子分类：
| 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 | Microparticles comprising diketopiperazine salts for drug delivery | EP10075512.3 | 2005-08-23 | EP2314298B1 | 2015-05-27 | Leone-Bay, Andrea; Moye-Sherman, Destardi; Wilson, Bryan R. |
| 82 | DIKETOPIPERAZINE SALTS FOR DRUG DELIVERY | EP05791798.1 | 2005-08-23 | EP1791542B1 | 2015-05-20 | LEONE-BAY, Andrea; MOYE-SHERMAN, Destardi; WILSON, Bryan, R. |
| 83 | QUINOLIZIDINONE CARBOXAMIDE M1 RECEPTOR POSITIVE ALLOSTERIC MODULATORS | EP10832030 | 2010-11-15 | EP2501231A4 | 2013-05-15 | KUDUK SCOTT D; CHANG RONALD K; GRESHOCK THOMAS J |
| 84 | Novel piperazine amide derivatives | EP08786826.1 | 2008-08-04 | EP2188266B1 | 2012-10-17 | DEHMLOW, Henrietta; KUHN, Bernd; OBST SANDER, Ulrike; ROEVER, Stephan; SCHULZ-GASCH, Tanja; WRIGHT, Matthew; WYLER, René |
| 85 | QUINOLIZIDINONE CARBOXAMIDE M1 RECEPTOR POSITIVE ALLOSTERIC MODULATORS | EP10832030.0 | 2010-11-15 | EP2501231A1 | 2012-09-26 | KUDUK, Scott, D.; CHANG, Ronald, K.; GRESHOCK, Thomas, J. |
| The present invention is directed to compounds of formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor. | ||||||
| 86 | NOVEL PIPERAZINE AMIDE DERIVATIVES | EP08786826.1 | 2008-08-04 | EP2188266A2 | 2010-05-26 | DEHMLOW, Henrietta; KUHN, Bernd; OBST SANDER, Ulrike; ROEVER, Stephan; SCHULZ-GASCH, Tanja; WRIGHT, Matthew; WYLER, René |
| The invention is concerned with novel piperazine amide derivatives of formula (I) wherein R1 to R11, W, X and Y are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds bind to LXR alpha and LXR beta and can be used as medicaments. | ||||||
| 87 | DIKETOPIPERAZINE SALTS, DIKETOMORPHOLINE SALTS OR DIKETODIOXANE SALTS FOR DRUG DELIVERY | EP05791798.1 | 2005-08-23 | EP1791542A1 | 2007-06-06 | LEONE-BAY, Andrea; MOYE-SHERMAN, Destardi; WILSON, Bryan, R. |
| Biologically active agent delivery compositions, which comprise diketopiperazine carboxylate salts are provided. Related methods for making and using the biologically active agent delivery compositions are also provided. | ||||||
| 88 | ANTIBACTERIAL AGENTS | EP03780379.8 | 2003-12-11 | EP1572630A1 | 2005-09-14 | EAST, Stephen Peter; BRAGG, Ryan Ashley; TAYLOR, Steven |
| Compounds of formula (I) have antibacterial activity, wherein Q represents -N(OH)CH(=O) or -C(=O)NH(OH); Y represents -C(=O)-, - C(=S)-, -S(=O)-, or -SO2-; R1 represents hydrogen, C1-C6 alkyl or C1-C6 alkyl substituted by one or more halogen atoms, or, except when Q is a radical of formula -N(OH)CH(=O), a hydroxy, Cl-C6 alkoxy, Cl-C6 alkenyloxy, halogen, amino, Cl-C6 alkylamino, or di-( C1-C6 alkyl)amino group; R2 represents a substituted or unsubstituted C1-C6 alkyl, C1-C3 alkyl-O-Cl-C3 alkyl, Cl-C3 alkyl-S-C1-C3 alkyl, cycloalkyl(C1-C3 alkyl)-, aryl(C1-C3 alkyl)-, heterocyclyl(C1-C3 alkyl)-, or R1R2N-C1-C3 alkyl group wherein R1 represents hydrogen or Cl-C3 alkyl and R2 represents Cl-C3 alkyl, or R1R2N- represents a cyclic amino group; R3 and R5 independently represent hydrogen or a substituted or unsubstituted C1-C6 alkyl group or R3 and R5 taken together with the carbon and nitrogen atoms to which they are respectively attached form a saturated heterocyclic ring of from 5 to 7 ring atoms, which may be fused to a second carbocyclic or heterocyclic ring, either of which rings may optionally be substituted; R4 represents hydrogen or a substituted or unsubstituted Cl-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, cycloalkyl, aryl, heterocyclyl, Cl-C3 alkyl-O-CI-C3 alkyl, C1-C3 alkyl-S-C1-C3 alkyl, C1-C3 alkyl-NH-(CI-C3 alkyl)-, cycloalkyl(C1-C3 alkyl)-, heterocyclic(C1-C3 alkyl)- or aryl(C1-C3 alkyl)- group; and A represents a primary, secondary or tertiary amino group or a group -R6, -OR6, wherein R6 is a substituted or unsubstituted Cl-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, cycloalkyl, aryl, heterocyclyl, C1-C3 alkyl-O-(C1-C3 alky)-l, C1-C3 alkyl-S-(C1-C3 alkyl)-, Cl-C3 alkyl-NH-(C1-C3 alkyl)-, cycloalkyl(C1-C3 alkyl)-, heterocyclic(C1-C3 alky)-l or aryl(C1-C3 alkyl)- group. | ||||||
| 89 | PHARMACEUTICAL PIPERAZINE COMPOUNDS | EP95908314.0 | 1995-02-14 | EP0745070A1 | 1996-12-04 | BROCCHINI, Stephen, James; BRYANS, Justin, Stephen; FOLKES, Adrian, John; LATHAM, Christopher, John; BRUMWELL, Julie, Elizabeth |
| A diketopiperazine of formula (A), wherein one or both of R1 and R2, which may be the same or different, is: (I) X, or a phenyl group which is substituted by X, C(O)X, OC(O)CH2X, OCH2CH2X, CH2X, CONH(CH2)nX, O(CH2)nCH(OH) (CH2)nX or (a) or which is fused to a group X; (II) a phenyl group substituted by CH2NR12R13, OC(O) (CH2)nZ, CH(OR12)(OR13), (CH2)nNR14C(O) (CH2)mNR12R13 or O(CH2)nCH(OH) (CH2)nN(R12R13); (III) a group CH=C(W)V; or (IV) a cyclohexyl group; and where appropriate, the other of R1 and R2 is a phenyl group optionally substituted by one or more groups independently selected from halogen, nitro, methoxy, NHC(O)R12, CO2H, O(CH2)nN(R12R13) and CH2Y(CH2)nN(R12R13); R3 is C1-C4 alkyl or (CH2)nC(O)OR12; Y is O or S; Z is a C3-C6 cycloalkyl group; W is hydrogen or a phenyl group; and the pharmaceutically acceptable salts and esters thereof having activity as inhibitors of plasminogen activator inhibitor. | ||||||
| 90 | Piperazin-2,5-dion und Piperazin-2-on Derivate | EP91113808.9 | 1991-08-17 | EP0477528B1 | 1995-12-13 | Diblitz, Christina, Dr.; Höchstetter, Hans, Dr. |
| 91 | PHARMACEUTICALLY ACTIVE DIKETOPIPERAZINES | EP93918033.0 | 1993-08-16 | EP0672036A1 | 1995-09-20 | COLLINS, Mark, Anthony, David 240 Bath Road; CHICARELLI-ROBINSON, Maria, Inês 240 Bath Road; BRYANS, Justin, Stephen; BROCCHINI, Stephen, James; LATHAM, Christopher, John 240 Bath Road |
| A diketopiperazine of formula (A) wherein each of R14 and R15, which may be the same or different, is independently selected from hydrogen and C1-C6 alkyl provided at least one of R14 and R15 is C1-C6 alkyl; and R1 to R10, which may be the same or different, is independently selected from hydrogen, C1-C6 alkyl unsubstituted or substituted by one or more hydrogen atoms, C1-C6 alkoxy, C1-C6 alkylthio, halogen, hydroxy, nitro, optionally substituted phenyl, cyano, -CH2OH, -CH2COOH, -CO2R11, -NHCOR11, -NHSO¿2?R?13, -SO¿2R13, -CON(R?11)R12, -SOR13, -SO¿2N(R?11R12), -N(R11R12¿), -O(CH¿2?)nN(R?11R12¿), -O(CH¿2?)nCO2R?11, -OCOR11, -CH¿2OCOR11, -CH2NHCOR11, -CH2NHCOOR13, -CH2SR11, -CH2SCOR11, -CH2S(O)mR13 wherein m is 1 or 2, -CH¿2?NHCO(CH2)nCO2R?11, -N(R11COR12¿), -NHCOCF¿3?, -NHCO(CH2)nCO2R?11¿, -NHCO(CH¿2?)nOCOR?11¿ and -NHCO(CH¿2)nOR?11 wherein n is 0 or is an integer of from 1 to 6, each of R?11 and R12¿ is independently H or C¿1?-C6 alkyl or, when R?11 and R12¿ are attached to the same nitrogen atom, they may alternatively form with the nitrogen atom a saturated five or six-membered ring; and R13 is C1-C6 alkyl; or any of R1 and R2, R2 and R3, R3 and R4 and R4 and R5, or R6 and R7, R7 and R8, R8 and R9 and R9 and R10, form together with the carbon atoms to which they are attached a benzene ring which is optionally substituted; and pharmaceutically acceptable salts and esters thereof; are modulators of multiple drug resistance. | ||||||
| 92 | PHARMACEUTICALLY ACTIVE DIKETOPIPERAZINES | EP93918032.0 | 1993-08-16 | EP0655060A1 | 1995-05-31 | COLLINS, Mark, Anthony, David 240 Bath Road; CHICARELLI-ROBINSON, Maria, Inês 240 Bath Road; BRYANS, Justin, Stephen 240 Bath Road; BROCCHINI, Stephen, James 240 Bath Road; LATHAM, Christopher, John 240 Bath Road; SHAW, John, Richardson 240 Bath Road |
| A diketopiperazine of formula (A) wherein each of R1 to R10, which may be the same or different, is independently selected from hydrogen, C1-C6 alkyl unsubstituted or substituted by one or more hydrogen atoms, C1-C6 alkoxy, C1-C6 alkylthio, halogen, hydroxy, nitro, optionally substituted phenyl, -cyano, -CH2COOH, -CH2OH, -CO2R11, -NHCOR11, -NHSO¿2?R?13, -SO¿2R13, -CON(R?11R12), -SOR13, -SO¿2N(R?11R12), -N(R11R12¿), -O(CH¿2?)nN(R?11R12¿), -O(CH¿2?)nCO2R?11, -OCOR11, -CH¿2OCOR11, -CH2NHCOR11, -CH2NHCOOR13, -CH2SR11, -CH2SCOR11, -CH2S(O)mR13 wherein m is 1 or 2, -CH¿2?NHCO(CH2)nCO2R?11, -N(R11)COR12¿, -NHCOCF¿3?, -NHCO(CH2)nCO2R?11¿, -NHCO(CH¿2?)nOCOR?11¿ and -NHCO(CH¿2)nOR?11 wherein n is 0 or is an integer of from 1 to 6, each of R?11 and R12¿ is independently H or C¿1?-C6 alkyl and R?13 is C¿1-C6 alkyl; or any of R1 and R2, R2 and R3, R3 and R4 and R4 and R5, or R6 and R7, R7 and R8, R8 and R9 and R9 and R10, form together with the carbon atoms to which they are attached a benzene ring which is optionally substituted; and pharmaceutically acceptable salts and esters thereof; are inhibitors of the plasminogen activator inhibitor. | ||||||
| 93 | Diketopiperazin Derivate, deren Herstellung und deren Vervendung zum Färben von Kunststoffen | EP90109736.0 | 1990-05-22 | EP0403812A3 | 1991-04-10 | Höchstetter, Hans Dr. |
Verbindungen der Formeln
|
||||||
| 94 | Diketopiperazin Derivate, deren Herstellung und deren Vervendung zum Färben von Kunststoffen | EP90109736.0 | 1990-05-22 | EP0403812A2 | 1990-12-27 | Höchstetter, Hans Dr. |
Verbindungen der Formeln
|
||||||
| 95 | 약물 전달용 디케토피페라진염, 디케토모르포린염 또는 디케토디옥산염 | KR1020147011493 | 2005-08-23 | KR1020140069314A | 2014-06-09 | 레온-베이안드레아; 모예-셔먼데스타디; 윌슨브라이언알 |
| 디케토피페라진 카르복실레이트 염을 포함하는 생리활성제 전달 조성물이 제공된다. 관련된 상기 생리활성제 전달 조성물의 제조 및 사용에 관련된 방법 또한 제공된다. | ||||||
| 96 | 약물 전달용 디케토피페라진염, 디케토모르포린염 또는디케토디옥산염 | KR1020077006720 | 2005-08-23 | KR101306384B1 | 2013-09-09 | 레온-베이안드레아; 모예-셔먼데스타디; 윌슨브라이언알 |
| 디케토피페라진 카르복실레이트 염을 포함하는 생리활성제 전달 조성물이 제공된다. 관련된 상기 생리활성제 전달 조성물의 제조 및 사용에 관련된 방법 또한 제공된다. | ||||||
| 97 | 약물 전달용 디케토피페라진염, 디케토모르포린염 또는 디케토디옥산염 | KR1020137011089 | 2005-08-23 | KR1020130066695A | 2013-06-20 | 레온-베이안드레아; 모예-셔먼데스타디; 윌슨브라이언알 |
| 디케토피페라진 카르복실레이트 염을 포함하는 생리활성제 전달 조성물이 제공된다. 관련된 상기 생리활성제 전달 조성물의 제조 및 사용에 관련된 방법 또한 제공된다. | ||||||
| 98 | 신규 피페라진 아마이드 유도체 | KR1020107005485 | 2008-08-04 | KR101171507B1 | 2012-08-07 | 뎀로우헨리에타; 쿤베른트; 오브스트산더울리케; 뢰버스테판; 슐츠-가쉬탄자; 롸이트매튜 |
| 본 발명은 하기 화학식 I의 신규 피페라진 아마이드 유도체뿐만 아니라 이의 생리학적으로 허용가능한 염에 관한 것이다.
화학식 I 상기 식에서, R 1 내지 R 11 , W, X 및 Y는 명세서 및 청구범위에 정의된 바와 같다. 상기 화합물은 LXR 알파 및 LXR 베타에 결합하며 약제로서 사용될 수 있다. |
||||||
| 99 | 신규 피페라진 아마이드 유도체 | KR1020107005485 | 2008-08-04 | KR1020100043096A | 2010-04-27 | 뎀로우헨리에타; 쿤베른트; 오브스트산더울리케; 뢰버스테판; 슐츠-가쉬탄자; 롸이트매튜 |
| The invention is concerned with novel piperazine amide derivatives of formula (I) wherein Rto R, W, X and Y are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds bind to LXR alpha and LXR beta and can be used as medicaments. | ||||||
QQ群二维码
意见反馈
意见反馈