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1.Photocleavable and acid cleavable linkers for combinatorial chemistry 失效
Title translation: 用于组合化学的可透光和可酸切割接头公开(公告)号:US06642417B2
公开(公告)日:2003-11-04
申请号:US09766987
申请日:2001-01-22
Applicant: Vinh D. Tran , Vu Van Ma , Ruiyan Liu
Inventor: Vinh D. Tran , Vu Van Ma , Ruiyan Liu
IPC: C07C23304
CPC classification number: C40B80/00 , C07B2200/11 , C07C59/74 , C07C205/37 , C07C205/44 , C07C235/06
Abstract: A substrate for solid phase synthesis comprising a solid phase-linker combination of the formula I is disclosed. Also disclosed are processes for preparing the substrate and chemical intermediates useful therein. Among the novel intermediates are compounds of the formula II wherein R1 is —NO2 or —CHO; R2 is —OCH3, —CHO or —H; R3 is chosen from the group consisting of hydroxyl, the residue of a solid support having a plurality of amino groups, and the residue of an ester, and n=1 or 3-12. A substrate of solid phase synthesis of the formula III is also disclosed.
Abstract translation: 公开了一种用于固相合成的底物,其包含式I的固相 - 连接体组合。 还公开了制备基材和其中有用的化学中间体的方法。 其中新的中间体是式II化合物,其中R 1是-NO 2或-CHO; R 2是-OCH 3,-CHO或-H; R 3选自羟基,具有多个氨基的固体支持物的残基和酯的残基,n = 1或3-12。A的固相合成底物 还公开了式III。
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2.Photocleavable and acid cleavable linkers for combinatorial chemistry 失效
Title translation: 用于组合化学的可透光和可酸切割接头公开(公告)号:US06310244B1
公开(公告)日:2001-10-30
申请号:US09121262
申请日:1998-07-23
Applicant: Vinh D. Tran , Vu Van Ma , Ruiyan Liu
Inventor: Vinh D. Tran , Vu Van Ma , Ruiyan Liu
IPC: C07C23304
CPC classification number: C40B80/00 , C07B2200/11 , C07C59/74 , C07C205/37 , C07C205/44 , C07C235/06
Abstract: A substrate for solid phase synthesis comprising a solid phase-linker combination of the formula I is disclosed. Also disclosed are processes for preparing the substrate and chemical intermediates useful therein. Among the novel intermediates are compounds of the formula II wherein R1 is —NO2 or —CHO; R2 is —OCH3, —CHO or —H; R3 is chosen from the group consisting of hydroxyl, the residue of a solid support having a plurality of amino groups, and the residue of an ester, and n=1 or 3. A substrate of solid phase synthesis of the formula III is also disclosed.
Abstract translation: 公开了一种用于固相合成的底物,其包含式I的固相 - 连接体组合。 还公开了制备基材和其中有用的化学中间体的方法。 其中新型中间体为式II化合物,其中R 1为-NO 2或-CHO; R2是-OCH3,-CHO或-H; R3选自羟基,具有多个氨基的固体支持物的残基和酯的残基,n = 1或3.还公开了式III的固相合成底物 。
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公开(公告)号:US20130157996A1
公开(公告)日:2013-06-20
申请号:US13529860
申请日:2012-06-21
Applicant: Kaustav Biswas , James Brown , Jian J. Chen , Vijay Keshav Gore , Scott Harried , Daniel B. Horne , Matthew R. Kaller , Qingyian Liu , Vu Van Ma , Holger Monenschein , Thomas T. Nguyen , David J. St. Jean, JR. , Chester Chenguang Yuan , Wenge Zhong
Inventor: Kaustav Biswas , James Brown , Jian J. Chen , Vijay Keshav Gore , Scott Harried , Daniel B. Horne , Matthew R. Kaller , Qingyian Liu , Vu Van Ma , Holger Monenschein , Thomas T. Nguyen , David J. St. Jean, JR. , Chester Chenguang Yuan , Wenge Zhong
IPC: C07D498/04 , C07D401/14 , C07D213/81 , C07D487/04 , C07D413/12 , C07D401/12 , C07D471/04
CPC classification number: C07D213/82 , C07D213/40 , C07D213/61 , C07D213/81 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D405/14 , C07D409/12 , C07D413/12 , C07D417/12 , C07D471/04 , C07D487/04 , C07D498/04
Abstract: Compounds of Formula I are useful as antagonists of TRPM8. Such compounds are useful in treating a number of TRPM8 mediated disorders and conditions and may be used to prepare medicaments and pharmaceutical compositions useful for treating such disorders and conditions. Examples of such disorders include, but are not limited to, migraines and neuropathic pain. Compounds of Formula I have the following structure: where the definitions of the variables are provided herein.
Abstract translation: 式I的化合物可用作TRPM8的拮抗剂。 这些化合物可用于治疗多种TRPM8介导的病症和病症,并且可用于制备用于治疗这种病症和病症的药物和药物组合物。 这些疾病的实例包括但不限于偏头痛和神经性疼痛。 式I的化合物具有以下结构:其中本文提供变量的定义。
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4.
公开(公告)号:US08026241B2
公开(公告)日:2011-09-27
申请号:US12367352
申请日:2009-02-06
Applicant: Chenera Balan , Yunxin Bo , Celia Dominguez , Christopher H. Fotsch , Vijay K. Gore , Vu Van Ma , Mark H. Norman , Vassil I. Ognyanov , Yi-xin Qian , Xianghong Wang , Ning Xi , Shimin Xu
Inventor: Chenera Balan , Yunxin Bo , Celia Dominguez , Christopher H. Fotsch , Vijay K. Gore , Vu Van Ma , Mark H. Norman , Vassil I. Ognyanov , Yi-xin Qian , Xianghong Wang , Ning Xi , Shimin Xu
IPC: A61K31/497 , C07D403/04 , C07D401/04
CPC classification number: C07D401/04 , C07D235/30 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D405/14 , C07D409/14 , C07D417/12 , C07D417/14 , C07D471/04
Abstract: Therapeutic benzimidazoles and compositions containing them, for the treatment of acute, inflammatory and neuropathic pain, dental pain, general headache, migraine, cluster headache, mixed-vascular and non-vascular syndromes, tension headache, general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, inflammatory pain and associated hyperalgesia and allodynia, neuropathic pain and associated hyperalgesia and allodynia, diabetic neuropathy pain, causalgia, sympathetically maintained pain, deafferentation syndromes, asthma, epithelial tissue damage or dysfunction, herpes simplex, disturbances of visceral motility at respiratory, genitourinary, gastrointestinal or vascular regions, wounds, burns, allergic skin reactions, pruritus, vitiligo, general gastrointestinal disorders, gastric ulceration, duodenal ulcers, diarrhea, gastric lesions induced by necrotizing agents, hair growth, vasomotor or allergic rhinitis, bronchial disorders or bladder disorders.
Abstract translation: 治疗性苯并咪唑和含有它们的组合物,用于治疗急性,炎性和神经性疼痛,牙痛,一般头痛,偏头痛,丛集性头痛,混合血管和非血管综合征,紧张性头痛,一般炎症,关节炎,风湿性疾病,骨关节炎 ,炎症性肠病,炎症性眼病,炎症性或不稳定性膀胱病,银屑病,皮肤炎症成分炎症,慢性炎性病症,炎性疼痛及相关的痛觉过敏和异常性疼痛,神经性疼痛及相关的痛觉过敏和异常性疼痛,糖尿病性神经病疼痛,灼痛,交感神经痛 维持疼痛,输血综合征,哮喘,上皮组织损伤或功能障碍,单纯疱疹,呼吸道,泌尿生殖道,胃肠道或血管区内脏运动紊乱,伤口,烧伤,过敏性皮肤反应,瘙痒,白癜风,一般胃肠道疾病,胃溃疡 十二指肠溃疡,腹泻,坏死因子诱发的胃损伤,毛发生长,血管舒缩或过敏性鼻炎,支气管疾病或膀胱疾病。
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公开(公告)号:US07514438B2
公开(公告)日:2009-04-07
申请号:US10916011
申请日:2004-08-11
Applicant: Christopher Hulme , Paul A. Tempest , Vu Van Ma , Thomas Nixey , Guity Balow
Inventor: Christopher Hulme , Paul A. Tempest , Vu Van Ma , Thomas Nixey , Guity Balow
IPC: A61K31/496 , C07D257/04 , C07D403/06
CPC classification number: C07D257/04 , C07D401/06 , C07D403/06 , C07D403/10 , C07D403/12 , C07D405/06 , C07D405/12
Abstract: Novel compounds, or pharmaceutically-acceptable salts, tautomers or prodrugs thereof, of Formula I wherein A, W, X, Z, R1-R3, and R8 are as defined in the specification, are provided. Also provided are methods of treating or preventing a melanin concentrating hormone-mediated disorder in a subject, comprising administering to a subject in need of such treatment or prevention a compound of Formula I.
Abstract translation: 其中A,W,X,Z,R 1 -R 3和R 8如说明书中所定义的式I的新化合物或其药学上可接受的盐,互变异构体或前药。 还提供了治疗或预防受试者中黑色素浓缩激素介导的病症的方法,其包括向需要这种治疗或预防的受试者施用式I化合物。
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6.SPIRO-TETRACYCLIC RING COMPOUNDS AS BETA-SECRETASE MODULATORS AND METHODS OF USE 有权
Title translation: 作为β-分泌酶调节剂的螺环四环化合物及其使用方法公开(公告)号:US20110251190A1
公开(公告)日:2011-10-13
申请号:US13047734
申请日:2011-03-14
Applicant: Yuan CHENG , Ryan White , Albert Amegadzie , James Brown , Alan C. Cheng , Erin F. Dimauro , Thomas Dineen , Oleg Epstein , Vijay Keshav Gore , Jason Brooks Human , Ted Judd , Charles Kreiman , Qingyian Liu , Patricia Lopez , Vu Van Ma , Isaac Marx , Ana Minatti , Hanh Nho Nguyen , Nick A. Paras , Vinod F. Patel , Wenyuan Qian , Matthew Weiss , Qiufen Xue , Xiao Mei Zheng , Wenge Zhong
Inventor: Yuan CHENG , Ryan White , Albert Amegadzie , James Brown , Alan C. Cheng , Erin F. Dimauro , Thomas Dineen , Oleg Epstein , Vijay Keshav Gore , Jason Brooks Human , Ted Judd , Charles Kreiman , Qingyian Liu , Patricia Lopez , Vu Van Ma , Isaac Marx , Ana Minatti , Hanh Nho Nguyen , Nick A. Paras , Vinod F. Patel , Wenyuan Qian , Matthew Weiss , Qiufen Xue , Xiao Mei Zheng , Wenge Zhong
IPC: A61K31/538 , A61K31/436 , C07D413/14 , C07D417/14 , A61K31/444 , A61P25/00 , C07D513/10 , A61K31/4545 , C07D498/10 , A61K31/497 , A61P25/28 , A61P25/16 , C07D513/20 , A61K31/506
CPC classification number: C07D491/10 , A61K31/42 , A61K31/422 , A61K31/4439 , A61K31/506 , A61K31/5377 , C07D221/20 , C07D235/02 , C07D263/08 , C07D295/135 , C07D498/10 , C07D498/20 , C07D513/10 , C09B11/28
Abstract: The present invention comprises a new class of compounds useful for the modulation of Beta-secretase enzyme activity and for the treatment of Beta-secretase mediated diseases, including Alzheimer's disease (AD) and other related conditions. In one embodiment, the compounds have a general Formula I wherein A1, A2, A3, A4, A5, A6, R2, R7, X and Y of Formula I are defined herein. The invention also includes use of these compounds in pharmaceutical compositions for treatment, prophylactic or therapeutic, of disorders and conditions related to the activity of beta-secretase protein. Such disorders include, for example, Alzheimer's Disease, cognitive deficits, cognitive impairment, schizophrenia and other central nervous system conditions related to and/or caused by the formation and/or deposition of plaque on the brain. The invention also comprises further embodiments of Formula I, intermediates and processes useful for the preparation of compounds of Formula I.
Abstract translation: 本发明包括可用于调节β-分泌酶酶活性和用于治疗β-分泌酶介导的疾病(包括阿尔茨海默氏病(AD))和其它相关病症的新一类化合物。 在一个实施方案中,化合物具有通式I,其中式I中的A1,A2,A3,A4,A5,A6,R2,R7,X和Y如本文所定义。 本发明还包括在药物组合物中用于治疗,预防或治疗与β-分泌酶蛋白活性相关的病症和病症的用途。 这种病症包括例如阿尔茨海默氏病,认知缺陷,认知障碍,精神分裂症和与脑上形成和/或沉积斑块相关和/或引起的其他中枢神经系统病症。 本发明还包括式I的其它实施方案,可用于制备式I化合物的中间体和方法。
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7.
公开(公告)号:US20100261728A1
公开(公告)日:2010-10-14
申请号:US12746292
申请日:2008-12-04
Applicant: Mark H. Norman , Yunxin Y. Bo , Vijay K. Gore , Daniel Horne , Matthew Kaller , Vu Van Ma , Holger Monenschein , Thomas Nguyen , Nobuko Nishimura , Nuria Tamayo
Inventor: Mark H. Norman , Yunxin Y. Bo , Vijay K. Gore , Daniel Horne , Matthew Kaller , Vu Van Ma , Holger Monenschein , Thomas Nguyen , Nobuko Nishimura , Nuria Tamayo
IPC: A61K31/472 , C07D217/18 , C07D401/12 , A61K31/4725 , A61K31/506 , C07D405/06 , C07D413/06 , C07D417/06 , C07D417/12 , C07D405/12 , A61K31/501 , C07D401/04 , A61P29/00 , A61P1/00 , A61P25/06 , A61P25/24 , A61P19/02 , A61P25/22 , A61P11/06 , A61P17/02 , A61P17/00 , A61P13/10 , A61P1/12
CPC classification number: C07D217/04 , C07D217/06 , C07D217/22 , C07D401/04 , C07D401/06 , C07D401/10 , C07D401/12 , C07D405/06 , C07D405/12 , C07D413/06 , C07D417/06
Abstract: Tetrahydroisoquinoline compounds of formula (I), and compositions containing them, for the treatment of acute, inflammatory and neurophatic pain, dental pain, general headache, migraine, cluster headache, mixed-vascular and non-vascular syndromes, tension headache, general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, inflammatory pain and associated hyperalgesia and allodynia, neurophatic pain and associated hyperalgesia and allodynia, diabetic neuropathy pain, causalgia, sympathetically maintained pain, deafferentation syndromes, asthma, epithelial tissue damage or dysfunction, herpes simplex, disturbances of visceral motility at respiratory, genitourinary, gastrointestinal or vascular regions, wounds, burns, allergic skin reactions, pruritus, vitiligo, general gastrointestinal disorders, gastric ulceration, duodenal ulcers, diarrhea, gastric lesions induced by necrotising agents, hair growth, vasomotor or allergic rhinitis, bronchial disorders or bladder disorders.
Abstract translation: 式(I)的四氢异喹啉化合物和含有它们的组合物,用于治疗急性,炎性和神经性疼痛,牙痛,一般头痛,偏头痛,丛集性头痛,混合血管和非血管综合征,紧张性头痛,一般炎症, 关节炎,风湿性疾病,骨关节炎,炎症性肠病,炎症性眼病,炎性或不稳定性膀胱病,牛皮癣,皮肤炎症成分投诉,慢性炎性病症,炎性疼痛及相关的痛觉过敏和异常性疼痛,神经性疼痛及相关的痛觉过敏和异常性疼痛,糖尿病 神经病痛,咳嗽痛,交感神经保持疼痛,交感综合征,哮喘,上皮组织损伤或功能障碍,单纯疱疹,呼吸道内脏运动性紊乱,泌尿生殖道,胃肠道或血管区,伤口,烧伤,过敏性皮肤反应,瘙痒,白癜风,一般 胃肠道 胃溃疡,十二指肠溃疡,腹泻,坏死因子诱导的胃损伤,毛发生长,血管舒缩或过敏性鼻炎,支气管疾病或膀胱疾病。
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8.
公开(公告)号:US20090143575A1
公开(公告)日:2009-06-04
申请号:US12367352
申请日:2009-02-06
Applicant: Chenera Balan , Yunxin Bo , Celia Dominguez , Christopher H. Fotsch , Vijay K. Gore , Vu Van Ma , Mark H. Norman , Vassil I. Ognyanov , Yi-xin Qian , Xianghong Wang , Ning Xi , Shimin Xu
Inventor: Chenera Balan , Yunxin Bo , Celia Dominguez , Christopher H. Fotsch , Vijay K. Gore , Vu Van Ma , Mark H. Norman , Vassil I. Ognyanov , Yi-xin Qian , Xianghong Wang , Ning Xi , Shimin Xu
IPC: C07D413/14 , C07D471/04 , C07D401/14
CPC classification number: C07D401/04 , C07D235/30 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D405/14 , C07D409/14 , C07D417/12 , C07D417/14 , C07D471/04
Abstract: Therapeutic benzimidazoles and compositions containing them, for the treatment of acute, inflammatory and neuropathic pain, dental pain, general headache, migraine, cluster headache, mixed-vascular and non-vascular syndromes, tension headache, general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, inflammatory pain and associated hyperalgesia and allodynia, neuropathic pain and associated hyperalgesia and allodynia, diabetic neuropathy pain, causalgia, sympathetically maintained pain, deafferentation syndromes, asthma, epithelial tissue damage or dysfunction, herpes simplex, disturbances of visceral motility at respiratory, genitourinary, gastrointestinal or vascular regions, wounds, burns, allergic skin reactions, pruritus, vitiligo, general gastrointestinal disorders, gastric ulceration, duodenal ulcers, diarrhea, gastric lesions induced by necrotizing agents, hair growth, vasomotor or allergic rhinitis, bronchial disorders or bladder disorders.
Abstract translation: 治疗性苯并咪唑和含有它们的组合物,用于治疗急性,炎性和神经性疼痛,牙痛,一般头痛,偏头痛,丛集性头痛,混合血管和非血管综合征,紧张性头痛,一般炎症,关节炎,风湿性疾病,骨关节炎 ,炎症性肠病,炎症性眼病,炎症性或不稳定性膀胱病,银屑病,皮肤炎症成分炎症,慢性炎性病症,炎性疼痛及相关的痛觉过敏和异常性疼痛,神经性疼痛及相关的痛觉过敏和异常性疼痛,糖尿病性神经病疼痛,灼痛,交感神经痛 维持疼痛,输血综合征,哮喘,上皮组织损伤或功能障碍,单纯疱疹,呼吸道,泌尿生殖道,胃肠道或血管区内脏运动紊乱,伤口,烧伤,过敏性皮肤反应,瘙痒,白癜风,一般胃肠道疾病,胃溃疡 十二指肠溃疡,腹泻,坏死因子诱发的胃损伤,毛发生长,血管舒缩或过敏性鼻炎,支气管疾病或膀胱疾病。
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公开(公告)号:US08710043B2
公开(公告)日:2014-04-29
申请号:US13529860
申请日:2012-06-21
Applicant: Jian J. Chen , Daniel B. Horne , Matthew R. Kaller , Vu Van Ma
Inventor: Jian J. Chen , Daniel B. Horne , Matthew R. Kaller , Vu Van Ma
IPC: C07D498/04 , C07D401/12 , C07D471/04 , C07D213/81
CPC classification number: C07D213/82 , C07D213/40 , C07D213/61 , C07D213/81 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D405/14 , C07D409/12 , C07D413/12 , C07D417/12 , C07D471/04 , C07D487/04 , C07D498/04
Abstract: Compounds of Formula I are useful as antagonists of TRPM8. Such compounds are useful in treating a number of TRPM8 mediated disorders and conditions and may be used to prepare medicaments and pharmaceutical compositions useful for treating such disorders and conditions. Examples of such disorders include, but are not limited to, migraines and neuropathic pain. Compounds of Formula I have the following structure: where the definitions of the variables are provided herein.
Abstract translation: 式I的化合物可用作TRPM8的拮抗剂。 这些化合物可用于治疗多种TRPM8介导的病症和病症,并且可用于制备用于治疗这种病症和病症的药物和药物组合物。 这些疾病的实例包括但不限于偏头痛和神经性疼痛。 式I的化合物具有以下结构:其中本文提供变量的定义。
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10.
公开(公告)号:US08476297B2
公开(公告)日:2013-07-02
申请号:US12746292
申请日:2008-12-04
Applicant: Mark H. Norman , Yunxin Y. Bo , Vijay K. Gore , Daniel Horne , Matthew Kaller , Vu Van Ma , Holger Monenschein , Thomas Nguyen , Nobuko Nishimura , Nuria Tamayo
Inventor: Mark H. Norman , Yunxin Y. Bo , Vijay K. Gore , Daniel Horne , Matthew Kaller , Vu Van Ma , Holger Monenschein , Thomas Nguyen , Nobuko Nishimura , Nuria Tamayo
IPC: C07D217/04 , A61K31/47
CPC classification number: C07D217/04 , C07D217/06 , C07D217/22 , C07D401/04 , C07D401/06 , C07D401/10 , C07D401/12 , C07D405/06 , C07D405/12 , C07D413/06 , C07D417/06
Abstract: Tetrahydroisoquinoline compounds of formula (I), and compositions containing them, for the treatment of acute, inflammatory and neurophatic pain, dental pain, general headache, migraine, cluster headache, mixed-vascular and non-vascular syndromes, tension headache, general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, inflammatory pain and associated hyperalgesia and allodynia, neurophatic pain and associated hyperalgesia and allodynia, diabetic neuropathy pain, causalgia, sympathetically maintained pain, deafferentation syndromes, asthma, epithelial tissue damage or dysfunction, herpes simplex, disturbances of visceral motility at respiratory, genitourinary, gastrointestinal or vascular regions, wounds, burns, allergic skin reactions, pruritus, vitiligo, general gastrointestinal disorders, gastric ulceration, duodenal ulcers, diarrhea, gastric lesions induced by necrotising agents, hair growth, vasomotor or allergic rhinitis, bronchial disorders or bladder disorders.
Abstract translation: 式(I)的四氢异喹啉化合物和含有它们的组合物,用于治疗急性,炎性和神经性疼痛,牙痛,一般头痛,偏头痛,丛集性头痛,混合血管和非血管综合征,紧张性头痛,一般炎症, 关节炎,风湿性疾病,骨关节炎,炎症性肠病,炎症性眼病,炎性或不稳定性膀胱病,牛皮癣,皮肤炎症成分投诉,慢性炎性病症,炎性疼痛及相关的痛觉过敏和异常性疼痛,神经性疼痛及相关的痛觉过敏和异常性疼痛,糖尿病 神经病痛,咳嗽痛,交感神经保持疼痛,交感综合征,哮喘,上皮组织损伤或功能障碍,单纯疱疹,呼吸道内脏运动紊乱,泌尿生殖道,胃肠道或血管区,伤口,烧伤,过敏性皮肤反应,瘙痒,白癜风,一般 胃肠道 胃溃疡,十二指肠溃疡,腹泻,坏死因子诱导的胃损伤,毛发生长,血管舒缩或过敏性鼻炎,支气管疾病或膀胱疾病。
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