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1. 发明申请

US20060040934A1 Use of STAT-6 inhibitors as therapeutic agents 审中-公开
公开(公告)号：US20060040934A1
公开(公告)日：2006-02-23
申请号：US11077986
申请日：2005-03-11
申请人： Howard Cottam , Lorenzo Leoni , Dennis Carson
发明人： Howard Cottam , Lorenzo Leoni , Dennis Carson
IPC分类号： A61K31/5377 , A61K31/429 , A61K31/424 , A61K31/4188
CPC分类号： C07D513/04 , A61K31/519 , C07D487/04
摘要： The present invention provides novel indole derivatives useful to inhibit cancer or sensitize cancer cells to chemotherapeutic agents, radiation or other anti-cancer treatments.

2. 发明申请

US20050239752A1 Indole compounds useful for the treatment of cancer 失效
标题翻译：吲哚化合物可用于治疗癌症
公开(公告)号：US20050239752A1
公开(公告)日：2005-10-27
申请号：US11013955
申请日：2004-12-16
申请人： Dennis Carson , Howard Cottam , Lorenzo Leoni
发明人： Dennis Carson , Howard Cottam , Lorenzo Leoni
IPC分类号： A61K31/407 , A61K31/4439 , A61K31/7052 , C07D491/02 , C07D491/04 , C07D498/02
CPC分类号： C07D491/04
摘要： The present invention provides novel indole derivatives useful to inhibit cancer or sensitize cancer cells to chemotherapeutic agents, radiation or other anti-cancer treatments.
摘要翻译：本发明提供了可用于抑制癌症或使癌细胞对化学治疗剂，辐射或其它抗癌治疗敏感的新型吲哚衍生物。

3. 发明申请

US20070111950A1 INDOLE COMPOUNDS USEFUL FOR THE TREATMENT OF CANCER 审中-公开
标题翻译：单用化合物治疗癌症有用
公开(公告)号：US20070111950A1
公开(公告)日：2007-05-17
申请号：US11612414
申请日：2006-12-18
申请人： Dennis Carson , Lorenzo Leoni , Howard Cottam
发明人： Dennis Carson , Lorenzo Leoni , Howard Cottam
IPC分类号： A61K31/7056 , A61K31/5377 , A61K31/4439 , A61K31/407 , C07D491/04 , C07D498/04
CPC分类号： A61K31/535 , A61K45/06 , A61K2300/00
摘要： The present invention provides novel indole derivatives useful to inhibit cancer or sensitize cancer cells to chemotherapeutic agents, radiation or other anti-cancer treatments.
摘要翻译：本发明提供了可用于抑制癌症或使癌细胞对化学治疗剂，辐射或其它抗癌治疗敏感的新型吲哚衍生物。

4. 发明申请

US20060293253A1 INDOLE COMPOUNDS USEFUL FOR THE TREATMENT OF CANCER 失效
标题翻译：单用化合物治疗癌症有用
公开(公告)号：US20060293253A1
公开(公告)日：2006-12-28
申请号：US11467472
申请日：2006-08-25
申请人： Dennis Carson , Howard Cottam , Lorenzo Leoni
发明人： Dennis Carson , Howard Cottam , Lorenzo Leoni
IPC分类号： A61K31/7056 , A61K31/675 , A61K31/541 , A61K31/5377 , A61K31/496 , A61K31/4439 , A61K31/407
CPC分类号： A61K31/407 , A61K31/4439 , A61K31/496 , A61K31/5377 , A61K31/541 , A61K31/675 , A61K31/7056 , G01N33/57434 , G01N2800/52
摘要： The present invention provides novel indole derivatives useful to inhibit cancer or sensitize cancer cells to chemotherapeutic agents, radiation or other anti-cancer treatments.
摘要翻译：本发明提供了可用于抑制癌症或使癌细胞对化学治疗剂，辐射或其它抗癌治疗敏感的新型吲哚衍生物。

5. 发明申请

US20050154010A1 Treatment of cancer with mefloquine, its purified enantiomers, and mefloquine analogs 审中-公开
标题翻译：用梅氟喹，其纯化的对映异构体和甲氟喹类似物治疗癌症
公开(公告)号：US20050154010A1
公开(公告)日：2005-07-14
申请号：US10509693
申请日：2003-05-16
申请人： Dennis Carson , Lorenzo Leoni , Howard Cottam
发明人： Dennis Carson , Lorenzo Leoni , Howard Cottam
IPC分类号： A61K31/4709 , A61K31/4745
CPC分类号： A61K31/4745 , A61K31/4709
摘要： Cancers, particularly solid tumors (e.g., breast, lung, renal, colon and ovarian cancers and melanomas) and cancers of the hematologic system, e.g., hemopoietic cancers such as leukemias, lymphomas or myelomas, are treated by administration of a therapeutically effective amount of a compound having the formula (1): (I)in which the quinoline ring is substituted by from one to three groups selected from halogen and trifluoromethyl (designated in the formula by “A”), and is optionally further substituted by one or more other moieties and R is (a) NR1R2 in which R1 and R2 are independently hydrogen or C1-C4 alkyl; (b) 2-piperidyl, (c) 2-pyridyl, and (d) 5-(ethyl or vinyl)-quinuclidin-4-yl; an enantiomer of such a compound; a pharmaceutically acceptable salts of such a compound or of an enantiomer thereof; a prodrug of such a compound or of an enantiomer thereof; a metabolite of such a compound or of an enantiomer thereof; and mixtures of two or more of the foregoing. A particularly preferred compound is mefloquine.
摘要翻译：癌症，特别是实体肿瘤（例如乳腺癌，肺癌，结肠癌，卵巢癌和黑素瘤）和血液系统的癌症，例如造血性癌症如白血病，淋巴瘤或骨髓瘤，通过施用治疗有效量的具有式（1）：（I）的化合物，其中喹啉环被选自卤素和三氟甲基（式中“A”表示）的一至三个基团取代，并且任选进一步被一个或多个其它部分和R是（a）NR1R2，其中R1和R2独立地是氢或C1-C4烷基; （b）2-哌啶基，（c）2-吡啶基和（d）5-（乙基或乙烯基） - 奎宁环-4-基; 这种化合物的对映异构体; 这种化合物或其对映异构体的药学上可接受的盐; 这种化合物或其对映异构体的前药; 这种化合物或其对映异构体的代谢物; 以及上述两种或更多种的混合物。特别优选的化合物是甲氟喹。

6. 发明申请

US20070299042A1 USE OF ETODOLAC TO TREAT HYPERPLASIA 审中-公开
公开(公告)号：US20070299042A1
公开(公告)日：2007-12-27
申请号：US11615396
申请日：2006-12-22
申请人： Dennis Carson , Lorenzo Leoni , Mary Corr
发明人： Dennis Carson , Lorenzo Leoni , Mary Corr
IPC分类号： A61K31/407 , A61K31/496 , A61K31/56 , A61P35/00
CPC分类号： A61K31/12 , A61K31/18 , A61K31/40 , A61K31/407 , A61K31/4745 , A61K31/496 , A61K31/50 , A61K31/56 , A61K31/675 , A61K31/7052
摘要： The present invention provides a therapeutic method to treat non-malignant diseases characterized by the excessive tissue growth, e.g., hyperplastic diseases, comprising administering to a mammal (e.g., human) afflicted with excessive tissue growth, an effective amount of a derivative of an indole compound of formula (I):formula (I): wherein R1 is lower alkyl, (hydroxy)lower alkyl, lower alkenyl, lower alkynyl, lower cycloalkyl, phenyl, benzyl or 2-thienyl; R2, R3, R4 and R5 are the same or different and are each hydrogen or lower alkyl; each R6 is individually hydrogen, lower alkyl, hydroxy, (hydroxy)lower alkyl, lower alkoxy, benzyloxy, lower alkanoyloxy, nitro or halo, R7 is hydrogen, lower alkyl or lower alkenyl, X is oxy and thio, Y is carbonyl, —(CH2)1-3—, —(C1-C3)alkyl(CO)—, or —(CH2)1-3SO2—; Z is hydroxy, lower alkoxy, (C2-C4)acyloxy, —N(R8)(R9), phenylamino, (ω-(4-pyridyl)(C2-C4 alkoxy), (ω-((R8)(R9) amino)(C2-C4 alkoxy), an amino acid ester of (ω-(HO)(C2-C4))alkoxy, —N(R8)CH(R8)CO2H, 1′-D-glucuronyloxy, —SO3H, —PO4H2, —N(NO)(OH), —SO2NH2, —PO(OH)(NH2), —OCH2CH2N(CH3)3+, or tetrazolyl; wherein R8 and R9 are each H, (C1-C3)alkyl or together with N are a 5- or 6-membered heterocyclic ring comprising 1-3 N(R8), S or nonperoxide O; n is 0, 1, 2, or 3; wherein R8 and R9 are each H, (C1-C3)alkyl or together with N are a 5- or 6-membered heterocyclic ring comprising 1-3 N(R8), S or nonperoxide O; each alkyl or phenyl group of R1, R2, R3, R4,R5, R6, R7 and Z is optionally substituted with 1, 2, or 3 (C1-C4)alkyl groups; or a pharmaceutically acceptable salt thereof.

7. 发明申请

US20060122178A1 Compounds having activity as inhibitors of apoptosis 失效
公开(公告)号：US20060122178A1
公开(公告)日：2006-06-08
申请号：US11271511
申请日：2005-11-10
申请人： Howard Cottam , Dennis Carson , Sylvie Barchechath
发明人： Howard Cottam , Dennis Carson , Sylvie Barchechath
IPC分类号： A61K31/5377 , A61K31/454 , A61K31/429 , A61K31/424 , A61K31/4188 , C07D498/02 , C07D491/02 , C07D487/02
CPC分类号： C07D487/04 , C07D513/04
摘要： The present invention provides compounds that can protect mammalian cells from the damaging effects of chemotherapy, irradiation, or in other situations in which it is desirable to protect tissue from the consequences of clinical or environmental stress.

8. 发明申请

US20050065116A1 Thiazolopyrimidines useful as TNFalpha inhibitors 失效
标题翻译：噻唑并嘧啶可用作TNFα抑制剂
公开(公告)号：US20050065116A1
公开(公告)日：2005-03-24
申请号：US10952077
申请日：2004-09-28
申请人： Dennis Carson , Howard Cottam , Lynn Deng
发明人： Dennis Carson , Howard Cottam , Lynn Deng
IPC分类号： C07D239/54 , A61K9/08 , A61K9/14 , A61K9/48 , A61K31/513 , A61K31/519 , A61P1/00 , A61P3/10 , A61P9/10 , A61P17/06 , A61P19/02 , A61P25/00 , A61P29/00 , A61P37/00 , A61P37/06 , C07D513/04 , A61K31/675 , C07D498/02
CPC分类号： C07D513/04
摘要： The invention provides derivatives of thiazolo[4,5-d1]pyrimidine and their use as inhibitors of proinflammatory cytokines.
摘要翻译：本发明提供噻唑并[4,5-d]嘧啶的衍生物及其作为促炎细胞因子抑制剂的用途。

9. 发明申请

US20050004144A1 Combined use of IMPDH inhibitors with toll-like receptor agonists 审中-公开
标题翻译： IMPDH抑制剂与toll样受体激动剂的组合使用
公开(公告)号：US20050004144A1
公开(公告)日：2005-01-06
申请号：US10824833
申请日：2004-04-14
申请人： Dennis Carson , Howard Cottam , Jongdae Lee
发明人： Dennis Carson , Howard Cottam , Jongdae Lee
IPC分类号： A61K31/519 , A61K45/06 , C07D471/04 , C07D487/04 , C07D513/04 , C07D487/02 , C07D498/02
CPC分类号： A61K45/06 , A61K31/519 , C07D471/04 , C07D487/04 , C07D513/04 , A61K2300/00
摘要： The present invention provides a broad-spectrum, long-lasting, and non-toxic combination of synthetic immunostimulatory agents, which are useful for activating the immune system of a mammal and treating diseases such as cancer and autoimmune disease. These agents include TLR-ligands and ligand analogs which induce interferon production, in combination with inhibitors of inosine monophosphate dehydrogenase (IMPDH), that further enhance the induction of interferon production.
摘要翻译：本发明提供合成免疫刺激剂的广谱，持久且无毒的组合，其可用于激活哺乳动物的免疫系统并治疗疾病例如癌症和自身免疫性疾病。这些药物包括TLR-配体和诱导干扰素产生的配体类似物，与肌苷一磷酸脱氢酶（IMPDH）的抑制剂组合，进一步增强干扰素产生的诱导。

10. 发明授权

US6147123A Treatment and prevention of hepatic disorders 失效
公开(公告)号：US6147123A
公开(公告)日：2000-11-14
申请号：US274624
申请日：1999-03-23
申请人： Mario Chojkier , Dennis Carson
发明人： Mario Chojkier , Dennis Carson
IPC分类号： A61K31/05 , A61K31/355 , A61K31/522 , C07C39/04
CPC分类号： A61K31/355 , A61K31/05 , A61K31/522 , Y10S514/893 , Y10S514/894
摘要： New methods are described for the treatment of viral hepatitis C involving the administration of vitamin E and other compounds with antioxidant properties. Treatment with high doses of vitamin E is effective in treating chronic hepatitis C in patients refractory to interferon. In addition, new methods are described for the treatment of hepatic fibrosis and hepatic conditions manifesting hepatic fibrosis involving the administration of butylated hydroxytoluene and a metabolite of pentoxifylline, 1-[3-carboxypropyl]-3, 7-dimethylxanthine.

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