ES2571928T3 - Agonistas de receptores de V1a - Google Patents

Agonistas de receptores de V1a

Info

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
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ES
Spain
Prior art keywords
alkylene
alkyl
unsubstituted
hydrogen
substituted
Prior art date
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Active
Application number
ES13729826T
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English (en)
Inventor
Kazimierz Wisniewski
Geoffrey S Harris
Robert Felix Galyean
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Ferring BV
Original Assignee
Ferring BV
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Publication date
Application filed by Ferring BV filed Critical Ferring BV
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Publication of ES2571928T3 publication Critical patent/ES2571928T3/es
Active legal-status Critical Current
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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)
  • Diabetes (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Pulmonology (AREA)
  • Urology & Nephrology (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)

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.
ES13729826T 2012-05-10 2013-05-09 Agonistas de receptores de V1a Active ES2571928T3 (es)

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 (29)

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)
HK (1) HK1205706A1 (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 (7)

* Cited by examiner, † Cited by third party
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
CA3026074A1 (en) 2016-06-01 2017-12-07 M3 Biotechnology, Inc. N-hexanoic-l-tyrosine-l-isoleucine-(6)-aminohexanoic amide compounds and their use to treat neurodegenerative diseases
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
KR20230041029A (ko) * 2020-07-17 2023-03-23 파마인 코포레이션 V1a 수용체 부분 효능제 및 이용 방법
WO2023183339A1 (en) * 2022-03-22 2023-09-28 Ocelot Bio, Inc. Selective vasopressin receptor agonist for end-stage liver disease
WO2024073451A1 (en) * 2022-09-30 2024-04-04 Ocelot Bio, Inc. Mixed vasopressin receptor agonist-antagonist for treating end-stage liver disease and complications associated thereof

Family Cites Families (7)

* Cited by examiner, † Cited by third party
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
DE602006004997D1 (de) * 2005-07-14 2009-03-12 Hoffmann La Roche Indol-3-carbonyl-spiro-piperidinderivate als antagonisten des v1a-rezeptors
WO2007039438A1 (en) * 2005-09-28 2007-04-12 F. Hoffmann-La Roche Ag Indol-3-yl-carbonyl-azaspiro derivatives as vasopressin receptor antagonists
HUE027174T2 (en) * 2006-02-13 2016-10-28 Ferring Bv Use of peptide agonists of the vasopressin receptor
US7960336B2 (en) * 2007-08-03 2011-06-14 Pharmain Corporation Composition for long-acting peptide analogs

Also Published As

Publication number Publication date
DK2847210T3 (en) 2016-05-02
JP6231554B2 (ja) 2017-11-15
TW201348262A (zh) 2013-12-01
BR112014027996B1 (pt) 2021-07-27
HK1205706A1 (zh) 2015-12-24
SA113340536B1 (ar) 2015-10-08
WO2013170077A2 (en) 2013-11-14
BR112014027996A2 (pt) 2017-07-25
IL235558A0 (en) 2015-01-29
KR20150008175A (ko) 2015-01-21
JP2015518820A (ja) 2015-07-06
HUE027519T2 (en) 2016-10-28
WO2013170077A3 (en) 2014-03-27
IL235558A (en) 2017-07-31
SI2847210T1 (sl) 2016-06-30
AU2013259393A1 (en) 2014-11-20
EP2847210A2 (en) 2015-03-18
CA2871776A1 (en) 2013-11-14
RS54722B1 (en) 2016-08-31
PH12014502510B1 (en) 2014-12-22
HRP20160468T1 (hr) 2016-06-03
RU2014143941A (ru) 2016-07-10
PH12014502510A1 (en) 2014-12-22
MX353864B (es) 2018-02-01
CN104350065B (zh) 2020-04-28
CN104350065A (zh) 2015-02-11
SG11201407400XA (en) 2014-12-30
ZA201408172B (en) 2015-12-23
NZ701365A (en) 2016-05-27
KR102050356B1 (ko) 2019-11-29
US20150126432A1 (en) 2015-05-07
CA2871776C (en) 2021-09-07
US9644000B2 (en) 2017-05-09
MX2014013646A (es) 2015-03-03
AU2013259393B2 (en) 2017-02-02
AR091013A1 (es) 2014-12-30
EP2847210B1 (en) 2016-02-17
JO3109B1 (ar) 2017-09-20
MY167248A (en) 2018-08-14
PL2847210T3 (pl) 2016-08-31
RU2634617C2 (ru) 2017-11-02
TWI632161B (zh) 2018-08-11

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