AR094225A1 - Peptidos como agonistas de oxitocina - Google Patents
Peptidos como agonistas de oxitocinaInfo
- Publication number
- AR094225A1 AR094225A1 ARP130104962A ARP130104962A AR094225A1 AR 094225 A1 AR094225 A1 AR 094225A1 AR P130104962 A ARP130104962 A AR P130104962A AR P130104962 A ARP130104962 A AR P130104962A AR 094225 A1 AR094225 A1 AR 094225A1
- Authority
- AR
- Argentina
- Prior art keywords
- lower alkyl
- hydroxy
- hydrogen
- cycloalkyl
- amino
- Prior art date
Links
- 239000000556 agonist Substances 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
- 229910052739 hydrogen Inorganic materials 0.000 abstract 5
- 239000001257 hydrogen Substances 0.000 abstract 5
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 5
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 3
- 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 -CH2-cycloalkyl Chemical group 0.000 abstract 1
- HBAQYPYDRFILMT-UHFFFAOYSA-N 8-[3-(1-cyclopropylpyrazol-4-yl)-1H-pyrazolo[4,3-d]pyrimidin-5-yl]-3-methyl-3,8-diazabicyclo[3.2.1]octan-2-one Chemical class C1(CC1)N1N=CC(=C1)C1=NNC2=C1N=C(N=C2)N1C2C(N(CC1CC2)C)=O HBAQYPYDRFILMT-UHFFFAOYSA-N 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
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 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
- 201000010769 Prader-Willi syndrome Diseases 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
- 229910052736 halogen Chemical group 0.000 abstract 1
- 150000002367 halogens Chemical group 0.000 abstract 1
- 150000002431 hydrogen 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
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)
- 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
Se refiere a compuestos de la fórmula (1) 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 heterocíclico aromático de cinco eslabones; R⁴ es hidrógeno o alquilo inferior; R⁵ es hidrógeno o alquilo inferior; o R⁴ y R⁵ junto con los átomos de N y C a los que están unidos pueden formar un anillo de pirrolidina, opcionalmente sustituido por hidroxi o halógeno, un anillo de piperidina o un anillo de azetidina; R⁶ es hidrógeno, alquilo inferior, alquilo inferior sustituido por hidroxi, -(CH₂)₂C(O)OH, -(CH₂)₂C(O)NH₂, bencilo opcionalmente sustituido por amino o hidroxi, -CH₂-grupo heterocíclico aromático de cinco eslabones, indolilo, -CH₂-cicloalquilo, cicloalquilo, -(CH₂)₂-S-alquilo inferior o es -(CH₂)₁₋₄-NH₂; R⁶ es hidrógeno o alquilo inferior; o R⁶ y R⁶ juntos son cicloalquilo; X es C(O)-CHR-NR-C(O)-; R / R con independencia entre sí son hidrógeno o alquilo inferior; m es el número 2; o es el número 0 ó 1; o a una sal de adición de ácido farmacéuticamente aceptable, a una mezcla racémica o a sus enantiómeros correspondientes y/o isómeros ópticos de los mismos. Ahora se ha encontrado que los compuestos presentes son agonistas de receptores de oxitocina para el tratamiento del autismo, el estrés, incluido el trastorno del estrés postraumático, la ansiedad, incluidos los trastornos de ansiedad y la depresión, la esquizofrenia, los trastornos psiquiátricos y la pérdida de memoria, la abstinencia del alcohol, la adicción a las drogas y para el tratamiento del síndrome de Prader-Willi.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP12199012 | 2012-12-21 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR094225A1 true AR094225A1 (es) | 2015-07-22 |
Family
ID=47471593
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP130104962A AR094225A1 (es) | 2012-12-21 | 2013-12-20 | 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)
| 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 |
| KR102168621B1 (ko) | 2012-12-21 | 2020-10-22 | 얀센 바이오파마, 인코퍼레이트. | 치환된 뉴클레오사이드, 뉴클레오타이드 및 그것의 유사체 |
| CA2895150C (en) | 2012-12-21 | 2019-11-26 | F. Hoffmann-La Roche Ag | Peptides as oxytocin agonists |
| UA111305C2 (uk) | 2012-12-21 | 2016-04-11 | Пфайзер Інк. | Конденсовані лактами арилу та гетероарилу |
| KR102116107B1 (ko) | 2013-12-30 | 2020-05-28 | 삼성디스플레이 주식회사 | 표시 장치 |
| USRE49816E1 (en) | 2014-01-10 | 2024-01-30 | Cornell University | Dipeptides as inhibitors of human immunoproteasomes |
| EA030091B1 (ru) | 2014-06-03 | 2018-06-29 | Ф. Хоффманн-Ля Рош Аг | Пептиды, выполняющие роль агонистов окситоцина |
| WO2015193765A1 (en) | 2014-06-17 | 2015-12-23 | Pfizer Inc. | Substituted dihydroisoquinolinone compounds |
| US10588980B2 (en) | 2014-06-23 | 2020-03-17 | Novartis Ag | Fatty acids and their use in conjugation to biomolecules |
| PL3177635T3 (pl) * | 2014-08-07 | 2019-02-28 | F. Hoffmann-La Roche Ag | Sposoby wytwarzania analogów oksytocyny |
| US11202817B2 (en) | 2014-08-18 | 2021-12-21 | Cornell University | Dipeptidomimetics as inhibitors of human immunoproteasomes |
| WO2016044131A1 (en) * | 2014-09-19 | 2016-03-24 | Ferring B.V. | Method of treating prader-willi syndrome |
| EP3362754B1 (en) | 2015-10-15 | 2021-12-22 | Cornell University | Proteasome inhibitors and uses thereof |
| WO2019075252A1 (en) | 2017-10-11 | 2019-04-18 | Cornell University | PEPTIDOMIMETIC INHIBITORS OF PROTEASOME |
| AU2019345313A1 (en) | 2018-09-20 | 2021-03-18 | Levo Therapeutics, Inc. | Carbetocin drug product and process for preparing same |
| AU2019345166B2 (en) | 2018-09-20 | 2021-09-02 | Levo Therapeutics, Inc. | Stable intranasal formulations of carbetocin |
| 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 |
|---|---|---|---|---|
| NZ587817A (en) | 2008-03-31 | 2012-05-25 | Ferring Bv | Oxytocin analogues |
| TWI463990B (zh) * | 2009-09-21 | 2014-12-11 | Ferring Bv | 催產素受體促進劑 |
| WO2011038451A1 (en) * | 2009-10-01 | 2011-04-07 | The University Of Sydney | Therapy and prevention of problem drinking |
| CA2895150C (en) | 2012-12-21 | 2019-11-26 | F. Hoffmann-La Roche Ag | Peptides as oxytocin agonists |
-
2013
- 2013-12-17 CA CA2895150A patent/CA2895150C/en not_active Expired - Fee Related
- 2013-12-17 HU HUE13814079A patent/HUE039848T2/hu unknown
- 2013-12-17 UA UAA201506906A patent/UA119034C2/uk unknown
- 2013-12-17 ES ES13814079.3T patent/ES2690317T3/es active Active
- 2013-12-17 WO PCT/EP2013/076783 patent/WO2014095773A1/en active Application Filing
- 2013-12-17 PE PE2015001058A patent/PE20151446A1/es unknown
- 2013-12-17 JP JP2015548420A patent/JP6067878B2/ja not_active Expired - Fee Related
- 2013-12-17 AU AU2013363768A patent/AU2013363768B2/en not_active Ceased
- 2013-12-17 BR BR112015014010A patent/BR112015014010A2/pt not_active IP Right Cessation
- 2013-12-17 EA EA201591078A patent/EA026687B1/ru not_active IP Right Cessation
- 2013-12-17 EP EP13814079.3A patent/EP2935312B1/en active Active
- 2013-12-17 RS RS20181124A patent/RS57690B1/sr unknown
- 2013-12-17 MY MYPI2015001585A patent/MY176398A/en unknown
- 2013-12-17 DK DK13814079.3T patent/DK2935312T3/en active
- 2013-12-17 PT PT13814079T patent/PT2935312T/pt unknown
- 2013-12-17 LT LTEP13814079.3T patent/LT2935312T/lt unknown
- 2013-12-17 SI SI201331190T patent/SI2935312T1/sl unknown
- 2013-12-17 KR KR1020157016376A patent/KR101819804B1/ko active IP Right Grant
- 2013-12-17 MX MX2015007365A patent/MX358684B/es active IP Right Grant
- 2013-12-17 PL PL13814079T patent/PL2935312T3/pl unknown
- 2013-12-17 SG SG11201504883PA patent/SG11201504883PA/en unknown
- 2013-12-17 NZ NZ708175A patent/NZ708175A/en not_active IP Right Cessation
- 2013-12-17 CN CN201380066617.7A patent/CN104870466B/zh not_active Expired - Fee Related
- 2013-12-17 MA MA38272A patent/MA38272A1/fr unknown
- 2013-12-20 TW TW102147655A patent/TWI558726B/zh not_active IP Right Cessation
- 2013-12-20 AR ARP130104962A patent/AR094225A1/es unknown
-
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 US US14/743,009 patent/US9868766B2/en active Active
- 2015-06-18 CL CL2015001724A patent/CL2015001724A1/es unknown
- 2015-09-18 HK HK15109189.5A patent/HK1208477A1/xx not_active IP Right Cessation
-
2018
- 2018-10-02 HR HRP20181569TT patent/HRP20181569T1/hr unknown
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FB | Suspension of granting procedure |