RU2011115815A - Комбинации средства, регулирующего частоту сердечных сокращений и агониста а-2-альфа рецепторов для применения в способах мультидетекторной компьютерной томографии - Google Patents
Комбинации средства, регулирующего частоту сердечных сокращений и агониста а-2-альфа рецепторов для применения в способах мультидетекторной компьютерной томографии Download PDFInfo
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- RU2011115815A RU2011115815A RU2011115815/15A RU2011115815A RU2011115815A RU 2011115815 A RU2011115815 A RU 2011115815A RU 2011115815/15 A RU2011115815/15 A RU 2011115815/15A RU 2011115815 A RU2011115815 A RU 2011115815A RU 2011115815 A RU2011115815 A RU 2011115815A
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- Prior art keywords
- receptor agonist
- pharmaceutical composition
- heart rate
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- 229940044601 receptor agonist Drugs 0.000 title claims abstract 19
- 239000000018 receptor agonist Substances 0.000 title claims abstract 19
- 230000001105 regulatory effect Effects 0.000 title claims abstract 12
- 238000000034 method Methods 0.000 title claims 17
- 238000002591 computed tomography Methods 0.000 title claims 3
- RYYVLZVUVIJVGH-UHFFFAOYSA-N caffeine Chemical compound CN1C(=O)N(C)C(=O)C2=C1N=CN2C RYYVLZVUVIJVGH-UHFFFAOYSA-N 0.000 claims abstract 16
- 239000008194 pharmaceutical composition Substances 0.000 claims abstract 13
- 239000003795 chemical substances by application Substances 0.000 claims abstract 10
- AQHHHDLHHXJYJD-UHFFFAOYSA-N propranolol Chemical compound C1=CC=C2C(OCC(O)CNC(C)C)=CC=CC2=C1 AQHHHDLHHXJYJD-UHFFFAOYSA-N 0.000 claims abstract 10
- LPHGQDQBBGAPDZ-UHFFFAOYSA-N Isocaffeine Natural products CN1C(=O)N(C)C(=O)C2=C1N(C)C=N2 LPHGQDQBBGAPDZ-UHFFFAOYSA-N 0.000 claims abstract 8
- 229960001948 caffeine Drugs 0.000 claims abstract 8
- VJEONQKOZGKCAK-UHFFFAOYSA-N caffeine Natural products CN1C(=O)N(C)C(=O)C2=C1C=CN2C VJEONQKOZGKCAK-UHFFFAOYSA-N 0.000 claims abstract 8
- ZFXYFBGIUFBOJW-UHFFFAOYSA-N theophylline Chemical compound O=C1N(C)C(=O)N(C)C2=C1NC=N2 ZFXYFBGIUFBOJW-UHFFFAOYSA-N 0.000 claims abstract 8
- 102000012740 beta Adrenergic Receptors Human genes 0.000 claims abstract 7
- 108010079452 beta Adrenergic Receptors Proteins 0.000 claims abstract 7
- -1 levoprolol Chemical compound 0.000 claims abstract 7
- 229960004195 carvedilol Drugs 0.000 claims abstract 6
- NPAKNKYSJIDKMW-UHFFFAOYSA-N carvedilol Chemical compound COC1=CC=CC=C1OCCNCC(O)COC1=CC=CC2=NC3=CC=C[CH]C3=C12 NPAKNKYSJIDKMW-UHFFFAOYSA-N 0.000 claims abstract 6
- 239000003087 receptor blocking agent Substances 0.000 claims abstract 6
- 229960003712 propranolol Drugs 0.000 claims abstract 5
- BYPFEZZEUUWMEJ-UHFFFAOYSA-N Pentoxifylline Chemical compound O=C1N(CCCCC(=O)C)C(=O)N(C)C2=C1N(C)C=N2 BYPFEZZEUUWMEJ-UHFFFAOYSA-N 0.000 claims abstract 4
- 229960003556 aminophylline Drugs 0.000 claims abstract 4
- FQPFAHBPWDRTLU-UHFFFAOYSA-N aminophylline Chemical compound NCCN.O=C1N(C)C(=O)N(C)C2=C1NC=N2.O=C1N(C)C(=O)N(C)C2=C1NC=N2 FQPFAHBPWDRTLU-UHFFFAOYSA-N 0.000 claims abstract 4
- 229960002237 metoprolol Drugs 0.000 claims abstract 4
- IUBSYMUCCVWXPE-UHFFFAOYSA-N metoprolol Chemical compound COCCC1=CC=C(OCC(O)CNC(C)C)C=C1 IUBSYMUCCVWXPE-UHFFFAOYSA-N 0.000 claims abstract 4
- 229960001476 pentoxifylline Drugs 0.000 claims abstract 4
- 229960000278 theophylline Drugs 0.000 claims abstract 4
- CEMAWMOMDPGJMB-UHFFFAOYSA-N (+-)-Oxprenolol Chemical compound CC(C)NCC(O)COC1=CC=CC=C1OCC=C CEMAWMOMDPGJMB-UHFFFAOYSA-N 0.000 claims abstract 3
- METKIMKYRPQLGS-GFCCVEGCSA-N (R)-atenolol Chemical compound CC(C)NC[C@@H](O)COC1=CC=C(CC(N)=O)C=C1 METKIMKYRPQLGS-GFCCVEGCSA-N 0.000 claims abstract 3
- TWBNMYSKRDRHAT-RCWTXCDDSA-N (S)-timolol hemihydrate Chemical compound O.CC(C)(C)NC[C@H](O)COC1=NSN=C1N1CCOCC1.CC(C)(C)NC[C@H](O)COC1=NSN=C1N1CCOCC1 TWBNMYSKRDRHAT-RCWTXCDDSA-N 0.000 claims abstract 3
- KOHIRBRYDXPAMZ-YHBROIRLSA-N (S,R,R,R)-nebivolol Chemical compound C1CC2=CC(F)=CC=C2O[C@H]1[C@H](O)CNC[C@@H](O)[C@H]1OC2=CC=C(F)C=C2CC1 KOHIRBRYDXPAMZ-YHBROIRLSA-N 0.000 claims abstract 3
- RZPZLFIUFMNCLY-WLHGVMLRSA-N (e)-but-2-enedioic acid;1-(propan-2-ylamino)-3-[4-(2-propan-2-yloxyethoxymethyl)phenoxy]propan-2-ol Chemical compound OC(=O)\C=C\C(O)=O.CC(C)NCC(O)COC1=CC=C(COCCOC(C)C)C=C1 RZPZLFIUFMNCLY-WLHGVMLRSA-N 0.000 claims abstract 3
- UUOJIACWOAYWEZ-UHFFFAOYSA-N 1-(tert-butylamino)-3-[(2-methyl-1H-indol-4-yl)oxy]propan-2-yl benzoate Chemical compound C1=CC=C2NC(C)=CC2=C1OCC(CNC(C)(C)C)OC(=O)C1=CC=CC=C1 UUOJIACWOAYWEZ-UHFFFAOYSA-N 0.000 claims abstract 3
- SGUAFYQXFOLMHL-UHFFFAOYSA-N 2-hydroxy-5-{1-hydroxy-2-[(4-phenylbutan-2-yl)amino]ethyl}benzamide Chemical compound C=1C=C(O)C(C(N)=O)=CC=1C(O)CNC(C)CCC1=CC=CC=C1 SGUAFYQXFOLMHL-UHFFFAOYSA-N 0.000 claims abstract 3
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- YARKMNAWFIMDKV-UHFFFAOYSA-N Epanolol Chemical compound C=1C=CC=C(C#N)C=1OCC(O)CNCCNC(=O)CC1=CC=C(O)C=C1 YARKMNAWFIMDKV-UHFFFAOYSA-N 0.000 claims abstract 3
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- ZPQPDBIHYCBNIG-UHFFFAOYSA-N befunolol Chemical compound CC(C)NCC(O)COC1=CC=CC2=C1OC(C(C)=O)=C2 ZPQPDBIHYCBNIG-UHFFFAOYSA-N 0.000 claims abstract 3
- 229960004374 befunolol Drugs 0.000 claims abstract 3
- 229960004324 betaxolol Drugs 0.000 claims abstract 3
- NWIUTZDMDHAVTP-UHFFFAOYSA-N betaxolol Chemical compound C1=CC(OCC(O)CNC(C)C)=CC=C1CCOCC1CC1 NWIUTZDMDHAVTP-UHFFFAOYSA-N 0.000 claims abstract 3
- 229960003588 bevantolol Drugs 0.000 claims abstract 3
- HXLAFSUPPDYFEO-UHFFFAOYSA-N bevantolol Chemical compound C1=C(OC)C(OC)=CC=C1CCNCC(O)COC1=CC=CC(C)=C1 HXLAFSUPPDYFEO-UHFFFAOYSA-N 0.000 claims abstract 3
- 229960002781 bisoprolol Drugs 0.000 claims abstract 3
- VHYCDWMUTMEGQY-UHFFFAOYSA-N bisoprolol Chemical compound CC(C)NCC(O)COC1=CC=C(COCCOC(C)C)C=C1 VHYCDWMUTMEGQY-UHFFFAOYSA-N 0.000 claims abstract 3
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- NMBNQRJDEPOXCP-UHFFFAOYSA-N butofilolol Chemical compound CCCC(=O)C1=CC(F)=CC=C1OCC(O)CNC(C)(C)C NMBNQRJDEPOXCP-UHFFFAOYSA-N 0.000 claims abstract 3
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- 229960002711 epanolol Drugs 0.000 claims abstract 3
- 229960003745 esmolol Drugs 0.000 claims abstract 3
- AQNDDEOPVVGCPG-UHFFFAOYSA-N esmolol Chemical compound COC(=O)CCC1=CC=C(OCC(O)CNC(C)C)C=C1 AQNDDEOPVVGCPG-UHFFFAOYSA-N 0.000 claims abstract 3
- MPGBPFMOOXKQRX-UHFFFAOYSA-N indenolol Chemical compound CC(C)NCC(O)COC1=CC=CC2=C1C=CC2 MPGBPFMOOXKQRX-UHFFFAOYSA-N 0.000 claims abstract 3
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- 229950005241 landiolol Drugs 0.000 claims abstract 3
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- IXHBTMCLRNMKHZ-LBPRGKRZSA-N levobunolol Chemical compound O=C1CCCC2=C1C=CC=C2OC[C@@H](O)CNC(C)(C)C IXHBTMCLRNMKHZ-LBPRGKRZSA-N 0.000 claims abstract 3
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- KQXKVJAGOJTNJS-HNNXBMFYSA-N penbutolol Chemical compound CC(C)(C)NC[C@H](O)COC1=CC=CC=C1C1CCCC1 KQXKVJAGOJTNJS-HNNXBMFYSA-N 0.000 claims abstract 3
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- MXFWWQICDIZSOA-UHFFFAOYSA-N talinolol Chemical compound C1=CC(OCC(O)CNC(C)(C)C)=CC=C1NC(=O)NC1CCCCC1 MXFWWQICDIZSOA-UHFFFAOYSA-N 0.000 claims abstract 3
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- TWUSDDMONZULSC-HZMBPMFUSA-N (1r,2s)-2-(tert-butylamino)-1-(2,5-dimethoxyphenyl)propan-1-ol Chemical compound COC1=CC=C(OC)C([C@@H](O)[C@H](C)NC(C)(C)C)=C1 TWUSDDMONZULSC-HZMBPMFUSA-N 0.000 claims abstract 2
- 229950009770 butaxamine Drugs 0.000 claims abstract 2
- 239000003937 drug carrier Substances 0.000 claims abstract 2
- UAORFCGRZIGNCI-UHFFFAOYSA-N nifenalol Chemical compound CC(C)NCC(O)C1=CC=C([N+]([O-])=O)C=C1 UAORFCGRZIGNCI-UHFFFAOYSA-N 0.000 claims abstract 2
- 229950000096 nifenalol Drugs 0.000 claims abstract 2
- 239000000296 purinergic P1 receptor antagonist Substances 0.000 claims abstract 2
- TWVUMMQUXMYOOH-UHFFFAOYSA-N tilisolol Chemical compound C1=CC=C2C(=O)N(C)C=C(OCC(O)CNC(C)(C)C)C2=C1 TWVUMMQUXMYOOH-UHFFFAOYSA-N 0.000 claims abstract 2
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- VXNZUUAINFGPBY-UHFFFAOYSA-N 1-Butene Chemical compound CCC=C VXNZUUAINFGPBY-UHFFFAOYSA-N 0.000 claims 3
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- 238000003384 imaging method Methods 0.000 claims 2
- LFTFGCDECFPSQD-NSHDSACASA-N levomoprolol Chemical compound COC1=CC=CC=C1OC[C@@H](O)CNC(C)C LFTFGCDECFPSQD-NSHDSACASA-N 0.000 claims 2
- 229950001994 levomoprolol Drugs 0.000 claims 2
- 230000002107 myocardial effect Effects 0.000 claims 2
- 230000010412 perfusion Effects 0.000 claims 2
- JWHAUXFOSRPERK-UHFFFAOYSA-N propafenone Chemical compound CCCNCC(O)COC1=CC=CC=C1C(=O)CCC1=CC=CC=C1 JWHAUXFOSRPERK-UHFFFAOYSA-N 0.000 claims 2
- 229960000203 propafenone Drugs 0.000 claims 2
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- 239000003071 vasodilator agent Substances 0.000 claims 2
- SGTNSNPWRIOYBX-UHFFFAOYSA-N 2-(3,4-dimethoxyphenyl)-5-{[2-(3,4-dimethoxyphenyl)ethyl](methyl)amino}-2-(propan-2-yl)pentanenitrile Chemical compound C1=C(OC)C(OC)=CC=C1CCN(C)CCCC(C#N)(C(C)C)C1=CC=C(OC)C(OC)=C1 SGTNSNPWRIOYBX-UHFFFAOYSA-N 0.000 claims 1
- DXPOSRCHIDYWHW-UHFFFAOYSA-N Xamoterol Chemical compound C=1C=C(O)C=CC=1OCC(O)CNCCNC(=O)N1CCOCC1 DXPOSRCHIDYWHW-UHFFFAOYSA-N 0.000 claims 1
- 229960001222 carteolol Drugs 0.000 claims 1
- LWAFSWPYPHEXKX-UHFFFAOYSA-N carteolol Chemical compound N1C(=O)CCC2=C1C=CC=C2OCC(O)CNC(C)(C)C LWAFSWPYPHEXKX-UHFFFAOYSA-N 0.000 claims 1
- 238000001990 intravenous administration Methods 0.000 claims 1
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- 238000012800 visualization Methods 0.000 claims 1
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- 101150051188 Adora2a gene Proteins 0.000 abstract 2
Classifications
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
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- 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
- A61K31/13—Amines
- A61K31/135—Amines having aromatic rings, e.g. ketamine, nortriptyline
- A61K31/138—Aryloxyalkylamines, e.g. propranolol, tamoxifen, phenoxybenzamine
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- A—HUMAN NECESSITIES
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- 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
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
- A61K31/52—Purines, e.g. adenine
- A61K31/522—Purines, e.g. adenine having oxo groups directly attached to the heterocyclic ring, e.g. hypoxanthine, guanine, acyclovir
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- A—HUMAN NECESSITIES
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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
- A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
- A61K31/7052—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
- A61K31/706—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom
- A61K31/7064—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines
- A61K31/7076—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines containing purines, e.g. adenosine, adenylic acid
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K49/00—Preparations for testing in vivo
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- A—HUMAN NECESSITIES
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- A61K49/0004—Screening or testing of compounds for diagnosis of disorders, assessment of conditions, e.g. renal clearance, gastric emptying, testing for diabetes, allergy, rheuma, pancreas functions
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- 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
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- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Epidemiology (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Engineering & Computer Science (AREA)
- Molecular Biology (AREA)
- Endocrinology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Biomedical Technology (AREA)
- Gastroenterology & Hepatology (AREA)
- Pathology (AREA)
- Rheumatology (AREA)
- Toxicology (AREA)
- Urology & Nephrology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Organic Chemistry (AREA)
- Diabetes (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
1. Фармацевтическая композиция, содержащая средство, регулирующее частоту сердечных сокращений, по меньшей мере, 10 мкг, по меньшей мере, одного агониста A2A рецепторов и, по меньшей мере, один фармацевтически приемлемый носитель. ! 2. Фармацевтическая композиция по п.1, где средство, регулирующее частоту сердечных сокращений, представляет собой не селективный антагонист аденозина. ! 3. Фармацевтическая композиция по п.1, где средство, регулирующее частоту сердечных сокращений, выбрано из группы, состоящей из кофеина, аминофиллин кофеина, дифиллина, энпрофиллина, пентоксифиллина, теофиллина, блокатора β-адренергических рецепторов и их комбинаций. ! 4. Фармацевтическая композиция по п.3, где блокатор β-адренергических рецепторов выбран из группы, состоящей из ацебутолола, албутерола, амосулалола, аротинолола, атенолола, бефунолола, бетаксолола, бевантолола, бисопролола, бисопролола фумарата, бопиндолола, буциндолола, буфетолола, бунитролола, бутаксамина, бутофилолола, каразолола, картеолола, карведилола, целипролола, клоранолола, дивалпроекса, эпанолола, карведилола, эсмолола, инденолола, ландиолола, лабеталола, левобунолола, левомопролола, лизиноприла, медроксалола, мепиндолола, метипранолола, метопролола, надолола, небиволола, нифеналола, нипрадилола, окспренолола, пенбутолола, пиндолола, пропафенона, пропранолола, салметерола, соталола, талинолола, тертатолола, тилисолола, тимолола, верапамила, ксамотерола, ксибенолола и их комбинаций. ! 5. Фармацевтическая композиция по п.1, где агонист A2A рецепторов выбран из группы, состоящей из регаденозона, биноденозона, CVT-3033 и их комбинаций. ! 6. Фармацевтическая композиция
Claims (23)
1. Фармацевтическая композиция, содержащая средство, регулирующее частоту сердечных сокращений, по меньшей мере, 10 мкг, по меньшей мере, одного агониста A2A рецепторов и, по меньшей мере, один фармацевтически приемлемый носитель.
2. Фармацевтическая композиция по п.1, где средство, регулирующее частоту сердечных сокращений, представляет собой не селективный антагонист аденозина.
3. Фармацевтическая композиция по п.1, где средство, регулирующее частоту сердечных сокращений, выбрано из группы, состоящей из кофеина, аминофиллин кофеина, дифиллина, энпрофиллина, пентоксифиллина, теофиллина, блокатора β-адренергических рецепторов и их комбинаций.
4. Фармацевтическая композиция по п.3, где блокатор β-адренергических рецепторов выбран из группы, состоящей из ацебутолола, албутерола, амосулалола, аротинолола, атенолола, бефунолола, бетаксолола, бевантолола, бисопролола, бисопролола фумарата, бопиндолола, буциндолола, буфетолола, бунитролола, бутаксамина, бутофилолола, каразолола, картеолола, карведилола, целипролола, клоранолола, дивалпроекса, эпанолола, карведилола, эсмолола, инденолола, ландиолола, лабеталола, левобунолола, левомопролола, лизиноприла, медроксалола, мепиндолола, метипранолола, метопролола, надолола, небиволола, нифеналола, нипрадилола, окспренолола, пенбутолола, пиндолола, пропафенона, пропранолола, салметерола, соталола, талинолола, тертатолола, тилисолола, тимолола, верапамила, ксамотерола, ксибенолола и их комбинаций.
5. Фармацевтическая композиция по п.1, где агонист A2A рецепторов выбран из группы, состоящей из регаденозона, биноденозона, CVT-3033 и их комбинаций.
6. Фармацевтическая композиция по п.1, где агонист A2A рецепторов представляет собой регаденозон.
7. Фармацевтическая композиция по п.1, где агонист A2A рецепторов представляет собой регаденозон, а средство, регулирующее частоту сердечных сокращений, выбрано из группы, состоящей из кофеина, аминофиллин кофеина, дифиллина, энпрофиллина, пентоксифиллина, теофиллина, метопролола и пропранолола.
8. Способ визуализации миокарда млекопитающего с помощью мультидетекторной компьютерной томографией при вызванной сосудорасширяющим средством стрессовой перфузии миокарда, включающий введение млекопитающему терапевтически эффективного количества средства, регулирующего частоту сердечных сокращений, и, по меньшей мере, 10 мкг, по меньшей мере, одного агониста A2A рецепторов и визуализацию миокарда млекопитающего.
9. Способ визуализации миокарда млекопитающего мультидетекторной компьютерной томографией при вызванной сосудорасширяющим средством стрессовой перфузии миокарда, включающий введение млекопитающему терапевтически эффективного количества средства, регулирующего частоту сердечных сокращений, и не более чем 1000 мкг, по меньшей мере, одного агониста A2A рецепторов и визуализацию миокарда млекопитающего.
10. Способ по п.8 или 9, где средство, регулирующее частоту сердечных сокращений, вводится млекопитающему перед и одновременно, по меньшей мере, с одним агонистом A2A рецепторов.
11. Способ по п.10, где агонист A2A рецепторов вводится млекопитающему в количестве в диапазоне от приблизительно 10 до приблизительно 600 мкг.
12. Способ по п.8 или 9, где агонист A2A рецепторов вводится менее чем приблизительно за 10 секунд.
13. Способ по п.8 или 9, где агонист A2A рецепторов вводится в количестве более чем приблизительно 10 мкг.
14. Способ по п.8 или 9, где агонист A2A рецепторов вводится в количестве более чем приблизительно 100 мкг.
15. Способ по п.8 или 9, где агонист A2A рецепторов вводится в количестве не более чем 600 мкг.
16. Способ по п.15, где агонист A2A рецепторов вводится в количестве не более чем 500 мкг.
17. Способ по п.8 или 9, где агонист A2A рецепторов вводится в количестве в диапазоне от приблизительно 100 мкг до приблизительно 500 мкг.
18. Способ по п.8 или 9, где агонист A2A рецепторов выбран из группы, состоящей из CVT-3033, регаденозона и их комбинаций.
19. Способ по п.8 или 9, где средство, регулирующее частоту сердечных сокращений, выбрано из группы, состоящей из кофеина, аминофиллин кофеина, дифиллина, энпрофиллина, пентоксифиллина, теофиллина, блокаторов β-адренергических рецепторов и их комбинаций.
20. Способ по п.19, где блокатор β-адренергических рецепторов выбран из группы, состоящей из ацебутолола, албутерола, амосулалола, аротинолола, атенолола, бефунолола, бетаксолола, бевантолола, бисопролола, бисопролола фумарата, бопиндолола, буциндолола, буфетолола, бунитролола, бутаксамина, бутофилолола, каразолола, картеолола, карведилола, целипролола, клоранолола, дивалпроекса, эпанолола, карведилола, эсмолола, инденолола, ландиолола, лабеталола, левобунолола, левомопролола, лизиноприла, медроксалола, мепиндолола, метипранолола, метопролола, надолола, небиволола, нифеналола, нипрадилола, окспренолола, пенбутолола, пиндолола, пропафенона, пропранолола, салметерола, соталола, талинолола, тертатолола, тилисолола, тимолола, верапамила, ксамотерола, ксибенолола и их комбинаций.
21. Способ по п.20, где блокатор β-адренергических рецепторов выбран из метопролола или пропранолола.
22. Способ по любому из п.п.8 или 9, где млекопитающее представляет собой человека.
23. Способ по любому из п.п.8 или 9, где агонист A2A рецепторов вводится в одном внутривенном болюсе.
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-
2009
- 2009-09-29 RU RU2011115815/15A patent/RU2011115815A/ru unknown
- 2009-09-29 US US12/569,643 patent/US20100086483A1/en not_active Abandoned
- 2009-09-29 MX MX2011003168A patent/MX2011003168A/es unknown
- 2009-09-29 CN CN200980138322XA patent/CN102164591A/zh active Pending
- 2009-09-29 JP JP2011529367A patent/JP2012504147A/ja not_active Withdrawn
- 2009-09-29 AU AU2009296235A patent/AU2009296235A1/en not_active Abandoned
- 2009-09-29 EP EP09741075A patent/EP2344145A1/en not_active Withdrawn
- 2009-09-29 CA CA2737077A patent/CA2737077A1/en not_active Abandoned
- 2009-09-29 WO PCT/US2009/058850 patent/WO2010037122A1/en not_active Ceased
- 2009-09-29 BR BRPI0918962A patent/BRPI0918962A2/pt not_active Application Discontinuation
- 2009-09-29 KR KR1020117009103A patent/KR20110063556A/ko not_active Withdrawn
Also Published As
| Publication number | Publication date |
|---|---|
| EP2344145A1 (en) | 2011-07-20 |
| AU2009296235A1 (en) | 2010-04-01 |
| WO2010037122A1 (en) | 2010-04-01 |
| JP2012504147A (ja) | 2012-02-16 |
| CN102164591A (zh) | 2011-08-24 |
| CA2737077A1 (en) | 2010-04-01 |
| KR20110063556A (ko) | 2011-06-10 |
| US20100086483A1 (en) | 2010-04-08 |
| BRPI0918962A2 (pt) | 2015-12-01 |
| MX2011003168A (es) | 2011-05-19 |
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