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1. 发明申请

US20080280903A1 Apoptosis Inhibitors 有权
标题翻译：细胞凋亡抑制剂
公开(公告)号：US20080280903A1
公开(公告)日：2008-11-13
申请号：US11885463
申请日：2006-03-10
申请人： Dennis A. Carson , Howard B. Cottam , Sylvie Barchechath , Mary Patricia Corr
发明人： Dennis A. Carson , Howard B. Cottam , Sylvie Barchechath , Mary Patricia Corr
IPC分类号： A61K31/5377 , C07D213/02 , A61K31/4439 , A61K31/44 , C07D401/02 , C07D403/02 , A61K31/497 , A61K31/4545 , A61P43/00 , C07D413/02
CPC分类号： C07D513/04 , C07D213/20 , C07D215/227
摘要： The present invention provides compounds that act as selective agents to protect against unintentional cell death or tissue damage and can relieve side effects of cancer treatment such as, for example, oral mucositis, hair loss, diarrhea due to damage to the gastrointestinal epithelium, and myelosuppression. In addition, these compounds can be used to prevent premature cell death when the cell death is caused by signals from damaged cells, for example, signals generated as the result of a traumatic incident or an ischemic episode.
摘要翻译：本发明提供了用作选择剂以防止无意的细胞死亡或组织损伤并可以减轻癌症治疗的副作用的化合物，例如口腔粘膜炎，脱发，胃肠上皮损伤引起的腹泻和骨髓抑制。此外，当细胞死亡是由受损细胞的信号引起的，例如作为创伤事件或缺血发作的结果产生的信号，这些化合物可用于防止过早的细胞死亡。

2. 发明授权

US07816352B2 Apoptosis inhibitors 有权
标题翻译：凋亡抑制剂
公开(公告)号：US07816352B2
公开(公告)日：2010-10-19
申请号：US11885463
申请日：2006-03-10
申请人： Dennis A. Carson , Howard B. Cottam , Sylvie Barchéchath , Mary Patricia Corr
发明人： Dennis A. Carson , Howard B. Cottam , Sylvie Barchéchath , Mary Patricia Corr
IPC分类号： A61K31/535 , A61K31/47 , A61K31/497 , C07D213/56 , C07D217/00 , C07D215/38
CPC分类号： C07D513/04 , C07D213/20 , C07D215/227
摘要： The present invention provides compounds that act as selective agents to protect against unintentional cell death or tissue damage and can relieve side effects of cancer treatment such as, for example, oral mucositis, hair loss, diarrhea due to damage to the gastrointestinal epithelium, and myelosuppression. In addition, these compounds can be used to prevent premature cell death when the cell death is caused by signals from damaged cells, for example, signals generated as the result of a traumatic incident or an ischemic episode.
摘要翻译：本发明提供了用作选择剂以防止无意的细胞死亡或组织损伤并可以减轻癌症治疗的副作用的化合物，例如口腔粘膜炎，脱发，胃肠上皮损伤引起的腹泻和骨髓抑制。此外，当细胞死亡是由受损细胞的信号引起的，例如作为创伤事件或缺血发作的结果产生的信号，这些化合物可用于防止过早的细胞死亡。

3. 发明授权

US07601846B2 Compounds having activity as inhibitors of apoptosis 失效
标题翻译：具有凋亡抑制剂活性的化合物
公开(公告)号：US07601846B2
公开(公告)日：2009-10-13
申请号：US11271511
申请日：2005-11-10
申请人： Howard B. Cottam , Dennis A. Carson , Sylvie Barchechath
发明人： Howard B. Cottam , Dennis A. Carson , Sylvie Barchechath
IPC分类号： C07D513/04 , A61K31/429
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.
摘要翻译：本发明提供了可以保护哺乳动物细胞免受化学疗法，照射的损伤作用或其它期望保护组织免受临床或环境压力后果的其它情况的化合物。

4. 发明授权

US07211599B2 Use of etodolac to treat hyperplasia 失效
公开(公告)号：US07211599B2
公开(公告)日：2007-05-01
申请号：US10667208
申请日：2003-09-19
申请人： Dennis A. Carson , Lorenzo M. Leoni , Mary Patricia Corr
发明人： Dennis A. Carson , Lorenzo M. Leoni , Mary Patricia Corr
IPC分类号： A61K31/40 , A61K31/56 , A61K31/50 , A61K31/18 , A61K31/12
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.

5. 发明申请

US20090324551A1 TLR AGONISTS 审中-公开
公开(公告)号：US20090324551A1
公开(公告)日：2009-12-31
申请号：US12064529
申请日：2006-08-21
申请人： Dennis A. Carson , Kenji Takabayshi , Suzanne Grimshaw , Howard B. Cottam , Michael Chan , Christina C.N. Wu
发明人： Dennis A. Carson , Kenji Takabayshi , Suzanne Grimshaw , Howard B. Cottam , Michael Chan , Christina C.N. Wu
IPC分类号： A61K45/00 , C07D473/00 , A61K31/522 , C12N1/20 , C12N7/00 , A61P35/00
CPC分类号： C07D473/16 , C07D473/18 , C07D473/24 , C07D473/34
摘要： The present invention provides for TLR agonist conjugates (compounds) and compositions, as well as methods of using them. The compounds of the invention are broad-spectrum, long-lasting, and non-toxic combination of synthetic immunostimulatory agents, which are useful for activating the immune system of a mammal, preferably a human and can help direct the pharmacophore to the receptor within the endosomes of target cells and enhance the signal transduction induced by the pharmacophore.
摘要翻译：本发明提供了TLR激动剂缀合物（化合物）和组合物，以及使用它们的方法。本发明的化合物是合成免疫刺激剂的广谱，持久和无毒组合，其可用于激活哺乳动物，优选人的免疫系统，并且可以帮助将药效团引导至受体内的受体靶细胞的内体，并增强由药效团诱导的信号转导。

6. 发明授权

US06696441B1 Inhibition of p53-induced stress response 失效
标题翻译：抑制p53诱导的应激反应
公开(公告)号：US06696441B1
公开(公告)日：2004-02-24
申请号：US09637531
申请日：2000-08-11
申请人： Howard B. Cottam , Lorenzo M. Leoni , Dennis A. Carson
发明人： Howard B. Cottam , Lorenzo M. Leoni , Dennis A. Carson
IPC分类号： A61K31425
CPC分类号： C07D513/04 , A61K31/519 , C07D487/04
摘要： The present invention provides compounds that act to suppress p53 activity in mammalian cells, and a method to effectively suppress p53 activity in the cells of a mammal subject to a stress or pathology that is ameliorated by such suppression.
摘要翻译：本发明提供了用于抑制哺乳动物细胞中p53活性的化合物，以及有效抑制经受这种抑制而改善的应激或病理学的哺乳动物细胞中p53活性的方法。

7. 发明授权

US07361680B2 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：US07361680B2
公开(公告)日：2008-04-22
申请号：US11467472
申请日：2006-08-25
申请人： Dennis A. Carson , Howard B. Cottam , Lorenzo M. Leoni
发明人： Dennis A. Carson , Howard B. Cottam , Lorenzo M. Leoni
IPC分类号： A61K31/407 , C07D471/04
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。

8. 发明授权

US07098216B2 Thiazolopyrimidines useful as TNFα inhibitors 失效
标题翻译：噻唑并嘧啶可用作TNFα抑制剂
公开(公告)号：US07098216B2
公开(公告)日：2006-08-29
申请号：US10952077
申请日：2004-09-28
申请人： Dennis A. Carson , Howard B. Cottam , Lynn Deng
发明人： Dennis A. Carson , Howard B. Cottam , Lynn Deng
IPC分类号： C07D513/04 , A61K31/519 , A61P11/06 , A61P19/02 , A61P37/06
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. 发明授权

US06930101B1 Thiazolopyrimidines useful as TNFα inhibitors 失效
标题翻译：噻唑并嘧啶可用作TNFα抑制剂
公开(公告)号：US06930101B1
公开(公告)日：2005-08-16
申请号：US09313048
申请日：1999-05-17
申请人： Dennis A. Carson , Howard B. Cottam , Lynn Deng
发明人： Dennis A. Carson , Howard B. 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 , A61P11/06
CPC分类号： C07D513/04
摘要： The invention provides derivatives of thiazolo[4,5-dl]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。

10. 发明授权

US06214571B1 Method for inhibiting adenylosuccinate synthetase activity in malignant methylthioadenosine phosphorylase deficient cells 失效
标题翻译：恶性甲基硫代腺苷磷酸化酶缺陷型细胞中腺苷酸琥珀酸合成酶抑制活性的方法
公开(公告)号：US06214571B1
公开(公告)日：2001-04-10
申请号：US09199137
申请日：1998-11-24
申请人： Carlos J. Carrera , Dennis A. Carson , Howard B. Cottam , Tsutomu Nobori
发明人： Carlos J. Carrera , Dennis A. Carson , Howard B. Cottam , Tsutomu Nobori
IPC分类号： C12Q134
CPC分类号： C12Q1/6886 , A61K31/198 , C12N9/1077
摘要： An in vivo method for depleting mammalian cells of adenosine 5′-monophosphate (AMP) useful in the treatment of certain cancers is provided. According to the method, a population of cells is obtained from a host and assayed for loss of methylthioadenosine phosphorylase (MTAse) activity. MTAse catabolizes methylthioadenosine to adenine for endogenous salvage incorporation into the intracellular AMP pool. The preferred method for assaying loss of MTAse activity is a hybridization technique for detection of a homozygous loss of the gene which encodes MTAse. Hosts having MTAse deficient tumors are treated with a therapeutically effective amount of an agent which inhibits the activity of adenylsuccinate synthetase, which converts inosine 5-monophosphate to AMP, thus depleting the tumor cells of substrates for de novo AMP production. L-alanosine is the preferred ASS inhibitory agent for use in the method of the invention.
摘要翻译：提供了用于消除用于治疗某些癌症的腺苷5'-单磷酸（AMP）的哺乳动物细胞的体内方法。根据该方法，从宿主获得细胞群并测定甲硫基腺苷磷酸化酶（MTAse）活性的损失。 MTAs将甲基硫代腺苷分解为腺嘌呤，用于内源性补救并入细胞内AMP库。用于测定MTAse活性丧失的优选方法是用于检测编码MTAse的基因的纯合丢失的杂交技术。具有MTAse缺陷肿瘤的宿主用治疗有效量的抑制腺苷酸琥珀酸合成酶活性的药物进行治疗，其将5-单磷酸肌苷转化为AMP，从而消耗底物的肿瘤细胞用于从头AMP产生。 L-肌氨酸是用于本发明方法的优选的ASS抑制剂。

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