专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

1. 发明授权

US12006294B2 Therapeutic compounds 有权
公开(公告)号：US12006294B2
公开(公告)日：2024-06-11
申请号：US16429507
申请日：2019-06-03
申请人： REGENTS OF THE UNIVERSITY OF MINNESOTA
发明人： Swati S. More , Robert Vince
IPC分类号： C07D233/64 , A61K31/167 , A61P5/48 , A61P25/16 , A61P35/00 , C07C279/06 , C07C279/08 , C07C279/18 , C07C279/22 , C07C281/14 , C07C281/16 , C07C281/18 , C07C335/04 , C07C335/12 , C07C335/40 , C07D213/61 , C07D231/38 , C07D233/44 , C07D233/50 , C07D233/52 , C07D239/06 , C07D239/18 , C07D239/22 , C07D239/47
CPC分类号： C07D233/44 , A61P5/48 , A61P25/16 , A61P35/00 , C07C279/06 , C07C279/08 , C07C279/18 , C07C279/22 , C07C281/14 , C07C281/16 , C07C281/18 , C07C335/04 , C07C335/12 , C07C335/40 , C07D213/61 , C07D231/38 , C07D233/50 , C07D233/52 , C07D233/64 , C07D239/06 , C07D239/18 , C07D239/22 , C07D239/47 , A61K31/167
摘要： The invention provides methods for producing analgesia in an animal comprising administering to the animal a compound of the formula Ia′, Ib′, Ic′, and Id′:

and pharmaceutically acceptable salts thereof, wherein the variables A, R6, R7, R8, R9, Rx, L, X, Y, and Z have the meaning as described herein.

2. 发明申请

US20220213081A1 GEM-DISUBSTITUTED PYRROLIDINES, PIPERAZINES, AND DIAZEPANES, AND COMPOSITIONS AND METHODS OF MAKING THE SAME 有权
公开(公告)号：US20220213081A1
公开(公告)日：2022-07-07
申请号：US17566915
申请日：2021-12-31
申请人： California Institute of Technology
发明人： Brian M. Stoltz , Alexander W. Sun , Stephan N. Hess , Carina I. Jette , Irina Geibel , Shoshana Bachman , Masaki Hayashi , Hideki Shimizu , Jeremy B. Morgan , Shunya Sakurai , Zachary P. Sercel
IPC分类号： C07D413/14 , C07D207/26 , C07D243/08 , C07D239/06 , C07D507/00 , C07D241/08
摘要： Described here are transition metal-catalyzed enantioselective arylation and vinylation reactions of α-substituted lactams, such as γ-lactams. The use of various electrophiles and ligands are described, and result in the construction of α-quaternary centers in good yields (up to 91% yield) and high enantioselectivities (up to 97% ee).

3. 发明申请

US20210213039A1 COMPOSITION CONTAINING ECTOINE OR HYDROXYECTOINE AS AN ACTIVE SUBSTANCE FOR PROMOTING THE REGENERATION OF INJURED BODY TISSUE 有权
公开(公告)号：US20210213039A1
公开(公告)日：2021-07-15
申请号：US17218814
申请日：2021-03-31
申请人： Bitop AG
发明人： Andreas Bilstein , Olaf Scherner , Georg Lentzen
IPC分类号： A61K31/7032 , A61L26/00 , A61K31/505 , A61K45/06 , C07D239/06 , C07H15/04
摘要： The invention relates to a composition containing as active agent ectoine, hydroxyectoine, glucosylglycerol and/or salts, esters or amides of these compounds for promoting the regeneration of injured body tissue. The invention has special significance for the treatment of chronic wounds or ulcers.

4. 发明授权

US10829501B2 Spiroheptane salicylamides and related compounds as inhibitors of ROCK 有权
公开(公告)号：US10829501B2
公开(公告)日：2020-11-10
申请号：US16739363
申请日：2020-01-10
申请人： BRISTOL-MYERS SQUIBB COMPANY
发明人： Leon M. Smith, II , Vladimir Ladziata , Indawati DeLucca , Donald J. P. Pinto , Michael J. Orwat , Andrew K. Dilger , Kumar Balashanmuga Pabbisetty , Wu Yang , Scott A. Shaw , Peter W. Glunz , Manoranjan Panda
IPC分类号： C07D513/04 , C07D213/64 , C07D231/18 , C07D471/04 , C07D471/12 , C07D413/12 , C07D401/12 , C07D231/54 , C07D401/14 , C07D231/12 , A61P15/10 , A61P9/10 , C07D239/06
摘要： The present invention provides compounds of Formula (I): or stereoisomers, tautomers, or pharmaceutically-acceptable salts thereof, wherein all the variables are as defined herein. These compounds are selective ROCK inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating cardiovascular, smooth muscle, oncologic, neuropathologic, autoimmune, fibrotic, and/or inflammatory disorders using the same.

5. 发明授权

US10647681B2 Amidine catalyst for curable compositions 有权
公开(公告)号：US10647681B2
公开(公告)日：2020-05-12
申请号：US15580967
申请日：2016-06-21
申请人： SIKA TECHNOLOGY AG
发明人： Rita Cannas , Urs Burckhardt
IPC分类号： C07D239/06 , C08G77/38 , C09D183/06 , C09J183/06
摘要： The present invention relates to an amidine of the formula (I) and its use as a catalyst for crosslinking a curable composition. The amidine of the formula (I) contains at least one aliphatic amidine group. It is substantially odorless and nonvolatile at room temperature and accelerates the crosslinking of curable compositions very efficiently, without impairing the storage stability of the compositions. It is particularly suitable for compositions based on polymers containing silane groups, with which it is compatible, as a result of which such compositions do not have a tendency to separation or migration or evaporation of the catalyst.

6. 发明授权

US10352857B2 Use of penta-substituted tetrahydropyrimidines in preparation of thermo-sensitive fluorescent materials 有权
公开(公告)号：US10352857B2
公开(公告)日：2019-07-16
申请号：US15518246
申请日：2016-04-05
申请人： SOUTHERN MEDICAL UNIVERSITY
发明人： Qiuhua Zhu
IPC分类号： G01N21/64 , C07D239/06 , C09K11/06 , G01K11/00 , C09K9/02 , G01K11/20
摘要： The present invention provides use of penta-substituted tetrahydropyrimidines in preparation of thermo-sensitive fluorescent materials. Said penta-substituted tetrahydropyrimidine compounds have linear temperature dependence of red-edge excitation wavelength (LTDREEW). When different excitation wavelengths are chosen, such compounds present fluorescence color and/or fluorescence on-off switch in different temperature ranges. Also their fluorescence intensity ratios or fluorescence intensities exhibit good linear relation or power function relation to temperature, which can be used as the thermo-sensitive fluorescent materials with high sensitivity and wide temperature range (0-450 K).

7. 发明授权

US09751831B2 Blood brain barrier-penetrating oximes for cholistenerases reactivation 有权
公开(公告)号：US09751831B2
公开(公告)日：2017-09-05
申请号：US13994682
申请日：2011-12-16
申请人： John R. Cashman , Jarosiaw Kalisiak
发明人： John R. Cashman , Jarosiaw Kalisiak
IPC分类号： C07D249/04 , C07D239/06 , C07D233/24 , C07C251/40 , C07C279/12 , C07C257/12 , C07C257/18 , C07C257/14
CPC分类号： C07C251/40 , C07C257/12 , C07C257/14 , C07C257/18 , C07C279/12 , C07D233/24 , C07D239/06 , C07D249/04
摘要： The invention describes pharmaceutical agents capable of crossing the blood brain barrier to protect against organophosphate pesticides and nerve agents or other electrophiles by reactivating inhibited cholinesterase (i.e., acetylcholinesterase and butyrylcholinesterase) and other proteins in the peripheral and central nervous system.

8. 发明申请

US20160039857A1 ANTIBACTERIAL COMPOUNDS TARGETING ISOPRENOID BIOSYNTHESIS 有权
标题翻译：抗真菌化合物对异丙酚生物合成
公开(公告)号：US20160039857A1
公开(公告)日：2016-02-11
申请号：US14649153
申请日：2013-12-04
申请人： THE BOARD OF TRUSTEES OF THE UNIVERSITY OF ILLINOIS , THE REGENTS OF THE UNIVERSITY OF CALIFORNIA
发明人： Wei Zhu , Steffen Lindert , Yonghui Zhang , William Sinko , Kai Li , James Andrew McCammon , Eric Oldfield
IPC分类号： C07H15/26 , C07D233/24 , A61K31/4178 , A61K31/7056 , C07H15/203 , A61K31/506 , C07D243/04 , A61K31/551 , A61K31/7034 , A61K31/43 , C07D239/06
CPC分类号： C07H15/26 , A61K31/167 , A61K31/4178 , A61K31/43 , A61K31/4439 , A61K31/506 , A61K31/551 , A61K31/7034 , A61K31/7056 , C07D209/08 , C07D233/24 , C07D239/06 , C07D239/28 , C07D243/04 , C07H15/203
摘要： With the rise in resistance to antibiotics such as methicillin, there is a need for new drugs. The invention provides small molecules that inhibit cellular drug targets such as UPPS and FPPS by interacting with binding pockets, thereby preventing enzyme function. Compounds described herein are also active against Staphylococcus aureus (MIC90˜0.25 μg/mL), can potently synergize with methicillin (fractional inhibitory concentration index=0.25), and are protective in a mouse infection model. The invention therefore provides numerous compounds for anti-bacterial treatments and for restoring sensitivity to drugs such as methicillin, using combination therapies.
摘要翻译：随着抗生素如甲氧西林的抗药性上升，需要新药。本发明提供了通过与结合袋相互作用来抑制细胞药物靶标如UPPS和FPPS的小分子，从而防止酶功能。本文所述的化合物对金黄色葡萄球菌（MIC90〜0.25μg/ mL）也具有活性，可以与甲氧西林（分数抑制浓度指数= 0.25）有效协同，并且在小鼠感染模型中是保护性的。因此，本发明提供了许多用于抗菌处理的化合物，并且使用联合疗法来恢复药物如甲氧西林的敏感性。

9. 发明申请

US20100297034A1 OSMOLYTE-CONTAINING PREPARATION FOR USE IN CASE OF DRY MUCOUS MEMBRANES 审中-公开
标题翻译：用于干燥密封膜的含OSMOLYTE的制备方法
公开(公告)号：US20100297034A1
公开(公告)日：2010-11-25
申请号：US12740021
申请日：2008-10-29
申请人： Hans Bernd Schmittmann
发明人： Hans Bernd Schmittmann
IPC分类号： A61K36/82 , A61K31/505 , C07D239/06 , C07D243/04 , C07F9/06 , C07C57/02 , A61K9/12 , A61P43/00
CPC分类号： A61K31/505 , A61K31/205 , A61K31/66
摘要： The present invention relates to osmolyte-containing preparations for the local treatment of dry mucous membranes. It describes the use of osmolytes for the production of a medicament, medical product or cosmetic product for the prevention, therapy and/or care of dry mucous membranes. The present invention relates to topical compositions based on osmolytes to which sodium chloride and/or moisturizers can optionally be added. The group of osmolytes proposed by the invention embraces various low-molecular substances, in particular ectoine, homoectoine, hydroxyectoine, di-myo-inositol phosphate (DIP), cyclic 2,3-diphosphoglycerate (cDPG), 1,1-di-glycerol phosphate (DGP), β-mannosylglycerate (Firoin), β-mannosylglyceramide (Firoin-A), di-mannosyl di-inositol phosphate (DMIP), glucosylglycerol and/or a derivative, e.g. an acid, salt or ester, of these compounds.
摘要翻译：本发明涉及用于局部治疗干粘膜的含有渗透液的制剂。它描述了渗透剂用于生产用于预防，治疗和/或护理干性粘膜的药物，医疗产品或化妆品的用途。本发明涉及可以任选地加入氯化钠和/或保湿剂的基于渗透剂的局部组合物。本发明提出的渗透剂组包括各种低分子物质，特别是ectoine，homoectoine，羟基洗涤剂，二肌醇磷酸酯（DIP），环状2,3-二磷酸甘油酸酯（cDPG），1,1-二甘油磷酸盐（DGP），甘露糖基甘油酸酯（Firoin），甘露糖基甘油酰胺（Firoin-A），二甘油糖基二 - 肌醇磷酸酯（DMIP），葡糖基甘油和/或衍生物，例如这些化合物的酸，盐或酯。

10. 发明授权

US06881735B2 Sulfur substituted sulfonylaminocarboxylic acid N-arylamides, their preparation, their use and pharmaceutical preparations comprising them 有权
标题翻译：硫取代磺酰氨基羧酸N-芳基酰胺，其制备方法及其应用和包含它们的药物制剂
公开(公告)号：US06881735B2
公开(公告)日：2005-04-19
申请号：US09994730
申请日：2001-11-28
申请人： Ursula Schindler , Karl Schönafinger , Hartmut Strobel
发明人： Ursula Schindler , Karl Schönafinger , Hartmut Strobel
IPC分类号： A61K31/18 , A61K31/275 , A61K31/38 , A61K31/381 , A61K31/40 , A61K31/401 , A61K31/403 , A61K31/404 , A61K31/415 , A61K31/4166 , A61K31/4184 , A61K31/42 , A61K31/426 , A61K31/428 , A61K31/435 , A61K31/44 , A61K31/4402 , A61K31/4409 , A61K31/4427 , A61K31/4433 , A61K31/4436 , A61K31/4439 , A61K31/445 , A61K31/4453 , A61K31/4462 , A61K31/4535 , A61K31/454 , A61K31/4545 , A61K31/4725 , A61K31/495 , A61K31/496 , A61K31/505 , A61K31/506 , A61K31/5355 , A61K31/5375 , A61K31/5377 , A61K31/54 , A61K31/541 , A61K31/551 , A61P1/16 , A61P3/10 , A61P7/02 , A61P9/00 , A61P9/02 , A61P9/04 , A61P9/10 , A61P9/12 , A61P11/06 , A61P13/12 , A61P15/10 , A61P25/28 , A61P43/00 , C07C311/21 , C07C311/46 , C07C311/51 , C07C311/58 , C07C317/40 , C07C323/41 , C07C323/42 , C07C323/52 , C07C323/60 , C07C331/12 , C07D207/12 , C07D207/16 , C07D207/48 , C07D209/10 , C07D209/14 , C07D211/54 , C07D211/96 , C07D213/42 , C07D213/71 , C07D213/78 , C07D213/80 , C07D213/82 , C07D215/36 , C07D221/20 , C07D231/18 , C07D231/42 , C07D233/42 , C07D233/84 , C07D235/18 , C07D235/28 , C07D239/06 , C07D239/42 , C07D243/08 , C07D261/10 , C07D261/16 , C07D265/30 , C07D277/04 , C07D277/10 , C07D277/20 , C07D277/36 , C07D277/46 , C07D277/54 , C07D277/64 , C07D295/08 , C07D295/22 , C07D295/26 , C07D333/34 , C07D333/38 , C07D333/40 , C07D333/62 , C07D333/70 , C07D401/12 , C07D409/12 , C07D413/12 , C07D279/12
CPC分类号： C07C311/21 , C07C311/46 , C07C311/51 , C07C311/58 , C07C317/40 , C07C323/42 , C07C323/52 , C07C323/60 , C07C331/12 , C07C2601/02 , C07C2601/14 , C07C2602/04 , C07C2602/08 , C07D207/12 , C07D207/16 , C07D207/20 , C07D207/48 , C07D209/10 , C07D209/14 , C07D211/46 , C07D211/54 , C07D211/62 , C07D211/96 , C07D213/71 , C07D213/78 , C07D213/80 , C07D213/82 , C07D215/36 , C07D221/20 , C07D231/18 , C07D231/38 , C07D231/42 , C07D233/84 , C07D235/18 , C07D239/06 , C07D239/26 , C07D239/42 , C07D243/08 , C07D261/10 , C07D261/16 , C07D265/30 , C07D277/04 , C07D277/36 , C07D277/46 , C07D277/52 , C07D277/54 , C07D277/64 , C07D279/12 , C07D295/26 , C07D333/34 , C07D333/38 , C07D333/40 , C07D401/12 , C07D413/12 , C07D491/10
摘要： The present invention relates to compounds of the formula I wherein A1, A2, R1, R2, R3, X and n are as defined in the claims, which are valuable pharmaceutically active compounds for the therapy and prophylaxis of diseases, for example of cardiovascular diseases such as hypertension, angina pectoris, cardiac insufficiency, thromboses or atherosclerosis. The compounds of the formula I are capable of modulating the body's production of cyclic guanosine monophosphate (cGMP) and are generally suitable for the therapy and prophylaxis of diseases which are associated with a disturbed cGMP balance. The invention furthermore relates to processes for preparing compounds of the formula I, to their use for the therapy and prophylaxis of the abovementioned diseases and for preparing pharmaceuticals for this purpose, and to pharmaceutical preparations which comprise compounds of the formula I.
摘要翻译：本发明涉及式I化合物，其中A 1，A 2，R 1，R 2， R 3，X和n如权利要求中所定义，其是用于治疗和预防疾病的有价值的药学活性化合物，例如心血管疾病如高血压，心绞痛，心功能不全，血栓形成或动脉粥样硬化。式I的化合物能够调节身体的环鸟苷酸（cGMP）的产生，并且通常适用于治疗和预防与扰乱的cGMP平衡相关的疾病。本发明还涉及制备式I化合物的方法，其用于治疗和预防上述疾病和用于制备用于此目的的药物以及包含式I化合物的药物制剂。

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式