ES2571928T3 - Agonistas de receptores de V1a - Google Patents
Agonistas de receptores de V1aInfo
- Publication number
- ES2571928T3 ES2571928T3 ES13729826T ES13729826T ES2571928T3 ES 2571928 T3 ES2571928 T3 ES 2571928T3 ES 13729826 T ES13729826 T ES 13729826T ES 13729826 T ES13729826 T ES 13729826T ES 2571928 T3 ES2571928 T3 ES 2571928T3
- Authority
- ES
- Spain
- Prior art keywords
- alkylene
- alkyl
- unsubstituted
- hydrogen
- substituted
- Prior art date
- Legal status (The legal status 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 status listed.)
- Active
Links
- 239000000018 receptor agonist Substances 0.000 title 1
- 229940044601 receptor agonist Drugs 0.000 title 1
- 125000002947 alkylene group Chemical group 0.000 abstract 26
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 10
- 229910052739 hydrogen Inorganic materials 0.000 abstract 10
- 239000001257 hydrogen Substances 0.000 abstract 10
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 abstract 6
- 125000003107 substituted aryl group Chemical group 0.000 abstract 6
- 125000001072 heteroaryl group Chemical group 0.000 abstract 5
- 125000003118 aryl group Chemical group 0.000 abstract 4
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 4
- 125000005346 substituted cycloalkyl group Chemical group 0.000 abstract 4
- 125000000008 (C1-C10) alkyl group Chemical group 0.000 abstract 2
- 125000000217 alkyl group Chemical group 0.000 abstract 2
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 2
- 125000000027 (C1-C10) alkoxy group Chemical group 0.000 abstract 1
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 abstract 1
- 125000003161 (C1-C6) alkylene group Chemical group 0.000 abstract 1
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 abstract 1
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 abstract 1
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 abstract 1
- 125000003342 alkenyl group Chemical group 0.000 abstract 1
- 125000000304 alkynyl group Chemical group 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 1
- 125000001188 haloalkyl group Chemical group 0.000 abstract 1
- 229910052736 halogen Chemical group 0.000 abstract 1
- 150000002367 halogens Chemical group 0.000 abstract 1
- 150000003839 salts Chemical class 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
- C07K7/02—Linear peptides containing at least one abnormal peptide link
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/12—Drugs for disorders of the urinary system of the kidneys
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
- A61P7/04—Antihaemorrhagics; Procoagulants; Haemostatic agents; Antifibrinolytic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
- A61P7/06—Antianaemics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/02—Non-specific cardiovascular stimulants, e.g. drugs for syncope, antihypotensives
-
- 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
-
- 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
-
- 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
- C07K7/06—Linear peptides containing only normal peptide links having 5 to 11 amino acids
-
- Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
- Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
- Y02P—CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
- Y02P20/00—Technologies relating to chemical industry
- Y02P20/50—Improvements relating to the production of bulk chemicals
- Y02P20/55—Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Molecular Biology (AREA)
- Biophysics (AREA)
- Genetics & Genomics (AREA)
- Biochemistry (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Hematology (AREA)
- Gastroenterology & Hepatology (AREA)
- Diabetes (AREA)
- Urology & Nephrology (AREA)
- Pulmonology (AREA)
- Rheumatology (AREA)
- Pain & Pain Management (AREA)
- Immunology (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Peptides Or Proteins (AREA)
- Plural Heterocyclic Compounds (AREA)
- Polyurethanes Or Polyureas (AREA)
- Polyesters Or Polycarbonates (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Abstract
Compuesto según la fórmula (I): **Fórmula** o una sal del mismo, en la que: R1 se selecciona de alquilo (C1-C10), alcoxilo (C1-C10), alquil (C1-C10)-NH, Ar1-L1- y cicloalquilo no sustituido o sustituido, Ar1-L1- se selecciona de Ar1-, Ar1-CH2-, Ar1-CH2CH2-, Ar1-O-, Ar1-CH2O-, Ar1-NH- y Ar1-CH2NH-; Ar1 es arilo no sustituido o arilo sustituido; R2 se selecciona de hidrógeno, alquilo (C1-C6), hidroxilo, alcoxilo (C1-C6) y halógeno; R3 se selecciona de alquilo (C1-C6), cicloalquilo no sustituido o sustituido y Cy3-CH2-; Cy3- es arilo no sustituido o sustituido o cicloalquilo no sustituido o sustituido; R4 se selecciona de alquilo (C1-C6), alquenilo (C2-C6), alquinilo (C2-C6), haloalquilo (C1-C6), -(alquilen (C1-C6))-OR4a, -(alquilen (C1-C6))-NR4a2, -(alquilen (C1-C6))-S-alquilo (C1-C6), -(alquilen (C1-C6))-C(>=O)OR4a2, -(alquilen (C1-C6))-C(>=O)NR4a2, -(alquilen (C1-C6))-C(>=NR4a)NR4a2, -(alquilen (C1-C6))-OC(>=O)R4a, -(alquilen (C1-C6))-OC(>=O)OR4a, -(alquilen (C1-C6))-OC(>=O)NR4a2, -(alquilen (C1-C6))-NR4aC(>=O)R4a, -(alquilen (C1-C6))-NR4aC(>=O)OR4a, -(alquilen (C1-C6))-NR4aC(>=O)NR4a2, -(alquilen (C1-C6))-NR4aC(>=NR4a)NR4a2, Ar4 y -(alquilen (C1-C6))-Ar4; cada R4a se selecciona independientemente de hidrógeno y alquilo (C1-C6); Ar4 se selecciona de arilo no sustituido o sustituido y heteroarilo no sustituido o sustituido; R5 se selecciona de -(alquilen (C1-C6))-NR5a2 y -(alquilen (C1-C6))-NR5aC(>=NR5a)NR5a2; cada R5a se selecciona independientemente de hidrógeno y alquilo (C1-C6); Q se selecciona de los grupos Q1, Q2, Q3 y Q4: **Fórmula** a y b representan los enlaces que unen Q al resto de la molécula; R6 se selecciona de hidrógeno, alquilo (C1-C6) y -C(>=NR6a)NR6a2; cada R6a es hidrógeno o alquilo (C1-C6); R7 se selecciona de alquilo (C1-C6), arilo no sustituido, arilo sustituido, cicloalquilo no sustituido y cicloalquilo sustituido; R8 se selecciona de NH2 e hidroxilo; R9 se selecciona de hidrógeno, alquilo (C1-C6), alquenilo (C2-C6), alquinilo (C2-C6), haloalquilo (C1-C6), -(alquilen (C1-C6))-OR9a, -(alquilen (C1-C6))-NR9a2, -(alquilen (C1-C6))-SR9a, -(alquilen (C1-C6))-C(>=O)OR9a2, 10 -(alquilen (C1-C6))-C(>=O)NR9a2, -(alquilen (C1-C6))-C(>=NR9a)NR9a2, -(alquilen (C1-C6))-OC(>=O)R9a, -(alquilen (C1-C6))-OC(>=O)OR9a, -(alquilen (C1-C6))-OC(>=O)NR9a2, -(alquilen (C1-C6))-NR9aC(>=O)R9b, -(alquilen (C1-C6))-NR9aC(>=O)OR9a, -(alquilen (C1-C6))-NR9aC(>=O)NR9a2, -(alquilen (C1-C6))-NR9aC(>=NR9a)NR9a2, Ar9 y -(alquilen (C1-C6))-Ar9; cada R9a se selecciona independientemente de hidrógeno y alquilo (C1-C6); cada R9b se selecciona independientemente de hidrógeno y alquilo (C1-C10); Ar9 se selecciona de arilo no sustituido, arilo sustituido, heteroarilo no sustituido o heteroarilo sustituido; R10 se selecciona de -(alquilen (C1-C6))-OR10a, -(alquilen (C1-C6))-C(>=O)NR10a2 y Ar10-CH2-; Ar10 es heteroarilo no sustituido o heteroarilo sustituido; cada R10a se selecciona de hidrógeno y alquilo (C1-C6); Ar se selecciona de arilo o arilo sustituido; cada X es NH y cada Y es C>=O; o cada X es C>=O y cada Y es NH; m es 0, 1, 2, 3, 4 ó 5; n es 0, 1, 2, 3 ó 4; o es 1 ó 2; p es 1, 2 ó 3; y r es 0, 1, 2, 3, 4, 5 ó 6; con la condición de que R9 sea hidrógeno si r es mayor de uno.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201261645558P | 2012-05-10 | 2012-05-10 | |
| PCT/US2013/040414 WO2013170077A2 (en) | 2012-05-10 | 2013-05-09 | V1a receptor agonists |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ES2571928T3 true ES2571928T3 (es) | 2016-05-27 |
Family
ID=48652296
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ES13729826T Active ES2571928T3 (es) | 2012-05-10 | 2013-05-09 | Agonistas de receptores de V1a |
Country Status (28)
| Country | Link |
|---|---|
| US (1) | US9644000B2 (es) |
| EP (1) | EP2847210B1 (es) |
| JP (1) | JP6231554B2 (es) |
| KR (1) | KR102050356B1 (es) |
| CN (1) | CN104350065B (es) |
| AR (1) | AR091013A1 (es) |
| AU (1) | AU2013259393B2 (es) |
| BR (1) | BR112014027996B1 (es) |
| CA (1) | CA2871776C (es) |
| DK (1) | DK2847210T3 (es) |
| ES (1) | ES2571928T3 (es) |
| HR (1) | HRP20160468T1 (es) |
| HU (1) | HUE027519T2 (es) |
| IL (1) | IL235558A (es) |
| JO (1) | JO3109B1 (es) |
| MX (1) | MX353864B (es) |
| MY (1) | MY167248A (es) |
| NZ (1) | NZ701365A (es) |
| PH (1) | PH12014502510A1 (es) |
| PL (1) | PL2847210T3 (es) |
| RS (1) | RS54722B1 (es) |
| RU (1) | RU2634617C2 (es) |
| SA (1) | SA113340536B1 (es) |
| SG (1) | SG11201407400XA (es) |
| SI (1) | SI2847210T1 (es) |
| TW (1) | TWI632161B (es) |
| WO (1) | WO2013170077A2 (es) |
| ZA (1) | ZA201408172B (es) |
Families Citing this family (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US9388214B2 (en) | 2014-11-05 | 2016-07-12 | Ferring B.V. | V1A receptor agonists |
| JP2017014206A (ja) | 2015-06-30 | 2017-01-19 | ナノアンティバイオティクス，インコーポレイテッド | 腹水の治療 |
| AU2017273857B2 (en) | 2016-06-01 | 2021-08-19 | Athira Pharma, Inc. | Compounds |
| CN109010795B (zh) * | 2018-09-12 | 2021-10-22 | 南京康舟医药科技有限公司 | 醋酸特利加压素注射液以及其制备方法 |
| KR20220011697A (ko) | 2019-05-22 | 2022-01-28 | 바이오비에 아이앤씨. | 테를리프레신 제형 |
| EP4182021A4 (en) * | 2020-07-17 | 2024-10-30 | PharmaIN Corporation | V1A RECEPTOR PARTIAL AGONIST AND METHOD OF USE |
| WO2023183339A1 (en) * | 2022-03-22 | 2023-09-28 | Ocelot Bio, Inc. | Selective vasopressin receptor agonist for end-stage liver disease |
| KR20250077588A (ko) * | 2022-09-30 | 2025-05-30 | 훼링 비.브이. | 말기 간 질환 및 이와 관련된 합병증을 치료하기 위한 혼합 바소프레신 수용체 작용제-길항제 |
Family Cites Families (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CZ20021492A3 (cs) * | 1999-11-04 | 2003-06-18 | Ortho-Mcneil Pharmaceutical, Inc. | Nepeptidové substituované benzothiazepiny jako antagonisté vazopresinu |
| EP1188443A1 (en) * | 2000-09-15 | 2002-03-20 | Ferring BV | Improved protocol for paracentesis |
| JO2937B1 (en) * | 2004-08-11 | 2016-03-15 | فيرينغ.بي.في | Tight muscles of the peptide vascular tensioner receptor |
| PL1904477T3 (pl) * | 2005-07-14 | 2009-07-31 | Hoffmann La Roche | Pochodne indolo-3-karbonylo-spiro-piperydyny jako antagoniści receptora V1a |
| KR101018934B1 (ko) * | 2005-09-28 | 2011-03-02 | 에프. 호프만-라 로슈 아게 | 바소프레신 수용체 길항물질로서인돌-3-일-카보닐-아자스피로 유도체 |
| US8222202B2 (en) * | 2006-02-13 | 2012-07-17 | Ferring B.V. | Use of peptidic vasopressin receptor agonists |
| US7960336B2 (en) * | 2007-08-03 | 2011-06-14 | Pharmain Corporation | Composition for long-acting peptide analogs |
-
2013
- 2013-04-24 JO JOP/2013/0118A patent/JO3109B1/ar active
- 2013-04-30 TW TW102115416A patent/TWI632161B/zh active
- 2013-05-08 SA SA113340536A patent/SA113340536B1/ar unknown
- 2013-05-09 NZ NZ701365A patent/NZ701365A/en unknown
- 2013-05-09 AU AU2013259393A patent/AU2013259393B2/en active Active
- 2013-05-09 KR KR1020147034501A patent/KR102050356B1/ko active Active
- 2013-05-09 MX MX2014013646A patent/MX353864B/es active IP Right Grant
- 2013-05-09 JP JP2015511718A patent/JP6231554B2/ja active Active
- 2013-05-09 ES ES13729826T patent/ES2571928T3/es active Active
- 2013-05-09 WO PCT/US2013/040414 patent/WO2013170077A2/en not_active Ceased
- 2013-05-09 BR BR112014027996-9A patent/BR112014027996B1/pt active IP Right Grant
- 2013-05-09 EP EP13729826.1A patent/EP2847210B1/en active Active
- 2013-05-09 SI SI201330175A patent/SI2847210T1/sl unknown
- 2013-05-09 MY MYPI2014703280A patent/MY167248A/en unknown
- 2013-05-09 RU RU2014143941A patent/RU2634617C2/ru active
- 2013-05-09 SG SG11201407400XA patent/SG11201407400XA/en unknown
- 2013-05-09 DK DK13729826.1T patent/DK2847210T3/en active
- 2013-05-09 HU HUE13729826A patent/HUE027519T2/en unknown
- 2013-05-09 CN CN201380024444.2A patent/CN104350065B/zh active Active
- 2013-05-09 PL PL13729826T patent/PL2847210T3/pl unknown
- 2013-05-09 RS RS20160293A patent/RS54722B1/sr unknown
- 2013-05-09 US US14/400,282 patent/US9644000B2/en active Active
- 2013-05-09 CA CA2871776A patent/CA2871776C/en active Active
- 2013-05-09 HR HRP20160468TT patent/HRP20160468T1/hr unknown
- 2013-05-10 AR ARP130101626 patent/AR091013A1/es active IP Right Grant
-
2014
- 2014-11-06 IL IL235558A patent/IL235558A/en active IP Right Grant
- 2014-11-07 ZA ZA2014/08172A patent/ZA201408172B/en unknown
- 2014-11-10 PH PH12014502510A patent/PH12014502510A1/en unknown
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