| 序号 | 专利名 | 申请号 | 申请日 | 公开（公告）号 | 公开（公告）日 | 发明人 |
|---|---|---|---|---|---|---|
| 81 | CYCLOALKYL PIPERIDINE TACHYKININ RECEPTOR ANTAGONISTS | EP05851957.0 | 2005-11-18 | EP1817284A2 | 2007-08-15 | DEVITA, Robert, J.; MILLS, Sander, G.; EID, Ronsar; YOUNG, Jonathan, R. |
| The present invention is directed to certain piperidine compounds which are useful as neurokinin-1 (NK-1) receptor antagonists, and inhibitors of tachykinin and in particular substance P. The invention is also concerned with pharmaceutical formulations comprising these compounds as active ingredients and the use of the compounds and their formulations in the treatment of certain disorders, including emesis, urinary incontinence, depression, and anxiety. | ||||||
| 82 | COMPOUND FOR ORGANIC PHOTOELECTRIC DEVICE AND ORGANIC PHOTOELECTRIC DEVICE, IMAGE SENSOR, AND ELECTRONIC DEVICE INCLUDING THE SAME | EP15196179.4 | 2015-11-25 | EP3026722B1 | 2021-01-06 | LIM, Seon-Jeong; RO, Takkyun; YAGI, Tadao; PARK, Kyung Bae; YUN, Sung Young; JIN, Yong Wan; HEO, Chul-Joon |
| A compound for an organic photoelectric device is represented by Chemical Formula 1, and an organic photoelectric device, an image sensor and an electronic device include the same. | ||||||
| 83 | SELENOPHENE DERIVATIVES AND ORGANIC PHOTOELECTRIC DEVICE, IMAGE SENSOR AND ELECTRONIC DEVICE INCLUDING THE SAME | EP17170200.4 | 2017-05-09 | EP3243822A1 | 2017-11-15 | YAGI, Tadao; XAVIER, Bulliard; CHOI, Hyesung; SAKURAI, Rie; SHIBUYA, Hiromasa; LIM, Youn Hee; YUN, Sung Young; LEE, Gae Hwang; LEE, Kwang Hee; LEEM, Dong-Seok |
A compound of Chemical Formula 1, and an organic photoelectric device, an image sensor, and an electronic device including the same are disclosed:
In Chemical Formula 1, each substituent is the same as defined in the detailed description. |
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| 84 | INHIBITORS OF C-FMS KINASE | EP05815361.0 | 2005-10-20 | EP1807077B1 | 2016-11-23 | ILLIG, Carl R.; BALLENTINE, Shelley K.; CHEN, Jinsheng; MEEGALLA, Sanath; RUDOLPH, M. Jonathan; WALL, Mark J.; WILSON, Ken; DESJARLAIS, Renee; MOLLOY, Christopher; MANTHEY, Carl; FLORES, Christopher |
| 85 | HIV INTEGRASE INHIBITORS | EP05724616.7 | 2005-03-04 | EP1725535A2 | 2006-11-29 | MORRISSETTE, Matthew, M.; WILLIAMS, Peter, D.; WAI, John, S.; FISHER, Thorsten, E.; LYLE, Terry, A. |
| Compounds of Formula I are inhibitors of HIV integrase and inhibitors of HIV replication: (I) wherein Z, R1, R2, R3, R4, R5, R6, R7, R8 and R9 are defined herein. The compounds are useful in the prevention and treatment of infection by HIV and in the prevention, delay in the onset, and treatment of AIDS. The compounds are employed against HIV infection and AIDS as compounds per se or in the form of pharmaceutically acceptable salts. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines. | ||||||
| 86 | PHARMACEUTICAL FORMULATIONS WITH IMPROVED AQUEOUS SOLUBILITY | EP00918139.7 | 2000-03-20 | EP1163234B1 | 2005-10-26 | ERKOBONI, David, F.; VLADYKA, Ronald, S., Jr.; STERGIOS, Pamela, R. |
| A formulation of a sparingly water-soluble, crystalline pharmaceutically active agent wherein the active agent is converted to and stabilized in its amorphous form as a solid solution of a normally hydrophobic vehicle is described. The amorphous state is stabilized by the composition of the formulation, providing long shelf life of the improved composition. This stabilized formulation also provides increased solubility and bioavailability of the active agent. Solutions of the active agent are stabilized by the composition, preventing recrystallization and precipitation of the less soluble, crystalline form of the active agent from aqueous solutions thereof. | ||||||
| 87 | PYRIDINE CARBOXAMIDE OR SULFONAMIDE DERIVATIVES AND COMBINATORIAL LIBRARIES THEREOF | EP00953818.2 | 2000-08-03 | EP1218343A1 | 2002-07-03 | CHEN, Yuewu; LANG, Hengyuan; PEI, Yazhong |
| The present invention relates to novel pyridine carboxamide or sulfonamide derivative compounds of formula (I), wherein R1 to R6 have the meanings provided herein. The invention further relates to combinatorial libraries containing two or more such compounds, as well as methods of preparing pyridine carboxamide or sulfonamide derivative compounds. | ||||||
| 88 | COMPOUND AND ORGANIC PHOTOELECTRIC DEVICE, IMAGE SENSOR AND ELECTRONIC DEVICE INCLUDING THE SAME | EP18188464.4 | 2018-08-10 | EP3442022B1 | 2019-12-25 | ISHII, Norihito; SHIBATA, Katsunori; RO, Takkyun; KWON, Ohkyu; KIM, Sang Mo; PARK,, Kyung Bae; YUN, Sung Young; LEEM, Dong-Seok; LIM, Youn Hee; JIN, Yong Wan; CHOI, Yeong Suk; CHOI, Jong Won; CHOI, Taejin; CHOI, Hyesung; HEO, Chul Joon |
| 89 | COMPOUND AND ORGANIC PHOTOELECTRIC DEVICE, IMAGE SENSOR AND ELECTRONIC DEVICE INCLUDING THE SAME | EP18188464.4 | 2018-08-10 | EP3442022A1 | 2019-02-13 | ISHII, Norihito; SHIBATA, Katsunori; RO, Takkyun; KWON, Ohkyu; KIM, Sang Mo; PARK,, Kyung Bae; YUN, Sung Young; LEEM, Dong-Seok; LIM, Youn Hee; JIN, Yong Wan; CHOI, Yeong Suk; CHOI, Jong Won; CHOI, Taejin; CHOI, Hyesung; HEO, Chul Joon |
A compound of Chemical Formula 1, and an organic photoelectric device, an image sensor, and an electronic device including the same are disclosed:
|
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| 90 | INHIBITORS OF C-FMS KINASE | EP05815361 | 2005-10-20 | EP1807077A4 | 2011-09-21 | ILLIG CARL R; BALLENTINE SHELLEY K; CHEN JINSHENG; MEEGALLA SANATH; RUDOLPH M JONATHAN; WALL MARK J; WILSON KEN; DESJARLAIS RENEE; MOLLOY CHRISTOPHER; MANTHEY CARL; FLORES CHRISTOPHER |
| 91 | CYCLOALKYL KETO PIPERIDINE TACHYKININ RECEPTOR ANTAGONISTS | EP05856976 | 2005-11-18 | EP1817285A4 | 2009-01-21 | DEVITA ROBERT J; MILLS SANDER G; EID RONSAR; YOUNG JONATHAN R |
| 92 | WEAK BASE SALTS | EP04720454.0 | 2004-03-12 | EP1606290A1 | 2005-12-21 | YALKOWSKY, Samuel, H.; SANGHVI, Tapan |
| Pharmaceutical compositions comprising a salt of a weak base compound of formula: wherein X is hydrogen, halogen, alkyl of less than 7 carbon atoms or alkoxy of less than 7 carbon atoms; n is a positive integer of less than 4; Y is hydrogen, chlorine, nitro, methyl, ethyl or oxychloro; R is hydrogen, alkylaminocarbonyl wherein the alkyl group has from 3 to 6 carbon atoms or an alkyl group having from 1 to 8 carbons and R2 is 4-thiazolyl, NHCOOR1 wherein R, is aliphatic hydrocarbon of less than 7 carbon atoms, or an alkyl group of less than 7 carbon atoms; one or more free acids; and optional pharmaceutical additives are provided. | ||||||
| 93 | THERAPEUTIC COMPOUNDS FOR TREATING DYSLIPIDEMIC CONDITIONS | EP03771693.3 | 2003-07-21 | EP1534696A1 | 2005-06-01 | JONES, A., Brian; ADAMS, Alan, D.; GREEN, Ahren, I.; HUANG, Shaei, Y.; TSE, Bruno; GUTTERIDGE, Clare, E.; CHENG, Yuan |
| The present invention relates to novel LXR ligands of Formula I and the pharmaceutically acceptable salts, esters and tautomers thereof, which are useful in the treatment of dyslipidemic conditions, particularly depressed levels of HDL cholesterol. | ||||||
| 94 | IMPROVED AQUEOUS SOLUBILITY PHARMACEUTICAL FORMULATIONS | EP00918139 | 2000-03-20 | EP1163234A4 | 2003-05-02 | ERKOBONI DAVID F; VLADYKA RONALD S JR; STERGIOS PAMELA R |
| 95 | IMPROVED AQUEOUS SOLUBILITY PHARMACEUTICAL FORMULATIONS | EP00918139.7 | 2000-03-20 | EP1163234A1 | 2001-12-19 | ERKOBONI, David, F.; VLADYKA, Ronald, S., Jr.; STERGIOS, Pamela, R. |
| A formulation of a sparingly water-soluble, crystalline pharmaceutically active agent wherein the active agent is converted to and stabilized in its amorphous form as a solid solution of a normally hydrophobic vehicle is described. The amorphous state is stabilized by the composition of the formulation, providing long shelf life of the improved composition. This stabilized formulation also provides increased solubility and bioavailability of the active agent. Solutions of the active agent are stabilized by the composition, preventing recrystallization and precipitation of the less soluble, crystalline form of the active agent from aqueous solutions thereof. | ||||||
| 96 | ALPHA-KETOAMIDE MULTICATALYTIC PROTEASE INHIBITORS | EP98953274.2 | 1998-10-07 | EP1027056A1 | 2000-08-16 | CHATTERJEE, Sankar; MALLAMO, John, P. |
| This invention relates to α-ketoamide inhibitors of multicatalytic protease (MCP), to compositions including such inhibitors, and to methods for the use of MCP inhibitors. The MCP inhibitors of the present invention are useful, for example, to retard loss of muscle mass incident to various physiological states. | ||||||
| 97 | METHODS FOR SYNTHESIZING 2-SUBSTITUTED IMIDAZOLES | EP98915593.2 | 1998-04-17 | EP0977740A1 | 2000-02-09 | HONG, Yaping; BAKALE, Roger, P.; SENANAYAKE, Chrisantha, H. |
| The present invention is a method of preparing 2-substituted imidazoles from readily available imidazoles having a leaving group in the 2-position, by alkylating the imidazole under mild conditions to afford a 3-N-alkylated imidazolium salt; and coupling the imidazolium salt with a nucleophile also under mild conditions to afford a 2-substituted 3-N-alkylated imidazolium salt. The reaction product can optionally be isolated and purified. The 2-substituted 3-N-alkylated imidazolium salt is hydrolyzed to afford a 2-substituted imidazole. Alternatively, the imidazole is coupled with a nucleophile in the presence of fluoride ion to provide a 2-substituted imidazole. | ||||||
| 98 | Substituted 2-azabicycles and their use as orexin receptor modulators | US14774555 | 2014-03-12 | US09611277B2 | 2017-04-04 | Christine F. Gelin; Terry P. Lebold; Brock T. Shireman; Jeannie M. Ziff |
| The present invention is directed to compounds of Formula I: wherein X is N or CR1; Y is N or CR2; R1 is H, alkoxy, halo, triazolyl, pyrimidinyl, oxazolyl, isoxazole, oxadiazolyl, or pyrazolyl; R2 is H, alkyl, alkoxy, or halo; Z is NH or O; R3 is H, alkyl, alkoxy, halo, or triazolyl; R4 is H or alkyl; or R3 and R4, together with the atoms to which they are attached, form a 6-membered aryl ring or a 5- or 6-membered heteroaryl ring; R5 is pyridyl, pyrazinyl, or pyrimidinyl, wherein the pyridyl, pyrazinyl, or pyrimidinyl is optionally substituted with halo or alkyl; and n is 1 or 2. Methods of making the compounds of Formula I are also described. The invention also relates to pharmaceutical compositions comprising compounds of Formula I. Methods of using the compounds of the invention are also within the scope of the invention. | ||||||
| 99 | Biaryl imidazole derivatives for regulating CYP17 | US13632007 | 2012-09-30 | US09199975B2 | 2015-12-01 | Roger Astbury Smith; Nicholas James Laping; Scott Kevin Thompson; Raghava Reddy Kethiri; Dhanalakshmi Sivanandhan; Chandregowda Venkateshappa; Bheemashankar Kulkarni; Purushottam Dewang; Rajendra Kristam; Srinivas Kasibhatla; Rajesh Devraj |
| The present application provides novel imidazole compounds and pharmaceutically acceptable salts thereof. Also provided are methods for preparing these compounds. These compounds are useful in inhibiting CYP17 activity by administering a therapeutically effective amount of one or more of the compounds to a patient. By doing so, these compounds are effective in treating conditions associated with CPY17 activity. A variety of conditions can be treated using these compounds and include diseases which are characterized by abnormal cellular proliferation. In one embodiment, the disease is cancer, such as prostate cancer. | ||||||
| 100 | Neuroprotective multifunctional compounds and pharmaceutical compositions comprising them | US13146975 | 2010-01-31 | US08802675B2 | 2014-08-12 | Moussa B. H. Youdim; Mati Fridkin; Hailin Zheng |
| Multifunctional compounds are provided, comprising two or more functional moieties selected from: (i) a moiety that imparts an iron chelator function; (ii) a moiety that imparts a neuroprotective function; (iii) a moiety that imparts combined antiapoptotic, neuroprotective and/or neurorestorative functions; (iv) a moiety that imparts brain MAO inhibition, preferably with little or no MAO inhibition in liver and small intestine; (v) a moiety that imparts cholinesterase inhibitory function; and (vi) a moiety that imparts an N-methyl-D-aspartic acid receptor (NMDAR) inhibition, and pharmaceutically acceptable salts and optical isomers thereof. The multifunctional compounds are useful in the treatment or prevention of diseases, disorders or conditions that can be prevented and/or treated by iron chelation therapy, and/or neuroprotection and/or neurorestoration, and/or apoptosis inhibition and/or MAO inhibition and/or cholinesterase inhibition and/or NMADR inhibition. The present invention encompasses compounds of the formulas I to VI. | ||||||
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