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1. 发明申请

WO2022204125A1 POLYMORPHIC FORMS OF N-(TRANS-4-HYDROXYCYCLOHEXYL)-6-PHENYLHEXANAMIDE 审中-公开
公开(公告)号：WO2022204125A1
公开(公告)日：2022-09-29
申请号：PCT/US2022/021321
申请日：2022-03-22
申请人： MITOCHONDRIA EMOTION, INC. , DORN, Gerald, W.
发明人： DORN, Gerald, W.
IPC分类号： C07C213/10 , C07C215/42
摘要： The present disclosure relates to crystalline polymorphs of N-(trans-4-hydroxycyclohexyl)-6-phenylhexanamide, and to pharmaceutical compositions that may be prepared from the polymorphs. The present disclosure also relates to uses of the crystalline polymorphs, e.g., in treating or preventing a disease, disorder, or condition.

2. 发明申请

WO2011084273A1 AMINOALCOHOL COMPOUNDS, PRECURSORS, AND METHODS OF PREPARATION AND USE 审中-公开
标题翻译：氨基醇化合物，前驱体和制备和使用方法
公开(公告)号：WO2011084273A1
公开(公告)日：2011-07-14
申请号：PCT/US2010/058547
申请日：2010-12-01
申请人： DOW GLOBAL TECHNOLOGIES LLC , ANGUS CHEMICAL COMPANY , TOMLINSON, Ian , PEERA, Asghar , GREEN, George
发明人： TOMLINSON, Ian , PEERA, Asghar , GREEN, George
IPC分类号： C07C215/10 , C07C215/18 , C07C215/42 , C07C215/08 , C07D303/08
CPC分类号： C07D303/08 , C07C215/08 , C07C215/14 , C07C215/42 , C08K5/17 , C09D5/024 , C09D7/63
摘要： Provided are aminoalcohol compounds for use as neutralizing agents for paints and coatings. The compounds are of the formula (I): or salt thereof, wherein R 1 , R 2 , R 3 , R 4 , R 5 , and n are as defined herein. Also provided are precursors of the aminoalcohol compounds and processes for making and using them.
摘要翻译：提供用作油漆和涂料中和剂的氨基醇化合物。所述化合物具有式（I）：或其盐，其中R 1，R 2，R 3，R 4，R 5和n如本文所定义。还提供了氨基醇化合物的前体和其制备和使用方法。

3. 发明申请

WO2008041054A1 POSITIVELY CHARGED WATER-SOLUBLE PRODRUGS OF PROSTAGLANDINS AND RELATED COMPOUNDS WITH VERY HIGH SKIN PENETRATION RATES 审中-公开
标题翻译：具有非常高的皮肤渗透率的PROSTAGLANDINS和相关化合物的正式充电水溶性产品
公开(公告)号：WO2008041054A1
公开(公告)日：2008-04-10
申请号：PCT/IB2006/053594
申请日：2006-10-02
申请人： TECHFIELDS BIOCHEM CO. LTD , YU, Chongxi , XU, Lina
发明人： YU, Chongxi , XU, Lina
IPC分类号： C07C215/40 , C07C215/42
CPC分类号： C07C405/0041
摘要： The novel positively charged pro-drugs of prostaglandins, prostacyclins and related compounds in the general formula (2) 'Structure 2' were designed and synthesized. The compounds of the general formula (2) 'Structure 2' indicated above can be prepared from protected prostaglandins, prostacyclins, and related compounds, by reaction with suitable alcohols, thiols, or amines and coupling reagents, such as N, N'-Dicyclohexylcarbodiimide, N, N'-Diisopropylcarbodiimide, O-(Benzotriazol-1-yl)-N,N,N',N'-tetramethyluronium tetrafluoroborate, O-(Benzotriazol-1-yl)-N,N,N',N'-tetramethyluronium hexafluorophosphate, Benzotriazol-1-yl-oxy-tris (dimethylamino)phosphonium hexafluorophosphate, et al. The positively charged amino groups of these pro-drugs not only largely increases the solubility of the drugs in water, but also bonds to the negative charge on the phosphate head group of membranes and pushes the pro-drug into the cytosol. The results suggest that the pro-drugs diffuse through human skin ~1000 times faster than do prostaglandins, prostacyclins, and related compounds. In plasma, more than 90% of these pro-drugs can change back to the parent drugs in a few minutes. The prodrugs can be used medicinally in treating any prostaglandins, prostacyclins, and related compounds-treatable conditions in humans or animals. The prodrugs can be administered transdermally for any kind of medical treatments and avoid most of the side effects of prostaglandins, prostacyclins, and related compounds. Controlled transdermal administration systems of the prodrug enable prostaglandins, prostacyclins, and related compounds to reach constantly optimal therapeutic blood levels to increase effectiveness and reduce the side effects of prostaglandins, prostacyclins, and related compounds. Another great benefit of transdermal administration of these pro-drugs is that administering medication, especially to children, will be much easier.
摘要翻译：设计并合成了通式（2）“结构2”中前列腺素，前列环素及相关化合物的新型带正电荷的前药。上述通式（2）“结构2”的化合物可以由保护的前列腺素，前列环素和相关化合物通过与合适的醇，硫醇或胺的反应和偶联试剂如N，N'-二环己基碳二亚胺，N，N'-二异丙基碳二亚胺，O-（苯并三唑-1-基）-N，N，N'，N'-四甲基脲四氟硼酸盐，O-（苯并三唑-1-基）-N，N，N'，N' 四甲基脲六氟磷酸盐，苯并三唑-1-基 - 氧 - 三（二甲基氨基）鏻六氟磷酸盐等。这些前药的带正电荷的氨基不仅大大增加了药物在水中的溶解度，而且还与磷酸盐头基上的负电荷键合，并将前药推入胞质溶胶中。结果表明，前药通过人体皮肤分散，比前列腺素，前列环素及相关化合物快1000倍。在血浆中，超过90％的这些前药可以在几分钟内改变为母体药物。前药可以在医学上用于治疗人或动物中的任何前列腺素，前列环素和相关化合物 - 可治疗的病症。前药可以通过皮肤施用于任何种类的医学治疗，并避免前列腺素，前列环素和相关化合物的大部分副作用。前药的受控透皮给药系统使前列腺素，前列环素和相关化合物达到不断优化的治疗血液水平以增加有效性并减少前列腺素，前列环素和相关化合物的副作用。经皮给药这些前药的另一大好处是给予药物，尤其是给儿童服用药物将容易得多。

4. 发明申请

WO2004092100A8 INDENE DERIVATIVES AS PHARMACEUTICAL AGENTS 审中-公开
标题翻译：作为药剂的INDENE衍生物
公开(公告)号：WO2004092100A8
公开(公告)日：2005-05-19
申请号：PCT/CA2004000566
申请日：2004-04-15
申请人： INFLAZYME PHARM LTD , RAYMOND JEFFERY R , HAN KANG , ZHOU YUANLIN , HE YUEHUA , NOREN BRADLEY , YEE JAMES GEE KEN
发明人： RAYMOND JEFFERY R , HAN KANG , ZHOU YUANLIN , HE YUEHUA , NOREN BRADLEY , YEE JAMES GEE KEN
IPC分类号： C07C35/21 , C07C35/32 , C07C69/013 , C07C69/03 , C07C311/04 , C07D211/58 , C07D213/30 , C07D213/38 , C07D213/74 , C07D233/54 , C07D233/56 , C07D295/096 , C07D307/66 , C07D317/66 , A61K31/047 , A61K31/133 , A61K31/155 , A61K31/164 , A61K31/18 , C07C35/52 , C07C215/42 , C07C233/18 , C07C279/08
CPC分类号： C07C35/32 , C07C35/14 , C07C35/21 , C07C51/083 , C07C51/347 , C07C62/34 , C07C69/013 , C07C213/00 , C07C213/08 , C07C215/42 , C07C233/18 , C07C233/21 , C07C233/72 , C07C247/14 , C07C279/08 , C07C311/04 , C07C315/00 , C07C2601/14 , C07C2602/08 , C07C2602/24 , C07D207/335 , C07D211/58 , C07D213/30 , C07D213/38 , C07D213/74 , C07D233/54 , C07D233/64 , C07D295/096 , C07D307/66 , C07D317/66 , C07D317/70 , Y10S514/825 , Y10S514/826 , Y10S514/863
摘要： Compounds of formula (Ia): wherein R , R , R , R , R , R and R are defined herein, as well as other indene derivatives are disclosed herein. Pharmaceutical compositions containing the compounds and methods of using the compounds are also disclosed.
摘要翻译：式（Ia）化合物：其中R 1，R 2，R 3，R 4a，R 4b，R 5和R 6在本文中定义，以及其它茚衍生物在本文中公开。还公开了含有化合物的药物组合物和使用该化合物的方法。

5. 发明申请

WO0230870A3 SUBSTITUTED C-CYCLOHEXYLMETHYLAMINE DERIVATIVES 审中-公开
标题翻译：取代基的C-环己基甲胺衍生物
公开(公告)号：WO0230870A3
公开(公告)日：2003-10-02
申请号：PCT/EP0111246
申请日：2001-09-28
申请人： GRUENENTHAL GMBH , SUNDERMANN BERND , MAUL CORINNA , BUSCHMANN HELMUT , FINKAM MICHAEL , KOEGEL BABETTE-YVONNE
发明人： SUNDERMANN BERND , MAUL CORINNA , BUSCHMANN HELMUT , FINKAM MICHAEL , KOEGEL BABETTE-YVONNE
IPC分类号： C07D295/08 , A61K31/135 , A61K31/136 , A61K31/145 , A61K31/165 , A61K31/166 , A61K31/215 , A61K31/216 , A61K31/222 , A61K31/24 , A61K31/33 , A61K31/341 , A61K31/38 , A61K31/495 , A61P23/00 , A61P25/04 , A61P29/00 , C07C211/28 , C07C211/29 , C07C215/42 , C07C217/52 , C07C217/54 , C07C217/62 , C07C219/24 , C07C233/41 , C07C233/79 , C07C235/14 , C07C235/36 , C07C235/54 , C07C317/32 , C07D307/54 , C07D307/68 , C07D333/16 , C07D333/20 , C07F7/10 , A61K31/133
CPC分类号： C07C215/42 , C07C217/52 , C07C217/54 , C07C219/24 , C07C233/41 , C07C233/79 , C07C235/14 , C07C235/54 , C07C2601/14 , C07C2601/16 , C07D307/54 , C07D333/16 , C07D333/20
摘要： The invention relates to substituted C-cyclohexylmethylamine derivatives, methods for the production thereof, pharmaceuticals containing said compounds and the use of substituted C-cyclohexylmethylamine derivatives for producing pharmaceuticals.
摘要翻译：本发明涉及取代的C-环己基甲胺衍生物，其制备方法，包含这些化合物和用于生产药物的用途取代的C-环己基甲胺衍生物的药物组合物。

6. 发明申请

WO02026694A1 O-SUBSTITUTED 6-METHYL-TRAMADOL DERIVATIVES 审中-公开
标题翻译： O-取代的6-甲基曲马朵衍生物
公开(公告)号：WO02026694A1
公开(公告)日：2002-04-04
申请号：PCT/EP2001/011276
申请日：2001-09-28
IPC分类号： C07D333/20 , A61K31/135 , A61K31/35 , A61K31/381 , A61P1/06 , A61P15/12 , A61P25/00 , A61P25/02 , A61P25/04 , A61P25/06 , A61P25/08 , A61P25/14 , A61P25/16 , A61P25/18 , A61P25/22 , A61P25/24 , A61P25/28 , A61P29/00 , A61P41/00 , C07C213/00 , C07C215/42 , C07C215/64 , C07C217/74 , C07D333/32
CPC分类号： C07C217/74 , C07C215/42 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07D333/32
摘要： The invention relates to O-substituted 6-methyl-tramadol derivatives, to methods for producing them, to medicaments containing these compounds and to the use of O-substituted 6-methyl-tramadol derivatives for producing medicaments for treating pain.
摘要翻译：本发明涉及O-取代-6-甲基反胺苯环醇衍生物，它们的制备方法，包含这些化合物和用于制备药物用于治疗疼痛的药物中的用途O-取代-6-甲基反胺苯环醇衍生物的药物组合物。

7. 发明申请

WO9824741A3 PROCESS FOR RESOLVING MIXTURES OF CARBOCYCLIC STEREOISOMERS 审中-公开
标题翻译：用于分解碳化硅立方体的混合物的方法
公开(公告)号：WO9824741A3
公开(公告)日：1998-09-11
申请号：PCT/EP9706782
申请日：1997-12-04
申请人： GLAXO GROUP LTD , SICKLES BARRY RIDDLE , INGOLD KENNETH JAMES , WALLIS CHRISTOPHER JOHN
发明人： SICKLES BARRY RIDDLE , INGOLD KENNETH JAMES , WALLIS CHRISTOPHER JOHN
IPC分类号： C07B57/00 , C07C213/00 , C07C215/42 , C07C229/48 , C07C269/06 , C07C269/08 , C07C271/24 , C07D209/52
CPC分类号： C07D209/52 , C07C229/48 , Y02P20/55
摘要： A process for the preparation of carbocyclic stereoisomers of formulae (I), (I'), (IIA'), (IIB'), (VA') and (VB'), including enantiomerically pure (IIA'), (I) and (I') utilising fractional crystallisation of salts formed with a chiral base; a reducing agent; a protecting group removing agent or a protecting group providing agent.

8. 发明申请

WO2013168005A3 COMPOSITIONS AND METHODS FOR THE TREATMENT OF RESTLESS LEG SYNDROME AND FIBROMYALGIA 审中-公开
公开(公告)号：WO2013168005A3
公开(公告)日：2013-11-14
申请号：PCT/IB2013/051266
申请日：2013-02-16
申请人： CELLIXBIO PRIVATE LIMITED
发明人： KANDULA, Mahesh
IPC分类号： C07C215/42 , A61K31/135 , A61P25/04 , A61P25/00 , A61P29/00
摘要： The invention relates to the compounds of formula (I) or its pharmaceutical acceptable salts, as well as polymorphs, solvates, enantiomers, stereoisomers and hydrates thereof. The pharmaceutical compositions comprising an effective amount of compounds of formula (I), and methods for the treatment of fibromyalgia, restless leg syndrome may be formulated for oral, buccal, rectal, topical, transdermal, transmucosal, intravenous, parenteral administration, syrup, or injection. Such compositions may be used to treatment of motor neurone disease, diabetic neuropathy, postherpetic neuralgia, acute opioid withdrawal management, obsessive-compulsive disorder, premature ejaculation, PTSD, injury, post-operative pain, osteoarthritis, rheumatoid arthritis, multiple sclerosis, spinal cord injury1, migraine, HIV related neuropathic pain, bipolar depression, depression, stress, cancer pain and lower back pain.

9. 发明申请

WO2008077799A3 COMPOUNDS AND METHODS FOR AMINO-ALKYLENEDIOL SYNTHESIS 审中-公开
标题翻译：氨基 - 烷基二醇合成的化合物和方法
公开(公告)号：WO2008077799A3
公开(公告)日：2008-08-14
申请号：PCT/EP2007063835
申请日：2007-12-12
申请人： HOFFMANN LA ROCHE , CAIN ROBERT O , MOORLAG HENDRICK , TUCKER CHARLES E , WONG JIM-WAH
发明人： CAIN ROBERT O , MOORLAG HENDRICK , TUCKER CHARLES E , WONG JIM-WAH
IPC分类号： C07C213/02 , C07C215/10 , C07C215/20 , C07C215/40 , C07C215/42
CPC分类号： C07C213/02 , C07C215/16 , Y02P20/55 , C07C215/10
摘要： A method of making an amino-alkylenediol and intermediate compounds useful in the method is disclosed. The method includes preparing a first intermediate compound comprising an aminoalkylene diol wherein a protecting group is linked to the amino functionality, and optionally, preparing a second intermediate compound comprising a salt of the first intermediate compound. The first intermediate compound has the structure of Formula (II ) wherein R is a divalent alkylene radical having from 2 to 20 carbon atoms, X and Y are independently a divalent linking moiety or a single bond, and Z is a protecting group. The second intermediate compound has the structure of Formula (III ) wherein R is a divalent alkylene radical having from 2 to 20 carbon atoms, X and Y are independently a divalent linking moiety or a single bond, TsO - is toluene sulfonate, and Z is a protecting group.
摘要翻译：公开了一种制备氨基亚烷基二醇的方法和用于该方法的中间体化合物。该方法包括制备包含氨基亚烷基二醇的第一中间体化合物，其中保护基与氨基官能团连接，并且任选地制备包含第一中间体化合物的盐的第二中间体化合物。第一中间体化合物具有式（II）的结构，其中R为具有2至20个碳原子的二价亚烷基，X和Y独立地为二价连接部分或单键，并且Z为保护基。第二中间体化合物具有式（III）的结构，其中R为具有2至20个碳原子的二价亚烷基，X和Y独立地为二价连接部分或单键，TsO-为甲苯磺酸盐，并且Z为一个保护组。

10. 发明申请

WO2008012605A1 POSITIVELY CHARGED WATER-SOLUBLE PRODRUGS OF KETOPROFEN AND RELATED COMPOUNDS WITH VERY FAST SKIN PENETRATION RATE 审中-公开
标题翻译：具有非常快速皮肤渗透速率的KETOPROFEN及相关化合物的积极充电水溶性产品
公开(公告)号：WO2008012605A1
公开(公告)日：2008-01-31
申请号：PCT/IB2006/052575
申请日：2006-07-27
申请人： TECHFIELDS BIOCHEM CO. LTD , YU, Chongxi , XU, Lina
发明人： YU, Chongxi , XU, Lina
IPC分类号： C07C215/72 , C07C215/40 , C07C215/42 , C07C225/16
CPC分类号： C07C219/14 , C07C235/34
摘要： The novel positively charged pro-drugs of ketoprofen and fenoprofen in the general formula(1) 'Structure 1' were designed and synthesized. The compounds of the general formula(1) 'Structure 1' indicated above can be prepared from functional derivatives of ketoprofen and fenoprofen, (for example acid halides or mixed anhydrides), by reaction with suitable alcohols, thiols, or amines. The positively charged amino groups of these pro-drugs not only largely increases the solubility of the drugs, but also bonds to the negative charge on the phosphate head group of membranes and pushes the pro-drug into the cytosol. The results suggest that the pro-drugs, diethylaminoethyl 2-(3-benzoylphenyl) propionate.AcOH and diethylaminoethyl 2-(3-phenoxyphenyl) propionate.AcOH diffuses through human skin ~125 times faster than does ketoprofen and fenoprofen. It takes 1-2 hours for ketoprofen or fenoprofen to reach the peak ketoprofen or fenoprofen plasma level when they are taken orally, but diethylaminoethyl 2-(3-benzoylphenyl) propionate.AcOH or diethylaminoethyl 2-(3-phenoxyphenyl) propionate.AcOH only took about 40 minutes to reach the ketoprofen or fenoprofen peak plasma level. In plasma, more than 90% of these pro-drugs can change back to the drug in a few minutes. The prodrugs can be used medicinally in treating any ketoprofen and fenoprofen-treatable conditions in humans or animals. The prodrugs can be administered not only orally, but also transdermally for any kind of medical treatments and avoid most of the side effects of ketoprofen and fenoprofen, most notably GI disturbances such as dyspepsia, gastroduodenal bleeding, gastric ulcerations, and gastritis. Controlled transdermal administration systems of the prodrug enables ketoprofen and fenoprofen to reach constantly optimal therapeutic blood levels to increase effectiveness and reduce the side effects of ketoprofen and fenoprofen. Another great benefit of transdermal administration of these pro-drugs is that administering medication, especially to children, will be much easier.
摘要翻译：设计并合成了通式（1）“结构1”中酮洛芬和非诺洛芬的新型带正电荷的前药。上述通式（1）'结构1'的化合物可以通过与合适的醇，硫醇或胺的反应由酮洛芬和非诺洛芬的功能衍生物（例如酰卤或混合酸酐）制备。这些前药的带正电荷的氨基不仅大大增加了药物的溶解度，而且还与磷酸盐头基团上的负电荷键合，并将前药推入细胞溶质中。结果表明，前药，2-（3-苯甲酰基苯基）丙酸二乙基氨基乙酯，AcOH和2-（3-苯氧基苯基）丙酸二乙基氨基乙酯。通过人皮肤扩散至酮洛芬和非诺洛芬的125倍。口服口服酮洛芬或非诺洛芬时，需要1-2小时才能达到酮洛芬或非诺洛芬血药浓度，但2-（3-苯甲酰基苯基）丙酸二乙氨基乙酯。乙酸或二乙基氨基乙基2-（3-苯氧基苯基）丙酸酯。仅AcOH 花了约40分钟达到酮洛芬或非诺洛芬峰值血浆水平。在血浆中，超过90％的这些前药可以在几分钟内恢复到药物。前药可以在医学上用于治疗人或动物中的任何酮洛芬和非诺洛芬治疗性病症。前药可以不仅口服给药，而且可以经皮用于任何种类的药物治疗，并避免酮洛芬和非诺洛芬的大部分副作用，最明显的是GI紊乱如消化不良，胃十二指肠出血，胃溃疡和胃炎。前药的受控透皮给药系统使酮洛芬和非诺洛芬达到不断优化的治疗血液水平以增加效力并降低酮洛芬和非诺洛芬的副作用。经皮给药这些前药的另一大好处是给予药物，尤其是给儿童服用药物将容易得多。

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