EA201591078A1 - Пептиды в качестве агонистов окситоцина - Google Patents
Пептиды в качестве агонистов окситоцинаInfo
- 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
- Authority
- EA
- Eurasian Patent Office
- Prior art keywords
- lower alkyl
- hydrogen atom
- hydroxy group
- cycloalkyl
- substituted
- Prior art date
Links
- 239000000556 agonist Substances 0.000 title 1
- XNOPRXBHLZRZKH-DSZYJQQASA-N oxytocin Chemical compound C([C@H]1C(=O)N[C@H](C(N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CSSC[C@H](N)C(=O)N1)C(=O)N1[C@@H](CCC1)C(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)=O)[C@@H](C)CC)C1=CC=C(O)C=C1 XNOPRXBHLZRZKH-DSZYJQQASA-N 0.000 title 1
- 102000004196 processed proteins & peptides Human genes 0.000 title 1
- 108090000765 processed proteins & peptides Proteins 0.000 title 1
- 125000000217 alkyl group Chemical group 0.000 abstract 9
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 5
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 5
- 208000019901 Anxiety disease Diseases 0.000 abstract 2
- 125000006615 aromatic heterocyclic group Chemical group 0.000 abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 2
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 2
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 abstract 2
- -1 -CH-cycloalkyl Chemical group 0.000 abstract 1
- 208000000044 Amnesia Diseases 0.000 abstract 1
- 206010003805 Autism Diseases 0.000 abstract 1
- 208000020706 Autistic disease Diseases 0.000 abstract 1
- 208000020401 Depressive disease Diseases 0.000 abstract 1
- 208000026139 Memory disease Diseases 0.000 abstract 1
- 102000004279 Oxytocin receptors Human genes 0.000 abstract 1
- 108090000876 Oxytocin receptors Proteins 0.000 abstract 1
- RWRDLPDLKQPQOW-UHFFFAOYSA-N Pyrrolidine Chemical group C1CCNC1 RWRDLPDLKQPQOW-UHFFFAOYSA-N 0.000 abstract 1
- 239000002253 acid Substances 0.000 abstract 1
- 208000029650 alcohol withdrawal Diseases 0.000 abstract 1
- 230000036506 anxiety Effects 0.000 abstract 1
- 125000002393 azetidinyl group Chemical group 0.000 abstract 1
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 abstract 1
- 125000004432 carbon atom Chemical group C* 0.000 abstract 1
- 206010013663 drug dependence Diseases 0.000 abstract 1
- 125000005843 halogen group Chemical group 0.000 abstract 1
- 125000001041 indolyl group Chemical group 0.000 abstract 1
- 125000000959 isobutyl group Chemical group [H]C([H])([H])C([H])(C([H])([H])[H])C([H])([H])* 0.000 abstract 1
- 230000006984 memory degeneration Effects 0.000 abstract 1
- 208000023060 memory loss Diseases 0.000 abstract 1
- 239000000203 mixture Substances 0.000 abstract 1
- 125000004433 nitrogen atom Chemical group N* 0.000 abstract 1
- 230000003287 optical effect Effects 0.000 abstract 1
- 125000003386 piperidinyl group Chemical group 0.000 abstract 1
- 208000028173 post-traumatic stress disease Diseases 0.000 abstract 1
- 208000020016 psychiatric disease Diseases 0.000 abstract 1
- 239000000018 receptor agonist Substances 0.000 abstract 1
- 229940044601 receptor agonist Drugs 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 201000000980 schizophrenia Diseases 0.000 abstract 1
- 125000002914 sec-butyl group Chemical group [H]C([H])([H])C([H])([H])C([H])(*)C([H])([H])[H] 0.000 abstract 1
- 208000011117 substance-related disease Diseases 0.000 abstract 1
- 208000011580 syndromic disease Diseases 0.000 abstract 1
Classifications
-
- 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
Landscapes
- 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)
- Biophysics (AREA)
- Molecular Biology (AREA)
- Biochemistry (AREA)
- Addiction (AREA)
- Epidemiology (AREA)
- Immunology (AREA)
- Gastroenterology & Hepatology (AREA)
- Hematology (AREA)
- Hospice & Palliative Care (AREA)
- Obesity (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Physical Education & Sports Medicine (AREA)
- Anesthesiology (AREA)
- Pain & Pain Management (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
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.
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
ID=47471593
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| EA201591078A EA026687B1 (ru) | 2012-12-21 | 2013-12-17 | Пептиды в качестве агонистов окситоцина |
Country Status (33)
| 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) |
| 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) |
Families Citing this family (17)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2013139861A1 (en) | 2012-03-20 | 2013-09-26 | Luc Montagnier | Methods and pharmaceutical compositions of the treatment of autistic syndrome disorders |
| KR102788773B1 (ko) | 2012-12-21 | 2025-03-28 | 얀센 바이오파마, 인코퍼레이트. | 치환된 뉴클레오사이드, 뉴클레오타이드 및 그것의 유사체 |
| 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 |
| KR102116107B1 (ko) | 2013-12-30 | 2020-05-28 | 삼성디스플레이 주식회사 | 표시 장치 |
| ES2748434T3 (es) | 2014-01-10 | 2020-03-16 | Univ Cornell | Dipéptidos como inhibidores de inmunoproteasomas humanos |
| WO2015185467A1 (en) | 2014-06-03 | 2015-12-10 | F. Hoffmann-La Roche Ag | Peptides as oxytocin agonists |
| NZ726108A (en) | 2014-06-17 | 2020-06-26 | Pfizer | Substituted dihydroisoquinolinone compounds |
| US10588980B2 (en) | 2014-06-23 | 2020-03-17 | Novartis Ag | Fatty acids and their use in conjugation to biomolecules |
| HK1231495A1 (zh) * | 2014-08-07 | 2017-12-22 | 豪夫迈．罗氏有限公司 | 用於製備催產素類似物的方法 |
| US11202817B2 (en) | 2014-08-18 | 2021-12-21 | Cornell University | Dipeptidomimetics as inhibitors of human immunoproteasomes |
| HRP20240166T1 (hr) * | 2014-09-19 | 2024-04-26 | Ferring B.V. | Postupak liječenja prader-willijevog sindroma |
| US11066397B2 (en) | 2015-10-15 | 2021-07-20 | Cornell University | Proteasome inhibitors and uses thereof |
| EP3694605A4 (en) | 2017-10-11 | 2021-10-27 | Cornell University | PEPTIDOMIMETIC INHIBITORS OF PROTEASOME |
| CN112969450B (zh) | 2018-09-20 | 2023-05-30 | 阿卡蒂亚药品公司 | 卡贝缩宫素药物产品及用于制备其的方法 |
| JP7535050B2 (ja) | 2018-09-20 | 2024-08-15 | アカディア ファーマシューティカルズ インコーポレイテッド | カルベトシンの安定的鼻腔内製剤 |
| WO2021126990A1 (en) * | 2019-12-16 | 2021-06-24 | The Scripps Research Institute | Oxytocin derivatives with improved properties |
Family Cites Families (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| HRP20140716T1 (hr) | 2008-03-31 | 2014-08-29 | Ferring B.V. | Analozi oksitocina |
| TWI463990B (zh) | 2009-09-21 | 2014-12-11 | Ferring Bv | 催產素受體促進劑 |
| EP2482835B1 (en) * | 2009-10-01 | 2014-07-02 | The University Of Sydney | Therapy and prevention of problem drinking |
| KR101819804B1 (ko) | 2012-12-21 | 2018-01-17 | 에프. 호프만-라 로슈 아게 | 옥시토신 작용제로서의 펩타이드 |
-
2013
- 2013-12-17 KR KR1020157016376A patent/KR101819804B1/ko not_active Expired - Fee Related
- 2013-12-17 PL PL13814079T patent/PL2935312T3/pl unknown
- 2013-12-17 EA EA201591078A patent/EA026687B1/ru not_active IP Right Cessation
- 2013-12-17 UA UAA201506906A patent/UA119034C2/uk unknown
- 2013-12-17 AU AU2013363768A patent/AU2013363768B2/en not_active Ceased
- 2013-12-17 DK DK13814079.3T patent/DK2935312T3/en active
- 2013-12-17 LT LTEP13814079.3T patent/LT2935312T/lt unknown
- 2013-12-17 HU HUE13814079A patent/HUE039848T2/hu unknown
- 2013-12-17 RS RS20181124A patent/RS57690B1/sr unknown
- 2013-12-17 BR BR112015014010A patent/BR112015014010A2/pt not_active IP Right Cessation
- 2013-12-17 ES ES13814079.3T patent/ES2690317T3/es active Active
- 2013-12-17 HR HRP20181569TT patent/HRP20181569T1/hr unknown
- 2013-12-17 NZ NZ708175A patent/NZ708175A/en not_active IP Right Cessation
- 2013-12-17 MA MA38272A patent/MA38272A1/fr unknown
- 2013-12-17 SI SI201331190T patent/SI2935312T1/sl unknown
- 2013-12-17 CN CN201380066617.7A patent/CN104870466B/zh not_active Expired - Fee Related
- 2013-12-17 PT PT13814079T patent/PT2935312T/pt unknown
- 2013-12-17 JP JP2015548420A patent/JP6067878B2/ja not_active Expired - Fee Related
- 2013-12-17 WO PCT/EP2013/076783 patent/WO2014095773A1/en active Application Filing
- 2013-12-17 MX MX2015007365A patent/MX358684B/es active IP Right Grant
- 2013-12-17 CA CA2895150A patent/CA2895150C/en not_active Expired - Fee Related
- 2013-12-17 MY MYPI2015001585A patent/MY176398A/en unknown
- 2013-12-17 PE PE2015001058A patent/PE20151446A1/es unknown
- 2013-12-17 SG SG11201504883PA patent/SG11201504883PA/en unknown
- 2013-12-17 EP EP13814079.3A patent/EP2935312B1/en not_active Not-in-force
- 2013-12-20 AR ARP130104962A patent/AR094225A1/es unknown
- 2013-12-20 TW TW102147655A patent/TWI558726B/zh not_active IP Right Cessation
-
2015
- 2015-05-21 CR CR20150271A patent/CR20150271A/es unknown
- 2015-05-22 PH PH12015501145A patent/PH12015501145B1/en unknown
- 2015-06-10 ZA ZA2015/04186A patent/ZA201504186B/en unknown
- 2015-06-18 IL IL239519A patent/IL239519A/en active IP Right Grant
- 2015-06-18 CL CL2015001724A patent/CL2015001724A1/es unknown
- 2015-06-18 US US14/743,009 patent/US9868766B2/en active Active
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