ME02218B - Jedinjenja piruvamida kao inhibitori peptidaza alergena grinja grupe 1 - Google Patents
Jedinjenja piruvamida kao inhibitori peptidaza alergena grinja grupe 1Info
- Publication number
- ME02218B ME02218B MEP-2015-115A MEP11515A ME02218B ME 02218 B ME02218 B ME 02218B ME P11515 A MEP11515 A ME P11515A ME 02218 B ME02218 B ME 02218B
- Authority
- ME
- Montenegro
- Prior art keywords
- asthma
- piperizino
- compound according
- 4alkyl
- independently
- Prior art date
Links
- 239000013566 allergen Substances 0.000 title claims 8
- 102000035195 Peptidases Human genes 0.000 title claims 6
- 108091005804 Peptidases Proteins 0.000 title claims 6
- 235000019833 protease Nutrition 0.000 title claims 6
- 239000000428 dust Substances 0.000 title claims 3
- 239000003112 inhibitor Substances 0.000 title 1
- FPOLWERNILTNDK-UHFFFAOYSA-N pyruvamide Chemical class CC(=O)C(N)=O FPOLWERNILTNDK-UHFFFAOYSA-N 0.000 title 1
- 208000006673 asthma Diseases 0.000 claims 38
- 150000001875 compounds Chemical class 0.000 claims 32
- 125000001424 substituent group Chemical group 0.000 claims 22
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 16
- -1 pyrrolidino, piperidino, morpholino Chemical group 0.000 claims 11
- 208000015181 infectious disease Diseases 0.000 claims 10
- 230000002458 infectious effect Effects 0.000 claims 10
- 230000001404 mediated effect Effects 0.000 claims 6
- 206010039083 rhinitis Diseases 0.000 claims 6
- 125000000876 trifluoromethoxy group Chemical group FC(F)(F)O* 0.000 claims 6
- 238000000034 method Methods 0.000 claims 5
- 241000238876 Acari Species 0.000 claims 4
- 208000036065 Airway Remodeling Diseases 0.000 claims 4
- 206010027654 Allergic conditions Diseases 0.000 claims 4
- 206010003645 Atopy Diseases 0.000 claims 4
- 206010066091 Bronchial Hyperreactivity Diseases 0.000 claims 4
- 101100493048 Drosophila melanogaster nrv2 gene Proteins 0.000 claims 4
- 230000000895 acaricidal effect Effects 0.000 claims 4
- 239000000642 acaricide Substances 0.000 claims 4
- 125000001931 aliphatic group Chemical group 0.000 claims 4
- 201000009961 allergic asthma Diseases 0.000 claims 4
- 125000006272 (C3-C7) cycloalkyl group Chemical group 0.000 claims 3
- 125000001313 C5-C10 heteroaryl group Chemical group 0.000 claims 3
- 125000003118 aryl group Chemical group 0.000 claims 3
- 239000003814 drug Substances 0.000 claims 3
- 125000001624 naphthyl group Chemical group 0.000 claims 3
- 208000035143 Bacterial infection Diseases 0.000 claims 2
- 206010006458 Bronchitis chronic Diseases 0.000 claims 2
- 241000282465 Canis Species 0.000 claims 2
- 208000006545 Chronic Obstructive Pulmonary Disease Diseases 0.000 claims 2
- 206010010741 Conjunctivitis Diseases 0.000 claims 2
- 206010010744 Conjunctivitis allergic Diseases 0.000 claims 2
- 206010012438 Dermatitis atopic Diseases 0.000 claims 2
- 206010014561 Emphysema Diseases 0.000 claims 2
- 206010017533 Fungal infection Diseases 0.000 claims 2
- 208000019693 Lung disease Diseases 0.000 claims 2
- 208000031888 Mycoses Diseases 0.000 claims 2
- 208000010362 Protozoan Infections Diseases 0.000 claims 2
- 206010062106 Respiratory tract infection viral Diseases 0.000 claims 2
- 206010039085 Rhinitis allergic Diseases 0.000 claims 2
- 206010039094 Rhinitis perennial Diseases 0.000 claims 2
- 208000036142 Viral infection Diseases 0.000 claims 2
- 208000002205 allergic conjunctivitis Diseases 0.000 claims 2
- 230000000172 allergic effect Effects 0.000 claims 2
- 201000010105 allergic rhinitis Diseases 0.000 claims 2
- 208000024998 atopic conjunctivitis Diseases 0.000 claims 2
- 201000008937 atopic dermatitis Diseases 0.000 claims 2
- 208000010668 atopic eczema Diseases 0.000 claims 2
- 208000022362 bacterial infectious disease Diseases 0.000 claims 2
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims 2
- 206010006451 bronchitis Diseases 0.000 claims 2
- 239000003795 chemical substances by application Substances 0.000 claims 2
- 208000007451 chronic bronchitis Diseases 0.000 claims 2
- 239000003937 drug carrier Substances 0.000 claims 2
- 125000000623 heterocyclic group Chemical group 0.000 claims 2
- 150000004677 hydrates Chemical class 0.000 claims 2
- 238000000338 in vitro Methods 0.000 claims 2
- 208000030603 inherited susceptibility to asthma Diseases 0.000 claims 2
- 230000002401 inhibitory effect Effects 0.000 claims 2
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 2
- 238000004519 manufacturing process Methods 0.000 claims 2
- 230000002085 persistent effect Effects 0.000 claims 2
- 239000000546 pharmaceutical excipient Substances 0.000 claims 2
- 208000023504 respiratory system disease Diseases 0.000 claims 2
- 150000003839 salts Chemical class 0.000 claims 2
- 229920006395 saturated elastomer Polymers 0.000 claims 2
- 239000012453 solvate Substances 0.000 claims 2
- 239000002904 solvent Substances 0.000 claims 2
- 229940124597 therapeutic agent Drugs 0.000 claims 2
- 230000001960 triggered effect Effects 0.000 claims 2
- 230000009385 viral infection Effects 0.000 claims 2
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims 1
- 125000006713 (C5-C10) cycloalkyl group Chemical group 0.000 claims 1
- IMROMDMJAWUWLK-UHFFFAOYSA-N Ethenol Chemical compound OC=C IMROMDMJAWUWLK-UHFFFAOYSA-N 0.000 claims 1
- 241001465754 Metazoa Species 0.000 claims 1
- 150000001555 benzenes Chemical group 0.000 claims 1
- 125000003785 benzimidazolyl group Chemical group N1=C(NC2=C1C=CC=C2)* 0.000 claims 1
- 125000001164 benzothiazolyl group Chemical group S1C(=NC2=C1C=CC=C2)* 0.000 claims 1
- 125000002837 carbocyclic group Chemical group 0.000 claims 1
- 229910052799 carbon Inorganic materials 0.000 claims 1
- 125000004432 carbon atom Chemical group C* 0.000 claims 1
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 1
- 125000003453 indazolyl group Chemical group N1N=C(C2=C1C=CC=C2)* 0.000 claims 1
- 125000002183 isoquinolinyl group Chemical group C1(=NC=CC2=CC=CC=C12)* 0.000 claims 1
- 150000003951 lactams Chemical group 0.000 claims 1
- 125000004573 morpholin-4-yl group Chemical group N1(CCOCC1)* 0.000 claims 1
- 229910052757 nitrogen Inorganic materials 0.000 claims 1
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 1
- 125000000587 piperidin-1-yl group Chemical group [H]C1([H])N(*)C([H])([H])C([H])([H])C([H])([H])C1([H])[H] 0.000 claims 1
- 125000004076 pyridyl group Chemical group 0.000 claims 1
- 125000002112 pyrrolidino group Chemical group [*]N1C([H])([H])C([H])([H])C([H])([H])C1([H])[H] 0.000 claims 1
- 125000002943 quinolinyl group Chemical group N1=C(C=CC2=CC=CC=C12)* 0.000 claims 1
- 125000006413 ring segment Chemical group 0.000 claims 1
- 238000002560 therapeutic procedure Methods 0.000 claims 1
- 125000000391 vinyl group Chemical group [H]C([*])=C([H])[H] 0.000 claims 1
Classifications
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- C07K5/0202—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link containing the structure -NH-X-X-C(=0)-, X being an optionally substituted carbon atom or a heteroatom, e.g. beta-amino acids
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- C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
- C07K5/08—Tripeptides
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- C07K5/0802—Tripeptides with the first amino acid being neutral
- C07K5/0812—Tripeptides with the first amino acid being neutral and aromatic or cycloaliphatic
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- C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
- C07K5/06—Dipeptides
- C07K5/06008—Dipeptides with the first amino acid being neutral
- C07K5/06078—Dipeptides with the first amino acid being neutral and aromatic or cycloaliphatic
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
- C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
- C07K5/06—Dipeptides
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- C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
- C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
- C07K5/06—Dipeptides
- C07K5/06191—Dipeptides containing heteroatoms different from O, S, or N
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
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- C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
- C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
- C07K5/08—Tripeptides
- C07K5/0802—Tripeptides with the first amino acid being neutral
- C07K5/0804—Tripeptides with the first amino acid being neutral and aliphatic
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
- C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
- C07K5/08—Tripeptides
- C07K5/0802—Tripeptides with the first amino acid being neutral
- C07K5/0804—Tripeptides with the first amino acid being neutral and aliphatic
- C07K5/0806—Tripeptides with the first amino acid being neutral and aliphatic the side chain containing 0 or 1 carbon atoms, i.e. Gly, Ala
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
- C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
- C07K5/08—Tripeptides
- C07K5/0802—Tripeptides with the first amino acid being neutral
- C07K5/0804—Tripeptides with the first amino acid being neutral and aliphatic
- C07K5/0808—Tripeptides with the first amino acid being neutral and aliphatic the side chain containing 2 to 4 carbon atoms, e.g. Val, Ile, Leu
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- C—CHEMISTRY; METALLURGY
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- C07K—PEPTIDES
- C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
- C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
- C07K5/08—Tripeptides
- C07K5/0821—Tripeptides with the first amino acid being heterocyclic, e.g. His, Pro, Trp
-
- C—CHEMISTRY; METALLURGY
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- C07K—PEPTIDES
- C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
- C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
- C07K5/08—Tripeptides
- C07K5/0827—Tripeptides containing heteroatoms different from O, S, or N
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
- C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
- C07K5/10—Tetrapeptides
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
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- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
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| GBGB1001070.0A GB201001070D0 (en) | 2010-01-22 | 2010-01-22 | Theraputic compounds and their use |
| EP20110701854 EP2526116B1 (en) | 2010-01-22 | 2011-01-21 | Pyruvamide compounds as inhibitors of dust mite group 1 peptidase allergen |
| PCT/GB2011/000097 WO2011092461A2 (en) | 2010-01-26 | 2011-01-26 | Elapsed time indicator |
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| ME02218B true ME02218B (me) | 2016-02-20 |
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| MEP-2015-115A ME02218B (me) | 2010-01-22 | 2011-01-21 | Jedinjenja piruvamida kao inhibitori peptidaza alergena grinja grupe 1 |
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| EP (1) | EP2526116B1 (OSRAM) |
| JP (1) | JP5859980B2 (OSRAM) |
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| GB201001070D0 (en) | 2010-01-22 | 2010-03-10 | St George's Hospital Medical School | Theraputic compounds and their use |
| RU2015117578A (ru) * | 2012-10-11 | 2016-11-27 | Ф. Хоффманн-Ля Рош Аг | Кетоамидные ингибиторы иммунопротеасом |
| CN103724334A (zh) * | 2013-10-02 | 2014-04-16 | 张惠琳 | 新的抗变态反应的苯并环庚并噻吩类化合物 |
| WO2015106240A1 (en) | 2014-01-13 | 2015-07-16 | The General Hospital Corporation | Heteroaryl disulfide compounds as allosteric effectors for increasing the oxygen-binding affinity of hemoglobin |
| US20160331783A1 (en) * | 2014-01-13 | 2016-11-17 | The General Hospital Corporation | Bisamide compounds as allosteric effectors for reducing the oxygen-binding affinity of hemoglobin |
| GB201908511D0 (en) | 2019-06-13 | 2019-07-31 | Adorx Therapeutics Ltd | Hydroxamate compounds |
| US20240317801A1 (en) * | 2020-12-17 | 2024-09-26 | Disc Medicine, Inc. | Peptidomimetic matriptase 2 inhibitors and uses thereof |
| WO2023165334A1 (zh) * | 2022-03-01 | 2023-09-07 | 成都威斯克生物医药有限公司 | 酮酰胺类衍生物及其制药用途 |
| WO2024028417A1 (en) | 2022-08-03 | 2024-02-08 | Institut National de la Santé et de la Recherche Médicale | New composition for the treatment and/or prevention of vitiligo |
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| US3149159A (en) | 1962-04-16 | 1964-09-15 | Smith Kline French Lab | Substituted 7-aminoalkylbicyclo-[4. 2. 0] octa-1, 3, 5-trienes |
| EP0100673A2 (en) | 1982-08-02 | 1984-02-15 | The Research Foundation Of State University Of New York | A method of enhancing neurofiber regrowth |
| US5066785A (en) | 1988-11-15 | 1991-11-19 | City Of Hope | Carboxyl terminal peptide and protein sequencing |
| WO1990012805A1 (fr) | 1989-04-15 | 1990-11-01 | Zaidan Hojin Biseibutsu Kagaku Kenkyu Kai | Postostatine et son compose connexe, ou leurs sels |
| US6235929B1 (en) * | 1991-12-27 | 2001-05-22 | Georgia Tech Research Corporation | Tripeptide α-ketoamides |
| DE4331135A1 (de) | 1993-09-14 | 1995-03-16 | Bayer Ag | Neue antiviral wirksame valinhaltige Pseudopeptide |
| US5580854A (en) | 1994-03-04 | 1996-12-03 | Mount Sinai School Of Medicine Of The City University Of New York | Substrate-related peptidyl-aldehyde inhibitors of the proteolytic activity of the multicatalytic proteinase complex |
| JPH08208462A (ja) * | 1994-11-24 | 1996-08-13 | Takeda Chem Ind Ltd | カテプシンl阻害剤 |
| AU3935895A (en) | 1994-11-24 | 1996-06-17 | Takeda Chemical Industries Ltd. | Alpha-ketoamide derivatives as cathepsin l inhibitor |
| EP0820464A2 (en) | 1995-03-31 | 1998-01-28 | Takeda Chemical Industries, Ltd. | Cysteine protease inhibitor |
| AU716716B2 (en) | 1995-07-17 | 2000-03-02 | Medivir Uk Ltd | Cysteine protease inhibitors for use in treatment of IgE mediated allergic diseases |
| AU728373B2 (en) | 1995-12-07 | 2001-01-11 | Scripps Research Institute, The | HIV protease inhibitors |
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| CA2225325A1 (en) | 1997-12-19 | 1999-06-19 | The University Of British Columbia | Hemiasterlin analogs |
| TR200103406T2 (tr) | 1998-03-19 | 2002-06-21 | Vertex Pharmaceuticals Incorporated | Kaspaz inhibitörleri. |
| US7521068B2 (en) | 1998-11-12 | 2009-04-21 | Elan Pharma International Ltd. | Dry powder aerosols of nanoparticulate drugs |
| WO2001040262A1 (en) | 1999-12-03 | 2001-06-07 | Bristol-Myers Squibb Pharma Company | Alpha-ketoamide inhibitors of hepatitis c virus ns3 protease |
| JP2002030053A (ja) * | 2000-07-13 | 2002-01-29 | Senju Pharmaceut Co Ltd | α−ケトアミド誘導体の製造法 |
| CZ2003195A3 (cs) | 2000-07-21 | 2003-04-16 | Schering Corporation | Peptidové inhibitory serinové proteázy NS3 a farmaceutický prostředek |
| EP1553964A4 (en) * | 2002-09-25 | 2009-08-12 | Georgia Tech Res Inst | INHIBITORS OF CETOAMIDES IN CHRONIC NERVOUS DISEASES |
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| CA2617294A1 (en) | 2005-08-03 | 2007-02-08 | Boehringer Ingelheim International Gmbh | Substituted ethane-1,2-diamines for the treatment of alzheimer's disease ii |
| WO2007041775A1 (en) | 2005-10-10 | 2007-04-19 | The University Of Queensland | Cysteine protease inhibitors incorporating azide groups |
| GB201001070D0 (en) | 2010-01-22 | 2010-03-10 | St George's Hospital Medical School | Theraputic compounds and their use |
| GB201011411D0 (en) | 2010-07-06 | 2010-08-18 | St Georges Hosp Medical School | Therapeutic compounds and their use |
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- 2011-01-21 US US13/521,067 patent/US8541363B2/en not_active Expired - Fee Related
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