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1. 发明专利

BRPI0409928A 未知
公开(公告)号：BRPI0409928A
公开(公告)日：2006-04-25
申请号：BRPI0409928
申请日：2004-04-29
申请人： POLYPHOR AG , UNIVERSITOT ZUERICH
发明人： ZUMBRUNN JUERG , DEMARCO STEVEN J , MUKHERJEE RESHMI , ROBINSON JOHN ANTHONY , HENZE HEIKO , ROMAGNOLI BARBARA , LOCIURO SERGIO , VRIJBLOED JAN WIM , GOMBERT FRANK , 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.

2. 发明专利

BR0215855A 未知
公开(公告)号：BR0215855A
公开(公告)日：2005-07-12
申请号：BR0215855
申请日：2002-08-20
申请人： UNIVERSITOT ZUERICH , POLYPHOR LTD
发明人： VRIJBLOED JAN WIM , OBRECHT DANIEL , ROBINSON JOHN ANTHONY , SELLIER ODILE , KESSLER MARC
IPC分类号： A61K38/00 , A61P31/04 , C07K1/04 , C07K5/078 , C07K7/64 , C07K7/08 , A61K38/12
摘要： Template-fixed &bgr;-hairpin peptidomimetics of the general formula (I) wherein Z is a template-fixed chain of 12 α-amino acid residues which, depend on their positions in the chain (counted starting from the N-terminal amino acid) are Gly, or Pro, 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 the property to selectively inhibit the growth of or to kill microorganisms such as Pseudomonas aeruginosa and Acinetobacter. They can be used as disinfectants for foodstuffs, cosmetics, medicaments or other nutrient-containing materials, or as medicaments to treat or prevent infections. In a specific embodiment, the template is based on the D-Pro-L-Pro dipeptides. These &bgr;-hairpin peptidomimetics can be manufactured by processes which are based on a mixed solid—and solution phase synthetic strategy.

3. 发明专利

BRPI0707144A2 未知
公开(公告)号：BRPI0707144A2
公开(公告)日：2011-04-19
申请号：BRPI0707144
申请日：2007-01-15
申请人： POLYPHOR LTD , UNIVERSITOT ZUERICH
发明人： GOMBERT FRANK , OBRECHT DANIEL , VRIJBLOED WIM , DIAS RICARDO , DEMARCO STEVEN J , ROBINSON JOHN ANTHONY , SRINIVAS NITYAKALYANA
IPC分类号： C07K7/06 , A61K38/04 , C07K7/08 , C07K7/64 , C07K14/00
摘要： These β-hairpin peptidomimetics can be manufactured by processes which are based on a mixed solid- and solution phase synthetic strategy.

4. 发明申请

WO2011014973A3 CONFORMATIONALLY CONSTRAINED, FULLY SYNTHETIC MACROCYCLIC COMPOUNDS 审中-公开
标题翻译：构象受限的完全合成的大环化合物
公开(公告)号：WO2011014973A3
公开(公告)日：2011-04-21
申请号：PCT/CH2010000191
申请日：2010-08-03
申请人： POLYPHOR AG , OBRECHT DANIEL , ERMERT PHILIPP , OUMOUCH SAID , LACH FRANCK , LUTHER ANATOL , MARX KARSTEN , MOEHLE KERSTIN
发明人： OBRECHT DANIEL , ERMERT PHILIPP , OUMOUCH SAID , LACH FRANCK , LUTHER ANATOL , MARX KARSTEN , MOEHLE KERSTIN
IPC分类号： C07D498/04 , A61K31/4745 , A61K31/695 , A61P1/06 , A61P25/24 , C07D497/18 , C07D498/18 , C07F7/08
CPC分类号： C07D498/04 , A61K31/407 , A61K31/437 , A61K31/4985 , C07D497/18 , C07D498/18
摘要： Conformationally restricted, spatially defined 12-30 membered macrocyclic ring systems of formulae Ia and Ib are constituted by three distinct molecular parts: Template A, conformation Modulator B and Bridge C. These macrocycles Ia and Ib 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 the agonistic or antagonistic activity on G-protein coupled receptors (GPCRs), ion channels and signal transduction pathways. In particular, these macrocycles act as antagonists of the motilin receptor, the FP receptor and the purinergic receptors P2Y1, as modulators of the serotonin receptor of subtype 5-HT2B, as blockers of the voltage-gated potassium channel Kv1.3 and as inhibitors of the ß-catenin-dependent "canonical" Wnt pathway. Thus they are showing great potential as medicaments for a variety of diseases.
摘要翻译：式Ia和Ib的空间限定的12-30元大环系统由三个不同的分子部分构成：模板A，构象调节剂B和桥C.这些大环Ia和Ib易于通过平行合成或组合化学溶液或固相。它们被设计成与各种特定的生物靶类相互作用，例如对G蛋白偶联受体（GPCR），离子通道和信号转导途径的激动或拮抗活性。特别地，这些大环作为胃动素受体，FP受体和嘌呤能受体P2Y1的拮抗剂，作为5-HT2B亚型的血清素受体的调节剂，作为电压门控钾通道Kv1.3的阻断剂和作为 β-连环蛋白依赖的“典型”Wnt途径。因此，它们显示出作为用于各种疾病的药物的巨大潜力。

5. 发明申请

WO2010015287A3 TEMPLATE-FIXED PEPTIDOMIMETICS 审中-公开
标题翻译：模板固定蛋白质
公开(公告)号：WO2010015287A3
公开(公告)日：2010-04-15
申请号：PCT/EP2008060494
申请日：2008-08-08
申请人： POLYPHOR AG , UNIV ZUERICH , ROBINSON JOHN ANTHONY , MOEHLE KERSTIN , SEITZ MARKUS , MAILLARD LUDOVIC T , MOUNME ROBA , GOMBERT FRANK OTTO , SELLIER-KESSLER ODILE , HENZE HEIKO , OBRECHT DANIEL , BISANG CHRISTIAN , LEDERER ALEXANDER
发明人： ROBINSON JOHN ANTHONY , MOEHLE 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
CPC分类号： C07K1/02 , C07K7/56 , C07K7/64
摘要： Template-fixed ß-hairpin peptidomimetics of the general formula (I) wherein Z is a template-fixed chain of 8 a-amino acid residues which, depending on their positions in the chain (counted starting from the N-terminal amino acid), are GIy or Pro 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 agonizing or antagonizing activity against urotensin II or show inhibition of the STAT6/NCoA-1 interaction and can be used for preventing or treating diseases or disorders related to urotensin II, STAT6 and NCoA-1. These ß-hairpin peptidomimetics can be manufactured by a process which is based on a mixed solid- and solution phase synthetic strategy.
摘要翻译：通式（I）的模板固定的β-发夹肽模拟物，其中Z是8个α-氨基酸残基的模板固定链，其取决于其在链中的位置（从N-末端氨基酸开始计数），是Gly或Pro或某些类型，其作为上述式中的其余符号在说明书和权利要求书及其权利要求书中定义，并且具有针对泌尿前列腺素II的激动或拮抗活性或显示STAT6 / NCoA-1的抑制相互作用并且可以用于预防或治疗与泌尿前列腺素II，STAT6和NCoA-1相关的疾病或病症。这些β-发夹肽模拟物可以通过基于混合固相和溶液相合成策略的方法制备。

6. 发明专利

CA2908388C BETA-HAIRPIN PEPTIDOMIMETICS 未知
公开(公告)号：CA2908388C
公开(公告)日：2022-07-12
申请号：CA2908388
申请日：2014-03-28
申请人： POLYPHOR AG
发明人： OBRECHT DANIEL , LUTHER ANATOL , BERNARDINI FRANCESCA , ZBINDEN PETER
IPC分类号： C07K7/64 , A61K38/12
摘要： Beta-hairpin peptidomimetics of the general formula (I), cyclo(P1-p2-p3-p4-p5-p6- p7p8p9-p10-p11-p12-T1-T2], a nd pharmaceutically acceptable salts thereof, with P1 to P12, T1 and T2 being elements as defined in the description and the claims, have broad spectrum Gram-negative antimicrobial activity to e.g. inhibit the growth or to kill microorganisms such as Klebsiella pneumoniae and/or Acinetobacter baumannii and/or Escherichia coli. They can be used as medicaments to treat or prevent infections or as disinfectants for foodstuffs, cosmetics, medicaments or other nutrient-containing materials. These peptidomimetics can be manufactured by a process which is based on a mixed solid- and solution phase synthetic strategy.

7. 发明专利

NZ712736A Beta-hairpin peptidomimetics 未知
公开(公告)号：NZ712736A
公开(公告)日：2021-07-30
申请号：NZ71273614
申请日：2014-03-28
申请人： POLYPHOR AG
发明人： OBRECHT DANIEL , LUTHER ANATOL , BERNARDINI FRANCESCA , ZBINDEN PETER
IPC分类号： C07K7/64 , A61K38/12
摘要： Beta-hairpin peptidomimetics of the general formula (I), cyclo(P1-p2-p3-p4-p5-p6- p7p8p9-p10-p11-p12-T1-T2], a nd pharmaceutically acceptable salts thereof, with P1 to P12, T1 and T2 being elements as defined in the description and the claims, have broad spectrum Gram-negative antimicrobial activity to e.g. inhibit the growth or to kill microorganisms such as Klebsiella pneumoniae and/or Acinetobacter baumannii and/or Escherichia coli. They can be used as medicaments to treat or prevent infections or as disinfectants for foodstuffs, cosmetics, medicaments or other nutrient-containing materials. These peptidomimetics can be manufactured by a process which is based on a mixed solid- and solution phase synthetic strategy.

8. 发明专利

MA50565A PEPTIDOMIMÉTIQUES EN ÉPINGLE À CHEVEUX BÊTA 未知
公开(公告)号：MA50565A
公开(公告)日：2020-09-16
申请号：MA50565
申请日：2018-11-12
申请人： POLYPHOR AG
发明人： BERNARDINI FRANCESCA , BRABET EMILE , DALE GLENN E , DESJONQUERES NICOLAS , LUTHER ANATOL , OBRECHT DANIEL , UPERT GRÉGORY
IPC分类号： A61K38/00 , C07K7/64

9. 发明专利

CA2789030C TEMPLATE - FIXED PEPTIDOMIMETICS WITH CXCR7 MODULATING ACTIVITY 未知
公开(公告)号：CA2789030C
公开(公告)日：2020-07-21
申请号：CA2789030
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： A61K38/12 , C07K7/64 , C07K14/72
摘要： Specific template-fixed ß- hairpin peptidomimetics of the general formula (I) wherein the single elements T or P are a-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 ß-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.

10. 发明专利

ES2750528T3 Peptidomiméticos en horquilla beta 未知
公开(公告)号：ES2750528T3
公开(公告)日：2020-03-26
申请号：ES14714670
申请日：2014-03-28
申请人： POLYPHOR AG
发明人： OBRECHT DANIEL , LUTHER ANATOL , BERNARDINI FRANCESCA , ZBINDEN PETER
IPC分类号： C07K7/08 , C07K7/64
摘要： Compuesto de fórmula general (I), Ciclo[P1-P2-P3-P4-P5-P6-P7-P8-P9-P10-P11-P12-T1-T2] (I) en la que los elementos individuales T o P están conectados en cualquier dirección desde el punto de unión del carbonilo (C=O) al nitrógeno (N) del siguiente elemento, y en la que T1 es D10 Pro; T2 es Pro; Pro((3S)OH); Pro((4S)OBn); Pic; o Tic(7OH); P1 es Ala(CF3); Ala(2ClPhUr); Ala(4ClPhUr); Leu; Ile; Val; Nva; Trp; Phe, Tyr; Tza; o Thr; P2 es Ala; Abu; Ala(2ClPhUr); Ala(3PyrMeUr); Ala(4butoxiPhUr); Ala(iPrUr); Dab(2PyrMe); Dap; Dap(2,3-OH-propionilo); Dap(AcThr); Dap(iPr); Dap(Thr); Ser; Ser(Me); Hse; Thr; aloThr; Asp; Asn; o Gly; P3 es Chg; Cha; tBuGly; Phe; Phe (4NH2); Phe(4F); Tyr(3F); Phe(4CF3); Tyr; Tyr(Me); o Trp; P4 es Dab; Dab(2PyrMe); Dap; Orn; o Arg; P5 es Lys; Orn; Orn(iPr); Dap; Dab; o Arg; P6 es Dab; DDab; o Pip; P7 es Dab; Dab(2PyrMe); Dap; Orn; Arg; o DDab; P8 es Trp; P9 es Hse; Dab; Dap; Arg; o Lys; P10 es tBuGly; Ile; Val; Nva; Chg; Cha; Trp; Tyr; Tyr(Me); o Phg; P11 es Ala; Ser; Ser(Me); Tza; Agp; Tyr; Dab; Thr; Asn; Asp; o DAla; y P12 es Ser; Thr; Dap; Ala(iPrUr); Leu; o Tyr; o una sal aceptable farmacéuticamente del mismo; con la condición de que si P2 es Ala(2ClPhUr); Ala(3PyrMeUr); Ala(4butoxiPhUr); Ala(iPrUr); Dab(2PyrMe); Dap; Dap(2,3-OHpropionilo); Dap(AcThr); Dap(iPr); Dap(Thr); Ser(Me); Asp; o Asn; entonces P11 es Ala; Ser; Ser(Me); Thr; Asn; Asp; o D Ala.

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