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11. 发明申请

US20050119257A1 Cyclic sulfone containing retroviral protease inhibitors 失效
公开(公告)号：US20050119257A1
公开(公告)日：2005-06-02
申请号：US10932331
申请日：2004-09-02
申请人： Deborah Bertenshaw , Daniel Getman , Robert Heintz , John Talley , Kathryn Reed , Robert Chrusciel , Michael Clare
发明人： Deborah Bertenshaw , Daniel Getman , Robert Heintz , John Talley , Kathryn Reed , Robert Chrusciel , Michael Clare
IPC分类号： A61K31/38 , A61K31/381 , A61K31/382 , A61K31/415 , A61K31/425 , A61K31/4433 , A61K31/445 , A61K31/54 , A61P31/12 , A61P43/00 , C07D279/12 , C07D283/00 , C07D333/48 , C07D335/02 , C07D409/12 , C07D417/12 , C07D521/00 , C07D417/02 , C07D49/02
CPC分类号： C07D333/48 , C07D231/12 , C07D233/56 , C07D249/08 , C07D279/12 , C07D335/02 , C07D409/12
摘要： The present invention relates to cyclic sulfone moiety-containing hydroxyethylamine protease inhibitor compounds and pharmaceutical or method of use therefor, particularly as an inhibitor of HIV protease.

12. 发明授权

US5644054A Process for preparing diltiazem 失效
标题翻译：制备地尔硫卓的方法
公开(公告)号：US5644054A
公开(公告)日：1997-07-01
申请号：US601182
申请日：1996-02-14
申请人： Martti Hytonen
发明人： Martti Hytonen
IPC分类号： C07C281/10 , A61K31/55 , A61K31/554 , A61P9/00 , A61P9/06 , A61P9/14 , C07D281/10 , C07D281/00 , C07D283/00 , C07D285/00
CPC分类号： C07D281/10
摘要： A process is provided for preparing cis-(+)-hydroxy-5-[2-(dimethylamine)ethyl]-2,3-dihydro-2-(4-methoxyphenyl)-benzothiazepin-4(5H)-one that is a useful intermediate in the preparation of diltiazem. It has been found that the requisite N-alkylation reaction proceeds rapidly and with an excellent yield when the solvent is a mixture of toluene and N-methylpyrrolidin-2-one and the base is finely-divided sodium carbonate under anhydrous conditions. Such diltiazem commonly is used in the treatment of angina pectoris.
摘要翻译：提供了制备顺式 - （+） - 羟基-5- [2-（二甲基胺）乙基] -2,3-二氢-2-（4-甲氧基苯基） - 苯并硫氮杂-4（5H） - 酮的方法，其为在制备地尔硫卓时有用的中间体。已经发现，当溶剂是甲苯和N-甲基吡咯烷-2-酮的混合物时，所需的N-烷基化反应快速进行，产率优异，碱是在无水条件下细碎的碳酸钠。这种地尔硫通常用于治疗心绞痛。

13. 发明授权

US5559229A Method for the manufacture of benzothiazepine 失效
标题翻译：苯并硫氮杂的制备方法
公开(公告)号：US5559229A
公开(公告)日：1996-09-24
申请号：US456761
申请日：1995-06-01
申请人： Keshava Murthy , Gamini Weeratunga , Burchat Andrew
发明人： Keshava Murthy , Gamini Weeratunga , Burchat Andrew
IPC分类号： C07D281/10 , C07D281/00 , C07D283/00 , C07D285/00
CPC分类号： C07D281/10
摘要： A process for the manufacture of Diltiazem or deacetyl-Diltiazem, which comprises the use of MIBK as solvent and NaOH as base.
摘要翻译：一种制备地尔硫卓或脱乙酰基地尔硫卓的方法，其包括使用MIBK作为溶剂和NaOH作为碱。

14. 发明授权

US5554663A .alpha.-aminoacetophenones as photoinitiators 失效
公开(公告)号：US5554663A
公开(公告)日：1996-09-10
申请号：US466847
申请日：1995-06-06
申请人： Vincent Desobry , Kurt Dietliker , Rinaldo H usler , Werner Rutsch , Manfred Rembold , Franciszek Sitek
发明人： Vincent Desobry , Kurt Dietliker , Rinaldo H usler , Werner Rutsch , Manfred Rembold , Franciszek Sitek
IPC分类号： C07D209/12 , C07C67/00 , C07C209/86 , C07C213/00 , C07C219/02 , C07C219/04 , C07C225/16 , C07C225/22 , C07C229/06 , C07C229/14 , C07C229/16 , C07C229/34 , C07C229/52 , C07C233/36 , C07C253/00 , C07C255/56 , C07C313/00 , C07C317/32 , C07C317/36 , C07C323/23 , C07C323/25 , C07C323/31 , C07C323/32 , C07C323/65 , C07D209/86 , C07D219/02 , C07D219/04 , C07D223/22 , C07D263/32 , C07D263/56 , C07D265/30 , C07D265/36 , C07D265/38 , C07D279/18 , C07D283/00 , C07D295/02 , C07D295/10 , C07D295/104 , C07D295/112 , C07D295/12 , C07D307/91 , C07F7/18 , C08F2/46 , C08F2/50 , C09D4/00 , C09D5/32 , C09D7/12 , C09D11/10 , G03F7/031
CPC分类号： C07D295/112 , C07D209/86 , C07D295/104 , C08F2/50 , G03F7/031
摘要： Compounds of the formula I, II, III and IIIa ##STR1## in which Ar.sup.1 is an unsubstituted or substituted aromatic radical and at least one of the radicals R.sup.1 and R.sup.2 is an alkenyl, cycloalkenyl or arylmethyl group, are effective photoinitiators for photopolymerization of unsaturated compounds. They are particularly suitable for photocuring of pigmented systems.

15. 发明授权

US4816482A Radioprotective agents having an amino-thioalkyl structure 失效
标题翻译：具有氨基 - 硫烷基结构的放射防护剂
公开(公告)号：US4816482A
公开(公告)日：1989-03-28
申请号：US704548
申请日：1985-02-22
申请人： Joel Oiry , Jean-Louis Imbach
发明人： Joel Oiry , Jean-Louis Imbach
IPC分类号： A61K31/16 , A61K31/255 , A61K31/265 , A61K31/395 , A61K31/66 , A61K38/00 , A61P35/00 , A61P43/00 , C07C67/00 , C07C313/00 , C07C323/59 , C07C325/00 , C07C327/20 , C07C327/38 , C07C329/00 , C07C333/02 , C07C333/14 , C07C335/30 , C07C335/32 , C07C381/02 , C07D283/00 , C07F9/165 , C07F9/22 , C07K5/00 , C07K5/06
CPC分类号： C07F9/1651 , C07C335/32 , C07K5/06026
摘要： A pharmaceutical composition effective in the protection of normal tissues against radiation induced damage comprising administration a compound of the formulaR.sub.1 --CO--NR.sub.3 --/A/--S--R.sub.2in which R.sub.1 is a radical corresponding to an amino acid R.sub.1 --COOH, /A/ is a C.sub.2 or C.sub.3 alkylene radical which can be substituted with a C.sub.1 to C.sub.3 alkyl radical, or with a hydroxy or hydroxycarbonyl radical or a --COR radical where R is an amino or --NH--CH.sub.2 --CO.sub.2 H radical, R.sub.2 is an acyl radical which protects the thiol group and which liberates the thiol group in vivo, R.sub.3 is a hydrogen, and also the salts of this compound with pharmaceutically acceptable acids.
摘要翻译：一种有效保护正常组织免受辐射诱发的损伤的药物组合物，其包括施用式R1-CO-NR3- / A / -S-R2的化合物，其中R1是对应于氨基酸R1-COOH的基团， A /是可以被C1至C3烷基取代的C2或C3亚烷基，或与羟基或羟基羰基或-COR基团取代，其中R是氨基或-NH-CH2-CO2H基，R2是保护硫醇基并在体内释放硫醇基的酰基，R3是氢，以及该化合物与药学上可接受的酸的盐。

16. 发明授权

US4788206A Pentadieneamides 失效
标题翻译：戊二酰胺
公开(公告)号：US4788206A
公开(公告)日：1988-11-29
申请号：US72389
申请日：1987-07-10
申请人： Robert W. Guthrie , Richard W. Kierstead , Jefferson W. Tilley
发明人： Robert W. Guthrie , Richard W. Kierstead , Jefferson W. Tilley
IPC分类号： C07D213/38 , A61K31/16 , A61K31/34 , A61K31/35 , A61K31/38 , A61K31/40 , A61K31/415 , A61K31/42 , A61K31/425 , A61K31/435 , A61K31/44 , A61K31/4402 , A61K31/4406 , A61K31/4409 , A61K31/4418 , A61K31/47 , A61K31/472 , A61K31/495 , A61K31/535 , A61K31/54 , A61P7/02 , C07C233/38 , C07D207/335 , C07D213/40 , C07D213/56 , C07D217/02 , C07D217/14 , C07D217/16 , C07D227/00 , C07D247/00 , C07D269/00 , C07D283/00 , C07D409/12 , C07D521/00 , C07D213/00
CPC分类号： C07D409/12 , C07D213/56 , C07D217/02 , C07D217/16
摘要： Compounds of the formula ##STR1## Y is O ir S, *A is paraphenylene or *----(CH.sub.2)n----(X).sub.m --(CH.sub.2).sub.r ----, X is O, S or --CH.dbd.CH--, n or r, independently, are integers from 0 to 3, s is an integer from 0 to 1, m is an integer from 0 to 1, provided that when m is 1, n+s must be at least 2, R.sub.1 and R.sub.2, independently, are hydrogen, lower alkyl, cycloalkyl, lower alkenyl, Het, aryl, R.sub.3, R.sub.4 and R.sub.8, independently, are hydrogen, lower alkyl, aryl, R.sub.5 and R.sub.6, independently, are hydrogen or lower alkyl, R.sub.7 is hydrogen, lower alkyl, cycloalkyl, Het-lower alkyl or aryl, Het is a monocyclic 5- or 6-membered hetero aromatic or a bicyclic heteroaromatic radical containing one or two hetero atoms selected from nitrogen, oxygen and sulfur, which radical may be substituted by lower alkyl, halogen or aryl, and the asterisk denotes the point of attachment,and when R.sub.6 and R.sub.7 are different, their enantiomers and racemic mixtures thereof, when R.sub.1 and R.sub.2 are different, their geometric isomers, and pharmaceutically acceptable acid addition salts thereof, are described.The compounds of formula I exhibit activity as platelet activating factor (PAF) antagonists and are, therefore, useful in disease states characerized by excess platelet activating factor or for the prevention and treatment of cardiovascular disease, pulmonary diseases, immunological disorders, inflammatory diseases, dermatological disorders, shock or transplant rejection.
摘要翻译：式（I）的化合物是O，S是对亚苯基或* - （CH 2）n - （X）m - （CH 2）r - ，X是O，S或-CH = CH- ，n或r独立地为0至3的整数，s为0至1的整数，m为0至1的整数，条件是当m为1时，n + s必须至少为2，R1和 R2独立地是氢，低级烷基，环烷基，低级烯基，Het，芳基，R3，R4和R8独立地是氢，低级烷基，芳基，R5和R6独立地是氢或低级烷基，R7是氢，低级烷基，环烷基，Het-低级烷基或芳基，Het是含有一个或两个选自氮，氧和硫的杂原子的单环五元或六元杂芳族或双环杂芳族基团，该基团可以被低级烷基，卤素或芳基，星号表示连接点，当R 6和R 7不同时，当R 1和R 2不同时，它们的对映异构体和外消旋混合物，它们的几何异构体和药学上可接受的描述了它们的酸加成盐。式I的化合物表现出作为血小板活化因子（PAF）拮抗剂的活性，因此可用于由过量血小板活化因子引起的疾病状态或用于预防和治疗心血管疾病，肺部疾病，免疫学疾病，炎性疾病，皮肤病学疾病，休克或移植排斥。

17. 发明授权

US4644006A Substituted 3,4-diamino-1,2,5-thiadiazoles having histamine H.sub.2 -receptor antagonist activity 失效
公开(公告)号：US4644006A
公开(公告)日：1987-02-17
申请号：US623588
申请日：1984-06-22
申请人： Aldo A. Algieri , Ronnie R. Crenshaw
发明人： Aldo A. Algieri , Ronnie R. Crenshaw
IPC分类号： C07D239/47 , A61K31/425 , A61K31/426 , A61K31/433 , A61K31/496 , A61K31/505 , A61P1/04 , A61P43/00 , C07D233/64 , C07D239/42 , C07D263/48 , C07D277/20 , C07D277/48 , C07D283/00 , C07D285/10 , C07D417/12 , C07D417/14 , A61K31/41
CPC分类号： C07D285/10 , C07D277/48 , C07D417/12
摘要： Histamine H.sub.2 -receptor antagonists of the formula ##STR1## wherein A, m, Z, n and R.sup.1 are as defined herein, and their nontoxic pharmaceutically acceptable salts are novel anti-ulcer agents which are prepared by ring closure of a substituted ethanediimidamide of the formula ##STR2##

18. 发明授权

US4065459A Process for the preparation of thieno(3,2-c) pyridine and derivatives thereof 失效
标题翻译：噻吩并（3,2-c）吡啶及其衍生物的制备方法
公开(公告)号：US4065459A
公开(公告)日：1977-12-27
申请号：US655966
申请日：1976-02-06
申请人： Alan Heymes , Jean-Pierre Maffrand
发明人： Alan Heymes , Jean-Pierre Maffrand
IPC分类号： C07D513/04 , A61K20060101 , A61K31/425 , A61K31/545 , A61K31/546 , A61P31/04 , C07D20060101 , C07D495/04 , C07D501/00 , C07D501/04 , C07D501/20 , C07D501/22 , C07D501/24 , C07D501/34 , C07D501/36 , C07D501/56 , C07D501/60 , C07D519/06 , C07D283/00
CPC分类号： C07D495/04 , C07D501/20
摘要： This invention relates to a process for the preparation of compounds having the formula: ##STR1## in which R.sub.1 is H or lower alkyl and R.sub.2 is H or lower alkyl, or phenyl or benzyl optionally substituted with at least one halogen or a lower alkyl, lower alkoxy, trifluoromethyl or nitro group.According to this method, a compound of the formula: ##STR2## in which R.sub.1 and R.sub.2 are as defined above and R.sub.3 is H or optionally substituted alkyl or benzyl, is reacted with a derivative Hal--SO.sub.2 --R (III) in which Hal is halogen and R is optionally substituted alkyl, aryl or aralkyl, to give a derivative of the formula: ##STR3## in which the various symbols have the above-defined meanings, and the sulfonated derivative of the formula (IV) is heated in the presence of an acid, to give the compound of the formula (I).
摘要翻译：本发明涉及一种制备具有下式的化合物的方法：其中R 1为H或低级烷基且R 2为H或低级烷基，或任选被至少一个卤素取代的苯基或苄基，低级烷基，低级烷氧基，三氟甲基或硝基。

19. 发明授权

US09873671B2 Azepane derivatives and methods of treating hepatitis B infections 有权
公开(公告)号：US09873671B2
公开(公告)日：2018-01-23
申请号：US15277421
申请日：2016-09-27
申请人： Novira Therapeutics, Inc.
发明人： George D. Hartman , Scott Kuduk
IPC分类号： C07D223/08 , A61K31/55 , A61K45/06 , C07D267/10 , A61K31/553 , C07D223/32 , A61K31/439 , A61K31/551 , C07D221/22 , C07D223/06 , C07D243/08 , A61K38/21 , A61K47/48 , A61K31/554 , C07D283/00 , C07D295/26 , C07D403/12
CPC分类号： C07D223/08 , A61K31/439 , A61K31/55 , A61K31/551 , A61K31/553 , A61K31/554 , A61K38/21 , A61K45/06 , A61K47/60 , C07D221/22 , C07D223/06 , C07D223/32 , C07D243/08 , C07D267/10 , C07D283/00 , C07D295/26 , C07D403/12 , A61K2300/00
摘要： Provided herein are compounds useful for the treatment of HBV infection in a subject in need thereof, pharmaceutical compositions thereof, and methods of inhibiting, suppressing, or preventing HBV infection in the subject.

20. 发明申请

US20170305861A1 HETEROARYL COMPOUNDS COMPRISING NITROGEN AND USE THEREOF 审中-公开
公开(公告)号：US20170305861A1
公开(公告)日：2017-10-26
申请号：US15496631
申请日：2017-04-25
申请人： ImmunoMet Therapeutics, Inc
发明人： Sung Wuk Kim , Hong Woo Kim , SangHee Yoo , Hyunwook Kim , Hye Jin Heo , Hong Bum Lee , Jiae Kook , Young Woo Lee
IPC分类号： C07D227/02 , A61K45/06 , C07C11/02 , C07D283/00
CPC分类号： C07D227/02 , A61K45/06 , A61P35/00 , C07C11/02 , C07D283/00
摘要： The present invention relates to heteroaryl compounds comprising nitrogen and use thereof, and more specifically to compounds which exhibit a remarkable effect on inhibiting proliferation of cancer cells and metastasis and recurrence of cancer, a preparation method of the same, and a pharmaceutical composition comprising the same as an active ingredient.The compounds according to the present invention exhibit a remarkable effect on inhibiting proliferation of cancer cells and metastasis and recurrence of cancer with a reduced dose compared to that of existing drugs. Accordingly, the compounds can be effectively used for treating various types of cancer, such as uterine cancer, breast cancer, gastric cancer, brain cancer, rectal cancer, colorectal cancer, lung cancer, skin cancer, blood cancer, pancreatic cancer, renal cancer, prostate cancer, bladder cancer, and liver cancer, and for inhibiting proliferation of cancer cells and metastasis of cancer.

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