JP2004523571A5 - - Google Patents
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- JP2004523571A5 JP2004523571A5 JP2002571459A JP2002571459A JP2004523571A5 JP 2004523571 A5 JP2004523571 A5 JP 2004523571A5 JP 2002571459 A JP2002571459 A JP 2002571459A JP 2002571459 A JP2002571459 A JP 2002571459A JP 2004523571 A5 JP2004523571 A5 JP 2004523571A5
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- JP
- Japan
- Prior art keywords
- residue
- substituted
- alkyl
- molecule
- side pocket
- 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
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- -1 amino, monosubstituted amino Chemical group 0.000 claims 39
- 125000000547 substituted alkyl group Chemical group 0.000 claims 28
- 125000000217 alkyl group Chemical group 0.000 claims 24
- 125000005432 dialkylcarboxamide group Chemical group 0.000 claims 22
- 239000000203 mixture Substances 0.000 claims 22
- 229910052739 hydrogen Inorganic materials 0.000 claims 21
- 239000001257 hydrogen Substances 0.000 claims 21
- 125000004435 hydrogen atom Chemical class [H]* 0.000 claims 20
- 125000004438 haloalkoxy group Chemical group 0.000 claims 18
- 125000005431 alkyl carboxamide group Chemical class 0.000 claims 17
- 125000005415 substituted alkoxy group Chemical group 0.000 claims 16
- 125000003545 alkoxy group Chemical group 0.000 claims 15
- 125000004429 atom Chemical group 0.000 claims 15
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 15
- 150000002367 halogens Chemical class 0.000 claims 14
- 125000003342 alkenyl group Chemical group 0.000 claims 13
- 125000000304 alkynyl group Chemical group 0.000 claims 13
- 125000001188 haloalkyl group Chemical group 0.000 claims 13
- 125000005017 substituted alkenyl group Chemical group 0.000 claims 13
- 125000004426 substituted alkynyl group Chemical group 0.000 claims 13
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 12
- 229910052736 halogen Inorganic materials 0.000 claims 11
- 125000004423 acyloxy group Chemical group 0.000 claims 10
- 125000004422 alkyl sulphonamide group Chemical group 0.000 claims 10
- 125000004421 aryl sulphonamide group Chemical group 0.000 claims 10
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 10
- 150000001875 compounds Chemical class 0.000 claims 10
- 125000004001 thioalkyl group Chemical group 0.000 claims 10
- 125000004093 cyano group Chemical group *C#N 0.000 claims 9
- 125000001072 heteroaryl group Chemical group 0.000 claims 9
- 238000000034 method Methods 0.000 claims 8
- 229910052760 oxygen Inorganic materials 0.000 claims 8
- 229910052717 sulfur Inorganic materials 0.000 claims 8
- 125000004432 carbon atom Chemical group C* 0.000 claims 7
- 125000005842 heteroatom Chemical group 0.000 claims 7
- 150000003839 salts Chemical class 0.000 claims 7
- 125000000392 cycloalkenyl group Chemical group 0.000 claims 6
- 125000000753 cycloalkyl group Chemical group 0.000 claims 6
- ZOBPZXTWZATXDG-UHFFFAOYSA-N 1,3-thiazolidine-2,4-dione Chemical group O=C1CSC(=O)N1 ZOBPZXTWZATXDG-UHFFFAOYSA-N 0.000 claims 5
- 125000003118 aryl group Chemical group 0.000 claims 5
- 150000003857 carboxamides Chemical class 0.000 claims 5
- 125000004122 cyclic group Chemical group 0.000 claims 5
- MJAMNJNCEOHYIU-UHFFFAOYSA-N 1,2-oxazolidine-3,4-dione Chemical group O=C1CONC1=O MJAMNJNCEOHYIU-UHFFFAOYSA-N 0.000 claims 4
- 125000002252 acyl group Chemical group 0.000 claims 4
- 229910052799 carbon Inorganic materials 0.000 claims 4
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims 3
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 3
- 201000010099 disease Diseases 0.000 claims 3
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 3
- 239000003937 drug carrier Substances 0.000 claims 3
- 230000009878 intermolecular interaction Effects 0.000 claims 3
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 3
- 125000006413 ring segment Chemical group 0.000 claims 3
- 125000005346 substituted cycloalkyl group Chemical group 0.000 claims 3
- SHGAZHPCJJPHSC-ZVCIMWCZSA-N 9-cis-retinoic acid Chemical compound OC(=O)/C=C(\C)/C=C/C=C(/C)\C=C\C1=C(C)CCCC1(C)C SHGAZHPCJJPHSC-ZVCIMWCZSA-N 0.000 claims 2
- 201000001320 Atherosclerosis Diseases 0.000 claims 2
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 2
- 208000035150 Hypercholesterolemia Diseases 0.000 claims 2
- 230000004913 activation Effects 0.000 claims 2
- 229960001445 alitretinoin Drugs 0.000 claims 2
- WJRBRSLFGCUECM-UHFFFAOYSA-N hydantoin Chemical group O=C1CNC(=O)N1 WJRBRSLFGCUECM-UHFFFAOYSA-N 0.000 claims 2
- UHOVQNZJYSORNB-UHFFFAOYSA-N monobenzene Natural products C1=CC=CC=C1 UHOVQNZJYSORNB-UHFFFAOYSA-N 0.000 claims 2
- 229910052757 nitrogen Inorganic materials 0.000 claims 2
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 2
- 150000002923 oximes Chemical group 0.000 claims 2
- 239000008194 pharmaceutical composition Substances 0.000 claims 2
- 125000005403 thiohaloalkoxy group Chemical group 0.000 claims 2
- 208000001072 type 2 diabetes mellitus Diseases 0.000 claims 2
- XDENVSFWQSKKLZ-UHFFFAOYSA-N 1,2,4-oxadiazolidine-3,5-dione Chemical group O=C1NOC(=O)N1 XDENVSFWQSKKLZ-UHFFFAOYSA-N 0.000 claims 1
- WKBOTKDWSSQWDR-UHFFFAOYSA-N Bromine atom Chemical compound [Br] WKBOTKDWSSQWDR-UHFFFAOYSA-N 0.000 claims 1
- ZAMOUSCENKQFHK-UHFFFAOYSA-N Chlorine atom Chemical compound [Cl] ZAMOUSCENKQFHK-UHFFFAOYSA-N 0.000 claims 1
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical compound FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 claims 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 claims 1
- 241000124008 Mammalia Species 0.000 claims 1
- 241000699670 Mus sp. Species 0.000 claims 1
- YIKSCQDJHCMVMK-UHFFFAOYSA-N Oxamide Chemical group NC(=O)C(N)=O YIKSCQDJHCMVMK-UHFFFAOYSA-N 0.000 claims 1
- OAICVXFJPJFONN-UHFFFAOYSA-N Phosphorus Chemical compound [P] OAICVXFJPJFONN-UHFFFAOYSA-N 0.000 claims 1
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical compound [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims 1
- 229940123464 Thiazolidinedione Drugs 0.000 claims 1
- 206010067584 Type 1 diabetes mellitus Diseases 0.000 claims 1
- 210000001789 adipocyte Anatomy 0.000 claims 1
- 125000000539 amino acid group Chemical group 0.000 claims 1
- 150000001413 amino acids Chemical class 0.000 claims 1
- 238000003556 assay Methods 0.000 claims 1
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims 1
- 239000008280 blood Substances 0.000 claims 1
- 210000004369 blood Anatomy 0.000 claims 1
- GDTBXPJZTBHREO-UHFFFAOYSA-N bromine Substances BrBr GDTBXPJZTBHREO-UHFFFAOYSA-N 0.000 claims 1
- 229910052794 bromium Inorganic materials 0.000 claims 1
- 239000000460 chlorine Substances 0.000 claims 1
- 229910052801 chlorine Inorganic materials 0.000 claims 1
- 229940125904 compound 1 Drugs 0.000 claims 1
- 230000004069 differentiation Effects 0.000 claims 1
- 239000011737 fluorine Substances 0.000 claims 1
- 229910052731 fluorine Inorganic materials 0.000 claims 1
- 125000000524 functional group Chemical group 0.000 claims 1
- 239000008103 glucose Substances 0.000 claims 1
- 125000001183 hydrocarbyl group Chemical group 0.000 claims 1
- DWRDBJCTLDOPFZ-UHFFFAOYSA-N imidazole-2,4-dione Chemical compound O=C1NC(=O)N=C1 DWRDBJCTLDOPFZ-UHFFFAOYSA-N 0.000 claims 1
- PNDPGZBMCMUPRI-UHFFFAOYSA-N iodine Chemical compound II PNDPGZBMCMUPRI-UHFFFAOYSA-N 0.000 claims 1
- 239000003446 ligand Substances 0.000 claims 1
- 239000001301 oxygen Substances 0.000 claims 1
- 125000004430 oxygen atom Chemical group O* 0.000 claims 1
- 125000001997 phenyl group Chemical class [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 1
- 239000011574 phosphorus Substances 0.000 claims 1
- 229910052698 phosphorus Inorganic materials 0.000 claims 1
- 125000000714 pyrimidinyl group Chemical group 0.000 claims 1
- 125000003107 substituted aryl group Chemical group 0.000 claims 1
- 239000011593 sulfur Substances 0.000 claims 1
- 125000004434 sulfur atom Chemical group 0.000 claims 1
- UFTFJSFQGQCHQW-UHFFFAOYSA-N triformin Chemical compound O=COCC(OC=O)COC=O UFTFJSFQGQCHQW-UHFFFAOYSA-N 0.000 claims 1
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US27434201P | 2001-03-08 | 2001-03-08 | |
| PCT/US2002/007342 WO2002072543A2 (en) | 2001-03-08 | 2002-03-08 | Rxr activating molecules |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2004523571A JP2004523571A (ja) | 2004-08-05 |
| JP2004523571A5 true JP2004523571A5 (https=) | 2005-12-22 |
Family
ID=23047783
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2002571459A Pending JP2004523571A (ja) | 2001-03-08 | 2002-03-08 | Ｒｘｒ活性化分子 |
Country Status (6)
| Country | Link |
|---|---|
| US (2) | US7265139B2 (https=) |
| EP (1) | EP1377559A4 (https=) |
| JP (1) | JP2004523571A (https=) |
| AU (1) | AU2002254171A2 (https=) |
| CA (1) | CA2473156A1 (https=) |
| WO (1) | WO2002072543A2 (https=) |
Families Citing this family (17)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2003508391A (ja) | 1999-08-31 | 2003-03-04 | マキシア・ファーマシューティカルズ・インコーポレイテッド | ベンジリデン−チアゾリジンジオン類およびアナログ類ならびに糖尿病の治療におけるその使用 |
| AU2002252227A1 (en) | 2001-03-07 | 2002-09-24 | Maxia Pharmaceuticals, Inc. | Heterocyclic derivatives for the treatment of cancer and other proliferative diseases |
| JP2004523571A (ja) * | 2001-03-08 | 2004-08-05 | マキシア・ファーマシューティカルズ・インコーポレイテッド | Ｒｘｒ活性化分子 |
| WO2003016267A1 (en) * | 2001-08-17 | 2003-02-27 | Incyte San Diego Incorporated | Oxime derivatives for the treatment of dyslipidemia and hypercholesteremia |
| JP2005513026A (ja) | 2001-11-15 | 2005-05-12 | インサイト サン ディエゴ インコーポレイテッド | 高コレステロール血症、異脂肪血症および他の代謝障害；癌、および他の疾患を治療するｎ−置換複素環 |
| US7102000B2 (en) * | 2002-03-08 | 2006-09-05 | Incyte San Diego Inc. | Heterocyclic amide derivatives for the treatment of diabetes and other diseases |
| US7196108B2 (en) * | 2002-03-08 | 2007-03-27 | Incyte San Diego Inc. | Bicyclic heterocycles for the treatment of diabetes and other diseases |
| US20050038098A1 (en) * | 2003-04-18 | 2005-02-17 | Catherine Tachdjian | Substituted dihydronaphthalene and isochroman compounds for the treatment of metabolic disorders, cancer and other diseases |
| WO2005100396A1 (en) * | 2004-04-16 | 2005-10-27 | Bayer Healthcare Ag | Diagnostics and therapeutics for diseases associated with retinoid x receptor alpha (rxra) |
| WO2005101006A2 (en) * | 2004-04-16 | 2005-10-27 | Bayer Healthcare Ag | Diagnostics and therapeutics for diseases associated with retinoid x receptor beta (rxrb) |
| EP1937641A2 (en) * | 2005-09-30 | 2008-07-02 | Janssen Pharmaceutica, N.V. | Dihydro-[1h]-quinolin-2-one derivatives as rxr agonists for the treatment of dyslipidemia, hypercholesterolemia and diabetes |
| MX2009013332A (es) | 2007-06-08 | 2010-01-25 | Mannkind Corp | Inhibidores de ire-1 alfa. |
| EP2345409A4 (en) * | 2008-09-22 | 2012-03-28 | Univ Kagoshima | TREATMENT AGENT FOR T-CELL LEUKEMIA IN ADULTS |
| WO2010074807A1 (en) * | 2008-10-30 | 2010-07-01 | Gilead Palo Alto, Inc. | 3, 4-dihydroquinolin-2 ( 1h ) -one derivatives as sodium channel modulators |
| BR112020018094A2 (pt) | 2018-03-08 | 2020-12-22 | Incyte Corporation | Compostos de aminopirazina diol como inibidores de pi3k-¿ |
| US11046658B2 (en) | 2018-07-02 | 2021-06-29 | Incyte Corporation | Aminopyrazine derivatives as PI3K-γ inhibitors |
| CN109628328B (zh) * | 2019-01-11 | 2022-02-15 | 河南省农业科学院植物保护研究所 | 一株能够防治芝麻枯萎病且具有促生和诱导抗性作用的拜赖青霉及其筛选方法和应用 |
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| US4051842A (en) * | 1975-09-15 | 1977-10-04 | International Medical Corporation | Electrode and interfacing pad for electrical physiological systems |
| DE2626348C3 (de) * | 1976-06-11 | 1980-01-31 | Siemens Ag, 1000 Berlin Und 8000 Muenchen | Implantierbare Dosiereinrichtung |
| JPS5538359A (en) | 1978-09-12 | 1980-03-17 | Hamari Yakuhin Kogyo Kk | Preparation of 2-(3-benzoylphenyl)-propionic acid |
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| JP2003508391A (ja) | 1999-08-31 | 2003-03-04 | マキシア・ファーマシューティカルズ・インコーポレイテッド | ベンジリデン−チアゾリジンジオン類およびアナログ類ならびに糖尿病の治療におけるその使用 |
| FR2812876B1 (fr) * | 2000-08-08 | 2002-09-27 | Galderma Res & Dev | Nouveaux composes bi-aromatiques activateurs des recepteurs de type ppar-gamma et leur utilisation dans des compositions cosmetiques ou pharmaceutiques |
| AU2002252227A1 (en) * | 2001-03-07 | 2002-09-24 | Maxia Pharmaceuticals, Inc. | Heterocyclic derivatives for the treatment of cancer and other proliferative diseases |
| JP2004523571A (ja) | 2001-03-08 | 2004-08-05 | マキシア・ファーマシューティカルズ・インコーポレイテッド | Ｒｘｒ活性化分子 |
| DE60204674T2 (de) | 2001-03-14 | 2006-05-18 | Eli Lilly And Co., Indianapolis | Retinoid x rezeptormodulatoren |
| WO2002080935A1 (en) | 2001-04-04 | 2002-10-17 | Ortho Mcneil Pharmaceutical, Inc. | Combination therapy comprising glucose reabsorption inhibitors and retinoid-x receptor modulators |
| WO2003016267A1 (en) * | 2001-08-17 | 2003-02-27 | Incyte San Diego Incorporated | Oxime derivatives for the treatment of dyslipidemia and hypercholesteremia |
| JP2005513026A (ja) * | 2001-11-15 | 2005-05-12 | インサイト サン ディエゴ インコーポレイテッド | 高コレステロール血症、異脂肪血症および他の代謝障害；癌、および他の疾患を治療するｎ−置換複素環 |
| AR037714A1 (es) * | 2001-12-06 | 2004-12-01 | Maxia Pharmaceuticals Inc | Derivados de tiazolidinona y oxazolidinona 2-sustituidos para la inhibicion de fosfatasas y el tratamiento de cancer |
| US7196108B2 (en) * | 2002-03-08 | 2007-03-27 | Incyte San Diego Inc. | Bicyclic heterocycles for the treatment of diabetes and other diseases |
| US7102000B2 (en) * | 2002-03-08 | 2006-09-05 | Incyte San Diego Inc. | Heterocyclic amide derivatives for the treatment of diabetes and other diseases |
| US20050014767A1 (en) * | 2003-01-29 | 2005-01-20 | Magnus Pfahl | Benzoxazole, benzothiazole, and benzimidazole derivatives for the treatment of cancer and other diseases |
| US20050038098A1 (en) * | 2003-04-18 | 2005-02-17 | Catherine Tachdjian | Substituted dihydronaphthalene and isochroman compounds for the treatment of metabolic disorders, cancer and other diseases |
-
2002
- 2002-03-08 JP JP2002571459A patent/JP2004523571A/ja active Pending
- 2002-03-08 CA CA002473156A patent/CA2473156A1/en not_active Abandoned
- 2002-03-08 US US10/098,184 patent/US7265139B2/en not_active Expired - Fee Related
- 2002-03-08 EP EP02723389A patent/EP1377559A4/en not_active Withdrawn
- 2002-03-08 WO PCT/US2002/007342 patent/WO2002072543A2/en not_active Ceased
- 2002-03-08 AU AU2002254171A patent/AU2002254171A2/en not_active Abandoned
-
2005
- 2005-03-01 US US11/069,930 patent/US20050209286A1/en not_active Abandoned
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