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    O-aryl, O-alkyl, O-alkenyl and O-alkynylmacrolides having immunosuppressive activity
    52.
    发明授权
    O-aryl, O-alkyl, O-alkenyl and O-alkynylmacrolides having immunosuppressive activity 失效
    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

    Applicant: Mark Goulet ,  Frederick Wong ,  Peter J. Sinclair ,  Matthew J. Wyvratt

    Inventor： Mark Goulet ,  Frederick Wong ,  Peter J. Sinclair ,  Matthew J. Wyvratt

    IPC: A61K31/41 ,  A61K31/40 ,  A61K31/445 ,  A61P17/00 ,  A61P29/00 ,  A61P31/12 ,  A61P37/06 ,  C07D498/18 ,  C07D491/16 ,  A61K31/435

    CPC classification number: C07D498/18

    Abstract: 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.

    Halomacrolides and derivatives having immunosuppressive activity
    53.
    发明授权
    Halomacrolides and derivatives having immunosuppressive activity 失效
    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

    Applicant: Richard J. Bochis ,  Matthew J. Wyvratt, Jr.

    Inventor： Richard J. Bochis ,  Matthew J. Wyvratt, Jr.

    IPC: C07H19/01

    CPC classification number: C07H19/01

    Abstract: 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.

    Abstract translation: 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。

    Hydroxymacrolide derivatives having immunosuppressive activity
    54.
    发明授权
    Hydroxymacrolide derivatives having immunosuppressive activity 失效
    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

    Applicant: Richard J. Bochis ,  Huyn O. Ok ,  Matthew J. Wyvratt

    Inventor： Richard J. Bochis ,  Huyn O. Ok ,  Matthew J. Wyvratt

    IPC: A61K31/40 ,  A61K31/445 ,  A61P17/00 ,  A61P37/06 ,  C07D498/18 ,  C07H19/01

    CPC classification number: C07H19/01

    Abstract: 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.

    Antiprotozoal imidazopyridine compounds
    57.
    发明授权
    Antiprotozoal imidazopyridine compounds 有权
    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

    Applicant: Matthew J. Wyvratt ,  Tesfaye Biftu ,  Michael H. Fisher ,  Dennis M. Schmatz

    Inventor： Matthew J. Wyvratt ,  Tesfaye Biftu ,  Michael H. Fisher ,  Dennis M. Schmatz

    IPC: C07D403/04 ,  A61K31/429

    CPC classification number: C07D471/04 ,  C07D519/00

    Abstract: 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).

    Abstract translation: 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。

    Antiprotozoal imidazopyridine compounds
    58.
    发明授权
    Antiprotozoal imidazopyridine compounds 有权
    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

    Applicant: Tesfaye Biftu ,  Matthew J. Wyvratt ,  Louis L. Zuegner, III, legal representative

    Inventor： Michael H. Fisher

    IPC: C07D401/04 ,  C07D403/04 ,  C07D417/04 ,  A61K31/4188

    CPC classification number: C07D471/04

    Abstract: 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).

    Abstract translation: 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。

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