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1. 发明授权

US08268789B2 PAR-2 antagonists 失效
标题翻译： PAR-2拮抗剂
公开(公告)号：US08268789B2
公开(公告)日：2012-09-18
申请号：US11576304
申请日：2005-09-30
申请人： Mototsugu Kabeya , Kyoko Yasuoka , Toru Kanke , Hiroyuki Ishiwata , Junya Tagashira
发明人： Mototsugu Kabeya , Kyoko Yasuoka , Toru Kanke , Hiroyuki Ishiwata , Junya Tagashira
IPC分类号： A61K38/06 , A61K38/02
CPC分类号： C07K5/0827 , A61K38/00 , C07D209/14 , C07K5/0806 , C07K5/0812
摘要： Compounds represented by the general formula (1) or salts thereof or solvates of both; PAR-2 antagonists containing the compounds; and preventive or therapeutic agents for PAR-2 related diseases containing the antagonists as the active ingredient: (1) wherein R1 is hydrogen, halogeno, or a group represented by the general formula (2): (wherein R11 is straight-chain or branched C1-6 alkylene or the like; and R12 and R13 together with the nitrogen atom adjacent to them form a 5- to 7-membered ring); R2 is straight-chain or branched C1-6 alkyl or the like; R3 and R4 are each independently hydrogen, one to three halogen atoms, or the like; and A1-A2-A3 is a tripeptide residue composed of α-amino acids each independently selected from the group consisting of glycine, alanine, cyclohexylalanine, and so on.
摘要翻译：由通式（1）表示的化合物或其盐或两者的溶剂合物; 含有这些化合物的PAR-2拮抗剂; 以及含有拮抗剂作为活性成分的PAR-2相关疾病的预防或治疗剂：（1）其中R1是氢，卤素或由通式（2）表示的基团：（其中R11是直链或支链的 C 1-6亚烷基等; R 12和R 13与它们相邻的氮原子一起形成5-至7-元环）; R2是直链或支链C 1-6烷基等; R3和R4各自独立地为氢，一至三个卤素原子等; A1-A2-A3是由各自独立地选自甘氨酸，丙氨酸，环己基丙氨酸等的α-氨基酸组成的三肽残基。

2. 发明申请

US20090131330A1 PAR-2 AGONIST 失效
公开(公告)号：US20090131330A1
公开(公告)日：2009-05-21
申请号：US11722952
申请日：2005-12-27
申请人： Hiroyuki Ishiwata , Mototsugu Kabeya , Toru Kanke
发明人： Hiroyuki Ishiwata , Mototsugu Kabeya , Toru Kanke
IPC分类号： A61K38/00 , C07K5/00 , A61P1/00
CPC分类号： C07K5/1016 , A61K38/00 , C07K7/06
摘要： Disclosed is a compound represented by the following general formula (1): Ar—CO-AA1-AA2-AA3-AA4-NH—X—NR1R2 (1) (wherein Ar represents an optionally substituted phenyl group or an aromatic heterocyclic group; AA1 represents a hydrophobic amino acid; AA2 represents an unsubstituted amino acid containing 2 or more carbon atoms; AA3 represents an unsubstituted amino acid containing 2 or more carbon atoms; AA4 represents a hydrophobic amino acid; X represents a divalent saturated aliphatic hydrocarbon group having 2-6 carbon atoms; and R1 and R2 may be the same or different and independently represent a saturated or unsubstituted aliphatic hydrocarbon group having 1-8 carbon atoms, or alternatively R1 and R2 may form a ring together with an adjacent nitrogen atom), a salt thereof, or a solvate of them. Also disclosed is a pharmaceutical composition for prevention/treatment of diseases associated with PAR-2 which is composed of the compound represented by the above general formula (1), a salt thereof or a solvate of them and a pharmaceutically acceptable carrier.
摘要翻译：公开了由以下通式（1）表示的化合物：Ar-CO-AA1-AA2-AA3-AA4-NH-X-NR1R2（1）（其中Ar表示任选取代的苯基或芳族杂环基; AA1 表示疏水性氨基酸; AA2表示含有2个以上碳原子的未取代氨基酸; AA3表示含有2个以上碳原子的未取代氨基酸; AA4表示疏水性氨基酸; X表示二价饱和脂肪族烃基， 6个碳原子; R1和R2可以相同或不同，并且独立地表示具有1-8个碳原子的饱和或未取代的脂族烃基，或者R1和R2可以与相邻的氮原子一起形成环），盐或它们的溶剂合物。还公开了用于预防/治疗与由上述通式（1）表示的化合物，其盐或它们的溶剂化物和药学上可接受的载体组成的PAR-2相关疾病的药物组合物。

3. 发明授权

US08133864B2 PAR-2 agonist 失效
标题翻译： PAR-2激动剂
公开(公告)号：US08133864B2
公开(公告)日：2012-03-13
申请号：US11909931
申请日：2006-03-29
申请人： Hiroyuki Ishiwata , Mototsugu Kabeya , Toru Kanke
发明人： Hiroyuki Ishiwata , Mototsugu Kabeya , Toru Kanke
IPC分类号： A61K38/08 , C07K5/083 , C07K5/087
CPC分类号： C07K5/0812 , A61K38/00 , C07K5/101 , C07K5/1016
摘要： The present invention relates to a pharmaceutical composition for preventing/treating conditions associated with PAR-2. The present invention also relates to a method for preventing/treating the condition using the pharmaceutical composition and use for manufacturing the pharmaceutical composition. The pharmaceutical composition comprises a compound represented by the following general formula (1), salt or solvate thereof and a pharmaceutically acceptable carrier: Ar—CO—AA1—AA2—AA3—AA4—NH—X—Y (1) wherein, Ar represents a phenyl group or an aromatic heterocyclic group optionally having substituent(s): AA1 represents a hydrophobic amino acid: AA2 represents an amino acid absent of substituent(s) having more than two carbon atoms: AA3 represents an amino acid absent of substituent(s) having more than two carbon atoms: AA4 represents a basic amino acid: X represents a straight chain or branched bivalent saturated aliphatic hydrocarbon group having 1 to 6 carbon atoms: Y represents basic substituent(s); straight chain, branched, or cyclic bivalent saturated aliphatic hydrocarbon group having 1 to 6 carbon atoms; or an aromatic hydrocarbon group having 6 to 10 carbon atoms. The compound represented by the general formula (1) has dramatically improved PAR-2 activation potency compared to peptide comprised of 6 amino acids (Tethered receptor agonist peptide: TRAP) in spite of reduction of the number of amino acid.
摘要翻译：本发明涉及用于预防/治疗与PAR-2相关的病症的药物组合物。本发明还涉及使用药物组合物预防/治疗病症的方法以及用于制造药物组合物的方法。药物组合物包含由以下通式（1）表示的化合物，其盐或溶剂合物和药学上可接受的载体：Ar-CO-AA1-AA2-AA3-AA4-NH-X-Y（1）其中Ar表示任选具有取代基的苯基或芳族杂环基：AA1表示疏水性氨基酸：AA2表示不具有多于两个碳原子的取代基的氨基酸：AA3表示不存在取代基的氨基酸（s ）：AA4表示碱性氨基酸：X表示具有1〜6个碳原子的直链或支链二价饱和脂肪族烃基：Y表示碱性取代基; 具有1至6个碳原子的直链，支链或环状二价饱和脂族烃基; 或碳原子数为6〜10的芳香族烃基。尽管氨基酸数量的减少，但由通式（1）表示的化合物与包含6个氨基酸的肽（束缚受体激动剂肽：TRAP）相比，显着提高了PAR-2的活化效力。

4. 发明申请

US20090012006A1 Par-2 Antagonists 失效
标题翻译： Par-2拮抗剂
公开(公告)号：US20090012006A1
公开(公告)日：2009-01-08
申请号：US11576304
申请日：2005-09-30
申请人： Mototsugu Kabeya , Kyoko Yasuoka , Toru Kanke , Hiroyuki Ishiwata , Junya Tagashira
发明人： Mototsugu Kabeya , Kyoko Yasuoka , Toru Kanke , Hiroyuki Ishiwata , Junya Tagashira
IPC分类号： A61K38/06 , C07K5/083 , A61P35/00 , A61P11/06
CPC分类号： C07K5/0827 , A61K38/00 , C07D209/14 , C07K5/0806 , C07K5/0812
摘要： Compounds represented by the general formula (1) or salts thereof or solvates of both; PAR-2 antagonists containing the compounds; and preventive or therapeutic agents for PAR-2 related diseases containing the antagonists as the active ingredient: (1) wherein R1 is hydrogen, halogeno, or a group represented by the general formula (2): (wherein R11 is straight-chain or branched C1-6 alkylene or the like; and R12 and R13 together with the nitrogen atom adjacent to them form a 5- to 7-membered ring); R2 is straight-chain or branched C1-6 alkyl or the like; R3 and R4 are each independently hydrogen, one to three halogen atoms, or the like; and A1-A2-A3 is a tripeptide residue composed of α-amino acids each independently selected from the group consisting of glycine, alanine, cyclohexylalanine, and so on.
摘要翻译：由通式（1）表示的化合物或其盐或两者的溶剂合物; 含有这些化合物的PAR-2拮抗剂; 以及含有拮抗剂作为活性成分的PAR-2相关疾病的预防或治疗剂：（1）其中R1是氢，卤素或由通式（2）表示的基团：（其中R11是直链或支链的 C 1-6亚烷基等; R 12和R 13与它们相邻的氮原子一起形成5-至7-元环）; R2是直链或支链C 1-6烷基等; R3和R4各自独立地为氢，一至三个卤素原子等; 并且A1-A2-A3是由各自独立地选自甘氨酸，丙氨酸，环己基丙氨酸等的α-氨基酸组成的三肽残基。

5. 发明申请

US20090215703A1 PAR-2 Agonist 失效
标题翻译： PAR-2激动剂
公开(公告)号：US20090215703A1
公开(公告)日：2009-08-27
申请号：US11909931
申请日：2006-03-29
申请人： Hiroyuki Ishiwata , Mototsugu Kabeya , Toru Kanke
发明人： Hiroyuki Ishiwata , Mototsugu Kabeya , Toru Kanke
IPC分类号： A61K38/03 , C07K4/00 , A61P27/00
CPC分类号： C07K5/0812 , A61K38/00 , C07K5/101 , C07K5/1016
摘要： The present invention relates to a pharmaceutical composition for preventing/treating conditions associated with PAR-2. The present invention also relates to a method for preventing/treating the condition using the pharmaceutical composition and use for manufacturing the pharmaceutical composition. The pharmaceutical composition comprises a compound represented by the following general formula (1), salt or solvate thereof and a pharmaceutically acceptable carrier: Ar—CO-AA1-AA2-AA3-AA4-NH—X—Y (1) wherein, Ar represents a phenyl group or an aromatic heterocyclic group optionally having substituent(s): AA1 represents a hydrophobic amino acid: AA2 represents an amino acid absent of substituent (s) having more than two carbon atoms: AA3 represents an amino acid absent of substituent(s) having more than two carbon atoms: AA4 represents a basic amino acid: X represents a straight-chain or branched bivalent saturated aliphatic hydrocarbon group having 1 to 6 carbon atoms: Y represents basic substituent (s); straight-chain, branched, or cyclic bivalent saturated aliphatic hydrocarbon group having 1 to 6 carbon atoms, or an aromatic hydrocarbon group having 6 to 10 carbon atoms. The compound represented by the general formula (1) has dramatically improved PAR-2 activation potency compared to peptide comprised of 6 amino acids (Tethered receptor agonist peptide: TRAP) in spite of reduction of the number of amino acid.
摘要翻译：本发明涉及用于预防/治疗与PAR-2相关的病症的药物组合物。本发明还涉及使用药物组合物预防/治疗病症的方法以及用于制造药物组合物的方法。药物组合物包含由以下通式（1）表示的化合物，其盐或溶剂化物和药学上可接受的载体：Ar-CO-AA1-AA2-AA3-AA4-NH-XY（1）其中Ar表示苯基基团或任选具有取代基的芳族杂环基：AA1表示疏水性氨基酸：AA2表示不具有多于两个碳原子的取代基的氨基酸：AA3表示不具有取代基的氨基酸，两个以上碳原子：AA4表示碱性氨基酸：X表示碳原子数1〜6的直链或支链二价饱和脂肪族烃基，Y表示碱性取代基。具有1至6个碳原子的直链，支链或环状二价饱和脂族烃基或具有6至10个碳原子的芳族烃基。尽管氨基酸数量的减少，但由通式（1）表示的化合物与包含6个氨基酸的肽（束缚受体激动剂肽：TRAP）相比，显着提高了PAR-2的活化效力。

6. 发明授权

US07910556B2 PAR-2 agonist 失效
标题翻译： PAR-2激动剂
公开(公告)号：US07910556B2
公开(公告)日：2011-03-22
申请号：US11722952
申请日：2005-12-27
申请人： Hiroyuki Ishiwata , Mototsugu Kabeya , Toru Kanke
发明人： Hiroyuki Ishiwata , Mototsugu Kabeya , Toru Kanke
IPC分类号： A61K38/07 , C07K5/10
CPC分类号： C07K5/1016 , A61K38/00 , C07K7/06
摘要： A compound, or a salt or solvate thereof having a structure of Ar—CO-AA1-AA2-AA3-AA4-NH—X—NR1R2 is disclosed. Ar represents an optionally substituted phenyl group or an aromatic heterocyclic group; AA1 represents a hydrophobic amino acid; AA2 represents an unsubstituted amino acid containing 2 or more carbon atoms; AA3 represents an unsubstituted amino acid containing 2 or more carbon atoms; AA4 represents a hydrophobic amino acid; X represents a divalent saturated aliphatic hydrocarbon group having 2-6 carbon atoms; and R1 and R2 represent a saturated or unsubstituted aliphatic hydrocarbon group having 1-8 carbon atoms, or alternatively R1 and R2 may form a ring together with an adjacent nitrogen atom. A pharmaceutical composition for prevention/treatment of diseases associated with PAR-2 is also disclosed. The pharmaceutical composition includes the above compound, a salt or a solvate thereof and a pharmaceutically acceptable carrier.
摘要翻译：公开了具有Ar-CO-AA1-AA2-AA3-AA4-NH-X-NR1R2结构的化合物或其盐或溶剂化物。 Ar表示可以具有取代基的苯基或芳香族杂环基; AA1表示疏水性氨基酸; AA2表示含有2个以上碳原子的未取代氨基酸; AA3表示含有2个以上碳原子的未取代氨基酸; AA4表示疏水性氨基酸; X表示具有2-6个碳原子的二价饱和脂族烃基; 并且R 1和R 2表示具有1-8个碳原子的饱和或未取代的脂族烃基，或者R 1和R 2可以与相邻的氮原子一起形成环。还公开了用于预防/治疗与PAR-2相关的疾病的药物组合物。药物组合物包括上述化合物，其盐或其溶剂化物和药学上可接受的载体。

7. 发明授权

US07196101B2 Bis(5-aryl-2-pyridyl) derivatives 失效
标题翻译：双（5-芳基-2-吡啶基）衍生物
公开(公告)号：US07196101B2
公开(公告)日：2007-03-27
申请号：US10690671
申请日：2003-10-23
申请人： Hiroyuki Ishiwata , Seiichi Sato , Mototsugu Kabeya , Soichi Oda , Makoto Suda , Manabu Shibasaki
发明人： Hiroyuki Ishiwata , Seiichi Sato , Mototsugu Kabeya , Soichi Oda , Makoto Suda , Manabu Shibasaki
IPC分类号： A61P37/08 , A61K31/44 , C07D213/00
CPC分类号： C07D487/04 , C07D213/74 , C07D401/14 , C07D405/14 , C07D409/14
摘要： A bis(5-aryl-2-pyridyl) compound represented by formula (1) or a salt thereof: wherein A is a substituted or unsubstituted aromatic hydrocarbyl group or a substituted or unsubstituted aromatic heterocyclic group, and X is a group selected from the group consisting of moieties having formulas (2) to (5): wherein, in formula (2), m is an integer of 1 or 2; in formula (3), n is an integer of 1 to 6; and in formula (4), R is hydrogen or a lower alkyl group and p is an integer of 1 to 6.
摘要翻译：由式（1）表示的双（5-芳基-2-吡啶基）化合物或其盐：

8. 发明授权

US06890940B2 Bis(2-aryl-5-pyridyl) derivatives 失效
标题翻译：双（2-芳基-5-吡啶基）衍生物
公开(公告)号：US06890940B2
公开(公告)日：2005-05-10
申请号：US09893680
申请日：2001-06-29
申请人： Hiroyuki Ishiwata , Seiichi Sato , Mototsugu Kabeya , Soichi Oda , Makoto Suda , Manabu Shibasaki
发明人： Hiroyuki Ishiwata , Seiichi Sato , Mototsugu Kabeya , Soichi Oda , Makoto Suda , Manabu Shibasaki
IPC分类号： A61P37/00 , A61P37/08 , A61P43/00 , C07D213/74 , C07D401/14 , C07D405/14 , A61K31/44 , C07D213/00
CPC分类号： C07D213/74 , C07D401/14 , C07D405/14
摘要： A bis(2-aryl-5-pyridyl) compound having formula (1) or a salt thereof: wherein A is a substituted or unsubstituted aromatic hydrocarbon group, and X is a substituent having one of the following formulas (2) to (4): wherein, in formula (2), R1 is a hydrogen atom or a di(lower alkyl)amino(lower alkyl) group, and m is an integer of 1 or 2; in formula (3), Y1 and Y2 each is a nitrogen atom or a CH group, and n is 0 or an integer of 1 to 6; in formula (4), R2 and R3 each is a hydrogen atom or a lower alkyl group, Z represents a single bond, a substituted methylene group, a substituted imino group, an oxygen atom or a cycloalkylene group, and p and q each is 0 or an integer of 1 to 6.
摘要翻译：具有式（1）的双（2-芳基-5-吡啶基）化合物或其盐：其中A是取代或未取代的芳族烃基，X是具有下式（2）至（4）中的一个的取代基）其中，在式（2）中，R 1是氢原子或二（低级烷基）氨基（低级烷基）基团，m是1或2的整数; 在式（3）中，Y 1和Y 2各自为氮原子或CH基团，n为0或1至6的整数; 在式（4）中，R 2和R 3各自为氢原子或低级烷基，Z表示单键，取代亚甲基，取代亚氨基基团，氧原子或亚环烷基，p和q各自为0或1〜6的整数。

9. 发明授权

US06576642B2 Diamide compounds and compositions containing the same 失效
标题翻译：二酰胺化合物和含有它们的组合物
公开(公告)号：US06576642B2
公开(公告)日：2003-06-10
申请号：US09858592
申请日：2001-05-17
申请人： Hiroyuki Ishiwata , Mototsugu Kabeya , Masami Shiratsuchi , Yukio Hattori , Hiroshi Nakao , Takao Nagoya , Seiichi Sato , Soichi Oda , Makoto Suda , Manabu Shibasaki
发明人： Hiroyuki Ishiwata , Mototsugu Kabeya , Masami Shiratsuchi , Yukio Hattori , Hiroshi Nakao , Takao Nagoya , Seiichi Sato , Soichi Oda , Makoto Suda , Manabu Shibasaki
IPC分类号： A61K31165
CPC分类号： C07D213/40 , C07C235/34 , C07C235/36 , C07C235/38 , C07C235/44 , C07C235/56 , C07C237/34 , C07C2601/14 , C07C2602/08 , C07C2602/10 , C07D207/09 , C07D207/14 , C07D213/75 , C07D213/82
摘要： Compounds having the formula (1): wherein A is a phenyl, naphthyl, dihydronaphthyindeny, pyridyl, indolyl,isoindolyl, quinolyl or isoquinolyl group which are optionally substituted; X is optionally substituted alicyclic, aromatic, imino or heterocyclic groups or —S— or —O—; Y is a single bond or an alkylene group; Z is an unsubstituted aliphatic group or divalent residue of benzene or pyridine, which is optionally substituted; anis hydrogen, lower alkyl, cycloalkyl, aryl or aralkyl; with certain provisos. These compounds exhibit an inhibitory effect on the production of IgE antibodies and are, hence, useful as antiallergic agents.
摘要翻译：具有式（1）的化合物：其中A是任选取代的苯基，萘基，二氢萘并噻吩基，吡啶基，吲哚基，异吲哚基，喹啉基或异喹啉基; X是任选取代的脂环族，芳族，亚氨基或杂环基或-S-或-O-; Y是单键或亚烷基; Z是任选取代的未取代的脂族基团或苯或吡啶的二价残基; 芳烃氢，低级烷基，环烷基，芳基或芳烷基; 具有一定的条件。这些化合物对IgE抗体的产生具有抑制作用，因此可用作抗过敏剂。

10. 发明授权

US06448242B1 Cyclic amide compounds 失效
标题翻译：环状酰胺化合物
公开(公告)号：US06448242B1
公开(公告)日：2002-09-10
申请号：US09622586
申请日：2000-08-21
申请人： Hiroyuki Ishiwata , Seiichi Sato , Mototsugu Kabeya , Soichi Oda , Yukio Hattori , Makoto Suda , Manabu Shibasaki , Hiroshi Nakao , Takao Nagoya
发明人： Hiroyuki Ishiwata , Seiichi Sato , Mototsugu Kabeya , Soichi Oda , Yukio Hattori , Makoto Suda , Manabu Shibasaki , Hiroshi Nakao , Takao Nagoya
IPC分类号： A07N4300
CPC分类号： C07D213/70 , C07C2601/14 , C07D211/26 , C07D211/34 , C07D211/58 , C07D213/38 , C07D213/82 , C07D295/185 , C07D295/192 , C07D401/14
摘要： The invention relates to compounds represented by the following general formula (1): wherein A is an aromatic compound which may be substituted, or the like, B is a nitrogen atom or CH, X is a lower alkylene group which may be substituted, or the like, Y is a single bond or the like; Z is a divalent residue of benzene which may be substituted, or the like, and m and n are independently an integer of 1 to 4, and medicines comprising such a compound. These compounds have an excellent inhibitory effect on the production of an IgE antibody and are hence useful as antiallergic agents and the like.
摘要翻译：本发明涉及由以下通式（1）表示的化合物：其中A是可被取代的芳族化合物等，B是氮原子或CH，X是可被取代的低级亚烷基，或类似物，Y是单键等; Z是可以被取代的苯的二价残基等，m和n分别是1〜4的整数，以及包含这种化合物的药物。这些化合物对IgE抗体的产生具有优异的抑制作用，因此可用作抗变应性剂等。

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