公开(公告)号：US5057499A

公开(公告)日：1991-10-15

申请号：US360621

申请日：1989-06-02

Applicant: Helmut Mrozik ,  Peter J. Sinclair

Inventor： Helmut Mrozik ,  Peter J. Sinclair

IPC: C07H17/08 ,  A01N43/90 ,  A61K31/365 ,  A61K31/70 ,  A61K31/7042 ,  A61K31/7048 ,  A61P33/10 ,  C07D493/22 ,  C07H19/01

CPC classification number: C07H19/01 ,  A01N43/90

Abstract: There are disclosed novel avermectin derivatives wherein the outer oleandrose ring of avermectin or avermectin monosaccharide is homologated by addition of diazomethane to 4"- or 4'-oxo-avermectin to afford the perhydrooxepine derivatives. The homologated avermectins can then be further derivatized to afford additional novel avermectins. The new compounds are potent antiparasitic agents, in particular, the compounds are anthelmintic, insecticidal and acaricidal agents.

公开(公告)号：US4978656A

公开(公告)日：1990-12-18

申请号：US231318

申请日：1988-08-12

Applicant: Timothy A. Blizzard ,  Helmut Mrozik ,  Gaye Marino ,  Peter J. Sinclair

Inventor： Timothy A. Blizzard ,  Helmut Mrozik ,  Gaye Marino ,  Peter J. Sinclair

IPC: H04N5/222 ,  A01N43/90 ,  A61K31/435 ,  A61K31/495 ,  A61P33/10 ,  C07D471/18 ,  C07D471/22 ,  C07D491/22 ,  C07D498/22 ,  C07F7/18 ,  C07F9/6561 ,  G06T7/00 ,  H04N5/232 ,  H04N5/33 ,  H04N5/365 ,  H04N17/00

CPC classification number: C07D491/22 ,  A01N43/90 ,  C07D498/22 ,  C07F7/1856 ,  C07F9/6561

Abstract: There are disclosed synthetic derivatives of the natural product paraherquamide. The synthetic derivatives are prepared by reactions at the parahequamide A, B, E, F and G rings, that is at carbon atoms 14 to 16, the lactam ring and carbon atoms 24 to 26 as well as carbon atoms 5 and 12. The compounds are active antiparasitic agents and compositions for that use are also disclosed.

公开(公告)号：US5030622A

公开(公告)日：1991-07-09

申请号：US360620

申请日：1989-06-02

Applicant: Helmut Mrozik ,  Peter J. Sinclair

Inventor： Helmut Mrozik ,  Peter J. Sinclair

IPC: C07H17/08 ,  A01N43/90 ,  A61K31/70 ,  A61K31/7042 ,  A61K31/7048 ,  A61P33/10 ,  C07H19/01

CPC classification number: C07H19/01

Abstract: There are disclosed novel avermectin derivatives wherein the outer oleandrose ring of avermectin or avermectin monosaccharide is homologated by addition of diazomethane to 4"- or 4'-oxo-avermectin to afford the oleandrose 4"- or 4'-spiro-epoxide. The homologated avermectins can then be further derivatized to afford additional novel avermectins. The new compounds are potent antiparasitic agents, in particular, the compounds are anthelmintic, insecticidal and acaricidal agents.

公开(公告)号：US08933113B2

公开(公告)日：2015-01-13

申请号：US13979875

申请日：2012-01-19

Applicant: Alejandro Crespo ,  Ping Lan ,  Rudrajit Mal ,  Anthony Ogawa ,  Hong Shen ,  Peter J. Sinclair ,  Zhongxiang Sun ,  Ellen K. Vande Bunte ,  Zhicai Wu ,  Kun Liu ,  Robert J. DeVita ,  Dong-Ming Shen ,  Min Shu ,  John Qiang Tan ,  Changhe Qi ,  Yuguang Wang ,  Richard Beresis

Inventor： Alejandro Crespo ,  Ping Lan ,  Rudrajit Mal ,  Anthony Ogawa ,  Hong Shen ,  Peter J. Sinclair ,  Zhongxiang Sun ,  Ellen K. Vande Bunte ,  Zhicai Wu ,  Kun Liu ,  Robert J. DeVita ,  Dong-Ming Shen ,  Min Shu ,  John Qiang Tan ,  Changhe Qi ,  Yuguang Wang ,  Richard Beresis

IPC: A61K31/416 ,  C07D231/56 ,  A61K31/405 ,  A61K31/404 ,  C07D403/06 ,  C07D209/08 ,  C07D209/10 ,  A61K31/4196 ,  A61K31/422 ,  A61K31/4245 ,  A61K45/06 ,  C07D413/06

CPC classification number: C07D413/06 ,  A61K31/404 ,  A61K31/4045 ,  A61K31/405 ,  A61K31/416 ,  A61K31/4196 ,  A61K31/422 ,  A61K31/4245 ,  A61K45/06 ,  C07D209/08 ,  C07D209/10 ,  C07D231/56 ,  C07D403/04 ,  C07D403/06 ,  C07D405/06

Abstract: Disclosed are the compounds of the Formula (I) as well as pharmaceutically acceptable salts thereof, which are useful for treating aldosterone-mediated diseases. The processes for preparing compounds of the Formula (I), the use for the therapy and prophylaxis of the abovementioned diseases and for preparing pharmaceuticals for this purpose, and the pharmaceutical compositions which comprise compounds of the formula (I) are disclosed too.

Abstract translation: 公开了式（I）化合物及其药学上可接受的盐，其可用于治疗醛固酮介导的疾病。 还公开了制备式（I）化合物，用于治疗和预防上述疾病和用于制备用于此目的的药物的方法和包含式（I）化合物的药物组合物。

公开(公告)号：US20090018054A1

公开(公告)日：2009-01-15

申请号：US12087189

申请日：2006-12-29

Applicant: Amjad Ali ,  Peter J. Sinclair ,  Gayle E. Taylor

Inventor： Amjad Ali ,  Peter J. Sinclair ,  Gayle E. Taylor

IPC: A61K38/28 ,  C07D265/10 ,  A61K31/535 ,  A61K31/5355 ,  C07D413/06 ,  A61K31/45 ,  C07D211/76 ,  A61P9/10

CPC classification number: C07D265/10 ,  C07D413/06

Abstract: Compounds of Formula (I), including pharmaceutically acceptable salts of the compounds, are CETP inhibitors, and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis. In the compounds of Formula (I), A1 is a cyclic group, and B is a cyclic group which is attached to the heterocyclic ring directly or through a methylene group.

Abstract translation: 包括化合物的药学上可接受的盐的式（I）化合物是CETP抑制剂，可用于升高HDL-胆固醇，降低LDL-胆固醇，以及用于治疗或预防动脉粥样硬化。 在式（I）的化合物中，A1是环状基团，B是直接或通过亚甲基与杂环连接的环状基团。

公开(公告)号：US5693648A

公开(公告)日：1997-12-02

申请号：US619638

申请日：1996-03-27

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

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

IPC: C07D491/16 ,  A61K31/435

CPC classification number: C07D491/16

Abstract: 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.

Abstract translation: 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：US5262533A

公开(公告)日：1993-11-16

申请号：US876634

申请日：1992-05-06

Applicant: Peter J. Sinclair ,  Helen M. Organ ,  Matthew J. Wyvratt

Inventor： Peter J. Sinclair ,  Helen M. Organ ,  Matthew J. Wyvratt

IPC: C07D498/18 ,  C07D491/16 ,  A61K31/395

CPC classification number: C07D498/18

Abstract: Amino O-aryl macrolides of the general structural Formula I: ##STR1## have been prepared from suitable precursors by arylation and amination at C-3"/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, inflammatory 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.

Abstract translation: 一般结构式I的氨基O-芳基大环内酯是通过在环己基环的C-3“/ C-4”处的芳基化和胺化由合适的前体制备的。 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反应。 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。 此外，这些大环内酯可用于治疗可逆性阻塞性气道疾病，特别是哮喘; 作为头发活化剂，特别是在治疗男性脱发或脱发性秃发症中， 在逆转肿瘤细胞的多药耐药性; 治疗粘膜和血管的炎症，胃溃疡，血管损伤，缺血性肠病，炎性肠病，坏死性小肠结肠炎，与热灼伤相关的肠道损伤; 在治疗巨细胞病毒感染; 并在治疗特发性血小板减少性紫癜和基诺病。

公开(公告)号：US5252732A

公开(公告)日：1993-10-12

申请号：US921851

申请日：1992-08-05

Applicant: Peter J. Sinclair ,  Joung Goulet ,  Frederick Wong ,  Mark Goulet ,  William H. Parsons ,  Matthew J. Wyvratt

Inventor： Peter J. Sinclair ,  Joung Goulet ,  Frederick Wong ,  Mark Goulet ,  William H. Parsons ,  Matthew J. Wyvratt

IPC: A61K31/40 ,  A61K31/445 ,  A61K31/495 ,  A61K31/70 ,  A61P37/06 ,  C07D498/18 ,  C07H19/01 ,  A61K31/395 ,  C07D491/16

CPC classification number: C07H19/01

Abstract: 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

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.

公开(公告)号：US08445480B2

公开(公告)日：2013-05-21

申请号：US12664757

申请日：2008-06-16

Applicant: Julianne A. Hunt ,  Ramzi F. Sweis ,  Dooseop Kim ,  Florida Kallashi ,  Peter J. Sinclair

Inventor： Julianne A. Hunt ,  Ramzi F. Sweis ,  Dooseop Kim ,  Florida Kallashi ,  Peter J. Sinclair

IPC: A61K31/553 ,  A61K31/5377 ,  A61K31/506 ,  A61K31/443 ,  A61K31/4525 ,  A61K31/423 ,  A61K31/438 ,  C07D239/42 ,  C07D267/10 ,  C07D413/14 ,  C07D401/14 ,  C07D221/20 ,  C07D211/26 ,  C07D263/57

CPC classification number: C07D413/14 ,  C07D413/10 ,  C07D413/12

Abstract: Compounds having the structure of Formula I1 including pharmaceutically acceptable salts of the compounds, are potent CETP (cholesterol ester transfer protein) inhibitors, and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis Atherosclerosis and its clinical consequences, coronary heart disease (CHD), stroke and penpheral vascular disease, represent a truly enormous burden to the health care systems of the industrialized world In formula I, A-B is an arylamide moiety.

Abstract translation: 具有式I结构的化合物，包括化合物的药学上可接受的盐，是有效的CETP（胆固醇酯转移蛋白）抑制剂，可用于培养HDL-胆固醇，降低LDL-胆固醇，并用于治疗或预防动脉粥样硬化。动脉粥样硬化及其临床 后果，冠心病（CHD），中风和血管性血管疾病对工业化世界的保健系统来说是一个真正的巨大负担。在公式I中，AB是芳基酰胺部分。