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21. 发明申请

US20080090848A1 Substituted Purinyl Derivatives With Immunomodulator And Chemoprotective Activity And Use Alone Or With Medium-Chain Length Fatty Acids Or Glycerides 审中-公开
标题翻译：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
IPC分类号： A61K31/52 , A61P35/00 , A61P39/00
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。

22. 发明授权

US5994361A Substituted purinyl derivatives with immunomodulating activity 失效
标题翻译：具有免疫调节活性的取代的嘌呤基衍生物
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。

23. 发明申请

US20100279959A1 Medium-Chain Length Fatty Acids, Glycerides and Analogues as Neutrophil Survival and Activation Factors 有权
标题翻译：中链长度脂肪酸，甘油酯和类似物作为中性粒细胞存活和激活因子
公开(公告)号：US20100279959A1
公开(公告)日：2010-11-04
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。

24. 发明授权

US08487001B2 Medium-chain length fatty acids, glycerides and analogues as neutrophil survival and activation factors 有权
标题翻译：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。

25. 发明申请

US20060128800A1 Medium-chain length fatty acids, glycerides and analogues as stimulators of erythropoiesis 有权
标题翻译：中链长度脂肪酸，甘油酯和类似物作为红细胞生成的刺激剂
公开(公告)号：US20060128800A1
公开(公告)日：2006-06-15
申请号：US10544350
申请日：2004-02-06
申请人： Christopher Penney , Lyne Gagnon , Pierre Laurin , Boulos Zacharie
发明人： Christopher Penney , Lyne Gagnon , Pierre Laurin , Boulos Zacharie
IPC分类号： A61K31/255 , A61K31/225
CPC分类号： A61K31/20 , A61K31/23 , A61K45/06 , A61K47/14 , A61K2300/00
摘要： Use of a composition comprising a compound of any of formulae I, II, Ila, III and Illa; or a combination thereof wherein each R1 is independently C7-11 alkyl; A and B are independently H or CO—R1; R2 is H or C1-4 alkyl; M is a metal monocation (k=1) or dication (k=2); Y is 0 or NH; and Z is 0, NH, CH2O or a bond; for the manufacture of a medicament for stimulating erythropoiesis. Preferably, the composition further comprises human erythroporietin.
摘要翻译：使用包含式I，II，IIa，III和IIIa中任何一种的化合物的组合物; 或其组合，其中每个R 1独立地为C 11-11烷基; A和B独立地为H或CO-R 1; R 2是H或C 1-4烷基; M是金属单能（k = 1）或双面（k = 2）; Y为0或NH; Z为0，NH，CH 2 O或键; 用于制造用于刺激红细胞生成的药物。优选地，组合物还包含人类红细胞生成素。

26. 发明授权

US5688771A Lipophilic oligopeptides with immunomodulating activity 失效
标题翻译：具有免疫调节活性的亲脂寡肽
公开(公告)号：US5688771A
公开(公告)日：1997-11-18
申请号：US313304
申请日：1994-10-03
申请人： Christopher Penney , Boulos Zacharie
发明人： Christopher Penney , Boulos Zacharie
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。

27. 发明授权

US08071580B2 Medium-chain length fatty alcohols as stimulators of hematopoiesis 有权
标题翻译：中链长脂肪醇作为造血刺激物
公开(公告)号：US08071580B2
公开(公告)日：2011-12-06
申请号：US11663888
申请日：2005-09-29
申请人： Christopher Penney , Lyne Gagnon , Jean Barabé
发明人： Christopher Penney , Lyne Gagnon , Jean Barabé
IPC分类号： A61K31/33 , A61K31/045
CPC分类号： A61K31/045
摘要： Medium-chain length fatty alcohols such as octanol, decanol, dodecanol, or analogues thereof can be used as a stimulator of hematopoiesis, hematopoietic stem cell proliferation, and/or proliferation of one or more of the progenitors of red or white blood cells (e.g., erythrocyte, leukocyte, neutrophil, granulocyte, megakaryocyte, or any combination thereof). It also relates to the treatment of myelosuppression; in particular, this includes the treatment of anemia and/or neutropenia associated with chemotherapy and/or radiotherapy. Moreover, anemia arising from chronic renal failure or treatment of HIV-infected patients with AZT (zidovudine), or other inhibitors of reverse transcriptase, can be treated. Furthermore, neutropenia arising from infections, hematologic diseases, or nutritional deficiencies can be treated. It also relates to reducing drug toxicity and enhancing drug efficiency.
摘要翻译：中链长度脂肪醇如辛醇，癸醇，十二烷醇或其类似物可用作红细胞或白细胞的一种或多种祖细胞造血干细胞增殖和/或增殖的刺激物（例如，，红细胞，白细胞，嗜中性粒细胞，粒细胞，巨核细胞或其任何组合）。它还涉及骨髓抑制的治疗; 特别地，这包括治疗与化学疗法和/或放射疗法相关的贫血和/或中性白细胞减少症。此外，可以治疗由慢性肾衰竭引起的贫血或治疗感染AZT（齐多夫定）的HIV感染患者或其他逆转录酶抑制剂的贫血。此外，可以治疗由感染，血液病或营养缺乏引起的中性粒细胞减少症。它还涉及降低药物毒性和提高药物效率。

28. 发明授权

US08946190B2 Medium-chain length fatty acids, salts and triglycerides in combination with gemcitabine for treatment of pancreatic cancer 有权
标题翻译：中链长度脂肪酸，盐和甘油三酯与吉西他滨联合治疗胰腺癌
公开(公告)号：US08946190B2
公开(公告)日：2015-02-03
申请号：US12809380
申请日：2008-12-18
申请人： Lyne Gagnon , Lilianne Geerts , Christopher Penney
发明人： Lyne Gagnon , Lilianne Geerts , Christopher Penney
IPC分类号： A61K31/7068 , A61K31/517 , A61K31/23 , A61K31/20 , A61P35/00
CPC分类号： A61K31/23 , A61K31/20 , A61K31/517 , A61K31/7068 , A61K2300/00
摘要： The present invention relates to the use of medium-chain length fatty acids of formula I, triglycerides of formula 2 (wherein n=6-10), salts thereof, or mixtures thereof, in combination with gemcitabine and optionally erlotinib in the treatment of pancreatic cancer in human patients. Exemplary medium-chain length fatty acid/triglyceride compounds include capric acid, sodium caprate, tricaprin, lauric acid, sodium laurate, and trilaurin.
摘要翻译：本发明涉及式I的中链长度脂肪酸，式2的甘油三酯（其中n = 6-10），其盐或其混合物与吉西他滨和任选的厄洛替尼联合用于胰腺治疗的用途人类癌症。示例性的中链长度脂肪酸/甘油三酸酯化合物包括癸酸，癸酸钠，三萜素，月桂酸，月桂酸钠和三月桂酸。

29. 发明申请

US20080051324A1 Medium-Chain Length Fatty Alcohols as Stimulators of Hematopoiesis 有权
标题翻译：中链长度脂肪醇作为造血细胞的刺激因子
公开(公告)号：US20080051324A1
公开(公告)日：2008-02-28
申请号：US11663888
申请日：2005-09-29
申请人： Christopher Penney , Lyne Gagnon , Jean Barabe
发明人： Christopher Penney , Lyne Gagnon , Jean Barabe
IPC分类号： A61K31/045 , A61K38/22 , A61P37/00 , A61P7/06
CPC分类号： A61K31/045
摘要： Medium-chain length fatty alcohols such as octanol, decanol, dodecanol, or analogues thereof can be used as a stimulator of hematopoiesis, hematopoietic stem cell proliferation, and/or proliferation of one or more of the progenitors of red or white blood cells (e.g., erythrocyte, leukocyte, neutrophil, granulocyte, megakaryocyte, or any combination thereof). It also relates to the treatment of myelosuppression; in particular, this includes the treatment of anemia and/or neutropenia associated with chemotherapy and/or radiotherapy. Moreover, anemia arising from chronic renal failure or treatment of HIV-infected patients with AZT (zidovudine), or other inhibitors of reverse transcriptase, can be treated. Furthermore, neutropenia arising from infections, hematologic diseases, or nutritional deficiencies can be treated. It also relates to reducing drug toxicity and enhancing drug efficiency.
摘要翻译：中链长度脂肪醇如辛醇，癸醇，十二烷醇或其类似物可用作红细胞或白细胞的一种或多种祖细胞造血干细胞增殖和/或增殖的刺激物（例如，，红细胞，白细胞，嗜中性粒细胞，粒细胞，巨核细胞或其任何组合）。它还涉及骨髓抑制的治疗; 特别地，这包括治疗与化学疗法和/或放射疗法相关的贫血和/或中性白细胞减少症。此外，可以治疗由慢性肾衰竭引起的贫血或治疗感染AZT（齐多夫定）的HIV感染患者或其他逆转录酶抑制剂的贫血。此外，可以治疗由感染，血液病或营养缺乏引起的中性粒细胞减少症。它还涉及降低药物毒性和提高药物效率。

30. 发明申请

US20100273731A1 Medium-Chain Length Fatty Acids, Salts and Triglycerides in Combination with Gemcitabine for Treatment of Pancreatic Cancer 有权
标题翻译：中链长度脂肪酸，盐酸和甘油三酯联合吉西他滨治疗胰腺癌
公开(公告)号：US20100273731A1
公开(公告)日：2010-10-28
申请号：US12809380
申请日：2008-12-18
申请人： Lyne Gagnon , Lilianne Geerts , Christopher Penney
发明人： Lyne Gagnon , Lilianne Geerts , Christopher Penney
IPC分类号： A61K31/7068 , A61P35/00
CPC分类号： A61K31/23 , A61K31/20 , A61K31/517 , A61K31/7068 , A61K2300/00
摘要： The present invention relates to the use of medium-chain length fatty acids of formula I, triglycerides of formula 2 (wherein n=6-10), salts thereof, or mixtures thereof, in combination with gemcitabine and optionally erlotinib in the treatment of pancreatic cancer in human patients. Exemplary medium-chain length fatty acid/triglyceride compounds include capric acid, sodium caprate, tricaprin, lauric acid, sodium laurate, and trilaurin.
摘要翻译：本发明涉及式I的中链长度脂肪酸，式2的甘油三酯（其中n = 6-10），其盐或其混合物与吉西他滨和任选的厄洛替尼联合用于胰腺治疗的用途人类癌症。示例性的中链长度脂肪酸/甘油三酸酯化合物包括癸酸，癸酸钠，三萜素，月桂酸，月桂酸钠和三月桂酸。

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