MX361923B - Compuestos macrociclicos totalmente sinteticos limitados de modo conformacional. - Google Patents

Compuestos macrociclicos totalmente sinteticos limitados de modo conformacional.

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Publication number
MX361923B
MX361923B MX2014011078A MX2014011078A MX361923B MX 361923 B MX361923 B MX 361923B MX 2014011078 A MX2014011078 A MX 2014011078A MX 2014011078 A MX2014011078 A MX 2014011078A MX 361923 B MX361923 B MX 361923B
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MX
Mexico
Prior art keywords
receptor
variety
ring system
activity
macrocycles
Prior art date
Application number
MX2014011078A
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English (en)
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MX2014011078A (es
Inventor
Obrecht Daniel
Ermert Philipp
Oumouch Said
Piettre Arnaud
Gosalbes Jean-François
Thommen Marc
Original Assignee
Polyphor Ag
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Application filed by Polyphor Ag filed Critical Polyphor Ag
Publication of MX2014011078A publication Critical patent/MX2014011078A/es
Publication of MX361923B publication Critical patent/MX361923B/es

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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D273/00Heterocyclic compounds containing rings having nitrogen and oxygen atoms as the only ring hetero atoms, not provided for by groups C07D261/00 - C07D271/00
    • C07D273/02Heterocyclic compounds containing rings having nitrogen and oxygen atoms as the only ring hetero atoms, not provided for by groups C07D261/00 - C07D271/00 having two nitrogen atoms and only one oxygen atom
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
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    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
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    • A61P25/28Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
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    • A61P37/02Immunomodulators
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    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/08Antiallergic agents
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D291/00Heterocyclic compounds containing rings having nitrogen, oxygen and sulfur atoms as the only ring hetero atoms
    • C07D291/08Heterocyclic compounds containing rings having nitrogen, oxygen and sulfur atoms as the only ring hetero atoms condensed with carbocyclic rings or ring systems
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D498/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/04Ortho-condensed systems
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    • C07DHETEROCYCLIC COMPOUNDS
    • C07D498/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/08Bridged systems
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    • C07DHETEROCYCLIC COMPOUNDS
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    • C07D498/12Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
    • C07D498/18Bridged systems
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    • C07DHETEROCYCLIC COMPOUNDS
    • C07D515/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen, oxygen, and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D515/02Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen, oxygen, and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
    • C07D515/06Peri-condensed systems
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    • C07DHETEROCYCLIC COMPOUNDS
    • C07D515/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen, oxygen, and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D515/02Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen, oxygen, and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
    • C07D515/08Bridged systems
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D515/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen, oxygen, and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D515/12Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen, oxygen, and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains three hetero rings
    • C07D515/18Bridged systems
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    • C07D515/22Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen, oxygen, and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains four or more hetero rings

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Engineering & Computer Science (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Diabetes (AREA)
  • Immunology (AREA)
  • Pulmonology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Urology & Nephrology (AREA)
  • Endocrinology (AREA)
  • Hematology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Cardiology (AREA)
  • Dermatology (AREA)
  • Rheumatology (AREA)
  • Obesity (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Pain & Pain Management (AREA)
  • Psychiatry (AREA)
  • Oncology (AREA)
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  • Child & Adolescent Psychology (AREA)
  • Vascular Medicine (AREA)
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Abstract

El sistema de anillo macrocíclico de la formula (I) definido espacialmente y restringido de modo conformacional, se encuentra constituido por tres partes moleculares distintas: Plantilla A, Modulador B de conformación y Puente C. Los macrociclos descritos por este sistema de anillo I se fabrican fácilmente por síntesis en paralelo o química combinatorial en solución o en fase sólida. Se diseñan para interactuar con una variedad de clases de objetivos biológicos específicos, ejemplos son su actividad agonista o antagonista sobre los receptores acoplados a la proteína G (GPCR), la actividad inhibidora sobre las enzimas o su actividad antimicrobiana. En particular, estos macrociclos muestran una actividad inhibidora en la enzima que convierte endotelina del subtipo 1 (ECE-1) y/o la cisteína proteasa de catepsina S (CatS), y/o actúan como antagonistas del receptor de oxitocina (OT), el receptor de hormona que libera tirotropina (TRH) y/o receptor B4 de leucotrieno (LTB4), y/o como agonistas del receptor de bombesina 3 (BB3), y/o muestran actividad antimicrobiana contra al menos una cepa bacteriana. De este modo, también muestran gran potencial como medicamentos para una variedad de enfermedades.
MX2014011078A 2012-03-17 2013-03-15 Compuestos macrociclicos totalmente sinteticos limitados de modo conformacional. MX361923B (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP12001830 2012-03-17
PCT/EP2013/055368 WO2013139697A1 (en) 2012-03-17 2013-03-15 Conformationally constrained, fully synthetic macrocyclic compounds

Publications (2)

Publication Number Publication Date
MX2014011078A MX2014011078A (es) 2014-11-21
MX361923B true MX361923B (es) 2018-12-19

Family

ID=47882188

Family Applications (1)

Application Number Title Priority Date Filing Date
MX2014011078A MX361923B (es) 2012-03-17 2013-03-15 Compuestos macrociclicos totalmente sinteticos limitados de modo conformacional.

Country Status (13)

Country Link
US (1) US10017481B2 (es)
EP (1) EP2836485B1 (es)
JP (1) JP6111276B2 (es)
CN (1) CN104284891B (es)
AU (1) AU2013234499B2 (es)
CA (1) CA2867494C (es)
DK (1) DK2836485T3 (es)
HK (1) HK1206032A1 (es)
IL (1) IL234595A (es)
MX (1) MX361923B (es)
NZ (1) NZ630901A (es)
SG (1) SG11201405628YA (es)
WO (1) WO2013139697A1 (es)

Families Citing this family (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2008104090A1 (en) 2007-02-28 2008-09-04 Polyphor Ag Template-fixed peptidomimetics
WO2016061097A1 (en) * 2014-10-13 2016-04-21 Atrin Pharmaceuticals LLC Ataxia telengiectasia and rad3-related (atr) protein kinase inhibitors
GB201509006D0 (en) * 2015-05-26 2015-07-08 Redx Pharma Plc Antibacterial compounds
WO2017063757A1 (en) 2015-10-12 2017-04-20 Polyphor Ag Conformationally constrained macrocyclic compounds
WO2017063755A1 (en) 2015-10-12 2017-04-20 Polyphor Ag Conformationally constrained macrocyclic compounds
WO2017063754A1 (en) 2015-10-12 2017-04-20 Polyphor Ag Conformationally constrained macrocyclic compounds as pin1 modulators
GB201705686D0 (en) * 2017-04-07 2017-05-24 Centauri Therapeutics Ltd Novel compounds and therapeutic uses thereof
CA3155885A1 (en) 2019-11-25 2021-06-03 Lewis D. Pennington Substituted macrocyclic compounds and related methods of treatment
US11760747B2 (en) 2020-12-21 2023-09-19 Alkermes, Inc. Substituted piperidino compounds and related methods of treatment
WO2023225661A1 (en) * 2022-05-20 2023-11-23 Bristol-Myers Squibb Company Macrocyclic immunomodulators

Family Cites Families (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR2399247A1 (fr) * 1977-08-04 1979-03-02 Rhone Poulenc Ind Antibiotique 35665 rp, sa preparation et les compositions qui les contiennent
JPS6016236B2 (ja) * 1977-11-18 1985-04-24 武田薬品工業株式会社 抗生物質c―15003 p―3の製造法
CN102584940B (zh) * 2005-01-13 2014-12-31 卧龙岗大学 肽化合物
CL2008000629A1 (es) * 2007-03-01 2008-08-29 Chugai Pharmaceutical Co Ltd Compuestos macrociclicos derivados de 6-aril-4-mercapto-[1.3.5]triazina/[1.3]pirimidin-2-amina; composicion farmaceutica, utiles en el tratamiento del cancer.
US7732434B2 (en) * 2007-04-20 2010-06-08 Bristol-Myers Squibb Company Macrocyclic acyl guanidines as beta-secretase inhibitors
MX2011012155A (es) * 2009-05-13 2012-02-28 Enanta Pharm Inc Compuestos macrociclicos como inhibidores del virus de hepatitis c.
EP2462147B8 (en) * 2009-08-05 2015-03-18 Polyphor AG Conformationally constrained, fully synthetic macrocyclic compounds

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HK1206032A1 (en) 2015-12-31
EP2836485A1 (en) 2015-02-18
EP2836485B1 (en) 2018-01-10
WO2013139697A1 (en) 2013-09-26
JP2015509970A (ja) 2015-04-02
SG11201405628YA (en) 2014-10-30
US10017481B2 (en) 2018-07-10
DK2836485T3 (en) 2018-04-23
AU2013234499A1 (en) 2014-10-09
US20150051183A1 (en) 2015-02-19
NZ630901A (en) 2015-09-25
AU2013234499B2 (en) 2017-07-27
CN104284891A (zh) 2015-01-14
CA2867494A1 (en) 2013-09-26
JP6111276B2 (ja) 2017-04-05
CN104284891B (zh) 2018-04-17
MX2014011078A (es) 2014-11-21
IL234595A (en) 2016-08-31
CA2867494C (en) 2020-03-24

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