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91. 发明专利

AU2013234499A1 Conformationally constrained, fully synthetic macrocyclic compounds 未知
公开(公告)号：AU2013234499A1
公开(公告)日：2014-10-09
申请号：AU2013234499
申请日：2013-03-15
申请人： POLYPHOR AG
发明人： OBRECHT DANIEL , ERMERT PHILIPP , OUMOUCH SAID , PIETTRE ARNAUD , GOSALBES JEAN-FRANCOIS , THOMMEN MARC
IPC分类号： C07D273/02 , A61K31/395 , A61P31/04 , C07D291/08 , C07D498/04 , C07D498/18 , C07D515/06 , C07D515/18 , C07D515/22
摘要： The conformationally restricted, spatially defined macrocyclic ring system of formula (I) is constituted by three distinct molecular parts: Template A, conformation Modulator B and Bridge C. Macrocycles described by this ring system I are readily manufactured by parallel synthesis or combinatorial chemistry in solution or on solid phase. They are designed to interact with a variety of specific biological target classes, examples being agonistic or antagonistic activity on G-protein coupled receptors (GPCRs), inhibitory activity on enzymes or antimicrobial activity. In particular, these macrocycles show inhibitory activity on endothelin converting enzyme of subtype 1 (ECE-1 ) and/or the cysteine protease cathepsin S (CatS), and/or act as antagonists of the oxytocin (OT) receptor, thyrotropin-releasing hormone (TRH) receptor and/or leukotriene B4 (LTB4) receptor, and/or as agonists of the bombesin 3 (BB3) receptor, and/or show antimicrobial activity against at least one bacterial strain. Thus they are showing great potential as medicaments for a variety of diseases.

92. 发明专利

MX2014003960A PEPTIDOMIMETICOS FIJADOS A PLANTILLA COMO INHIBIDORES DE RECEPTOR DE FORMIL-PEPTIDO 1. 未知
公开(公告)号：MX2014003960A
公开(公告)日：2014-05-14
申请号：MX2014003960
申请日：2012-10-02
申请人： POLYPHOR AG
发明人： OBRECHT DANIEL , ZIMMERMANN JOHANN , JUNG FRANÇOISE , LÖWE RALF , LEMERCIER GUILLAUME , CHEVALIER ERIC
IPC分类号： C07K7/64 , A61K38/04
摘要： Peptidomiméticos de horquilla ß fijados a plantilla novedosos de la fórmula general (I) ciclo[P1-P2-P3-P4-P5-P6-P7-P8-P9-P10-P11-P1 2-P13-P14-T1-T2] en donde los elementos T o P únicos son residuos de a-aminoácidos conectados en cualquier dirección que, dependiendo de sus posiciones en la cadena, son como se define en la descripción y las reivindicaciones, y sales de los mismos, tienen la propiedad de antagonizar el efecto biológico del receptor FRP1. Se pueden usar como medicamentos para tratar o prevenir enfermedades o condiciones en las áreas de enfermedades inflamatorias, condiciones alérgicas, trastornos inmunológicos, neuroinflamación, trastornos neurológicos, enfermedades obstructivas de las vías respiratorias, enfermedades infecciosas, lesiones por reperfusión isquémica y trastornos proliferativos tales como, por ejemplo, cáncer. Estos peptidomiméticos de horquilla ß pueden ser fabricados por un proceso que se basa en una estrategia sintética mixta de fase sólida y solución.

93. 发明专利

AU2012320674A1 Template -fixed peptidomimetics as inhibitors of FPR1 未知
公开(公告)号：AU2012320674A1
公开(公告)日：2014-03-20
申请号：AU2012320674
申请日：2012-10-02
申请人： POLYPHOR AG
发明人： JUNG FRANCOISE , OBRECHT DANIEL , LOWE RALF , ZIMMERMANN JOHANN , LEMERCIER GUILLAUME , CHEVALIER ERIC
IPC分类号： C07K7/64 , A61K38/04
摘要： Novel template-fixed &bgr;-hairpin peptidomimetics of the general formula (I): cyclo[P

94. 发明专利

NZ599667A CONFORMATIONALLY CONSTRAINED, FULLY SYNTHETIC MACROCYCLIC COMPOUNDS 未知
公开(公告)号：NZ599667A
公开(公告)日：2013-04-26
申请号：NZ59966710
申请日：2010-08-03
申请人： POLYPHOR AG
发明人： OBRECHT DANIEL , ERMERT PHILIPP , OUMOUCH SAID , LACH FRANCK , LUTHER ANATOL , MARX KARSTEN , MOHLE KERSTIN
IPC分类号： C07D498/04 , A61K31/4745 , A61K31/695 , A61P1/06 , A61P25/24 , C07D497/18 , C07D498/18 , C07F7/08
摘要： Disclosed are macrocyclic compounds according to formulae Ia or Ib, salts thereof, and methods for their preparation. Specific examples of Formulae Ia and Ib include: (2S,11S,19aS)-N-[2-(dimethylamino)ethyl]-15-fluoro-7,12-dimethyl-2-{ [(1-naphthylamino)carbonyl]amino} -5,S,13-trioxo-2,3,6,7,S,9,10,11,12,13,19,19a-dodecahydro-1H,5H-pyrro10[2,1-c][1,4,7,12]benzoxatriazacyclopentadecine1-carboxamide, N-[(45,65,10S)-14-methyl-6-[2-(2-naphthyl)acetyl]amino-9,15-dioxo-2-oxa-8,14-diazatricyclo[14.3.1.04,B]icosa-1(20),16,18-trien-10-yl]decanamide, and N-[(4S,6S,10S)-14-methyl-6-{ [2-(2-naphthyl)acetyl]amino} -9,15-dioxo-2-oxa-8,14-diazatricyclo[14.3.1.04,8]icosa-1(20),16,18-trien-10-yl]-6-phenylhexanamide. Compounds of formula Ia and Ib have agonistic or antagonistic activity on the motilin receptor (MR receptor), on the serotonin receptor of subtype 5-HT2B (5-HT2B receptor), on the prostaglandin F2alpha receptor (FP receptor) on the purinoreceptor P2Y1, on the voltage gated potassium channel Ky1.3, and on the canonical (beta-catenin-dependent) Wnt pathway. The compounds are useful for treating motility disorders of the gastrointestinal tract such as functional dyspepsia, diabetic gastroparesis or constipation type irritable bowel syndrome; of CNS related diseases like migraine, schizophrenia, psychosis, depression or Alzheimer disease; of ocular hypertension such as associated with glaucoma and of preterm labour; of CNS inflammatory disorders like multiple sclerosis; of thromboembolic disorders; of cell proliferation disorders, especially various cancer types; or of bone and cartilage-related disorders.

95. 发明专利

SG183180A1 TEMPLATE-FIXED PEPTIDOMIMETICS WITH CXCR7 MODULATING ACTIVITY 未知
公开(公告)号：SG183180A1
公开(公告)日：2012-09-27
申请号：SG2012057907
申请日：2011-02-04
申请人： POLYPHOR AG
发明人： GOMBERT FRANK OTTO , LEDERER ALEXANDER , LOEWE RALF , OBRECHT DANIEL , ROMAGNOLI BARBARA , ZIMMERMANN JOHANN , PATEL KALPANA
摘要： Novel template-fixed &bgr;-hairpin peptidomimetics of the general formula (I), wherein the single elements T or P are α-amino acid residues connected from the carbonyl (C=O) point of attachment to the nitrogen (N) of the next element in clockwise direction and wherein said elements, depending on their positions in the chain, are defined in the description and the claims have the property to act on the receptor CXCR7. Thus, these &bgr;-hairpin peptidomimetics can be useful in the treatment or prevention of diseases or conditions in the area of dermatological disorders, metabolic diseases, inflammatory diseases, fibrotic diseases, infectious diseases, neurological diseases, cardiovascular diseases, respiratory diseases, gastro-intestinal tract disorders, urological diseases, ophthalmic diseases, stomatological diseases, haematological diseases and cancer; or the mobilisation of stem cells.

96. 发明专利

AU2010344997A1 Template - fixed peptidomimetics with CXCR7 modulating activity 未知
公开(公告)号：AU2010344997A1
公开(公告)日：2012-08-30
申请号：AU2010344997
申请日：2010-02-05
申请人： POLYPHOR AG
发明人： GOMBERT FRANK OTTO , LEDERER ALEXANDER , OBRECHT DANIEL , ROMAGNOLI BARBARA , BISANG CHRISTIAN , LUDIN CHRISTIAN
IPC分类号： C07K7/64 , A61K38/12 , C07K14/72
摘要： Specific template-fixed &bgr;- hairpin peptidomimetics of the general formula (I) wherein the single elements T or P are α-amino acid residues connected from the carbonyl (C=O) point of attachment to the nitrogen (N) of the next element in clockwise direction and wherein said elements, depending on their positions in the chain, are defined in the description and the claims have the property to act on the receptor CXCR7. Thus, these &bgr;-hairpin peptidomimetics can be useful in the treatment or prevention of diseases or conditions in the area of dermatological disorders, metabolic diseases, inflammatory diseases, fibrotic diseases, infectious diseases, neurological diseases, cardiovascular diseases, respiratory diseases, gastro-intestinal tract disorders, urological diseases, ophthalmic diseases, stomatological diseases, haematological diseases and cancer; or the mobilisation of stem cells.

97. 发明专利

AU2008360223A1 Template-fixed peptidomimetics 未知
公开(公告)号：AU2008360223A1
公开(公告)日：2010-02-11
申请号：AU2008360223
申请日：2008-08-08
申请人： POLYPHOR AG , UNIV ZUERICH
发明人： ROBINSON JOHN ANTHONY , MOHLE KERSTIN , SEITZ MARKUS , MAILLARD LUDOVIC T , MOUNME ROBA , GOMBERT FRANK OTTO , SELLIER-KESSLER ODILE , HENZE HEIKO , OBRECHT DANIEL , BISANG CHRISTIAN , LEDERER ALEXANDER
IPC分类号： C07K7/56 , C07K1/02 , C07K7/64

98. 发明专利

NO20055585L 未知
公开(公告)号：NO20055585L
公开(公告)日：2005-11-25
申请号：NO20055585
申请日：2005-11-25
申请人： POLYPHOR AG
发明人： GOMBERT FRANK , ZUMBRUNN JUERG , DEMARCO STEVEN J , MUKHERJEE RESHIMI , MOEHLE KERSTIN , ROBINSON JOHN ANTHONY , HENZE HEIKO , ROMAGNOLI BARBARA , VRIJBLOD JAN , OBRECHT DANIEL , LUDIN CHRISTIAN
IPC分类号： A61K38/00 , A61K38/12 , C07K1/04 , C07K7/64
摘要： Template-fixed ²-hairpin peptidomimetics of the general formula wherein Z is a template-fixed chain of 18 ±-amino acid residues which, depending on their positions in the chain (counted starting from the N-terminal amino acid), are Gly, NMeGly, Pro or Pip, or of certain types which, as the remaining symbols in the above formula, are defined in the description and the claims, and salts thereof, have CXCR4 antagonizing properties and can be used for preventing HIV infections in healthy individuals or for slowing and halting viral progression in infected patients; or where cancer is mediated or resulting from CXCR4 receptor activity; or where immunological diseases are mediated or resulting from CXCR4 receptor activity; or for treating immuno suppression; or during apheresis collections of peripheral blood stem cells. These ²-hairpin peptidomimetics can be manufactured by a process which is based on a mixed solid- and solution phase synthetic strategy.

99. 发明专利

CA2847486A1 TEMPLATE-FIXED BETA-HAIRPIN PEPTIDOMIMETICS WITH CXCR4 ANTAGONIZING ACTIVITY 未知
公开(公告)号：CA2847486A1
公开(公告)日：2004-11-11
申请号：CA2847486
申请日：2004-04-29
申请人： POLYPHOR AG , UNIV ZUERICH
发明人： ZUMBRUNN JURG , DEMARCO STEVEN J , MUKHERJEE RESHMI , MOEHLE KERSTIN , ROBINSON JOHN ANTHONY , HENZE HEIKO , ROMAGNOLI BARBARA , LOCIURO SERGIO , VRIJBLOED JAN WIM , GOMBERT FRANK , OBRECHT DANIEL , LUDIN CHRISTIAN
IPC分类号： C07K14/00 , A61K38/00 , A61K38/12 , A61K38/19 , A61P31/18 , C07K1/04 , C07K1/06 , C07K7/64 , C07K14/715 , C40B40/10
摘要： Template-fixed ²-hairpin peptidomimetics of the general formula wherein Z is a template-fixed chain of 18 ±-amino acid residues which, depending on their positions in the chain (counted starting from the N-terminal amino acid), are Gly, NMeGly, Pro or Pip, or of certain types which, as the remaining symbols in the above formula, are defined in the description and the claims, and salts thereof, have CXCR4 antagonizing properties and can be used for preventing HIV infections in healthy individuals or for slowing and halting viral progression in infected patients; or where cancer is mediated or resulting from CXCR4 receptor activity; or where immunological diseases are mediated or resulting from CXCR4 receptor activity; or for treating immuno suppression; or during apheresis collections of peripheral blood stem cells. These ²-hairpin peptidomimetics can be manufactured by a process which is based on a mixed solid- and solution phase synthetic strategy.

100. 发明专利

BR9917475A 未知
公开(公告)号：BR9917475A
公开(公告)日：2002-05-14
申请号：BR9917475
申请日：1999-08-30
申请人： POLYPHOR AG , UNIVERSITOT Z RICH
发明人： ROBINSON JOHN A , OBRECHT DANIEL
IPC分类号： C07K5/10 , C07H21/04 , C07K1/04 , C07K7/02 , C07K7/06 , C07K7/08 , C07K7/64 , C07K14/00 , G01N33/53
摘要： Template-fixed beta-hairpin loop mimetics comprising a template corresponding to one of the structures (a), (b), (c), (d), (e), (f), (g), (h) and a template-fixed chain of 4 to 20 alpha-amino acid residues which, if their alpha-C atom is asymmetric, have L-configuration can be manufactured by a novel process which is based on a mixed solid- and solution phase synthetic strategy. If desired, this process can be modified to give the enantiomers of these template-fixed beta-hairpin loop mimetics. These enantiomers are novel compounds, and many of said template-fixed beta-hairpin loop mimetics themselves are also novel compounds. The template-fixed beta-hairpin loop mimetics and their enantiomers can mimic flat surfaces of proteins and thus be used to probe large surface protein-protein interactions. Accordingly they can serve as lead finding tools for protein targets where it is difficult to find small-molecular-weight lead compounds.

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