EA201591078A1 - Пептиды в качестве агонистов окситоцина - Google Patents

Пептиды в качестве агонистов окситоцина

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Publication number
EA201591078A1
EA201591078A1 EA201591078A EA201591078A EA201591078A1 EA 201591078 A1 EA201591078 A1 EA 201591078A1 EA 201591078 A EA201591078 A EA 201591078A EA 201591078 A EA201591078 A EA 201591078A EA 201591078 A1 EA201591078 A1 EA 201591078A1
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EA
Eurasian Patent Office
Prior art keywords
lower alkyl
hydrogen atom
hydroxy group
cycloalkyl
substituted
Prior art date
Application number
EA201591078A
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English (en)
Other versions
EA026687B1 (ru
Inventor
Катерина Биссанц
Конрад Блайгер
Кристоф Грундшобер
Original Assignee
Ф. Хоффманн-Ля Рош Аг
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Publication date
Application filed by Ф. Хоффманн-Ля Рош Аг filed Critical Ф. Хоффманн-Ля Рош Аг
Publication of EA201591078A1 publication Critical patent/EA201591078A1/ru
Publication of EA026687B1 publication Critical patent/EA026687B1/ru

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K7/00—Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
    • C07K7/64—Cyclic peptides containing only normal peptide links
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • A61K38/04—Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
    • A61K38/08—Peptides having 5 to 11 amino acids
    • A61K38/095—Oxytocins; Vasopressins; Related peptides
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/20—Hypnotics; Sedatives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/22—Anxiolytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/24—Antidepressants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/32—Alcohol-abuse
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/04—Anorexiants; Antiobesity agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K7/00—Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
    • C07K7/04—Linear peptides containing only normal peptide links
    • C07K7/16—Oxytocins; Vasopressins; Related peptides
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal 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)
  • Pain & Pain Management (AREA)
  • Diabetes (AREA)
  • Anesthesiology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Child & Adolescent Psychology (AREA)
  • Hospice & Palliative Care (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Peptides Or Proteins (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

Изобретение относится к соединениям формулы (I), где Rпредставляет собой гидрокси или амино; Rпредставляет собой втор-бутил или изобутил; Rпредставляет собой низший алкил, низший алкил, замещенный гидроксигруппой, -(CH)C(O)-NH, -(CH)-NHили -СН-пятичленную ароматическую гетероциклическую группу; Rпредставляет собой атом водорода или низший алкил; Rпредставляет собой атом водорода или низший алкил или Rи Rмогут образовать вместе с атомом N и С, к которому они присоединены, пирролидиновое кольцо, необязательно замещенное гидроксигруппой или атомом галогена, пиперидиновое кольцо или азетидиновое кольцо; Rпредставляет собой атом водорода, низший алкил, низший алкил, замещенный гидроксигруппой, -(СН)С(О)ОН, -(CH)C(O)NH, бензил, необязательно замещенный амино- или гидроксигруппой, -СН-пятичленную ароматическую гетероциклическую группу, индолил, -СН-циклоалкил, циклоалкил, -(CH)-S-низший алкил или представляет собой -(CH)-NH; R представляет собой атом водорода или низший алкил или Rи Rвместе представляют собой циклоалкил; X представляет собой -C(O)-CHR-NR'-C(O)-; R/R' независимо друг от друга представляют собой атом водорода или низший алкил; m равно 2; о равно 0 или 1; или к их фармацевтически приемлемой соли присоединения кислоты, к рацемической смеси или к ее соответствующему энантиомеру и/или оптическим изомерам. Обнаружено, что настоящие соединения являются агонистами рецептора окситоцина для лечения аутизма, стресса, включая посттравматическое стрессовое расстройство, тревоги, включая тревожные расстройства и депрессию, шизофрении, психиатрических расстройств и потери памяти, отмены алкоголя, привыкания к лекарственным средствам, а также для лечения синдрома Прадера-Вилли.
EA201591078A 2012-12-21 2013-12-17 Пептиды в качестве агонистов окситоцина EA026687B1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP12199012 2012-12-21
PCT/EP2013/076783 WO2014095773A1 (en) 2012-12-21 2013-12-17 Peptides as oxytocin agonists

Publications (2)

Publication Number Publication Date
EA201591078A1 true EA201591078A1 (ru) 2015-10-30
EA026687B1 EA026687B1 (ru) 2017-05-31

Family

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EA201591078A EA026687B1 (ru) 2012-12-21 2013-12-17 Пептиды в качестве агонистов окситоцина

Country Status (34)

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

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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
PE20151446A1 (es) 2015-09-28
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
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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