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51. 发明授权

US5252732A D-heteroaryl, O-alkylheteroaryl, O-alkenylheteroaryl and O-alkynylheteroarylmacrolides having immunosuppressive activity 失效
标题翻译：具有免疫抑制活性的D-杂芳基，O-烷基杂芳基，O-烯基杂芳基和O-炔基杂芳基大环内酯
公开(公告)号：US5252732A
公开(公告)日：1993-10-12
申请号：US921851
申请日：1992-08-05
申请人： Peter J. Sinclair , Joung Goulet , Frederick Wong , Mark Goulet , William H. Parsons , Matthew J. Wyvratt
发明人： Peter J. Sinclair , Joung Goulet , Frederick Wong , Mark Goulet , William H. Parsons , Matthew J. Wyvratt
IPC分类号： A61K31/40 , A61K31/445 , A61K31/495 , A61K31/70 , A61P37/06 , C07D498/18 , C07H19/01 , A61K31/395 , C07D491/16
CPC分类号： C07H19/01
摘要： O-Heteroaryl, O-alkylheteroaryl, O-alkenylheteroaryl and O-alkynylheteroarylmacrolides of the general structural Formula I: ##STR1## have been prepared from suitable precursors by alkylation and/or arylation at C-3" and/or C-4" of the cyclohexyl ring. These macrolide immunosuppressants are useful in a mammalian host for the treatment of autoimmune diseases, infectious diseases, the prevention of rejection of foreign organ transplants and/or related afflictions, diseases and illnesses.

52. 发明授权

US5250678A O-aryl, O-alkyl, O-alkenyl and O-alkynylmacrolides having immunosuppressive activity 失效
标题翻译：具有免疫抑制活性的O-芳基，O-烷基，O-烯基和O-炔基大环内酯
公开(公告)号：US5250678A
公开(公告)日：1993-10-05
申请号：US875036
申请日：1992-05-01
申请人： Mark Goulet , Frederick Wong , Peter J. Sinclair , Matthew J. Wyvratt
发明人： Mark Goulet , Frederick Wong , Peter J. Sinclair , Matthew J. Wyvratt
IPC分类号： A61K31/41 , A61K31/40 , A61K31/445 , A61P17/00 , A61P29/00 , A61P31/12 , A61P37/06 , C07D498/18 , C07D491/16 , A61K31/435
CPC分类号： C07D498/18
摘要： O-Aryl, O-alkyl, O-alkenyl and O-alkynyl-macrolides of the general structural Formula I: ##STR1## have been prepared from suitable precursors by alkylation and/or arylation at C-3" and/or C-4" of the cyclohexyl ring. These macrolide immunosuppressants are useful in a mammalian host for the treatment of autoimmune diseases, infectious diseases and/or the prevention of rejection of foreign organ transplants. In addition, these macrolide immunosuppressants are useful in the topical treatment of inflammatory and hyperproliferative skin diseases and cutaneous manifestations of immunologically-mediated illnesses. Also, these macrolides are useful in the treatment of reversible obstructive airways disease, particularly asthma; as hair revitalizing agents, especially in the treatment of male pattern alopecia or alopecia senilis; in the reversal of multidrug resistance of tumor cells; in treatment of inflammation of mucosa and blood vessels, gastric ulcers, vascular damage, ischemic bowel disease, necrotizing enterocolitis, intestinal lesions associated with thermal burns; in the treatment of cytomegalovirus infection; and in the treatment of idiopathic thrombocytopenic purpura and Basedow's disease.

53. 发明授权

US5143918A Halomacrolides and derivatives having immunosuppressive activity 失效
标题翻译：具有免疫抑制活性的灭麦芽糖和衍生物
公开(公告)号：US5143918A
公开(公告)日：1992-09-01
申请号：US759747
申请日：1991-09-12
申请人： Richard J. Bochis , Matthew J. Wyvratt, Jr.
发明人： Richard J. Bochis , Matthew J. Wyvratt, Jr.
IPC分类号： C07H19/01
CPC分类号： C07H19/01
摘要： Novel C-3" and C-4" halogen-substituted macrolides of FK-506 type structural Formula I: ##STR1## are described. These macrolide immunosuppressants are useful in a mammalian host for the treatment of autoimmune diseases (such as juvenile-onset diabetes melitus, multiple sclerosis and rheumatoid arthritis), infectious diseases and/or the prevention of rejection of foreign organ transplants, e.g. bone marrow and heart transplants. In addition, these macrolide immunosuppressants are useful in the topical treatment of inflammatory and hyperproliferative skin diseases and cutaneous manifestations of immunologically-mediated illnesses such as: psoriasis, atopical dermatitiis, contact dermatitis and further eczematous dermatitises, seborrhoeic dermatitis, Lichen planus, Pemphigus, bullous Pemphigoid, Epidermolysis bullosa, urticaria, angioedemas, vasulitides erythemas, cutaneous eosinophilias, Lupus erythematosus or Alopecia areata.
摘要翻译：描述了FK-506型结构式I的新型C-3“和C-4”卤素取代的大环内酯类。这些大环内酯类免疫抑制剂可用于哺乳动物宿主中用于治疗自身免疫性疾病（如幼年型糖尿病，多发性硬化和类风湿性关节炎），感染性疾病和/或预防外来器官移植排斥反应。骨髓和心脏移植。此外，这些大环内酯类免疫抑制剂可用于局部治疗炎性和过度增生性皮肤病以及免疫介导疾病的皮肤表现，如牛皮癣，特应性皮肤病，接触性皮炎和进一步湿疹性皮肤病，脂溢性皮炎，扁平苔藓，天疱疮，大疱类天疱疮，大疱性表皮松解症，荨麻疹，血管紧张素，血管舒张红斑，皮肤嗜酸粒细胞，红斑狼疮或斑秃。

54. 发明授权

US5064835A Hydroxymacrolide derivatives having immunosuppressive activity 失效
标题翻译：具有免疫抑制活性的羟肟酸衍生物
公开(公告)号：US5064835A
公开(公告)日：1991-11-12
申请号：US486700
申请日：1990-03-01
申请人： Richard J. Bochis , Huyn O. Ok , Matthew J. Wyvratt
发明人： Richard J. Bochis , Huyn O. Ok , Matthew J. Wyvratt
IPC分类号： A61K31/40 , A61K31/445 , A61P17/00 , A61P37/06 , C07D498/18 , C07H19/01
CPC分类号： C07H19/01
摘要： Novel hydroxymacrolide derivatives of the general structural Formula I: ##STR1## have been prepared from (a) suitable precursor(s) by selective reduction of the ketone at C-2. These macrolide immunosuppressants are useful in a human host for the treatment of autoimmune diseases (such as juvenile-onset diabetes melitus, multiple sclerosis and rheumatoid arthritis), infectious diseases and/or the prevention of rejection of foreign organ transplants, e.g. bone marrow and heart transplants. In addition, these macrolide immunosuppressants are useful in the topical treatment of inflammatory and hyperproliferative skin diseases and cutaneous manifestations of immunologically-mediated illnesses such as: psoriasis, atopical dermatitiis, contact dermatitis and further eczematous dermatitises, seborrhoeic dermatitis, Lichen planus, Pemphigus, bullous Pemphigoid, Epidermolysis bullosa, urticaria, angioedemas, vasculitides, erythemas, cutaneous eospinphilias, Lupus erythematosus or Alopecia areata.

55. 发明授权

US5057608A Immunoregulants, immunosuppressants, process to make ring expanded macrolide related to FK-506/FK-520 失效
标题翻译：免疫调节剂，免疫抑制剂，制备与FK-506 / FK-520相关的环扩展大环内酯的方法
公开(公告)号：US5057608A
公开(公告)日：1991-10-15
申请号：US508519
申请日：1990-04-10
申请人： Matthew J. Wyvratt, Jr. , Thomas R. Beattie , Hyun O. Ok , Byron H. Arison , Michael H. Fisher
发明人： Matthew J. Wyvratt, Jr. , Thomas R. Beattie , Hyun O. Ok , Byron H. Arison , Michael H. Fisher
IPC分类号： C07D498/18 , C07H19/01
CPC分类号： C07D498/18 , C07H19/01
摘要： Ring-expanded, immunosuppressive macrolides, are produced by heating and rearranging FK-506 and related compounds.
摘要翻译：通过加热和重排FK-506和相关化合物产生环扩展的免疫抑制性大环内酯类。

56. 发明申请

US20090298949A1 AMINOALKYLPHENOLS, METHODS OF USING AND MAKING THE SAME 有权
标题翻译：氨基醇，其使用方法和制备方法
公开(公告)号：US20090298949A1
公开(公告)日：2009-12-03
申请号：US12540445
申请日：2009-08-13
申请人： Conrad P. Dorn , Mary Ann Powles , Thomas F. Walsh , Matthew J. Wyvratt
发明人： Conrad P. Dorn , Mary Ann Powles , Thomas F. Walsh , Matthew J. Wyvratt
IPC分类号： A61K31/138
CPC分类号： C07C233/18 , C07C215/50 , C07C215/52 , C07C217/58 , C07C229/14 , C07C2601/02 , C07C2601/14 , C07C2602/08 , C07C2602/10 , C07C2602/28 , C07D213/38 , C07D241/12 , C07D249/12 , C07D295/096 , C07D307/52 , C07D309/04 , C07D309/14 , C07D319/12 , C07D333/48
摘要： The present invention relates to Mannich base antimalarial aminoalkylphenol compounds and their use against protozoa of the genus Plasmodium, particularly emerging strains of drug-resistant Plasmodia. This invention further relates to compositions containing such compounds and a process for making the compounds. This and other aspects of the invention are realized upon review of the entire specification.
摘要翻译：本发明涉及曼尼希碱抗疟氨基烷基苯酚化合物及其抗疟原虫的原生动物的用途，特别是新出现的抗药性血浆的菌株。本发明还涉及含有这些化合物的组合物和制备该化合物的方法。本发明的这个和其它方面在整个说明书的审查之后实现。

57. 发明授权

US07504501B2 Antiprotozoal imidazopyridine compounds 有权
标题翻译：抗原虫咪唑并吡啶化合物
公开(公告)号：US07504501B2
公开(公告)日：2009-03-17
申请号：US10548154
申请日：2004-03-02
申请人： Matthew J. Wyvratt , Tesfaye Biftu , Michael H. Fisher , Dennis M. Schmatz
发明人： Matthew J. Wyvratt , Tesfaye Biftu , Michael H. Fisher , Dennis M. Schmatz
IPC分类号： C07D403/04 , A61K31/429
CPC分类号： C07D471/04 , C07D519/00
摘要： Compounds described by the Formula (I): (I) or pharmaceutically acceptable salts, or N-oxides thereof. The compounds are useful for the treatment and prevention of protozoal diseases in mammals and birds. A method for controlling coccidiosis in poultry comprises administering an effective amount of the compound alone, or in combination with one or more anticoccidial agent(s). A composition for controlling coccidiosis in poultry comprises the compound alone, or in combination with one or more anticoccidial agent(s). Methods for the treatment and prevention of mammalian protozoal diseases, such as, for example, toxoplasmosis, malaria, African trypanosomiasis, Chagas disease, and opportunistic infections comprise administering the compound alone, or in combination with one or more antiprotozoal agent(s).
摘要翻译：由式（I）表示的化合物：（I）或其药学上可接受的盐或N-氧化物。该化合物可用于治疗和预防哺乳动物和鸟类中的原生动物疾病。控制家禽中球虫病的方法包括单独施用有效量的化合物，或与一种或多种抗球虫剂组合施用。用于控制家禽中球虫病的组合物包含单独的化合物，或与一种或多种抗球虫剂组合。用于治疗和预防哺乳动物原生动物疾病的方法，例如弓形虫病，疟疾，非洲锥虫病，恰加斯病和机会性感染包括单独施用化合物，或与一种或多种抗原虫剂组合施用。

58. 发明授权

US07429590B2 Antiprotozoal imidazopyridine compounds 有权
标题翻译：抗原虫咪唑并吡啶化合物
公开(公告)号：US07429590B2
公开(公告)日：2008-09-30
申请号：US10573363
申请日：2004-12-06
申请人： Tesfaye Biftu , Matthew J. Wyvratt , Louis L. Zuegner, III, legal representative
发明人： Michael H. Fisher
IPC分类号： C07D401/04 , C07D403/04 , C07D417/04 , A61K31/4188
CPC分类号： C07D471/04
摘要： Compounds described by the Formula (I) or (II): or pharmaceutically acceptable salts, or N-oxides thereof. The compounds are useful for the treatment and prevention of protozoal diseases in mammals and birds. A method for controlling coccidiosis in poultry comprises administering an effective amount of the compound alone, or in combination with one or more anticoccidieal agent(s). A composition for controlling coccidiosis in poultry comprises the compound alone, or in combination with one or more anticoccidial agent(s). Methods for the treatment and prevention of mammalian protozoal diseases, such as, for example, toxoplasmosis, malaria. African typanosomiasis, Chagas disease, and opportunistic infections comprise administering the compound alone, or in combination with one or more antiprotozoal agent(s).
摘要翻译：由式（I）或（II）表示的化合物：或其药学上可接受的盐或N-氧化物。该化合物可用于治疗和预防哺乳动物和鸟类中的原生动物疾病。用于控制家禽中球虫病的方法包括单独施用有效量的化合物，或与一种或多种抗球虫剂组合施用。用于控制家禽中球虫病的组合物包含单独的化合物，或与一种或多种抗球虫剂组合。用于治疗和预防哺乳动物原生动物疾病的方法，例如弓形体病，疟疾。非洲typanosomias，恰加斯病和机会性感染包括单独施用化合物，或与一种或多种抗原虫剂组合施用。

59. 发明授权

US06586452B1 C1 to C4 side chain modified nodulisporic acid analogs 有权
标题翻译： C1至C4侧链修饰的nodulisporic酸类似物
公开(公告)号：US06586452B1
公开(公告)日：2003-07-01
申请号：US09901266
申请日：2001-07-09
申请人： Thomas Shih , Steven L. Colletti , Michael H. Fisher , Peter T. Meinke , Howard C. H. Kuo , Prasun K. Chakravarty , Matthew J. Wyvratt , Sriram Tyagarajan , Richard Berger
发明人： Thomas Shih , Steven L. Colletti , Michael H. Fisher , Peter T. Meinke , Howard C. H. Kuo , Prasun K. Chakravarty , Matthew J. Wyvratt , Sriram Tyagarajan , Richard Berger
IPC分类号： C07D48716
CPC分类号： C07D491/16 , A61K31/407 , C07D491/22
摘要： The present invention relates to novel nodulosporic acid derivatives, which are acaricidal, antiparasitic, insecticidal and anthelmintic agents.
摘要翻译：本发明涉及杀螨，抗寄生虫，杀虫剂和驱肠虫剂的新型节肢动物酸衍生物。

60. 发明授权

US06528531B1 Aliphatic hydroxy substituted piperidyl diaryl pyrrole derivatives as antiprotozoal agents 失效
标题翻译：脂肪族羟基取代的哌啶基二芳基吡咯衍生物作为抗原虫剂
公开(公告)号：US06528531B1
公开(公告)日：2003-03-04
申请号：US09709961
申请日：2000-11-10
申请人： Tesfaye Bitfu , Danqing D. Feng , Gui-Bai Liang , Mitree M. Ponpipom , Xiaoxia Qian , Michael H. Fisher , Matthew J. Wyvratt , Robert L. Bugianesi
发明人： Tesfaye Bitfu , Danqing D. Feng , Gui-Bai Liang , Mitree M. Ponpipom , Xiaoxia Qian , Michael H. Fisher , Matthew J. Wyvratt , Robert L. Bugianesi
IPC分类号： A61K31445
CPC分类号： C07D401/14 , C07D405/14
摘要： Trisubstituted pyrroles are antiprotozoal agents useful in the treatment and prevention of protozoal diseases in human and animals, including the control of coccidiosis in poultry.
摘要翻译：三取代吡咯是可用于治疗和预防人类和动物中的原生动物疾病的抗原虫剂，包括控制家禽中的球虫病。

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