RU2005133631A - Новый дифенилазетидинон с улучшенными физиологическими свойствами, способы его получения, содержащие эти соединения лекарственные средства и их применение - Google Patents
Новый дифенилазетидинон с улучшенными физиологическими свойствами, способы его получения, содержащие эти соединения лекарственные средства и их применение Download PDFInfo
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- RU2005133631A RU2005133631A RU2005133631/04A RU2005133631A RU2005133631A RU 2005133631 A RU2005133631 A RU 2005133631A RU 2005133631/04 A RU2005133631/04 A RU 2005133631/04A RU 2005133631 A RU2005133631 A RU 2005133631A RU 2005133631 A RU2005133631 A RU 2005133631A
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- agonists
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- compound according
- antagonists
- biologically active
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- 150000001875 compounds Chemical class 0.000 title claims 13
- 239000003814 drug Substances 0.000 title claims 10
- 238000004519 manufacturing process Methods 0.000 title claims 5
- 238000000034 method Methods 0.000 title claims 2
- 230000001766 physiological effect Effects 0.000 title 1
- 239000000556 agonist Substances 0.000 claims 15
- 239000003112 inhibitor Substances 0.000 claims 6
- 239000005557 antagonist Substances 0.000 claims 4
- 229940079593 drug Drugs 0.000 claims 4
- 125000004400 (C1-C12) alkyl group Chemical group 0.000 claims 3
- 125000002777 acetyl group Chemical group [H]C([H])([H])C(*)=O 0.000 claims 3
- 125000003118 aryl group Chemical group 0.000 claims 3
- 125000003236 benzoyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C(*)=O 0.000 claims 3
- 229940088623 biologically active substance Drugs 0.000 claims 3
- HVYWMOMLDIMFJA-DPAQBDIFSA-N cholesterol Chemical compound C1C=C2C[C@@H](O)CC[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@H]([C@H](C)CCCC(C)C)[C@@]1(C)CC2 HVYWMOMLDIMFJA-DPAQBDIFSA-N 0.000 claims 3
- 239000013067 intermediate product Substances 0.000 claims 3
- HSINOMROUCMIEA-FGVHQWLLSA-N (2s,4r)-4-[(3r,5s,6r,7r,8s,9s,10s,13r,14s,17r)-6-ethyl-3,7-dihydroxy-10,13-dimethyl-2,3,4,5,6,7,8,9,11,12,14,15,16,17-tetradecahydro-1h-cyclopenta[a]phenanthren-17-yl]-2-methylpentanoic acid Chemical compound C([C@@]12C)C[C@@H](O)C[C@H]1[C@@H](CC)[C@@H](O)[C@@H]1[C@@H]2CC[C@]2(C)[C@@H]([C@H](C)C[C@H](C)C(O)=O)CC[C@H]21 HSINOMROUCMIEA-FGVHQWLLSA-N 0.000 claims 2
- 229940127470 Lipase Inhibitors Drugs 0.000 claims 2
- 239000013543 active substance Substances 0.000 claims 2
- 239000003613 bile acid Substances 0.000 claims 2
- 239000000122 growth hormone Substances 0.000 claims 2
- 230000037356 lipid metabolism Effects 0.000 claims 2
- QZAYGJVTTNCVMB-UHFFFAOYSA-N serotonin Chemical compound C1=C(O)C=C2C(CCN)=CNC2=C1 QZAYGJVTTNCVMB-UHFFFAOYSA-N 0.000 claims 2
- 102000008645 11-beta-Hydroxysteroid Dehydrogenase Type 1 Human genes 0.000 claims 1
- 108010088011 11-beta-Hydroxysteroid Dehydrogenase Type 1 Proteins 0.000 claims 1
- 102000004146 ATP citrate synthases Human genes 0.000 claims 1
- 108090000662 ATP citrate synthases Proteins 0.000 claims 1
- 102000013585 Bombesin Human genes 0.000 claims 1
- 108010051479 Bombesin Proteins 0.000 claims 1
- 102100033868 Cannabinoid receptor 1 Human genes 0.000 claims 1
- 101710187010 Cannabinoid receptor 1 Proteins 0.000 claims 1
- 108010067722 Dipeptidyl Peptidase 4 Proteins 0.000 claims 1
- 102100025012 Dipeptidyl peptidase 4 Human genes 0.000 claims 1
- KRHYYFGTRYWZRS-UHFFFAOYSA-M Fluoride anion Chemical compound [F-] KRHYYFGTRYWZRS-UHFFFAOYSA-M 0.000 claims 1
- 102000019432 Galanin Human genes 0.000 claims 1
- 101800002068 Galanin Proteins 0.000 claims 1
- DTHNMHAUYICORS-KTKZVXAJSA-N Glucagon-like peptide 1 Chemical class C([C@@H](C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](C)C(=O)N[C@@H](CC=1C2=CC=CC=C2NC=1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCNC(N)=N)C(N)=O)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CCC(N)=O)NC(=O)CNC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC=1C=CC(O)=CC=1)NC(=O)[C@H](CO)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](CC=1C=CC=CC=1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](C)NC(=O)[C@@H](N)CC=1N=CNC=1)[C@@H](C)O)[C@@H](C)O)C(C)C)C1=CC=CC=C1 DTHNMHAUYICORS-KTKZVXAJSA-N 0.000 claims 1
- 102000018997 Growth Hormone Human genes 0.000 claims 1
- 108010051696 Growth Hormone Proteins 0.000 claims 1
- 229940121710 HMGCoA reductase inhibitor Drugs 0.000 claims 1
- 208000031226 Hyperlipidaemia Diseases 0.000 claims 1
- 102000004877 Insulin Human genes 0.000 claims 1
- 108090001061 Insulin Proteins 0.000 claims 1
- 206010022489 Insulin Resistance Diseases 0.000 claims 1
- 108010092277 Leptin Proteins 0.000 claims 1
- 102000016267 Leptin Human genes 0.000 claims 1
- 102000004882 Lipase Human genes 0.000 claims 1
- 108090001060 Lipase Proteins 0.000 claims 1
- 239000004367 Lipase Substances 0.000 claims 1
- 108010013563 Lipoprotein Lipase Proteins 0.000 claims 1
- 102100022119 Lipoprotein lipase Human genes 0.000 claims 1
- 102000004895 Lipoproteins Human genes 0.000 claims 1
- 108090001030 Lipoproteins Proteins 0.000 claims 1
- 229940124757 MC-4 agonist Drugs 0.000 claims 1
- 102000029828 Melanin-concentrating hormone receptor Human genes 0.000 claims 1
- 108010047068 Melanin-concentrating hormone receptor Proteins 0.000 claims 1
- 239000000637 Melanocyte-Stimulating Hormone Substances 0.000 claims 1
- 108010007013 Melanocyte-Stimulating Hormones Proteins 0.000 claims 1
- 102000002512 Orexin Human genes 0.000 claims 1
- 108010016731 PPAR gamma Proteins 0.000 claims 1
- 229940124754 PPAR-alpha/gamma agonist Drugs 0.000 claims 1
- 102000003728 Peroxisome Proliferator-Activated Receptors Human genes 0.000 claims 1
- 108090000029 Peroxisome Proliferator-Activated Receptors Proteins 0.000 claims 1
- 102100038831 Peroxisome proliferator-activated receptor alpha Human genes 0.000 claims 1
- 102100038825 Peroxisome proliferator-activated receptor gamma Human genes 0.000 claims 1
- 102000004257 Potassium Channel Human genes 0.000 claims 1
- 229940100389 Sulfonylurea Drugs 0.000 claims 1
- 108060008682 Tumor Necrosis Factor Proteins 0.000 claims 1
- 102000005630 Urocortins Human genes 0.000 claims 1
- 108010059705 Urocortins Proteins 0.000 claims 1
- 229940121373 acetyl-coa carboxylase inhibitor Drugs 0.000 claims 1
- 239000003392 amylase inhibitor Substances 0.000 claims 1
- 239000000883 anti-obesity agent Substances 0.000 claims 1
- 239000003472 antidiabetic agent Substances 0.000 claims 1
- 229940125708 antidiabetic agent Drugs 0.000 claims 1
- 239000003963 antioxidant agent Substances 0.000 claims 1
- 239000002830 appetite depressant Substances 0.000 claims 1
- 210000000227 basophil cell of anterior lobe of hypophysis Anatomy 0.000 claims 1
- DNDCVAGJPBKION-DOPDSADYSA-N bombesin Chemical compound C([C@@H](C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCSC)C(N)=O)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](CC=1NC2=CC=CC=C2C=1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H]1NC(=O)CC1)C(C)C)C1=CN=CN1 DNDCVAGJPBKION-DOPDSADYSA-N 0.000 claims 1
- OZVBMTJYIDMWIL-AYFBDAFISA-N bromocriptine Chemical compound C1=CC(C=2[C@H](N(C)C[C@@H](C=2)C(=O)N[C@]2(C(=O)N3[C@H](C(N4CCC[C@H]4[C@]3(O)O2)=O)CC(C)C)C(C)C)C2)=C3C2=C(Br)NC3=C1 OZVBMTJYIDMWIL-AYFBDAFISA-N 0.000 claims 1
- 229960002802 bromocriptine Drugs 0.000 claims 1
- 235000012000 cholesterol Nutrition 0.000 claims 1
- 239000003354 cholesterol ester transfer protein inhibitor Substances 0.000 claims 1
- 230000001419 dependent effect Effects 0.000 claims 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 1
- 208000035475 disorder Diseases 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 229940125753 fibrate Drugs 0.000 claims 1
- 239000002471 hydroxymethylglutaryl coenzyme A reductase inhibitor Substances 0.000 claims 1
- 230000002218 hypoglycaemic effect Effects 0.000 claims 1
- 239000004026 insulin derivative Substances 0.000 claims 1
- 229940039781 leptin Drugs 0.000 claims 1
- NRYBAZVQPHGZNS-ZSOCWYAHSA-N leptin Chemical compound O=C([C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CC=1C2=CC=CC=C2NC=1)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](N)CC(C)C)CCSC)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CS)C(O)=O NRYBAZVQPHGZNS-ZSOCWYAHSA-N 0.000 claims 1
- 235000019421 lipase Nutrition 0.000 claims 1
- 239000002697 lyase inhibitor Substances 0.000 claims 1
- 229940126601 medicinal product Drugs 0.000 claims 1
- 239000000203 mixture Substances 0.000 claims 1
- SLZIZIJTGAYEKK-CIJSCKBQSA-N molport-023-220-247 Chemical compound C([C@@H](C(=O)N[C@@H](C)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CC(O)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC=1N=CNC=1)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC=1C=CC=CC=1)C(=O)N[C@@H](CC=1N=CNC=1)C(=O)N[C@@H](CC(O)=O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC=1C=CC(O)=CC=1)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(N)=O)NC(=O)[C@H]1N(CCC1)C(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC=1C=CC(O)=CC=1)NC(=O)CNC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)[C@H](CC=1C2=CC=CC=C2NC=1)NC(=O)CN)[C@@H](C)O)C1=CNC=N1 SLZIZIJTGAYEKK-CIJSCKBQSA-N 0.000 claims 1
- 230000002474 noradrenergic effect Effects 0.000 claims 1
- 108060005714 orexin Proteins 0.000 claims 1
- 108091008725 peroxisome proliferator-activated receptors alpha Proteins 0.000 claims 1
- 229940096701 plain lipid modifying drug hmg coa reductase inhibitors Drugs 0.000 claims 1
- 108020001213 potassium channel Proteins 0.000 claims 1
- 102000004169 proteins and genes Human genes 0.000 claims 1
- 108090000623 proteins and genes Proteins 0.000 claims 1
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- 239000002464 receptor antagonist Substances 0.000 claims 1
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- 150000003839 salts Chemical class 0.000 claims 1
- 229940076279 serotonin Drugs 0.000 claims 1
- 239000000952 serotonin receptor agonist Substances 0.000 claims 1
- 239000003772 serotonin uptake inhibitor Substances 0.000 claims 1
- 230000002295 serotoninergic effect Effects 0.000 claims 1
- 239000004059 squalene synthase inhibitor Substances 0.000 claims 1
- 102000003390 tumor necrosis factor Human genes 0.000 claims 1
- 208000001072 type 2 diabetes mellitus Diseases 0.000 claims 1
- 239000000777 urocortin Substances 0.000 claims 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C233/00—Carboxylic acid amides
- C07C233/01—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
- C07C233/16—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by singly-bound oxygen atoms
- C07C233/17—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by singly-bound oxygen atoms with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by an acyclic carbon atom
- C07C233/18—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by singly-bound oxygen atoms with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by an acyclic carbon atom having the carbon atom of the carboxamide group bound to a hydrogen atom or to a carbon atom of an acyclic saturated carbon skeleton
-
- 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
- A61K31/397—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having four-membered rings, e.g. azetidine
-
- 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
-
- 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
- A61P3/04—Anorexiants; Antiobesity agents
-
- 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
- A61P3/06—Antihyperlipidemics
-
- 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
-
- 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
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D205/00—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom
- C07D205/02—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings
- C07D205/06—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
- C07D205/08—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member with one oxygen atom directly attached in position 2, e.g. beta-lactams
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Diabetes (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Engineering & Computer Science (AREA)
- Pharmacology & Pharmacy (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Obesity (AREA)
- Hematology (AREA)
- Emergency Medicine (AREA)
- Endocrinology (AREA)
- Cardiology (AREA)
- Vascular Medicine (AREA)
- Urology & Nephrology (AREA)
- Heart & Thoracic Surgery (AREA)
- Child & Adolescent Psychology (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
Claims (14)
1. Соединение формулы (I)
а также его фармацевтически приемлемые соли.
2. Лекарственное средство, содержащее соединение по п.1.
3. Лекарственное средство, содержащее соединение по п.1 и по меньшей мере одно другое биологически активное вещество.
4. Лекарственное средство по п.3, отличающееся тем, что в качестве другого биологически активного вещества оно содержит одно или несколько соединений, которые нормализуют липидный обмен.
5. Лекарственное средство по п.3 или 4, отличающееся тем, что в качестве другого биологически активного вещества оно содержит одно или несколько антидиабетических средств, гипогликемических биологически активных веществ, средств против ожирения, подавляющих аппетит средств, ингибиторов HMGCoA-редуктазы, ингибиторов резорбции холестерина, агонистов PPAR-гамма, агонистов PPAR-альфа, агонистов PPAR-альфа/гамма, фибратов, ингибиторов МТР, ингибиторов резорбции желчной кислоты, ингибиторов СЕТР, полимерных адсорберов желчной кислоты, активаторов рецептора LDL, ингибиторов АСАТ, антиоксидантов, ингибиторов липопротеин-липазы, ингибиторов АТФ-цитрат-лиазы, ингибиторов скваленсинтетазы, антагонистов липопротеина(а), ингибиторов липазы, инсулинов, сульфонилмочевин, бигуанидов, меглитинидов, тиазолидиндионов, ингибиторов α-глюкозидазы; биологически активных веществ, воздействующих на АТФ-зависимый калиевый канал бета-клеток; агонистов CART, агонистов NPY, антагонистов каннабиноидного рецептора 1, антагонистов рецептора МСН, агонистов МС4, агонистов орексина, агонистов Н3, агонистов фактора некроза опухоли, агонистов CRF, антагонистов CRF BP, производных GLP-1, агонистов урокортина, агонистов β3, агонистов MSH (меланоцитстимулирующий гормон), агонистов ССК-А, ингибиторов повторного поглощения серотонина, смешанных серотонин- и нор- адренергических соединений, агонистов 5НТ, агонистов бомбезина, антагонистов галанина, гормонов роста, высвобождающих гормон роста соединений, агонистов TRH, 2- или 3-модуляторов разрывающих связь протеинов, агонистов лептина, агонистов DA (бромкриптин, допрексин), ингибиторов липазы/амилазы, ингибиторов 11β-HSD1, ингибиторов АСС, ингибиторов DPP-IV, модуляторов PPAR, модуляторов RXR или агонистов TR-β или амфетаминов.
6. Соединение по п.1 для использования в качестве лекарственного средства в целях лечения нарушений липидного обмена.
7. Способ получения лекарственного средства, содержащего соединение по п.1, отличающийся тем, что действующее начало смешивают с фармацевтически приемлемым носителем и эту смесь переводят в пригодную для введения форму.
8. Применение соединения по п.1 для получения лекарственного средства в целях лечения гиперлипидемии.
9. Применение соединения по п.1 для получения лекарственного средства в целях снижения уровня холестерина в сыворотке.
10. Применение соединения по п.1 для получения лекарственного средства в целях лечения артериосклеротических явлений.
11. Применение соединения по п.1 для получения лекарственного средства в целях лечения резистентности к инсулину.
12. Промежуточный продукт формулы (III)
где R означает ацетил, бензоил, арил, (С1-С12)-алкиларил, (С1-С12)-алкил.
13. Промежуточный продукт формулы (IV)
где R означает ацетил, бензоил, арил, (С1-С12)-алкиларил, (С1-С12)-алкил.
14. Промежуточный продукт формулы (VIII)
где R означает ацетил, бензоил, арил, (С1-С12)-алкиларил, (С1-С12)-алкил.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
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| US20080319218A1 (en) * | 2007-06-22 | 2008-12-25 | Andreas Haubrich | Processes for Making and Using Benzyl Pentahydroxyhexylcarbamoylundecanoate |
| US20080319221A1 (en) * | 2007-06-22 | 2008-12-25 | Bernd Junker | Esters of Pentahydroxyhexylcarbamoyl Alkanoic Acids |
| DE102007029612A1 (de) * | 2007-06-27 | 2009-01-08 | Sanofi-Aventis Deutschland Gmbh | Verfahren zur Herstellung von Pentahydroxyhexylcarbamoylundekan- säurebenzylester |
| EP2025674A1 (de) | 2007-08-15 | 2009-02-18 | sanofi-aventis | Substituierte Tetrahydronaphthaline, Verfahren zu ihrer Herstellung und ihre Verwendung als Arzneimittel |
| DE102007054497B3 (de) * | 2007-11-13 | 2009-07-23 | Sanofi-Aventis Deutschland Gmbh | Neue kristalline Diphenylazetidinonhydrate und Verfahren zu deren Herstellung |
| WO2009100258A1 (en) * | 2008-02-05 | 2009-08-13 | Hollis-Eden Pharmaceuticals, Inc. | Pharmaceutical solid state forms |
| DE102008059772A1 (de) | 2008-12-01 | 2010-06-02 | Sanofi-Aventis Deutschland Gmbh | Verfahren zur Herstellung eines Diphenylazetidinons |
| WO2009112203A1 (de) * | 2008-03-14 | 2009-09-17 | Sanofi-Aventis Deutschland Gmbh | Verfahren zur herstellung eines diphenylazetidinons |
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| US8809325B2 (en) | 2011-03-08 | 2014-08-19 | Sanofi | Benzyl-oxathiazine derivatives substituted with adamantane and noradamantane, medicaments containing said compounds and use thereof |
| EP2683705B1 (de) | 2011-03-08 | 2015-04-22 | Sanofi | Di- und trisubstituierte oxathiazinderivate, verfahren zu deren herstellung, ihre verwendung als medikament sowie sie enthaltendes arzneimittel und deren verwendung |
| US8710050B2 (en) | 2011-03-08 | 2014-04-29 | Sanofi | Di and tri- substituted oxathiazine derivatives, method for the production, method for the production thereof, use thereof as medicine and drug containing said derivatives and use thereof |
| WO2012120050A1 (de) | 2011-03-08 | 2012-09-13 | Sanofi | Neue substituierte phenyl-oxathiazinderivate, verfahren zu deren herstellung, diese verbindungen enthaltende arzneimittel und deren verwendung |
| WO2012120052A1 (de) | 2011-03-08 | 2012-09-13 | Sanofi | Mit carbozyklen oder heterozyklen substituierte oxathiazinderivate, verfahren zu deren herstellung, diese verbindungen enthaltende arzneimittel und deren verwendung |
| EP2683701B1 (de) | 2011-03-08 | 2014-12-24 | Sanofi | Mit benzyl- oder heteromethylengruppen substituierte oxathiazinderivate, verfahren zu deren herstellung, ihre verwendung als medikament sowie sie enthaltendes arzneimittel und deren verwendung |
| EP2683704B1 (de) | 2011-03-08 | 2014-12-17 | Sanofi | Verzweigte oxathiazinderivate, verfahren zu deren herstellung, ihre verwendung als medikament sowie sie enthaltendes arzneimittel und deren verwendung |
| US8871758B2 (en) | 2011-03-08 | 2014-10-28 | Sanofi | Tetrasubstituted oxathiazine derivatives, method for producing them, their use as medicine and drug containing said derivatives and the use thereof |
| EP2683703B1 (de) | 2011-03-08 | 2015-05-27 | Sanofi | Neue substituierte phenyl-oxathiazinderivate, verfahren zu deren herstellung, diese verbindungen enthaltende arzneimittel und deren verwendung |
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