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1. 发明申请

WO2011140393A1 CONTROLLED RELEASE FROM MACROMOLECULAR CONJUGATES 审中-公开
标题翻译：从大分子结合物的控制释放
公开(公告)号：WO2011140393A1
公开(公告)日：2011-11-10
申请号：PCT/US2011/035423
申请日：2011-05-05
申请人： PROLYNX LLC , ASHLEY, Gary , SANTI, Daniel, V.
发明人： ASHLEY, Gary , SANTI, Daniel, V.
IPC分类号： A01N57/00
CPC分类号： A61K47/48215 , A61K9/0019 , A61K9/08 , A61K47/48023 , A61K47/54 , A61K47/60 , C07D487/04 , C07D491/22
摘要： The invention relates to conjugates of macromolecular carriers and drugs comprising linkers that release the drug or a prodrug through rate-controlled beta-elimination, and methods of making and using the conjugates.
摘要翻译：本发明涉及大分子载体的缀合物和包含通过速率控制的β-消除释放药物或前药的接头的药物，以及制备和使用缀合物的方法。

2. 发明申请

WO2011140376A1 CONTROLLED DRUG RELEASE FROM DENDRIMERS 审中-公开
标题翻译：控制药物从DENDRIMERS发布
公开(公告)号：WO2011140376A1
公开(公告)日：2011-11-10
申请号：PCT/US2011/035403
申请日：2011-05-05
申请人： PROLYNX LLC , ASHLEY, Gary , SANTI, Daniel, V.
发明人： ASHLEY, Gary , SANTI, Daniel, V.
IPC分类号： A61K9/22 , A61K9/52
CPC分类号： A61K47/48315 , A61K38/2242 , A61K38/26 , A61K38/50 , A61K47/60 , A61K47/641 , A61K47/645 , C08G83/003 , C08G83/004
摘要： The invention relates to compositions that comprise dendrimers useful in medical and veterinary applications that provide controlled release of drugs, such as peptides, nucleic acids and small molecules. The drugs are covalently coupled to the dendrimer through a linkage that releases the drug or a prodrug through controlled beta elimination.
摘要翻译：本发明涉及包含用于医学和兽医学应用中的树枝状大分子的组合物，其提供药物（例如肽，核酸和小分子）的受控释放。这些药物通过通过对照β消除释放药物或前药的连接共价偶联到树状聚合物上。

3. 发明申请

WO2009158668A1 PRODRUGS AND DRUG-MACROMOLECULE CONJUGATES HAVING CONTROLLED DRUG RELEASE RATES 审中-公开
标题翻译：具有控制药物释放率的产品和药物 - 大分子药物
公开(公告)号：WO2009158668A1
公开(公告)日：2009-12-30
申请号：PCT/US2009/048943
申请日：2009-06-26
申请人： PROLYNX LLC , SANTI, Daniel, V. , ASHLEY, Gary , HEARN, Brian
发明人： SANTI, Daniel, V. , ASHLEY, Gary , HEARN, Brian
IPC分类号： A61K9/22
CPC分类号： A61K47/48023 , A61K47/54 , A61K47/60 , C08G65/329 , C08G65/33317 , C08G65/33396 , C08L2203/02
摘要： The present invention provides methods and compositions that permit controlled and prolonged drug release in vivo . The compounds are either prodrugs with tunable rates of release, or conjugates of the drug with macromolecules which exhibit tunable controlled rates of release.
摘要翻译：本发明提供允许体内可控和延长的药物释放的方法和组合物。化合物是具有可调节释放速率的前药或药物与大分子的缀合物，其表现出可调节的释放速率。

4. 发明申请

WO2011140392A1 CONTROLLED DRUG RELEASE FROM SOLID SUPPORTS 审中-公开
标题翻译：控制药物从固体支持中释放
公开(公告)号：WO2011140392A1
公开(公告)日：2011-11-10
申请号：PCT/US2011/035422
申请日：2011-05-05
申请人： PROLYNX LLC , ASHLEY, Gary , SANTI, Daniel, V.
发明人： ASHLEY, Gary , SANTI, Daniel, V.
IPC分类号： A01N57/00
CPC分类号： A61K47/48215 , A61K47/58 , A61K47/60 , A61K47/6435 , A61K47/6903 , A61K47/6953 , A61K47/6957 , A61K49/0043 , A61K49/0054 , A61L15/44 , A61L27/54 , A61L29/16 , A61L31/16 , A61L2300/252 , A61L2300/258
摘要： The invention relates to solid supports useful in medical applications that provide controlled release of drugs, such as peptides, nucleic acids and small molecules. The drugs are covalently coupled to the solid support through a linkage that releases the drug or a prodrug through controlled beta elimination.
摘要翻译：本发明涉及用于医疗应用中的固体支持物，其提供药物如肽，核酸和小分子的受控释放。这些药物通过通过控制β消除释放药物或前药的连接共价偶联到固体支持物上。

5. 发明申请

WO2007070536A3 7-QUINOLYL KETOLIDE ANTIBACTERIAL AGENTS 审中-公开
标题翻译： 7-QUINOLYL KETOLIDE抗菌剂
公开(公告)号：WO2007070536A3
公开(公告)日：2008-04-03
申请号：PCT/US2006047439
申请日：2006-12-12
申请人： KOSAN BIOSCIENCES INC , SHAW SIMON JAMES , ASHLEY GARY W , BURLINGAME MARK A
发明人： SHAW SIMON JAMES , ASHLEY GARY W , BURLINGAME MARK A
IPC分类号： A01N43/04 , A61K31/70
CPC分类号： C07D405/14
摘要： 15-fluoroketolides of the formula (I): having improved activity and safety, compositions comprising them, and methods for their preparation and use in the treatment of bacterial infections.
摘要翻译：式（I）的15-氟代内酯：具有改善的活性和安全性，包含它们的组合物及其制备和用于治疗细菌感染的方法。

6. 发明申请

WO2007070536A2 7-QUINOLYL KETOLIDE ANTIBACTERIAL AGENTS 审中-公开
标题翻译： 7-喹诺酮类抗生素代谢物
公开(公告)号：WO2007070536A2
公开(公告)日：2007-06-21
申请号：PCT/US2006/047439
申请日：2006-12-12
申请人： KOSAN BIOSCIENCES INCORPORATED , SHAW, Simon, James , ASHLEY, Gary, W. , BURLINGAME, Mark, A.
发明人： SHAW, Simon, James , ASHLEY, Gary, W. , BURLINGAME, Mark, A.
IPC分类号： A61K31/7052
CPC分类号： C07D405/14
摘要： 15-fluoroketolides of the formula (I): having improved activity and safety, compositions comprising them, and methods for their preparation and use in the treatment of bacterial infections.
摘要翻译：式（I）的15-氟代内酯：具有改善的活性和安全性，包含它们的组合物及其制备和用于治疗细菌感染的方法。

7. 发明申请

WO2002097062A3 RECOMBINANT NARBONOLIDE POLYKETIDE SYNTHASE 审中-公开
公开(公告)号：WO2002097062A3
公开(公告)日：2002-12-05
申请号：PCT/US2002/005642
申请日：2002-02-22
申请人： KOSAN BIOSCIENCES, INC. , ASHLEY, Gary , BETLACH, Melanie, C. , BETLACH, Mary , MCDANIEL, Robert , TANG, Li
发明人： ASHLEY, Gary , BETLACH, Melanie, C. , BETLACH, Mary , MCDANIEL, Robert , TANG, Li
IPC分类号： C12N1/20
摘要： Recombinant DNA compounds that encode all or a portion of the narbonolide polyketide synthase are used to express recombinant polyketide synthase genes in host cells for the production of narbonolide, narbonolide derivatives, and polyketides that are useful as antibiotics and as intermediates in the synthesis of compounds with pharmaceutical value.

8. 发明申请

WO0192255A3 EPOTHILONE DERIVATIVES AND METHODS FOR MAKING AND USING THE SAME 审中-公开
标题翻译： EPOTHILONE衍生物及其制备和使用方法
公开(公告)号：WO0192255A3
公开(公告)日：2002-02-28
申请号：PCT/US0115763
申请日：2001-05-15
申请人： KOSAN BIOSCIENCES INC , SANTI DANIEL , FARDIS MARIA , ASHLEY GARY
发明人： SANTI DANIEL , FARDIS MARIA , ASHLEY GARY
IPC分类号： C07D417/06 , C07D417/14 , C07D491/04 , C07D493/04 , A61K31/335 , A61P35/00
CPC分类号： C07D417/06 , C07D417/14 , C07D491/04 , C07D493/04
摘要： The present invention relates to 16-membered macrocyclic compounds. In one aspect of the present invention, compounds of the formula (I), are provided wherein: R , R , R , and R are each independently hydrogen, methyl or ethyl; R is hydrogen, hydroxyl, oxo, or NRR' where R and R' are independently hydrogen, C1-C10 aliphatic, aryl or alkylaryl; R is hydrogen, oxo, or C1-C10 aliphatic, or optionally R and R together form a carbon-carbon double bond; R is hydrogen, hydroxyl, oxo, C1-C10 aliphatic, C1-C10 alkylester, or halide; R is hydrogen or C1-C10 aliphatic that is optionally substituted C1-C5 aliphatic, C1-C5 alkoxy, aryl, or a functional group selected from the group consisting of acetal, alcohol, aldehyde, amide, amine, carbamate, carboalkoxy, carbonate, carbodiimide, carboxylic acid, dioxolane and halogen, or optionally, R and R together form a 1,3-dioxane that is optionally substituted at the 2-position; R and R are both hydrogen or together form a carbon-carbon double bond or an epoxide; Ar is aryl; and, W is O or NR where R is hydrogen, C1-C10 aliphatic, aryl or alkylaryl provided that at least one of R , R , and R is not hydrogen. These compounds are cytotoxic agents and can be used to treat cancer and non-cancer disorders characterized by cellular hyperproliferation.
摘要翻译：本发明涉及16元大环化合物。在本发明的一个方面，提供式（I）化合物，其中：R 1，R 2，R 3和R 10各自独立地为氢，甲基或乙基; R 4是氢，羟基，氧代或NRR'，其中R和R'独立地是氢，C 1 -C 10脂族，芳基或烷基芳基; R 5是氢，氧代或C 1 -C 10脂族基，或任选地R 4和R 5一起形成碳 - 碳双键; R 6是氢，羟基，氧代，C 1 -C 10脂族，C 1 -C 10烷基酯或卤化物; R 7是氢或C 1 -C 10脂族基，其是任选取代的C 1 -C 5脂族，C 1 -C 5烷氧基，芳基或选自缩醛，醇，醛，酰胺，胺，氨基甲酸酯，烷氧羰基的官能团，碳酸酯，碳二亚胺，羧酸，二氧戊环和卤素，或任选地，R 6和R 7一起形成任选在2-位取代的1,3-二恶烷; R 8和R 9均为氢或一起形成碳 - 碳双键或环氧化物; Ar为芳基; 并且W是O或NR 11，其中R 11是氢，C 1 -C 10脂族，芳基或烷基芳基，条件是R 4，R 5和R 6中的至少一个不是氢。这些化合物是细胞毒性剂，可用于治疗以细胞过度增殖为特征的癌症和非癌症疾病。

9. 发明申请

WO0063224A3 MACROLIDE ANTIINFECTIVE AGENTS 审中-公开
标题翻译：麦角抗菌药
公开(公告)号：WO0063224A3
公开(公告)日：2001-01-18
申请号：PCT/US0009914
申请日：2000-04-14
申请人： KOSAN BIOSCIENCES INC , CHU DANIEL T W , ASHLEY GARY W
发明人： CHU DANIEL T W , ASHLEY GARY W
IPC分类号： A61K31/7048 , A61P31/04 , C07H17/00 , C07H17/08 , A61K31/70
CPC分类号： C07H17/08 , Y02P20/55
摘要： Compounds of formula (1), (2) or (3), wherein Ra is H; substituted or unsubstituted alkyl (1-10C); substituted or unsubstituted alkenyl (2-10C); substituted or unsubstituted alkynyl (2-10C); substituted or unsubstituted aryl (4-14C); substituted or unsubstituted arylalkyl (5-20C); or ORa is replaced by H; Rb is H or halogen; Rc is H or a protecting group; Rd is methyl, unsubstituted alkyl (3-10C); substituted alkyl (1-10C); substituted or unsubstituted alkynyl (2-10C); substituted or unsubstituted aryl (4-14C); substituted or unsubstituted arylalkyl (5-20C); substituted or unsubstituted arylalkenyl (5-20C); substituted or unsubstituted arylalkynyl (5-20C); substituted or unsubstituted amidoarylalkyl (5-20C); substituted or unsubstituted amidoarylalkenyl (5-20C); or substituted or unsubstituted amidoarylalkynyl (5-20C); Re is H or a protecting group; L is methylene or carbonyl; T is -O-, -N(R)-, -N(OR)-, -N(NHCOR)-, -N(N=CHR)-, or -N(NHR)- wherein R is H or Ra as defined above, with the proviso that when L is methylene, T is -O-; one of Z and Y is H and the other is OH, protected OH, or amino, mono- or dialkylamino, protected amino, or an amino heterocycle or Z and Y together are =O, =NOH or a derivatized oxime; including any pharmaceutically acceptable salts thereof and any stereoisomeric forms and mixtures of stereoisomeric forms thereof, are antimicrobial agents.
摘要翻译：式（1），（2）或（3）的化合物，其中R a是H; 取代或未取代的烷基（1-10C）; 取代或未取代的烯基（2-10C）; 取代或未取代的炔基（2-10C）; 取代或未取代的芳基（4-14C）; 取代或未取代的芳基烷基（5-20℃）; 或ORa被H代替; Rb是H或卤素; Rc是H或保护基; Rd为甲基，未取代的烷基（3-10C）; 取代的烷基（1-10C）; 取代或未取代的炔基（2-10C）; 取代或未取代的芳基（4-14C）; 取代或未取代的芳基烷基（5-20℃）; 取代或未取代的芳基烯基（5-20℃）; 取代或未取代的芳基炔基（5-20℃）; 取代或未取代的酰氨基芳基烷基（5-20℃）; 取代或未取代的酰氨基芳基烯基（5-20℃）; 或取代或未取代的酰氨基芳基炔基（5-20℃）; Re为H或保护基; L是亚甲基或羰基; T是-O - ， - N（R） - ， - N（OR） - ， - N（NHCOR） - ， - N（N = CHR） - 或-N（NHR） - ，其中R是H或Ra 条件是当L是亚甲基时，T是-O-; Z和Y之一是H，另一个是OH，保护的OH或氨基，单或二烷基氨基，保护的氨基或氨基杂环，或Z和Y一起是= O，= NOH或衍生化的肟; 包括其任何药学上可接受的盐和其立体异构体形式及其立体异构形式的混合物均为抗微生物剂。

10. 发明申请

WO2013059323A1 PEG CONJUGATES OF EXENATIDE 审中-公开
标题翻译： PEG联合使用
公开(公告)号：WO2013059323A1
公开(公告)日：2013-04-25
申请号：PCT/US2012/060618
申请日：2012-10-17
申请人： PROLYNX LLC , SCHNEIDER, Eric, L. , SANTI, Daniel, V. , ASHLEY, Gary, W.
发明人： SCHNEIDER, Eric, L. , SANTI, Daniel, V. , ASHLEY, Gary, W.
IPC分类号： C07K16/00 , A61K38/26 , C08G59/00
CPC分类号： A61K47/48215 , A61K38/00 , A61K47/60
摘要： Slow release forms of exenatide wherein exenatide is releasably linked to polyethylene glycol carriers are disclosed.
摘要翻译：公开了艾塞那肽的缓释形式，其中艾塞那肽可释放地连接到聚乙二醇载体上。

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