CO5080726A1 - Drogas antiangiogenicas basadas en peptidos - Google Patents
Drogas antiangiogenicas basadas en peptidosInfo
- Publication number
- CO5080726A1 CO5080726A1 CO99031377A CO99031377A CO5080726A1 CO 5080726 A1 CO5080726 A1 CO 5080726A1 CO 99031377 A CO99031377 A CO 99031377A CO 99031377 A CO99031377 A CO 99031377A CO 5080726 A1 CO5080726 A1 CO 5080726A1
- Authority
- CO
- Colombia
- Prior art keywords
- alanyl
- phenylalanyl
- seryl
- threonyl
- methionyl
- Prior art date
Links
- 239000004037 angiogenesis inhibitor Substances 0.000 title 1
- 102000004196 processed proteins & peptides Human genes 0.000 title 1
- 108090000765 processed proteins & peptides Proteins 0.000 title 1
- -1 N-acetylamino Chemical group 0.000 abstract 26
- 125000001980 alanyl group Chemical group 0.000 abstract 19
- 125000000405 phenylalanyl group Chemical group 0.000 abstract 10
- 125000000266 alpha-aminoacyl group Chemical group 0.000 abstract 9
- 125000002073 methionyl group Chemical group 0.000 abstract 8
- 125000001288 lysyl group Chemical group 0.000 abstract 7
- 125000002072 seryl group Chemical group 0.000 abstract 7
- 125000002436 D-phenylalanyl group Chemical group N[C@@H](C(=O)*)CC1=CC=CC=C1 0.000 abstract 6
- 125000003630 glycyl group Chemical group [H]N([H])C([H])([H])C(*)=O 0.000 abstract 6
- 125000001500 prolyl group Chemical group [H]N1C([H])(C(=O)[*])C([H])([H])C([H])([H])C1([H])[H] 0.000 abstract 6
- 125000000291 glutamic acid group Chemical group N[C@@H](CCC(O)=O)C(=O)* 0.000 abstract 5
- 125000001939 glutaminyl group Chemical group 0.000 abstract 5
- 229910052739 hydrogen Inorganic materials 0.000 abstract 5
- 239000001257 hydrogen Substances 0.000 abstract 5
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 abstract 5
- 125000000341 threoninyl group Chemical group [H]OC([H])(C([H])([H])[H])C([H])(N([H])[H])C(*)=O 0.000 abstract 5
- JIZNFRPSBHXXMD-SCSAIBSYSA-N (4R)-1,4-diaminopentan-3-one Chemical compound C[C@@H](N)C(=O)CCN JIZNFRPSBHXXMD-SCSAIBSYSA-N 0.000 abstract 4
- 125000000217 alkyl group Chemical group 0.000 abstract 4
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 4
- 125000000722 D-seryl group Chemical group N[C@@H](C(=O)*)CO 0.000 abstract 3
- 125000000197 D-threonyl group Chemical group N[C@@H](C(=O)*)[C@H](C)O 0.000 abstract 3
- 125000000240 D-tyrosyl group Chemical group N[C@@H](C(=O)*)CC1=CC=C(C=C1)O 0.000 abstract 3
- 125000000637 arginyl group Chemical group N[C@@H](CCCNC(N)=N)C(=O)* 0.000 abstract 3
- 125000001942 asparaginyl group Chemical group 0.000 abstract 3
- 125000000051 benzyloxy group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])O* 0.000 abstract 3
- 125000000487 histidyl group Chemical group [H]N([H])C(C(=O)O*)C([H])([H])C1=C([H])N([H])C([H])=N1 0.000 abstract 3
- 150000002431 hydrogen Chemical group 0.000 abstract 3
- 125000000741 isoleucyl group Chemical group [H]N([H])C(C(C([H])([H])[H])C([H])([H])C([H])([H])[H])C(=O)O* 0.000 abstract 3
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 abstract 3
- AHLPHDHHMVZTML-BYPYZUCNSA-N ornithyl group Chemical group N[C@@H](CCCN)C(=O)O AHLPHDHHMVZTML-BYPYZUCNSA-N 0.000 abstract 3
- OGQDIIKRQRZXJH-UHFFFAOYSA-N protriptyline hydrochloride Chemical group [Cl-].C1=CC2=CC=CC=C2C(CCC[NH2+]C)C2=CC=CC=C21 OGQDIIKRQRZXJH-UHFFFAOYSA-N 0.000 abstract 3
- 125000001493 tyrosinyl group Chemical group [H]OC1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])C([H])(N([H])[H])C(*)=O 0.000 abstract 3
- HQMLIDZJXVVKCW-UWTATZPHSA-N (2r)-2-aminopropanamide Chemical compound C[C@@H](N)C(N)=O HQMLIDZJXVVKCW-UWTATZPHSA-N 0.000 abstract 2
- WAMWSIDTKSNDCU-ZETCQYMHSA-N (2s)-2-azaniumyl-2-cyclohexylacetate Chemical group OC(=O)[C@@H](N)C1CCCCC1 WAMWSIDTKSNDCU-ZETCQYMHSA-N 0.000 abstract 2
- 125000001622 2-naphthyl group Chemical group [H]C1=C([H])C([H])=C2C([H])=C(*)C([H])=C([H])C2=C1[H] 0.000 abstract 2
- 125000003349 3-pyridyl group Chemical group N1=C([H])C([*])=C([H])C([H])=C1[H] 0.000 abstract 2
- 125000000988 D-alanyl group Chemical group N[C@@H](C(=O)*)C 0.000 abstract 2
- 125000003032 D-cystyl group Chemical group C([C@H](C(=O)*)N)SSC[C@H](C(=O)*)N 0.000 abstract 2
- 125000003442 D-glutaminyl group Chemical group N[C@@H](C(=O)*)CCC(=O)N 0.000 abstract 2
- 125000002058 D-lysyl group Chemical group N[C@@H](C(=O)*)CCCCN 0.000 abstract 2
- 125000000180 D-prolyl group Chemical group N1[C@@H](C(=O)*)CCC1 0.000 abstract 2
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical group [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 abstract 2
- 125000003545 alkoxy group Chemical group 0.000 abstract 2
- 125000003118 aryl group Chemical group 0.000 abstract 2
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical group [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 abstract 2
- 125000005842 heteroatom Chemical group 0.000 abstract 2
- 125000001998 leucyl group Chemical group 0.000 abstract 2
- 229910052757 nitrogen Inorganic materials 0.000 abstract 2
- 229910052760 oxygen Inorganic materials 0.000 abstract 2
- 239000001301 oxygen Chemical group 0.000 abstract 2
- 125000004482 piperidin-4-yl group Chemical group N1CCC(CC1)* 0.000 abstract 2
- 229910052717 sulfur Chemical group 0.000 abstract 2
- 239000011593 sulfur Chemical group 0.000 abstract 2
- ODANWMOQWMHGCY-UHFFFAOYSA-N 1,4-diaminobutan-2-one Chemical compound NCCC(=O)CN ODANWMOQWMHGCY-UHFFFAOYSA-N 0.000 abstract 1
- 125000001637 1-naphthyl group Chemical group [H]C1=C([H])C([H])=C2C(*)=C([H])C([H])=C([H])C2=C1[H] 0.000 abstract 1
- 125000004575 3-pyrrolidinyl group Chemical group [H]N1C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 abstract 1
- 125000000170 D-asparaginyl group Chemical group N[C@@H](C(=O)*)CC(=O)N 0.000 abstract 1
- 125000002237 D-aspartyl group Chemical group [H]OC(=O)[C@]([H])(N([H])[H])C([H])([H])C(*)=O 0.000 abstract 1
- 125000004077 D-glutamic acid group Chemical group [H]N([H])[C@@]([H])(C(=O)[*])C([H])([H])C([H])([H])C(N([H])[H])=O 0.000 abstract 1
- 125000002437 D-histidyl group Chemical group N[C@@H](C(=O)*)CC=1N=CNC1 0.000 abstract 1
- 125000000505 D-methionyl group Chemical group N[C@@H](C(=O)*)CCSC 0.000 abstract 1
- 125000003625 D-valyl group Chemical group N[C@@H](C(=O)*)C(C)C 0.000 abstract 1
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 abstract 1
- UKAUYVFTDYCKQA-VKHMYHEASA-N L-homoserine Chemical compound OC(=O)[C@@H](N)CCO UKAUYVFTDYCKQA-VKHMYHEASA-N 0.000 abstract 1
- 125000002252 acyl group Chemical group 0.000 abstract 1
- 150000001408 amides Chemical class 0.000 abstract 1
- 150000001413 amino acids Chemical class 0.000 abstract 1
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 abstract 1
- 125000004063 butyryl group Chemical group O=C([*])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 abstract 1
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 1
- 125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 abstract 1
- 125000004177 diethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 abstract 1
- 239000003814 drug Substances 0.000 abstract 1
- 229940079593 drug Drugs 0.000 abstract 1
- 150000002148 esters Chemical class 0.000 abstract 1
- BEBCJVAWIBVWNZ-UHFFFAOYSA-N glycinamide Chemical compound NCC(N)=O BEBCJVAWIBVWNZ-UHFFFAOYSA-N 0.000 abstract 1
- 229910052736 halogen Inorganic materials 0.000 abstract 1
- 150000002367 halogens Chemical class 0.000 abstract 1
- 125000000623 heterocyclic group Chemical group 0.000 abstract 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 1
- 229950003188 isovaleryl diethylamide Drugs 0.000 abstract 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 abstract 1
- GRVDJDISBSALJP-UHFFFAOYSA-N methyloxidanyl Chemical group [O]C GRVDJDISBSALJP-UHFFFAOYSA-N 0.000 abstract 1
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 abstract 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 1
- 239000002243 precursor Substances 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 239000012453 solvate Substances 0.000 abstract 1
- 150000003457 sulfones Chemical class 0.000 abstract 1
- 150000003462 sulfoxides Chemical class 0.000 abstract 1
- 125000002114 valyl group Chemical group 0.000 abstract 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K7/00—Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
-
- 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]
-
- 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
- A61P19/00—Drugs for skeletal disorders
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
-
- 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
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/04—Antibacterial agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- 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
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Animal Behavior & Ethology (AREA)
- General Chemical & Material Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Diabetes (AREA)
- Rheumatology (AREA)
- Biochemistry (AREA)
- Oncology (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Molecular Biology (AREA)
- Communicable Diseases (AREA)
- Genetics & Genomics (AREA)
- Biophysics (AREA)
- Emergency Medicine (AREA)
- Pain & Pain Management (AREA)
- Ophthalmology & Optometry (AREA)
- Immunology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Physical Education & Sports Medicine (AREA)
- Dermatology (AREA)
- Toxicology (AREA)
- Zoology (AREA)
- Gastroenterology & Hepatology (AREA)
- Obesity (AREA)
- Hematology (AREA)
- Endocrinology (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Peptides Or Proteins (AREA)
Abstract
Un Compuesto de fórmula A0-A1-A2-A3-A4-A5-A6-A7-A8-A9-A10ó una sal, éster, solvato ó precursor de droga farmacéuticamente aceptables de éste, en dondeA0 es hidrógeno ó un grupo acilo seleccionado entre:R-(CH2 )n -C(O)- ; en donde n es un número entero entre 0 - 8 y R se selecciona entre hidroxil; metil; N-acetilamino; metoxil; carboxil; ciclohexil, el cual opcionalmente contiene de uno a dos dobles enlaces y opcionalmente va sustituido con uno a tres grupos hidroxilo; y un anillo aromático, ó uno no aromático, de 5 ó 6 miembros que opcionalmente contiene uno ó dos heteroátomos seleccionados entre nitrógeno, oxígeno, y azufre, en donde el anillo va opcionalmente sustituido con una porción molecular seleccionada entre alquil, alcoxi, y halógeno; yR1-CH2CH2 -(OCH2CH2O)p -CH2 -C(O)- ; en donde R1 se selecciona entre hidrógeno, alquil, y N-acetilamino, y p es un entero entre 1 y 8:A1 es un residuo aminoacil seleccionado entre:(1) alanil(2) asparaginil,(3) citrulil,(4) glutaminil,(5) glutamil,(6) N-etilglicil,(7) metionil,(8) N-metilalanil,(9) prolil,(10) piro-glutamil,(11) sarcosil,(12) seril,(13) treonil,(14) -HN-(CH2 )q -C(O)- ; en donde q va de 1 a 8, y(15) -HN-CH2 CH2 -(OCH2 CH2 O)r -CH2 -C(O)- , en donde r va de 0 a 8;A2 es un residuo aminoacil seleccionado entre:(1) alanil,(2) asparaginil,(3) aspartil(4) glutaminil,(5) glutamil,(6) leucil,(7) metionil,(8) fenilalanil(9) prolil(10) seril(11) -HN-(CH2 )q -C(O)- ; en donde q va de 1 a 8, y- 2 -(12) -HN-CH2 CH2 -(OCH2 CH2 O)r -CH2 -C(O)- , en donde r va de 0 a 8;A3 es un residuo aminoacil seleccionado entre:(1) alanil,(2) asparaginil,(3) citrulil,(4) ciclohexilalanil,(5) ciciohexilglicil,(6) glutaminil,(7) glutamil(8) glicil,(9) isoleucil,(10) leucil,(11) metionil,(12) norvalil,(13) fenilalanil,(14) seril,(15) t-butilglicil,(16) treonil, y(17) valil;A4 es un residuo aminoacil de configuración L ó D seleccionado entre:(1) alo-isoleucil,(2) glicil,(3) isoleucil,(4) prolil,(5) dehidroleucil,(6) D-alanil,(7) D-3-(naft-1-il)alanil,(8) D-3-(naft-2-il)alanil,(9) D-(3-piridil)-alanil,(10) D-2-aminobutiril,(11) D-alo-isoleucil,(12) D-alo-treonil;(13) alilglicil,(14) D-asparaginil,(15) D-aspartil,(16) D-benzotienil,(17) D-4,4'-bifenilalanil,(18) D-cloro-fenilalanil,(19) D-3-CF3 fenilalanil,(20) D-3-cianofenilalanil,(21) D-3,4-difluorofenilalanil,(22) D-citrulil,(23) D-ciclohexilalanil,(24) D-ciclohexilglicil,(25) D-cistil(S-acetamidometil),(26) D-cistil(S-t-butil),(27) D-glutaminil,(28) D-glutamil,(29) D-histidil,(30) D-homoisoleucil,(31) D-homofenilalanil,(32) D-homoseril,(33) D-isoleucil,(34) D-leucil,(35) D-lisil(N-epsilon-nicotinil),(36) D-lisil,(37) D-metionil(38) D-neopentilglicil,(39) D-norleucil,(40) D-norvalil,(41) D-ornitil,(42) D-penacilaminil,(43) D-penacilaminil(acetamidometil),(44) D-penacilaminil(bencil),(45) D-fenilalanil,(46) D-fenilalanil(4-amino),(47) D-fenilalanil(4-metil),(48) D-fenilalanil(4-nitro),(49) D-fenilalanil(3,4-dimetoxi),(50) D-fenilalanil(3,4,5-trifluoro),(51) D-prolil,(52) D-seril,(53) D-seril(O-bencil),(54) D-t-butilglicil,(55) D-tienilalanil,(56) D-treonil(57) D-treonil(O-bencil),(58) D-triptil,(59) D-tirosil(O-bencil),(60) D-tirosil(O-etil)(61) D-tirosil, y(62) D-valil;A5 es un residuo aminoacil de configuración L ó D seleccionado entre:(1) alanil,(2) (3-piridil)alanil,(3) N-(naft-1-il)alanil(4) N-(naft-2-il)alanil,(5) alo-treonil,(6) alilglicil,(7) glutaminil,(8) glicil,(9) histidil,(10) homoseril,(11) isoleucil,(12) lisil(N-epsilon-acetil)(13) metionil,(14) norvalil,(15) octilglicil, (16) ornitil,(17) fenilalanil(4-CH2 OH),(18) prolil,(19) seril,- 3 -(20) treonil,(21) triptil,(22) tirosil,(23) D-alo-treonil,(24) D-homoseril,(25) D-seril, y(26) D-treonil;A6 es un residuo aminoacil de configuración L ó D seleccionado entre:(1) alanil,(2) N-(naft-1-il)alanil(3) N-(naft-2-il)alanil(4) (3-piridil)alanil,(5) 2-aminobutiril,(6) alilglicil,(7) arginil,(8) asparaginil,(9) aspartil,(10) citrulil,(11) ciclohexilalanil,(12) glutaminil,(13) glutamil,(14) glicil,(15) histidil, (16) homoalanil,(17) homoleucil,(18) homoseril,(19) isoleucil,(20) leucil,(21) lisil(N-epsilon-acetil),(22) lisil(N-epsilon-isopropil),(23) metionil(sulfona),(24) metionil(sulfóxido),(25) metionil,(26) norleucil,(27) norvalil,(28) octilglicil,(29) fenilalanil,(30) fenilalanil(4-CONH2 ),(31) propargilglicil,(32) seril,(33) treonil,(34) triptil,(35) tirosil,(36) valil,(37) D-3-(naft-1-il)alanil,(38) D-3-(naft-2-il)alanil,(39) D-glutaminil,(40) D-homoseril,(41) D-leucil,(42) D-norvalil, y(43) D-seril;A7 es un residuo aminoacil de configuración L ó D seleccionado entre:(1) alanil,(2) alilglicil,(3) aspartil,(4) citrulil,(5) ciclohexilglicil,(6) glutamil,(7) glicil,(8) homoseril,(9) isoleucil,(10) leucil,(11) lisil(N-epsilon-acetil),(12) metionil,(13) N-(naft-1-il)alanil,(14) N-(naft-2-il)alanil,(15) norvalil,(16) fenilalanil,(17) prolil,(18) seril,(19) t-butilglicil,(20) triptil,(21) tirosil,(22) valil, y(23) D-isoleucil;A8 es un residuo aminoacil seleccionado entre:(1) 2-amino-4-((2-amino)-pirimidinil(butanoil,(2) alanil(3-guanidino),(3) alanil(3-pirrolidinil(2-N-amidino)(,(4) alanil(4-piperidinil(N-amidino)(,(5) arginil,(6) arginil(NG NG'dietil),(7) citrulil,(8) ciclohexilalanil(4-amino-N-isopropil),(9) glicil(4-piperidinil(N-amidino) (,(10) histidil,(11) homoarginil,(12) lisil,(13) lisil(N-epsilon-isopropil),(14) lisil(N-epsilon-nicotinil),(15) norarginil,(16) ornitil(N-delta-isopropi1),(17) ornitil(N-delta-nicotinil),(18) ornitil(N-delta-(2-imidazolinil)(,(19) fenilalanil(4-CH2 -NH-isopropil),(20) fenilalanil(4-guanidino), y(21) fenilalanil(4-NH-isopropil);A9 es un residuo aminoacil de configuración L ó D seleccionado entre:- 4 -(1) 2-amino-butiril,(2) 2-amino-isobutiril,(3) homoprolil,(4) hidroxiprolil,(5) isoleucil,(6) leucil,(7) fenilalanil,(8) prolil,(9) seril,(10) t-butilglicil,(11) 1,2,3,4-tetrahidroisoquinolina-3-carbonil,(12) treonil,(13) valil,(14) D-alanil, y(15) D-prolil;A10 es una amida de un aminoácido seleccionada entre:(1) azaglicilamida,(2) D-alanilamida, (3) D-alaniletilamida,(4) glicilamida,(5) gliciletilamida,(6) sarcosilamida, y(7) seril amida,(8) un grupo representado por la fórmulaR2|-NH-(CH2)S-CHR3; y (9) un grupo representado por la fórmula -NH-R4;en donde:S es un entero seleccionado entre O y 8,R2 se selecciona entre hidrógeno, alquil, y un anillo cicloalquil de 5 a 6 miembros;R3 se selecciona entre hidrógeno, hidroxi, alquil, fenil, alcoxi, y un anillo heterociclo de 5 a 6 miembros que opcionalmente contiene de uno a dos heteroátomos seleccionados entre oxígeno, nitrógeno, y azufre; yR4 se selecciona entre hidrógeno e hidroxi.
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US8374598A | 1998-05-22 | 1998-05-22 | |
US25057499A | 1999-02-16 | 1999-02-16 | |
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JP (3) | JP3753612B2 (es) |
KR (1) | KR100447696B1 (es) |
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CO (1) | CO5080726A1 (es) |
CY (1) | CY1109118T1 (es) |
CZ (1) | CZ299639B6 (es) |
DE (1) | DE69938782D1 (es) |
ES (1) | ES2307337T3 (es) |
HK (1) | HK1037376A1 (es) |
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PL (1) | PL200471B1 (es) |
PT (1) | PT1078002E (es) |
SI (1) | SI1078002T1 (es) |
SK (1) | SK286554B6 (es) |
TR (1) | TR200003442T2 (es) |
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Families Citing this family (28)
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US6774211B1 (en) | 1998-05-22 | 2004-08-10 | Abbott Laboratories | Peptide antiangiogenic drugs |
CA2622786A1 (en) * | 1998-10-16 | 2000-04-27 | Naoto Oku | Neovascular-specific peptides |
US7488590B2 (en) | 1998-10-23 | 2009-02-10 | Amgen Inc. | Modified peptides as therapeutic agents |
SI2319928T1 (sl) | 1998-10-23 | 2013-08-30 | Kirin-Amgen, Inc. | Dimerni trombopoietinski peptidni mimetiki, ki se veĺ˝ejo na receptor mp1 in imajo trombopoietinsko aktivnost |
US20020183242A1 (en) * | 2001-04-11 | 2002-12-05 | Jack Henkin | Peptide antiangiogenic drugs |
US20030050246A1 (en) * | 2001-07-26 | 2003-03-13 | Fortuna Haviv | Peptides having antiangiogenic activity |
US7169888B2 (en) | 2001-10-31 | 2007-01-30 | Abbott Laboratories | Tetra-, penta-, hexa- and heptapeptides having antiangiogenic activity |
CN1639188A (zh) * | 2001-10-31 | 2005-07-13 | 艾博特公司 | 具有抗血管形成活性的七-、八-和九-肽 |
US7001984B2 (en) | 2001-10-31 | 2006-02-21 | Abbott Laboratories | Di-, tri-, and tetra-peptides having antiangiogenic activity |
US20030125260A1 (en) * | 2001-10-31 | 2003-07-03 | Fortuna Haviv | Tetra-and pentapeptides having antiangiogenic activity |
US20030105025A1 (en) * | 2001-10-31 | 2003-06-05 | Fortuna Haviv | Tri-and tetrapeptides having antiangiogenic activity |
US20030119746A1 (en) * | 2001-10-31 | 2003-06-26 | Fortuna Haviv | Hepta-and octapeptides having antiangiogenic activity |
US20030125259A1 (en) | 2001-10-31 | 2003-07-03 | Fortuna Haviv | Octa- and nonapeptides having antiangiogenic activity |
WO2003037266A2 (en) * | 2001-10-31 | 2003-05-08 | Abbott Laboratories | Tetra-, penta-, hexa- and heptapeptides having antiangiogenic activity |
US7122625B2 (en) | 2001-10-31 | 2006-10-17 | Abbott Laboratories | Hexa-, hepta-, and octapeptides having antiangiogenic activity |
US7037897B2 (en) | 2001-10-31 | 2006-05-02 | Abbott Laboratories | TRI-, TETRA-, and penta-peptides having antiangiogenic activity |
US7067490B2 (en) | 2001-10-31 | 2006-06-27 | Abbott Laboratories | Hepta-, Octa-and nonapeptides having antiangiogenic activity |
CN1652810A (zh) | 2002-03-22 | 2005-08-10 | Gpc生物科技股份公司 | 免疫抑制化合物、方法及其相关应用 |
US7432245B2 (en) | 2002-06-07 | 2008-10-07 | Abbott Laboratories Inc. | Pharmaceutical formulation comprising a peptide angiogenesis inhibitor |
US20030228365A1 (en) * | 2002-06-07 | 2003-12-11 | Fortuna Haviv | Pharmaceutical formulation |
JP5167473B2 (ja) | 2005-03-03 | 2013-03-21 | コヴェックス・テクノロジーズ・アイルランド・リミテッド | 抗血管新生化合物 |
US8008453B2 (en) | 2005-08-12 | 2011-08-30 | Amgen Inc. | Modified Fc molecules |
JP2007255910A (ja) * | 2006-03-20 | 2007-10-04 | Hokkaido Univ | Nmrシグナルの帰属方法 |
JO3324B1 (ar) | 2006-04-21 | 2019-03-13 | Amgen Inc | مركبات علاجية مجففة بالتبريد تتعلق بالعصارة الهضمية |
WO2008003013A2 (en) * | 2006-06-29 | 2008-01-03 | Abbott Laboratories | Antitumorigenic drug combination comprising an hdac inhibitor and a tsp-1 peptidomimetic |
CN104004057B (zh) * | 2013-02-25 | 2016-08-24 | 上海市第一人民医院 | 一类抑制新生血管的小肽及其应用 |
CN107778355B (zh) * | 2016-08-25 | 2021-04-20 | 成都圣诺生物制药有限公司 | 一种合成西曲瑞克的方法 |
WO2023033016A1 (ja) * | 2021-09-01 | 2023-03-09 | 積水メディカル株式会社 | アルギニン誘導体 |
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US5200397A (en) * | 1990-02-22 | 1993-04-06 | W. R. Grace & Co.-Conn. | Use of peptide analogs of thrombospondin for the inhibition of angiogenic activity |
WO1993016716A1 (en) * | 1992-02-24 | 1993-09-02 | Northwestern University | Method and composition for inhibiting angiogenesis |
IL126626A0 (en) * | 1996-05-03 | 1999-08-17 | Abbott Lab | Novel antiangiogenic peptides polynucleotides encoding same and methods for inhibiting angiogenesis |
PT918795E (pt) * | 1997-03-17 | 2005-02-28 | Abbott Lab | Droga antiangiogenica para tratar cancro artrite e retinopatia |
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