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1. 发明专利

AU2001283998B2 Tetrazolyl-phenyl acetamide glucokinase activators 未知
公开(公告)号：AU2001283998B2
公开(公告)日：2005-10-20
申请号：AU2001283998
申请日：2001-08-09
申请人： HOFFMANN LA ROCHE
发明人： SIDDURI ACHYUTHARAO
IPC分类号： A61K31/41 , A61K31/427 , A61K31/4427 , A61K31/4439 , A61P3/10 , C07D257/04 , C07D277/28 , C07D401/12 , C07D417/12 , A61K031/4427 , A61P003/10 , A61K031/41 , A61K031/427
摘要： Tetrazolyl-phenyl acetamides are active as glucokinase activators, and are able to increase insulin secretion, which makes them useful for treating type II diabetes.

2. 发明专利

AU2001246883B2 Stabilized pharmaceutical compositions containing calcium channel blockers 未知
公开(公告)号：AU2001246883B2
公开(公告)日：2004-08-12
申请号：AU2001246883
申请日：2001-04-10
申请人： SANKYO CO , UBE INDUSTRIES
发明人： NISHIMURA KENJI , USUI FUSAO , WAKIYAMA NAOKI
IPC分类号： A61K9/20 , A61K31/4418 , A61K31/4422 , A61K31/4427 , A61K31/443 , A61K31/4439 , A61K31/444 , A61K31/4545 , A61K31/496 , A61K31/675 , A61K47/02 , A61P9/12 , C07D211/90 , C07D401/06 , C07F9/6571 , A61K031/4422 , C07D405/06 , C07D211/92 , A61K047/02 , A61K031/4545 , A61K031/443 , A61K031/675 , A61K031/444 , A61K031/4439 , A61K031/4427 , C07F009/59
摘要： The present invention provides a pharmaceutical composition containing a calcium blocker of the following formula or a pharmacologically acceptable salt thereof and a pharmacologically acceptable alkaline material which is added to an extent such that an aqueous solution or dispersion solution of said pharmaceutical composition containing a calcium blocker has a pH of at least 8: Äwherein R represents an optionally substituted C1-C4 alkyl group, an amino group or a cyano group; R represents an optionally substituted C1-C4 alkyl group, a substituted C3-C4 alkenyl group, or a substituted 4- to 6-membered cyclic amino group; R represents a substituted phenyl group; R represents an optionally substituted C1-C4 alkoxycarbonyl group, a 1,3,2-phosphorinan-2-yl group, or a 5,5-dimethyl-1,3,2-phosphorinan-2-yl group, R represents a C1-C4 alkyl groupÜ.

3. 发明申请

US20020013346A1 C7 ester substituted taxanes 失效
标题翻译： C7酯取代紫杉烷
公开(公告)号：US20020013346A1
公开(公告)日：2002-01-31
申请号：US09775851
申请日：2001-02-02
发明人： Robert A. Holton
IPC分类号： A61K031/4427 , A61K031/381 , A61K031/34 , A61K031/337
CPC分类号： C07D405/12 , C07D305/14 , C07D407/12 , C07D409/12 , C07D417/12
摘要： Taxanes having an ester substituent at C(7), a hydroxy substituent at C(10), and a range of C(2), C(9), C(14), and side chain substituents.
摘要翻译： C（7）具有酯取代基，C（10）羟基取代基，C（2），C（9），C（14）和侧链取代基的紫杉烷。

4. 发明申请

US20010051640A1 C7 carbamoyloxy substituted taxanes 失效
标题翻译： C7氨基甲酰氧基取代紫杉烷
公开(公告)号：US20010051640A1
公开(公告)日：2001-12-13
申请号：US09776494
申请日：2001-02-02
发明人： Robert A. Holton
IPC分类号： A61K031/397 , A61K031/38 , A61K031/337 , A61K031/4427 , C07D35/14
CPC分类号： C07D407/12 , C07D305/14 , C07D405/12 , C07D409/12
摘要： Taxanes having a carbamoyloxy substituent at C(7), a hydroxy substituent at C(10, and a range of C(2), C(9), C(14), and side chain substituents.
摘要翻译：在C（7）具有氨基甲酰氧基取代基的紫杉烷，C（10，C（2），C（9），C（14）和侧链取代基的羟基取代基。

5. 发明申请

US20020077341A1 C10 carbamoyloxy substituted taxanes 失效
标题翻译： C10氨基甲酰氧基取代紫杉烷
公开(公告)号：US20020077341A1
公开(公告)日：2002-06-20
申请号：US09775852
申请日：2001-02-02
发明人： Robert A. Holton , Weishuo Fang
IPC分类号： A61K031/4427 , A61K031/381 , A61K031/337
CPC分类号： A61K31/335 , A61K9/0019 , A61K9/08 , A61K47/10 , A61K47/44 , C07D305/14 , C07D405/12 , C07D407/12 , C07D409/12
摘要： Taxanes having a carbamoyloxy substituent at C(10), a hydroxy substituent at C(7), and a range of C(2), C(9), C(14), and side chain substituents.
摘要翻译：在C（10）具有氨基甲酰氧基取代基的紫杉烷，C（7）的羟基取代基，C（2），C（9），C（14）和侧链取代基的范围。

6. 发明申请

US20020065304A1 C7 carbonate substituted taxanes 失效
标题翻译： C7碳酸酯取代紫杉烷
公开(公告)号：US20020065304A1
公开(公告)日：2002-05-30
申请号：US09776137
申请日：2001-02-02
发明人： Robert A. Holton
IPC分类号： A61K031/397 , A61K031/4427 , A61K031/381 , A61K031/337
CPC分类号： A61K31/335 , C07D409/12
摘要： Taxanes having a carbonate substituent at C(7), a hydroxy substituent at C(10), and a range of C(2), C(9), C(14), and side chain substituents.
摘要翻译： C（7）具有碳酸酯取代基，C（10）羟基取代基，C（2），C（9），C（14）和侧链取代基的紫杉烷类。

7. 发明申请

US20010014689A1 2-aminopyridines containing fused ring substituents 失效
标题翻译：含有稠环取代基的2-氨基吡啶
公开(公告)号：US20010014689A1
公开(公告)日：2001-08-16
申请号：US09779318
申请日：2001-02-08
发明人： John A. Lowe III
IPC分类号： A61K031/4427 , A61K031/44 , C07D211/72
CPC分类号： C07D213/73
摘要： The present invention relates to 2-aminopyridine derivatives of the formula I: 1 or pharmaceutically acceptable salts thereof, wherein A and B are each independently H, or together, A and B form a ring fused to the phenyl ring, said ring being saturated or unsaturated and containing from 5 to 7 ring member atoms, where said ring member atoms may optionally comprise from 1 to 2 heteroatoms selected independently from the group consisting of N, O or S, provided that no two adjacent ring members are heteroatoms; X is oxygen or a single bond; Y is (C1-C6)alkyl; R1 is hydrogen, (C1-C6)alkyl or a (C1-C6 alkyl) group substituted with nullNR2R3 wherein R2 and R3 are either selected independently from the group consisting of H, alkyl, aryl, aralkyl or tetrahydronaphthalene, wherein said aryl group or said aryl moiety of said aralkyl group is phenyl or naphthyl, said alkyl group or said alkyl moiety of said aralkyl group contains from one to six carbon atoms and is straight-chained or branched, and said aryl group, said tetrahydronaphthalene or said aryl moiety of said aralkyl group is optionally substituted with from one to three of halogen, nitro, cyano, amino, (C1-C4)alkoxy and (C1-C4)alkylamino moieties, or R2 and R3 form, together with the nitrogen to which they are attached, a heterocyclic ring, or a cyclic or bicyclic ring which is saturated or unsaturated. The compounds of the invention have the ability to inhibit the activity of nitric oxide synthases (NOS), and hence, are useful in the treatment of diseases, conditions and disorders of the central nervous system, among others.
摘要翻译：本发明涉及式I的2-氨基吡啶衍生物或其药学上可接受的盐，其中A和B各自独立地为H，或者一起A和B形成与苯环稠合的环，所述环为饱和或不饱和的并且含有5至7个环成员原子，其中所述环成员原子可以任选地包含1至2个独立地选自N，O或S的杂原子，条件是不存在两个相邻的环成员是杂原子; X是氧或单键; Y是（C 1 -C 6）烷基; R 1是氢，（C 1 -C 6）烷基或被-NR 2 R 3取代的（C 1 -C 6烷基）基团，其中R 2和R 3独立地选自H，烷基，芳基，芳烷基或四氢萘，其中所述芳基或所述芳烷基的所述芳基部分是苯基或萘基，所述烷基或所述芳烷基的所述烷基部分含有1至6个碳原子并且是直链或支链的，并且所述芳基，所述四氢萘或所述芳基部分的所述芳烷基任选被1至3个卤素，硝基，氰基，氨基，（C 1 -C 4）烷氧基和（C 1 -C 4）烷基氨基部分取代，或者R 2和R 3与氮原子一起形成杂环，或饱和或不饱和的环状或双环。本发明的化合物具有抑制一氧化氮合酶（NOS）活性的能力，因此可用于治疗中枢神经系统的疾病，病症和病症等。

8. 发明申请

US20030125362A1 Synthesis of epothilones, intermediates thereto, analogues and uses thereof 有权
公开(公告)号：US20030125362A1
公开(公告)日：2003-07-03
申请号：US09808451
申请日：2001-03-14
发明人： Samuel J. Danishefsky , Peter Bertinato , Dai-Shi Su , Dong Fang Meng , Ting-Chao Chou , Ted Kamenecka , Erik J. Sorensen , Aaron Balog , Kenneth A. Savin
IPC分类号： A61K031/427 , A61K031/4427 , A61K031/4178 , A61K031/365 , C07D417/02 , C07D47/02
CPC分类号： A61K31/704 , A61K31/335 , A61K31/337 , A61K31/425 , A61K31/475 , A61K31/70 , A61K45/06 , C07C69/007 , C07D277/24 , C07D313/00 , C07D417/06 , C07D417/14 , C07D493/04 , C07F7/1804 , A61K2300/00
摘要： The present invention provides convergent processes for preparing epothilone A and B, desoxyepothilones A and B, and analogues thereof. Also provided are analogues related to epothilone A and B and intermediates useful for preparing same. The present invention further provides novel compositions based on analogues of the epothilones and methods for the treatment of cancer and cancer which has developed a multidrug-resistant phenotype.

9. 发明申请

US20020068755A1 C10 heterosubstituted acetate taxanes 失效
标题翻译： C10异取代乙酸酯紫杉烷
公开(公告)号：US20020068755A1
公开(公告)日：2002-06-06
申请号：US09775912
申请日：2001-02-02
发明人： Robert A. Holton
IPC分类号： A61K031/4427 , A61K031/381 , A61K031/337 , C07D35/14
CPC分类号： C07D405/12 , C07D305/14 , C07D407/12 , C07D409/12
摘要： Taxanes having a heterosubstituted acetate substituent at C(10), a hydroxy substituent at C(7), and a range of C(2), C(9), C(14), and side chain substituents.
摘要翻译： C（10）具有异构取代的乙酸酯取代基，C（7）的羟基取代基，C（2），C（9），C（14）和侧链取代基的紫杉烷。

10. 发明申请

US20020028798A1 Irrigation solution and method for inhibition of pain and inflammation 审中-公开
标题翻译：灌注溶液和抑制疼痛和炎症的方法
公开(公告)号：US20020028798A1
公开(公告)日：2002-03-07
申请号：US09839633
申请日：2001-04-20
申请人： Omeros Medical Systems
发明人： Gregory A. Demopulos , Pamela Pierce-Palmer , Jeffrey M. Herz
IPC分类号： A61K031/4427 , A61K031/4439 , A61K031/55
CPC分类号： A61K31/18 , A61K9/08 , A61K31/00 , A61K31/352 , A61K31/4045 , A61K31/4164 , A61K31/4168 , A61K31/4174 , A61K31/439 , A61K31/4406 , A61K31/4427 , A61K31/4439 , A61K31/444 , A61K31/465 , A61K31/48 , A61K31/498 , A61K31/506 , A61K31/538 , A61K31/55 , A61K31/675 , A61K38/1793 , A61K45/06 , A61K2300/00
摘要： A method and solution for perioperatively inhibiting a variety of pain and inflammation processes at wounds from general surgical procedures including oral/dental procedures. The solution preferably includes at least one pharmacological agent selected from the group consisting of a mitogen-activated protein kinase (MAPK) inhibitor, an null2-receptor agonist, a neuronal nicotinic acetylcholine receptor agonist, a cyclooxygenase-2 (COX-2) inhibitor, a soluble receptor and mixtures thereof, and optionally additional multiple pain and inflammation inhibitory agents at dilute concentration in a physiologic carrier, such as saline or lactated Ringer's solution. The solution is applied by continuous irrigation of a wound during a surgical procedure for preemptive inhibition of pain and while avoiding undesirable side effects associated with oral, intramuscular, subcutaneous or intravenous application of larger doses of the agents.
摘要翻译：一种围手术期抑制来自一般外科手术（包括口腔/牙科手术）的伤口的各种疼痛和炎症过程的方法和解决方案。该溶液优选包含至少一种选自丝裂原活化蛋白激酶（MAPK）抑制剂，α2-受体激动剂，神经元烟碱乙酰胆碱受体激动剂，环氧合酶-2（COX-2）抑制剂，可溶性受体及其混合物，以及任选地在生理载体例如盐水或乳酸林格溶液中稀释浓度的另外多种疼痛和炎症抑制剂。在外科手术过程中连续冲洗伤口以解决疼痛的预防性作用，同时避免与口服，肌肉内，皮下或静脉内施用较大剂量的药剂相关的不良副作用。

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