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1. 发明授权

US09688616B2 Neprilysin inhibitors 有权
公开(公告)号：US09688616B2
公开(公告)日：2017-06-27
申请号：US15219478
申请日：2016-07-26
申请人： THERAVANCE BIOPHARMA R&D IP, LLC
发明人： Erik Fenster , Melissa Fleury , Adam D. Hughes
IPC分类号： A61K31/40 , A61K31/42 , A61K31/44 , A61K31/197 , A61K31/397 , A61K31/5375 , C07D205/04 , C07D207/09 , C07D207/14 , C07D213/56 , C07C235/34 , C07D261/04 , C07D295/32 , C07C243/38 , C07D491/107 , C07D213/75 , C07C259/04 , C07D309/08 , C07D233/06 , C07D401/04 , C07D405/06 , C07D239/36 , C07D261/02 , C07C233/56 , C07C235/12 , C07C235/20 , C07C235/74 , C07C235/78 , C07D265/30 , C07D207/08 , C07D207/12 , C07D207/16 , C07D493/10 , C07C243/24 , C07C243/32 , C07D211/22 , C07D211/38 , C07D211/42 , C07D211/46 , C07D211/48 , C07D211/60 , C07D211/62 , C07D213/61 , C07D307/68 , A61K31/4015 , A61K31/495 , A61K45/06 , A61K31/192 , A61K31/4406 , C07C235/80 , C07D213/65 , A61K31/341 , A61K31/4409 , C07D213/86 , C07D213/87
CPC分类号： C07C243/38 , A61K31/192 , A61K31/197 , A61K31/341 , A61K31/397 , A61K31/40 , A61K31/4015 , A61K31/42 , A61K31/44 , A61K31/4406 , A61K31/4409 , A61K31/495 , A61K31/5375 , A61K45/06 , C07C233/56 , C07C235/12 , C07C235/20 , C07C235/34 , C07C235/74 , C07C235/78 , C07C235/80 , C07C243/24 , C07C243/32 , C07C259/04 , C07C2601/08 , C07C2601/16 , C07D205/04 , C07D207/08 , C07D207/09 , C07D207/12 , C07D207/14 , C07D207/16 , C07D211/22 , C07D211/38 , C07D211/42 , C07D211/46 , C07D211/48 , C07D211/60 , C07D211/62 , C07D213/56 , C07D213/61 , C07D213/65 , C07D213/75 , C07D213/86 , C07D213/87 , C07D233/06 , C07D239/36 , C07D261/02 , C07D261/04 , C07D265/30 , C07D295/32 , C07D307/68 , C07D309/08 , C07D401/04 , C07D405/06 , C07D491/107 , C07D493/10
摘要： In one aspect, the invention relates to compounds having the formula: where R1-R5 and X are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and processes and intermediates for preparing such compounds.

2. 发明授权

US6096890A Process for substituted hydrazides using carboxylic acids 失效
标题翻译：使用羧酸的取代酰肼的方法
公开(公告)号：US6096890A
公开(公告)日：2000-08-01
申请号：US383158
申请日：1999-08-25
申请人： Catherine Dubuisson-Brengel , Heather Lynnette Rayle
发明人： Catherine Dubuisson-Brengel , Heather Lynnette Rayle
IPC分类号： C07D251/16 , C07C241/02 , C07C241/04 , C07C243/24 , C07C243/38 , C07D251/22 , C07D251/30 , C07C243/28 , C07C243/36
CPC分类号： C07C241/04
摘要： This invention provides a convenient process for the preparation of monoacylhydrazines from carboxylic acids or their salts and hydrazine or substituted hydrazine in the presence of a 1,3,5-triazine substituted with at least one chloro or fluoro. The resulting monoacylhydrazine can further be converted to a diacylhydrazine by effectively either repeating the reaction or through reaction with a carboxylic acid chloride.
摘要翻译：本发明提供了在由至少一个氯或氟取代的1,3,5-三嗪存在下，从羧酸或其盐和肼或取代的肼制备单酰肼的方便方法。通过有效地重复反应或通过与羧酰氯反应，可以将所得的单酰基肼进一步转化为二酰基肼。

3. 发明授权

US3334991A Plant growth regulant composition and method 失效
标题翻译：植物生长调节剂的组成和方法
公开(公告)号：US3334991A
公开(公告)日：1967-08-08
申请号：US38829764
申请日：1964-08-07
申请人： UNIROYAL INC
发明人： HAGEMAN HOWARD A , HUBBARD WINCHESTER L
IPC分类号： A01N43/36 , C07C233/00 , C07C243/24 , C07D207/50 , C07D295/13 , C07D295/14 , C07D295/22 , C07D295/28 , C07D295/32
CPC分类号： C07D295/28 , C07C243/00 , C07C243/24 , C07D295/13 , C07D295/14 , C07D295/32

4. 发明授权

US10308594B2 Curing agents and degradable polymers and composites based thereon 有权
公开(公告)号：US10308594B2
公开(公告)日：2019-06-04
申请号：US14781242
申请日：2014-04-18
申请人： ADESSO ADVANCED MATERIALS WUXI CO., LTD.
发明人： Bing Qin , Xin Li , Bo Liang
IPC分类号： B32B27/26 , B32B27/38 , B32B27/04 , C08G59/50 , C08J5/24 , C07C43/30 , C07C235/00 , C07C235/08 , C07C243/00 , C07C243/24 , C07C243/26 , C07C243/28 , C07C243/38 , C07C217/84 , C08J11/16 , C08J11/26 , C07C201/12 , C07C213/02 , C07C241/02 , C08G59/14 , C08K7/06 , C08L63/00 , C09J9/00 , C09J163/00
摘要： The present invention provides, among others, compounds of Formula (I) or a salt thereof, methods for making these compounds, degradable polymers and reinforced composites made therefrom, and methods for degrading and/or recycling the degradable polymers and reinforced composites.

5. 发明授权

US09840460B2 Neprilysin inhibitors 有权
公开(公告)号：US09840460B2
公开(公告)日：2017-12-12
申请号：US15600998
申请日：2017-05-22
申请人： THERAVANCE BIOPHARMA R&D IP, LLC
发明人： Erik Fenster , Melissa Fleury , Adam D. Hughes
IPC分类号： A61K31/40 , A61K31/42 , A61K31/44 , A61K31/197 , A61K31/397 , A61K31/5375 , C07D205/04 , C07D207/09 , C07D207/14 , C07D213/56 , C07C235/34 , C07D261/04 , C07D295/32 , C07C243/38 , C07D491/107 , C07D213/87 , A61K31/341 , A61K31/4409 , C07D213/86 , C07D213/65 , C07C235/80 , A61K31/4406 , A61K31/192 , A61K45/06 , A61K31/495 , A61K31/4015 , C07D307/68 , C07D213/61 , C07D211/62 , C07D211/60 , C07D211/48 , C07D211/46 , C07D211/42 , C07D211/38 , C07D211/22 , C07C243/32 , C07C243/24 , C07D493/10 , C07D207/16 , C07D207/12 , C07D207/08 , C07D265/30 , C07C235/78 , C07C235/74 , C07C235/20 , C07C235/12 , C07C233/56 , C07D261/02 , C07D239/36 , C07D405/06 , C07D401/04 , C07D233/06 , C07D309/08 , C07C259/04 , C07D213/75
CPC分类号： C07C243/38 , A61K31/192 , A61K31/197 , A61K31/341 , A61K31/397 , A61K31/40 , A61K31/4015 , A61K31/42 , A61K31/44 , A61K31/4406 , A61K31/4409 , A61K31/495 , A61K31/5375 , A61K45/06 , C07C233/56 , C07C235/12 , C07C235/20 , C07C235/34 , C07C235/74 , C07C235/78 , C07C235/80 , C07C243/24 , C07C243/32 , C07C259/04 , C07C2601/08 , C07C2601/16 , C07D205/04 , C07D207/08 , C07D207/09 , C07D207/12 , C07D207/14 , C07D207/16 , C07D211/22 , C07D211/38 , C07D211/42 , C07D211/46 , C07D211/48 , C07D211/60 , C07D211/62 , C07D213/56 , C07D213/61 , C07D213/65 , C07D213/75 , C07D213/86 , C07D213/87 , C07D233/06 , C07D239/36 , C07D261/02 , C07D261/04 , C07D265/30 , C07D295/32 , C07D307/68 , C07D309/08 , C07D401/04 , C07D405/06 , C07D491/107 , C07D493/10
摘要： In one aspect, the invention relates to compounds having the formula: where R1-R5 and X are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and processes and intermediates for preparing such compounds.

6. 发明授权

US09428457B2 Neprilysin inhibitors 有权
公开(公告)号：US09428457B2
公开(公告)日：2016-08-30
申请号：US14749949
申请日：2015-06-25
申请人： Erik Fenster , Melissa Fleury , Adam D. Hughes
发明人： Erik Fenster , Melissa Fleury , Adam D. Hughes
IPC分类号： C07C235/74 , A61K31/7048 , C07C231/02 , A61K31/24 , C07D407/12 , A61K31/365 , A61K31/22 , C07D317/40 , A61K31/265 , C07C243/28 , C07C241/02 , A61P9/12 , A61P9/04 , A61P13/12 , A61K31/197 , C07D213/65 , A61K31/5375 , A61K31/397 , A61K31/40 , A61K31/42 , A61K31/44 , C07C235/34 , C07D205/04 , C07D207/09 , C07D207/14 , C07D213/56 , C07D261/04 , C07D295/32 , C07D491/107 , C07D213/75 , C07C259/04 , C07D309/08 , C07D233/06 , C07D401/04 , C07D405/06 , C07D239/36 , C07D261/02 , C07C233/56 , C07C235/12 , C07C235/20 , C07C235/78 , C07D265/30 , C07D207/08 , C07D207/12 , C07D207/16 , C07D493/10 , C07C243/24 , C07C243/32 , C07C243/38 , C07D211/22 , C07D211/38 , C07D211/42 , C07D211/46 , C07D211/48 , C07D211/60 , C07D211/62 , C07D213/61 , C07D307/68 , A61K31/4015 , A61K31/495 , A61K45/06 , A61K31/192 , A61K31/4406 , C07C235/80
CPC分类号： C07C243/38 , A61K31/192 , A61K31/197 , A61K31/341 , A61K31/397 , A61K31/40 , A61K31/4015 , A61K31/42 , A61K31/44 , A61K31/4406 , A61K31/4409 , A61K31/495 , A61K31/5375 , A61K45/06 , C07C233/56 , C07C235/12 , C07C235/20 , C07C235/34 , C07C235/74 , C07C235/78 , C07C235/80 , C07C243/24 , C07C243/32 , C07C259/04 , C07C2601/08 , C07C2601/16 , C07D205/04 , C07D207/08 , C07D207/09 , C07D207/12 , C07D207/14 , C07D207/16 , C07D211/22 , C07D211/38 , C07D211/42 , C07D211/46 , C07D211/48 , C07D211/60 , C07D211/62 , C07D213/56 , C07D213/61 , C07D213/65 , C07D213/75 , C07D213/86 , C07D213/87 , C07D233/06 , C07D239/36 , C07D261/02 , C07D261/04 , C07D265/30 , C07D295/32 , C07D307/68 , C07D309/08 , C07D401/04 , C07D405/06 , C07D491/107 , C07D493/10
摘要： In one aspect, the invention relates to compounds having the formula: where R1-R5 and X are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and processes and intermediates for preparing such compounds.

7. 发明申请

US20030195258A1 Taxol enhancer compounds 失效
标题翻译：紫杉醇增强剂化合物
公开(公告)号：US20030195258A1
公开(公告)日：2003-10-16
申请号：US10345885
申请日：2003-01-15
申请人： Synta Pharmaceuticals Corp.
发明人： Keizo Koya , Lijun Sun , Shoujun Chen , Noriaki Tatsuta , Yaming Wu , Mitsunori Ono
IPC分类号： A61K031/16 , A61K031/165 , C07C327/28 , C07C243/24
CPC分类号： C07D307/68 , A45D2008/006 , A61K31/337 , A61K47/58 , C07C327/56 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07D209/42 , C07D209/44 , C07D213/83 , C07D261/18 , C07D333/38 , C07D333/68
摘要： Disclosed is a compound represented by the Structural Formula (I): 1 Y is a covalent bond, a phenylene group or a substituted or unsubstituted straight chained hydrocarbyl group. In addition, Y, taken together with both >CnullZ groups to which it is bonded, is a substituted or unsubstituted aromatic group. Preferably, Y is a covalent bond or nullC(R7R8)null. R1 and R2 are independently an aryl group or a substituted aryl group, R3 and R4 are independently nullH, an aliphatic group, a substituted aliphatic group, an aryl group or a substituted aryl group. R5-R6 are independently nullH, an aliphatic group, a substituted aliphatic group, an aryl group or a substituted aryl group. R7 and R8 are each independently nullH, an aliphatic or substituted aliphatic group, or R7 is nullH and R8 is a substituted or unsubstituted aryl group, or, R7 and R8, taken together, are a C1-C6 substituted or unsubstituted alkylene group. Z is nullO or nullS. Also disclosed are pharmaceutical compositions comprising the compound of the present invention and a pharmaceutically acceptable carrier or diluent. Also disclosed is a method of treating a subject with cancer by administering to the subject a compound of Structural Formula (I) in combination with taxol or an analog of taxol.
摘要翻译：公开了由结构式（I）表示的化合物：Y是共价键，亚苯基或取代或未取代的直链烃基。此外，Y与它所键合的两个> C = Z基团一起是取代或未取代的芳族基团。优选地，Y是共价键或-C（R <下标> 7 R <下标> 8 ） - 。 R <下标> 1 和R <下标> 2 独立地是芳基或取代的芳基，R <下标3 和R <下标4 独立的-H，脂族基团，取代的脂族基团，芳基或取代的芳基。 R <下标> 5 -R <下标> 6 独立地是-H，脂族基团，取代的脂族基团，芳基或取代的芳基。 R <下标> 7 和R <下标> 8 各自独立地为-H，脂族或取代的脂族基团，或R <下标7 为-H，R < 8 是一个取代或未取代的芳基，或者，R“下标”，“高亮”和“低级”）是C1-C6取代或未取代的亚烷基。 Z = 0或= S。还公开了包含本发明化合物和药学上可接受的载体或稀释剂的药物组合物。还公开了通过向受试者施用结构式（I）的化合物与紫杉醇或紫杉醇的类似物组合治疗患有癌症的受试者的方法。

8. 发明授权

US09169210B2 Bioavailable diacylhydrazine ligands for modulating the expression of exogenous genes via an ecdysone receptor complex 有权
公开(公告)号：US09169210B2
公开(公告)日：2015-10-27
申请号：US13603965
申请日：2012-09-05
申请人： Robert Eugene Hormann , David W. Potter , Orestes Chortyk , Colin M. Tice , Glenn Richard Carlson , Andrew Meyer , Thomas R. Opie
发明人： Robert Eugene Hormann , David W. Potter , Orestes Chortyk , Colin M. Tice , Glenn Richard Carlson , Andrew Meyer , Thomas R. Opie
IPC分类号： C07C243/38 , C07D213/63 , C07D213/87 , C07C243/24 , C07C251/08 , C07C251/38 , C07C255/66 , C07C281/10 , C07C309/59 , C07C317/44 , C07C317/46 , C07D209/42 , C07D213/81 , C07D213/82 , C07D231/14 , C07D231/56 , C07D235/06 , C07D237/24 , C07D239/52 , C07D241/24 , C07D271/12 , C07D317/68 , C07D319/18 , C07D405/12 , C07C243/18
CPC分类号： C07C241/04 , A61K31/166 , A61K31/222 , A61K31/357 , A61K31/404 , A61K31/415 , A61K31/4184 , A61K31/455 , A61K31/4965 , C07C243/18 , C07C243/24 , C07C243/38 , C07C251/08 , C07C251/38 , C07C255/66 , C07C281/10 , C07C309/59 , C07C315/02 , C07C317/44 , C07C317/46 , C07D209/42 , C07D213/81 , C07D213/82 , C07D213/86 , C07D213/87 , C07D231/14 , C07D231/56 , C07D235/06 , C07D235/24 , C07D237/24 , C07D239/52 , C07D241/24 , C07D271/12 , C07D317/68 , C07D319/08 , C07D319/18 , C07D319/20 , C07D405/12 , C12N9/0069 , C12N15/635 , C12P21/00 , Y02A50/471
摘要： The present invention relates to non-steroidal ligands for use in nuclear receptor-based inducible gene expression system, and a method to modulate exogenous gene expression in which an ecdysone receptor complex comprising: a DNA binding domain; a ligand binding domain; a transactivation domain; and a ligand is contacted with a DNA construct comprising: the exogenous gene and a response element; wherein the exogenous gene is under the control of the response element and binding of the DNA binding domain to the response element in the presence of the ligand results in activation or suppression of the gene.

9. 发明授权

US5977401A Process and novel intermediates for preparing triazolinones 失效
标题翻译：制备三唑啉酮的方法和新型中间体
公开(公告)号：US5977401A
公开(公告)日：1999-11-02
申请号：US291318
申请日：1999-04-14
申请人： Heinz-Jurgen Wroblowsky
发明人： Heinz-Jurgen Wroblowsky
IPC分类号： C07C281/02 , C07C281/04 , C07D249/12 , C07C229/24 , C07C241/02 , C07C243/14 , C07C243/24
CPC分类号： C07C281/02 , C07C281/04 , C07D249/12
摘要： The present invention relates to a novel intermediate compound for preparing optionally substituted 1,2,4-triazolinones and a process for preparing that intermediate compound.
摘要翻译：本发明涉及用于制备任选取代的1,2,4-三唑啉酮的新型中间体化合物及其制备方法。

10. 发明授权

US5837874A Hydrazide intermediates 失效
标题翻译：酰肼中间体
公开(公告)号：US5837874A
公开(公告)日：1998-11-17
申请号：US631260
申请日：1996-04-15
申请人： Otohiko Tsuge , Taizo Hatta , Satoshi Urano , Noriyuki Tsuboniwa , Ryuzo Mizuguchi
发明人： Otohiko Tsuge , Taizo Hatta , Satoshi Urano , Noriyuki Tsuboniwa , Ryuzo Mizuguchi
IPC分类号： C07C281/06 , C07C281/08 , C07C281/10 , C07C281/14 , C07D249/12 , C07C243/24
CPC分类号： C07C281/14 , C07C281/06 , C07C281/10 , C07D249/12
摘要： The present invention relates to a triazole compound represented by the formula (1): ##STR1## wherein R.sup.1 represents a lower alkyl group which may have a substituent; R.sup.2 and R.sup.3 represent respectively hydrogen, an aryl group, a benzoyl group, a tosyl group, a lower alkoxy carbonyl group, or an aryl sulfonyl group, each of which except for hydrogen may have a substituent; provided that when R.sup.2 is hydrogen, the triazole compound is represented by the formula (2): ##STR2## wherein R.sup.1 and R.sup.3 have the same as defined above.
摘要翻译：本发明涉及由式（1）表示的三唑化合物：其中R 1表示可以具有取代基的低级烷基; R2和R3分别表示氢，芳基，苯甲酰基，甲苯磺酰基，低级烷氧基羰基或芳基磺酰基，除氢以外可以具有取代基。条件是当R 2为氢时，三唑化合物由式（2）表示：其中R 1和R 3具有与上述相同的含义。

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