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1. 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。

2. 发明专利

AU2016235590B2 Beta-hairpin peptidomimetics 未知
公开(公告)号：AU2016235590B2
公开(公告)日：2020-09-17
申请号：AU2016235590
申请日：2016-03-23
申请人： POLYPHOR AG
发明人： OBRECHT DANIEL , LUTHER ANATOL , BERNARDINI FRANCESCA , ZBINDEN PETER , LEDERER ALEXANDER
IPC分类号： C07K7/08 , C07K7/60 , C07K7/64
摘要： Beta-hairpin peptidomimetics of the general formula (I), and pharmaceutically acceptable salts thereof, with P, T, Q., and optionally L being elements as defined in the description and the claims, have Gram-negative antimicrobial activity to e.g. inhibit the growth or to kill microorganisms such as

3. 发明专利

CA2963226A1 BETA-HAIRPIN PEPTIDOMIMETICS 未知
公开(公告)号：CA2963226A1
公开(公告)日：2016-04-07
申请号：CA2963226
申请日：2015-09-29
申请人： POLYPHOR AG
发明人： OBRECHT DANIEL , LUTHER ANATOL , BERNARDINI FRANCESCA , ZBINDEN PETER , BARTHELEMY SOPHIE , LEDERER ALEXANDER
IPC分类号： C07K7/64 , C07K7/08 , C07K7/50
摘要： Beta-hairpin peptidomimetics of the general formula (I), cyclo[P1-P2-P3-P4-P5-P6- P7-P8-P9-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 Gramnegative 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.

4. 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.

5. 发明专利

NZ712739A Beta-hairpin peptidomimetics 未知
公开(公告)号：NZ712739A
公开(公告)日：2021-07-30
申请号：NZ71273914
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： Beta-hairpin peptidomimetics of the general formula (I), cyclo[P1-p2-p3-p4-p5-p6- p7-p8.p9- 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 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.

6. 发明专利

EA035407B1 БЕТА-ШПИЛЕЧНЫЕ ПЕПТИДОМИМЕТИКИ 未知
公开(公告)号：EA035407B1
公开(公告)日：2020-06-09
申请号：EA201591895
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： -Шпилечныепептидомиметикиобщейформулы (I), цикло[P-P-P-P-P-P-P-P-P-P-P-P-T-T] иихфармацевтическиприемлемыесоли, вкоторых P-P, Tи Tявляютсяэлементами, какопределенов описаниии формулеизобретения, имеющиеширокийспектрпротивомикробнойактивностипоотношениюк грамотрицательнымбактериям, напримерактивностиингибироватьростилиубиватьмикроорганизмы, такиекак Klebsiella pneumoniae и/или Acinetobacter baumannii, и/или Escherichia coli. Онимогутприменятьсяв качествелекарственныхсредствдлялеченияилипрофилактикиинфекцийилив качестведезинфицирующихсредствдляпищевыхпродуктов, косметическихсредств, лекарственныхсредствилидругихматериалов, содержащихпитательныевещества. Этипептидомиметикимогутбытьполученыс помощьюспособа, восновекотороголежитсмешаннаястратегиятвердофазногосинтезаи синтезав растворе.

7. 发明专利

SG11202003773UA BETA-HAIRPIN PEPTIDOMIMETICS 未知
公开(公告)号：SG11202003773UA
公开(公告)日：2020-05-28
申请号：SG11202003773U
申请日：2018-11-12
申请人： POLYPHOR AG
发明人： OBRECHT DANIEL , LUTHER ANATOL , BERNARDINI FRANCESCA , DALE GLENN , DESJONQUERES NICOLAS , BRABET EMILE , UPERT GRÉGORY
IPC分类号： C07K7/64 , A61K38/00
摘要： Beta-hairpin peptidomimetics of the general formula (I), and pharmaceutically acceptable salts thereof, with P, X, Q., and optionally L being elements as defined in the description and the claims, have Gram-negative antimicrobial activity to e.g. inhibit the growth or to kill microorganisms such as Klebsiella pneumoniae and/or Acinetobacterbaumannii and/or Escherichia coli and/or Pseudomonas aeruginosa and/or Enterobacter cloacae. 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

MX2015013762A PEPTIDOMIMETICOS BETA-HORQUILLA. 未知
公开(公告)号：MX2015013762A
公开(公告)日：2016-02-26
申请号：MX2015013762
申请日：2014-03-28
申请人： POLYPHOR AG
发明人： OBRECHT DANIEL , BERNARDINI FRANCESCA , LUTHER ANATOL , ZBINDEN PETER
IPC分类号： C07K7/64 , A61K38/12
摘要： Se describen peptidomiméticos beta-horquilla de fórmula general (I), ciclo[P1-p2-p3-p4-p5-p6-p7-p8-p9-p10-p11-p12-T1- T2] y las sales aceptadas para el uso farmacéutico de éstos, siendo P1 a P12, y T1 y T2 elementos definidos en la descripción y las reivindicaciones, los cuales tienen actividad de amplio espectro contra microbios Gram negativos, para, por ejemplo, inhibir el crecimiento o matar a microorganismos como puede ser Klebsiella pneumoniae y/o Acinetobacter baumannii y/o Escherichia coli. Estos pueden utilizarse como medicamentos para tratar o prevenir infecciones, o como desinfectantes para productos alimenticios, cosméticos, medicamentos u otros materiales que contengan nutrientes. Estos peptidomiméticos pueden ser fabricados mediante un proceso basado en una estrategia de síntesis en fase sólida y en solución, mixta.

9. 发明专利

SG11201507960RA BETA-HAIRPIN PEPTIDOMIMETICS 未知
公开(公告)号：SG11201507960RA
公开(公告)日：2015-10-29
申请号：SG11201507960R
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： These peptidomimetics can be manufactured by a process which is based on a mixed solid- and solution phase synthetic strategy.

10. 发明专利

AU2014247188A1 Beta-hairpin peptidomimetics 未知
公开(公告)号：AU2014247188A1
公开(公告)日：2015-10-22
申请号：AU2014247188
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： Beta-hairpin peptidomimetics of the general formula (I), cyclo[P

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