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1. 发明申请

US20060234927A1 Neuroprotective iron chelators and pharmaceutical compositions comprising them 有权
标题翻译：神经保护性铁螯合剂和包含它们的药物组合物
公开(公告)号：US20060234927A1
公开(公告)日：2006-10-19
申请号：US10534357
申请日：2006-02-21
申请人： Moussa Youdim , Matityahu Fridkin , Hailin Zheng , Abraham Warshawsky , Rivka Warshawsky
发明人： Moussa Youdim , Matityahu Fridkin , Hailin Zheng , Abraham Warshawsky , Rivka Warshawsky
IPC分类号： A61K38/22 , C07K14/575 , A61K31/496 , A61K31/4709 , C07D403/14
CPC分类号： C07D295/15 , A61K38/00 , A61K45/06 , A61K47/547 , C07D213/69 , C07D215/26 , C07D295/205 , C07K7/06 , C07K7/22 , C07K7/23 , C07K14/57563 , C07K14/70 , Y02A50/411
摘要： Novel iron chelators exhibiting neuroprotective and good transport properties are useful in iron chelation therapy for treatment of a disease, disorder or condition associated with iron overload and oxidative stress, eg. a neurodegenerative or cerebrovascular disease or disorder, a neoplastic disease, hemochromatosis, thalassemia, a cardiovascular disease, diabetes, a inflammatory disorder, anthracycline cardiotoxicity, a viral infection, a protozoal infection, a yeast infection, retarding ageing, and prevention and/or treatment of skin ageing and skin protection against sunlight and/or UV light. The iron chelator function is provided by a 8-hydroxyquinoline, a hydroxypyridinone or a hydroxamate moiety, the neuroprotective function is imparted to the compound e.g. by a neuroprotective peptide, and a combined antiapoptotic and neuroprotective function by a propargyl group.
摘要翻译：显示出神经保护和良好转运性质的新型铁螯合剂可用于铁螯合治疗用于治疗与铁过载和氧化应激相关的疾病，病症或病症，例如，神经变性或脑血管疾病或病症，肿瘤性疾病，血色素沉着病，地中海贫血，心血管疾病，糖尿病，炎性病症，蒽环类心脏毒性，病毒感染，原生动物感染，酵母感染，延迟衰老以及预防和/或治疗的皮肤老化和皮肤防晒防晒和/或紫外线。铁螯合剂功能由8-羟基喹啉，羟基吡啶酮或异羟肟酸盐部分提供，神经保护功能被赋予化合物例如通过神经保护肽，以及由炔丙基组合的抗细胞凋亡和神经保护功能。

2. 发明授权

US4215219A Reagents from phenolic and 8-hydroxyquinolinic aldehyde oximes 失效
标题翻译：酚类和8-羟基喹啉醛肟的试剂
公开(公告)号：US4215219A
公开(公告)日：1980-07-29
申请号：US802897
申请日：1977-06-02
申请人： Avraham Patchornik , Abraham Warshawsky , Matityahu Fridkin , Rami Kalir
发明人： Avraham Patchornik , Abraham Warshawsky , Matityahu Fridkin , Rami Kalir
IPC分类号： B01J45/00 , C07C45/68 , C07C205/22 , C07D213/06 , C07D213/16 , C07D215/24 , C07D215/26 , C08F8/00 , C08F8/24 , C08F8/30 , C08F212/00 , C22B3/26 , C07D215/14 , C07C119/00
CPC分类号： C07D213/16 , B01J45/00 , C07C205/22 , C07C205/45 , C07C45/68 , C07D213/06 , C07D215/24 , C07D215/26 , C08F8/24 , C08F8/30 , C22B3/0097 , C22B3/42 , Y02P10/234
摘要： A process for producing reagents useful in organic synthesis, for removing metal values from solutions thereof, for the capture of aldehydes, of the general formula ##STR1## wherein Z designates a recurring part (CH.sub.2 --CH--CH.sub.2) of a polymeric backbone of a polymer like polystyrene, of a copolymer comprising polystyrene and divinylbenzene, and butadiene, or other copolymers comprising styrene moieties; or wherein Z is the aliphatic moiety of a long-chain aralkyl compound having a terminal aryl group; or wherein Z designates alkyl; corresponding compounds wherein instead of the optionally substituted phenyl group there is present an optionally substituted naphthyl group; wherein n is an integer of from 1 to 15, and wherein Q designates a group selected from: ##STR2## wherein R designates --H, lower alkyl, aryl, which may be substituted and wherein R" designates --H, alkyl, aryl, halogen, nitro or carboxy, or ##STR3## wherein R is --H, lower alkyl, aryl (which may be substituted), R.sub.1 is --H, alkyl, aryl (which may be substituted), R.sub.2 is --H, alkyl, aryl or substituted aryl, and wherein Y is --H or a non-interferring substituent, which comprises chemically binding an activated chemical moiety to a group ##STR4## or a corresponding naphthyl-containing group, wherein Z is as defined above, according to the reaction scheme: ##STR5## wherein Q is as defined above, or a functional group which can be converted to such group after the chemical bonding; and X is --Cl or --Br.
摘要翻译：一种制备用于有机合成的试剂的方法，用于从其溶液中除去金属，用于捕获醛，通式为：其中Z表示聚合物主链的重复部分（CH 2 -CH-CH 2）聚苯乙烯，包含聚苯乙烯和二乙烯基苯的共聚物，丁二烯，或包含苯乙烯部分的其它共聚物; 或其中Z是具有末端芳基的长链芳烷基化合物的脂族部分; 或其中Z表示烷基; 相应的化合物，其中代替任选取代的苯基存在任选取代的萘基; 其中n是1至15的整数，并且其中Q表示选自以下的基团：其中R表示-H，低级烷基，可被取代的芳基，其中R' 表示-H，烷基，芳基，卤素，硝基或羧基，或其中R是-H，低级烷基，芳基（其可被取代的），R 1是-H，烷基，芳基（其可以被取代），R2是-H，烷基，芳基或取代的芳基，并且其中Y是-H或非干扰性取代基，其包括将活化的化学部分与基团或相应的萘基 - 其中Z如上所定义，根据反应方案：其中Q如上所定义，或在化学键合后可以转化为这种基团的官能团; X是-Cl或-Br。

3. 发明授权

US4085261A Organic reagents and process of preparing same 失效
标题翻译：有机试剂及其制备方法
公开(公告)号：US4085261A
公开(公告)日：1978-04-18
申请号：US545220
申请日：1975-01-29
申请人： Avraham Patchornik , Abraham Warshawsky , Matityahu Fridkin , Rami Kalir
发明人： Avraham Patchornik , Abraham Warshawsky , Matityahu Fridkin , Rami Kalir
IPC分类号： B01J45/00 , C07C45/68 , C07C205/22 , C07D213/06 , C07D213/16 , C07D215/24 , C07D215/26 , C08F8/00 , C08F8/24 , C08F8/30 , C08F212/00 , C22B3/26 , B01D11/00 , C08C19/00 , C08F232/00
CPC分类号： C07D213/16 , B01J45/00 , C07C205/22 , C07C205/45 , C07C45/68 , C07D213/06 , C07D215/24 , C07D215/26 , C08F8/24 , C08F8/30 , C22B3/0097 , C22B3/42 , Y02P10/234
摘要： A process for producing reagents useful in organic synthesis, for removing metal values from solutions thereof, for the capture of aldehydes, of the general formula ##STR1## wherein Z designates a recurring part (CH.sub.2 --CH--CH.sub.2 -- of a polymeric backbone of a polymer like polystyrene, of a copolymer comprising polystyrene and divinylbenzene, and butadiene, or other copolymers comprising styrene moieties; or wherein Z is the aliphatic moiety of a long-chain aralkyl compound having a terminal aryl group; or wherein Z designates alkyl; corresponding compounds wherein instead of the optionally substituted phenyl group there is present an optionally substituted naphthyl group; wherein n is an integer of from 1 to 15, and wherein Q designates a group selected from: ##STR2## wherein R designates --H, lower alkyl, aryl, which may be substituted and wherein R" designates --H, alkyl, aryl, halogen, nitro or carboxy, or ##STR3## wherein R is --H, lower alkyl, aryl (which may be substituted), R.sub.1 is --H, alkyl, aryl (which may be substituted), R.sub.2 is --H, alkyl, aryl or substituted aryl, and wherein Y is --H or a non-interfering substituent;which comprises chemically binding an activated chemical moiety to a group Z- -, or a corresponding naphthyl-containing group, wherein Z is as defined above, according to the reaction scheme: ##STR4## wherein Q is as defined above, or a functional group which can be converted to such group after the chemical bonding; and X is --Cl or --Br.
摘要翻译：用于生产有机合成中的试剂的方法，用于从其溶液中除去金属，用于捕获醛，通式为“IMAGE”，其中Z表示重复部分（CH2-CH-CH2- 聚苯乙烯，包含聚苯乙烯和二乙烯基苯的共聚物，丁二烯或包含苯乙烯部分的其它共聚物;或其中Z是具有末端芳基的长链芳烷基化合物的脂族部分;或其中Z表示烷基;相应的化合物其中代替任选取代的苯基，存在任选取代的萘基;其中n为1至15的整数，并且其中Q表示选自以下的基团：其中R表示-H，可以被取代的低级烷基，芳基，其中R“表示-H，烷基，芳基，卤素，硝基或羧基，或者” IMAGE> wherei n为低级烷基，芳基（其可被取代），R 1为-H，烷基，芳基（其可被取代），R 2为-H，烷基，芳基或取代的芳基，并且其中Y为-H 或非干扰性取代基; 其包括根据反应方案将活化的化学部分与基团Z-或相应的含萘基团（其中Z如上所定义）化学结合：其中Q如上所定义或在化学键合后可以转化为这种基团的官能团; X是-Cl或-Br。

4. 发明申请

US20050004000A1 Oral absorbed drugs 审中-公开
标题翻译：口服吸毒
公开(公告)号：US20050004000A1
公开(公告)日：2005-01-06
申请号：US10473721
申请日：2002-03-26
申请人： Yoram Shechter , Matityahu Fridkin , Iris Lavon , David Brodie , Nurit Eyal , Stanley Fass , Matityahu Fridkin
发明人： Yoram Shechter , Matityahu Fridkin , Iris Lavon , David Brodie , Nurit Eyal , Stanley Fass , Matityahu Fridkin
IPC分类号： C07H15/234 , C07H15/236 , C07K7/23 , C07K14/70 , A61K38/00 , A61K31/66 , C07F9/02
CPC分类号： C07K14/70 , C07H15/234 , C07H15/236 , C07K7/23
摘要： Orally nonabsorbed or poorly absorbed drugs may be converted to orally absorbed prodrug derivatives by derivatization of free functional groups selected from amino, hydroxyl, mercapto, phosphate and/or carboxyl with groups sensitive to mild basic conditions such as 9-fluorenylmethoxycarbonyl (Fmoc), 2-sulfo-9-fluorenylmethoxycarbonyl (Fms), and fluorenylmethyl (Fm).
摘要翻译：口服非吸收或吸收不良的药物可以通过衍生化为选自氨基，羟基，巯基，磷酸酯和/或羧基的游离官能团，并对温和的碱性条件敏感的基团，如9-芴基甲氧基羰基（Fmoc），2 - 磺基-9-芴基甲氧基羰基（Fms）和芴基甲基（Fm）。

5. 发明授权

US09155780B2 Short beta-defensin-derived peptides 有权
标题翻译：短的β-防御素衍生肽
公开(公告)号：US09155780B2
公开(公告)日：2015-10-13
申请号：US13148376
申请日：2010-02-10
申请人： Tsvee Lapidot , Alexander Kalinkovich , Matityahu Fridkin
发明人： Tsvee Lapidot , Alexander Kalinkovich , Matityahu Fridkin
IPC分类号： A61K38/08 , C07K7/06 , A61K38/17 , A61K38/12 , C07K14/47
CPC分类号： A61K38/1729 , A61K38/00 , A61K38/12 , A61K38/193 , C07K7/52 , C07K14/4723
摘要： The invention is directed to beta-defensin-derived peptides and their use in modulating the activity of hematopoietic cells and other CXCR4-expressing cells. Specifically, the invention provides compositions and methods useful in the treatment of cancer. The invention further provides compositions and methods useful for promoting mobilization and transplantation of hematopoietic stem cells and progenitor cells.
摘要翻译：本发明涉及β-防御素衍生肽及其在调节造血细胞和其他CXCR4表达细胞活性中的用途。具体地，本发明提供了可用于治疗癌症的组合物和方法。本发明还提供了用于促进造血干细胞和祖细胞的移动和移植的组合物和方法。

6. 发明申请

US20150202310A1 ALBUMIN BINDING PROBES AND DRUG CONJUGATES THEREOF 有权
公开(公告)号：US20150202310A1
公开(公告)日：2015-07-23
申请号：US14111347
申请日：2012-04-04
申请人： Yoram Shechter , Matityahu Fridkin
发明人： Yoram Shechter , Matityahu Fridkin
IPC分类号： A61K47/48 , A61K38/37 , A61K38/22 , A61K38/48 , C07C309/17 , A61K38/28
CPC分类号： A61K47/48038 , A61K38/22 , A61K38/28 , A61K38/37 , A61K38/4846 , A61K47/542 , C07C309/17 , C07D207/46 , C07D213/70 , C12Y304/21021
摘要： The present invention provides a long chain fatty acid (LCFA)-like albumin-binding probe/ligand containing no hydrolysable bond and having an enhanced associating affinity with human serum albumin, which upon conjugation with an amino- or mercapto-containing short-lived drug and administration of the conjugate, significantly prolongs the life time of said drug without substantially interfering with its pharmacological activity. The invention further provides conjugates of said probe with amino- or mercapto-containing drugs, as well as pharmaceutical compositions and uses thereof.
摘要翻译：本发明提供了一种长链脂肪酸（LCFA）样白蛋白结合探针/配体，其不含可水解键并且与人血清白蛋白具有增强的缔合亲和力，其在与含氨基或巯基的短寿命药物和施用所述缀合物，显着延长所述药物的使用寿命，而基本上不干扰其药理学活性。本发明还提供了所述探针与含氨基或巯基的药物的结合物，以及药物组合物及其用途。

7. 发明申请

US20100041867A1 REVERSIBLE PEGYLATED DRUGS 有权
标题翻译：可逆的PEGY药物
公开(公告)号：US20100041867A1
公开(公告)日：2010-02-18
申请号：US12540169
申请日：2009-08-12
申请人： Yoram SHECHTER , Matityahu Fridkin , Haim Tsubery
发明人： Yoram SHECHTER , Matityahu Fridkin , Haim Tsubery
IPC分类号： A61K47/48 , C07D207/40 , C07D403/02 , C07K2/00 , C07D403/12
CPC分类号： A61K47/60 , A61K31/7036 , A61K38/1709 , A61K38/212 , A61K38/22 , A61K38/2242 , A61K38/2278 , A61K38/26 , A61K38/27 , A61K38/28 , A61K47/54 , A61K47/545 , C07D207/404 , C07D207/416 , C07D207/452 , C07D403/12
摘要： Reversible pegylated drugs are provided by derivatization of free functional groups of the drug selected from amino, hydroxyl, mercapto, phosphate and/or carboxyl with groups sensitive to mild basic conditions such as 9-fluorenylmethoxycarbonyl (Fmoc) or 2-sulfo-9-fluorenylmethoxycarbonyl (FMS), to which group a PEG moiety is attached. In these pegylated drugs, the PEG moiety and the drug residue are not linked directly to each other, but rather both residues are linked to different positions of the scaffold Fmoc or FMS structure that is highly sensitive to bases and is removable under physiological conditions. The drugs are preferably drugs containing an amino group, most preferably peptides and proteins of low or medium molecular weight. Similar molecules are provided wherein a protein carrier or another polymer carrier replaces the PEG moiety.
摘要翻译：可逆的聚乙二醇化药物通过衍生自选自氨基，羟基，巯基，磷酸酯和/或羧基的药物的游离官能团与对温和碱性条件敏感的基团如9-芴基甲氧基羰基（Fmoc）或2-磺基-9-芴基甲氧基羰基（FMS），连接有PEG部分的基团。在这些聚乙二醇化药物中，PEG部分和药物残留物不直接相互连接，而是两个残基都连接到对碱基高度敏感并在生理条件下可去除的支架Fmoc或FMS结构的不同位置。药物优选是含有氨基的药物，最优选低分子量或中等分子量的肽和蛋白质。提供了类似的分子，其中蛋白质载体或另一种聚合物载体取代了PEG部分。

8. 发明申请

US20050075284A1 Pharmaceutical compositions comprising vip-related peptides for the treatment of sexual disorders 审中-公开
标题翻译：包含用于治疗性障碍的vip相关肽的药物组合物
公开(公告)号：US20050075284A1
公开(公告)日：2005-04-07
申请号：US10240392
申请日：2001-05-22
申请人： Illana Gozes , Matityahu Fridkin
发明人： Illana Gozes , Matityahu Fridkin
IPC分类号： A61K9/06 , A61K9/08 , A61K9/10 , A61K9/127 , A61K38/22 , A61K47/48 , A61P15/02 , A61P15/08 , C07K14/47
CPC分类号： A61K38/2278 , A61K47/54 , A61K47/542 , A61K47/64
摘要： The present invention relates to pharmaceutical compositions for the treatment of female sexual dysfunction, for vaginal relaxation and/or for modulation of sperm motility. The composition comprises as active ingredient (i) a peptide analogue or conjugate of vasoactive intestinal peptide (VIP) as defined in the specification and is preferably formulated for topical application in the vaginal, vulvar and/or clitorial area. The invention also relates to the use of the VIP peptide analogue or conjugate for the preparation of a pharmaceutical composition for the treatment of female sexual dysfunction, for vaginal relaxation and/or for modulation of sperm motility. Yet further, the invention provides a method of treatment of female sexual dysfunctions and/or vaginal relaxation by the use of said peptide analogue and/or conjugate.
摘要翻译：本发明涉及用于治疗女性性功能障碍，阴道松弛和/或调节精子活力的药物组合物。组合物包含作为活性成分（i）如说明书中定义的血管活性肠肽（VIP）的肽类似物或缀合物，并且优选配制用于阴道，外阴和/或阴蒂区域的局部应用。本发明还涉及VIP肽类似物或缀合物用于制备用于治疗女性性功能障碍，用于阴道松弛和/或调节精子活力的药物组合物的用途。此外，本发明提供了通过使用所述肽类似物和/或缀合物来治疗女性性功能障碍和/或阴道松弛的方法。

9. 发明授权

US09480751B2 Albumin binding probes and drug conjugates thereof 有权
标题翻译：白蛋白结合探针及其药物偶联物
公开(公告)号：US09480751B2
公开(公告)日：2016-11-01
申请号：US14111347
申请日：2012-04-04
申请人： Yoram Shechter , Matityahu Fridkin
发明人： Yoram Shechter , Matityahu Fridkin
IPC分类号： A61K38/00 , A61K47/48 , C07C309/17 , C07D207/46 , C07D213/70 , A61K38/22 , A61K38/28 , A61K38/37 , A61K38/48
CPC分类号： A61K47/48038 , A61K38/22 , A61K38/28 , A61K38/37 , A61K38/4846 , A61K47/542 , C07C309/17 , C07D207/46 , C07D213/70 , C12Y304/21021
摘要： The present invention provides a long chain fatty acid (LCFA)-like albumin-binding probe/ligand containing no hydrolysable bond and having an enhanced associating affinity with human serum albumin, which upon conjugation with an amino- or mercapto-containing short-lived drug and administration of the conjugate, significantly prolongs the life time of said drug without substantially interfering with its pharmacological activity. The invention further provides conjugates of said probe with amino- or mercapto-containing drugs, as well as pharmaceutical compositions and uses thereof.
摘要翻译：本发明提供了一种长链脂肪酸（LCFA）样白蛋白结合探针/配体，其不含可水解键并且与人血清白蛋白具有增强的缔合亲和力，其在与含氨基或巯基的短寿命药物和施用所述缀合物，显着延长所述药物的使用寿命，而基本上不干扰其药理学活性。本发明还提供了所述探针与含氨基或巯基的药物的结合物，以及药物组合物及其用途。

10. 发明授权

US08343910B2 Reversible pegylated drugs 有权
公开(公告)号：US08343910B2
公开(公告)日：2013-01-01
申请号：US12540169
申请日：2009-08-12
申请人： Yoram Shechter , Matityahu Fridkin , Haim Tsubery
发明人： Yoram Shechter , Matityahu Fridkin , Haim Tsubery
IPC分类号： A61K38/00
CPC分类号： A61K47/60 , A61K31/7036 , A61K38/1709 , A61K38/212 , A61K38/22 , A61K38/2242 , A61K38/2278 , A61K38/26 , A61K38/27 , A61K38/28 , A61K47/54 , A61K47/545 , C07D207/404 , C07D207/416 , C07D207/452 , C07D403/12
摘要： Reversible pegylated drugs are provided by derivatization of free functional groups of the drug selected from amino, hydroxyl, mercapto, phosphate and/or carboxyl with groups sensitive to mild basic conditions such as 9-fluorenylmethoxycarbonyl (Fmoc) or 2-sulfo-9-fluorenylmethoxycarbonyl (FMS), to which group a PEG moiety is attached. In these pegylated drugs, the PEG moiety and the drug residue are not linked directly to each other, but rather both residues are linked to different positions of the scaffold Fmoc or FMS structure that is highly sensitive to bases and is removable under physiological conditions. The drugs are preferably drugs containing an amino group, most preferably peptides and proteins of low or medium molecular weight. Similar molecules are provided wherein a protein carrier or another polymer carrier replaces the PEG moiety.

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