公开(公告)号：US5565560A

公开(公告)日：1996-10-15

申请号：US132072

申请日：1993-10-04

申请人： Mark Goulet ,  Helen M. Organ ,  William H. Parsons ,  Peter J. Sinclair ,  Frederick Wong ,  Matthew J. Wyvratt

发明人： Mark Goulet ,  Helen M. Organ ,  William H. Parsons ,  Peter J. Sinclair ,  Frederick Wong ,  Matthew J. Wyvratt

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

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 and/or related afflictions, diseases and illnesses.

摘要翻译： 一般结构式I的O-芳基，O-烷基，O-链烯基和O-炔基 - 大环内酯类：已经通过C-3“和/或C的烷基化和/或芳基化由合适的前体制备 -4“。 这些大环内酯类免疫抑制剂可用于哺乳动物宿主用于治疗自身免疫性疾病，感染性疾病和/或预防外来器官移植排斥和/或相关疾病，疾病和疾病。

公开(公告)号：US5532248A

公开(公告)日：1996-07-02

申请号：US440180

申请日：1995-05-12

申请人： Mark Goulet ,  William H. Parsons ,  Helen M. Organ ,  Peter J. Sinclair ,  Frederick Wong ,  Matthew J. Wyvratt

发明人： Mark Goulet ,  William H. Parsons ,  Helen M. Organ ,  Peter J. Sinclair ,  Frederick Wong ,  Matthew J. Wyvratt

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

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 and/or related afflictions, diseases and illnesses.

摘要翻译： 一般结构式I的O-芳基，O-烷基，O-链烯基和O-炔基 - 大环内酯类：已经通过C-3“和/或C的烷基化和/或芳基化由合适的前体制备 -4“。 这些大环内酯类免疫抑制剂可用于哺乳动物宿主用于治疗自身免疫性疾病，感染性疾病和/或预防外来器官移植排斥和/或相关疾病，疾病和疾病。

公开(公告)号：US5344925A

公开(公告)日：1994-09-06

申请号：US124137

申请日：1993-09-20

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

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

IPC分类号： C07H19/01 ,  A61K20060101 ,  A61K31/395 ,  A61K31/4178 ,  A61K31/4184 ,  A61K31/422 ,  A61K31/423 ,  A61K31/427 ,  A61K31/428 ,  A61K31/435 ,  A61K31/436 ,  A61K31/70 ,  A61K31/7056 ,  A61P37/06 ,  C07D20060101 ,  C07D498/12 ,  C07D498/18 ,  C07H7/06 ,  C07H15/04 ,  C07H19/02 ,  C07D491/16

CPC分类号： C07H19/01

摘要： Imidazolidyl 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 the prevention of rejection of foreign organ transplants and/or related afflictions, diseases and illnesses.

摘要翻译： 一般结构式I的咪唑烷基大环内酯：通过在环己基环的C-3“和/或C-4”进行烷基化和/或芳基化，由合适的前体制备。 这些大环内酯类免疫抑制剂可用于哺乳动物宿主用于治疗自身免疫性疾病，感染性疾病，预防外来器官移植排斥和/或相关疾病，疾病和疾病。

公开(公告)号：US5258389A

公开(公告)日：1993-11-02

申请号：US973807

申请日：1992-11-09

申请人： Mark Goulet ,  William H. Parsons ,  Peter J. Sinclair ,  Frederick Wong ,  Matthew J. Wyvratt

发明人： Mark Goulet ,  William H. Parsons ,  Peter J. Sinclair ,  Frederick Wong ,  Matthew J. Wyvratt

IPC分类号： C07D498/18 ,  A61K31/395 ,  C07D498/16

CPC分类号： C07D498/18

摘要： O-Aryl, O-alkyl, O-alkenyl and O-alkynylrapamycin derivatives of the general structural Formula I: ##STR1## have been prepared from suitable precursors by alkylation and/or arylation at C-42 and/or C-31. These compounds are useful in a mammalian host for the treatment of autoimmune diseases and diseases of inflammation, infectious diseases, the prevention of rejection of foreign organ transplants and the treatment of solid tumors.

摘要翻译： 通式I的O-芳基，O-烷基，O-烯基和O-炔基雷帕霉素衍生物：通过C-42和/或C-31的烷基化和/或芳基化，由合适的前体制备。 这些化合物可用于哺乳动物宿主用于治疗自身免疫性疾病和炎症疾病，感染性疾病，预防外来器官移植排斥和治疗实体瘤。

公开(公告)号：US5247076A

公开(公告)日：1993-09-21

申请号：US921181

申请日：1992-08-04

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

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

IPC分类号： C07H19/01 ,  A61K20060101 ,  A61K31/395 ,  A61K31/4178 ,  A61K31/4184 ,  A61K31/422 ,  A61K31/423 ,  A61K31/427 ,  A61K31/428 ,  A61K31/435 ,  A61K31/436 ,  A61K31/70 ,  A61K31/7056 ,  A61P37/06 ,  C07D20060101 ,  C07D498/12 ,  C07D498/18 ,  C07H7/06 ,  C07H15/04 ,  C07H19/02

CPC分类号： C07H19/01

摘要： Imidazolidyl 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 the prevention of rejection of foreign organ transplants and/or related afflictions, diseases and illnesses.

公开(公告)号：US5693648A

公开(公告)日：1997-12-02

申请号：US619638

申请日：1996-03-27

申请人： Mark Goulet ,  Helen M. Organ ,  William H. Parsons ,  Peter J. Sinclair ,  Frederick Wong ,  Matthew J. Wyvratt

发明人： Mark Goulet ,  Helen M. Organ ,  William H. Parsons ,  Peter J. Sinclair ,  Frederick Wong ,  Matthew J. Wyvratt

IPC分类号： C07D491/16 ,  A61K31/435

CPC分类号： C07D491/16

摘要： Substituted compounds of the FK-506 Type. These compounds are useful for the same or essentially the same purposes as FK-506 and are applied in the same or a similar manner. These compounds are immunosuppressants and useful for the treatment of autoimmune diseases, infectious diseases and/or the prevention of rejection of foreign organ transplants. Still other uses are described in the disclosure.

摘要翻译： PCT No.PCT / US94 / 11114 Sec。 371日期：1996年3月27日 102（e）1996年3月27日PCT 1994年9月30日PCT公布。 公开号WO95 / 09857 日期：1995年04月13日FK-506型的取代化合物。 这些化合物可用于与FK-506相同或基本相同的目的，并以相同或相似的方式施用。 这些化合物是免疫抑制剂，可用于治疗自身免疫疾病，感染性疾病和/或预防外来器官移植排斥反应。 在本公开中描述了其他用途。

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.

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.

公开(公告)号：US5349061A

公开(公告)日：1994-09-20

申请号：US135200

申请日：1993-10-12

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 ,  A61K31/345 ,  C07D491/16

CPC分类号： C07H19/01

摘要： O-Heteroaryl, O-alkylheteroaryl, O-alkenylheteroaryl and O-alkynylheteroaryl-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, the prevention of rejection of foreign organ transplants and/or related afflictions, diseases and illnesses.

摘要翻译： 通式I的O-杂芳基，O-烷基杂芳基，O-链烯基杂芳基和O-炔基杂芳基 - 大环内酯：通过C-3“和/或C的烷基化和/或芳基化从合适的前体制备 -4“。 这些大环内酯类免疫抑制剂可用于哺乳动物宿主用于治疗自身免疫疾病，感染性疾病，预防外来器官移植排斥和/或相关疾病，疾病和疾病。

公开(公告)号：US5310901A

公开(公告)日：1994-05-10

申请号：US26926

申请日：1993-03-05

申请人： William H. Parsons ,  Peter J. Sinclair ,  Frederick Wong ,  Matthew J. Wyvratt

发明人： William H. Parsons ,  Peter J. Sinclair ,  Frederick Wong ,  Matthew J. Wyvratt

IPC分类号： C07D498/18 ,  A61K31/395 ,  C07D471/18

CPC分类号： C07D498/18

摘要： O-Heteroaryl, O-alkylheteroaryl, O-alkenylheteroaryl and O-alkynylheteroarylrapamycin derivatives of the general structural Formula I: ##STR1## have been prepared from suitable precursors by alkylation and/or arylation at C-42 and/or C-31. These compounds are useful in a mammalian host for the treatment of autoimmune diseases and diseases of inflammation, infectious diseases, the prevention of rejection of foreign organ transplants and the treatment of solid tumors.

摘要翻译： 通过在C-42和/或C-31上烷基化和/或芳基化从合适的前体制备通式I的O-杂芳基，O-烷基杂芳基，O-链烯基杂芳基和O-炔基杂芳基雷帕霉素衍生物。 这些化合物可用于哺乳动物宿主用于治疗自身免疫性疾病和炎症疾病，感染性疾病，预防外来器官移植排斥和治疗实体瘤。