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21.发明授权Medium-chain length fatty acids, glycerides and analogues as neutrophil survival and activation factors 有权中链长度脂肪酸，甘油酯和类似物作为嗜中性粒细胞存活和激活因子公开(公告)号：US07745488B2
公开(公告)日：2010-06-29
申请号：US10475266
申请日：2002-04-18
申请人： Lyne Gagnon , Jean Barabe , Pierre Laurin , Christopher Penney , Boulos Zacharie
发明人： Lyne Gagnon , Jean Barabe , Pierre Laurin , Christopher Penney , Boulos Zacharie
IPC分类号： A61K31/255 , A61K31/225
CPC分类号： C07C237/22 , A61K31/18 , A61K31/194 , A61K31/20 , A61K31/23 , A61K31/255 , A61K31/7024 , A61K38/193 , A61K38/2013 , A61K38/2086 , A61K45/06 , C07B2200/11 , C07C233/18 , C07C233/47 , C07C235/06 , C07C235/08 , C11C3/003 , C11C3/02 , C40B40/00 , Y02A50/387 , Y02A50/483 , A61K2300/00
摘要： A composition and method for promoting neutrophil survival and activation such as the treatment of neutropenia arising as an undesirable side effect of chemotherapy and radiation therapy. A composition containing medium-chain fatty acids, such as Capri acid or caprylic acid, or salts or triglycerides thereof, or mono- or diglycerides or other analogues thereof or medium-chain triglycerides (MCT) is administered to a human or animal needing treatment in an amount sufficient to reduce or eliminate neutropenia. The composition is administered in an amount effective to treat the disorder. The methods are also useful in the management of bone narrow transplantation and in the treatment of various neutropenic diseases.
摘要翻译： 用于促进嗜中性粒细胞存活和激活的组合物和方法，例如治疗作为化疗和放射治疗的不良副作用引起的中性粒细胞减少。 将含有中链脂肪酸的组合物，例如Capri酸或辛酸，或其盐或甘油三酯，或甘油单酯或甘油二酯或其它类似物或中链甘油三酸酯（MCT）给予需要治疗的人或动物 足以减少或消除中性粒细胞减少的量。 组合物以有效治疗病症的量给药。 该方法也可用于骨狭窄移植的治疗和各种嗜中性粒细胞减少症的治疗。
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22.发明申请Triazine Derivatives, Compositions Containing Such Derivatives, and Methods of Treatment of Cancer and Autoimmune Diseases Using Such Derivatives 有权三嗪衍生物，含有此类衍生物的组合物，以及使用此类衍生物治疗癌症和自身免疫性疾病的方法公开(公告)号：US20100129350A1
公开(公告)日：2010-05-27
申请号：US12598273
申请日：2008-04-25
申请人： Boulos Zacharie , Christopher Penney , Lyne Gagnon , Brigitte Grouix , Lilianne Geerts , Shaun D. Abbott
发明人： Boulos Zacharie , Christopher Penney , Lyne Gagnon , Brigitte Grouix , Lilianne Geerts , Shaun D. Abbott
IPC分类号： A61K31/53 , C07D251/54 , A61K31/704 , A61K31/675 , A61K38/00 , A61K31/7048 , A61K31/7068 , A61K33/24 , A61K39/395 , A61P35/00 , A61P37/00
CPC分类号： C07D251/18 , C07D251/70
摘要： We describe compounds of the following general formula (I): wherein X is fluorine or chlorine; Y is oxygen, sulfur, or an amino group; R is an amino, hydroxyl, sulfonamide, or carboxamide group or an N-monomethyl or N-dimethyl analog thereof; m is an integer from 2 to 6, and n is an integer from 0 to 2. The compounds may be used for treating certain cancers and autoimmune diseases.
摘要翻译： 我们描述以下通式（I）的化合物：其中X是氟或氯; Y是氧，硫或氨基; R是氨基，羟基，磺酰胺或羧酰胺基团或其N-甲基或N-二甲基类似物; m为2〜6的整数，n为0〜2的整数。化合物可用于治疗某些癌症和自身免疫性疾病。
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23.发明申请Substituted Purinyl Derivatives With Immunomodulator And Chemoprotective Activity And Use Alone Or With Medium-Chain Length Fatty Acids Or Glycerides 审中-公开具有免疫调节剂和化学保护活性和单独使用的中链链脂肪酸或甘油酯的取代的紫杉基衍生物公开(公告)号：US20080090848A1
公开(公告)日：2008-04-17
申请号：US11661108
申请日：2005-09-02
申请人： Christopher Penney , Boulos Zacharie , Jean Barabe , Pierre Laurin , Lyne Gagnon
发明人： Christopher Penney , Boulos Zacharie , Jean Barabe , Pierre Laurin , Lyne Gagnon
CPC分类号： A61K31/20 , A61K31/23 , A61K31/417 , A61K31/52 , A61K2300/00
摘要： The present invention describes new biological activities of immunomodulating 6-substituted purinyl compounds which make them particularly useful during the treatment of cancer. Collectively, these new biological activities make these purinyl compounds useful chemoprotective agents for the treatment of myelosuppression which is associated with cancer chemotherapy and/or radiotherapy. This chemoprotective activity is in addition to the immunomodulating and subsequent anticancer activity displayed by these compounds. The chemoprotective usefulness of these compounds is further enhanced by the use of medium-chain fatty acids or salts or triglycerides or mono- or diglycerides in combination with the 6-substituted purinyl compounds of this invention.
摘要翻译： 本发明描述了使其在癌症治疗期间特别有用的免疫调节6-取代嘌呤基化合物的新生物活性。 总的来说，这些新的生物活性使得这些嘌呤基化合物可用于治疗与癌症化学疗法和/或放射疗法相关的骨髓抑制的化学保护剂。 这种化学保护活性是由这些化合物显示的免疫调节和随后的抗癌活性的补充。 通过使用中链脂肪酸或甘油三酯或甘油单酯或甘油二酯与本发明的6-取代的嘌呤基化合物的组合，这些化合物的化学保护作用进一步增强。
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公开(公告)号：US5688771A
公开(公告)日：1997-11-18
申请号：US313304
申请日：1994-10-03
IPC分类号： A61K38/00 , A61K31/52 , A61P31/12 , C07C327/42 , C07K1/113 , C07K5/02 , C07K5/037 , C07K5/06 , C07K5/062 , C07K5/065 , C07K5/068 , C07K5/072 , C07K5/087
CPC分类号： C07K5/0812 , C07C327/42 , C07K5/0215 , C07K5/06026 , C07K5/06052 , C07K5/0606 , C07K5/06069 , C07K5/06078 , C07K5/06086 , C07K5/06104 , A61K38/00
摘要： New, small and structurally simple immunomodulating oligopeptides are disclosed. The oligopeptides of this invention possess a long, lipophilic alkyl chain. These immunomodulating oligopeptides can be used in conjunction with anti-viral or anti-cancer agents in the treatment of human and animal diseases. Processes for the syntheses of immunomodulating chemicals are also disclosed.
摘要翻译： PCT No.PCT / CA93 / 00144 Sec。 371日期：1994年10月3日 102（e）日期1994年10月3日PCT提交1993年4月2日PCT公布。 公开号WO93 / 20100 PCT 日期：1993年10月14日新的，小型和结构简单的免疫调节寡肽被公开。 本发明的寡肽具有长的亲脂性烷基链。 这些免疫调节寡肽可以与抗病毒剂或抗癌剂联合用于治疗人和动物疾病。 还公开了免疫调节化学品的合成方法。
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公开(公告)号：US5371185A
公开(公告)日：1994-12-06
申请号：US839609
申请日：1992-02-21
申请人： Bernard Belleau , Denis Brillon , Gilles Sauve , Boulos Zacharie
发明人： Bernard Belleau , Denis Brillon , Gilles Sauve , Boulos Zacharie
IPC分类号： C07D209/14 , A61K38/00 , C07D233/64 , C07D235/26 , C07D403/06 , C07D403/12 , C07K1/06 , C07K1/113 , C07K5/02 , C07K5/06 , C07K5/08 , C07K5/09 , C07K5/093 , C07K5/10 , C07K5/103 , C07K14/66 , C07K7/08 , C07K7/06
CPC分类号： C07D403/12 , C07D235/26 , C07K14/66 , C07K5/02 , C07K5/0815 , C07K5/0819 , C07K5/1013 , A61K38/00
摘要： This invention relates to 1-amino thioacylbenzimidazoyl-2-one derivatives having the formula: ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3 are defined herein. These compounds are useful as thioacylating reagents. This invention also relates to a process for producing cyclic and linear thiopeptides using the thioacylating reagents of this invention. This invention further relates to intermediate anilide compounds, which are produced by reacting an ortho phenylene diamine with an amino acid chain or peptide. This invention also relates to intermediate thioanilide compounds, which are produced by thionating the intermediate anilide compounds. This invention further relates to a process for producing the thioacylating reagents of this invention by cyclizing the intermediate thioanilide compounds.
摘要翻译： 本发明涉及具有下式的1-氨基硫代酰基苯并咪唑-2-酮衍生物：其中R 1，R 2和R 3在本文中定义。 这些化合物可用作硫代酰化试剂。 本发明还涉及使用本发明的硫代酰化试剂制备环状和线性硫代肽的方法。 本发明还涉及通过使邻苯二胺与氨基酸链或肽反应制备的中间体酰苯胺化合物。 本发明还涉及通过硫化中间体酰苯胺化合物而制备的中间体硫代苯胺化合物。 本发明还涉及通过使中间体硫代苯胺化合物环化来制备本发明的硫代酰化试剂的方法。
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公开(公告)号：US5138061A
公开(公告)日：1992-08-11
申请号：US389852
申请日：1989-08-04
IPC分类号： C07D209/14 , A61K38/00 , C07D233/64 , C07D235/26 , C07D403/06 , C07D403/12 , C07K1/06 , C07K1/113 , C07K5/02 , C07K5/06 , C07K5/08 , C07K5/09 , C07K5/093 , C07K5/10 , C07K5/103 , C07K14/66
CPC分类号： C07D403/12 , C07D235/26 , C07K14/66 , C07K5/02 , C07K5/0815 , C07K5/0819 , C07K5/1013 , A61K38/00
摘要： Thioacylating reagents are provided for the introduction of thioamide bonds into growing peptides represented by the structure: ##STR1## where the substituents are disclosed herein. Intermediate precursors for preparing these thioacylating reagents are also provided. A process for preparing the thioacylating reagents and the intermediate precursors is further provided.
摘要翻译： 提供硫酰胺化试剂以将硫代酰胺键引入由以下结构表示的生长肽中：其中本文公开了取代基。 还提供了制备这些硫代酰化试剂的中间体前体。 还提供了制备硫代酰化试剂和中间体前体的方法。
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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：US08927765B2
公开(公告)日：2015-01-06
申请号：US13289592
申请日：2011-11-04
申请人： Boulos Zacharie , Christopher Penney , Lyne Gagnon , Jean-François Bienvenu , Valérie Perron , Brigitte Grouix
发明人： Boulos Zacharie , Christopher Penney , Lyne Gagnon , Jean-François Bienvenu , Valérie Perron , Brigitte Grouix
IPC分类号： C07C53/134 , C07C57/30 , C07C61/39 , C07D257/04 , C07C59/48 , C07D213/55 , C07C57/58 , C07C59/52
CPC分类号： C07C57/58 , A61K31/19 , A61K31/192 , C07C57/30 , C07C57/42 , C07C59/48 , C07C59/52 , C07C61/39 , C07D213/55 , C07D257/04
摘要： The present invention relates to substituted aromatic compounds of Formula I and their pharmaceutical uses. Particular aspects of the invention relate to the use of those compounds in the prevention and/or treatment of various diseases and conditions in subjects, including the prevention or treatment of (i) blood disorders, (ii) renal disorders, a nephropathies, or renal disorder complications; (iii) inflammatory-related diseases; and/or (iv) oxidative stress related disorders.
摘要翻译： 本发明涉及取代的式I的芳族化合物及其药物用途。 本发明的特定方面涉及这些化合物在预防和/或治疗受试者的各种疾病和病症中的用途，包括预防或治疗（i）血液病症，（ii）肾病，肾病或肾脏 疾病并发症; （iii）炎性相关疾病; 和/或（iv）氧化应激相关疾病。
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29.发明授权Medium-chain length fatty acids, glycerides and analogues as neutrophil survival and activation factors 有权中链长度脂肪酸，甘油酯和类似物作为嗜中性粒细胞存活和激活因子公开(公告)号：US08487001B2
公开(公告)日：2013-07-16
申请号：US12814028
申请日：2010-06-11
申请人： Lyne Gagnon , Jean Barabe , Pierre Laurin , Christopher Penney , Boulos Zacharie
发明人： Lyne Gagnon , Jean Barabe , Pierre Laurin , Christopher Penney , Boulos Zacharie
IPC分类号： A61K31/7024 , A61K31/23 , A61K31/22 , A61K31/198 , C07C235/06 , C07C235/12 , A61P7/00
CPC分类号： C07C237/22 , A61K31/18 , A61K31/194 , A61K31/20 , A61K31/23 , A61K31/255 , A61K31/7024 , A61K38/193 , A61K38/2013 , A61K38/2086 , A61K45/06 , C07B2200/11 , C07C233/18 , C07C233/47 , C07C235/06 , C07C235/08 , C11C3/003 , C11C3/02 , C40B40/00 , Y02A50/387 , Y02A50/483 , A61K2300/00
摘要： A composition and method for promoting neutrophil survival and activation such as the treatment of neutropenia arising as an undesirable side effect of chemotherapy and radiation therapy. A composition containing medium-chain fatty acids, such as Capri acid or caprylic acid, or salts or triglycerides thereof, or mono- or diglycerides or other analogues thereof or medium-chain triglycerides (MCT) is administered to a human or animal needing treatment in an amount sufficient to reduce or eliminate neutropenia. The composition is administered in an amount effective to treat the disorder. The methods are also useful in the management of bone narrow transplantation and in the treatment of various neutropenic diseases.
摘要翻译： 用于促进嗜中性粒细胞存活和激活的组合物和方法，例如治疗作为化疗和放射治疗的不良副作用引起的中性粒细胞减少。 将含有中链脂肪酸的组合物，例如Capri酸或辛酸，或其盐或甘油三酯，或甘油单酯或甘油二酯或其它类似物或中链甘油三酸酯（MCT）给予需要治疗的人或动物 足以减少或消除中性粒细胞减少的量。 组合物以有效治疗病症的量给药。 该方法也可用于骨狭窄移植的治疗和各种嗜中性粒细胞减少症的治疗。
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30.发明授权Triazine derivatives, compositions containing such derivatives, and methods of treatment of cancer and autoimmune diseases using such derivatives 有权三嗪衍生物，含有这些衍生物的组合物，以及使用这些衍生物治疗癌症和自身免疫性疾病的方法公开(公告)号：US08258295B2
公开(公告)日：2012-09-04
申请号：US12598273
申请日：2008-04-25
申请人： Boulos Zacharie , Christopher Penney , Lyne Gagnon , Brigitte Grouix , Lilianne Geerts , Shaun D. Abbott
发明人： Boulos Zacharie , Christopher Penney , Lyne Gagnon , Brigitte Grouix , Lilianne Geerts , Shaun D. Abbott
CPC分类号： C07D251/18 , C07D251/70
摘要： We describe compounds of the following general formula (I): wherein X is fluorine or chlorine; Y is oxygen, sulfur, or an amino group; R is an amino, hydroxyl, sulfonamide, or carboxamide group or an N-monomethyl or N-dimethyl analog thereof; m is an integer from 2 to 6, and n is an integer from 0 to 2. The compounds may be used for treating certain cancers and autoimmune diseases.
摘要翻译： 我们描述以下通式（I）的化合物：其中X是氟或氯; Y是氧，硫或氨基; R是氨基，羟基，磺酰胺或羧酰胺基团或其N-甲基或N-二甲基类似物; m为2〜6的整数，n为0〜2的整数。化合物可用于治疗某些癌症和自身免疫性疾病。
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