CA2412849A1 - Agents pharmaceutiques antagonistes du recepteur de la vitronectine destines a etre utilises dans une therapie combinee - Google Patents
Agents pharmaceutiques antagonistes du recepteur de la vitronectine destines a etre utilises dans une therapie combinee Download PDFInfo
- Publication number
- CA2412849A1 CA2412849A1 CA002412849A CA2412849A CA2412849A1 CA 2412849 A1 CA2412849 A1 CA 2412849A1 CA 002412849 A CA002412849 A CA 002412849A CA 2412849 A CA2412849 A CA 2412849A CA 2412849 A1 CA2412849 A1 CA 2412849A1
- Authority
- CA
- Canada
- Prior art keywords
- substituted
- group
- independently selected
- bond
- carbamoyl
- 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.)
- Abandoned
Links
- 239000003814 drug Substances 0.000 title abstract description 35
- 238000002648 combination therapy Methods 0.000 title abstract description 13
- 102100022337 Integrin alpha-V Human genes 0.000 title description 13
- 108010048673 Vitronectin Receptors Proteins 0.000 title description 13
- 239000002464 receptor antagonist Substances 0.000 title description 2
- 229940044551 receptor antagonist Drugs 0.000 title description 2
- 206010028980 Neoplasm Diseases 0.000 claims abstract description 98
- 150000001875 compounds Chemical class 0.000 claims abstract description 84
- 201000011510 cancer Diseases 0.000 claims abstract description 48
- 230000008685 targeting Effects 0.000 claims abstract description 41
- 125000005647 linker group Chemical group 0.000 claims abstract description 38
- 230000033115 angiogenesis Effects 0.000 claims abstract description 29
- 238000011282 treatment Methods 0.000 claims abstract description 29
- 229910052717 sulfur Inorganic materials 0.000 claims description 375
- -1 2-benzimidazolylmethyl Chemical group 0.000 claims description 144
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 claims description 139
- 229910052757 nitrogen Inorganic materials 0.000 claims description 134
- 125000000623 heterocyclic group Chemical group 0.000 claims description 122
- QTBSBXVTEAMEQO-UHFFFAOYSA-N Acetic acid Chemical compound CC(O)=O QTBSBXVTEAMEQO-UHFFFAOYSA-N 0.000 claims description 118
- FERIUCNNQQJTOY-UHFFFAOYSA-N Butyric acid Chemical compound CCCC(O)=O FERIUCNNQQJTOY-UHFFFAOYSA-N 0.000 claims description 116
- 239000003446 ligand Substances 0.000 claims description 103
- 125000005842 heteroatom Chemical group 0.000 claims description 102
- 125000003118 aryl group Chemical group 0.000 claims description 101
- 238000000034 method Methods 0.000 claims description 88
- 125000000738 acetamido group Chemical group [H]C([H])([H])C(=O)N([H])[*] 0.000 claims description 77
- 229940121896 radiopharmaceutical Drugs 0.000 claims description 77
- 239000012217 radiopharmaceutical Substances 0.000 claims description 77
- 230000002799 radiopharmaceutical effect Effects 0.000 claims description 77
- 229910052760 oxygen Inorganic materials 0.000 claims description 73
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 claims description 71
- 239000000203 mixture Substances 0.000 claims description 69
- 239000003795 chemical substances by application Substances 0.000 claims description 67
- 125000000217 alkyl group Chemical group 0.000 claims description 57
- 229940127044 therapeutic radiopharmaceutical Drugs 0.000 claims description 55
- 150000003839 salts Chemical class 0.000 claims description 52
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- 238000003384 imaging method Methods 0.000 claims description 39
- 125000000008 (C1-C10) alkyl group Chemical group 0.000 claims description 38
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims description 38
- 239000003504 photosensitizing agent Substances 0.000 claims description 37
- 125000001301 ethoxy group Chemical group [H]C([H])([H])C([H])([H])O* 0.000 claims description 32
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims description 32
- 229910052739 hydrogen Inorganic materials 0.000 claims description 31
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- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims description 30
- 229940024606 amino acid Drugs 0.000 claims description 30
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- 150000001413 amino acids Chemical class 0.000 claims description 29
- 125000004093 cyano group Chemical group *C#N 0.000 claims description 28
- 229910052751 metal Inorganic materials 0.000 claims description 28
- 239000002184 metal Substances 0.000 claims description 28
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- 229920000858 Cyclodextrin Chemical group 0.000 claims description 24
- 125000006297 carbonyl amino group Chemical group [H]N([*:2])C([*:1])=O 0.000 claims description 24
- 125000003349 3-pyridyl group Chemical group N1=C([H])C([*])=C([H])C([H])=C1[H] 0.000 claims description 23
- 239000001257 hydrogen Substances 0.000 claims description 23
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims description 22
- 125000004051 hexyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])* 0.000 claims description 21
- OHSVLFRHMCKCQY-NJFSPNSNSA-N lutetium-177 Chemical compound [177Lu] OHSVLFRHMCKCQY-NJFSPNSNSA-N 0.000 claims description 21
- 125000006527 (C1-C5) alkyl group Chemical group 0.000 claims description 20
- 229910052740 iodine Inorganic materials 0.000 claims description 20
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 19
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- MKXKFYHWDHIYRV-UHFFFAOYSA-N flutamide Chemical compound CC(C)C(=O)NC1=CC=C([N+]([O-])=O)C(C(F)(F)F)=C1 MKXKFYHWDHIYRV-UHFFFAOYSA-N 0.000 claims description 18
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 18
- 125000000391 vinyl group Chemical group [H]C([*])=C([H])[H] 0.000 claims description 18
- 125000003545 alkoxy group Chemical group 0.000 claims description 17
- 239000003638 chemical reducing agent Substances 0.000 claims description 17
- 229920002554 vinyl polymer Polymers 0.000 claims description 17
- KFZMGEQAYNKOFK-UHFFFAOYSA-N 2-propanol Substances CC(C)O KFZMGEQAYNKOFK-UHFFFAOYSA-N 0.000 claims description 15
- VWQVUPCCIRVNHF-OUBTZVSYSA-N Yttrium-90 Chemical group [90Y] VWQVUPCCIRVNHF-OUBTZVSYSA-N 0.000 claims description 15
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims description 15
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims description 15
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- 235000019260 propionic acid Nutrition 0.000 claims description 14
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 13
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- OUYCCCASQSFEME-UHFFFAOYSA-N tyrosine Natural products OC(=O)C(N)CC1=CC=C(O)C=C1 OUYCCCASQSFEME-UHFFFAOYSA-N 0.000 claims description 13
- DYCLHZPOADTVKK-UHFFFAOYSA-N 2-(2-azaniumyl-1,3-thiazol-4-yl)acetate Chemical compound NC1=NC(CC(O)=O)=CS1 DYCLHZPOADTVKK-UHFFFAOYSA-N 0.000 claims description 12
- KZSNJWFQEVHDMF-SCSAIBSYSA-N D-valine Chemical compound CC(C)[C@@H](N)C(O)=O KZSNJWFQEVHDMF-SCSAIBSYSA-N 0.000 claims description 12
- 229930182831 D-valine Natural products 0.000 claims description 12
- KZSNJWFQEVHDMF-BYPYZUCNSA-N L-valine Chemical compound CC(C)[C@H](N)C(O)=O KZSNJWFQEVHDMF-BYPYZUCNSA-N 0.000 claims description 12
- SVUOLADPCWQTTE-UHFFFAOYSA-N 1h-1,2-benzodiazepine Chemical compound N1N=CC=CC2=CC=CC=C12 SVUOLADPCWQTTE-UHFFFAOYSA-N 0.000 claims description 11
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- ZDXPYRJPNDTMRX-VKHMYHEASA-N L-glutamine Chemical compound OC(=O)[C@@H](N)CCC(N)=O ZDXPYRJPNDTMRX-VKHMYHEASA-N 0.000 claims description 11
- 230000002159 abnormal effect Effects 0.000 claims description 11
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- 150000001723 carbon free-radicals Chemical group 0.000 claims description 10
- 150000002431 hydrogen Chemical group 0.000 claims description 10
- 125000006850 spacer group Chemical group 0.000 claims description 10
- 150000003573 thiols Chemical group 0.000 claims description 10
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- NDMPLJNOPCLANR-UHFFFAOYSA-N 3,4-dihydroxy-15-(4-hydroxy-18-methoxycarbonyl-5,18-seco-ibogamin-18-yl)-16-methoxy-1-methyl-6,7-didehydro-aspidospermidine-3-carboxylic acid methyl ester Natural products C1C(CC)(O)CC(CC2(C(=O)OC)C=3C(=CC4=C(C56C(C(C(O)C7(CC)C=CCN(C67)CC5)(O)C(=O)OC)N4C)C=3)OC)CN1CCC1=C2NC2=CC=CC=C12 NDMPLJNOPCLANR-UHFFFAOYSA-N 0.000 claims description 9
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- ANOBYBYXJXCGBS-UHFFFAOYSA-L stannous fluoride Chemical compound F[Sn]F ANOBYBYXJXCGBS-UHFFFAOYSA-L 0.000 description 1
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- 150000003505 terpenes Chemical class 0.000 description 1
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- PGPJNVVZNGIMEW-IBGZPJMESA-N tert-butyl 3-[[[(2s)-2-amino-4-methoxy-4-oxobutanoyl]-[3-[(2-methylpropan-2-yl)oxycarbonylamino]propyl]amino]methyl]-4-fluorobenzoate Chemical compound CC(C)(C)OC(=O)NCCCN(C(=O)[C@@H](N)CC(=O)OC)CC1=CC(C(=O)OC(C)(C)C)=CC=C1F PGPJNVVZNGIMEW-IBGZPJMESA-N 0.000 description 1
- ZMESEBIFEZOHCI-QFIPXVFZSA-N tert-butyl 3-[[[(2s)-2-amino-4-methoxy-4-oxobutanoyl]-[6-[(2-methylpropan-2-yl)oxycarbonylamino]hexyl]amino]methyl]-4-fluorobenzoate Chemical compound CC(C)(C)OC(=O)NCCCCCCN(C(=O)[C@@H](N)CC(=O)OC)CC1=CC(C(=O)OC(C)(C)C)=CC=C1F ZMESEBIFEZOHCI-QFIPXVFZSA-N 0.000 description 1
- XJPPVNDOJKVRKC-UHFFFAOYSA-N tert-butyl 4-fluoro-3-[[6-[(2-methylpropan-2-yl)oxycarbonylamino]hexylamino]methyl]benzoate Chemical compound CC(C)(C)OC(=O)NCCCCCCNCC1=CC(C(=O)OC(C)(C)C)=CC=C1F XJPPVNDOJKVRKC-UHFFFAOYSA-N 0.000 description 1
- PUHUTEJEWJMQRG-UHFFFAOYSA-N tert-butyl 4-fluoro-3-[[methyl-[3-[(2-methylpropan-2-yl)oxycarbonylamino]propyl]amino]methyl]benzoate Chemical compound CC(C)(C)OC(=O)NCCCN(C)CC1=CC(C(=O)OC(C)(C)C)=CC=C1F PUHUTEJEWJMQRG-UHFFFAOYSA-N 0.000 description 1
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- 125000001412 tetrahydropyranyl group Chemical group 0.000 description 1
- 125000000147 tetrahydroquinolinyl group Chemical group N1(CCCC2=CC=CC=C12)* 0.000 description 1
- 230000004797 therapeutic response Effects 0.000 description 1
- 125000004627 thianthrenyl group Chemical group C1(=CC=CC=2SC3=CC=CC=C3SC12)* 0.000 description 1
- 125000000335 thiazolyl group Chemical group 0.000 description 1
- 125000002813 thiocarbonyl group Chemical group *C(*)=S 0.000 description 1
- 150000003585 thioureas Chemical class 0.000 description 1
- 125000002088 tosyl group Chemical group [H]C1=C([H])C(=C([H])C([H])=C1C([H])([H])[H])S(*)(=O)=O 0.000 description 1
- 231100000331 toxic Toxicity 0.000 description 1
- 230000002588 toxic effect Effects 0.000 description 1
- 230000009466 transformation Effects 0.000 description 1
- 229910052723 transition metal Inorganic materials 0.000 description 1
- 150000003624 transition metals Chemical class 0.000 description 1
- 125000004665 trialkylsilyl group Chemical group 0.000 description 1
- 125000004306 triazinyl group Chemical group 0.000 description 1
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- 230000005751 tumor progression Effects 0.000 description 1
- 238000000108 ultra-filtration Methods 0.000 description 1
- 238000002604 ultrasonography Methods 0.000 description 1
- 231100000402 unacceptable toxicity Toxicity 0.000 description 1
- 230000003827 upregulation Effects 0.000 description 1
- 150000003672 ureas Chemical class 0.000 description 1
- 239000004474 valine Substances 0.000 description 1
- 210000005167 vascular cell Anatomy 0.000 description 1
- 210000004509 vascular smooth muscle cell Anatomy 0.000 description 1
- 210000000264 venule Anatomy 0.000 description 1
- PXXNTAGJWPJAGM-UHFFFAOYSA-N vertaline Natural products C1C2C=3C=C(OC)C(OC)=CC=3OC(C=C3)=CC=C3CCC(=O)OC1CC1N2CCCC1 PXXNTAGJWPJAGM-UHFFFAOYSA-N 0.000 description 1
- 239000003039 volatile agent Substances 0.000 description 1
- 239000001993 wax Substances 0.000 description 1
- 125000001834 xanthenyl group Chemical group C1=CC=CC=2OC3=CC=CC=C3C(C12)* 0.000 description 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
- A61K31/551—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K51/00—Preparations containing radioactive substances for use in therapy or testing in vivo
- A61K51/02—Preparations containing radioactive substances for use in therapy or testing in vivo characterised by the carrier, i.e. characterised by the agent or material covalently linked or complexing the radioactive nucleus
- A61K51/04—Organic compounds
- A61K51/041—Heterocyclic compounds
- A61K51/044—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins
- A61K51/0468—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
- A61K51/047—Benzodiazepines
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K51/00—Preparations containing radioactive substances for use in therapy or testing in vivo
- A61K51/02—Preparations containing radioactive substances for use in therapy or testing in vivo characterised by the carrier, i.e. characterised by the agent or material covalently linked or complexing the radioactive nucleus
- A61K51/04—Organic compounds
- A61K51/0497—Organic compounds conjugates with a carrier being an organic compounds
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- A—HUMAN NECESSITIES
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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K51/00—Preparations containing radioactive substances for use in therapy or testing in vivo
- A61K51/02—Preparations containing radioactive substances for use in therapy or testing in vivo characterised by the carrier, i.e. characterised by the agent or material covalently linked or complexing the radioactive nucleus
- A61K51/04—Organic compounds
- A61K51/08—Peptides, e.g. proteins, carriers being peptides, polyamino acids, proteins
- A61K51/088—Peptides, e.g. proteins, carriers being peptides, polyamino acids, proteins conjugates with carriers being peptides, polyamino acids or proteins
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
- C07F9/02—Phosphorus compounds
- C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
- C07F9/645—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having two nitrogen atoms as the only ring hetero atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
- C07F9/02—Phosphorus compounds
- C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
- C07F9/6558—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system
- C07F9/65583—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system each of the hetero rings containing nitrogen as ring hetero atom
-
- 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
- C07K14/78—Connective tissue peptides, e.g. collagen, elastin, laminin, fibronectin, vitronectin or cold insoluble globulin [CIG]
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
- C07K5/02—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link
- C07K5/0215—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link containing natural amino acids, forming a peptide bond via their side chain functional group, e.g. epsilon-Lys, gamma-Glu
-
- 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
- C07K5/06008—Dipeptides with the first amino acid being neutral
- C07K5/06017—Dipeptides with the first amino acid being neutral and aliphatic
- C07K5/06026—Dipeptides with the first amino acid being neutral and aliphatic the side chain containing 0 or 1 carbon atom, i.e. Gly or Ala
-
- 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
- C07K5/06104—Dipeptides with the first amino acid being acidic
-
- 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
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K7/00—Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
- C07K7/50—Cyclic peptides containing at least one abnormal peptide link
- C07K7/52—Cyclic peptides containing at least one abnormal peptide link with only normal peptide links in the ring
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
-
- 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
- Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
- Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
- Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Molecular Biology (AREA)
- Biochemistry (AREA)
- Genetics & Genomics (AREA)
- Biophysics (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Epidemiology (AREA)
- Optics & Photonics (AREA)
- Physics & Mathematics (AREA)
- Toxicology (AREA)
- Zoology (AREA)
- Gastroenterology & Hepatology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US21321600P | 2000-06-21 | 2000-06-21 | |
US60/213,216 | 2000-06-21 | ||
PCT/US2001/020203 WO2001097861A2 (fr) | 2000-06-21 | 2001-06-21 | Agents pharmaceutiques antagonistes du recepteur de la vitronectine destines a etre utilises dans une therapie combinee |
Publications (1)
Publication Number | Publication Date |
---|---|
CA2412849A1 true CA2412849A1 (fr) | 2001-12-27 |
Family
ID=22794199
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
CA002412849A Abandoned CA2412849A1 (fr) | 2000-06-21 | 2001-06-21 | Agents pharmaceutiques antagonistes du recepteur de la vitronectine destines a etre utilises dans une therapie combinee |
Country Status (4)
Country | Link |
---|---|
EP (1) | EP1311292A2 (fr) |
AU (1) | AU2001271435A1 (fr) |
CA (1) | CA2412849A1 (fr) |
WO (1) | WO2001097861A2 (fr) |
Families Citing this family (19)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US6511649B1 (en) | 1998-12-18 | 2003-01-28 | Thomas D. Harris | Vitronectin receptor antagonist pharmaceuticals |
BR9917079A (pt) | 1998-12-18 | 2001-10-30 | Du Pont Pharm Co | Compostos antagonistas de receptor devitronectina, kit, composição metalofarmacêuticade diagnóstico ou terapêutica, composição deagente de contraste para ultra-som, composiçãoradiofarmacêutica terapêutica, composiçãofarmacêutica de diagnóstico, método detratamento da artrite reumatóide, do cancêr e darestenose em um paciente, método de formação deimagem da angiogênese terapêutica, do câncer, denovos vasos sanguìneos, da arteriosclerose, darestenose, da isquemia e da lesão por reperfusãodo miocárdio em um paciente |
EP1307226B1 (fr) * | 2000-06-21 | 2008-11-19 | Lantheus Medical Imaging, Inc. | Agents pharmaceutiques antagonistes du recepteur de vitronectine |
DE102004011512B4 (de) | 2004-03-08 | 2022-01-13 | Boehringer Ingelheim Vetmedica Gmbh | Pharmazeutische Zubereitung enthaltend Pimobendan |
US8980894B2 (en) | 2004-03-25 | 2015-03-17 | Boehringer Ingelheim Vetmedica Gmbh | Use of PDE III inhibitors for the treatment of asymptomatic (occult) heart failure |
EP1579862A1 (fr) | 2004-03-25 | 2005-09-28 | Boehringer Ingelheim Vetmedica Gmbh | Utilisation des inhibiteurs de PDE III pour la réduction de la taille du coeur chez des mammifères souffrant d'insufficances cardiaques |
US8926945B2 (en) | 2005-10-07 | 2015-01-06 | Guerbet | Compounds comprising a biological target recognizing part, coupled to a signal part capable of complexing gallium |
US8986650B2 (en) | 2005-10-07 | 2015-03-24 | Guerbet | Complex folate-NOTA-Ga68 |
EP1920785A1 (fr) | 2006-11-07 | 2008-05-14 | Boehringer Ingelheim Vetmedica Gmbh | Préparation liquide contenant un complexe du pimobendane et de la cyclodextrine |
ES2436716T3 (es) | 2008-11-25 | 2014-01-03 | Boehringer Ingelheim Vetmedica Gmbh | Pimobendan para uso en el tratamiento de la cardiomiopatía hipertrófica en gatos |
FR2942227B1 (fr) | 2009-02-13 | 2011-04-15 | Guerbet Sa | Utilisation de tampons pour la complexation de radionucleides |
RS55491B2 (sr) | 2010-01-28 | 2020-11-30 | Eagle Pharmaceuticals Inc | Formulacije bendamustina |
FR2968999B1 (fr) | 2010-12-20 | 2013-01-04 | Guerbet Sa | Nanoemulsion de chelate pour irm |
FR2980364B1 (fr) | 2011-09-26 | 2018-08-31 | Guerbet | Nanoemulsions et leur utilisation comme agents de contraste |
ES2924478T3 (es) | 2012-03-15 | 2022-10-07 | Boehringer Ingelheim Vetmedica Gmbh | Formulación de comprimidos farmacéuticos para el sector médico veterinario, método de producción y uso de los mismos |
FR3001154B1 (fr) | 2013-01-23 | 2015-06-26 | Guerbet Sa | Magneto-emulsion vectorisee |
CN105377235A (zh) | 2013-07-19 | 2016-03-02 | 勃林格殷格翰动物保健有限公司 | 含有防腐的醚化的环糊精衍生物的液体水性药物组合物 |
BR112016011111B1 (pt) | 2013-12-04 | 2022-11-16 | Boehringer Ingelheim Vetmedica Gmbh | Composições farmacêuticas aprimoradas de pimobendan |
US10537570B2 (en) | 2016-04-06 | 2020-01-21 | Boehringer Ingelheim Vetmedica Gmbh | Use of pimobendan for the reduction of heart size and/or the delay of onset of clinical symptoms in patients with asymptomatic heart failure due to mitral valve disease |
Family Cites Families (8)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
ZA955391B (en) * | 1994-06-29 | 1996-02-09 | Smithkline Beecham Corp | Vitronectin receptor antagonists |
WO1999005107A1 (fr) * | 1997-07-25 | 1999-02-04 | Smithkline Beecham Corporation | Antagonistes du recepteur de vitronectine |
US6093382A (en) * | 1998-05-16 | 2000-07-25 | Bracco Research Usa Inc. | Metal complexes derivatized with folate for use in diagnostic and therapeutic applications |
CA2349333A1 (fr) * | 1998-12-18 | 2000-06-22 | Du Pont Pharmaceuticals Company | Medicaments antagonistes du recepteur de la vitronectine |
WO2001098294A2 (fr) * | 2000-06-21 | 2001-12-27 | Bristol-Myers Squibb Pharma Company | Produits pharmaceutiques d'antagonistes recepteurs de la vitronectine utilises en polytherapie |
EP1307226B1 (fr) * | 2000-06-21 | 2008-11-19 | Lantheus Medical Imaging, Inc. | Agents pharmaceutiques antagonistes du recepteur de vitronectine |
JP2005538030A (ja) * | 2000-06-21 | 2005-12-15 | デュポン ファーマシューティカルズ カンパニー | 組み合わせ療法での使用のための血管新生障害の画像診断用医薬 |
AU2002218751A1 (en) * | 2000-07-06 | 2002-01-21 | Bristol-Myers Squibb Pharma Company | Stable radiopharmaceutical compositions |
-
2001
- 2001-06-21 EP EP01950446A patent/EP1311292A2/fr not_active Withdrawn
- 2001-06-21 AU AU2001271435A patent/AU2001271435A1/en not_active Abandoned
- 2001-06-21 WO PCT/US2001/020203 patent/WO2001097861A2/fr not_active Application Discontinuation
- 2001-06-21 CA CA002412849A patent/CA2412849A1/fr not_active Abandoned
Also Published As
Publication number | Publication date |
---|---|
WO2001097861A2 (fr) | 2001-12-27 |
AU2001271435A1 (en) | 2002-01-02 |
WO2001097861A3 (fr) | 2003-02-27 |
EP1311292A2 (fr) | 2003-05-21 |
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