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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

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.

3. 发明专利

AU2009350857A1 Conformationally constrained, fully synthetic macrocyclic compounds 未知
公开(公告)号：AU2009350857A1
公开(公告)日：2012-02-02
申请号：AU2009350857
申请日：2009-08-05
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 , C07D498/18 , C07F7/08
摘要： Conformationally restricted, spatially defined 12-30 membered macrocyclic ring systems of type (I) are constituted by three distinct building blocks: an aromatic template a, a conformation modulator b and a spacer moiety c as detailed in the description and the claims. Macrocycles of type (I) are readily manufactured by parallel synthesis or combinatorial chemistry. They are designed to interact with specific biological targets. In particular, they show agonistic or antagonistic activity on the motilin receptor (MR receptor), on the serotonin receptor of subtype 5-HT (5-HT receptor), and on the prostaglandin F2 • receptor (FP receptor). They are thus potentially useful for the treatment of hypomotility disorders of the gastrointestinal tract such as diabetic gastroparesis and constipation type irritable bowl syndrome; of CNS related diseases like migraine, schizophrenia, psychosis or depression; of ocular hypertension such as associated with glaucoma and preterm labour.

4. 发明专利

DK2462147T3 Konformationelt begrænsede fuldsyntetiske makrocykliske forbindelser 未知
公开(公告)号：DK2462147T3
公开(公告)日：2015-02-23
申请号：DK09781527
申请日：2009-08-05
申请人： POLYPHOR AG
发明人： OBRECHT DANIEL , ERMERT PHILIPP , OUMOUCH SAID , LACH FRANCK , LUTHER ANATOL , MARX KARSTEN , MÖHLE KERSTIN
IPC分类号： C07D498/04 , A61K31/4745 , A61K31/695 , A61P1/06 , A61P25/24 , C07D498/18 , C07F7/08

5. 发明专利

AU2010281287A1 Conformationally constrained, fully synthetic macrocyclic compounds 未知
公开(公告)号：AU2010281287A1
公开(公告)日：2012-08-02
申请号：AU2010281287
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： 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 P2Y, as modulators of the serotonin receptor of subtype 5-HT, as blockers of the voltage-gated potassium channel K1.3 and as inhibitors of the &bgr;-catenin-dependent "canonical" Wnt pathway. Thus they are showing great potential as medicaments for a variety of diseases.

6. 发明专利

CA2780829C CONFORMATIONALLY CONSTRAINED, FULLY SYNTHETIC MACROCYCLIC COMPOUNDS 未知
公开(公告)号：CA2780829C
公开(公告)日：2018-04-10
申请号：CA2780829
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： 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.

7. 发明专利

AU2010281287B2 Conformationally constrained, fully synthetic macrocyclic compounds 未知
公开(公告)号：AU2010281287B2
公开(公告)日：2015-05-14
申请号：AU2010281287
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： 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 P2Y

8. 发明专利

ES2530519T3 Compuestos macrocíclicos completamente sintéticos, con conformación restringida 未知
公开(公告)号：ES2530519T3
公开(公告)日：2015-03-03
申请号：ES09781527
申请日：2009-08-05
申请人： POLYPHOR AG
发明人： OBRECHT DANIEL , ERMERT PHILIPP , OUMOUCH SAID , LACH FRANCK , LUTHER ANATOL , MARX KARSTEN , MÖHLE KERSTIN
IPC分类号： C07D498/04 , A61K31/4745 , A61K31/695 , A61P1/06 , A61P25/24 , C07D498/18 , C07F7/08
摘要： Compuestos de fórmula I, que incorporan los bloques componentes A, B y C.**Fórmula** en las que los restos a, b y c de los bloques componentes A, B y C son seleccionados de las tablas 1, 2 y 3, respectivamente, y son apropiadamente sustituidos independientemente, tal como se define a continuación,**Fórmula** en las que los sustituyentes R1 a R17 acoplados directamente a los bloques componentes A, B y C, se definen del modo siguiente: R1: H; F; Cl; Br; I; CF3; OCF3; OCHF2; NO2; CN; alquilo; alquenilo; alquinilo; cicloalquilo; heterocicloalquilo; arilo; heteroarilo; arilalquilo; heteroarilalquilo; -(CR18R19)qOR20; -(CR18R19)qSR20; -(CR18R19)qNR4R11; -(CR18R19)qOCONR4R11; -(CR18R19)qOCOOR21; -(CR18R19)qNR4COOR21; -(CR18R19)qNR4COR22 ; -(CR18R19)qNR4CONR4R11; -(CR18R19)qNR4SO2R23;-(CR18R19)qNR4SO2NR4R11; -(CR18R19)qCOOR21; -(CR18R19)qCONR4R11; -(CR18R19)qSO2NR4R11; -(CR18R19)qPO(OR21)2; -(CR18R19)qOPO(OR21)2; -(CR18R19)qCOR22; -(CR18R19)qSO2R23; -(CR18R19)qOSO3R21; -(CR18R19)qR24; -(CR18R19)qR25; o -(CR18R19)qR26; R2:H; CF3; alquilo; alquenilo; cicloalquilo; heterocicloalquilo; arilo; heteroarilo; arilalquilo; heteroarilalquilo; -(CR18R19)qOR20; -(CR18R19)qSR20; -(CR18R19)qNR4R11; -(CR18R19)qOCONR4R11; -(CR18R19)qOCOOR21; -(CR18R19)qNR4COOR21; -(CR18R19)qNR4COR22 ; -(CR18R19)qNR4CONR4R11; -(CR18R19)qNR4SO2R23; -(CR18R19)qNR4SO2NR4R11;-(CR18R19)qCOOR21; -(CR18R19)qCONR4R11; -(CR18R19)qSO2NR4R11; -(CR18R19)qPO(OR21)2; -(CR18R19)qCOR22; -(CR18R19)qSO2R23; -(CR18R19)qR24; -(CR18R19)qR25; o -(CR18R19)qR26; R3: H; CF3; alquilo; cicloalquilo; heterocicloalquilo; arilo; heteroarilo; arilalquilo; heteroarilalquilo; R4: H; aqluilo; alquenilo; cicloalquilo; heterocicloalquilo; arilo; heteroarilo; arilalquilo; heteroarilalquilo; R5, R7 y R9 se definen independientemente como: H; F; CF3; alquilo; alquenilo; cicloalquilo; heterocicloalquilo; arilo; heteroarilo; arilalquilo; heteroarilaquilo; -(CR18R19)sOR20; -(CR18R19)sSR20; -(CR18R19)sNR4R11; -(CR18R19)sOCONR4R11; -(CR18R19)sOCOOR21; -(CR18R19)sNR4COOR21; -(CR18R19)sNR4COR22 ; -(CR18R19)sNR4CONR4R11; -(CR18R19)sNR4SO2R23; -(CR18R19)sNR4SO2NR4R11; -(CR18R19)qCOOR21; -(CR18R19)qCONR4R11; -(CR18R19)qSO2NR4R11; -(CR18R19)qPO(OR21)2; -(CR18R19)qCOR22; -(CR18R19)qSO2R23; -(CR18R19)qR24; -(CR18R19)qR25; o -(CR18R19)qR26; R6, R8 y R10 se definen independientemente como: H; F; CF3; alquilo; alquenilo; cicloalquilo; heterocicloalquilo; arilo; heteroarilo; arilalquilo; o heteroarilaquilo; R11: H; alquilo; alquenilo; cicloalquilo; heterocicloalquilo; arilo; heteroarilo; arilalquilo; heteroarilalquilo; -(CR18R19)rOR20; -(CR18R19)rSR20; -(CR18R19)rNR4R27; -(CR18R19)rOCONR4R27; -(CR18R19)rOCOOR2; -(CR18R19)rNR4COOR21; -(CR18R19)rNR4CONR4R27; -(CR18R19)rNR4SO2R23; -(CR18R19)rNR4SO2NR4R27; -(CR18R19)qCOOR21; -(CR18R19)qCONR4R27; -(CR18R19)qCOR22; -(CR18R19)qSO2R23; -(CR18R19)qSO2NR4R27; -(CR18R19)qR24; -(CR18R19)sR25; o -(CR18R19)qR26; R12 y R13 se definen independientemente como H; o alquilo; R14 y R16 se definen independientemente como: H; F; CF3; alquilo; alquenilo; cicloalquilo; heterocicloalquilo; arilo; heteroarilo; arilalquilo; heteroarilaquilo; -(CR18R19)sOR20; -(CR18R19)sNR4R11; -(CR18R19)sNR4COOR21; -(CR18R19)sNR4COR22 ; -(CR18R19)sNR4CONR4R11; -(CR18R19)sNR4SO2R23; -(CR18R19)sNR4SO2NR4R11; -(CR18R19)qCOOR21; -(CR18R19)qCONR4R11; -(CR18R19)qSO2NR4R11; o -(CR18R19)qCOR22; R15 y R17 se definen independientemente como: H; F; CF3; alquilo; alquenilo; cicloalquilo; heterocicloalquilo; arilo; heteroarilo; arilalquilo; o heteroarilalquilo; en el que los sustituyentes R1 a R17 se definen del modo siguiente: R18: H; F; CF3; alquilo; alquenilo; cicloalquilo; heterocicloalquilo; arilo; heteroarilo; arilalquilo; heteroarilalquilo; -(CR29R30)sOR31; -(CR29R30)sSR31; -(CR29R30)sNR28R31; -(CR29R30)sOCONR28R31; -(CR29R30)sOCOOR21; -(CR29R30)sNR28COOR21; -(CR29R30)sNR28COR31; -(CR29R30)sNR28CONR28R31; -(CR29R30)sNR28SO2R23; -(CR29R30)sNR28SO2NR28R31; -(CR29R30)qCOOR21; -(CR29R30)qCONR28R31; -(CR29R30)qSO2NR28R31; -(CR29R30)qPO(OR21)2; -(CR29R30)qCOR31; -(CR29R30)qSO2R23; -(CR29R30)qR24; -(CR29R30)qR25; o -(CR29R30)qR26; R19: H; CF3; alquilo; alquenilo; cicloalquilo; heterocicloalquilo; arilo; heteroarilo; arilalquilo; heteroarilalquilo; R20: H; alquilo; alquenilo; cicloalquilo; heterocicloalquilo; arilo; heteroarilo; heteroarilalquilo; -(CR29R30)rOR31; -(CR29R30)rSR31; -(CR29R30)rNR28R31; -(CR29R30)rOCONR28R31; -(CR29R30)rNR28COOR21; -(CR29R30)rNR28COR31; -(CR29R30)rNR28CONR28R31; -(CR29R30)rNR28SO2R23;-(CR29R30)rNR28SO2NR28R31; -(CR29R30)qCOOR21; -(CR29R30)qCONR28R31; -(CR29R30)qSO2NR28R31; -(CR29R30)qCOR31; -(CR29R30)qSO2R23; -(CR29R30)qR24; -(CR29R30)qR25; o -(CR29R30)qR26; R21: alquilo; alquenilo; cicloalquilo; heterocicloalquilo; arilo; heteroarilo; arilalquilo; heteroarilalquilo; R22: alquilo; alquenilo; cicloalquilo; heterocicloalquilo; arilo; heteroarilo; arilalquilo; heteroarilalquilo; -(CR29R30)sOR31; -(CR29R30)sSR31; -(CR29R30)sNR28R31; -(CR29R30)sOCONR28R31; -(CR29R30)sNR28COOR21; -(CR29R30)sNR28COR31 ; -(CR29R30)sNR28CONR28R31; -(CR29R30)sNR28SO2R23; -(CR29R30)sNR28SO2NR28R31; -(CR29R30)sCOOR21; -(CR29R30)sCONR28R31; -(CR29R30)sSO2NR28R31; -(CR29R30)tCOR31; -(CR29R30)sSO2R23; -(CR29R30)tR24; -(CR29R30)tR25; o -(CR29R30)tR26; R23: H; alquilo; alquenilo; cicloalquilo; heterocicloalquilo; arilo; heteroarilo; arilalquilo; heteroarilalquilo; o bien -(CR32R33)tR24; R24: arilo, o un grupo opcionalmente sustituido del tipo C6H2R34R35R31; o un grupo heteroarilo, uno de los grupos de fórmulas H1-H34, tal como se muestran a continuación en la Tabla 4:

9. 发明专利

CA2780829A1 CONFORMATIONALLY CONSTRAINED, FULLY SYNTHETIC MACROCYCLIC COMPOUNDS 未知
公开(公告)号：CA2780829A1
公开(公告)日：2011-02-10
申请号：CA2780829
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： 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.

10. 发明专利

SG177521A1 CONFORMATIONALLY CONSTRAINED, FULLY SYNTHETIC MACROCYCLIC COMPOUNDS 未知
公开(公告)号：SG177521A1
公开(公告)日：2012-02-28
申请号：SG2012000766
申请日：2009-08-05
申请人： POLYPHOR AG
发明人： OBRECHT DANIEL , ERMERT PHILIPP , OUMOUCH SAID , LACH FRANCK , LUTHER ANATOL , MARX KARSTEN , MOEHLE KERSTIN
摘要： Conformationally restricted, spatially defined 12-30 membered macrocyclic ring systems of type (I) are constituted by three distinct building blocks: an aromatic template a, a conformation modulator b and a spacer moiety c as detailed in the description and the claims. Macrocycles of type (I) are readily manufactured by parallel synthesis or combinatorial chemistry. They are designed to interact with specific biological targets. In particular, they show agonistic or antagonistic activity on the motilin receptor (MR receptor), on the serotonin receptor of subtype 5-HT2B (5-HT2B receptor), and on the prostaglandin F2 • receptor (FP receptor). They are thus potentially useful for the treatment of hypomotility disorders of the gastrointestinal tract such as diabetic gastroparesis and constipation type irritable bowl syndrome; of CNS related diseases like migraine, schizophrenia, psychosis or depression; of ocular hypertension such as associated with glaucoma and preterm labour.

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