JP2010526152A5 - - Google Patents
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- Publication number
- JP2010526152A5 JP2010526152A5 JP2010507578A JP2010507578A JP2010526152A5 JP 2010526152 A5 JP2010526152 A5 JP 2010526152A5 JP 2010507578 A JP2010507578 A JP 2010507578A JP 2010507578 A JP2010507578 A JP 2010507578A JP 2010526152 A5 JP2010526152 A5 JP 2010526152A5
- Authority
- JP
- Japan
- Prior art keywords
- medicament
- statins
- use according
- dioxoethyl
- phenylmethyl
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Pending
Links
- 239000003814 drug Substances 0.000 claims 21
- 229940121710 HMGCoA reductase inhibitor Drugs 0.000 claims 17
- 239000002471 hydroxymethylglutaryl coenzyme A reductase inhibitor Substances 0.000 claims 17
- 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 16
- QTBSBXVTEAMEQO-UHFFFAOYSA-N Acetic acid Chemical compound CC(O)=O QTBSBXVTEAMEQO-UHFFFAOYSA-N 0.000 claims 15
- 239000000651 prodrug Substances 0.000 claims 14
- 229940002612 prodrug Drugs 0.000 claims 14
- 150000003839 salts Chemical class 0.000 claims 11
- 239000012453 solvate Substances 0.000 claims 11
- 108010007622 LDL Lipoproteins Proteins 0.000 claims 10
- 239000013078 crystal Substances 0.000 claims 9
- 238000004519 manufacturing process Methods 0.000 claims 8
- -1 2-Amino-1,2-dioxoethyl Chemical group 0.000 claims 7
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims 6
- 239000000203 mixture Substances 0.000 claims 6
- 239000002245 particle Substances 0.000 claims 6
- 208000024172 Cardiovascular disease Diseases 0.000 claims 4
- 208000029078 coronary artery disease Diseases 0.000 claims 4
- 201000010099 disease Diseases 0.000 claims 4
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 4
- 210000001596 intra-abdominal fat Anatomy 0.000 claims 3
- 208000011580 syndromic disease Diseases 0.000 claims 3
- VJYDOJXJUCJUHL-UHFFFAOYSA-N varespladib methyl Chemical compound CCC1=C(C(=O)C(N)=O)C2=C(OCC(=O)OC)C=CC=C2N1CC1=CC=CC=C1 VJYDOJXJUCJUHL-UHFFFAOYSA-N 0.000 claims 3
- 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 2
- 101710095342 Apolipoprotein B Proteins 0.000 claims 2
- 102100040202 Apolipoprotein B-100 Human genes 0.000 claims 2
- 201000001320 Atherosclerosis Diseases 0.000 claims 2
- 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 2
- 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 2
- 208000032928 Dyslipidaemia Diseases 0.000 claims 2
- 108090001005 Interleukin-6 Proteins 0.000 claims 2
- 208000017170 Lipid metabolism disease Diseases 0.000 claims 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 2
- 208000018262 Peripheral vascular disease Diseases 0.000 claims 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 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 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 2
- 229960005370 atorvastatin Drugs 0.000 claims 2
- 208000026106 cerebrovascular disease Diseases 0.000 claims 2
- 229960005110 cerivastatin Drugs 0.000 claims 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 2
- 229960003765 fluvastatin Drugs 0.000 claims 2
- 230000002757 inflammatory effect Effects 0.000 claims 2
- 229960004844 lovastatin Drugs 0.000 claims 2
- PCZOHLXUXFIOCF-BXMDZJJMSA-N lovastatin Chemical compound 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 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 2
- 229950009116 mevastatin Drugs 0.000 claims 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 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 2
- 108010071584 oxidized low density lipoprotein Proteins 0.000 claims 2
- 229960002797 pitavastatin Drugs 0.000 claims 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 2
- 229960002965 pravastatin Drugs 0.000 claims 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 2
- 229960000672 rosuvastatin Drugs 0.000 claims 2
- 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 2
- 229960002855 simvastatin Drugs 0.000 claims 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 2
- UFTFJSFQGQCHQW-UHFFFAOYSA-N triformin Chemical compound O=COCC(OC=O)COC=O UFTFJSFQGQCHQW-UHFFFAOYSA-N 0.000 claims 2
- BHLXTPHDSZUFHR-UHFFFAOYSA-N varespladib Chemical compound CCC1=C(C(=O)C(N)=O)C2=C(OCC(O)=O)C=CC=C2N1CC1=CC=CC=C1 BHLXTPHDSZUFHR-UHFFFAOYSA-N 0.000 claims 2
- ZZRFQBQNZLFESZ-BTQNPOSSSA-N 2-[(3r)-4-[(4-chlorophenyl)methyl]-7-fluoro-5-methylsulfonyl-2,3-dihydro-1h-cyclopenta[b]indol-3-yl]acetic acid;pyridine-3-carboxylic acid Chemical compound OC(=O)C1=CC=CN=C1.C=1([C@@H](CC(O)=O)CCC=1C=1C=C(F)C=C(C2=1)S(=O)(=O)C)N2CC1=CC=C(Cl)C=C1 ZZRFQBQNZLFESZ-BTQNPOSSSA-N 0.000 claims 1
- 206010002329 Aneurysm Diseases 0.000 claims 1
- 206010002383 Angina Pectoris Diseases 0.000 claims 1
- PVNIIMVLHYAWGP-UHFFFAOYSA-N Niacin Chemical compound OC(=O)C1=CC=CN=C1 PVNIIMVLHYAWGP-UHFFFAOYSA-N 0.000 claims 1
- 206010047115 Vasculitis Diseases 0.000 claims 1
- 206010047249 Venous thrombosis Diseases 0.000 claims 1
- HKPPDMRSVIYYKG-FPDMAROZSA-M [1-[(3R)-1-(2,4-difluorophenyl)-1-hydroxy-3-[2-oxo-3-[4-(tetrazol-1-yl)phenyl]imidazolidin-1-yl]butyl]-1,2,4-triazol-4-ium-4-yl]methyl acetate chloride Chemical compound [Cl-].C[C@H](CC(O)(c1ccc(F)cc1F)n1c[n+](COC(C)=O)cn1)N1CCN(C1=O)c1ccc(cc1)-n1cnnn1 HKPPDMRSVIYYKG-FPDMAROZSA-M 0.000 claims 1
- 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 1
- 229960000528 amlodipine Drugs 0.000 claims 1
- 230000002490 cerebral effect Effects 0.000 claims 1
- 239000003795 chemical substances by application Substances 0.000 claims 1
- 239000002131 composite material Substances 0.000 claims 1
- 206010012601 diabetes mellitus Diseases 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- OLNTVTPDXPETLC-XPWALMASSA-N ezetimibe Chemical compound N1([C@@H]([C@H](C1=O)CC[C@H](O)C=1C=CC(F)=CC=1)C=1C=CC(O)=CC=1)C1=CC=C(F)C=C1 OLNTVTPDXPETLC-XPWALMASSA-N 0.000 claims 1
- 229960000815 ezetimibe Drugs 0.000 claims 1
- YMTINGFKWWXKFG-UHFFFAOYSA-N fenofibrate Chemical compound C1=CC(OC(C)(C)C(=O)OC(C)C)=CC=C1C(=O)C1=CC=C(Cl)C=C1 YMTINGFKWWXKFG-UHFFFAOYSA-N 0.000 claims 1
- 229960002297 fenofibrate Drugs 0.000 claims 1
- 238000009472 formulation Methods 0.000 claims 1
- 230000000302 ischemic effect Effects 0.000 claims 1
- 238000000034 method Methods 0.000 claims 1
- 208000010125 myocardial infarction Diseases 0.000 claims 1
- 229960003512 nicotinic acid Drugs 0.000 claims 1
- 235000001968 nicotinic acid Nutrition 0.000 claims 1
- 239000011664 nicotinic acid Substances 0.000 claims 1
- 238000013268 sustained release Methods 0.000 claims 1
- 239000012730 sustained-release form Substances 0.000 claims 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 claims 1
- 230000001052 transient effect Effects 0.000 claims 1
Applications Claiming Priority (4)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US91591007P | 2007-05-03 | 2007-05-03 | |
| US96959107P | 2007-08-31 | 2007-08-31 | |
| US87486907A | 2007-10-18 | 2007-10-18 | |
| PCT/US2008/062577 WO2008137803A1 (en) | 2007-05-03 | 2008-05-02 | Treatment of cardiovascular disease and dyslipidemia using secretory phospholipase a2 (spla2) inhibitors and spla2 inhibitor combination therapies |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2010526152A JP2010526152A (ja) | 2010-07-29 |
| JP2010526152A5 true JP2010526152A5 (https=) | 2012-06-07 |
Family
ID=39943969
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2010507578A Pending JP2010526152A (ja) | 2007-05-03 | 2008-05-02 | 分泌型ホスホリパーゼａ２（ｓｐｌａ２）インヒビターを用いる心血管疾患および脂質異常症の治療およびｓｐｌａ２インヒビター併用療法 |
Country Status (8)
| Country | Link |
|---|---|
| EP (1) | EP2154958A4 (https=) |
| JP (1) | JP2010526152A (https=) |
| CN (1) | CN101742907A (https=) |
| AU (1) | AU2008247451A1 (https=) |
| BR (1) | BRPI0811486A2 (https=) |
| CA (1) | CA2686157A1 (https=) |
| EA (1) | EA200971020A1 (https=) |
| WO (1) | WO2008137803A1 (https=) |
Families Citing this family (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102271507A (zh) * | 2009-01-08 | 2011-12-07 | 安塞拉制药有限公司 | 分泌型磷脂酶a2(spla2)抑制剂和烟酸药物组合物以及治疗心血管疾病和血脂异常的方法 |
| RU2483707C1 (ru) * | 2012-05-04 | 2013-06-10 | Лира Талгатовна Гильмутдинова | Способ санаторной терапии больных с метаболическим синдромом и артериальной гипертензией с применением сульфидных ванн |
| CN115040508A (zh) * | 2022-07-28 | 2022-09-13 | 上海市同仁医院 | 吲哚-3-乙醛在制备新型抗肥胖活性制剂中的应用 |
Family Cites Families (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GT199800127A (es) * | 1997-08-29 | 2000-02-01 | Combinaciones terapeuticas. | |
| ID27812A (id) * | 1998-05-01 | 2001-04-26 | Lilly Co Eli | ESTER PENGHAMBAT sPLA2 |
| WO2001055108A2 (en) * | 2000-01-25 | 2001-08-02 | Eli Lilly And Company | Use of spl a2 inhibitors for the treatment of inflammation |
| JP2004503604A (ja) * | 2000-07-24 | 2004-02-05 | ザ・ユニバーシティ・オブ・クイーンズランド | 化合物およびホスホリパーゼ阻害剤 |
| TWI314457B (https=) * | 2001-03-19 | 2009-09-11 | Shionogi & Co | |
| WO2006034435A2 (en) * | 2004-09-21 | 2006-03-30 | Point Therapeutics, Inc. | Methods and compositions for treating glucose-associated conditions, metabolic syndrome, dyslipidemias and other conditions |
| US7666898B2 (en) * | 2005-11-03 | 2010-02-23 | Ilypsa, Inc. | Multivalent indole compounds and use thereof as phospholipase-A2 inhibitors |
-
2008
- 2008-05-02 CN CN200880023061A patent/CN101742907A/zh active Pending
- 2008-05-02 BR BRPI0811486-2A2A patent/BRPI0811486A2/pt not_active IP Right Cessation
- 2008-05-02 WO PCT/US2008/062577 patent/WO2008137803A1/en not_active Ceased
- 2008-05-02 EA EA200971020A patent/EA200971020A1/ru unknown
- 2008-05-02 AU AU2008247451A patent/AU2008247451A1/en not_active Abandoned
- 2008-05-02 JP JP2010507578A patent/JP2010526152A/ja active Pending
- 2008-05-02 EP EP08747605A patent/EP2154958A4/en not_active Withdrawn
- 2008-05-02 CA CA002686157A patent/CA2686157A1/en not_active Abandoned
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