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1. 发明申请

US20050209221A1 Substituted heterocyclic compounds and methods of use 失效
标题翻译：取代的杂环化合物及其使用方法
公开(公告)号：US20050209221A1
公开(公告)日：2005-09-22
申请号：US10875896
申请日：2004-06-23
申请人： Joseph Nunes , Xiaotian Zhu , Patricia Amouzegh , Chiara Ghiron , David Johnston , Eoin Power
发明人： Joseph Nunes , Xiaotian Zhu , Patricia Amouzegh , Chiara Ghiron , David Johnston , Eoin Power
IPC分类号： C07D213/82 , C07D239/46 , C07D239/48 , C07D417/02 , A61K31/4439 , A61K31/496 , A61K31/513 , A61K31/5377 , A61K31/541 , C07D413/02 , C07D43/02
CPC分类号： C07D213/82 , C07D239/47 , C07D239/48
摘要： The present invention relates to pyrimidine or pyridine carboxamides or pharmaceutically-acceptable salts thereof. Also included is a method of treatment of inflammation, inhibition of T cell activation and proliferation, arthritis, rheumatoid arthritis, psoriatic arthritis, osteoarthritis, organ transplant, acute transplant or heterograft or homograft rejection, transplantation tolerance induction, ischemic or reperfusion injury, myocardial infarction, stroke, multiple sclerosis, inflammatory bowel disease, including ulcerative colitis, Crohn's disease, lupus, contact hypersensitivity, delayed-type hypersensitivity, and gluten-sensitive enteropathy, type 1 diabetes, psoriasis, contact dermatitis, Hashimoto's thyroiditis, Sjogren's syndrome, autoimmune hyperthyroidism, Addison's disease, autoimmune polyglandular disease, autoimmune alopecia, pernicious anemia, vitiligo, autoimmune hypopituatarism, Guillain-Barre syndrome, glomerulonephritis, serum sickness, uticaria, allergic diseases, asthma, hayfever, allergic rhinitis, scleracielma, mycosis fungoides, dermatomyositis, alopecia areata, chronic actinic dermatitis, eczema, Behcet's disease, Pustulosis palmoplanteris, Pyoderma gangrenum, Sezary's syndrome, atopic dermatitis, systemic schlerosis, morphea, atopic dermatitis, colon carcinoma or thymoma in a mammal comprising administering a therapeutically-effective amount a compound as described above.
摘要翻译：本发明涉及嘧啶或吡啶甲酰胺或其药学上可接受的盐。还包括治疗炎症，抑制T细胞活化和增殖，关节炎，类风湿性关节炎，银屑病关节炎，骨关节炎，器官移植，急性移植或异种移植或同种移植物排斥，移植耐受性诱导，缺血或再灌注损伤，心肌梗死的方法，中风，多发性硬化，炎症性肠病，包括溃疡性结肠炎，克罗恩病，狼疮，接触性超敏反应，迟发型超敏反应和麸质敏感性肠病，1型糖尿病，牛皮癣，接触性皮炎，桥本氏甲状腺炎，干燥综合征，自身免疫性甲状腺功能亢进，艾迪生病，自身免疫性多腺病，自身免疫性脱发，恶性贫血，白癜风，自身免疫性低位症，吉兰巴利综合征，肾小球性肾炎，血清病，荨麻疹，过敏性疾病，哮喘，高粱，过敏性鼻炎，巩膜瘤，蕈样真菌病，皮肌炎，斑秃，慢性交感包括给予治疗有效量的如上所述的化合物，包括给予治疗有效量的上述化合物，其中，所述治疗有效量的治疗有效量的药物组合物包括给予治疗有效量的上述化合物。

2. 发明申请

US20050070554A1 Substituted heterocyclic compounds and methods of use 审中-公开
标题翻译：取代的杂环化合物及其使用方法
公开(公告)号：US20050070554A1
公开(公告)日：2005-03-31
申请号：US10923523
申请日：2004-08-20
申请人： Joseph Nunes , Xiaotian Zhu , Monika Ermann , Chiara Ghiron , David Johnston , Carl-Gustaf Saluste
发明人： Joseph Nunes , Xiaotian Zhu , Monika Ermann , Chiara Ghiron , David Johnston , Carl-Gustaf Saluste
IPC分类号： C07D487/14 , A61K31/519 , A61K31/5377 , A61K31/541
CPC分类号： C07D487/14
摘要： The present invention relates to tetracyclic pyrimidines or pyridines or pharmaceutically-acceptable salts or derivatives thereof. Also included are methods of use of the tetracyclic pyrimidines or pyridines including use related to treating inflammation, inhibiting T cell activation and proliferation, arthritis, organ transplant, ischemic or reperfusion injury, myocardial infarction, stroke, multiple sclerosis, inflammatory bowel disease and many other related disorders in a subject, the methods comprising administering a therapeutically-effective amount a compound as described above to the subject.
摘要翻译：本发明涉及四环嘧啶或吡啶或其药学上可接受的盐或衍生物。还包括使用四环嘧啶或吡啶的方法，包括与治疗炎症有关的用途，抑制T细胞活化和增殖，关节炎，器官移植，缺血或再灌注损伤，心肌梗死，中风，多发性硬化，炎症性肠病等多种方法所述方法包括向受试者施用治疗有效量的如上所述的化合物。

3. 发明授权

US07504396B2 Substituted heterocyclic compounds and methods of use 失效
标题翻译：取代的杂环化合物及其使用方法
公开(公告)号：US07504396B2
公开(公告)日：2009-03-17
申请号：US10875896
申请日：2004-06-23
申请人： Joseph J. Nunes , Xiaotian Zhu , Patricia Amouzegh , Chiara Ghiron , David N. Johnson , Eoin Christopher Power
发明人： Joseph J. Nunes , Xiaotian Zhu , Patricia Amouzegh , Chiara Ghiron , David N. Johnson , Eoin Christopher Power
IPC分类号： C07D239/48 , C07D403/12 , A61K31/505
CPC分类号： C07D213/82 , C07D239/47 , C07D239/48
摘要： The present invention relates to pyrimidine or pyridine carboxamides or pharmaceutically-acceptable salts thereof. Also included is a method of treatment of inflammation, inhibition of T cell activation and proliferation, arthritis, rheumatoid arthritis, psoriatic arthritis, osteoarthritis, organ transplant, acute transplant or heterograft or homograft rejection, transplantation tolerance induction, ischemic or reperfusion injury, myocardial infarction, stroke, multiple sclerosis, inflammatory bowel disease, including ulcerative colitis, Crohn's disease, lupus, contact hypersensitivity, delayed-type hypersensitivity, and gluten-sensitive enteropathy, type 1 diabetes, psoriasis, contact dermatitis, Hashimoto's thyroiditis, Sjogren's syndrome, autoimmune hyperthyroidism, Addison's disease, autoimmune polyglandular disease, autoimmune alopecia, pernicious anemia, vitiligo, autoimmune hypopituatarism, Guillain-Barre syndrome, glomerulonephritis, serum sickness, uticaria, allergic diseases, asthma, hayfever, allergic rhinitis, scleracielma, mycosis fungoides, dermatomyositis, alopecia areata, chronic actinic dermatitis, eczema, Behcet's disease, Pustulosis palmoplanteris, Pyoderma gangrenum, Sezary's syndrome, atopic dermatitis, systemic schlerosis, morphea, atopic dermatitis, colon carcinoma or thymoma in a mammal comprising administering a therapeutically-effective amount a compound as described above.
摘要翻译：本发明涉及嘧啶或吡啶甲酰胺或其药学上可接受的盐。还包括治疗炎症，抑制T细胞活化和增殖，关节炎，类风湿性关节炎，银屑病关节炎，骨关节炎，器官移植，急性移植或异种移植或同种移植物排斥，移植耐受性诱导，缺血或再灌注损伤，心肌梗死的方法，中风，多发性硬化，炎症性肠病，包括溃疡性结肠炎，克罗恩病，狼疮，接触性超敏反应，迟发型超敏反应和麸质敏感性肠病，1型糖尿病，牛皮癣，接触性皮炎，桥本氏甲状腺炎，干燥综合征，自身免疫性甲状腺功能亢进，艾迪生病，自身免疫性多腺病，自身免疫性脱发，恶性贫血，白癜风，自身免疫性低位症，吉兰巴利综合征，肾小球性肾炎，血清病，荨麻疹，过敏性疾病，哮喘，高粱，过敏性鼻炎，巩膜瘤，蕈样真菌病，皮肌炎，斑秃，慢性交感包括给予治疗有效量的如上所述的化合物，包括给予治疗有效量的上述化合物，其中，所述治疗有效量的治疗有效量的药物组合物包括给予治疗有效量的上述化合物。

4. 发明申请

US20080275028A1 Modulators or Alpha7 Nicotinic Acetylcholine Receptors and Therapeutic Uses Thereof 审中-公开
标题翻译：调节剂或α7烟碱乙酰胆碱受体及其治疗用途
公开(公告)号：US20080275028A1
公开(公告)日：2008-11-06
申请号：US11632545
申请日：2005-07-19
申请人： Giovanni Gaviraghi , Chiara Ghiron , Hendrik Bothmann , Renza Roncarati , Georg Christian Terstappenn
发明人： Giovanni Gaviraghi , Chiara Ghiron , Hendrik Bothmann , Renza Roncarati , Georg Christian Terstappenn
IPC分类号： A61K31/445 , C07D401/12 , C07D211/12 , C07D295/15 , C07D243/08 , C07D211/60 , C07D409/12 , C07D207/09 , A61P29/00 , A61P25/28 , A61P37/00 , A61P25/00 , A61K31/5375 , A61K31/55 , A61K31/551 , A61K31/496 , A61K31/495 , A61K31/4545
CPC分类号： C07D213/40 , C07D209/08 , C07D209/18 , C07D211/52 , C07D211/60 , C07D213/56 , C07D213/82 , C07D215/38 , C07D217/04 , C07D239/26 , C07D243/08 , C07D295/13 , C07D295/15 , C07D295/185 , C07D319/18 , C07D333/20 , C07D401/04 , C07D401/12 , C07D401/14 , C07D409/12
摘要： The present invention relates to compounds with α7 nAChR agonistic activity, processes for their preparation, pharmaceutical compositions containing the same and the use thereof for the treatment of neurological, psychiatric, cognitive, immunological and inflammatory disorders.
摘要翻译：本发明涉及具有α7nAChR激动活性的化合物，其制备方法，含有它们的药物组合物及其用于治疗神经，精神，认知，免疫学和炎症性疾病的用途。

5. 发明申请

US20080221101A1 Calcium receptor modulating agents 有权
标题翻译：钙受体调节剂
公开(公告)号：US20080221101A1
公开(公告)日：2008-09-11
申请号：US11977777
申请日：2007-10-25
申请人： Thomas S. Coulter , Adam James Davenport , Christopher H. Fotsch , Chiara Ghiron , Paul E. Harrington , Michael Gerard Kelly , Steve Fong Poon , Andrew Tasker , Ning Xi , Qing Ping Zeng
发明人： Thomas S. Coulter , Adam James Davenport , Christopher H. Fotsch , Chiara Ghiron , Paul E. Harrington , Michael Gerard Kelly , Steve Fong Poon , Andrew Tasker , Ning Xi , Qing Ping Zeng
IPC分类号： A61K31/5377 , C07C211/29 , A61K31/137 , A61P13/12 , A61P9/00 , C07D401/04
CPC分类号： C07D261/18 , C07C211/29 , C07C217/58 , C07C233/43 , C07C233/44 , C07C233/80 , C07C271/28 , C07C311/37 , C07C317/32 , C07C323/32 , C07C2601/08 , C07C2601/16 , C07D207/06 , C07D207/09 , C07D207/48 , C07D211/22 , C07D211/62 , C07D213/30 , C07D213/38 , C07D213/81 , C07D213/82 , C07D231/14 , C07D233/60 , C07D235/06 , C07D237/14 , C07D239/42 , C07D249/08 , C07D261/08 , C07D263/24 , C07D263/34 , C07D271/06 , C07D285/06 , C07D295/088 , C07D295/185 , C07D295/205 , C07D295/26 , C07D307/68 , C07D317/58 , C07D333/38 , C07D333/40 , C07D409/04 , C07D413/12 , C07D417/04
摘要： The present invention relates generally to compounds represented in Formula I, pharmaceutical compositions comprising them and methods of treating of diseases or disorders related to the function of the calcium sensing receptor. The invention also relates to processes for making such compounds and to intermediates useful in these processes.
摘要翻译：本发明一般涉及式I所示的化合物，包含它们的药物组合物以及治疗与钙敏感受体的功能有关的疾病或病症的方法。本发明还涉及制备这些化合物和在这些方法中有用的中间体的方法。

6. 发明申请

US20100016360A1 ALPHA7 NICOTINIC ACETYLCHOLINE RECEPTOR INHIBITORS 审中-公开
标题翻译： ALPHA7 NICOTINIC乙酰胆碱受体抑制剂
公开(公告)号：US20100016360A1
公开(公告)日：2010-01-21
申请号：US12504547
申请日：2009-07-16
申请人： Simon N. Haydar , Chiara Ghiron , Michela Valacchi , Ugo Zanelli
发明人： Simon N. Haydar , Chiara Ghiron , Michela Valacchi , Ugo Zanelli
IPC分类号： A61K31/4545 , C07D401/12 , A61P25/18 , A61P25/28
CPC分类号： C07D231/12 , C07D213/75 , C07D401/04 , C07D401/12 , C07D405/04 , C07D409/04
摘要： The present invention provides compounds and compositions, methods of making them, and methods of using them to modulate α7 nicotinic acetylcholine receptors and/or to treat any of a variety of disorders, diseases, and conditions. Provided compounds can affect, among other things, neurological, psychiatric and/or inflammatory system.
摘要翻译：本发明提供化合物和组合物，制备它们的方法，以及使用它们调节α7烟碱乙酰胆碱受体和/或治疗多种疾病，疾病和病症中的任何一种的方法。提供的化合物可以影响神经系统，精神和/或炎症系统。

7. 发明申请

US20100016288A1 MODULATORS OF ALPHA7 NICOTINIC ACETYLCHOLINE RECEPTORS AND THERAPEUTIC USES THEREOF 审中-公开
标题翻译： ALPHA7非线性乙酰胆碱受体的调节剂及其治疗用途
公开(公告)号：US20100016288A1
公开(公告)日：2010-01-21
申请号：US12173376
申请日：2008-07-15
申请人： Hendrick BOTHMANN , Renza Roncarati , Jolanda Micco , Arianna Nencini , Chiara Ghiron
发明人： Hendrick BOTHMANN , Renza Roncarati , Jolanda Micco , Arianna Nencini , Chiara Ghiron
IPC分类号： A61K31/55 , A61K31/4465 , A61P25/18 , A61P25/28
CPC分类号： A61K31/4465 , A61K31/55
摘要： Compounds with α7 nicotinic acetylcholine receptor (α7 nAChR) agonistic activity, processes for their preparation, pharmaceutical compositions containing the same and the use thereof for the treatment of neurological and psychiatric diseases.
摘要翻译：具有α7烟碱乙酰胆碱受体（α7nAChR）激动活性的化合物，其制备方法，含有它们的药物组合物及其用于治疗神经和精神疾病的用途。

8. 发明授权

US07291612B2 Immunomodulatory compounds 有权
标题翻译：免疫调节化合物
公开(公告)号：US07291612B2
公开(公告)日：2007-11-06
申请号：US11442548
申请日：2006-05-30
申请人： Ian Richard Matthews , Thomas Stephen Coutler , Chiara Ghiron , Chris James Brennan , Muhammed Kamal Uddin , Lars Olof Goran Pettersson , Dorthe da Graca Thrige , Philip Huxley
发明人： Ian Richard Matthews , Thomas Stephen Coutler , Chiara Ghiron , Chris James Brennan , Muhammed Kamal Uddin , Lars Olof Goran Pettersson , Dorthe da Graca Thrige , Philip Huxley
IPC分类号： C07D471/06 , C07D495/06 , A61K31/437 , A61K31/4162 , A61P37/02
CPC分类号： C07D519/00 , C07D471/04 , C07D491/04 , C07D495/04
摘要： The present invention relates to novel heterocyclic compounds, to methods for their preparation, to compositions containing them, and to methods and use for clinical treatment of medical conditions which may benefit from immunomodulation, including rheumatoid arthritis, multiple sclerosis, diabetes, asthma, transplantation, systemic lupus erythematosis and psoriasis. More particularly the present invention relates to novel heterocyclic compounds, which are CD80 antagonists capable of inhibiting the interactions between CD80 and CD28.
摘要翻译：本发明涉及新的杂环化合物，其制备方法，含有它们的组合物，以及用于临床治疗可能受益于免疫调节的医学病症的方法和用途，所述免疫调节包括类风湿性关节炎，多发性硬化，糖尿病，哮喘，移植，系统性红斑狼疮和牛皮癣。更具体地说，本发明涉及能够抑制CD80和CD28之间相互作用的CD80拮抗剂的新型杂环化合物。

9. 发明授权

US07176322B2 Calcium receptor modulating agents 有权
标题翻译：钙受体调节剂
公开(公告)号：US07176322B2
公开(公告)日：2007-02-13
申请号：US10444945
申请日：2003-05-22
申请人： Michael G. Kelly , Shimin Xu , Ning Xi , Robert Townsend , David Semin , Chiara Ghiron , Thomas Coulter
发明人： Michael G. Kelly , Shimin Xu , Ning Xi , Robert Townsend , David Semin , Chiara Ghiron , Thomas Coulter
IPC分类号： C07D209/82 , C07D209/14 , C07D209/04 , A61K31/403 , A61K31/404 , A61K31/4045
CPC分类号： C07D235/06 , C07D209/08 , C07D209/10 , C07D209/12 , C07D209/86 , C07D209/88 , C07D249/04 , C07D401/04 , C07D403/04 , C07D413/04 , C07D471/04 , C07D491/04
摘要： The compounds of the invention are represented by the following general structure or a pharmaceutically acceptable salt thereof, and compositions containing them, wherein the variables are defined herein, and their use to reduce or inhibit PTH secretion, including methods for reducing or inhibiting PTH secretion and methods for treatment or prophylaxis of diseases associated with bone disorders, such as osteoporosis, or associated with excessive secretion of PTH, such as hyperparathyroidism. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.
摘要翻译：本发明的化合物由以下一般结构或其药学上可接受的盐以及含有它们的组合物表示，其中变量在本文中定义，及其用于减少或抑制PTH分泌的用途，包括减少或抑制PTH分泌的方法，以及用于治疗或预防与骨疾病相关的疾病如骨质疏松症或与过度分泌的PTH相关的疾病如甲状旁腺功能亢进的方法。本发明还涉及制备这些化合物的方法以及在这些方法中有用的中间体。

10. 发明授权

US07081456B2 Immunomodulatory compounds 有权
标题翻译：免疫调节化合物
公开(公告)号：US07081456B2
公开(公告)日：2006-07-25
申请号：US10717519
申请日：2003-11-21
申请人： Ian Richard Matthews , Thomas Stephen Coulter , Chiara Ghiron , Chris James Brennan , Muhammed Kamal Uddin , Lars Olof Göran Pettersson , Dorthe da Graca Thrige , Philip Huxley
发明人： Ian Richard Matthews , Thomas Stephen Coulter , Chiara Ghiron , Chris James Brennan , Muhammed Kamal Uddin , Lars Olof Göran Pettersson , Dorthe da Graca Thrige , Philip Huxley
IPC分类号： C07D471/06 , C07D495/06 , A61K31/437 , A61K31/4162 , A61P37/02
CPC分类号： C07D519/00 , C07D471/04 , C07D491/04 , C07D495/04
摘要： The present invention relates to novel heterocyclic compounds, to methods for their preparation, to compositions containing them, and to methods and use for clinical treatment of medical conditions which may benefit from immunomodulation, including rheumatoid arthritis, multiple sclerosis, diabetes, asthma, transplantation, systemic lupus erythematosis and psoriasis. More particularly the present invention relates to novel heterocyclic compounds, which are CD80 antagonists capable of inhibiting the interactions between CD80 and CD28.
摘要翻译：本发明涉及新的杂环化合物，其制备方法，含有它们的组合物，以及用于临床治疗可能受益于免疫调节的医学病症的方法和用途，所述免疫调节包括类风湿性关节炎，多发性硬化，糖尿病，哮喘，移植，系统性红斑狼疮和牛皮癣。更具体地说，本发明涉及能够抑制CD80和CD28之间相互作用的CD80拮抗剂的新型杂环化合物。

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