JP2004532186A5 - - Google Patents
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- Publication number
- JP2004532186A5 JP2004532186A5 JP2002559030A JP2002559030A JP2004532186A5 JP 2004532186 A5 JP2004532186 A5 JP 2004532186A5 JP 2002559030 A JP2002559030 A JP 2002559030A JP 2002559030 A JP2002559030 A JP 2002559030A JP 2004532186 A5 JP2004532186 A5 JP 2004532186A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- group
- aryl
- independently
- absorption inhibitor
- 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.)
- Granted
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- 125000000217 alkyl group Chemical group 0.000 claims 120
- 238000010521 absorption reaction Methods 0.000 claims 56
- 239000003112 inhibitor Substances 0.000 claims 56
- 230000002401 inhibitory effect Effects 0.000 claims 56
- 125000003118 aryl group Chemical group 0.000 claims 44
- 235000003702 sterols Nutrition 0.000 claims 39
- 150000003432 sterols Chemical class 0.000 claims 31
- 150000003839 salts Chemical class 0.000 claims 30
- 239000011780 sodium chloride Substances 0.000 claims 30
- 239000012453 solvate Substances 0.000 claims 30
- 239000000203 mixture Substances 0.000 claims 27
- -1 cholesterol sterol Chemical class 0.000 claims 22
- 125000003545 alkoxy group Chemical group 0.000 claims 21
- 229910052739 hydrogen Inorganic materials 0.000 claims 20
- 125000001424 substituent group Chemical group 0.000 claims 19
- 150000001875 compounds Chemical class 0.000 claims 18
- 239000001257 hydrogen Substances 0.000 claims 18
- 125000003107 substituted aryl group Chemical group 0.000 claims 18
- 125000005843 halogen group Chemical group 0.000 claims 12
- 125000001072 heteroaryl group Chemical group 0.000 claims 12
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 12
- 125000002947 alkylene group Chemical group 0.000 claims 11
- 150000002431 hydrogen Chemical class 0.000 claims 10
- 241000124008 Mammalia Species 0.000 claims 9
- 229940107161 Cholesterol Drugs 0.000 claims 8
- HVYWMOMLDIMFJA-DPAQBDIFSA-N Cholesterol Natural products 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 8
- 230000036201 Tissue concentration Effects 0.000 claims 8
- 235000012000 cholesterol Nutrition 0.000 claims 8
- UFHFLCQGNIYNRP-UHFFFAOYSA-N hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 8
- 239000000651 prodrug Substances 0.000 claims 8
- 229940002612 prodrugs Drugs 0.000 claims 8
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims 7
- 230000036470 plasma concentration Effects 0.000 claims 7
- 238000006467 substitution reaction Methods 0.000 claims 7
- 206010003210 Arteriosclerosis Diseases 0.000 claims 6
- 125000004432 carbon atoms Chemical group C* 0.000 claims 6
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 6
- 125000000753 cycloalkyl group Chemical group 0.000 claims 6
- 229910052736 halogen Inorganic materials 0.000 claims 6
- 150000002367 halogens Chemical group 0.000 claims 6
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 6
- 125000002541 furyl group Chemical group 0.000 claims 5
- 125000002883 imidazolyl group Chemical group 0.000 claims 5
- 125000003226 pyrazolyl group Chemical group 0.000 claims 5
- 125000004076 pyridyl group Chemical group 0.000 claims 5
- 125000000168 pyrrolyl group Chemical group 0.000 claims 5
- 125000003003 spiro group Chemical group 0.000 claims 5
- 125000000335 thiazolyl group Chemical group 0.000 claims 5
- 125000001544 thienyl group Chemical group 0.000 claims 5
- 206010063985 Phytosterolaemia Diseases 0.000 claims 4
- 208000002227 Sitosterolemia Diseases 0.000 claims 4
- 125000004450 alkenylene group Chemical group 0.000 claims 4
- 125000003282 alkyl amino group Chemical group 0.000 claims 4
- 229910052799 carbon Inorganic materials 0.000 claims 4
- 230000000271 cardiovascular Effects 0.000 claims 4
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 4
- 125000003387 indolinyl group Chemical group N1(CCC2=CC=CC=C12)* 0.000 claims 4
- 125000000842 isoxazolyl group Chemical group 0.000 claims 4
- 125000002757 morpholinyl group Chemical group 0.000 claims 4
- 229910052757 nitrogen Inorganic materials 0.000 claims 4
- 125000003386 piperidinyl group Chemical group 0.000 claims 4
- 230000002265 prevention Effects 0.000 claims 4
- 125000000719 pyrrolidinyl group Chemical group 0.000 claims 4
- 125000003342 alkenyl group Chemical group 0.000 claims 3
- 201000001320 atherosclerosis Diseases 0.000 claims 3
- OKTJSMMVPCPJKN-UHFFFAOYSA-N carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims 3
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims 3
- 125000001624 naphthyl group Chemical group 0.000 claims 3
- 125000002971 oxazolyl group Chemical group 0.000 claims 3
- 125000000951 phenoxy group Chemical group [H]C1=C([H])C([H])=C(O*)C([H])=C1[H] 0.000 claims 3
- 125000000843 phenylene group Chemical group C1(=C(C=CC=C1)*)* 0.000 claims 3
- 125000003373 pyrazinyl group Chemical group 0.000 claims 3
- 125000000714 pyrimidinyl group Chemical group 0.000 claims 3
- 201000011528 vascular disease Diseases 0.000 claims 3
- MNFORVFSTILPAW-UHFFFAOYSA-N Β-Lactam Chemical compound O=C1CCN1 MNFORVFSTILPAW-UHFFFAOYSA-N 0.000 claims 3
- 125000004453 alkoxycarbonyl group Chemical group 0.000 claims 2
- 125000004644 alkyl sulfinyl group Chemical group 0.000 claims 2
- 125000004390 alkyl sulfonyl group Chemical group 0.000 claims 2
- 125000004414 alkyl thio group Chemical group 0.000 claims 2
- 150000001413 amino acids Chemical class 0.000 claims 2
- 125000004104 aryloxy group Chemical group 0.000 claims 2
- IVRMZWNICZWHMI-UHFFFAOYSA-N azide Chemical compound [N-]=[N+]=[N-] IVRMZWNICZWHMI-UHFFFAOYSA-N 0.000 claims 2
- 125000001164 benzothiazolyl group Chemical group S1C(=NC2=C1C=CC=C2)* 0.000 claims 2
- 125000000051 benzyloxy group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])O* 0.000 claims 2
- 125000002993 cycloalkylene group Chemical group 0.000 claims 2
- 125000005879 dioxolanyl group Chemical group 0.000 claims 2
- 239000003814 drug Substances 0.000 claims 2
- 125000003392 indanyl group Chemical group C1(CCC2=CC=CC=C12)* 0.000 claims 2
- 125000003454 indenyl group Chemical group C1(C=CC2=CC=CC=C12)* 0.000 claims 2
- 125000001786 isothiazolyl group Chemical group 0.000 claims 2
- 238000004519 manufacturing process Methods 0.000 claims 2
- 125000004043 oxo group Chemical group O=* 0.000 claims 2
- 125000002098 pyridazinyl group Chemical group 0.000 claims 2
- 125000001712 tetrahydronaphthyl group Chemical group C1(CCCC2=CC=CC=C12)* 0.000 claims 2
- 125000001113 thiadiazolyl group Chemical group 0.000 claims 2
- 125000003821 2-(trimethylsilyl)ethoxymethyl group Chemical group [H]C([H])([H])[Si](C([H])([H])[H])(C([H])([H])[H])C([H])([H])C(OC([H])([H])[*])([H])[H] 0.000 claims 1
- 208000004981 Coronary Disease Diseases 0.000 claims 1
- 150000001204 N-oxides Chemical class 0.000 claims 1
- 210000002381 Plasma Anatomy 0.000 claims 1
- 125000004183 alkoxy alkyl group Chemical group 0.000 claims 1
- 125000005083 alkoxyalkoxy group Chemical group 0.000 claims 1
- 125000005085 alkoxycarbonylalkoxy group Chemical group 0.000 claims 1
- 125000000676 alkoxyimino group Chemical group 0.000 claims 1
- 125000004448 alkyl carbonyl group Chemical group 0.000 claims 1
- 125000000304 alkynyl group Chemical group 0.000 claims 1
- 125000005336 allyloxy group Chemical group 0.000 claims 1
- 125000005129 aryl carbonyl group Chemical group 0.000 claims 1
- 125000002047 benzodioxolyl group Chemical class O1OC(C2=C1C=CC=C2)* 0.000 claims 1
- 229910052801 chlorine Inorganic materials 0.000 claims 1
- 239000000460 chlorine Substances 0.000 claims 1
- ZAMOUSCENKQFHK-UHFFFAOYSA-N chlorine atom Chemical compound [Cl] ZAMOUSCENKQFHK-UHFFFAOYSA-N 0.000 claims 1
- 201000008739 coronary artery disease Diseases 0.000 claims 1
- 125000000392 cycloalkenyl group Chemical group 0.000 claims 1
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 1
- 229910052731 fluorine Inorganic materials 0.000 claims 1
- 239000011737 fluorine Substances 0.000 claims 1
- YCKRFDGAMUMZLT-UHFFFAOYSA-N fluorine atom Chemical compound [F] YCKRFDGAMUMZLT-UHFFFAOYSA-N 0.000 claims 1
- 150000002829 nitrogen Chemical group 0.000 claims 1
- 229920000728 polyester Polymers 0.000 claims 1
- 125000004306 triazinyl group Chemical group 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US26464501P | 2001-01-26 | 2001-01-26 | |
| US60/264,645 | 2001-01-26 | ||
| PCT/US2002/001195 WO2002058696A2 (en) | 2001-01-26 | 2002-01-25 | The use of substituted azetidinone compounds for the treatment of sitosterolemia |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2007005232A Division JP4614460B2 (ja) | 2001-01-26 | 2007-01-12 | シトステロール血症の処置のための置換アゼチジノン化合物の使用 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2004532186A JP2004532186A (ja) | 2004-10-21 |
| JP2004532186A5 true JP2004532186A5 (US07560449-20090714-C00027.png) | 2005-05-26 |
| JP4711600B2 JP4711600B2 (ja) | 2011-06-29 |
Family
ID=23006987
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2002559030A Expired - Lifetime JP4711600B2 (ja) | 2001-01-26 | 2002-01-25 | シトステロール血症の処置のための置換アゼチジノン化合物の使用 |
| JP2007005232A Expired - Lifetime JP4614460B2 (ja) | 2001-01-26 | 2007-01-12 | シトステロール血症の処置のための置換アゼチジノン化合物の使用 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2007005232A Expired - Lifetime JP4614460B2 (ja) | 2001-01-26 | 2007-01-12 | シトステロール血症の処置のための置換アゼチジノン化合物の使用 |
Country Status (33)
Families Citing this family (39)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| PL205343B1 (pl) * | 2001-01-26 | 2010-04-30 | Schering Corp | Zastosowanie inhibitora wchłaniania sterolu |
| DE60221798T2 (de) * | 2001-01-26 | 2008-06-05 | Schering Corp. | Kombinationen von gallensäure sequestriermitteln und hemmern der sterol absorption zur behandlung von kardiovaskulären indikationen |
| US20060287254A1 (en) * | 2001-01-26 | 2006-12-21 | Schering Corporation | Use of substituted azetidinone compounds for the treatment of sitosterolemia |
| EP1859796A3 (en) * | 2001-09-21 | 2008-07-02 | Schering Corporation | Treatment of xanthoma with azetidinone derivatives as sterol absorption inhibitors |
| EP1427409B1 (en) * | 2001-09-21 | 2008-10-15 | Schering Corporation | Methods for treating or preventing vascular inflammation using sterol absorption inhibitor(s) |
| EP1429756B1 (en) * | 2001-09-21 | 2006-11-22 | Schering Corporation | Treatment of xanthoma with azetidinone derivatives as sterol absorption inhibitors |
| GB0215579D0 (en) | 2002-07-05 | 2002-08-14 | Astrazeneca Ab | Chemical compounds |
| AR040588A1 (es) | 2002-07-26 | 2005-04-13 | Schering Corp | Formulacion farmaceutica que comprende un inhibidor de la absorcion del colesterol y un inhibidor de una hmg- co a reductasa |
| DE10259245A1 (de) | 2002-12-17 | 2004-07-01 | Merck Patent Gmbh | Derivate des Asimadolins mit kovalent gebundenen Säuren |
| PL377847A1 (pl) | 2003-01-14 | 2006-02-20 | Arena Pharmaceuticals Inc. | 1,2,3-Tripodstawione pochodne arylowe i heteroarylowe jako modulatory metabolizmu oraz profilaktyka i leczenie związanych z nim zaburzeń takich jak cukrzyca i hiperglikemia |
| US7208486B2 (en) | 2003-03-07 | 2007-04-24 | Schering Corporation | Substituted azetidinone compounds, processes for preparing the same, formulations and uses thereof |
| WO2004081002A1 (en) | 2003-03-07 | 2004-09-23 | Schering Corporation | Substituted azetidinone compounds, formulations and uses thereof for the treatment of hypercholesterolemia |
| EA010023B1 (ru) | 2003-07-14 | 2008-06-30 | Арена Фармасьютикалз, Инк. | Конденсированные арильные и гетероарильные производные в качестве модуляторов метаболизма и для профилактики и лечения расстройств, связанных с нарушением метаболизма |
| GB0322552D0 (en) * | 2003-09-26 | 2003-10-29 | Astrazeneca Uk Ltd | Therapeutic treatment |
| WO2005046797A2 (en) * | 2003-11-05 | 2005-05-26 | Schering Corporation | Combinations of lipid modulating agents and substituted azetidinones and treatments for vascular conditions |
| US7871998B2 (en) | 2003-12-23 | 2011-01-18 | Astrazeneca Ab | Diphenylazetidinone derivatives possessing cholesterol absorption inhibitory activity |
| TWI457079B (zh) * | 2004-03-29 | 2014-10-21 | Wyeth Corp | 複維生素及礦物質補充劑 |
| US7803838B2 (en) * | 2004-06-04 | 2010-09-28 | Forest Laboratories Holdings Limited | Compositions comprising nebivolol |
| US7838552B2 (en) | 2004-06-04 | 2010-11-23 | Forest Laboratories Holdings Limited | Compositions comprising nebivolol |
| 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 |
| SA06270191B1 (ar) | 2005-06-22 | 2010-03-29 | استرازينيكا ايه بي | مشتقات من 2- أزيتيدينون جديدة باعتبارها مثبطات لامتصاص الكوليسترول لعلاج حالات فرط نسبة الدهون في الدم |
| TW200811098A (en) | 2006-04-27 | 2008-03-01 | Astrazeneca Ab | Chemical compounds |
| WO2008010008A2 (en) * | 2006-07-17 | 2008-01-24 | Wockhardt Limited | Cardiovascular combinations using rennin-angiotensin inhibitors |
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| WO2009024889A2 (en) | 2007-08-21 | 2009-02-26 | Ranbaxy Laboratories Limited | Pharmaceutical composition comprising a hmg-coa reductase inhibitor and ezetimibe |
| KR100966630B1 (ko) * | 2008-04-23 | 2010-06-29 | 에스케이텔레시스 주식회사 | ＱｏＳ 제공 시스템 및 이를 이용한 방법 |
| US9817001B2 (en) * | 2008-05-27 | 2017-11-14 | Boston Heart Diagnostics Corporation | Methods for determining LDL cholesterol treatment |
| TR200806300A2 (tr) * | 2008-08-22 | 2010-03-22 | B�Lg�� Mahmut | Çözünürlük artırıcı farmasötlk formulasyon |
| US8470541B1 (en) | 2008-09-27 | 2013-06-25 | Boston Heart Diagnostics Corporation | Methods for separation and immuno-detection of biomolecules, and apparatus related thereto |
| WO2011019326A2 (en) | 2009-07-02 | 2011-02-17 | Mahmut Bilgic | Solubility and stability enchancing pharmaceutical formulation |
| EP2448564A2 (en) | 2009-07-02 | 2012-05-09 | Bilgic Mahmut | Solubility enhancing pharmaceutical formulation |
| EP3378854B1 (en) | 2010-01-27 | 2022-12-21 | Arena Pharmaceuticals, Inc. | Processes for the preparation of (r)-2-(7-(4-cyclopentyl-3-(trifluoromethyl)benzyloxy)-1,2,3,4-tetrahydrocyclopenta[b]indol-3-yl)acetic acid and salts thereof |
| BR112013008100A2 (pt) | 2010-09-22 | 2016-08-09 | Arena Pharm Inc | "moduladores do receptor de gpr19 e o tratamento de distúrbios relacionados a eles." |
| US8765377B2 (en) | 2011-10-13 | 2014-07-01 | Boston Heart Diagnostics Corporation | Compositions and methods for treating and preventing coronary heart disease |
| US9828624B2 (en) | 2013-07-24 | 2017-11-28 | Boston Heart Diagnostics Corporation | Driving patient compliance with therapy |
| US9739790B2 (en) | 2014-11-17 | 2017-08-22 | Boston Heart Diagnostic Corporation | Cardiovascular disease risk assessment |
| AU2016205361C1 (en) | 2015-01-06 | 2021-04-08 | Arena Pharmaceuticals, Inc. | Methods of treating conditions related to the S1P1 receptor |
| SI3310760T1 (sl) | 2015-06-22 | 2023-02-28 | Arena Pharmaceuticals, Inc. | Kristalinična L-argininska sol (R)-2-(7-(4-ciklopentil-3-(trifluorometil)benziloksi)-1,2,3,4- tetrahidrociklo-penta(b)indol-3-il)ocetne kisline za uporabo pri motnjah, povezanih z receptorjem S1P1 |
| KR20190116416A (ko) | 2017-02-16 | 2019-10-14 | 아레나 파마슈티칼스, 인크. | 원발 담즙성 담관염을 치료하기 위한 화합물 및 방법 |
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