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1. 发明公开

EP2022788A1 NOVEL CRYSTAL OF 3-Ý5-Ý4-(CYCLOPENTYLOXY)-2- HYDROXYBENZOYL¨-2-Ý(3-HYDROXY-1,2-BENZISOXAZOL-6- YL)METHOXY¨PHENYL¨PROPIONIC ACID 有权
标题翻译： NEUER KRISTALL VON 3- [5- [4-（环己基）-2-羟基苯甲酰基] -2 - [（3-羟基-1,2-苯并咪唑-6-基）甲氧基]苯基]丙酸
公开(公告)号：EP2022788A1
公开(公告)日：2009-02-11
申请号：EP07744104.6
申请日：2007-05-25
申请人： TOYAMA CHEMICAL CO., LTD.
发明人： YONEZAWA, Kenji , KOTSUBO, Hironori , BABA, Yasutaka , TADA, Yukie
IPC分类号： C07D261/12
CPC分类号： C07D261/20
摘要： The crystal of 3-{5-[4-(cyclopentyloxy)-2-hydroxybenzoyl]-2-[(3-hydroxy-1,2-benzisoxazol-6-yl)methoxy]phenyl}propionic acid having peaks at the position of 14.0, 16.0, 23.3, 23.7 and 26.3°and the crystal of 3-{5-[4-(cyclopentyloxy)-2-hydroxybenzoyl]-2-[(3-hydroxy-1,2-benzisoxazol-6-yl)methoxy]phenyl}propionic acid having peaks at the position of 14.6, 23.1, 24.7, 25.6 and 26.0° on 2θ of diffraction angle in a powder X-ray diffraction pattern have a small specific volume, are hard to be charged with electricity, are easily handled and are useful for an active pharmaceutical ingredient of excellent anti-rheumatic agents.
摘要翻译： 3- {5- [4-（环戊氧基）-2-羟基苯甲酰基] -2 - [（3-羟基-1,2-苯并异恶唑-6-基）甲氧基]苯基}丙酸的晶体在 14.0,16.0,23.3,23.7和26.3°，3- {5- [4-（环戊氧基）-2-羟基苯甲酰基] -2 - [（3-羟基-1,2-苯并异恶唑-6-基）甲氧基 ]苯基}丙酸在粉末X射线衍射图中的衍射角在14.6,23.1,24.7,25.6和26.0°处具有峰值，具有小的比容，难以被电荷充电易于处理，并且可用于优异的抗风湿剂的活性药物成分。

2. 发明授权

EP2022788B1 NOVEL CRYSTAL OF 3-[5-[4-(CYCLOPENTYLOXY)-2- HYDROXYBENZOYL]-2-[(3-HYDROXY-1,2-BENZISOXAZOL-6-YL)METHOXY]PHENYL]PROPIONIC ACID 有权
标题翻译：新的晶体形式的3- [5- [4-（环戊氧基）-2-羟基苯甲酰基] -2 - [（3-羟基-1,2-苯并异唑-6-基）甲氧基]苯基]丙酸
公开(公告)号：EP2022788B1
公开(公告)日：2010-09-01
申请号：EP07744104.6
申请日：2007-05-25
申请人： TOYAMA CHEMICAL CO., LTD.
发明人： YONEZAWA, Kenji , KOTSUBO, Hironori , BABA, Yasutaka , TADA, Yukie
IPC分类号： C07D261/12 , A61K31/42 , A61P19/02
CPC分类号： C07D261/20
摘要： Disclosed is a crystal of 3-[5-[4-(cyclopentyloxy)-2- hydroxybenzoyl]-2-[(3-hydroxy-1,2-benzisoxazol-6- yl)methoxy]phenyl]propionic acid having refraction angles of 14.0, 16.0, 23.3, 23.7 and 26.3˚ as measured in terms of 2ϑ in powder X-ray diffraction pattern. Also disclosed is a crystal of 3-[5-[4-(cyclopentyloxy)-2-hydroxybenzoyl]-2-[(3- hydroxy-1,2-benzisoxazol-6-yl)methoxy]phenyl]propionic acid having refraction angles of 14.6, 23.1, 24.7, 25.6 and 26.0˚ as measured in terms of 2ϑ in powder X-ray diffraction pattern. These crystals have small specific volumes, are hardly charged electrically, can be handled easily, and are useful as excellent active ingredients for anti-rheumatic drugs.

3. 发明授权

EP1031569B1 SALT OF A 7-ISOINDOLINEQUINOLONECARBOXYLIC ACID DERIVATIVE, MONOHYDRATE THEREOF AND COMPOSITION CONTAINING THE SAME AS ACTIVE INGREDIENT 有权
标题翻译： SALT 7-ISOINDOLINCHINOLONCARBONSÄURE衍生物，ITS MONOHYDRAT和组合物THESE作为活性成分的含
公开(公告)号：EP1031569B1
公开(公告)日：2010-03-17
申请号：EP98950405.5
申请日：1998-10-27
申请人： TOYAMA CHEMICAL CO., LTD.
发明人： YAMADA, Minoru , HAMAMOTO, Shoichi , HAYASHI, Kazuya , TAKAOKA, Kazuko , MATSUKURA, Hiroko , YOTSUJI, Minako , YONEZAWA, Kenji , OJIMA, Katsuji , TAKAMATSU, Tamotsu , TAYA, Kyoko , YAMAMOTO, Hirohiko , KIYOTO, Taro , KOTSUBO, Hironori
IPC分类号： C07D401/04 , A61K31/47
CPC分类号： C07D401/04 , A61K31/4709 , C07C217/48 , C07D209/44 , C07D215/56 , C07F5/025 , Y02P20/55
摘要： Processes for producing 7-isoindolinequinolonecarboxylic derivatives useful as antibacterials and represented by general formula (1) and intermediates therefor; salts of 7-isoindolinequinolonecarboxylic derivatives represented by formula (1) and hydrates thereof; and compositions containing the same as the active ingredient: (1) wherein R1 represents hydrogen or a carboxyl-protecting group; R2 represents cycloalkyl etc.; R3 represents at least one member selected among hydrogen, halogen, and the like; R4 represents at least one member selected among hydrogen, optionally substituted alkyl, and the like; R5 represents hydrogen, optionally substituted alkyl, etc.; R6 represents hydrogen etc.; and A represents CH or C-R7, wherein R7 represents alkoxy etc.

4. 发明公开

EP1445249A1 NOVEL BENSOPHENONE DERIVATIVES OR SALTS THEREOF 有权
标题翻译：新二苯甲酮及其盐的
公开(公告)号：EP1445249A1
公开(公告)日：2004-08-11
申请号：EP02781763.4
申请日：2002-11-13
申请人： TOYAMA CHEMICAL CO., LTD. , Hirono, Shuichi , Shiozawa, Shunichi
发明人： CHAKI, Hisaaki , KOTSUBO, Hironori , TANAKA, Tadashi , AIKAWA, Yukihiko , HIRONO, Shuichi , SHIOZAWA, Shunichi
IPC分类号： C07C59/90 , C07C69/734 , C07C69/76 , C07C205/34 , C07C219/32 , C07C255/54 , C07C255/37 , C07C271/64 , C07C235/42 , C07C311/29 , C07C311/51 , C07C311/53 , C07C317/22 , C07C323/19 , A61K31/192
CPC分类号： C07C235/42 , A61K31/192 , C07C59/90 , C07C65/34 , C07C65/40 , C07C69/738 , C07C69/76 , C07C69/88 , C07C69/94 , C07C205/34 , C07C217/76 , C07C255/54 , C07C259/10 , C07C271/64 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/10 , C07C2601/14 , C07C2601/18
摘要： A benzophenone derivative represented by the following formula:
wherein

R 1 represents, for example, an optionally substituted heterocyclic group, or a substituted phenyl group; Z represents, for example, an alkylene group; R 2 represents, for example, a carboxyl group optionally protected with alkyl;
R 3 represents, for example, an optionally protected hydroxyl group; R 4 represents, for example, an optionally substituted cycloalkyloxy group; and R 5 represents, for example, a hydrogen atom,
or a salt thereof has anti-arthritic activity, inhibits bone destruction caused by arthritis, and provides high safety and excellent pharmacokinetics and thus is useful as therapeutic agent for arthritis. These compounds have inhibitory effect on AP-1 activity and are useful as preventive or therapeutic agent for diseases in which excessive expression of AP-1 is involved.

5. 发明公开

EP1127869A1 NOVEL COMPOUNDS AND MEDICINAL USE THEREOF 审中-公开
标题翻译： NEUARTIGE VERBINDUNGEN UND IHRE VERWENDUNG
公开(公告)号：EP1127869A1
公开(公告)日：2001-08-29
申请号：EP99954398.6
申请日：1999-11-05
申请人： TOYAMA CHEMICAL CO., LTD.
发明人： CHAKI, Hisaaki , TAKAKURA, Tadakazu , TSUCHIDA, Keiichi , YOKOTANI, Junichi , KOTSUBO, Hironori , AIKAWA, Yukihiko , HIRONO, Shuichi , SHIOZAWA, Shunichi
IPC分类号： C07C69/73 , C07C69/767 , C07C205/49
CPC分类号： C07D207/333 , A61K38/00 , C07C59/64 , C07C59/84 , C07C65/24 , C07C65/34 , C07C65/36 , C07C65/38 , C07C65/40 , C07C69/738 , C07C69/94 , C07C229/34 , C07C233/01 , C07C233/47 , C07C235/20 , C07C235/84 , C07C251/32 , C07C251/48 , C07C251/60 , C07C255/49 , C07C275/24 , C07C311/06 , C07C311/51 , C07D207/08 , C07D209/42 , C07D235/26 , C07D277/60 , C07K7/06 , C07K7/64 , Y02P20/55
摘要： A compound comprising the atom corresponding to N 3 and the two or more atoms selected from N 1 , N 2 , N 4 and N 5 , said atoms constitute the pharmacophore represented by the following formula:
wherein N 1 represents an atom to which a donative hydrogen atom in a hydrogen-bond donating group is bonded or a hydrogen-bond accepting atom in a hydrogen-bond accepting group; N 3 represents a hydrogen-bond accepting atom in a hydrogen-bond accepting group; and N 2 , N 4 and N 5 independently represents an arbitrary carbon atom constituting a hydrophobic group and defined by the interatomic distances between N 1 , N 2 , N 3 , N 4 and N 5 ; and, in the optimized three-dimensional structure thereof, the distances between the atom corresponding to N 3 and the two or more atoms selected from N 1 , N 2 , N 4 and N 5 , in the optimized steric structure thereof, are the interatomic distances in a pharmacophore; or a salt thereof;
inhibits the activity of transcription factor AP-1 and is useful as an agent for preventing and treating the diseases into which overexpression of AP-1 participates and as an AP-1 inhibitor.
摘要翻译：包含对应于N 3的原子和选自N1，N2，N4和N5的两个或更多个原子的化合物，所述原子构成由下式表示的药效团：其中N1表示与在氢键接受基团中键合氢键供体基团或氢键接受原子; N3表示氢键接受基团中的氢键接受原子; N2，N4和N5独立地表示构成疏水基团的任意碳原子，由N1，N2，N3，N4和N5之间的原子间距离定义; 并且在其优化的三维结构中，在其优化的立体结构中，对应于N 3的原子与选自N1，N2，N4和N5的两个或更多个原子之间的距离是药效团中的原子间距离; 或其盐; 抑制转录因子AP-1的活性，可用作预防和治疗AP-1过表达的疾病和作为AP-1抑制剂的药物。

7. 发明公开

EP2562155A1 NOVEL HYDROXAMIC ACID DERIVATIVE 有权转让
标题翻译： NEW异羟肟酸
公开(公告)号：EP2562155A1
公开(公告)日：2013-02-27
申请号：EP11772045.8
申请日：2011-04-20
申请人： Taisho Pharmaceutical Co., Ltd. , Toyama Chemical Co., Ltd.
发明人： TAKASHIMA, Hajime , TSURUTA, Risa , YABUUCHI, Tetsuya , OKA, Yusuke , URABE, Hiroki , SUGA, Yoichiro , TAKAHASHI, Masato , UNEUCHI, Fumito , KOTSUBO, Hironori , SHOJI, Muneo , KAWAGUCHI, Yasuko
IPC分类号： C07C259/06 , A61K31/166 , A61K31/337 , A61K31/341 , A61K31/343 , A61K31/351 , A61K31/357 , A61K31/36 , A61K31/381 , A61K31/397 , A61K31/40 , A61K31/4015 , A61K31/402 , A61K31/403 , A61K31/4035 , A61K31/404 , A61K31/4045 , A61K31/407 , A61K31/415 , A61K31/416
CPC分类号： C07C233/83 , C07C235/84 , C07C237/36 , C07C259/06 , C07C271/22 , C07C271/28 , C07C309/30 , C07C311/08 , C07C317/28 , C07C317/44 , C07C323/41 , C07C323/62 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07C2601/16 , C07C2601/18 , C07C2602/08 , C07D205/04 , C07D205/12 , C07D207/10 , C07D207/12 , C07D207/27 , C07D207/327 , C07D209/08 , C07D209/12 , C07D209/14 , C07D209/44 , C07D209/52 , C07D211/14 , C07D211/18 , C07D211/38 , C07D211/46 , C07D211/56 , C07D211/70 , C07D213/38 , C07D213/40 , C07D213/54 , C07D213/61 , C07D213/64 , C07D213/65 , C07D213/70 , C07D213/74 , C07D213/81 , C07D215/14 , C07D217/04 , C07D217/12 , C07D231/12 , C07D231/56 , C07D233/61 , C07D235/04 , C07D257/04 , C07D261/08 , C07D263/14 , C07D263/32 , C07D263/56 , C07D265/30 , C07D265/36 , C07D265/38 , C07D267/10 , C07D271/12 , C07D277/20 , C07D277/30 , C07D277/62 , C07D277/66 , C07D285/12 , C07D295/08 , C07D295/12 , C07D295/14 , C07D295/16 , C07D305/06 , C07D305/08 , C07D307/14 , C07D307/18 , C07D307/52 , C07D307/54 , C07D307/78 , C07D307/81 , C07D307/82 , C07D307/87 , C07D309/04 , C07D309/14 , C07D317/30 , C07D317/60 , C07D319/18 , C07D319/20 , C07D333/24 , C07D405/06 , C07D413/06 , C07D471/04 , C07D471/10 , C07D487/08 , C07D491/20 , C07D498/04 , C07D498/08 , C07F9/091
摘要： Provided is a novel compound which is useful as a pharmaceutical composition by inhibiting an LpxC activity, thereby exhibiting potent antimicrobial activity against gram-negative bacteria including Pseudomonas aeruginosa and its drug resistant bacteria. Provided is a hydroxamic acid derivative represented by the following general formula [1] or a pharmaceutically acceptable salt thereof:

8. 发明授权

EP2562155B1 HYDROXAMIC ACID DERIVATIVE 有权转让
公开(公告)号：EP2562155B1
公开(公告)日：2019-06-05
申请号：EP11772045.8
申请日：2011-04-20
申请人： Taisho Pharmaceutical Co., Ltd. , FUJIFILM Toyama Chemical Co., Ltd.
发明人： TAKASHIMA, Hajime , TSURUTA, Risa , YABUUCHI, Tetsuya , OKA, Yusuke , URABE, Hiroki , SUGA, Yoichiro , TAKAHASHI, Masato , UNEUCHI, Fumito , KOTSUBO, Hironori , SHOJI, Muneo , KAWAGUCHI, Yasuko
IPC分类号： C07C259/06 , A61K31/166 , A61K31/337 , A61K31/341 , A61K31/343 , A61K31/351 , A61K31/357 , A61K31/36 , A61K31/381 , A61K31/397 , A61K31/40 , A61K31/4015 , A61K31/402 , A61K31/403 , A61K31/4035 , A61K31/404 , A61K31/4045 , A61K31/407 , A61K31/415 , A61K31/416
CPC分类号： C07C233/83 , C07C235/84 , C07C237/36 , C07C259/06 , C07C271/22 , C07C271/28 , C07C309/30 , C07C311/08 , C07C317/28 , C07C317/44 , C07C323/41 , C07C323/62 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07C2601/16 , C07C2601/18 , C07C2602/08 , C07D205/04 , C07D205/12 , C07D207/10 , C07D207/12 , C07D207/27 , C07D207/327 , C07D209/08 , C07D209/12 , C07D209/14 , C07D209/44 , C07D209/52 , C07D211/14 , C07D211/18 , C07D211/38 , C07D211/46 , C07D211/56 , C07D211/70 , C07D213/38 , C07D213/40 , C07D213/54 , C07D213/61 , C07D213/64 , C07D213/65 , C07D213/70 , C07D213/74 , C07D213/81 , C07D215/14 , C07D217/04 , C07D217/12 , C07D231/12 , C07D231/56 , C07D233/61 , C07D235/04 , C07D257/04 , C07D261/08 , C07D263/14 , C07D263/32 , C07D263/56 , C07D265/30 , C07D265/36 , C07D265/38 , C07D267/10 , C07D271/12 , C07D277/20 , C07D277/30 , C07D277/62 , C07D277/66 , C07D285/12 , C07D295/08 , C07D295/12 , C07D295/14 , C07D295/16 , C07D305/06 , C07D305/08 , C07D307/14 , C07D307/18 , C07D307/52 , C07D307/54 , C07D307/78 , C07D307/81 , C07D307/82 , C07D307/87 , C07D309/04 , C07D309/14 , C07D317/30 , C07D317/60 , C07D319/18 , C07D319/20 , C07D333/24 , C07D405/06 , C07D413/06 , C07D471/04 , C07D471/10 , C07D487/08 , C07D491/20 , C07D498/04 , C07D498/08 , C07F9/091
摘要： Provided is a novel compound which is useful as a pharmaceutical composition by inhibiting an LpxC activity, thereby exhibiting potent antimicrobial activity against gram-negative bacteria including Pseudomonas aeruginosa and its drug resistant bacteria. Provided is a hydroxamic acid derivative represented by the following general formula [1] or a pharmaceutically acceptable salt thereof:

10. 发明公开

EP1031569A1 PROCESSES FOR PRODUCING 7-ISOINDOLINEQUINOLONECARBOXYLIC DERIVATIVES AND INTERMEDIATES THEREFOR, SALTS OF 7-ISOINDOLINEQUINOLONECARBOXYLIC ACIDS, HYDRATES THEREOF, AND COMPOSITION CONTAINING THE SAME AS ACTIVE INGREDIENT 有权
标题翻译： SALT 7-ISOINDOLINCHINOLONCARBONSÄURE衍生物，ITS MONOHYDRAT和组合物THESE作为活性成分的含
公开(公告)号：EP1031569A1
公开(公告)日：2000-08-30
申请号：EP98950405.5
申请日：1998-10-27
申请人： TOYAMA CHEMICAL CO., LTD.
发明人： YAMADA, Minoru , HAMAMOTO, Shoichi , HAYASHI, Kazuya , TAKAOKA, Kazuko , MATSUKURA, Hiroko , YOTSUJI, Minako , YONEZAWA, Kenji , OJIMA, Katsuji , TAKAMATSU, Tamotsu , TAYA, Kyoko , YAMAMOTO, Hirohiko , KIYOTO, Taro , KOTSUBO, Hironori
IPC分类号： C07D401/04 , C07D209/44 , C07D215/32 , C07C217/48 , C07C311/04 , C07C311/17 , C07F5/02 , A61K31/47 , B01J23/44 , B01J31/24
CPC分类号： C07D401/04 , A61K31/4709 , C07C217/48 , C07D209/44 , C07D215/56 , C07F5/025 , Y02P20/55
摘要： This invention relates to processes for producing a 7-isoindoline-quinolonecarboxylic acid derivative represented by the general formula [1] which is useful as an antibacterial agent, and an intermediate thereof:
wherein R 1 represents a hydrogen atom or a carboxyl-protecting group; R 2 represents a substituted or unsubstituted alkyl, alkenyl, cycloalkyl, aryl or heterocyclic group; R 3 represents at least one group selected from hydrogen atom, halogen atoms, substituted or unsubstituted alkyl, alkenyl, cycloalkyl, aryl, alkoxy or alkylthio groups, nitro group, cyano group, acyl groups, protected or unprotected hydroxyl groups and protected or unprotected or substituted or unsubstituted amino groups; R 4 represents at least one group selected from hydrogen atom, halogen atoms, substituted or unsubstituted alkyl, alkenyl, cycloalkyl, aralkyl, aryl, alkoxy or alkylthio groups, protected or unprotected hydroxyl or imino groups, protected or unprotected or substituted or unsubstituted amino groups, alkylidene groups, oxo group and groups each forming a cycloalkane group together with the carbon atom to which R 4 bonds; R 5 represents a hydrogen atom, an amino-protecting group, a substituted or unsubstituted alkyl, cycloalkyl, alkylsulfonyl, arylsulfonyl, acyl or aryl group; R 6 represents a hydrogen atom, a halogen atom, a substituted or unsubstituted alkyl, alkoxy or alkylthio group, a protected or unprotected hydroxyl or amino group or a nitro group; and A represents CH or C-R 7 in which R 7 represents a halogen atom, a substituted or unsubstituted alkyl, alkoxy or alkylthio group or a protected or unprotected hydroxyl group, and to a salt of a 7-isoindoline-quinolonecarboxylic acid represented by the general formula [1], a hydrate thereof and a composition comprising them as an active ingredient.
摘要翻译：本发明涉及用于生产由通式A1U所有这些是作为抗菌剂有用的，并在中间它们代表一个7哚啉喹诺酮羧酸衍生物： worin - [R <1> darstellt一个氢原子或羧基保护基; [R <2>表示一个substituiertem奥德unsubstituiertem烷基，烯基，环烷基，芳基或杂环基; 选自氢原子，卤原子，substituiertem奥德unsubstituiertem烷基，烯基，环烷基，芳基，烷氧基或烷硫基，硝基，氰基，酰基，保护或未被保护的羟基基团和被保护 - [R <3> darstellt至少一个基团或未受保护的或substituiertem奥德unsubstituiertem氨基; 选自氢原子，卤原子，substituiertem奥德unsubstituiertem烷基，烯基，环烷基，芳烷基，芳基，烷氧基或烷硫基，保护或未保护的羟基或亚氨基团，保护或未保护的或substituiertem奥德unsubstituiertem选择的R <4> darstellt至少一个基团氨基，亚烷基，氧代基团和基团各自的碳原子一起形成的环烷烃基团，其中R <4>键; [R <5>代表氢原子，在氨基保护基，一个substituiertem奥德unsubstituiertem烷基，环烷基，烷基磺酰基，芳基磺酰基，酰基或芳基; [R <6>代表氢原子，卤原子，substituiertem奥德unsubstituiertem烷基，烷氧基或烷硫基，保护或未保护的羟基或氨基或硝基; 和A darstellt CH或CR <7>中R <7> darstellt卤原子，substituiertem奥德unsubstituiertem烷基，烷氧基或烷硫基，或保护或未保护的羟基基团，和一个7哚啉喹诺酮羧酸的盐由通式所表示A1U，其水合物和一组合物，包含它们作为对活性成分。

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