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1. 发明授权

US07622589B2 Substituted sulfonylaminoarylmethyl cyclopropanecarboxamide as VR1 receptor antagonists 失效
标题翻译：取代磺酰基氨基芳基甲基环丙烷甲酰胺作为VR1受体拮抗剂
公开(公告)号：US07622589B2
公开(公告)日：2009-11-24
申请号：US11384127
申请日：2006-03-17
申请人： Takeshi Hanazawa , Misato Hirano , Tadashi Inoue , Satoshi Nagayama , Kazunari Nakao , Yuji Shishido , Hirotaka Tanaka
发明人： Takeshi Hanazawa , Misato Hirano , Tadashi Inoue , Satoshi Nagayama , Kazunari Nakao , Yuji Shishido , Hirotaka Tanaka
IPC分类号： C07D213/02 , A61K31/44 , A61K31/445
CPC分类号： C07C61/28 , C07C61/40 , C07C311/08 , C07C317/44 , C07C323/62 , C07C2601/02 , C07D213/26 , C07D213/56 , C07D213/74 , C07D213/76
摘要： This invention provides a compound of the formula (I): wherein, variables A, B, D, E, and R1 to R11 are as defined in the specification.
摘要翻译：本发明提供式（I）的化合物：其中变量A，B，D，E和R 1至R 11如说明书中所定义。

2. 发明授权

US07915448B2 Substituted sulfonylaminoarylmethyl cyclopropanecarboxamide as VR1 receptor antagonists 失效
公开(公告)号：US07915448B2
公开(公告)日：2011-03-29
申请号：US12578061
申请日：2009-10-13
申请人： Takeshi Hanazawa , Misato Hirano , Tadashi Inoue , Satoshi Nagayama , Kazunari Nakao , Yuji Shishido , Hirotaka Tanaka
发明人： Takeshi Hanazawa , Misato Hirano , Tadashi Inoue , Satoshi Nagayama , Kazunari Nakao , Yuji Shishido , Hirotaka Tanaka
IPC分类号： C07C311/03 , A61K31/18
CPC分类号： C07C61/28 , C07C61/40 , C07C311/08 , C07C317/44 , C07C323/62 , C07C2601/02 , C07D213/26 , C07D213/56 , C07D213/74 , C07D213/76
摘要： This invention provides a compound of the formula (I): wherein A and B are independently CR12 or N; D and E are each independently CR9 or N; R1 represents (C1-C6)alkyl; R2 represents hydrogen, halogen, hydroxy, (C1-C6) alkyl, halo(C1-C6) alkyl, hydroxy(C1-C6) alkyl, (C1-C6)alkoxy or (C1-C6)alkoxy-(C1-C6)alkyl; R3, R4, R5, R6, R10 and R11 each independently represent hydrogen, halogen, (C1-C6)alkyl, halo(C1-C6)alkyl, (C1-C6)alkoxy, hydroxy(C1-C6)alkyl or (C1-C6)alkoxy-(C1-C6)alkyl; or R3 and R4 are taken together with the carbon atom to which they are attached to form a 3- to 7-membered carbocyclic ring or heterocyclic ring in which one or two non-adjacent carbon atoms are optionally replaced by an oxygen atom, a sulfur atom or NH; R7 and R9 each independently represent hydrogen, halogen, (C1-C6)alkyl, halo(C1-C6)alkyl, hydroxy(C1-C6)alkyl, (C1-C6)alkoxy, hydroxy(C1-C6)alkoxy, (C1-C6)alkoxy-(C1-C6)alkyl, (C1-C6)alkoxy-(C1-C6)alkoxy, (C1-C6)alkylthio, (C1-C6)alkylsulfinyl, (C1-C6)alkylsulfonyl, NH2, [(C1-C6)alkyl]NH—, [(C1-C6)alkyl]2N—, H2N—(C1-C6)alkoxy, (C1-C6)alkyl-NH—(C1-C6)alkoxy, [(C1-C6)alkyl]2N(C1-C6)alkoxy; H2N—(C1-C6)alkoxy-(C1-C6)alkyl, (C1-C6)alkyl-NH—(C1-C6)alkoxy-(C1-C6)alkyl, [(C1-C6)alkyl]2N(C1-C6)alkoxy-(C1-C6)alkyl or 5- or 6- membered heterocyclic ring containing at least one nitrogen atom; R8 represents halogen, (C1-C6)alkyl, halo(C1-C6)alkyl, hydroxy(C1-C6)alkyl, (C1-C6)alkoxy, hydroxy(C1-C6)alkoxy, (C1-C6)alkoxy-(C1-C6)alkyl, (C1-C6)alkoxy-(C1-C6)alkoxy, halo(C1-C6)alkylsulfonyl, halo(C1-C6)alkylsulfinyl, halo(C1-C6)alkoxy, halo(C1-C6)alkylthio, [(C1-C6)alkyl]NH— or [(C1-C6)alkyl]2N—; or R7 and R8, when E is CR9, are taken together with the carbon atoms to which they are attached form a 5-8 membered carbocyclic or heterocyclic ring, in which one or two non-adjacent carbon atoms are optionally replaced by oxygen, sulfur, N or NH groups, wherein the carbocyclic ring or the heterocyclic ring is unsubstituted or substituted with one or more substituents each independently selected from the group consisting of hydroxy, (C1-C6)alkyl, (C1-C6)alkoxy and hydroxy(C1-C6)alkyl; and R12 represents hydrogen, halogen, (C1-C6)alkyl or hydroxy(C1-C6)alkyl; or a pharmaceutically acceptable salt or solvate thereof.

3. 发明授权

US07514457B2 Substituted aryloxymethyl bicyclicmethyl acetamide compounds 失效
标题翻译：取代的芳氧基甲基双环甲基乙酰胺化合物
公开(公告)号：US07514457B2
公开(公告)日：2009-04-07
申请号：US11421242
申请日：2006-05-31
申请人： Tadashi Inoue , Satoshi Nagayama , Yuji Shishido
发明人： Tadashi Inoue , Satoshi Nagayama , Yuji Shishido
IPC分类号： A61K31/4045 , A61K31/4168 , A61K31/416 , A61K31/4192 , A61K31/428 , C07D235/12 , C07D231/56 , C07D277/62 , C07D209/14 , C07D249/18
CPC分类号： C07D277/62 , C07D209/34 , C07D231/56 , C07D235/06 , C07D235/26 , C07D249/18 , C07D263/58
摘要： Compounds of the general formula (I): pharmaceutical compositions comprising a compound of general formula (I); and methods of treating disease conditions caused by overactivation of the VR1 receptor by administering a compound of general formula (I) to a subject.
摘要翻译：通式（I）的化合物：包含通式（I）的化合物的药物组合物; 以及通过向受试者施用通式（I）的化合物来治疗由VR1受体的过度活化引起的疾病状态的方法。

4. 发明申请

US20060205980A1 Substituted N-sulfonylaminophenylethyl-2-phenoxyacetamide compounds as VR1 receptor antagonists 失效
公开(公告)号：US20060205980A1
公开(公告)日：2006-09-14
申请号：US11372706
申请日：2006-03-10
申请人： Takeshi Hanazawa , Misato Hirano , Tadashi Inoue , Satoshi Nagayama , Kazunari Nakao , Yuji Shishido , Hirotaka Tanaka
发明人： Takeshi Hanazawa , Misato Hirano , Tadashi Inoue , Satoshi Nagayama , Kazunari Nakao , Yuji Shishido , Hirotaka Tanaka
IPC分类号： C07C311/46
CPC分类号： C07C311/08
摘要： This invention provides a compound of the formula (I): wherein R1 represents (C1-C6)alkyl; R2 represents a hydrogen atom, a halogen atom, a hydroxy group, (C1-C6)alkyl, (C1-C6)alkoxy, hydroxy(C1-C6)alkyl, (C1-C6)alkoxy-(C1-C6)alkyl or halo(C1-C6)alkyl; R3 represents a halogen atom, (C1-C6)alkyl, (C1-C6)alkoxy, hydroxy(C1-C6)alkoxy, (C1-C6)alkoxy-(C1-C6)alkyl, (C1-C6)alkoxy-(C1-C6)alkoxy, halo(C1-C6)alkyl, (C1-C6)alkylthio, (C1-C6)alkylsulfinyl, (C1-C6)alkylsulfonyl, [(C1-C6)alkyl]NH—, or [(C1-C6)alkyl]2N—; R4 represents a halogen atom, (C1-C6)alkyl, halo(C1-C6)alkyl, (C1-C6)alkoxy, hydroxy(C1-C6)alkoxy, (C1-C6)alkoxy-(C1-C6)alkyl, (C1-C6)alkoxy-(C1-C6)alkoxy, [(C1-C6)alkyl]NH—, or [(C1-C6)alkyl]2N—; R5 represents a halogen atom, (C1-C6)alkyl, (C1-C6)alkoxy, hydroxy(C1-C6)alkoxy, (C1-C6)alkoxy-(C1-C6)alkyl, (C1-C6)alkoxy-(C1-C6)alkoxy, halo(C1-C6)alkyl, (C1-C6)alkylthio, (C1-C6)alkylsulfinyl, (C1-C6)alkylsulfonyl, [(C1-C6)alkyl]NH—, [(C1-C6)alkyl]2N—, H2N—(C1-C6)alkoxy, (C1-C6)alkyl-NH—(C1-C6)alkoxy, [(C1-C6)alkyl]2N(C1-C6)alkoxy, H2N—(C1-C6)alkoxy-(C1-C6)alkyl, (C1-C6)alkyl-NH—(C1-C6)alkoxy-(C1-C6)alkyl, or [(C1-C6)alkyl]2N(C1-C6)alkoxy-(C1-C6)alkyl; and * indicates a chiral centre; or a pharmaceutically acceptable salt or solvate thereof. These compounds are useful for the treatment of disease conditions caused by overactivation of VR1 receptor such of pain, or the like in mammalian. This invention also provides a pharmaceutical composition comprising the above compound.

5. 发明授权

US07566739B2 Substituted N-sulfonylaminophenylethyl-2-phenoxyacetamide compounds as VR1 receptor antagonists 失效
标题翻译：取代的N-磺酰基氨基苯乙基-2-苯氧基乙酰胺化合物作为VR1受体拮抗剂
公开(公告)号：US07566739B2
公开(公告)日：2009-07-28
申请号：US11372706
申请日：2006-03-10
申请人： Takeshi Hanazawa , Misato Hirano , Tadashi Inoue , Satoshi Nagayama , Kazunari Nakao , Yuji Shishido , Hirotaka Tanaka
发明人： Takeshi Hanazawa , Misato Hirano , Tadashi Inoue , Satoshi Nagayama , Kazunari Nakao , Yuji Shishido , Hirotaka Tanaka
IPC分类号： A61K31/18 , C07C311/09 , C07C311/08
CPC分类号： C07C311/08
摘要： This invention provides compounds of the formula (I) useful for the treatment of disease conditions caused by over activation of Vr1 receptors such as pain or the like in mammals as well as compositions comprising them.
摘要翻译：本发明提供了可用于治疗由过度活化Vr1受体（例如哺乳动物的疼痛等）引起的疾病状况的式（I）化合物以及包含它们的组合物。

6. 发明申请

US20060270682A1 Substituted Aryloxymethyl Bicyclicmethyl Acetamide Compounds 失效
公开(公告)号：US20060270682A1
公开(公告)日：2006-11-30
申请号：US11421242
申请日：2006-05-31
申请人： Tadashi Inoue , Satoshi Nagayama , Yuji Shishido
发明人： Tadashi Inoue , Satoshi Nagayama , Yuji Shishido
IPC分类号： A61K31/501 , A61K31/4439 , A61K31/428 , A61K31/423 , A61K31/4184 , A61K31/4192
CPC分类号： C07D277/62 , C07D209/34 , C07D231/56 , C07D235/06 , C07D235/26 , C07D249/18 , C07D263/58
摘要： This invention provides a compound of the formula (I): wherein A=B=D represents NR10—C(O)—NR9, S—C(O)—NR9, NR9—C(O)—S, NR9—C(O)—O, CR10—C(O)—NR9, O—C(O)—NR9, NR10—C(O)—CR9, NR10—NR9—C(O), C(O)—NR9—NR10, NR10—N═CR9, N═N—CR9, NR10—CR9═N, N═CR9—NR10, NR10—N═N, N═N—NR10, S—CR9═N or N═CR9—S; X1 represents CR1 or N; X2 and X3 each independently represents CR8 or N; R1, R6, R8, R9 and R10 each independently represents hydrogen, halogen, hydroxy, (C1-C6)alkyl, (C1-C6)alkoxy, hydroxy(C1-C6)alkoxy, (C1-C6)alkoxy-(C1-C6)alkyl, (C1-C6)alkoxy-(C1-C6)alkoxy, halo(C1-C6)alkyl, (C1-C6)alkylthio, (C1-C6)alkylsulfinyl or (C1-C6)alkylsulfonyl; R2, R3, R4, and R5 each independently represents hydrogen, (C1-C6)alkyl, halogen, halo(C1-C6)alkyl, or hydroxy(C1-C6)alkyl; and R7 represents halogen, (C1-C6)alkyl, halo(C1-C6)alkyl, (C1-C6)alkoxy, hydroxy(C1-C6)alkoxy, (C1-C6)alkoxy-(C1-C6)alkyl, (C1-C6)alkoxy-(C1-C6)alkoxy, [(C1-C6)alkyl]NH— or [(C1-C6)alkyl]2N—; or a pharmaceutically acceptable salt thereof, provided that: (i) when A=B=D represents NR10—N═N or N═N—NR10, then R2 represents (C1-C6)alkyl, halogen, halo(C1-C6)alkyl or hydroxy(C1-C6)alkyl; or (ii) when A=B=D represents NR10—N═N or N═N—NR10, and R2 represents (C1-C6)alkyl, then R7 represents halogen, (C1-C6)alkyl, (C1-C6)alkoxy, hydroxy(C1-C6)alkoxy, (C1-C6)alkoxy-(C1-C6)alkyl, (C1-C6)alkoxy-(C1-C6)alkoxy, [(C1-C6)alkyl]NH— or [(C1-C6)alkyl]2N—. These compounds are useful for the treatment of disease conditions caused by overactivation of VR1 receptor such of pain, or the like in mammalian. This invention also provides a pharmaceutical composition comprising the above compound.

7. 发明申请

US20060211741A1 Substituted sulfonylaminoarylmethyl cyclopropanecarboxamide as VR1 receptor antagonists 失效
公开(公告)号：US20060211741A1
公开(公告)日：2006-09-21
申请号：US11384127
申请日：2006-03-17
申请人： Takeshi Hanazawa , Misato Hirano , Tadashi Inoue , Satoshi Nagayama , Kazunari Nakao , Yuji Shishido , Hirotaka Tanaka
发明人： Takeshi Hanazawa , Misato Hirano , Tadashi Inoue , Satoshi Nagayama , Kazunari Nakao , Yuji Shishido , Hirotaka Tanaka
IPC分类号： A61K31/4412 , A61K31/18 , C07D213/75
CPC分类号： C07C61/28 , C07C61/40 , C07C311/08 , C07C317/44 , C07C323/62 , C07C2601/02 , C07D213/26 , C07D213/56 , C07D213/74 , C07D213/76
摘要： This invention provides a compound of the formula (I): wherein A and B are independently CR12 or N; D and E are each independently CR9 or N; R1 represents (C1-C6)alkyl; R2 represents hydrogen, halogen, hydroxy, (C1-C6)alkyl, halo(C1-C6)alkyl, hydroxy(C1-C6)alkyl, (C1-C6)alkoxy or (C1-C6)alkoxy-(C1-C6)alkyl; R3, R4, R5, R6, R10 and R11 each independently represent hydrogen, halogen, (C1-C6)alkyl, halo(C1-C6)alkyl, (C1-C6)alkoxy, hydroxy(C1-C6)alkyl or (C1-C6)alkoxy-(C1-C6)alkyl; or R3 and R4 are taken together with the carbon atom to which they are attached to form a 3- to 7-membered carbocyclic ring or heterocyclic ring in which one or two non-adjacent carbon atoms are optionally replaced by an oxygen atom, a sulfur atom or NH; R7 and R9 each independently represent hydrogen, halogen, (C1-C6)alkyl, halo(C1-C6)alkyl, hydroxy(C1-C6)alkyl, (C1-C6)alkoxy, hydroxy(C1-C6)alkoxy, (C1-C6)alkoxy-(C1-C6)alkyl, (C1-C6)alkoxy-(C1-C6)alkoxy, (C1-C6)alkylthio, (C1-C6)alkylsulfinyl, (C1-C6)alkylsulfonyl, NH2, [(C1-C6)alkyl]NH—, [(C1-C6)alkyl]2N—, H2N—(C1-C6)alkoxy, (C1-C6)alkyl-NH—(C1-C6)alkoxy, [(C1-C6)alkyl]2N(C1-C6)alkoxy; H2N—(C1-C6)alkoxy-(C1-C6)alkyl, (C1C6)alkyl-NH—(C1-C6)alkoxy-(C1-C6)alkyl, [(C1-C6)alkyl]2N(C1-C6)alkoxy-(C1-C6)alkyl or 5- or 6-membered heterocyclic ring containing at least one nitrogen atom; R8 represents halogen, (C1-C6)alkyl, halo(C1-C6)alkyl, hydroxy(C1-C6)alkyl, (C1-C6)alkoxy, hydroxy(C1-C6)alkoxy, (C1-C6)alkoxy-(C1-C6)alkyl, (C1-C6)alkoxy-(C1-C6)alkoxy, halo(C1-C6)alkylsulfonyl, halo(C1-C6)alkylsulfinyl, halo(C1-C6)alkoxy, halo(C1-C6)alkylthio, [(C1-C6)alkyl]NH— or [(C1-C6)alkyl]2N—; or R7 and R8, when E is CR9, are taken together with the carbon atoms to which they are attached form a 5-8 membered carbocyclic or heterocyclic ring, in which one or two non-adjacent carbon atoms are optionally replaced by oxygen, sulfur, N or NH groups, wherein the carbocyclic ring or the heterocyclic ring is unsubstituted or substituted with one or more substituents each independently selected from the group consisting of hydroxy, (C1-C6)alkyl, (C1-C6)alkoxy and hydroxy(C1-C6)alkyl; and R12 represents hydrogen, halogen, (C1-C6)alkyl or hydroxy(C1-C6)alkyl; or a pharmaceutically acceptable salt or solvate thereof. These compounds are useful for the treatment of disease conditions caused by overactivation of VR1 receptor such of pain, or the like in mammalian. This invention also provides a pharmaceutical composition comprising the above compound.

8. 发明授权

US08178558B2 Substituted pyridylmethyl bicycliccarboxyamide compounds 失效
标题翻译：取代的吡啶基甲基双环羧酰胺化合物
公开(公告)号：US08178558B2
公开(公告)日：2012-05-15
申请号：US12439888
申请日：2007-09-10
申请人： Satoshi Nagayama , Yuji Shishido , Hirotaka Tanaka
发明人： Satoshi Nagayama , Yuji Shishido , Hirotaka Tanaka
IPC分类号： A61K31/47 , C07D213/56
CPC分类号： C07D213/40 , C07D401/12
摘要： This invention relates to novel substituted pyridylmethyl bicyclocarboxamide compounds and to their use in therapy. These compounds are particularly useful as modulators of the VR1 (Type I Vanilloid) receptor, and are thus useful for the treatment of pain, neuralgia, neuropathies, nerve injury, burns, migraine, carpal tunnel syndrome, fibromyalgia, neuritis, sciatica, pelvic hypersensitivity, bladder disease, inflammation, or the like in mammals, especially humans.
摘要翻译：本发明涉及新型取代的吡啶基甲基双环胺化合物及其在治疗中的用途。这些化合物特别可用作VR1（I型香草素）受体的调节剂，因此可用于治疗疼痛，神经痛，神经病，神经损伤，烧伤，偏头痛，腕管综合征，纤维肌痛，神经炎，坐骨神经痛，盆腔超敏反应，膀胱疾病，炎症等，在哺乳动物，特别是人类中。

9. 发明申请

US20110021514A1 AMIDE DERIVATIVES AS ION-CHANNEL LIGANDS AND PHARMACEUTICAL COMPOSITIONS AND METHODS OF USING THE SAME 失效
标题翻译：作为离子通道配体和药物组合物的酰胺衍生物及其使用方法
公开(公告)号：US20110021514A1
公开(公告)日：2011-01-27
申请号：US12742425
申请日：2008-11-13
申请人： Matthew Cox , Donogh John Roger O'Mahony , Maria De Los Angeles Estiarte-Martinez , Tadashi Kawashima , Satoshi Nagayama , Yuji Shishido , Hirotaka Tanaka , Matthew Alexander James Duncton , Andrew Antony Calabrese
发明人： Matthew Cox , Donogh John Roger O'Mahony , Maria De Los Angeles Estiarte-Martinez , Tadashi Kawashima , Satoshi Nagayama , Yuji Shishido , Hirotaka Tanaka , Matthew Alexander James Duncton , Andrew Antony Calabrese
IPC分类号： A61K31/18 , C07D311/66 , A61K31/352 , C07C311/08 , C07D265/36 , A61K31/538 , C07D215/48 , A61K31/47 , C07D319/20 , A61K31/357 , C07D405/04 , A61K31/4709 , A61P29/00 , A61P37/06 , A61P13/10 , A61P3/00 , A61P9/00 , A61P35/00 , A61P19/00
CPC分类号： C07D215/48 , C07C311/08 , C07C2602/10 , C07D265/36 , C07D311/58 , C07D311/66 , C07D319/20 , C07D405/04
摘要： Compounds are disclosed that have a formula represented by the following: The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, pain, inflammation, traumatic injury, and others.
摘要翻译：公开了具有下列化学式的化合物：化合物可以制备成药物组合物，并且可以用于预防和治疗哺乳动物包括人的多种病症，包括作为非限制性实例的疼痛，炎症，创伤性损伤等。

10. 发明授权

US08153651B2 Amide derivatives as ion-channel ligands and pharmaceutical compositions and methods of using the same 失效
标题翻译：酰胺衍生物作为离子通道配体和药物组合物及其使用方法
公开(公告)号：US08153651B2
公开(公告)日：2012-04-10
申请号：US12742425
申请日：2008-11-13
申请人： Matthew Cox , Donogh John Roger O'Mahony , Maria De Los Angeles Estiarte-Martinez , Tadashi Kawashima , Satoshi Nagayama , Yuji Shishido , Hirotaka Tanaka , Matthew Alexander James Duncton , Andrew Antony Calabrese
发明人： Matthew Cox , Donogh John Roger O'Mahony , Maria De Los Angeles Estiarte-Martinez , Tadashi Kawashima , Satoshi Nagayama , Yuji Shishido , Hirotaka Tanaka , Matthew Alexander James Duncton , Andrew Antony Calabrese
IPC分类号： A01N43/42 , A61K31/44 , C07D471/02
CPC分类号： C07D215/48 , C07C311/08 , C07C2602/10 , C07D265/36 , C07D311/58 , C07D311/66 , C07D319/20 , C07D405/04
摘要： Compounds are disclosed that have a formula represented by the following: The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, pain, inflammation, traumatic injury, and others.
摘要翻译：公开了具有下列化学式的化合物：化合物可以制备成药物组合物，并且可以用于预防和治疗哺乳动物包括人的多种病症，包括作为非限制性实例的疼痛，炎症，创伤性损伤等。

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