steven Andrews , Atushi Sakai , Andrew Fryer , Takafumi Matsuo , Ellen Laird , Akira Suma , Yuichi Shinozaki , Yoshikazu Hori , Hiroto Imai , Tamotsu Negoro
发明人： Takashi Inaba , Julia Haas , Makoto Shiozaki , Nicole Littmann , Katsutaka Yasue , Steven Andrews , Atushi Sakai , Andrew Fryer , Takafumi Matsuo , Ellen Laird , Akira Suma , Yuichi Shinozaki , Yoshikazu Hori , Hiroto Imai , Tamotsu Negoro
IPC分类号： A61K31/496 , A61K31/4436 , A61K31/416 , C07D49/02
CPC分类号： C07C311/29 , C07C311/13 , C07C311/20 , C07C311/22 , C07C311/46 , C07C2601/02 , C07C2601/14 , C07C2603/08 , C07C2603/18 , C07C2603/30 , C07D205/04 , C07D207/48 , C07D209/44 , C07D211/58 , C07D211/96 , C07D213/18 , C07D213/65 , C07D213/71 , C07D213/74 , C07D213/81 , C07D213/82 , C07D217/08 , C07D231/12 , C07D233/64 , C07D237/12 , C07D239/22 , C07D243/08 , C07D257/04 , C07D261/08 , C07D271/06 , C07D271/107 , C07D277/26 , C07D277/36 , C07D277/82 , C07D295/26 , C07D307/79 , C07D307/91 , C07D333/18 , C07D333/34 , C07D333/36 , C07D333/38 , C07D333/62 , C07D401/04 , C07D409/04 , C07D409/12 , C07D413/04 , C07D417/04 , C07D417/12 , C07D471/04 , C07D487/04 , C07D513/04
摘要： The present invention provides a compound having aggrecanase inhibitory activity and MMP-13 inhibitory activity, and useful as a therapeutic agent for osteoarthritis, rheumatoid arthritis and the like, more specifically, a cyclopropane compound of formula (1): wherein R1 is —(CH2)m—X—(CH2)n-A1 etc., wherein m and n are the same or different and each is 0 to 6, X1 is a single bond, etc. and A1 is a substituted C3-14 hydrocarbon ring group, etc.; R2 and R3 are the same or different and each is a hydrogen atom, —(CH2)p—X1-(CH2)q-A2, etc., wherein p and q are the same or different and each is 0 to 6, X1 is a single bond, etc. and A2 is an optionally substituted C3-14 hydrocarbon ring group, etc.; R4 is —CO2R9, etc., wherein R9 is a hydrogen atom, etc.; and R20 and R21 are the same or different and each is a hydrogen atom, —(CH2)m12—X12—(CH2)m12—R30, etc., wherein m12 and m12 are the same or different and each is 0 to 6, X12 is a single bond, etc. and R30 is a hydrogen atom, etc.; or a prodrug thereof or a pharmaceutically acceptable salt thereof.
摘要翻译：本发明提供具有聚集蛋白聚糖蛋白聚糖酶抑制活性和MMP-13抑制活性的化合物，可用作骨关节炎，类风湿性关节炎等的治疗剂，更具体而言，可以使用式（1）的环丙烷化合物：其中R 1 是 - （CH 2）2 -X-（CH 2）n - SUP> 1等，其中m和n相同或不同，并且各自为0至6，X 1是单键等，而A 1， SUP>是取代的C 3-14烃环基等; R 2和R 3相同或不同，并且各自为氢原子， - （CH 2）2 N 其中p和q为 - （CH 2）2 - - - - CH 2 - 相同或不同，并且各自为0至6，X 1为单键等，而A 2为任选取代的C 3-14烷基，烃环等; R 4是-CO 2 R 9等，其中R 9是氢原子等。 ; 和R 20和R 21相同或不同，各自为氢原子， - （CH 2 CH 2）m 12 其中m12和m12（其中m12和m12）相同或不同，各自为0至6，X 12为单键等，R 30为氢原子等; 或其前药或其药学上可接受的盐。

3. 发明申请

US20080242656A1 N-Substituted-N-Sulfonylaminocyclopropane Compounds and Pharmaceutical Use Thereof 审中-公开
标题翻译： N-取代的N-磺酰氨基环丙烷化合物及其药物用途
公开(公告)号：US20080242656A1
公开(公告)日：2008-10-02
申请号：US11765136
申请日：2007-06-19
申请人： Andrew M. Fryer , Makoto Shiozaki , Nicole M. Littmann , Takashi Inaba , Steven W. Andrews , Katsutaka Yasue , Ellen R. Laird , Masahiro Yokota , Julia Haas , Hiroto Imai , Katsuya Maeda , Yuichi Shinozaki , Yoshikazu Hori
发明人： Andrew M. Fryer , Makoto Shiozaki , Nicole M. Littmann , Takashi Inaba , Steven W. Andrews , Katsutaka Yasue , Ellen R. Laird , Masahiro Yokota , Julia Haas , Hiroto Imai , Katsuya Maeda , Yuichi Shinozaki , Yoshikazu Hori
IPC分类号： A01N43/00
CPC分类号： C07C311/20 , C07C311/51 , C07C381/06 , C07C381/08 , C07C2601/02 , C07C2601/14 , C07D207/34 , C07D209/52 , C07D211/46 , C07D211/60 , C07D213/42 , C07D213/65 , C07D213/74 , C07D213/79 , C07D213/80 , C07D231/14 , C07D231/20 , C07D233/90 , C07D235/14 , C07D249/10 , C07D257/04 , C07D257/06 , C07D261/18 , C07D271/07 , C07D277/56 , C07D285/06 , C07D285/08 , C07D295/088 , C07D295/13 , C07D295/15 , C07D295/185 , C07D307/68 , C07D333/18 , C07D333/34 , C07D409/12 , C07D413/04 , C07D413/12
摘要： The present invention provides a compound having aggrecanase inhibitory activity and MMP-13 inhibitory activity, and useful as a therapeutic agent for osteoarthritis, rheumatoid arthritis and the like, more specifically, a N-substituted-N-sulfonylaminocyclopropane compound of formula (1) wherein R1 is —W-A1-W1-A2, W is —(CH2)m—X—(CH2)n—, wherein W1 is —(CH2)m1—X1—(CH2)n1—, m, m1, n and n1 are the same or different and each is 0 to 6, X and X1 are the same or different and each is a single bond, etc., A1 is an optionally substituted C3-14 hydrocarbon ring group, etc. and A2 is a substituted C3-14 hydrocarbon ring group etc.; R2 is —(CH2)r—CO—R8, etc., wherein r is 0 to 6 and R8 is a C1-6 alkoxy group, etc.; R3 and R4 are the same or different and each is a hydrogen atom, a C1-6 alkyl group, etc.; and R5 is —CO2R21, etc.; R30 and R31 are the same or different and each is a hydrogen atom, etc.; or a prodrug thereof or a pharmaceutically acceptable salt thereof.
摘要翻译：本发明提供具有聚集蛋白聚糖蛋白聚糖酶抑制活性和MMP-13抑制活性的化合物，可用作骨关节炎，类风湿性关节炎等的治疗剂，更具体地，可以使用式（1）的N-取代-N-磺酰氨基环丙烷化合物，其中 R 1是-WA 1 -W 1 -A 2，W是 - （CH 2）2 其中W 1 - （CH 2）n - （CH 2）n - 其中W 1是 - （ CH 2 - （CH 2）n1 - - - - - （CH 2）n1 - m，m1，n和n1相同或不同，各自为0〜6，X和X 1相同或不同，分别为单键等。任选取代的C 3-14-14烃环基等，并且A 2是取代的C 3-14烃基戒指组等 R 2是 - （CH 2 CH 2）n -CO-R 8等，其中r是0 至6和R 8是C 1-6烷氧基等; R 3和R 4相同或不同，各自为氢原子，C 1-6烷基等; 和R 5是-CO 2 R 21等; R 30和R 31相同或不同，各自为氢原子等; 或其前药或其药学上可接受的盐。

4. 发明授权

US07351825B2 Cyclopropane compounds and pharmaceutical use thereof 失效
标题翻译：环丙烷化合物及其药物用途
公开(公告)号：US07351825B2
公开(公告)日：2008-04-01
申请号：US11011773
申请日：2004-12-15
申请人： Takashi Inaba , Julia Haas , Makoto Shiozaki , Nicole M. Littmann , Katsutaka Yasue , Steven W. Andrews , Atushi Sakai , Andrew M. Fryer , Takafumi Matsuo , Ellen R. Laird , Akira Suma , Yuichi Shinozaki , Yoshikazu Hori , Hiroto Imai , Tamotsu Negoro
发明人： Takashi Inaba , Julia Haas , Makoto Shiozaki , Nicole M. Littmann , Katsutaka Yasue , Steven W. Andrews , Atushi Sakai , Andrew M. Fryer , Takafumi Matsuo , Ellen R. Laird , Akira Suma , Yuichi Shinozaki , Yoshikazu Hori , Hiroto Imai , Tamotsu Negoro
IPC分类号： C07D265/00 , C07D295/00 , C07D237/00 , C07D409/00 , C07D411/00 , C07D217/00 , C07D211/00 , C07D213/00 , C07D271/00 , C07D413/00 , C07D498/00 , C07D277/00 , C07D257/00 , C07D233/00 , C07D231/00 , C07D207/00 , C07D333/00 , C07D307/00 , C07D303/00 , C07D309/00 , C07D311/00
CPC分类号： C07C311/29 , C07C311/13 , C07C311/20 , C07C311/22 , C07C311/46 , C07C2601/02 , C07C2601/14 , C07C2603/08 , C07C2603/18 , C07C2603/30 , C07D205/04 , C07D207/48 , C07D209/44 , C07D211/58 , C07D211/96 , C07D213/18 , C07D213/65 , C07D213/71 , C07D213/74 , C07D213/81 , C07D213/82 , C07D217/08 , C07D231/12 , C07D233/64 , C07D237/12 , C07D239/22 , C07D243/08 , C07D257/04 , C07D261/08 , C07D271/06 , C07D271/107 , C07D277/26 , C07D277/36 , C07D277/82 , C07D295/26 , C07D307/79 , C07D307/91 , C07D333/18 , C07D333/34 , C07D333/36 , C07D333/38 , C07D333/62 , C07D401/04 , C07D409/04 , C07D409/12 , C07D413/04 , C07D417/04 , C07D417/12 , C07D471/04 , C07D487/04 , C07D513/04
摘要： The present invention provides a compound having aggrecanase inhibitory activity and MMP-13 inhibitory activity, and useful as a therapeutic agent for osteoarthritis, rheumatoid arthritis and the like, more specifically, a cyclopropane compound of formula (1): wherein R1 is —(CH2)m—X—(CH2)n-A1 etc., wherein m and n are the same or different and each is 0 to 6, X is a single bond, etc. and A1 is a substituted C3-14 hydrocarbon ring group, etc.; R2 and R3 are the same or different and each is a hydrogen atom, —(CH2)p—X1—(CH2)q-A2, etc., wherein p and q are the same or different and each is 0 to 6, X1 is a single bond, etc. and A2 is an optionally substituted C3-14 hydrocarbon ring group, etc.; R4 is —CO2R9, etc., wherein R9 is a hydrogen atom, etc.; and R20 and R21 are the same or different and each is a hydrogen atom, —(CH2)m12—X12—(CH2)m12—R30, etc., wherein m12 and m12 are the same or different and each is 0 to 6, X12 is a single bond, etc. and R30 is a hydrogen atom, etc.; or a prodrug thereof or a pharmaceutically acceptable salt thereof.
摘要翻译：本发明提供具有聚集蛋白聚糖蛋白聚糖酶抑制活性和MMP-13抑制活性的化合物，可用作骨关节炎，类风湿性关节炎等的治疗剂，更具体而言，可以使用式（1）的环丙烷化合物：其中R 1 是 - （CH 2）2 -X-（CH 2）n - SUP> 1等，其中m和n相同或不同，并且各自为0至6，X为单键等，而A 1为取代的C _{3-14个烃环基等; R 2和R 3相同或不同，并且各自为氢原子， - （CH 2）2 N 其中p和q为 - （CH 2）2 - - - - CH 2 - 相同或不同，并且各自为0至6，X 1为单键等，而A 2为任选取代的C 3-14烷基，烃环等; R 4是-CO 2 R 9等，其中R 9是氢原子等。 ; 和R 20和R 21相同或不同，各自为氢原子， - （CH 2 CH 2）m 12 其中m12和m12（其中m12和m12）相同或不同，各自为0至6，X 12为单键等，R 30为氢原子等; 或其前药或其药学上可接受的盐。}

5. 发明申请

US20100105894A1 Cyclopropane compounds and pharmaceutical use thereof 审中-公开
标题翻译：环丙烷化合物及其药物用途
公开(公告)号：US20100105894A1
公开(公告)日：2010-04-29
申请号：US12457391
申请日：2009-06-09
申请人： Takashi Inaba , Julia Haas , Makoto Shiozaki , Nicole M. Littmann , Katsutaka Yasue , Steven W. Andrews , Atushi Sakai , Andrew M. Fryer , Takafuml Matsuo , Ellen R. Laird , Akira Suma , Yuichi Shinozaki , Yoshikazu Hori , Hiroto Imai , Tamotsu Negoro
发明人： Takashi Inaba , Julia Haas , Makoto Shiozaki , Nicole M. Littmann , Katsutaka Yasue , Steven W. Andrews , Atushi Sakai , Andrew M. Fryer , Takafuml Matsuo , Ellen R. Laird , Akira Suma , Yuichi Shinozaki , Yoshikazu Hori , Hiroto Imai , Tamotsu Negoro
IPC分类号： C07D243/08 , C07C229/02 , C07C307/00 , C07D409/02 , C07D231/10 , C07D401/02 , C07D261/06 , C07D333/34 , C07D241/04 , C07D271/06 , C07D257/04 , C07D295/00 , C07D215/14 , C07D205/04 , C07D413/02 , C07D241/36 , C07D413/14 , C07D223/14
CPC分类号： C07C311/29 , C07C311/13 , C07C311/20 , C07C311/22 , C07C311/46 , C07C2601/02 , C07C2601/14 , C07C2603/08 , C07C2603/18 , C07C2603/30 , C07D205/04 , C07D207/48 , C07D209/44 , C07D211/58 , C07D211/96 , C07D213/18 , C07D213/65 , C07D213/71 , C07D213/74 , C07D213/81 , C07D213/82 , C07D217/08 , C07D231/12 , C07D233/64 , C07D237/12 , C07D239/22 , C07D243/08 , C07D257/04 , C07D261/08 , C07D271/06 , C07D271/107 , C07D277/26 , C07D277/36 , C07D277/82 , C07D295/26 , C07D307/79 , C07D307/91 , C07D333/18 , C07D333/34 , C07D333/36 , C07D333/38 , C07D333/62 , C07D401/04 , C07D409/04 , C07D409/12 , C07D413/04 , C07D417/04 , C07D417/12 , C07D471/04 , C07D487/04 , C07D513/04
摘要： The present invention provides a compound having aggrecanase inhibitory activity and MMP-13 inhibitory activity, and useful as a therapeutic agent for osteoarthritis, rheumatoid arthritis and the like, more specifically, a cyclopropane compound of formula (1): wherein R1 is —(CH2)m—X—(CH2)n-A1 etc., wherein m and n are the same or different and each is 0 to 6, X is a single bond, etc. and A1 is a substituted C3-14 hydrocarbon ring group, etc.; R2 and R3 are the same or different and each is a hydrogen atom, —(CH2)p—X1—(CH2)q-A2, etc., wherein p and q are the same or different and each is 0 to 6, X1 is a single bond, etc. and A2 is an optionally substituted C3-14 hydrocarbon ring group, etc.; R4 is —CO2R9, etc., wherein R9 is a hydrogen atom, etc.; and R20 and R21 are the same or different and each is a hydrogen atom, —(CH2)m12—X12—(CH2)m12—R30, etc., wherein m12 and m12 are the same or different and each is 0 to 6, X12 is a single bond, etc. and R30 is a hydrogen atom, etc.; or a prodrug thereof or a pharmaceutically acceptable salt thereof.
摘要翻译：本发明提供具有聚集蛋白聚糖蛋白聚糖酶抑制活性和MMP-13抑制活性的化合物，可用作骨关节炎，类风湿性关节炎等的治疗剂，更具体而言，可以使用式（1）所示的环丙烷化合物：其中，R 1为 - （CH 2 ）m-X-（CH 2）n -Al等，其中m和n相同或不同，各自为0〜6，X为单键等，而A1为取代的C3-14烃环基，等等。; R2和R3相同或不同，各自为氢原子， - （CH2）p-X1-（CH2）q-A2等，其中p和q相同或不同，各自为0至6，X1 是单键等，A2是任选取代的C 3-14烃环基等; R4是-CO 2 R 9等，其中R9是氢原子等; 和R 20和R 21相同或不同，各自为氢原子， - （CH 2）m 12 -X 12 - （CH 2）m 12 -R 30等，其中m12和m12相同或不同，各自为0至6， X12为单键等，R30为氢原子等; 或其前药或其药学上可接受的盐。

6. 发明申请

US20080306258A1 Cyclopropane compounds and pharmaceutical use thereof 审中-公开
标题翻译：环丙烷化合物及其药物用途
公开(公告)号：US20080306258A1
公开(公告)日：2008-12-11
申请号：US12149683
申请日：2008-05-06
申请人： Takashi Inaba , Julia Haas , Makoto Shiozaki , Nicole M. Littmann , Katsutaka Yasue , Steven W. Andrews , Atushi Sakai , Andrew M. Fryer , Takafumi Matsuo , Ellen R. Laird , Akira Suma , Yuichi Shinozaki , Yoshikazu Hori , Hiroto Imai , Tamotsu Negoro
发明人： Takashi Inaba , Julia Haas , Makoto Shiozaki , Nicole M. Littmann , Katsutaka Yasue , Steven W. Andrews , Atushi Sakai , Andrew M. Fryer , Takafumi Matsuo , Ellen R. Laird , Akira Suma , Yuichi Shinozaki , Yoshikazu Hori , Hiroto Imai , Tamotsu Negoro
IPC分类号： C07D243/08 , C07D413/14
CPC分类号： C07C311/29 , C07C311/13 , C07C311/20 , C07C311/22 , C07C311/46 , C07C2601/02 , C07C2601/14 , C07C2603/08 , C07C2603/18 , C07C2603/30 , C07D205/04 , C07D207/48 , C07D209/44 , C07D211/58 , C07D211/96 , C07D213/18 , C07D213/65 , C07D213/71 , C07D213/74 , C07D213/81 , C07D213/82 , C07D217/08 , C07D231/12 , C07D233/64 , C07D237/12 , C07D239/22 , C07D243/08 , C07D257/04 , C07D261/08 , C07D271/06 , C07D271/107 , C07D277/26 , C07D277/36 , C07D277/82 , C07D295/26 , C07D307/79 , C07D307/91 , C07D333/18 , C07D333/34 , C07D333/36 , C07D333/38 , C07D333/62 , C07D401/04 , C07D409/04 , C07D409/12 , C07D413/04 , C07D417/04 , C07D417/12 , C07D471/04 , C07D487/04 , C07D513/04
摘要： The present invention provides a compound having aggrecanase inhibitory activity and MMP-13 inhibitory activity, and useful as a therapeutic agent for osteoarthritis, rheumatoid arthritis and the like, more specifically, a cyclopropane compound of formula (1): wherein R1 is —(CH2)m—X—(CH2)n-A1 etc., wherein m and n are the same or different and each is 0 to 6, X is a single bond, etc. and A1 is a substituted C3-14 hydrocarbon ring group, etc.; R2 and R3 are the same or different and each is a hydrogen atom, —(CH2)p—X1—(CH2)q-A2, etc., wherein p and q are the same or different and each is 0 to 6, X1 is a single bond, etc. and A2 is an optionally substituted C3-14 hydrocarbon ring group, etc.; R4 is —CO2R9, etc., wherein R9 is a hydrogen atom, etc.; and R20 and R21 are the same or different and each is a hydrogen atom, —(CH2)m12—X12—(CH2)m12—R30 etc., wherein m12 and m12 are the same or different and each is 0 to 6, X12 is a single bond, etc. and R30 is a hydrogen atom, etc.; or a prodrug thereof or a pharmaceutically acceptable salt thereof.
摘要翻译：本发明提供具有聚集蛋白聚糖蛋白聚糖酶抑制活性和MMP-13抑制活性的化合物，可用作骨关节炎，类风湿性关节炎等的治疗剂，更具体而言，可以使用式（1）所示的环丙烷化合物：其中，R 1为 - （CH 2 ）mX-（CH2）n-A1等，其中m和n相同或不同，各自为0至6，X为单键等，而A1为取代的C3-14烃环基等。 ; R2和R3相同或不同，各自为氢原子， - （CH2）p-X1-（CH2）q-A2等，其中p和q相同或不同，各自为0至6，X1 是单键等，A2是任选取代的C 3-14烃环基等; R4是-CO 2 R 9等，其中R9是氢原子等; 和R 20和R 21相同或不同，各自为氢原子， - （CH 2）m 12 -X 12 - （CH 2）m 12 -R 30等，其中m12和m12相同或不同，各自为0至6，X12 是单键等，R30是氢原子等; 或其前药或其药学上可接受的盐。

7. 发明申请

US20080261994A1 CYCLOPROPANE COMPOUNDS AND PHARMACEUTICAL USE THEREOF 审中-公开
标题翻译：环丙沙星化合物及其药物用途
公开(公告)号：US20080261994A1
公开(公告)日：2008-10-23
申请号：US12016755
申请日：2008-01-18
申请人： Takashi INABA , Julia Hass , Makoto Shiozaki , Nicole M. Littmann , Katsutaka Yasue , Steven W. Andrews , Atushi Sakai , Andrew M. Fryer , Takafumi Matsuo , Ellen R. Laird , Akira Suma , Yuichi Shinozaki , Yoshikazu Hori , Hiroto Imai , Tamotsu Negoro
发明人： Takashi INABA , Julia Hass , Makoto Shiozaki , Nicole M. Littmann , Katsutaka Yasue , Steven W. Andrews , Atushi Sakai , Andrew M. Fryer , Takafumi Matsuo , Ellen R. Laird , Akira Suma , Yuichi Shinozaki , Yoshikazu Hori , Hiroto Imai , Tamotsu Negoro
IPC分类号： A61K31/496 , A61K31/4436 , A61K31/416 , C07D411/00 , C07D217/00 , C07D265/00 , C07D311/00 , A61P19/02
CPC分类号： C07C311/29 , C07C311/13 , C07C311/20 , C07C311/22 , C07C311/46 , C07C2601/02 , C07C2601/14 , C07C2603/08 , C07C2603/18 , C07C2603/30 , C07D205/04 , C07D207/48 , C07D209/44 , C07D211/58 , C07D211/96 , C07D213/18 , C07D213/65 , C07D213/71 , C07D213/74 , C07D213/81 , C07D213/82 , C07D217/08 , C07D231/12 , C07D233/64 , C07D237/12 , C07D239/22 , C07D243/08 , C07D257/04 , C07D261/08 , C07D271/06 , C07D271/107 , C07D277/26 , C07D277/36 , C07D277/82 , C07D295/26 , C07D307/79 , C07D307/91 , C07D333/18 , C07D333/34 , C07D333/36 , C07D333/38 , C07D333/62 , C07D401/04 , C07D409/04 , C07D409/12 , C07D413/04 , C07D417/04 , C07D417/12 , C07D471/04 , C07D487/04 , C07D513/04
摘要： The present invention provides a compound having aggrecanase inhibitory activity and MMP-13 inhibitory activity, and useful as a therapeutic agent for osteoarthritis, rheumatoid arthritis and the like, more specifically, a cyclopropane compound of formula (1): wherein R1 is —(CH2)m—X—(CH2)n-A1 etc., wherein m and n are the same or different and each is 0 to 6, X is a single bond, etc. and A1 is a substituted C3-14 hydrocarbon ring group, etc.; R2 and R3 are the same or different and each is a hydrogen atom, —(CH2)p—X1—(CH2)q-A2, etc., wherein p and q are the same or different and each is 0 to 6, X1 is a single bond, etc. and A2 is an optionally substituted C3-14 hydrocarbon ring group, etc.; R4 is —CO2R9, etc., wherein R9 is a hydrogen atom, etc.; and R20 and R21 are the same or different and each is a hydrogen atom, —(CH2)m12—X12—(CH2)m12—R30, etc., wherein m12 and m12 are the same or different and each is 0 to 6, X12 is a single bond, etc. and R30 is a hydrogen atom, etc.; or a prodrug thereof or a pharmaceutically acceptable salt thereof.
摘要翻译：本发明提供具有聚集蛋白聚糖蛋白聚糖酶抑制活性和MMP-13抑制活性的化合物，可用作骨关节炎，类风湿性关节炎等的治疗剂，更具体而言，可以使用式（1）的环丙烷化合物：其中R 1 是 - （CH 2）2 -X-（CH 2）n - SUP> 1等，其中m和n相同或不同，并且各自为0至6，X为单键等，而A 1为取代的C _{3-14个烃环基等; R 2和R 3相同或不同，并且各自为氢原子， - （CH 2）2 N 其中p和q为 - （CH 2）2 - - - - CH 2 - 相同或不同，并且各自为0至6，X 1为单键等，而A 2为任选取代的C 3-14烷基，烃环等; R 4是-CO 2 R 9等，其中R 9是氢原子等。 ; 和R 20和R 21相同或不同，各自为氢原子， - （CH 2 CH 2）m 12 其中m12和m12（其中m12和m12）相同或不同，各自为0至6，X 12为单键等，R 30为氢原子等; 或其前药或其药学上可接受的盐。}

8. 发明申请

US20080149898A1 Whiet Colored Electrically Conductive Primer Paint Compositions, A Method Of Painting In Which They Are Used And The Painted Objects Which Have Been Painted With Said Method Of Painting 审中-公开
标题翻译：彩色导电底漆涂料组合物，使用它们的绘画方法和所绘绘的所绘绘的物体
公开(公告)号：US20080149898A1
公开(公告)日：2008-06-26
申请号：US11815369
申请日：2006-02-08
申请人： Yuichi Shinozaki , Masato Tokieda , Kazunori Kawahara
发明人： Yuichi Shinozaki , Masato Tokieda , Kazunori Kawahara
IPC分类号： H01B1/20
CPC分类号： C09D123/286 , C09D4/06 , C09D5/002 , C08L2666/02
摘要： The present disclosure provides white colored electrically conductive primer paint compositions which in addition to good electrical conductivity on polyolefin base materials have excellent adhesion properties and water resistance.A white colored electrically conductive primer paint composition comprising (A) resin which includes chlorinated polyolefin resin, (B) white colored electrically conductive filler which has been treated with a coupling agent where the coupling agent surface coverage of the filler is from 10 to 90% and (C) solvent, and in which there are from 10 to 150 parts by weight of (B) per 100 parts by weight as solid fraction of the resin (A).
摘要翻译：本发明提供白色导电底漆涂料组合物，除了在聚烯烃基材上具有良好的导电性之外，还具有优异的粘附性和耐水性。一种白色导电底漆涂料组合物，其包含（A）树脂，其包括氯化聚烯烃树脂，（B）已经用偶联剂处理的白色导电填料，其中填料的偶联剂表面覆盖率为10至90％和（C）溶剂，其中作为树脂（A）的固体成分，每100重量份中含有10〜150重量份（B）。

9. 发明申请

US20080107904A1 Hydroxyl-Containing Resin Composition for Coating Materials, Coating Composition, Coating Finishing Method, and Coated Article 审中-公开
标题翻译：用于涂料的含羟基树脂组合物，涂料组合物，涂料整理方法和涂布制品
公开(公告)号：US20080107904A1
公开(公告)日：2008-05-08
申请号：US11576841
申请日：2005-10-05
申请人： Tetsu Konishi , Rui Niimi , Yuichi Shinozaki
发明人： Tetsu Konishi , Rui Niimi , Yuichi Shinozaki
IPC分类号： B32B27/00 , C08G65/34
CPC分类号： C08G18/6237 , C08F220/18 , C08F220/30 , C08G18/0823 , C09D175/04 , Y10T428/31504
摘要： The present invention relates to a hydroxyl-containing resin composition for a coating material, characterized in comprising a hydroxyl-containing resin that has a hydroxyl value of 50 to 400 mg KOH/g and a weight-average molecular weight of 2,000 to 100,000, and in being a resin obtained by copolymerizing, in the presence of (a) an acid compound containing one carboxyl group and two or more hydroxyl groups, (b) a radical-polymerizable monomer having an epoxy group and (c) another radical-polymerizable monomer, or a resin obtained by the addition reaction of (a) an acid compound containing one carboxyl group and two or more hydroxyl groups with a copolymer of (b) a radical-polymerizable monomer having an epoxy group and (c) another radical-polymerizable monomer. The invention also relates to a coating composition comprising the resin composition and a crosslinking agent, to a coating finishing method in which the coating composition is used, and to a coated article coated by the method.
摘要翻译：本发明涉及一种用于涂料的含羟基树脂组合物，其特征在于包含羟基值为50-400mg KOH / g，重均分子量为2,000至100,000的含羟基树脂，以及在（a）含有一个羧基和两个或更多个羟基的酸化合物的存在下，（b）具有环氧基的可自由基聚合的单体和（c）另一种可自由基聚合的单体或通过（a）含有一个羧基和两个或更多个羟基的酸化合物与（b）具有环氧基的可自由基聚合的单体的共聚物和（c）另一种可自由基聚合的单体。本发明还涉及包含树脂组合物和交联剂的涂料组合物，其中使用涂料组合物的涂料整理方法以及通过该方法涂覆的涂布制品。

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