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公开(公告)号：US06630488B1
公开(公告)日：2003-10-07
申请号：US09805780
申请日：2001-03-20
申请人： Serge Lamothe , Boulos Zacharie , Giorgio Attardo , Denis Labrecque , Marc Courchesne , Guy Falardeau , Rabindra Rej , Shaun Abbott
发明人： Serge Lamothe , Boulos Zacharie , Giorgio Attardo , Denis Labrecque , Marc Courchesne , Guy Falardeau , Rabindra Rej , Shaun Abbott
IPC分类号： C07D45502
CPC分类号： C07D455/02
摘要： The present invention is directed towards novel compounds that are effective inhibitors of integrins, particularly &agr;IIb&bgr;3 or &agr;v integrins such as &agr;v&bgr;3 and &agr;v&bgr;5. One embodiment of the present invention comprises a compound of formula (I) or formula (II) or a pharmaceutically acceptable salt, solvate, or metabolic precursor thereof. R1, R2, R3, and R4 are defined herein.
摘要翻译： 本发明涉及作为整合素的有效抑制剂的新化合物，特别是αIIbbeta3或alphav整联蛋白，例如alphavbeta3和alphavbeta5。 本发明的一个实施方案包括式（I）或式（II）化合物或其药学上可接受的盐，溶剂合物或代谢前体。 R1，R2，R3和R4在本文中定义。
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公开(公告)号：US06274620B1
公开(公告)日：2001-08-14
申请号：US09588574
申请日：2000-06-07
申请人： Denis Labrecque , Giorgio Attardo , Monica Bubenik , Laval Chan , Sylvie Charron , Réal Denis , Guy Falardeau , Serge Lamothe , Patrice Préville , Boulos Zacharie
发明人： Denis Labrecque , Giorgio Attardo , Monica Bubenik , Laval Chan , Sylvie Charron , Réal Denis , Guy Falardeau , Serge Lamothe , Patrice Préville , Boulos Zacharie
IPC分类号： A61K3138
CPC分类号： C07D333/34 , C07D307/64 , C07D307/68 , C07D333/38
摘要： The present invention comprises compounds that are effective inhibitors of integrins, particularly &agr;v&bgr;3 and &agr;v&bgr;5 integrins. Particularly, the compounds are of formula I and pharmaceutically acceptable salts thereof wherein X,Y1 W, R1 to R5, A and B are defined according to the disclosure herein.
摘要翻译： 本发明包括有效的整联蛋白抑制剂，特别是阿尔法博亚3和阿尔法肽5整合素的化合物。 特别地，所述化合物具有式I化合物及其药学上可接受的盐，其中X，Y1W，R1至R5，A和B根据本文的公开内容定义。
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公开(公告)号：US20050256034A1
公开(公告)日：2005-11-17
申请号：US11149193
申请日：2005-06-10
申请人： Giorgio Attardo , Boulos Zacharie , Rabindra Rej , Jean-Francois Lavallee , Louis Vaillancourt , Real Denis , Sophie Levesque
发明人： Giorgio Attardo , Boulos Zacharie , Rabindra Rej , Jean-Francois Lavallee , Louis Vaillancourt , Real Denis , Sophie Levesque
IPC分类号： A61K31/513 , A61K31/675 , A61K31/7068 , A61K38/00 , A61P35/00 , A61P35/02 , A61P43/00 , C07D405/04 , C07D405/14 , C07D473/18 , C07F9/655 , C07F9/6558 , C07F9/6561 , C07K5/06 , C07K5/08 , C07K5/10 , C07K7/06 , A61K38/16
CPC分类号： C07D405/04 , C07D473/18 , C07F9/65515 , C07F9/65586 , C07F9/65616
摘要： Dioxolane analogs of the following formula: wherein R1 and R2 are defined herein, are useful in the treatment of cancer. For example, the compounds can be used to treat patients with cancer in which the cancer cells are deficient in nucleoside or nucleoside base transporters.
摘要翻译： 下式的二氧杂环戊烷类似物：其中R1和R2如本文所定义，可用于治疗癌症。 例如，这些化合物可用于治疗癌细胞中核苷或核苷碱基转运蛋白缺乏的癌症患者。
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公开(公告)号：US5994361A
公开(公告)日：1999-11-30
申请号：US474073
申请日：1995-06-07
申请人： Christopher Penney , Boulos Zacharie , Lyne Gagnon , Giorgio Attardo , Timothy P. Connolly , Yves St-Denis , Salam Kadhim
发明人： Christopher Penney , Boulos Zacharie , Lyne Gagnon , Giorgio Attardo , Timothy P. Connolly , Yves St-Denis , Salam Kadhim
IPC分类号： C07D473/40 , A61K31/52 , A61K38/00 , A61K38/04 , A61P35/00 , A61P37/00 , A61P37/02 , A61P37/04 , C07D473/00 , C07D473/02 , C07D473/34 , C07K5/04 , C07K5/083 , C07D473/30
CPC分类号： A61K31/7052 , A61K31/52 , C07D473/00 , C07D473/34 , C07K5/0808 , A61K38/00
摘要： The present invention comprises a compound of formula I: ##STR1## R.sub.1 of Formula I is substituted amino represented by formula NR.sup.5 R.sup.6 wherein R.sup.5 and R.sup.6 are independently selected from the group consisting of hydrogen, C.sub.1-4 alkyl, and unsubstituted amino with the proviso that R.sup.5 and R.sup.6 are not both hydrogen, and further that R.sup.5 and R.sup.6 are not both amino. R.sub.2 and R.sub.3 of Formula I are independently selected from the group consisting of hydrogen; C.sub.1-4 alkyl; amino; substituted or unsubstituted thiol; and halogen. Moreover, R.sub.4 of Formula I is represented by the formula R.sup.12 -X.sup.12 wherein R.sup.12 is a saturated or unsaturated linear hydrocarbon chain of 5-20 carbons optionally containing one or more interruptions within the chain by a heteroatom, and optionally substituted with one or more .dbd.O, or .dbd.S. Finally, X.sup.12 is selected from the group consisting of hydroxy, an aminoalkyl group, and a known amino acid bound by its .alpha.-amino group.
摘要翻译： 本发明包括式I的化合物：式I的R 1是由式NR 5 R 6表示的取代的氨基，其中R 5和R 6独立地选自氢，C 1-4烷基和未被取代的氨基，条件是R 5和R 6 不是氢，而且R5和R6不是两个氨基。 式I的R 2和R 3独立地选自氢; C 1-4烷基; 氨基; 取代或未取代的硫醇; 和卤素。 此外，式I的R 4由式R 12 -X 12表示，其中R 12是5-20个碳的饱和或不饱和直链烃链，任选地在该链内通过杂原子一个或多个中断，并且任选地被一个或多个= O或= S。 最后，X 12选自羟基，氨基烷基和被其α-氨基结合的已知氨基酸。
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公开(公告)号：US20130225681A1
公开(公告)日：2013-08-29
申请号：US13882363
申请日：2011-10-26
申请人： Boulos Zacharie , Christopher Penney , Shaun Abbott , Lyne Gagnon , Brigette Grouix , Pierre Laurin
发明人： Boulos Zacharie , Christopher Penney , Shaun Abbott , Lyne Gagnon , Brigette Grouix , Pierre Laurin
IPC分类号： C07C59/90 , C07C229/18 , C07C59/84 , C07C69/92 , C07C59/68 , C07C62/38 , C07C323/52
CPC分类号： C07C59/90 , A61K31/192 , A61K31/196 , A61K31/222 , A61K31/235 , C07C59/68 , C07C59/84 , C07C62/38 , C07C65/32 , C07C69/92 , C07C217/84 , C07C225/22 , C07C229/18 , C07C323/20 , C07C323/52 , C07C323/62 , C07C2602/08
摘要： Phenylketone carboxylate compounds of Formula I, wherein n=2-6; R═C(0); —OC(O)— or —CH(OH)—; A is (CH2)mCOOH, W(CH2)mCOOH or YCH(COOH)((CH2)pCH3) when B is Ft B is (CH2)mCOOH, W(CH2)mCOOH or YCH(COOH)((CH2)pCH3) when A is Ft or A and B form a 5-7 membered cycloalkyl substituted with COOFt W=0, S or NFt Y=0,S,NH or CH2; m=0-2; p=1-7; have been prepared. These compounds and their pharmaceutically acceptable salts have beneficial therapeutic effects to prevent or treat a condition related to (l) blood disorders, (ii) inflammation related diseases, (iii) renal disorders and/or renal disorders complications, or (iv) fibrosis-related organ dysfunction.
摘要翻译： 式I的苯甲酮羧酸酯化合物，其中n = 2-6; R = C（0）; -OC（O） - 或-CH（OH） - ; 当B是Ft B是（CH2）mCOOH，W（CH2）mCOOH或YCH（COOH）（（CH2）pCH3）时，A是（CH2）mCOOH，W（CH2）mCOOH或YCH 当A为Ft或A和B形成被COOFt W = 0取代的5-7元环烷基时，S或NFt Y = 0，S，NH或CH 2; m = 0-2; p = 1-7; 已经准备好了 这些化合物及其药学上可接受的盐具有有益的治疗效果，以预防或治疗与（l）血液病症有关的病症，（ii）炎症相关疾病，（iii）肾脏疾病和/或肾脏疾病并发症，或（iv）纤维化 - 相关器官功能障碍。
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公开(公告)号：US20070149528A1
公开(公告)日：2007-06-28
申请号：US10580237
申请日：2004-11-22
申请人： Christopher Penney , Boulos Zacharie , Shaun Abbott , Jean-Francois Bienvenu , Alan Cameron , Jean-Simon Duceppe , Abdallah Ezzitouni , Daniel Fortin , Karine Houde , Nancia Moreau , Nicole Wilb , Brigitte Grouix , Lyne Gagnon
发明人： Christopher Penney , Boulos Zacharie , Shaun Abbott , Jean-Francois Bienvenu , Alan Cameron , Jean-Simon Duceppe , Abdallah Ezzitouni , Daniel Fortin , Karine Houde , Nancia Moreau , Nicole Wilb , Brigitte Grouix , Lyne Gagnon
IPC分类号： A61K31/53 , C07D403/14 , C07D403/02
CPC分类号： C07D401/14 , C07D251/70
摘要： Compounds containing two mono- or disubstituted triazine rings covalently linked by an organic linker, but not linked directly to each other, may be used to treat autoimmune diseases. Autoimmune diseases which are amenable to treatment with compounds of this invention include rheumatoid arthritis, systemic lupus erythematosus (SLE), idiopathic (immune) thrombocytopenia (ITP), glomerulonephritis and vasculitis. The present invention also relates to reducing drug toxicity which often accompanies traditional therapies for autoimmune diseases. The compounds may also be used to bind antibody in vitro or ex vivo.
摘要翻译： 含有通过有机接头共价连接但不直接相互连接的两个单取代或二取代的三嗪环的化合物可用于治疗自身免疫性疾病。 适合用本发明化合物治疗的自身免疫性疾病包括类风湿性关节炎，系统性红斑狼疮（SLE），特发性（免疫性）血小板减少症（ITP），肾小球性肾炎和血管炎。 本发明还涉及通常伴随着自身免疫疾病的传统疗法的药物毒性的降低。 该化合物也可用于体外或离体结合抗体。
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公开(公告)号：US09475750B2
公开(公告)日：2016-10-25
申请号：US13882363
申请日：2011-10-26
申请人： Boulos Zacharie , Christopher Penney , Shaun Abbott , Lyne Gagnon , Brigitte Grouix , Pierre Laurin , Jean-François Bienvenu
发明人： Boulos Zacharie , Christopher Penney , Shaun Abbott , Lyne Gagnon , Brigitte Grouix , Pierre Laurin , Jean-François Bienvenu
IPC分类号： C07C59/90 , C07C62/38 , C07C65/32 , C07C69/92 , C07C217/84 , C07C225/22 , C07C229/18 , C07C323/20 , C07C323/52 , C07C323/62 , A61K31/192 , A61K31/196 , A61K31/222 , A61K31/235 , C07C59/68 , C07C59/84
CPC分类号： C07C59/90 , A61K31/192 , A61K31/196 , A61K31/222 , A61K31/235 , C07C59/68 , C07C59/84 , C07C62/38 , C07C65/32 , C07C69/92 , C07C217/84 , C07C225/22 , C07C229/18 , C07C323/20 , C07C323/52 , C07C323/62 , C07C2602/08
摘要： Phenylketone carboxylate compounds of Formula I, wherein n=2-6; R═C(0); —OC(O)— or —CH(OH)—; A is (CH2)mCOOH, W(CH2)mCOOH or YCH(COOH)((CH2)pCH3) when B is Ft B is (CH2)mCOOH, W(CH2)mCOOH or YCH(COOH)((CH2)pCH3) when A is Ft or A and B form a 5-7 membered cycloalkyl substituted with COOFt W=0, S or NFt Y=0,S,NH or CH2; m=0-2; p=1-7; have been prepared. These compounds and their pharmaceutically acceptable salts have beneficial therapeutic effects to prevent or treat a condition related to (l) blood disorders, (ii) inflammation related diseases, (iii) renal disorders and/or renal disorders complications, or (iv) fibrosis-related organ dysfunction.
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公开(公告)号：US20130217645A1
公开(公告)日：2013-08-22
申请号：US13882355
申请日：2011-10-26
申请人： Lyne Gagnon , Brigitte Grouix , Lilianne Geerts , Pierre Laurin , Christopher Penney , Boulos Zacharie
发明人： Lyne Gagnon , Brigitte Grouix , Lilianne Geerts , Pierre Laurin , Christopher Penney , Boulos Zacharie
IPC分类号： A61K31/192 , C07C57/48 , C07C59/54 , C07C229/42 , A61K31/196 , A61K31/675 , C07C229/18 , C07C323/52 , C07C62/20 , A61K31/7068 , A61K31/513 , C07C57/46 , C07C59/84
CPC分类号： A61K31/192 , A61K31/196 , A61K31/22 , A61K31/513 , A61K31/675 , A61K31/7068 , C07C57/46 , C07C57/48 , C07C59/54 , C07C59/84 , C07C62/20 , C07C229/18 , C07C229/42 , C07C323/52
摘要： New uses for phenylketone carboxylate compounds and substituted aromatic compounds of Formula I, Formula I.1, Formula I.2, Formula IA, Formula IB, Formula IC and Formula II and their pharmaceutical acceptable salts for the treatment of cancer. The use of a combination of two of these compounds is described and the use of the combination of one of these compounds with an anticancer agent such as decarbazine, doxorubicin, daunorubicin, cyclophosphamide, busulfex, busulfan, vinblastine, vincristine, bleomycin, etoposide, topotecan, irinotecan, taxotere, taxol, 5-fluorouracil, methotrexate, gemcitabine, cisplatin, carboplatin and chlorambucil.
摘要翻译： 苯甲酮羧酸酯化合物和式I，式I.1，式I.2，式IA，式IB，式IC和式II的取代芳族化合物及其用于治疗癌症的药学上可接受的盐的新用途。 描述了这些化合物中的两种的组合的使用，并且使用这些化合物之一与抗癌剂如脱巴嗪，多柔比星，柔红霉素，环磷酰胺，总胆固醇，白消安，长春花碱，长春新碱，博来霉素，依托泊苷，拓扑替康 ，伊立替康，泰索帝，紫杉醇，5-氟尿嘧啶，甲氨蝶呤，吉西他滨，顺铂，卡铂和苯丁酸氮芥。
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9.发明申请公开(公告)号：US20090075867A1
公开(公告)日：2009-03-19
申请号：US11919984
申请日：2006-05-19
申请人： Lyne Gagnon , Boulos Zacharie , Christopher Penney
发明人： Lyne Gagnon , Boulos Zacharie , Christopher Penney
IPC分类号： A61K31/53 , A61P35/00 , A61K31/704 , A61K31/675 , A61K38/00 , A61K31/7048 , A61K31/7068
CPC分类号： A61K47/10 , A61K9/0019 , A61K31/53 , A61K31/675 , A61K38/2013 , A61K45/06 , A61K47/18 , A61K2300/00
摘要： Compounds useful in the treatment of metastatic melanoma and other cancers containing a triazine ring scaffold are described. These compounds may be classified into two groups: (1) two disubstituted triazine rings are covalently linked by an organic linker to each other and (2) one trisubstituted triazine ring.
摘要翻译： 描述了可用于治疗转移性黑素瘤和含有三嗪环支架的其它癌症的化合物。 这些化合物可以分为两类：（1）两个二取代的三嗪环通过有机连接体彼此共价连接，和（2）一个三取代的三嗪环。
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公开(公告)号：US20070027343A1
公开(公告)日：2007-02-01
申请号：US10565762
申请日：2004-07-23
IPC分类号： C07C53/126
CPC分类号： C07C51/412 , C07C53/126
摘要： A process for the preparation of metal salts of a medium-chain length monocarboxylic fatty acid comprises reacting the precursor free fatty acid, dissolved in a suitable solvent, with the appropriate metal salt. The process uses a relatively high concentration of free fatty acid as a soluble reactant and produces metal fatty acid salts at high purity and high yield at a reasonable cost.
摘要翻译： 制备中链长度单羧酸脂肪酸的金属盐的方法包括使溶解在合适溶剂中的前体游离脂肪酸与合适的金属盐反应。 该方法使用相对高浓度的游离脂肪酸作为可溶性反应物，以合理的成本产生高纯度和高收率的金属脂肪酸盐。
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