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1.发明申请Par-2-activating peptide derivative and pharmaceutical composition using the same 失效对二激活肽衍生物和使用其的药物组合物公开(公告)号：US20050222384A1
公开(公告)日：2005-10-06
申请号：US10517803
申请日：2003-06-10
申请人： Robert Ramage , Robin Plevin , Kevin Shaw , Lu Jiang , Louise Young , Alan Harvey , Pu Wang , Toru Kanke , Junichi Kawagoe , Mototsugu Kabeya
发明人： Robert Ramage , Robin Plevin , Kevin Shaw , Lu Jiang , Louise Young , Alan Harvey , Pu Wang , Toru Kanke , Junichi Kawagoe , Mototsugu Kabeya
IPC分类号： A61K38/00 , A61P1/00 , A61P1/02 , A61P1/04 , A61P1/12 , A61P1/14 , A61P27/02 , A61P27/04 , A61P43/00 , C07K7/06 , C07K14/705 , A61K38/08 , C07K5/06
CPC分类号： C07K14/705 , A61K38/00 , C07K7/06
摘要： The present invention relates to a peptide derivative represented by the general formula (I) or a salt thereof: Z-(CH2)n—CO—NH-Leu-Ile-Gly-AA1-AA2-CO—R (I) wherein Z represents an aryl group which may or may not have a substituent or a heteroaryl group which may or may not have a substituent; n represents 0, 1 or 2: AA1-AA2 represents Lys-Val or Arg-Leu; and R represents —OH or —NH2, and relates to a pharmaceutical composition comprising a peptide derivative represented by the general formula (I) or a salt thereof, and a pharmaceutically acceptable carrier thereof.
摘要翻译： 本发明涉及由通式（I）表示的肽衍生物或其盐：Z-（CH 2 CH 2）n -CO-NH-Leu-Ile 其中Z表示可以具有或可以不具有取代基的芳基或可以不具有取代基的芳基或可以具有取代基的杂芳基， 可能没有取代基; n表示0,1或2：AA 1 -A 2 2表示Lys-Val或Arg-Leu; 并且R表示-OH或-NH 2，并且涉及包含由通式（I）表示的肽衍生物或其盐及其药学上可接受的载体的药物组合物。
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2.发明授权Par-2-activating peptide derivative and pharmaceutical composition using the same 失效对二激活肽衍生物和使用其的药物组合物公开(公告)号：US07541339B2
公开(公告)日：2009-06-02
申请号：US10517803
申请日：2003-06-10
申请人： Robert Ramage , Robin Plevin , Kevin Thomas Shaw , Lu Jiang , Louise Claire Young , Alan Lang Harvey , Pu Wang , Toru Kanke , Junichi Kawagoe , Mototsugu Kabeya
发明人： Robert Ramage , Robin Plevin , Kevin Thomas Shaw , Lu Jiang , Louise Claire Young , Alan Lang Harvey , Pu Wang , Toru Kanke , Junichi Kawagoe , Mototsugu Kabeya
CPC分类号： C07K14/705 , A61K38/00 , C07K7/06
摘要： The present invention relates to a peptide derivative represented by the general formula (I) or a salt thereof: Z-(CH2)n—CO—NH-Leu-Ile-Gly-AA1-AA2-CO—R (I) wherein Z represents an aryl group which may or may not have a substituent or a heteroaryl group which may or may not have a substituent; n represents 0, 1 or 2: AA1-AA2 represents Lys-Val or Arg-Leu; and R represents —OH or —NH2, and relates to a pharmaceutical composition comprising a peptide derivative represented by the general formula (I) or a salt thereof, and a pharmaceutically acceptable carrier thereof. The peptide derivative is useful as a prophylactic and therapeutic agent of dysfunction of masticatory, dysphagia, dysgeusia, ozostomia, intra-oral cavity dysphoria, intra-oral cavity infections, intra-oral cavity inflammations, dry eye, ectocornea detachment, keratitis, corneal ulcer, conjunctivitis, stomach ulcer, duodenal ulcer, gastritis, diarrhea, enteritis or Sjogren's syndrome.
摘要翻译： 本发明涉及由通式（I）表示的肽衍生物或其盐：Z-（CH2）n-CO-NH-Leu-Ile-Gly-AA1-AA2-CO-R（Ⅰ）其中Z 表示可以具有也可以不具有取代基的芳基或可以具有取代基的杂芳基; n表示0,1或2：AA1-AA2表示Lys-Val或Arg-Leu; 和R表示-OH或-NH 2，并且涉及包含由通式（I）表示的肽衍生物或其盐及其药学上可接受的载体的药物组合物。 肽衍生物可用作咀嚼，吞咽困难，发重症，口臭，口腔内烦躁，口腔内感染，口腔内炎症，干眼症，异位角脱落，角膜炎，角膜溃疡功能障碍的预防和治疗剂 ，结膜炎，胃溃疡，十二指肠溃疡，胃炎，腹泻，肠炎或干燥综合征。
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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
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。
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公开(公告)号：US08268789B2
公开(公告)日：2012-09-18
申请号：US11576304
申请日：2005-09-30
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。
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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
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。
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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
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。
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公开(公告)号：US20090012006A1
公开(公告)日：2009-01-08
申请号：US11576304
申请日：2005-09-30
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。
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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
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。
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公开(公告)号：US20060183664A1
公开(公告)日：2006-08-17
申请号：US10496851
申请日：2002-12-13
申请人： Toshiaki Takizawa , Masaki Tamiya , Naohiro Saito , Toru Kanke , Jiro Matsumoto , Yasushi Wada , Junichi Kawagoe , William Ferrell , John Lockhart
发明人： Toshiaki Takizawa , Masaki Tamiya , Naohiro Saito , Toru Kanke , Jiro Matsumoto , Yasushi Wada , Junichi Kawagoe , William Ferrell , John Lockhart
IPC分类号： A61K38/54
CPC分类号： A61K45/06 , A61K31/00 , Y02A50/423 , A61K2300/00
摘要： The present invention provides a pharmaceutical composition by a novel action mechanism without serious side effects for delayed hypersensitivity and a screening method of the same. The invention also provides a novel assay method of inhibitors/suppressive agents of PAR-2. The invention relates to a pharmaceutical composition for delayed hypersensitivity containing one or two or more active ingredients selected from the group consisting of inhibitors of PAR-2 and suppressive agents of PAR-2 gene expression and a pharmaceutically acceptable carrier, and to a method for screening active ingredients for pharmaceutical composition for delayed hypersensitivity by contacting a subject substance with cells expressing PAR-2 and by determining expression or activity of PAR-2. The invention also relates to a method for detecting or quantifying actions of the subject substance for PAR-2 using cells expressing PAR-2 in a culture containing inositol.
摘要翻译： 本发明通过新颖的作用机理提供药物组合物，对迟发性超敏反应没有严重的副作用及其筛选方法。 本发明还提供了PAR-2抑制剂/抑制剂的新型测定方法。 本发明涉及一种用于延迟超敏反应的药物组合物，其含有选自PAR-2的抑制剂和PAR-2基因表达的抑制剂的一种或两种以上活性成分和药学上可接受的载体，以及筛选方法 通过使受试物质与表达PAR-2的细胞接触并通过测定PAR-2的表达或活性来延迟超敏反应的药物组合物的活性成分。 本发明还涉及使用含有肌醇的培养物中表达PAR-2的细胞检测或定量PAR-2的物质的作用的方法。
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公开(公告)号：US07423009B2
公开(公告)日：2008-09-09
申请号：US10673380
申请日：2003-09-30
申请人： Takashi Nakagawa , Hiroyuki Ishiwata , Toshiaki Takizawa , Toru Kanke , Yasushi Wada , Junichi Kawagoe
发明人： Takashi Nakagawa , Hiroyuki Ishiwata , Toshiaki Takizawa , Toru Kanke , Yasushi Wada , Junichi Kawagoe
CPC分类号： A61K38/4846 , A61K38/08 , A61K38/482 , A61K38/4826 , G01N33/6893 , G01N2500/00 , G01N2800/347
摘要： The present invention relates to a composition for prevention and treatment of kidney diseases comprising one or more effective component(s) of a PAR-2 activating agent which is able to activate PAR-2 and a pharmaceutically acceptable carrier. The present invention further relates to a method for prevention and treatment of kidney diseases comprising administration of a composition for prevention and treatment of kidney diseases containing a PAR-2 activating agent which is able to activate PAR-2 to patients suffering from kidney diseases, and also relates to the use of a PAR-2 activating agent which is able to activate PAR-2 for the manufacture of a composition for prevention and treatment of kidney diseases. The present invention furthermore relates to a method for screening an effective ingredient for prevention and treatment of kidney diseases comprising screening of the activating action of the test substance to PAR-2.
摘要翻译： 本发明涉及一种用于预防和治疗肾脏疾病的组合物，其包含能够激活PAR-2的PAR-2活化剂的一种或多种有效成分和药学上可接受的载体。 本发明还涉及一种用于预防和治疗肾脏疾病的方法，其包括给予含有能够使患有肾脏疾病的患者PAR-2的PAR-2激活剂的肾脏疾病的预防和治疗组合物，以及 还涉及能够激活PAR-2用于制备用于预防和治疗肾脏疾病的组合物的PAR-2活化剂的用途。 本发明还涉及筛选用于预防和治疗肾脏疾病的有效成分的方法，其包括将测试物质的活化作用筛选到PAR-2。
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