PE20151446A1 - Peptidos como agonistas de oxitocina - Google Patents

Peptidos como agonistas de oxitocina

Info

Publication number
PE20151446A1
PE20151446A1 PE2015001058A PE2015001058A PE20151446A1 PE 20151446 A1 PE20151446 A1 PE 20151446A1 PE 2015001058 A PE2015001058 A PE 2015001058A PE 2015001058 A PE2015001058 A PE 2015001058A PE 20151446 A1 PE20151446 A1 PE 20151446A1
Authority
PE
Peru
Prior art keywords
lower alkyl
hydrogen
hydroxy
cycloalkyl
amino
Prior art date
Application number
PE2015001058A
Other languages
English (en)
Inventor
Caterina Bissantz
Konrad Bleicher
Christophe Grundschober
Original Assignee
Hoffmann La Roche
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Hoffmann La Roche filed Critical Hoffmann La Roche
Publication of PE20151446A1 publication Critical patent/PE20151446A1/es

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Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K7/00Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
    • C07K7/64Cyclic peptides containing only normal peptide links
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides
    • A61K38/04Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
    • A61K38/08Peptides having 5 to 11 amino acids
    • A61K38/095Oxytocins; Vasopressins; Related peptides
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00Drugs for disorders of the muscular or neuromuscular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/18Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/20Hypnotics; Sedatives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/22Anxiolytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/24Antidepressants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/30Drugs for disorders of the nervous system for treating abuse or dependence
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/30Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/32Alcohol-abuse
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/04Anorexiants; Antiobesity agents
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K7/00Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
    • C07K7/04Linear peptides containing only normal peptide links
    • C07K7/16Oxytocins; Vasopressins; Related peptides
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Neurology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Psychiatry (AREA)
  • Genetics & Genomics (AREA)
  • Biochemistry (AREA)
  • Molecular Biology (AREA)
  • Biophysics (AREA)
  • Addiction (AREA)
  • Epidemiology (AREA)
  • Immunology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Hematology (AREA)
  • Anesthesiology (AREA)
  • Obesity (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pain & Pain Management (AREA)
  • Hospice & Palliative Care (AREA)
  • Diabetes (AREA)
  • Child & Adolescent Psychology (AREA)
  • Peptides Or Proteins (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

La invencion se refiere a compuestos de la formula (I); en la que: R1 es hidroxi o amino; R2 es sec-butilo o isobutilo; R3 es alquilo inferior, alquilo inferior sustituido por hidroxi, -(CH2)2C(O)-NH2, -(CH2)3-NH2 o -CH2-grupo heterociclico aromatico de cinco eslabones; R4 es hidrogeno o alquilo inferior; R5 es hidrogeno o alquilo inferior; o R4 y R5 junto con los atomos de N y C a los que estan unidos pueden formar un anillo de pirrolidina, opcionalmente sustituido por hidroxi o halogeno, un anillo de piperidina o un anillo de azetidina; R6 es hidrogeno, alquilo inferior, alquilo inferior sustituido por hidroxi, -(CH2)2C(O)OH, -(CH2)2C(O)NH2, bencilo opcionalmente sustituido por amino o hidroxi, -CH2-grupo heterociclico aromatico de cinco eslabones, indolilo, -CH2-ciclo alquilo, cicloalquilo, -(CH2)2-S-alquilo inferior o es - (CH2)1-4-NH2; R6' es hidrogeno o alquilo inferior; o R6 y R6' juntos son cicloalquilo; X es -C(O) -CHR-NR' -C(O)-; R/R' con independencia entre si son hidrogeno o alquilo inferior; m es el numero 2; "o" es el numero 0 o 1; o a una sal de adicion de acido farmaceuticamente aceptable, a una mezcla racemica o a sus enantiomeros correspondientes y/o isomeros opticos de los mismos. Dichos compuestos son agonistas de receptores de oxitocina y son utiles en el tratamiento del autismo, el estres, incluido el trastorno del estres postraumatico, la ansiedad, incluidos los trastornos de ansiedad y la depresion, la esquizofrenia y trastornos psiquiatricos
PE2015001058A 2012-12-21 2013-12-17 Peptidos como agonistas de oxitocina PE20151446A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP12199012 2012-12-21

Publications (1)

Publication Number Publication Date
PE20151446A1 true PE20151446A1 (es) 2015-09-28

Family

ID=47471593

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2015001058A PE20151446A1 (es) 2012-12-21 2013-12-17 Peptidos como agonistas de oxitocina

Country Status (34)

Country Link
US (1) US9868766B2 (es)
EP (1) EP2935312B1 (es)
JP (1) JP6067878B2 (es)
KR (1) KR101819804B1 (es)
CN (1) CN104870466B (es)
AR (1) AR094225A1 (es)
AU (1) AU2013363768B2 (es)
BR (1) BR112015014010A2 (es)
CA (1) CA2895150C (es)
CL (1) CL2015001724A1 (es)
CR (1) CR20150271A (es)
DK (1) DK2935312T3 (es)
EA (1) EA026687B1 (es)
ES (1) ES2690317T3 (es)
HK (1) HK1208477A1 (es)
HR (1) HRP20181569T1 (es)
HU (1) HUE039848T2 (es)
IL (1) IL239519A (es)
LT (1) LT2935312T (es)
MA (1) MA38272A1 (es)
MX (1) MX358684B (es)
MY (1) MY176398A (es)
NZ (1) NZ708175A (es)
PE (1) PE20151446A1 (es)
PH (1) PH12015501145B1 (es)
PL (1) PL2935312T3 (es)
PT (1) PT2935312T (es)
RS (1) RS57690B1 (es)
SG (1) SG11201504883PA (es)
SI (1) SI2935312T1 (es)
TW (1) TWI558726B (es)
UA (1) UA119034C2 (es)
WO (1) WO2014095773A1 (es)
ZA (1) ZA201504186B (es)

Families Citing this family (17)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US10039777B2 (en) 2012-03-20 2018-08-07 Neuro-Lm Sas Methods and pharmaceutical compositions of the treatment of autistic syndrome disorders
UA111305C2 (uk) 2012-12-21 2016-04-11 Пфайзер Інк. Конденсовані лактами арилу та гетероарилу
KR101819804B1 (ko) 2012-12-21 2018-01-17 에프. 호프만-라 로슈 아게 옥시토신 작용제로서의 펩타이드
EP3421482A1 (en) 2012-12-21 2019-01-02 Alios Biopharma, Inc. Substituted nucleosides, nucleotides and analogs thereof
KR102116107B1 (ko) 2013-12-30 2020-05-28 삼성디스플레이 주식회사 표시 장치
WO2015106200A2 (en) 2014-01-10 2015-07-16 Cornell University Dipeptides as inhibitors of human immunoproteasomes
PE20161559A1 (es) 2014-06-03 2017-01-12 Hoffmann La Roche Peptidos como agonistas de la oxitocina
AP2016009605A0 (en) 2014-06-17 2016-12-31 Pfizer Substituted dihydroisoquinolinone compounds
US10588980B2 (en) 2014-06-23 2020-03-17 Novartis Ag Fatty acids and their use in conjugation to biomolecules
TR201815872T4 (tr) * 2014-08-07 2018-11-21 Hoffmann La Roche Oksitosin analoglarının hazırlanması için prosesler.
WO2016028571A2 (en) * 2014-08-18 2016-02-25 Cornell University Dipeptidomimetics as inhibitors of human immunoproteasomes
US10441627B2 (en) 2014-09-19 2019-10-15 Ferring B.V. Method of treating prader-willi syndrome
EP3362754B1 (en) 2015-10-15 2021-12-22 Cornell University Proteasome inhibitors and uses thereof
EP3694605A4 (en) 2017-10-11 2021-10-27 Cornell University PEPTIDOMIMETIC PROTEASOME INHIBITORS
WO2020061414A1 (en) 2018-09-20 2020-03-26 Levo Therapeutics, Inc. Stable intranasal formulations of carbetocin
TW202034899A (zh) 2018-09-20 2020-10-01 克里斯托弗 S 布萊恩特 卡貝縮宮素藥品及其製備方法
WO2021126990A1 (en) * 2019-12-16 2021-06-24 The Scripps Research Institute Oxytocin derivatives with improved properties

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8673841B2 (en) 2008-03-31 2014-03-18 Ferring B.V. Oxytocin analogues
TWI463990B (zh) * 2009-09-21 2014-12-11 Ferring Bv 催產素受體促進劑
ES2509270T3 (es) * 2009-10-01 2014-10-17 The University Of Sydney Terapia y prevención del alcoholismo
KR101819804B1 (ko) 2012-12-21 2018-01-17 에프. 호프만-라 로슈 아게 옥시토신 작용제로서의 펩타이드

Also Published As

Publication number Publication date
CN104870466A (zh) 2015-08-26
KR20150085845A (ko) 2015-07-24
US20150284434A1 (en) 2015-10-08
WO2014095773A1 (en) 2014-06-26
CR20150271A (es) 2015-08-28
MY176398A (en) 2020-08-05
MX358684B (es) 2018-08-31
PL2935312T3 (pl) 2018-12-31
KR101819804B1 (ko) 2018-01-17
SG11201504883PA (en) 2015-07-30
TWI558726B (zh) 2016-11-21
JP6067878B2 (ja) 2017-01-25
PH12015501145A1 (en) 2015-08-10
TW201429994A (zh) 2014-08-01
CA2895150A1 (en) 2014-06-26
PT2935312T (pt) 2018-10-26
CN104870466B (zh) 2018-05-18
EA026687B1 (ru) 2017-05-31
DK2935312T3 (en) 2018-10-22
SI2935312T1 (sl) 2018-11-30
CL2015001724A1 (es) 2015-10-16
PH12015501145B1 (en) 2015-08-10
AU2013363768A1 (en) 2015-06-04
MA38272A1 (fr) 2017-07-31
JP2016503044A (ja) 2016-02-01
HUE039848T2 (hu) 2019-02-28
IL239519A (en) 2017-06-29
EA201591078A1 (ru) 2015-10-30
MX2015007365A (es) 2015-10-14
IL239519A0 (en) 2015-08-31
ES2690317T3 (es) 2018-11-20
RS57690B1 (sr) 2018-11-30
AU2013363768B2 (en) 2016-02-04
EP2935312B1 (en) 2018-08-08
BR112015014010A2 (pt) 2017-07-11
EP2935312A1 (en) 2015-10-28
UA119034C2 (uk) 2019-04-25
CA2895150C (en) 2019-11-26
AR094225A1 (es) 2015-07-22
US9868766B2 (en) 2018-01-16
NZ708175A (en) 2020-06-26
HK1208477A1 (en) 2016-03-04
ZA201504186B (en) 2016-04-28
LT2935312T (lt) 2018-10-25
HRP20181569T1 (hr) 2018-11-30

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