BRPI0606647A2 - antagonistas do receptor de c5a - Google Patents

antagonistas do receptor de c5a

Info

Publication number
BRPI0606647A2
BRPI0606647A2 BRPI0606647-0A BRPI0606647A BRPI0606647A2 BR PI0606647 A2 BRPI0606647 A2 BR PI0606647A2 BR PI0606647 A BRPI0606647 A BR PI0606647A BR PI0606647 A2 BRPI0606647 A2 BR PI0606647A2
Authority
BR
Brazil
Prior art keywords
bonds
substituted
radical
group
mimics
Prior art date
Application number
BRPI0606647-0A
Other languages
English (en)
Inventor
Gerd Hummel
Dirk Scharn
Elsa Locardi
Thomas Polakowski
Karsten Schnatbaum
Original Assignee
Jerini Ag
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by Jerini Ag filed Critical Jerini Ag
Publication of BRPI0606647A2 publication Critical patent/BRPI0606647A2/pt

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K14/00—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • C07K14/435—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • C07K14/46—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans from vertebrates
    • C07K14/47—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans from vertebrates from mammals
    • C07K14/4701—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans from vertebrates from mammals not used
    • C07K14/472—Complement proteins, e.g. anaphylatoxin, C3a, C5a
    • 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
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • 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
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
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    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
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    • 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
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/14—Drugs for dermatological disorders for baldness or alopecia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P7/06—Antianaemics
    • A—HUMAN NECESSITIES
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    • 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
    • A61P9/08—Vasodilators for multiple indications
    • 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
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K14/00—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • C07K14/435—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • C07K14/46—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans from vertebrates
    • C07K14/47—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans from vertebrates from mammals
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    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K14/00—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • C07K14/435—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • C07K14/705—Receptors; Cell surface antigens; Cell surface determinants
    • 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
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    • C07K—PEPTIDES
    • C07K7/00—Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
    • C07K7/50—Cyclic peptides containing at least one abnormal peptide link
    • C07K7/54—Cyclic peptides containing at least one abnormal peptide link with at least one abnormal peptide link in the ring
    • C07K7/56—Cyclic peptides containing at least one abnormal peptide link with at least one abnormal peptide link in the ring the cyclisation not occurring through 2,4-diamino-butanoic acid
    • 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

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  • Proteomics, Peptides & Aminoacids (AREA)
  • Immunology (AREA)
  • Diabetes (AREA)
  • Gastroenterology & Hepatology (AREA)
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  • Toxicology (AREA)
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Abstract

ANTAGONISTAS DO RECEPTOR DE C5a. A presente invenção refere-se a um composto, de preferência um antagonista de receptor de C5a, tendo a seguinte estrutura: segundo a qual X1 é um radical tendo uma massa de cerca de 1 a 300, segundo a qual X1 é de preferência selecionado do grupo que compreende R5-, R5-CO-, R5-N(R6)-CO-, R5-O-CO-, R5-SO2 22-, R5-N(R6)-SO2 22-, R5-N(R6)-, R5-N(R6)-CS-, R5-N(R6)-C(NH)-, R5-CS-, R5-P(O)OH-5, R5-B(OH)-, e R5-CH=N-O-CH2 22-CO-, segundo o que R5 e R6 são individualmente e independentemente selecionados do grupo que compreende H, F, hidróxi, alquila, alquila substituida, cicloalquila, cicloalquila substituida, heterociclila, heterociclila substituida, arilalquila, arilalquila substituida, arila, arila substituida, heteroarila, heteroarila substituida, acila, acila substituida, alcóxi, alcoxialquila, alcoxialquila substituida, ariloxialquila e ariloxialquila substituida, X2 é um radical que imita as características de ligação biológica de uma unidade de fenilalanina, X3 e X4 são individualmente e independentemente um espaçador, segundo o que o espaçador é de preferência selecionado do grupo que compreende aminoácidos, análogos de aminoácidos e derivados de aminoácidos, X5 é um radical que imita as características de ligação biológica de uma unidade de cicloexilalanina ou homoleucina, X6 é um radical que imita as características de ligação biológica de uma unidade de triptofano, X7 é um radical que imita as características de ligação biológica de uma unidade de norleucina ou fenilalanina, uma ligação química entre X3 e X7 é formada, e as linhas de conexão - na fórmula (1) indicam ligações químicas, segundo o que a ligação química é individualmente e independentemente selecionada do grupo que compreende ligações covalentes, ligações iónicas e ligações coordenativas, segundo o que de preferência a ligação é uma ligação química e mais preferivelmente a ligação química é uma ligação selecionada do grupo que compreende ligações de amida, ligações de dissulfeto, ligações de éter, ligações de tioéter, ligações de oxima e ligações de aminotriazina, segundo o que o composto é em particular útil para a fabricação de um medicamento para o tratamento de doenças auto-imunes.
BRPI0606647-0A 2005-01-17 2006-01-17 antagonistas do receptor de c5a BRPI0606647A2 (pt)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP05000857 2005-01-17
PCT/EP2006/000365 WO2006074964A1 (en) 2005-01-17 2006-01-17 C5a receptor antagonists

Publications (1)

Publication Number Publication Date
BRPI0606647A2 true BRPI0606647A2 (pt) 2009-07-14

Family

ID=36013361

Family Applications (1)

Application Number Title Priority Date Filing Date
BRPI0606647-0A BRPI0606647A2 (pt) 2005-01-17 2006-01-17 antagonistas do receptor de c5a

Country Status (14)

Country Link
US (1) US20080161232A1 (pt)
EP (1) EP1838725A1 (pt)
JP (1) JP2008526915A (pt)
KR (1) KR20070104355A (pt)
CN (1) CN101107264A (pt)
AU (1) AU2006205830A1 (pt)
BR (1) BRPI0606647A2 (pt)
CA (1) CA2594934A1 (pt)
IL (1) IL184278A0 (pt)
MX (1) MX2007008640A (pt)
RU (1) RU2007131267A (pt)
SG (1) SG158191A1 (pt)
WO (1) WO2006074964A1 (pt)
ZA (1) ZA200705237B (pt)

Families Citing this family (16)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2011195451A (ja) * 2008-06-20 2011-10-06 Fukuoka Univ ペプチド
US8425662B2 (en) 2010-04-02 2013-04-23 Battelle Memorial Institute Methods for associating or dissociating guest materials with a metal organic framework, systems for associating or dissociating guest materials within a series of metal organic frameworks, and gas separation assemblies
CA2811250C (en) 2011-10-21 2015-08-11 Abbvie Inc. Methods for treating hcv
GB2506086A (en) 2011-10-21 2014-03-19 Abbvie Inc Methods for treating HCV comprising at least two direct acting antiviral agent, ribavirin but not interferon
US8492386B2 (en) 2011-10-21 2013-07-23 Abbvie Inc. Methods for treating HCV
US8466159B2 (en) 2011-10-21 2013-06-18 Abbvie Inc. Methods for treating HCV
US9518265B2 (en) * 2012-01-10 2016-12-13 Noxxon Pharma Ag C5a binding nucleic acids
JP6754997B2 (ja) * 2013-08-26 2020-09-16 国立大学法人 東京大学 大環状ペプチド、その製造方法、及び大環状ペプチドライブラリを用いるスクリーニング方法
JO3669B1 (ar) * 2015-01-06 2020-08-27 Ferring Bv بيبتيدات مضَادَّة لببتيد المرتبط بجين الكالسيتونين
DK3368544T3 (da) 2015-10-27 2020-08-24 Hoffmann La Roche Peptidmakrocykler mod Acinetobacter baumannii
US11192914B2 (en) 2016-04-28 2021-12-07 Emory University Alkyne containing nucleotide and nucleoside therapeutic compositions and uses related thereto
AU2017304103A1 (en) * 2016-07-29 2019-01-17 Pfizer Inc. Cyclic peptides as C5 a receptor antagonists
EP3388444A1 (en) 2017-04-10 2018-10-17 F. Hoffmann-La Roche AG Anti-bacterial peptide macrocycles and use thereof
US11505573B2 (en) 2018-03-28 2022-11-22 Hoffmann-La Roche Inc. Peptide macrocycles against Acinetobacter baumannii
US11819532B2 (en) 2018-04-23 2023-11-21 Hoffmann-La Roche Inc. Peptide macrocycles against Acinetobacter baumannii
US11918624B2 (en) 2020-06-10 2024-03-05 Kelsius Laboratories LLC Therapeutic composition for use in the treatment of COVID-19 and other cytokine storm associated disorders

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2045578A1 (en) * 1989-01-31 1990-08-01 Megumi Kawai Anaphylatoxin-receptor ligands
US5190922A (en) * 1991-06-04 1993-03-02 Abbott Laboratories Terminally modified tri-, tetra- and pentapeptide anaphylatoxin receptor ligands
AUPO755097A0 (en) * 1997-06-25 1997-07-17 University Of Queensland, The Receptor agonist and antagonist
AUPR833401A0 (en) * 2001-10-17 2001-11-08 University Of Queensland, The G protein-coupled receptor antagonists
EP1498422A1 (de) * 2003-07-17 2005-01-19 Jerini AG C5a-Rezeptor-Antagonisten

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Publication number Publication date
WO2006074964A1 (en) 2006-07-20
CA2594934A1 (en) 2006-07-20
AU2006205830A1 (en) 2006-07-20
RU2007131267A (ru) 2009-02-27
KR20070104355A (ko) 2007-10-25
JP2008526915A (ja) 2008-07-24
CN101107264A (zh) 2008-01-16
ZA200705237B (en) 2009-06-24
EP1838725A1 (en) 2007-10-03
SG158191A1 (en) 2010-01-29
US20080161232A1 (en) 2008-07-03
MX2007008640A (es) 2007-09-12
IL184278A0 (en) 2007-10-31

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