ZA200409582B - Use of CETP inhibitors and optionally HMG Coa reductable inhibitors and/or antihypertensive agents - Google Patents
Use of CETP inhibitors and optionally HMG Coa reductable inhibitors and/or antihypertensive agents Download PDFInfo
- Publication number
- ZA200409582B ZA200409582B ZA200409582A ZA200409582A ZA200409582B ZA 200409582 B ZA200409582 B ZA 200409582B ZA 200409582 A ZA200409582 A ZA 200409582A ZA 200409582 A ZA200409582 A ZA 200409582A ZA 200409582 B ZA200409582 B ZA 200409582B
- Authority
- ZA
- South Africa
- Prior art keywords
- disease
- substituted
- optionally
- optionally mono
- pharmaceutically acceptable
- Prior art date
Links
- 239000003112 inhibitor Substances 0.000 title claims description 19
- 239000003354 cholesterol ester transfer protein inhibitor Substances 0.000 title claims description 14
- 229940030600 antihypertensive agent Drugs 0.000 title claims description 13
- 239000002220 antihypertensive agent Substances 0.000 title claims description 13
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims description 103
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical group [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims description 76
- 229920006395 saturated elastomer Polymers 0.000 claims description 74
- 229910052799 carbon Inorganic materials 0.000 claims description 57
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical compound [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims description 54
- 239000011593 sulfur Substances 0.000 claims description 54
- 229910052717 sulfur Inorganic materials 0.000 claims description 54
- 229910052757 nitrogen Inorganic materials 0.000 claims description 53
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 48
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims description 40
- 229910052760 oxygen Inorganic materials 0.000 claims description 40
- 239000001301 oxygen Substances 0.000 claims description 40
- 125000005842 heteroatom Chemical group 0.000 claims description 39
- 125000005843 halogen group Chemical group 0.000 claims description 38
- 150000003839 salts Chemical class 0.000 claims description 37
- 108010061846 Cholesterol Ester Transfer Proteins Proteins 0.000 claims description 32
- 102000012336 Cholesterol Ester Transfer Proteins Human genes 0.000 claims description 32
- 125000000217 alkyl group Chemical group 0.000 claims description 26
- 125000003545 alkoxy group Chemical group 0.000 claims description 25
- 208000035475 disorder Diseases 0.000 claims description 24
- 201000010099 disease Diseases 0.000 claims description 23
- 208000006011 Stroke Diseases 0.000 claims description 20
- 150000001875 compounds Chemical class 0.000 claims description 19
- 125000001424 substituent group Chemical group 0.000 claims description 18
- 208000019553 vascular disease Diseases 0.000 claims description 17
- 206010012601 diabetes mellitus Diseases 0.000 claims description 16
- 235000019000 fluorine Nutrition 0.000 claims description 16
- 125000001153 fluoro group Chemical group F* 0.000 claims description 16
- 208000029078 coronary artery disease Diseases 0.000 claims description 15
- 241000124008 Mammalia Species 0.000 claims description 14
- 229940121710 HMGCoA reductase inhibitor Drugs 0.000 claims description 13
- 230000003247 decreasing effect Effects 0.000 claims description 13
- 239000002471 hydroxymethylglutaryl coenzyme A reductase inhibitor Substances 0.000 claims description 13
- 208000037803 restenosis Diseases 0.000 claims description 13
- 230000003078 antioxidant effect Effects 0.000 claims description 12
- 239000003963 antioxidant agent Substances 0.000 claims description 11
- 235000006708 antioxidants Nutrition 0.000 claims description 11
- 208000026106 cerebrovascular disease Diseases 0.000 claims description 11
- 208000010877 cognitive disease Diseases 0.000 claims description 11
- 208000019693 Lung disease Diseases 0.000 claims description 10
- 206010028980 Neoplasm Diseases 0.000 claims description 10
- 206010003119 arrhythmia Diseases 0.000 claims description 10
- 201000011510 cancer Diseases 0.000 claims description 10
- NOESYZHRGYRDHS-UHFFFAOYSA-N insulin Chemical compound N1C(=O)C(NC(=O)C(CCC(N)=O)NC(=O)C(CCC(O)=O)NC(=O)C(C(C)C)NC(=O)C(NC(=O)CN)C(C)CC)CSSCC(C(NC(CO)C(=O)NC(CC(C)C)C(=O)NC(CC=2C=CC(O)=CC=2)C(=O)NC(CCC(N)=O)C(=O)NC(CC(C)C)C(=O)NC(CCC(O)=O)C(=O)NC(CC(N)=O)C(=O)NC(CC=2C=CC(O)=CC=2)C(=O)NC(CSSCC(NC(=O)C(C(C)C)NC(=O)C(CC(C)C)NC(=O)C(CC=2C=CC(O)=CC=2)NC(=O)C(CC(C)C)NC(=O)C(C)NC(=O)C(CCC(O)=O)NC(=O)C(C(C)C)NC(=O)C(CC(C)C)NC(=O)C(CC=2NC=NC=2)NC(=O)C(CO)NC(=O)CNC2=O)C(=O)NCC(=O)NC(CCC(O)=O)C(=O)NC(CCCNC(N)=N)C(=O)NCC(=O)NC(CC=3C=CC=CC=3)C(=O)NC(CC=3C=CC=CC=3)C(=O)NC(CC=3C=CC(O)=CC=3)C(=O)NC(C(C)O)C(=O)N3C(CCC3)C(=O)NC(CCCCN)C(=O)NC(C)C(O)=O)C(=O)NC(CC(N)=O)C(O)=O)=O)NC(=O)C(C(C)CC)NC(=O)C(CO)NC(=O)C(C(C)O)NC(=O)C1CSSCC2NC(=O)C(CC(C)C)NC(=O)C(NC(=O)C(CCC(N)=O)NC(=O)C(CC(N)=O)NC(=O)C(NC(=O)C(N)CC=1C=CC=CC=1)C(C)C)CC1=CN=CN1 NOESYZHRGYRDHS-UHFFFAOYSA-N 0.000 claims description 10
- 150000002632 lipids Chemical class 0.000 claims description 10
- 239000008194 pharmaceutical composition Substances 0.000 claims description 10
- 208000023275 Autoimmune disease Diseases 0.000 claims description 9
- 208000011191 Pulmonary vascular disease Diseases 0.000 claims description 9
- 201000001880 Sexual dysfunction Diseases 0.000 claims description 9
- 208000009982 Ventricular Dysfunction Diseases 0.000 claims description 9
- 208000017169 kidney disease Diseases 0.000 claims description 9
- 231100000872 sexual dysfunction Toxicity 0.000 claims description 9
- 208000012908 vascular hemostatic disease Diseases 0.000 claims description 9
- 230000006815 ventricular dysfunction Effects 0.000 claims description 9
- 229910052739 hydrogen Inorganic materials 0.000 claims description 8
- 239000001257 hydrogen Substances 0.000 claims description 8
- 208000027866 inflammatory disease Diseases 0.000 claims description 8
- 230000000302 ischemic effect Effects 0.000 claims description 8
- 201000004409 schistosomiasis Diseases 0.000 claims description 8
- 230000002792 vascular Effects 0.000 claims description 8
- 208000001145 Metabolic Syndrome Diseases 0.000 claims description 7
- 201000000690 abdominal obesity-metabolic syndrome Diseases 0.000 claims description 7
- 230000036737 immune function Effects 0.000 claims description 7
- 229940002612 prodrug Drugs 0.000 claims description 7
- 239000000651 prodrug Substances 0.000 claims description 7
- 101710115418 Apolipoprotein(a) Proteins 0.000 claims description 6
- 102100040214 Apolipoprotein(a) Human genes 0.000 claims description 6
- 108010074051 C-Reactive Protein Proteins 0.000 claims description 6
- 102100032752 C-reactive protein Human genes 0.000 claims description 6
- 239000003146 anticoagulant agent Substances 0.000 claims description 6
- 239000011575 calcium Substances 0.000 claims description 6
- 125000004432 carbon atom Chemical group C* 0.000 claims description 6
- 208000028867 ischemia Diseases 0.000 claims description 6
- 208000011580 syndromic disease Diseases 0.000 claims description 6
- 238000002560 therapeutic procedure Methods 0.000 claims description 6
- 230000002537 thrombolytic effect Effects 0.000 claims description 6
- 208000001072 type 2 diabetes mellitus Diseases 0.000 claims description 6
- 206010012689 Diabetic retinopathy Diseases 0.000 claims description 5
- 102000004877 Insulin Human genes 0.000 claims description 5
- 108090001061 Insulin Proteins 0.000 claims description 5
- 108010062497 VLDL Lipoproteins Proteins 0.000 claims description 5
- 229940125881 cholesteryl ester transfer protein inhibitor Drugs 0.000 claims description 5
- 229940125396 insulin Drugs 0.000 claims description 5
- 230000003907 kidney function Effects 0.000 claims description 5
- 239000002245 particle Substances 0.000 claims description 5
- 201000001320 Atherosclerosis Diseases 0.000 claims description 4
- XUKUURHRXDUEBC-KAYWLYCHSA-N Atorvastatin Chemical compound C=1C=CC=CC=1C1=C(C=2C=CC(F)=CC=2)N(CC[C@@H](O)C[C@@H](O)CC(O)=O)C(C(C)C)=C1C(=O)NC1=CC=CC=C1 XUKUURHRXDUEBC-KAYWLYCHSA-N 0.000 claims description 4
- XUKUURHRXDUEBC-UHFFFAOYSA-N Atorvastatin Natural products C=1C=CC=CC=1C1=C(C=2C=CC(F)=CC=2)N(CCC(O)CC(O)CC(O)=O)C(C(C)C)=C1C(=O)NC1=CC=CC=C1 XUKUURHRXDUEBC-UHFFFAOYSA-N 0.000 claims description 4
- 229940127291 Calcium channel antagonist Drugs 0.000 claims description 4
- 102100034221 Growth-regulated alpha protein Human genes 0.000 claims description 4
- 101001069921 Homo sapiens Growth-regulated alpha protein Proteins 0.000 claims description 4
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 4
- 206010052779 Transplant rejections Diseases 0.000 claims description 4
- 229960005370 atorvastatin Drugs 0.000 claims description 4
- 239000000480 calcium channel blocker Substances 0.000 claims description 4
- 239000003085 diluting agent Substances 0.000 claims description 4
- 239000003937 drug carrier Substances 0.000 claims description 4
- 230000001771 impaired effect Effects 0.000 claims description 4
- 238000004519 manufacturing process Methods 0.000 claims description 4
- 239000000203 mixture Substances 0.000 claims description 4
- 208000010125 myocardial infarction Diseases 0.000 claims description 4
- 230000004770 neurodegeneration Effects 0.000 claims description 4
- 239000003087 receptor blocking agent Substances 0.000 claims description 4
- 230000010410 reperfusion Effects 0.000 claims description 4
- 229960000672 rosuvastatin Drugs 0.000 claims description 4
- BPRHUIZQVSMCRT-VEUZHWNKSA-N rosuvastatin Chemical compound CC(C)C1=NC(N(C)S(C)(=O)=O)=NC(C=2C=CC(F)=CC=2)=C1\C=C\[C@@H](O)C[C@@H](O)CC(O)=O BPRHUIZQVSMCRT-VEUZHWNKSA-N 0.000 claims description 4
- 230000001052 transient effect Effects 0.000 claims description 4
- KKJUPNGICOCCDW-UHFFFAOYSA-N 7-N,N-Dimethylamino-1,2,3,4,5-pentathiocyclooctane Chemical compound CN(C)C1CSSSSSC1 KKJUPNGICOCCDW-UHFFFAOYSA-N 0.000 claims description 3
- 206010001580 Albuminuria Diseases 0.000 claims description 3
- 208000024827 Alzheimer disease Diseases 0.000 claims description 3
- 206010051113 Arterial restenosis Diseases 0.000 claims description 3
- 206010003225 Arteriospasm coronary Diseases 0.000 claims description 3
- 208000037260 Atherosclerotic Plaque Diseases 0.000 claims description 3
- 201000004569 Blindness Diseases 0.000 claims description 3
- OYPRJOBELJOOCE-UHFFFAOYSA-N Calcium Chemical compound [Ca] OYPRJOBELJOOCE-UHFFFAOYSA-N 0.000 claims description 3
- 208000003890 Coronary Vasospasm Diseases 0.000 claims description 3
- 206010012289 Dementia Diseases 0.000 claims description 3
- 208000002249 Diabetes Complications Diseases 0.000 claims description 3
- 208000007342 Diabetic Nephropathies Diseases 0.000 claims description 3
- 208000032781 Diabetic cardiomyopathy Diseases 0.000 claims description 3
- 206010070901 Diabetic dyslipidaemia Diseases 0.000 claims description 3
- 206010051153 Diabetic gastroparesis Diseases 0.000 claims description 3
- 206010013971 Dyspnoea exertional Diseases 0.000 claims description 3
- 102000001554 Hemoglobins Human genes 0.000 claims description 3
- 108010054147 Hemoglobins Proteins 0.000 claims description 3
- 208000016988 Hemorrhagic Stroke Diseases 0.000 claims description 3
- 206010061216 Infarction Diseases 0.000 claims description 3
- 206010022489 Insulin Resistance Diseases 0.000 claims description 3
- 206010048858 Ischaemic cardiomyopathy Diseases 0.000 claims description 3
- 208000032382 Ischaemic stroke Diseases 0.000 claims description 3
- 208000010415 Low Vision Diseases 0.000 claims description 3
- 206010054805 Macroangiopathy Diseases 0.000 claims description 3
- 208000008457 Neurologic Manifestations Diseases 0.000 claims description 3
- 208000001647 Renal Insufficiency Diseases 0.000 claims description 3
- 206010070834 Sensitisation Diseases 0.000 claims description 3
- 208000005475 Vascular calcification Diseases 0.000 claims description 3
- 206010000891 acute myocardial infarction Diseases 0.000 claims description 3
- 238000002266 amputation Methods 0.000 claims description 3
- 229910052791 calcium Inorganic materials 0.000 claims description 3
- 230000002490 cerebral effect Effects 0.000 claims description 3
- 201000011634 coronary artery vasospasm Diseases 0.000 claims description 3
- 210000004351 coronary vessel Anatomy 0.000 claims description 3
- 230000002950 deficient Effects 0.000 claims description 3
- 230000003111 delayed effect Effects 0.000 claims description 3
- 208000033679 diabetic kidney disease Diseases 0.000 claims description 3
- 239000003814 drug Substances 0.000 claims description 3
- 208000020658 intracerebral hemorrhage Diseases 0.000 claims description 3
- 201000006370 kidney failure Diseases 0.000 claims description 3
- 230000003908 liver function Effects 0.000 claims description 3
- 208000018769 loss of vision Diseases 0.000 claims description 3
- 231100000864 loss of vision Toxicity 0.000 claims description 3
- 206010062198 microangiopathy Diseases 0.000 claims description 3
- 210000004165 myocardium Anatomy 0.000 claims description 3
- 230000007830 nerve conduction Effects 0.000 claims description 3
- 230000001537 neural effect Effects 0.000 claims description 3
- 230000007971 neurological deficit Effects 0.000 claims description 3
- 230000007823 neuropathy Effects 0.000 claims description 3
- 108010071584 oxidized low density lipoprotein Proteins 0.000 claims description 3
- 230000009257 reactivity Effects 0.000 claims description 3
- 238000011084 recovery Methods 0.000 claims description 3
- 230000008313 sensitization Effects 0.000 claims description 3
- 108091008012 small dense LDL Proteins 0.000 claims description 3
- 208000024891 symptom Diseases 0.000 claims description 3
- 230000024883 vasodilation Effects 0.000 claims description 3
- 230000009278 visceral effect Effects 0.000 claims description 3
- 230000004393 visual impairment Effects 0.000 claims description 3
- FXAAOALUHHXBSO-ILDUYXDCSA-N (3,3,5-trimethylcyclohexyl) (2s)-5-oxopyrrolidine-2-carboxylate Chemical compound C1C(C)(C)CC(C)CC1OC(=O)[C@H]1NC(=O)CC1 FXAAOALUHHXBSO-ILDUYXDCSA-N 0.000 claims description 2
- ZGGHKIMDNBDHJB-NRFPMOEYSA-M (3R,5S)-fluvastatin sodium Chemical compound [Na+].C12=CC=CC=C2N(C(C)C)C(\C=C\[C@@H](O)C[C@@H](O)CC([O-])=O)=C1C1=CC=C(F)C=C1 ZGGHKIMDNBDHJB-NRFPMOEYSA-M 0.000 claims description 2
- VDSBXXDKCUBMQC-HNGSOEQISA-N (4r,6s)-6-[(e)-2-[2-(4-fluoro-3-methylphenyl)-4,4,6,6-tetramethylcyclohexen-1-yl]ethenyl]-4-hydroxyoxan-2-one Chemical compound C1=C(F)C(C)=CC(C=2CC(C)(C)CC(C)(C)C=2\C=C\[C@H]2OC(=O)C[C@H](O)C2)=C1 VDSBXXDKCUBMQC-HNGSOEQISA-N 0.000 claims description 2
- 239000005541 ACE inhibitor Substances 0.000 claims description 2
- 102100021943 C-C motif chemokine 2 Human genes 0.000 claims description 2
- 101710155857 C-C motif chemokine 2 Proteins 0.000 claims description 2
- 102100032367 C-C motif chemokine 5 Human genes 0.000 claims description 2
- 102000001902 CC Chemokines Human genes 0.000 claims description 2
- 108010040471 CC Chemokines Proteins 0.000 claims description 2
- 108050006947 CXC Chemokine Proteins 0.000 claims description 2
- 102000019388 CXC chemokine Human genes 0.000 claims description 2
- 108010082548 Chemokine CCL11 Proteins 0.000 claims description 2
- 108010055166 Chemokine CCL5 Proteins 0.000 claims description 2
- 208000032131 Diabetic Neuropathies Diseases 0.000 claims description 2
- 102100023688 Eotaxin Human genes 0.000 claims description 2
- LJIZUXQINHXGAO-ITWZMISCSA-N HR 780 Chemical compound C(\[C@H]1OC(=O)C[C@H](O)C1)=C/C=1C(C(C)C)=NC(C=2C=CC=CC=2)=CC=1C1=CC=C(F)C=C1 LJIZUXQINHXGAO-ITWZMISCSA-N 0.000 claims description 2
- 102000015696 Interleukins Human genes 0.000 claims description 2
- 108010063738 Interleukins Proteins 0.000 claims description 2
- 101710151805 Mitochondrial intermediate peptidase 1 Proteins 0.000 claims description 2
- PCZOHLXUXFIOCF-UHFFFAOYSA-N Monacolin X Natural products C12C(OC(=O)C(C)CC)CC(C)C=C2C=CC(C)C1CCC1CC(O)CC(=O)O1 PCZOHLXUXFIOCF-UHFFFAOYSA-N 0.000 claims description 2
- TUZYXOIXSAXUGO-UHFFFAOYSA-N Pravastatin Natural products C1=CC(C)C(CCC(O)CC(O)CC(O)=O)C2C(OC(=O)C(C)CC)CC(O)C=C21 TUZYXOIXSAXUGO-UHFFFAOYSA-N 0.000 claims description 2
- 108010080283 Pre-beta High-Density Lipoproteins Proteins 0.000 claims description 2
- RYMZZMVNJRMUDD-UHFFFAOYSA-N SJ000286063 Natural products C12C(OC(=O)C(C)(C)CC)CC(C)C=C2C=CC(C)C1CCC1CC(O)CC(=O)O1 RYMZZMVNJRMUDD-UHFFFAOYSA-N 0.000 claims description 2
- AJLFOPYRIVGYMJ-UHFFFAOYSA-N SJ000287055 Natural products C12C(OC(=O)C(C)CC)CCC=C2C=CC(C)C1CCC1CC(O)CC(=O)O1 AJLFOPYRIVGYMJ-UHFFFAOYSA-N 0.000 claims description 2
- 108060008682 Tumor Necrosis Factor Proteins 0.000 claims description 2
- 102000000852 Tumor Necrosis Factor-alpha Human genes 0.000 claims description 2
- 125000002777 acetyl group Chemical group [H]C([H])([H])C(*)=O 0.000 claims description 2
- 102000004305 alpha Adrenergic Receptors Human genes 0.000 claims description 2
- 108090000861 alpha Adrenergic Receptors Proteins 0.000 claims description 2
- 229960000528 amlodipine Drugs 0.000 claims description 2
- HTIQEAQVCYTUBX-UHFFFAOYSA-N amlodipine Chemical compound CCOC(=O)C1=C(COCCN)NC(C)=C(C(=O)OC)C1C1=CC=CC=C1Cl HTIQEAQVCYTUBX-UHFFFAOYSA-N 0.000 claims description 2
- 229940044094 angiotensin-converting-enzyme inhibitor Drugs 0.000 claims description 2
- 239000005557 antagonist Substances 0.000 claims description 2
- 229950005357 bervastatin Drugs 0.000 claims description 2
- 102000012740 beta Adrenergic Receptors Human genes 0.000 claims description 2
- 108010079452 beta Adrenergic Receptors Proteins 0.000 claims description 2
- 229960005110 cerivastatin Drugs 0.000 claims description 2
- SEERZIQQUAZTOL-ANMDKAQQSA-N cerivastatin Chemical compound COCC1=C(C(C)C)N=C(C(C)C)C(\C=C\[C@@H](O)C[C@@H](O)CC(O)=O)=C1C1=CC=C(F)C=C1 SEERZIQQUAZTOL-ANMDKAQQSA-N 0.000 claims description 2
- GPUADMRJQVPIAS-QCVDVZFFSA-M cerivastatin sodium Chemical compound [Na+].COCC1=C(C(C)C)N=C(C(C)C)C(\C=C\[C@@H](O)C[C@@H](O)CC([O-])=O)=C1C1=CC=C(F)C=C1 GPUADMRJQVPIAS-QCVDVZFFSA-M 0.000 claims description 2
- 229950002753 crilvastatin Drugs 0.000 claims description 2
- 229950003040 dalvastatin Drugs 0.000 claims description 2
- 239000002934 diuretic Substances 0.000 claims description 2
- 230000001882 diuretic effect Effects 0.000 claims description 2
- ZADJRRFMOOACHL-WQICJITCSA-N ethyl (e,3s,5r)-7-[4-(4-fluorophenyl)spiro[chromene-2,1'-cyclopentane]-3-yl]-3,5-dihydroxyhept-6-enoate Chemical compound C12=CC=CC=C2OC2(CCCC2)C(/C=C/[C@H](O)C[C@H](O)CC(=O)OCC)=C1C1=CC=C(F)C=C1 ZADJRRFMOOACHL-WQICJITCSA-N 0.000 claims description 2
- 229960003765 fluvastatin Drugs 0.000 claims description 2
- 125000002485 formyl group Chemical group [H]C(*)=O 0.000 claims description 2
- 229950000806 glenvastatin Drugs 0.000 claims description 2
- 108010077119 high density lipoprotein-1 Proteins 0.000 claims description 2
- 208000026278 immune system disease Diseases 0.000 claims description 2
- 229940047122 interleukins Drugs 0.000 claims description 2
- 229960004844 lovastatin Drugs 0.000 claims description 2
- PCZOHLXUXFIOCF-BXMDZJJMSA-N lovastatin Chemical group C([C@H]1[C@@H](C)C=CC2=C[C@H](C)C[C@@H]([C@H]12)OC(=O)[C@@H](C)CC)C[C@@H]1C[C@@H](O)CC(=O)O1 PCZOHLXUXFIOCF-BXMDZJJMSA-N 0.000 claims description 2
- QLJODMDSTUBWDW-UHFFFAOYSA-N lovastatin hydroxy acid Natural products C1=CC(C)C(CCC(O)CC(O)CC(O)=O)C2C(OC(=O)C(C)CC)CC(C)C=C21 QLJODMDSTUBWDW-UHFFFAOYSA-N 0.000 claims description 2
- 229950009116 mevastatin Drugs 0.000 claims description 2
- AJLFOPYRIVGYMJ-INTXDZFKSA-N mevastatin Chemical compound C([C@H]1[C@@H](C)C=CC2=CCC[C@@H]([C@H]12)OC(=O)[C@@H](C)CC)C[C@@H]1C[C@@H](O)CC(=O)O1 AJLFOPYRIVGYMJ-INTXDZFKSA-N 0.000 claims description 2
- BOZILQFLQYBIIY-UHFFFAOYSA-N mevastatin hydroxy acid Natural products C1=CC(C)C(CCC(O)CC(O)CC(O)=O)C2C(OC(=O)C(C)CC)CCC=C21 BOZILQFLQYBIIY-UHFFFAOYSA-N 0.000 claims description 2
- 210000000056 organ Anatomy 0.000 claims description 2
- 229960002797 pitavastatin Drugs 0.000 claims description 2
- VGYFMXBACGZSIL-MCBHFWOFSA-N pitavastatin Chemical compound OC(=O)C[C@H](O)C[C@H](O)\C=C\C1=C(C2CC2)N=C2C=CC=CC2=C1C1=CC=C(F)C=C1 VGYFMXBACGZSIL-MCBHFWOFSA-N 0.000 claims description 2
- 229960002965 pravastatin Drugs 0.000 claims description 2
- TUZYXOIXSAXUGO-PZAWKZKUSA-N pravastatin Chemical compound C1=C[C@H](C)[C@H](CC[C@@H](O)C[C@@H](O)CC(O)=O)[C@H]2[C@@H](OC(=O)[C@@H](C)CC)C[C@H](O)C=C21 TUZYXOIXSAXUGO-PZAWKZKUSA-N 0.000 claims description 2
- 230000009919 sequestration Effects 0.000 claims description 2
- 229960002855 simvastatin Drugs 0.000 claims description 2
- RYMZZMVNJRMUDD-HGQWONQESA-N simvastatin Chemical compound C([C@H]1[C@@H](C)C=CC2=C[C@H](C)C[C@@H]([C@H]12)OC(=O)C(C)(C)CC)C[C@@H]1C[C@@H](O)CC(=O)O1 RYMZZMVNJRMUDD-HGQWONQESA-N 0.000 claims description 2
- 239000007787 solid Substances 0.000 claims description 2
- 239000003053 toxin Substances 0.000 claims description 2
- 231100000765 toxin Toxicity 0.000 claims description 2
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 2
- 230000009897 systematic effect Effects 0.000 claims 2
- 230000001154 acute effect Effects 0.000 claims 1
- 125000004435 hydrogen atom Chemical class [H]* 0.000 claims 1
- 125000004356 hydroxy functional group Chemical group O* 0.000 description 36
- 238000000034 method Methods 0.000 description 24
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 description 22
- 125000004043 oxo group Chemical group O=* 0.000 description 22
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 description 21
- 125000003282 alkyl amino group Chemical group 0.000 description 20
- 125000004453 alkoxycarbonyl group Chemical group 0.000 description 19
- 125000004093 cyano group Chemical group *C#N 0.000 description 19
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 description 18
- -1 cholesteryl ester Chemical class 0.000 description 15
- 125000004414 alkyl thio group Chemical group 0.000 description 13
- 206010020772 Hypertension Diseases 0.000 description 12
- 108010010234 HDL Lipoproteins Proteins 0.000 description 10
- 102000015779 HDL Lipoproteins Human genes 0.000 description 10
- 125000003342 alkenyl group Chemical group 0.000 description 10
- 208000018262 Peripheral vascular disease Diseases 0.000 description 9
- 125000002619 bicyclic group Chemical group 0.000 description 8
- 230000009885 systemic effect Effects 0.000 description 7
- 208000005189 Embolism Diseases 0.000 description 6
- 108010007622 LDL Lipoproteins Proteins 0.000 description 6
- 102000007330 LDL Lipoproteins Human genes 0.000 description 6
- 239000013543 active substance Substances 0.000 description 6
- 208000032928 Dyslipidaemia Diseases 0.000 description 5
- 206010019280 Heart failures Diseases 0.000 description 5
- 208000017170 Lipid metabolism disease Diseases 0.000 description 5
- 239000003613 bile acid Substances 0.000 description 5
- 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 description 5
- 230000000694 effects Effects 0.000 description 5
- 150000002148 esters Chemical class 0.000 description 5
- 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 description 4
- 229910014585 C2-Ce Inorganic materials 0.000 description 4
- 208000024172 Cardiovascular disease Diseases 0.000 description 4
- 208000008589 Obesity Diseases 0.000 description 4
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 description 4
- 235000020824 obesity Nutrition 0.000 description 4
- 206010002383 Angina Pectoris Diseases 0.000 description 3
- 108010023302 HDL Cholesterol Proteins 0.000 description 3
- 102000004895 Lipoproteins Human genes 0.000 description 3
- 108090001030 Lipoproteins Proteins 0.000 description 3
- 230000002596 correlated effect Effects 0.000 description 3
- 230000002526 effect on cardiovascular system Effects 0.000 description 3
- 150000002431 hydrogen Chemical class 0.000 description 3
- 230000002265 prevention Effects 0.000 description 3
- 230000009467 reduction Effects 0.000 description 3
- 102000006410 Apoproteins Human genes 0.000 description 2
- 108010083590 Apoproteins Proteins 0.000 description 2
- 102000016289 Cell Adhesion Molecules Human genes 0.000 description 2
- 108010067225 Cell Adhesion Molecules Proteins 0.000 description 2
- 206010008479 Chest Pain Diseases 0.000 description 2
- 206010012655 Diabetic complications Diseases 0.000 description 2
- 206010012758 Diastolic hypertension Diseases 0.000 description 2
- 201000010046 Dilated cardiomyopathy Diseases 0.000 description 2
- 108010028554 LDL Cholesterol Proteins 0.000 description 2
- 238000008214 LDL Cholesterol Methods 0.000 description 2
- 102100031545 Microsomal triglyceride transfer protein large subunit Human genes 0.000 description 2
- 208000010378 Pulmonary Embolism Diseases 0.000 description 2
- 229930182558 Sterol Natural products 0.000 description 2
- 230000006907 apoptotic process Effects 0.000 description 2
- 230000007211 cardiovascular event Effects 0.000 description 2
- 235000012000 cholesterol Nutrition 0.000 description 2
- 230000034994 death Effects 0.000 description 2
- 231100000517 death Toxicity 0.000 description 2
- 206010020718 hyperplasia Diseases 0.000 description 2
- 208000002551 irritable bowel syndrome Diseases 0.000 description 2
- 108010038232 microsomal triglyceride transfer protein Proteins 0.000 description 2
- 150000003904 phospholipids Chemical class 0.000 description 2
- 238000001556 precipitation Methods 0.000 description 2
- 210000002966 serum Anatomy 0.000 description 2
- 150000003432 sterols Chemical class 0.000 description 2
- 235000003702 sterols Nutrition 0.000 description 2
- 125000002813 thiocarbonyl group Chemical group *C(*)=S 0.000 description 2
- UFTFJSFQGQCHQW-UHFFFAOYSA-N triformin Chemical compound O=COCC(OC=O)COC=O UFTFJSFQGQCHQW-UHFFFAOYSA-N 0.000 description 2
- 230000002861 ventricular Effects 0.000 description 2
- NWUYHJFMYQTDRP-UHFFFAOYSA-N 1,2-bis(ethenyl)benzene;1-ethenyl-2-ethylbenzene;styrene Chemical compound C=CC1=CC=CC=C1.CCC1=CC=CC=C1C=C.C=CC1=CC=CC=C1C=C NWUYHJFMYQTDRP-UHFFFAOYSA-N 0.000 description 1
- CQSGWFMVGDLSSR-UHFFFAOYSA-N 2-(trifluoromethyl)-3,4-dihydro-2h-quinoline-1-carboxylic acid Chemical compound C1=CC=C2N(C(=O)O)C(C(F)(F)F)CCC2=C1 CQSGWFMVGDLSSR-UHFFFAOYSA-N 0.000 description 1
- 108010071619 Apolipoproteins Proteins 0.000 description 1
- 102000007592 Apolipoproteins Human genes 0.000 description 1
- 206010003130 Arrhythmia supraventricular Diseases 0.000 description 1
- 206010060965 Arterial stenosis Diseases 0.000 description 1
- 206010003210 Arteriosclerosis Diseases 0.000 description 1
- 102000006996 Aryldialkylphosphatase Human genes 0.000 description 1
- 108010008184 Aryldialkylphosphatase Proteins 0.000 description 1
- 206010003658 Atrial Fibrillation Diseases 0.000 description 1
- 206010003662 Atrial flutter Diseases 0.000 description 1
- 206010007559 Cardiac failure congestive Diseases 0.000 description 1
- 208000031229 Cardiomyopathies Diseases 0.000 description 1
- 206010008190 Cerebrovascular accident Diseases 0.000 description 1
- 102000019034 Chemokines Human genes 0.000 description 1
- 108010012236 Chemokines Proteins 0.000 description 1
- 229940122502 Cholesterol absorption inhibitor Drugs 0.000 description 1
- 229940123239 Cholesterol synthesis inhibitor Drugs 0.000 description 1
- 108010004103 Chylomicrons Proteins 0.000 description 1
- 206010056370 Congestive cardiomyopathy Diseases 0.000 description 1
- 208000011231 Crohn disease Diseases 0.000 description 1
- 206010051055 Deep vein thrombosis Diseases 0.000 description 1
- 206010052337 Diastolic dysfunction Diseases 0.000 description 1
- 206010014561 Emphysema Diseases 0.000 description 1
- 208000037487 Endotoxemia Diseases 0.000 description 1
- 208000010228 Erectile Dysfunction Diseases 0.000 description 1
- 206010057671 Female sexual dysfunction Diseases 0.000 description 1
- WQZGKKKJIJFFOK-GASJEMHNSA-N Glucose Natural products OC[C@H]1OC(O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-GASJEMHNSA-N 0.000 description 1
- 208000002705 Glucose Intolerance Diseases 0.000 description 1
- 102000003886 Glycoproteins Human genes 0.000 description 1
- 108090000288 Glycoproteins Proteins 0.000 description 1
- 201000005569 Gout Diseases 0.000 description 1
- 241000282412 Homo Species 0.000 description 1
- 208000023105 Huntington disease Diseases 0.000 description 1
- 102000004286 Hydroxymethylglutaryl CoA Reductases Human genes 0.000 description 1
- 108090000895 Hydroxymethylglutaryl CoA Reductases Proteins 0.000 description 1
- 208000000563 Hyperlipoproteinemia Type II Diseases 0.000 description 1
- 206010021143 Hypoxia Diseases 0.000 description 1
- 208000031773 Insulin resistance syndrome Diseases 0.000 description 1
- 102000000589 Interleukin-1 Human genes 0.000 description 1
- 108010002352 Interleukin-1 Proteins 0.000 description 1
- 102000004889 Interleukin-6 Human genes 0.000 description 1
- 108090001005 Interleukin-6 Proteins 0.000 description 1
- 102000004890 Interleukin-8 Human genes 0.000 description 1
- 108090001007 Interleukin-8 Proteins 0.000 description 1
- 206010022562 Intermittent claudication Diseases 0.000 description 1
- 102100024640 Low-density lipoprotein receptor Human genes 0.000 description 1
- 206010057672 Male sexual dysfunction Diseases 0.000 description 1
- 241001465754 Metazoa Species 0.000 description 1
- PVNIIMVLHYAWGP-UHFFFAOYSA-N Niacin Chemical compound OC(=O)C1=CC=CN=C1 PVNIIMVLHYAWGP-UHFFFAOYSA-N 0.000 description 1
- 208000011623 Obstructive Lung disease Diseases 0.000 description 1
- 206010033645 Pancreatitis Diseases 0.000 description 1
- 102000003728 Peroxisome Proliferator-Activated Receptors Human genes 0.000 description 1
- 108090000029 Peroxisome Proliferator-Activated Receptors Proteins 0.000 description 1
- 108010022233 Plasminogen Activator Inhibitor 1 Proteins 0.000 description 1
- 102100039418 Plasminogen activator inhibitor 1 Human genes 0.000 description 1
- 206010062237 Renal impairment Diseases 0.000 description 1
- 208000027032 Renal vascular disease Diseases 0.000 description 1
- 208000017442 Retinal disease Diseases 0.000 description 1
- 206010038923 Retinopathy Diseases 0.000 description 1
- 206010042434 Sudden death Diseases 0.000 description 1
- 206010042600 Supraventricular arrhythmias Diseases 0.000 description 1
- 206010071436 Systolic dysfunction Diseases 0.000 description 1
- 206010042957 Systolic hypertension Diseases 0.000 description 1
- 208000007536 Thrombosis Diseases 0.000 description 1
- 208000032109 Transient ischaemic attack Diseases 0.000 description 1
- 206010045261 Type IIa hyperlipidaemia Diseases 0.000 description 1
- 208000007814 Unstable Angina Diseases 0.000 description 1
- 206010046996 Varicose vein Diseases 0.000 description 1
- 206010047115 Vasculitis Diseases 0.000 description 1
- 206010047249 Venous thrombosis Diseases 0.000 description 1
- GAZVSNAEUUUDEK-JDSLSITLSA-N [(1r,3r,4s)-4,7,7-trimethyl-3-bicyclo[2.2.1]heptanyl] 2-hydroxybenzoate Chemical compound O([C@H]1[C@@]2(C)CC[C@H](C1)C2(C)C)C(=O)C1=CC=CC=C1O GAZVSNAEUUUDEK-JDSLSITLSA-N 0.000 description 1
- 230000002159 abnormal effect Effects 0.000 description 1
- 239000012190 activator Substances 0.000 description 1
- 230000032683 aging Effects 0.000 description 1
- 125000004390 alkyl sulfonyl group Chemical group 0.000 description 1
- 230000004075 alteration Effects 0.000 description 1
- 230000003941 amyloidogenesis Effects 0.000 description 1
- 206010002022 amyloidosis Diseases 0.000 description 1
- 230000002429 anti-coagulating effect Effects 0.000 description 1
- 230000003110 anti-inflammatory effect Effects 0.000 description 1
- 230000002785 anti-thrombosis Effects 0.000 description 1
- 201000006800 aortic valve disease 1 Diseases 0.000 description 1
- 230000037007 arousal Effects 0.000 description 1
- 230000006793 arrhythmia Effects 0.000 description 1
- 208000011775 arteriosclerosis disease Diseases 0.000 description 1
- 210000001367 artery Anatomy 0.000 description 1
- 208000006673 asthma Diseases 0.000 description 1
- 230000003143 atherosclerotic effect Effects 0.000 description 1
- 229920000080 bile acid sequestrant Polymers 0.000 description 1
- 230000010261 cell growth Effects 0.000 description 1
- 238000002512 chemotherapy Methods 0.000 description 1
- 201000001883 cholelithiasis Diseases 0.000 description 1
- 230000001684 chronic effect Effects 0.000 description 1
- 208000024980 claudication Diseases 0.000 description 1
- 206010009887 colitis Diseases 0.000 description 1
- 230000004154 complement system Effects 0.000 description 1
- 239000000470 constituent Substances 0.000 description 1
- 230000001276 controlling effect Effects 0.000 description 1
- 230000007812 deficiency Effects 0.000 description 1
- 230000001419 dependent effect Effects 0.000 description 1
- 230000018109 developmental process Effects 0.000 description 1
- 230000001904 diabetogenic effect Effects 0.000 description 1
- 238000000502 dialysis Methods 0.000 description 1
- 235000001434 dietary modification Nutrition 0.000 description 1
- 201000011304 dilated cardiomyopathy 1A Diseases 0.000 description 1
- 238000002651 drug therapy Methods 0.000 description 1
- 230000004064 dysfunction Effects 0.000 description 1
- KAQKFAOMNZTLHT-VVUHWYTRSA-N epoprostenol Chemical compound O1C(=CCCCC(O)=O)C[C@@H]2[C@@H](/C=C/[C@@H](O)CCCCC)[C@H](O)C[C@@H]21 KAQKFAOMNZTLHT-VVUHWYTRSA-N 0.000 description 1
- FIBLYQZJDNLKSS-UHFFFAOYSA-N ethyl 2-(trifluoromethyl)-3,4-dihydro-2h-quinoline-1-carboxylate Chemical compound C1=CC=C2N(C(=O)OCC)C(C(F)(F)F)CCC2=C1 FIBLYQZJDNLKSS-UHFFFAOYSA-N 0.000 description 1
- 125000004494 ethyl ester group Chemical group 0.000 description 1
- 230000029142 excretion Effects 0.000 description 1
- 201000001386 familial hypercholesterolemia Diseases 0.000 description 1
- 229940125753 fibrate Drugs 0.000 description 1
- 230000006870 function Effects 0.000 description 1
- 208000001130 gallstones Diseases 0.000 description 1
- 239000008103 glucose Substances 0.000 description 1
- 210000002216 heart Anatomy 0.000 description 1
- 210000003709 heart valve Anatomy 0.000 description 1
- 208000006575 hypertriglyceridemia Diseases 0.000 description 1
- 230000001146 hypoxic effect Effects 0.000 description 1
- 201000001881 impotence Diseases 0.000 description 1
- 230000006872 improvement Effects 0.000 description 1
- 230000001939 inductive effect Effects 0.000 description 1
- 230000002757 inflammatory effect Effects 0.000 description 1
- 239000003456 ion exchange resin Substances 0.000 description 1
- 229920003303 ion-exchange polymer Polymers 0.000 description 1
- 208000023569 ischemic bowel disease Diseases 0.000 description 1
- 201000010901 lateral sclerosis Diseases 0.000 description 1
- 230000003902 lesion Effects 0.000 description 1
- 210000004185 liver Anatomy 0.000 description 1
- 206010025135 lupus erythematosus Diseases 0.000 description 1
- 230000004060 metabolic process Effects 0.000 description 1
- 208000005264 motor neuron disease Diseases 0.000 description 1
- 201000006417 multiple sclerosis Diseases 0.000 description 1
- 208000031225 myocardial ischemia Diseases 0.000 description 1
- 208000015122 neurodegenerative disease Diseases 0.000 description 1
- 201000001119 neuropathy Diseases 0.000 description 1
- 229960003512 nicotinic acid Drugs 0.000 description 1
- 235000001968 nicotinic acid Nutrition 0.000 description 1
- 239000011664 nicotinic acid Substances 0.000 description 1
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 description 1
- 201000008482 osteoarthritis Diseases 0.000 description 1
- 239000007800 oxidant agent Substances 0.000 description 1
- 230000036542 oxidative stress Effects 0.000 description 1
- 230000036284 oxygen consumption Effects 0.000 description 1
- 230000002093 peripheral effect Effects 0.000 description 1
- 208000033808 peripheral neuropathy Diseases 0.000 description 1
- 229940096701 plain lipid modifying drug hmg coa reductase inhibitors Drugs 0.000 description 1
- 230000036470 plasma concentration Effects 0.000 description 1
- 231100000857 poor renal function Toxicity 0.000 description 1
- 230000000291 postprandial effect Effects 0.000 description 1
- 201000009104 prediabetes syndrome Diseases 0.000 description 1
- 230000000207 pro-atherogenic effect Effects 0.000 description 1
- LVRKSPMHHHUSIE-UHFFFAOYSA-N propan-2-yl 4-[[3,5-bis(trifluoromethyl)phenyl]methyl-methoxycarbonylamino]-6-chloro-2-cyclopropyl-3,4-dihydro-2h-quinoline-1-carboxylate Chemical compound C1C(C2CC2)N(C(=O)OC(C)C)C2=CC=C(Cl)C=C2C1N(C(=O)OC)CC1=CC(C(F)(F)F)=CC(C(F)(F)F)=C1 LVRKSPMHHHUSIE-UHFFFAOYSA-N 0.000 description 1
- 102000004169 proteins and genes Human genes 0.000 description 1
- 108090000623 proteins and genes Proteins 0.000 description 1
- 208000005069 pulmonary fibrosis Diseases 0.000 description 1
- 208000002815 pulmonary hypertension Diseases 0.000 description 1
- 210000003492 pulmonary vein Anatomy 0.000 description 1
- 230000000306 recurrent effect Effects 0.000 description 1
- 208000015670 renal artery disease Diseases 0.000 description 1
- 206010038464 renal hypertension Diseases 0.000 description 1
- 230000004141 reverse cholesterol transport Effects 0.000 description 1
- 206010039073 rheumatoid arthritis Diseases 0.000 description 1
- 201000000306 sarcoidosis Diseases 0.000 description 1
- 230000002784 sclerotic effect Effects 0.000 description 1
- 230000028327 secretion Effects 0.000 description 1
- 230000001568 sexual effect Effects 0.000 description 1
- 208000007056 sickle cell anemia Diseases 0.000 description 1
- 230000000391 smoking effect Effects 0.000 description 1
- 208000010110 spontaneous platelet aggregation Diseases 0.000 description 1
- 230000006641 stabilisation Effects 0.000 description 1
- 238000011105 stabilization Methods 0.000 description 1
- 208000023516 stroke disease Diseases 0.000 description 1
- 125000000475 sulfinyl group Chemical group [*:2]S([*:1])=O 0.000 description 1
- 125000000472 sulfonyl group Chemical group *S(*)(=O)=O 0.000 description 1
- 229940124597 therapeutic agent Drugs 0.000 description 1
- CMSGWTNRGKRWGS-NQIIRXRSSA-N torcetrapib Chemical compound COC(=O)N([C@H]1C[C@@H](CC)N(C2=CC=C(C=C21)C(F)(F)F)C(=O)OCC)CC1=CC(C(F)(F)F)=CC(C(F)(F)F)=C1 CMSGWTNRGKRWGS-NQIIRXRSSA-N 0.000 description 1
- 229950004514 torcetrapib Drugs 0.000 description 1
- 201000010875 transient cerebral ischemia Diseases 0.000 description 1
- 230000032258 transport Effects 0.000 description 1
- 150000003626 triacylglycerols Chemical class 0.000 description 1
- 208000027185 varicose disease Diseases 0.000 description 1
- 210000005167 vascular cell Anatomy 0.000 description 1
Classifications
-
- 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
-
- 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
-
- 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
-
- 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/47—Quinolines; Isoquinolines
-
- 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/47—Quinolines; Isoquinolines
- A61K31/4706—4-Aminoquinolines; 8-Aminoquinolines, e.g. chloroquine, primaquine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/02—Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/12—Drugs for disorders of the urinary system of the kidneys
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
-
- 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
- A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
-
- 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
- A61P25/00—Drugs for disorders of the nervous system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/08—Antiepileptics; Anticonvulsants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
-
- 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
- A61P3/04—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
- 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
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/12—Drugs for disorders of the metabolism for electrolyte homeostasis
- A61P3/14—Drugs for disorders of the metabolism for electrolyte homeostasis for calcium homeostasis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P33/00—Antiparasitic agents
- A61P33/10—Anthelmintics
- A61P33/12—Schistosomicides
-
- 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
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
- A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P39/00—General protective or antinoxious agents
- A61P39/06—Free radical scavengers or antioxidants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
- A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
-
- 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
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/06—Antiarrhythmics
-
- 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
-
- 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
- A61P9/12—Antihypertensives
-
- 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
- A61P9/14—Vasoprotectives; Antihaemorrhoidals; Drugs for varicose therapy; Capillary stabilisers
-
- 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
- Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Organic Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Epidemiology (AREA)
- Diabetes (AREA)
- Immunology (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Hematology (AREA)
- Neurology (AREA)
- Obesity (AREA)
- Endocrinology (AREA)
- Urology & Nephrology (AREA)
- Rheumatology (AREA)
- Pain & Pain Management (AREA)
- Vascular Medicine (AREA)
- Psychiatry (AREA)
- Physical Education & Sports Medicine (AREA)
- Ophthalmology & Optometry (AREA)
- Emergency Medicine (AREA)
- Hospice & Palliative Care (AREA)
- Toxicology (AREA)
- Biochemistry (AREA)
- Transplantation (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Tropical Medicine & Parasitology (AREA)
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US39339502P | 2002-07-02 | 2002-07-02 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ZA200409582B true ZA200409582B (en) | 2006-08-30 |
Family
ID=30115572
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ZA200409582A ZA200409582B (en) | 2002-07-02 | 2004-11-26 | Use of CETP inhibitors and optionally HMG Coa reductable inhibitors and/or antihypertensive agents |
Country Status (23)
| Country | Link |
|---|---|
| US (1) | US20040053842A1 (es) |
| EP (1) | EP1519754A1 (es) |
| JP (1) | JP2005532388A (es) |
| KR (1) | KR20050025578A (es) |
| CN (1) | CN1665537A (es) |
| AP (1) | AP2004003189A0 (es) |
| AU (1) | AU2003244921A1 (es) |
| BR (1) | BR0312421A (es) |
| CA (1) | CA2488736A1 (es) |
| EA (1) | EA200401471A1 (es) |
| EC (1) | ECSP045520A (es) |
| HR (1) | HRP20041238A2 (es) |
| IL (1) | IL165328A0 (es) |
| IS (1) | IS7570A (es) |
| MA (1) | MA27311A1 (es) |
| MX (1) | MXPA05000015A (es) |
| NO (1) | NO20050497L (es) |
| OA (1) | OA12876A (es) |
| PL (1) | PL374878A1 (es) |
| TN (1) | TNSN04268A1 (es) |
| TW (1) | TW200401768A (es) |
| WO (1) | WO2004004778A1 (es) |
| ZA (1) | ZA200409582B (es) |
Families Citing this family (42)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7071210B2 (en) * | 2002-07-02 | 2006-07-04 | Pfizer Inc. | CETP inhibitors in combination with antihypertensive agents and uses thereof |
| US20040132771A1 (en) * | 2002-12-20 | 2004-07-08 | Pfizer Inc | Compositions of choleseteryl ester transfer protein inhibitors and HMG-CoA reductase inhibitors |
| DE60319877T2 (de) * | 2002-12-20 | 2009-04-30 | Pfizer Products Inc., Groton | Dosierungsform enthaltend einen cetp-hemmer und einen hmg-coa reduktase hemmer |
| ES2310676T3 (es) * | 2002-12-20 | 2009-01-16 | Pfizer Products Inc. | Formas de dosificacion que comprenden un inhibidor de cetp y un inhibidor de hmg-coa reductasa. |
| EP1599468B1 (en) | 2003-01-14 | 2007-10-03 | Arena Pharmaceuticals, Inc. | 1,2,3-trisubstituted aryl and heteroaryl derivatives as modulators of metabolism and the prophylaxis and treatment of disorders related thereto such as diabetes and hyperglycemia |
| BRPI0408442A (pt) * | 2003-03-17 | 2006-04-04 | Japan Tobacco Inc | método para aumento da biodisponibilidade oral de s-[2-([[1-(2-etilbutil)ciclohexil]carbonil]amino)fenil]2- metilpropanotioato |
| PL1603553T3 (pl) * | 2003-03-17 | 2012-04-30 | Japan Tobacco Inc | Kompozycje farmaceutyczne inhibitorów CETP |
| TWI494102B (zh) * | 2003-05-02 | 2015-08-01 | Japan Tobacco Inc | 包含ｓ-〔２（〔〔１-（２-乙基丁基）環己基〕羰基〕胺基）苯基〕２-甲基丙烷硫酯及ｈｍｇ輔酶ａ還原酶抑制劑之組合 |
| JP4901474B2 (ja) * | 2003-05-30 | 2012-03-21 | ランバクシー ラボラトリーズ リミテッド | 置換ピロール誘導体 |
| CN102417508A (zh) | 2003-07-14 | 2012-04-18 | 艾尼纳制药公司 | 作为新陈代谢调节剂的稠合芳基和杂芳基衍生物以及预防和治疗与其相关的病症 |
| CA2546793A1 (en) * | 2003-12-16 | 2005-06-30 | Novartis Ag | Use of stating for the treatment of metabolic syndrome |
| EP1740547A1 (en) * | 2004-04-07 | 2007-01-10 | Millennium Pharmaceuticals, Inc. | Pgd2 receptor antagonists for the treatment of inflammatory diseases |
| US20060063803A1 (en) * | 2004-09-23 | 2006-03-23 | Pfizer Inc | 4-Amino substituted-2-substituted-1,2,3,4-tetrahydroquinoline compounds |
| WO2007115131A2 (en) * | 2006-03-29 | 2007-10-11 | Guilford F Timothy | Liposomal reduced glutathione and 1-arginine, including other ingredient(s) |
| AU2005305460B2 (en) * | 2004-11-22 | 2011-04-21 | Dexcel Pharma Technologies Ltd. | Stable atorvastatin formulations |
| US7534806B2 (en) | 2004-12-06 | 2009-05-19 | Avigen, Inc. | Method for treating neuropathic pain and associated syndromes |
| WO2006069162A1 (en) * | 2004-12-20 | 2006-06-29 | Reddy Us Therapeutics, Inc. | Novel heterocyclic compounds and their pharmaceutical compositions |
| WO2006070248A1 (en) * | 2004-12-28 | 2006-07-06 | Ranbaxy Laboratories Limited | Methods for the preparation of stable pharmaceutical solid dosage forms of atorvastatin and amlodipine |
| US8604055B2 (en) * | 2004-12-31 | 2013-12-10 | Dr. Reddy's Laboratories Ltd. | Substituted benzylamino quinolines as cholesterol ester-transfer protein inhibitors |
| CA2605214C (en) * | 2004-12-31 | 2016-07-12 | Reddy Us Therapeutics, Inc. | Benzylamine derivatives as cetp inhibitors |
| MY148521A (en) | 2005-01-10 | 2013-04-30 | Arena Pharm Inc | Substituted pyridinyl and pyrimidinyl derivatives as modulators of metabolism and the treatment of disorders related thereto |
| WO2007106111A2 (en) * | 2005-07-01 | 2007-09-20 | Elan Pharma International Limited | Nanoparticulate and controlled release compositions comprising nilvadipine |
| EP1948600B1 (en) * | 2005-07-05 | 2014-04-16 | The President & Fellows Of Harvard College | Liver targeted conjugates |
| SG166829A1 (en) * | 2005-11-08 | 2010-12-29 | Ranbaxy Lab Ltd | Process for (3r, 5r)-7-[2-(4-fluorophenyl)-5-isopropyl-3-phenyl-4- [(4-hydroxy methyl phenyl amino) carbonyl]-pyrrol-1-yl]-3, 5-dihydroxy-heptanoic acid hemi calcium salt |
| CL2007000667A1 (es) * | 2006-03-14 | 2008-03-14 | Ranbaxi Lab Ltd | Composicion farmaceutica que comprende al acido 7-[2-(4-fluorofenil)-5-isopropil-3-fenil-4-[(4-hidroximetilfenilamino)carbonil]pirrol-1-il]-3,5-dihidroxi-heptanoico o una sal y al menos un agente estabilizante; procedimiento de preparacion, util en e |
| WO2007116243A2 (en) * | 2006-04-10 | 2007-10-18 | Mintails Limited | Method for treating fibromyalgia and related conditions |
| EP2049102A4 (en) * | 2006-07-14 | 2010-12-22 | Ranbaxy Lab Ltd | POLYMORPHIC FORMS OF AN HMG COA REDUCTASE HEATHER AND USE |
| DK2131841T3 (da) * | 2007-01-30 | 2012-10-15 | Avigen Inc | Fremgangsmåder til behandling af akut smerte |
| WO2008137012A1 (en) * | 2007-05-03 | 2008-11-13 | Avigen, Inc. | Use of a glial attenuator to prevent amplified pain responses caused by glial priming |
| WO2008143883A1 (en) * | 2007-05-14 | 2008-11-27 | Synvista Therapeutics, Inc. | Use of haptoglobin genotyping in diagnosis and treatment of defective reverse cholesterol transport (rct) |
| WO2009021113A1 (en) * | 2007-08-09 | 2009-02-12 | Holtzman, Jordan, L. | Methods for enhancing glutahione peroxidase activity |
| EP2070520A1 (en) | 2007-12-11 | 2009-06-17 | LEK Pharmaceuticals D.D. | Pharmaceutical composition comprising at least one active agent and a binder, which swells in an acidic media |
| WO2012046681A1 (ja) * | 2010-10-04 | 2012-04-12 | 興和株式会社 | 脂質代謝関連ｍＲＮＡの発現抑制剤 |
| KR101871011B1 (ko) | 2010-09-22 | 2018-06-25 | 아레나 파마슈티칼스, 인크. | Ｇｐｒ１１９ 수용체의 조절제 및 그와 관련된 장애의 치료 |
| JP5964965B2 (ja) | 2011-08-18 | 2016-08-03 | ドクター レディズ ラボラトリーズ リミテッド | コレステリルエステル転送タンパク質（ｃｅｔｐ）インヒビターとしての置換複素環式アミン化合物 |
| IN2014CN02290A (es) | 2011-09-27 | 2015-06-19 | Reddys Lab Ltd Dr | |
| EP4218765A3 (en) * | 2014-08-28 | 2023-08-09 | NewAmsterdam Pharma B.V. | Pharmaceutical composition and therapeutic combination comprising a cholesteryl ester transfer protein inhibitor and hmg coa reductase inhibitors |
| MX2017008925A (es) | 2015-01-06 | 2017-10-11 | Arena Pharm Inc | Metodos de condiciones de tratamiento relacionadas con el receptor s1p1. |
| PT3310760T (pt) | 2015-06-22 | 2022-11-10 | Arena Pharm Inc | Sal cristalino de l-arginina de ácido (r)-2-(7-(4-ciclopentil-3-(trifluorometil)benziloxi)-1,2,3,4-tetrahidrociclo-penta[b]indol-3-il)acético para utilização em distúrbios associados a recetores de s1p1 |
| WO2018019911A1 (en) * | 2016-07-27 | 2018-02-01 | Hartis-Pharma Sarl | Therapeutic combinations to treat red blood cell disorders |
| JP2020507611A (ja) | 2017-02-16 | 2020-03-12 | アリーナ ファーマシューティカルズ， インコーポレイテッド | 原発性胆汁性胆管炎の治療のための化合物および方法 |
| CN116196314B (zh) * | 2023-05-04 | 2023-08-15 | 广州市妇女儿童医疗中心 | Ri-1或其盐在制备防治胃肠道疾病的药物中的应用 |
Family Cites Families (17)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6144790A (en) * | 1997-02-07 | 2000-11-07 | Bledin; Anthony G | Contact fiber optic impact sensor |
| GT199800127A (es) * | 1997-08-29 | 2000-02-01 | Combinaciones terapeuticas. | |
| GT199800126A (es) * | 1997-08-29 | 2000-01-29 | Terapia de combinacion. | |
| NZ502283A (en) * | 1997-08-29 | 2002-05-31 | Pfizer Prod Inc | Cardiovascular therapy comprising amlodipine and a statin compound in amounts that are synergistically effective |
| US6147090A (en) * | 1998-09-17 | 2000-11-14 | Pfizer Inc. | 4-carboxyamino-2-methyl-1,2,3,4,-tetrahydroquinolines |
| US6197786B1 (en) * | 1998-09-17 | 2001-03-06 | Pfizer Inc | 4-Carboxyamino-2-substituted-1,2,3,4-tetrahydroquinolines |
| US6147089A (en) * | 1998-09-17 | 2000-11-14 | Pfizer Inc. | Annulated 4-carboxyamino-2-methyl-1,2,3,4,-tetrahydroquinolines |
| US6140342A (en) * | 1998-09-17 | 2000-10-31 | Pfizer Inc. | Oxy substituted 4-carboxyamino-2-methyl-1,2,3,4-tetrahydroquinolines |
| GT199900147A (es) * | 1998-09-17 | 1999-09-06 | 1, 2, 3, 4- tetrahidroquinolinas 2-sustituidas 4-amino sustituidas. | |
| SK16792001A3 (sk) * | 1999-05-27 | 2003-03-04 | Pfizer Products Inc. | Spoločné proliečivá amlodipínu a atorvastatínu |
| HN2000000050A (es) * | 1999-05-27 | 2001-02-02 | Pfizer Prod Inc | Sal mutua de amlodipino y atorvastatina |
| US20030092745A1 (en) * | 2000-02-25 | 2003-05-15 | Pfizer Inc. | Combination therapy |
| US20020013334A1 (en) * | 2000-06-15 | 2002-01-31 | Robl Jeffrey A. | HMG-CoA reductase inhibitors and method |
| AU2001270937A1 (en) * | 2000-08-15 | 2002-02-25 | Pfizer Products Inc. | Therapeutic combination |
| US6737430B2 (en) * | 2000-11-09 | 2004-05-18 | Pfizer, Inc. | Mutual prodrug of amlodipine and atorvastatin |
| EP1385501A2 (en) * | 2001-04-11 | 2004-02-04 | Atherogenics, Inc. | Probucol monoesters and their use to increase plasma hdl cholesterol levels and improve hdl functionality |
| US7071210B2 (en) * | 2002-07-02 | 2006-07-04 | Pfizer Inc. | CETP inhibitors in combination with antihypertensive agents and uses thereof |
-
2003
- 2003-06-10 US US10/459,683 patent/US20040053842A1/en not_active Abandoned
- 2003-06-18 AP AP2004003189A patent/AP2004003189A0/xx unknown
- 2003-06-18 AU AU2003244921A patent/AU2003244921A1/en not_active Abandoned
- 2003-06-18 BR BR0312421-5A patent/BR0312421A/pt not_active IP Right Cessation
- 2003-06-18 EP EP03738394A patent/EP1519754A1/en not_active Withdrawn
- 2003-06-18 CA CA002488736A patent/CA2488736A1/en not_active Abandoned
- 2003-06-18 PL PL03374878A patent/PL374878A1/xx not_active Application Discontinuation
- 2003-06-18 OA OA1200400342A patent/OA12876A/en unknown
- 2003-06-18 MX MXPA05000015A patent/MXPA05000015A/es not_active Application Discontinuation
- 2003-06-18 CN CN038155753A patent/CN1665537A/zh active Pending
- 2003-06-18 EA EA200401471A patent/EA200401471A1/ru unknown
- 2003-06-18 JP JP2004519080A patent/JP2005532388A/ja not_active Withdrawn
- 2003-06-18 WO PCT/IB2003/002792 patent/WO2004004778A1/en not_active Application Discontinuation
- 2003-06-18 IL IL16532803A patent/IL165328A0/xx unknown
- 2003-06-18 KR KR1020057000061A patent/KR20050025578A/ko not_active Application Discontinuation
- 2003-07-01 TW TW092117985A patent/TW200401768A/zh unknown
-
2004
- 2004-11-26 ZA ZA200409582A patent/ZA200409582B/en unknown
- 2004-11-29 IS IS7570A patent/IS7570A/is unknown
- 2004-12-17 MA MA28016A patent/MA27311A1/fr unknown
- 2004-12-30 EC EC2004005520A patent/ECSP045520A/es unknown
- 2004-12-30 TN TNP2004000268A patent/TNSN04268A1/fr unknown
- 2004-12-30 HR HR20041238A patent/HRP20041238A2/xx not_active Application Discontinuation
-
2005
- 2005-01-28 NO NO20050497A patent/NO20050497L/no not_active Application Discontinuation
Also Published As
| Publication number | Publication date |
|---|---|
| AU2003244921A1 (en) | 2004-01-23 |
| CN1665537A (zh) | 2005-09-07 |
| NO20050497L (no) | 2005-03-08 |
| PL374878A1 (en) | 2005-11-14 |
| EP1519754A1 (en) | 2005-04-06 |
| ECSP045520A (es) | 2005-03-10 |
| TNSN04268A1 (fr) | 2007-03-12 |
| AP2004003189A0 (en) | 2004-12-31 |
| BR0312421A (pt) | 2005-04-19 |
| KR20050025578A (ko) | 2005-03-14 |
| EA200401471A1 (ru) | 2005-06-30 |
| HRP20041238A2 (en) | 2005-06-30 |
| OA12876A (en) | 2006-09-15 |
| US20040053842A1 (en) | 2004-03-18 |
| IS7570A (is) | 2004-11-29 |
| WO2004004778A1 (en) | 2004-01-15 |
| JP2005532388A (ja) | 2005-10-27 |
| TW200401768A (en) | 2004-02-01 |
| CA2488736A1 (en) | 2004-01-15 |
| IL165328A0 (en) | 2006-01-15 |
| MXPA05000015A (es) | 2005-04-08 |
| MA27311A1 (fr) | 2005-05-02 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| ZA200409582B (en) | Use of CETP inhibitors and optionally HMG Coa reductable inhibitors and/or antihypertensive agents | |
| US6890925B2 (en) | Methods of using soluble epoxide hydrolase inhibitors | |
| McKeage et al. | Fenofibrate: a review of its use in dyslipidaemia | |
| CA3007081C (en) | Methods for inhibiting conversion of choline to trimethylamine (tma) | |
| RU2189973C2 (ru) | Новые бензамидоальдегиды | |
| KR20110050745A (ko) | 혈관항상성 유지제 및 그의 사용 방법 | |
| ZA200101745B (en) | 4-Amino substituted-2-substituted-1,2,3,4-tetrahydroquinolines as CETP inhibitors. | |
| Roth et al. | Efficacy and safety of rosuvastatin and fenofibric acid combination therapy versus simvastatin monotherapy in patients with hypercholesterolemia and hypertriglyceridemia: a randomized, double-blind study | |
| CN100467443C (zh) | 作为纤溶酶原激活物抑制剂1型(pai-1)的6-(芳基-酰氨基或芳基-酰氨甲基)-萘-2-基氧基-酸衍生物 | |
| FR16C0019I2 (fr) | Compositions pharmaceutiques a base de valsartan et d'inhibiteurs nep | |
| ZA200301755B (en) | Polyarylcarboxamides useful as lipid lowering agents. | |
| JP2016528276A (ja) | プラーク退縮を促進するための組成物及び治療法 | |
| IL296054A (en) | Oral preparations of the mk2 pathway inhibitor for the treatment of immune conditions | |
| AU2016247901A1 (en) | Ghrelin O-acyl transferase inhibitors | |
| AU2014353109A1 (en) | Novel DGAT2 inhibitors | |
| Yildirir et al. | Non-lipid effects of statins: emerging new indications | |
| JP2007501270A (ja) | Ｐ２Ｘ７受容体アンタゴニストおよび腫瘍壊死因子αを含む医薬組成物 | |
| Sawara et al. | Effects of lipid-lowering therapy with rosuvastatin on atherosclerotic burden in patients with chronic kidney disease | |
| UA58636C2 (uk) | Піразинонові інгібітори тромбіну, фармацевтична композиція, спосіб інгібування утворення тромбів у крові, спосіб лікування станів, пов'язаних із тромбоутворенням | |
| JP6837190B2 (ja) | トロンボキサン受容体アンタゴニスト | |
| US20030018040A1 (en) | Tnf-alpha inhibitors | |
| EP4011877A2 (en) | Method of treating elevated plasma cholesterol | |
| WO2007107843A1 (en) | Methods of treatment with cetp inhibitors | |
| EP1451138A2 (en) | Methods of reversing and preventing cardiovascular pathologies | |
| TW200403990A (en) | PTX3 gene expression suppressing method |