JP2010512342A5 - - Google Patents
Download PDFInfo
- Publication number
- JP2010512342A5 JP2010512342A5 JP2009540497A JP2009540497A JP2010512342A5 JP 2010512342 A5 JP2010512342 A5 JP 2010512342A5 JP 2009540497 A JP2009540497 A JP 2009540497A JP 2009540497 A JP2009540497 A JP 2009540497A JP 2010512342 A5 JP2010512342 A5 JP 2010512342A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- independently
- halogen
- optionally substituted
- haloalkyl
- 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
Links
- 150000001875 compounds Chemical class 0.000 claims description 93
- 125000000217 alkyl group Chemical group 0.000 claims description 74
- 229910052736 halogen Inorganic materials 0.000 claims description 52
- 150000002367 halogens Chemical class 0.000 claims description 52
- -1 chloro, methyl Chemical group 0.000 claims description 28
- 125000004093 cyano group Chemical group *C#N 0.000 claims description 25
- 125000000623 heterocyclic group Chemical group 0.000 claims description 24
- 229910052739 hydrogen Inorganic materials 0.000 claims description 23
- 239000001257 hydrogen Substances 0.000 claims description 23
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 20
- 125000001072 heteroaryl group Chemical group 0.000 claims description 18
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 18
- 150000002431 hydrogen Chemical class 0.000 claims description 17
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims description 16
- 125000003118 aryl group Chemical group 0.000 claims description 14
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 10
- 125000004043 oxo group Chemical group O=* 0.000 claims description 9
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims description 7
- 125000001931 aliphatic group Chemical group 0.000 claims description 7
- 125000004104 aryloxy group Chemical group 0.000 claims description 7
- 125000004429 atom Chemical group 0.000 claims description 7
- 125000002883 imidazolyl group Chemical group 0.000 claims description 7
- 125000000842 isoxazolyl group Chemical group 0.000 claims description 7
- 125000003226 pyrazolyl group Chemical group 0.000 claims description 7
- 125000000168 pyrrolyl group Chemical group 0.000 claims description 7
- 125000001544 thienyl group Chemical group 0.000 claims description 7
- 125000003545 alkoxy group Chemical group 0.000 claims description 6
- 206010012601 diabetes mellitus Diseases 0.000 claims description 6
- 208000035475 disorder Diseases 0.000 claims description 6
- 150000003839 salts Chemical class 0.000 claims description 6
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims description 6
- 229910052799 carbon Inorganic materials 0.000 claims description 5
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims description 5
- 125000001511 cyclopentyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims description 5
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims description 5
- 125000000719 pyrrolidinyl group Chemical group 0.000 claims description 5
- 125000001153 fluoro group Chemical group F* 0.000 claims description 4
- 125000002541 furyl group Chemical group 0.000 claims description 4
- 229910052757 nitrogen Inorganic materials 0.000 claims description 4
- 125000002971 oxazolyl group Chemical group 0.000 claims description 4
- 125000000335 thiazolyl group Chemical group 0.000 claims description 4
- 125000004504 1,2,4-oxadiazolyl group Chemical group 0.000 claims description 3
- 125000004506 1,2,5-oxadiazolyl group Chemical group 0.000 claims description 3
- 125000001781 1,3,4-oxadiazolyl group Chemical group 0.000 claims description 3
- 201000001320 Atherosclerosis Diseases 0.000 claims description 3
- 208000008589 Obesity Diseases 0.000 claims description 3
- 125000002102 aryl alkyloxo group Chemical group 0.000 claims description 3
- 125000005160 aryl oxy alkyl group Chemical group 0.000 claims description 3
- 125000002393 azetidinyl group Chemical group 0.000 claims description 3
- 235000020824 obesity Nutrition 0.000 claims description 3
- 125000003386 piperidinyl group Chemical group 0.000 claims description 3
- 125000003373 pyrazinyl group Chemical group 0.000 claims description 3
- 125000004076 pyridyl group Chemical group 0.000 claims description 3
- 125000000714 pyrimidinyl group Chemical group 0.000 claims description 3
- 125000001412 tetrahydropyranyl group Chemical group 0.000 claims description 3
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 claims description 2
- 208000024827 Alzheimer disease Diseases 0.000 claims description 2
- 208000024172 Cardiovascular disease Diseases 0.000 claims description 2
- 208000032928 Dyslipidaemia Diseases 0.000 claims description 2
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 2
- 208000035150 Hypercholesterolemia Diseases 0.000 claims description 2
- 208000031226 Hyperlipidaemia Diseases 0.000 claims description 2
- 206010061218 Inflammation Diseases 0.000 claims description 2
- 208000017170 Lipid metabolism disease Diseases 0.000 claims description 2
- 206010049287 Lipodystrophy acquired Diseases 0.000 claims description 2
- 206010028980 Neoplasm Diseases 0.000 claims description 2
- 208000018737 Parkinson disease Diseases 0.000 claims description 2
- 125000004171 alkoxy aryl group Chemical group 0.000 claims description 2
- 125000003710 aryl alkyl group Chemical group 0.000 claims description 2
- 230000037365 barrier function of the epidermis Effects 0.000 claims description 2
- 201000011510 cancer Diseases 0.000 claims description 2
- 201000001883 cholelithiasis Diseases 0.000 claims description 2
- 125000000392 cycloalkenyl group Chemical group 0.000 claims description 2
- 230000004069 differentiation Effects 0.000 claims description 2
- 239000003937 drug carrier Substances 0.000 claims description 2
- 210000002615 epidermis Anatomy 0.000 claims description 2
- 201000001421 hyperglycemia Diseases 0.000 claims description 2
- 208000020346 hyperlipoproteinemia Diseases 0.000 claims description 2
- 208000006575 hypertriglyceridemia Diseases 0.000 claims description 2
- 208000026278 immune system disease Diseases 0.000 claims description 2
- 230000004054 inflammatory process Effects 0.000 claims description 2
- 125000001786 isothiazolyl group Chemical group 0.000 claims description 2
- 150000002632 lipids Chemical class 0.000 claims description 2
- 208000006132 lipodystrophy Diseases 0.000 claims description 2
- 210000003491 skin Anatomy 0.000 claims description 2
- 208000024891 symptom Diseases 0.000 claims description 2
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 claims 17
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 6
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims 6
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 3
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims 3
- 125000000852 azido group Chemical group *N=[N+]=[N-] 0.000 claims 1
- 239000003112 inhibitor Substances 0.000 claims 1
- 210000004877 mucosa Anatomy 0.000 claims 1
- 230000002265 prevention Effects 0.000 claims 1
- 125000001188 haloalkyl group Chemical group 0.000 description 23
- 125000003342 alkenyl group Chemical group 0.000 description 10
- 125000000304 alkynyl group Chemical group 0.000 description 6
- 238000000034 method Methods 0.000 description 6
- 108020005497 Nuclear hormone receptor Proteins 0.000 description 4
- 201000010099 disease Diseases 0.000 description 4
- 102000006255 nuclear receptors Human genes 0.000 description 4
- 108020004017 nuclear receptors Proteins 0.000 description 4
- 230000000694 effects Effects 0.000 description 3
- 125000006163 5-membered heteroaryl group Chemical group 0.000 description 2
- 208000023275 Autoimmune disease Diseases 0.000 description 2
- 125000005157 alkyl carboxy group Chemical group 0.000 description 2
- 125000001309 chloro group Chemical group Cl* 0.000 description 2
- 125000005879 dioxolanyl group Chemical group 0.000 description 2
- 125000005411 dithiolanyl group Chemical group S1SC(CC1)* 0.000 description 2
- 125000002632 imidazolidinyl group Chemical group 0.000 description 2
- 125000002636 imidazolinyl group Chemical group 0.000 description 2
- 230000004060 metabolic process Effects 0.000 description 2
- 125000001715 oxadiazolyl group Chemical group 0.000 description 2
- 125000005880 oxathiolanyl group Chemical group 0.000 description 2
- 125000000160 oxazolidinyl group Chemical group 0.000 description 2
- 125000005968 oxazolinyl group Chemical group 0.000 description 2
- 125000003831 tetrazolyl group Chemical group 0.000 description 2
- 125000001113 thiadiazolyl group Chemical group 0.000 description 2
- 125000001984 thiazolidinyl group Chemical group 0.000 description 2
- 125000002769 thiazolinyl group Chemical group 0.000 description 2
- 125000001425 triazolyl group Chemical group 0.000 description 2
- 206010020772 Hypertension Diseases 0.000 description 1
- 206010022489 Insulin Resistance Diseases 0.000 description 1
- 208000001145 Metabolic Syndrome Diseases 0.000 description 1
- 201000000690 abdominal obesity-metabolic syndrome Diseases 0.000 description 1
- 125000004445 cyclohaloalkyl Chemical group 0.000 description 1
- 208000035474 group of disease Diseases 0.000 description 1
- 230000003463 hyperproliferative effect Effects 0.000 description 1
- 230000036039 immunity Effects 0.000 description 1
- 230000001771 impaired effect Effects 0.000 description 1
- 230000002401 inhibitory effect Effects 0.000 description 1
- 210000004400 mucous membrane Anatomy 0.000 description 1
- DYMRYCZRMAHYKE-UHFFFAOYSA-N n-diazonitramide Chemical compound [O-][N+](=O)N=[N+]=[N-] DYMRYCZRMAHYKE-UHFFFAOYSA-N 0.000 description 1
- 125000003566 oxetanyl group Chemical group 0.000 description 1
- SNOOUWRIMMFWNE-UHFFFAOYSA-M sodium;6-[(3,4,5-trimethoxybenzoyl)amino]hexanoate Chemical compound [Na+].COC1=CC(C(=O)NCCCCCC([O-])=O)=CC(OC)=C1OC SNOOUWRIMMFWNE-UHFFFAOYSA-M 0.000 description 1
- 229910052717 sulfur Inorganic materials 0.000 description 1
- 208000001072 type 2 diabetes mellitus Diseases 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US86919806P | 2006-12-08 | 2006-12-08 | |
| US60/869,198 | 2006-12-08 | ||
| PCT/US2007/086787 WO2008073825A1 (en) | 2006-12-08 | 2007-12-07 | Lxr and fxr modulators |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2010512342A JP2010512342A (ja) | 2010-04-22 |
| JP2010512342A5 true JP2010512342A5 (enExample) | 2012-01-26 |
| JP5399262B2 JP5399262B2 (ja) | 2014-01-29 |
Family
ID=39315799
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2009540497A Expired - Fee Related JP5399262B2 (ja) | 2006-12-08 | 2007-12-07 | Ｌｘｒおよびｆｘｒのモジュレーター |
Country Status (8)
| Country | Link |
|---|---|
| US (1) | US7998995B2 (enExample) |
| EP (1) | EP2121621B1 (enExample) |
| JP (1) | JP5399262B2 (enExample) |
| KR (1) | KR20090094125A (enExample) |
| CN (1) | CN101679297B (enExample) |
| AU (1) | AU2007333194A1 (enExample) |
| NO (1) | NO20092587L (enExample) |
| WO (1) | WO2008073825A1 (enExample) |
Families Citing this family (103)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE602004000260T2 (de) | 2003-07-22 | 2006-08-24 | Arena Pharmaceuticals, Inc., San Diego | Diaryl- und arylheteroarylharnstoffderivate als modulatoren des 5-ht2a-serotoninrezeptors, die sich zur prophylaxe und behandlung von damit im zusammenhang stehenden erkrankungen eignen |
| PL1879573T3 (pl) | 2005-05-10 | 2013-05-31 | Incyte Holdings Corp | Modulatory 2,3-dioksygenazy indoloaminy i sposoby ich zastosowania |
| BRPI0612287A8 (pt) | 2005-06-27 | 2019-01-22 | Exelixis Inc | composição para uso farmacêutico no tratamento de doenças através da medicina nuclear e métodos de uso e para modulação de atividade de receptor nuclear |
| US8450351B2 (en) | 2005-12-20 | 2013-05-28 | Incyte Corporation | N-hydroxyamidinoheterocycles as modulators of indoleamine 2,3-dioxygenase |
| CL2007002650A1 (es) | 2006-09-19 | 2008-02-08 | Incyte Corp | Compuestos derivados de heterociclo n-hidroxiamino; composicion farmaceutica, util para tratar cancer, infecciones virales y desordenes neurodegenerativos entre otras. |
| WO2008036642A2 (en) | 2006-09-19 | 2008-03-27 | Incyte Corporation | N-hydroxyamidinoheterocycles as modulators of indoleamine 2,3-dioxygenase |
| TWI415845B (zh) | 2006-10-03 | 2013-11-21 | Arena Pharm Inc | 用於治療與５-ｈｔ2ａ血清素受體相關聯病症之作為５-ｈｔ2ａ血清素受體之調節劑的吡唑衍生物 |
| EP2167464B1 (en) * | 2007-05-25 | 2014-12-03 | AbbVie Deutschland GmbH & Co KG | Heterocyclic compounds as positive modulators of metabotropic glutamate receptor 2 (mglu2 receptor) |
| HRP20151052T1 (xx) | 2007-07-19 | 2015-11-06 | H. Lundbeck A/S | Peteroäślani heterocikliäśki amidi i srodne tvari |
| JP5393677B2 (ja) | 2007-08-15 | 2014-01-22 | 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 | ５−ＨＴ２Ａセロトニン受容体に関連した障害の治療のための５−ＨＴ２Ａセロトニン受容体のモジュレーターとしてのイミダゾ［１，２−ａ］ピリジン誘導体 |
| US20110021538A1 (en) | 2008-04-02 | 2011-01-27 | Arena Pharmaceuticals, Inc. | Processes for the preparation of pyrazole derivatives useful as modulators of the 5-ht2a serotonin receptor |
| JP5465720B2 (ja) | 2008-07-08 | 2014-04-09 | インサイト・コーポレイション | インドールアミン２，３−ジオキシゲナーゼの阻害剤としての１，２，５−オキサジアゾール |
| TWI392673B (zh) * | 2008-08-27 | 2013-04-11 | Calcimedica Inc | 調控細胞內鈣離子濃度之化合物 |
| EA022417B1 (ru) * | 2008-10-21 | 2015-12-30 | Саймабэй Терапевтикс, Инк. | Арильные агонисты рецептора gpr120 и их применение |
| US9126946B2 (en) | 2008-10-28 | 2015-09-08 | Arena Pharmaceuticals, Inc. | Processes useful for the preparation of 1-[3-(4-bromo-2-methyl-2H-pyrazol-3-yl)-4-methoxy-phenyl]-3-(2,4-difluoro-phenyl)urea and crystalline forms related thereto |
| CA2741731A1 (en) | 2008-10-28 | 2010-06-03 | Arena Pharmaceuticals, Inc. | Compositions of a 5-ht2a serotonin receptor modulator useful for the treatment of disorders related thereto |
| US8853202B2 (en) | 2008-11-04 | 2014-10-07 | Chemocentryx, Inc. | Modulators of CXCR7 |
| CA2742515C (en) * | 2008-11-04 | 2017-07-11 | Chemocentryx, Inc. | 1,4-diazepane modulators of cxcr7 |
| AR074760A1 (es) | 2008-12-18 | 2011-02-09 | Metabolex Inc | Agonistas del receptor gpr120 y usos de los mismos en medicamentos para el tratamiento de diabetes y el sindrome metabolico. |
| WO2010117090A1 (en) * | 2009-04-10 | 2010-10-14 | Banyu Pharmaceutical Co.,Ltd. | Novel isoquinolinyloxymethyl heteroaryl derivatives |
| KR101676704B1 (ko) * | 2009-05-28 | 2016-11-16 | 엑셀리시스 페이턴트 컴퍼니 엘엘씨 | Ｌｘｒ 조절자 |
| GB0910003D0 (en) * | 2009-06-11 | 2009-07-22 | Univ Leuven Kath | Novel compounds for the treatment of neurodegenerative diseases |
| DE102009043260A1 (de) * | 2009-09-28 | 2011-04-28 | Merck Patent Gmbh | Pyridinyl-imidazolonderivate |
| CA2777782C (en) | 2009-10-15 | 2016-06-28 | Children's Medical Center Corporation | Sepiapterin reductase inhibitors for the treatment of pain |
| WO2011107494A1 (de) | 2010-03-03 | 2011-09-09 | Sanofi | Neue aromatische glykosidderivate, diese verbindungen enthaltende arzneimittel und deren verwendung |
| US8252826B2 (en) * | 2010-03-24 | 2012-08-28 | Hoffmann-La Roche Inc. | Cyclopentyl- and cycloheptylpyrazoles |
| US8299117B2 (en) | 2010-06-16 | 2012-10-30 | Metabolex Inc. | GPR120 receptor agonists and uses thereof |
| EP2582709B1 (de) | 2010-06-18 | 2018-01-24 | Sanofi | Azolopyridin-3-on-derivate als inhibitoren von lipasen und phospholipasen |
| WO2012033353A2 (ko) | 2010-09-07 | 2012-03-15 | 서울대학교 산학협력단 | 세스터터핀 화합물 및 이들 물질의 용도 |
| ES2541289T3 (es) | 2010-12-01 | 2015-07-17 | Nissan Chemical Industries, Ltd. | Compuestos de pirazol que tienen un efecto terapéutico sobre mieloma múltiple |
| AR088728A1 (es) * | 2011-03-25 | 2014-07-02 | Bristol Myers Squibb Co | Moduladores de lxr como prodroga de imidazol |
| JP2014527511A (ja) | 2011-06-24 | 2014-10-16 | アムジエン・インコーポレーテツド | Ｔｒｐｍ８拮抗剤及び治療におけるそれらの使用 |
| EP2723718A1 (en) | 2011-06-24 | 2014-04-30 | Amgen Inc. | Trpm8 antagonists and their use in treatments |
| EP2545964A1 (en) | 2011-07-13 | 2013-01-16 | Phenex Pharmaceuticals AG | Novel FXR (NR1H4) binding and activity modulating compounds |
| WO2013037482A1 (en) | 2011-09-15 | 2013-03-21 | Phenex Pharmaceuticals Ag | Farnesoid x receptor agonists for cancer treatment and prevention |
| US9289365B2 (en) * | 2011-10-24 | 2016-03-22 | Avon Products, Inc. | Compositions and methods for stimulating collagen synthesis in the skin |
| CN103087041B (zh) * | 2011-11-02 | 2014-06-18 | 中国中化股份有限公司 | 含二芳醚的吡唑酰胺类化合物作为农用杀菌剂的用途 |
| AU2012334066A1 (en) * | 2011-11-09 | 2014-05-22 | Grunenthal Gmbh | Substituted pyrazolyl-based carboxamide and urea derivatives bearing a phenyl moiety substituted with an N-containing group as vanilloid receptor ligands |
| HK1201839A1 (en) * | 2011-11-09 | 2015-09-11 | Grünenthal GmbH | Substituted pyrazolyl-based carboxamide and urea derivatives bearing a phenyl moiety substituted with an o-containing group as vanilloid receptor ligands |
| SG10201607345YA (en) | 2012-03-02 | 2016-11-29 | Ralexar Therapeutics Inc | Liver x receptor (lxr) modulators for the treatment of dermal diseases, disorders and conditions |
| CN104271562B (zh) | 2012-05-07 | 2017-03-15 | 株式会社经农 | 经氨基甲酸酯取代的二氨基芳基衍生物及包含所述衍生物的杀虫组合物 |
| US8952009B2 (en) | 2012-08-06 | 2015-02-10 | Amgen Inc. | Chroman derivatives as TRPM8 inhibitors |
| AU2013302861A1 (en) | 2012-08-13 | 2015-03-05 | The Rockefeller University | Treatment and diagnosis of melanoma |
| MX359651B (es) | 2012-11-29 | 2018-10-05 | Chemocentryx Inc | Antagonistas de cxcr7. |
| CA2894399A1 (en) | 2012-12-06 | 2014-06-12 | Quanticel Pharmaceuticals, Inc. | Histone demethylase inhibitors |
| ES2753386T3 (es) | 2013-03-13 | 2020-04-08 | Forma Therapeutics Inc | Derivados de 2-hidroxi-1-{4-[(4-fenil)fenil]carbonil}piperazin-1-il}etano-1-ona y compuestos relacionados como inhibidores de sintasa de ácido graso (FASN) para el tratamiento del cáncer |
| JP6456909B2 (ja) * | 2013-03-15 | 2019-01-23 | ブリストル−マイヤーズ スクイブ カンパニーＢｒｉｓｔｏｌ−Ｍｙｅｒｓ Ｓｑｕｉｂｂ Ｃｏｍｐａｎｙ | Ｌｘｒ調節因子 |
| CN105209039B (zh) * | 2013-03-15 | 2018-06-22 | 百时美施贵宝公司 | Lxr调节剂 |
| GB2513403A (en) * | 2013-04-26 | 2014-10-29 | Agency Science Tech & Res | WNT pathway modulators |
| JP2016532713A (ja) * | 2013-09-04 | 2016-10-20 | アレクサー セラピューティクス， インク． | 肝臓ｘ受容体（ｌｘｒ）調節因子 |
| RS60479B1 (sr) * | 2013-09-04 | 2020-08-31 | Ellora Therapeutics Inc | Modulatori receptora x jetre (lxr) |
| SI3043865T1 (sl) | 2013-09-11 | 2021-04-30 | Institut National De La Sante Et De La Recherche Medicale (Inserm) | Metode in farmacevtski sestavki za zdravljenje virusne okužbe s hepatitisom B |
| ES2799582T3 (es) | 2013-11-08 | 2020-12-18 | Incyte Holdings Corp | Proceso para la síntesis de un inhibidor de indoleamina 2,3-dioxigenasa |
| EP3092226B1 (en) | 2014-01-10 | 2019-03-13 | Aurigene Discovery Technologies Limited | Indazole compounds as irak4 inhibitors |
| WO2015106164A1 (en) | 2014-01-10 | 2015-07-16 | Rgenix, Inc. | Lxr agonists and uses thereof |
| LT3466955T (lt) | 2014-01-13 | 2021-02-25 | Aurigene Discovery Technologies Limited | Oksazol[4,5-b]piridino ir tiazol[4,5-b]piridino darinių, kaip irak4 inhibitorių, skirtų vėžio gydymui, gamybos būdas |
| KR102736869B1 (ko) | 2014-03-07 | 2024-12-02 | 바이오크리스트파마슈티컬즈,인코포레이티드 | 인간 혈장 칼리크레인 저해제 |
| US10301268B2 (en) | 2014-03-13 | 2019-05-28 | The Salk Institute For Biological Studies | Analogs of fexaramine and methods of making and using |
| US10077268B2 (en) | 2014-03-13 | 2018-09-18 | Salk Institute For Biological Studies | FXR agonists and methods for making and using |
| CN104045635A (zh) * | 2014-06-23 | 2014-09-17 | 华东理工大学 | 3,4,5-三取代异恶唑类化合物及其用途 |
| WO2016092375A1 (en) * | 2014-12-11 | 2016-06-16 | Zenith Epigenetics Corp. | Substituted heterocycles as bromodomain inhibitors |
| EP3034499A1 (en) * | 2014-12-17 | 2016-06-22 | Gilead Sciences, Inc. | Novel FXR (NR1H4) modulating compounds |
| EA036404B1 (ru) | 2015-02-06 | 2020-11-06 | Интерсепт Фармасьютикалз, Инк. | Фармацевтические композиции для комбинированной терапии |
| TWI698430B (zh) * | 2015-02-13 | 2020-07-11 | 南北兄弟藥業投資有限公司 | 三環化合物及其在藥物中的應用 |
| JP2018510866A (ja) * | 2015-03-13 | 2018-04-19 | ソーク インスティテュート フォー バイオロジカル スタディーズ | 腸受容体を活性化させるための、ファルネソイドｘ受容体アゴニストでの、成体の潜在性自己免疫性糖尿病の治療 |
| EP3715348A1 (en) | 2015-03-26 | 2020-09-30 | Akarna Therapeutics, Ltd. | Fused bicyclic compounds for the treatment of disease |
| CR20170456A (es) | 2015-04-07 | 2018-06-13 | Intercept Pharmaceuticals Inc | Composiciones farmacéuticas para terapias combinadas |
| US10022355B2 (en) | 2015-06-12 | 2018-07-17 | Axovant Sciences Gmbh | Diaryl and arylheteroaryl urea derivatives as modulators of the 5-HT2A serotonin receptor useful for the prophylaxis and treatment of REM sleep behavior disorder |
| BR112018000728A2 (pt) | 2015-07-15 | 2018-09-04 | Axovant Sciences Gmbh | resumo método para a profilaxia e/ou tratamento de alucinações visuais em um sujeito com necessidade do mesmo |
| EP3402477A4 (en) | 2016-01-11 | 2019-08-21 | The Rockefeller University | METHOD FOR THE TREATMENT OF DISEASES RELATED TO MYELOID-DERIVED SUPPRESSOR CELLS |
| KR20190040140A (ko) * | 2016-05-25 | 2019-04-17 | 아카나 테라퓨틱스, 엘티디. | 질환의 치료를 위한 융합된 비시클릭 화합물 |
| NZ748641A (en) | 2016-06-13 | 2020-04-24 | Gilead Sciences Inc | Fxr (nr1h4) modulating compounds |
| CA2968836C (en) | 2016-06-13 | 2025-09-02 | Gilead Sciences, Inc. | FXR MODULATING COMPOUNDS (NR1H4) |
| TW201808283A (zh) * | 2016-08-05 | 2018-03-16 | 廣東東陽光藥業有限公司 | 含氮三環化合物及其在藥物中的應用 |
| CN108059607B (zh) * | 2016-11-09 | 2020-11-17 | 中国科学院上海药物研究所 | 亚砜基乙酸或砜基乙酸类衍生物、其药物组合物、制备方法和用途 |
| SI4122464T1 (sl) | 2017-03-28 | 2024-07-31 | Gilead Sciences, Inc. | Terapevtske kombinacije za zdravljenje bolezni jeter |
| WO2018178260A1 (en) | 2017-03-30 | 2018-10-04 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Methods and pharmaceutical compositions for reducing persistence and expression of episomal viruses |
| EP3600270B1 (en) | 2017-03-31 | 2023-06-14 | Aurigene Oncology Limited | Compounds and compositions for treating hematological disorders |
| WO2018213082A1 (en) | 2017-05-18 | 2018-11-22 | Regeneron Pharmaceuticals, Inc. | Bis-octahydrophenanthrene carboxamides and protein conjugates thereof |
| HUE067356T2 (hu) | 2017-10-31 | 2024-10-28 | Curis Inc | IRAK4 inhibitor és BCL-2 inhibitor kombinációban, rák kezelésére való felhasználásra |
| CA3081424A1 (en) * | 2017-11-01 | 2019-05-09 | Bristol-Myers Squibb Company | Spirocyclic compounds as farnesoid x receptor modulators |
| CA3078981A1 (en) | 2017-11-21 | 2019-05-31 | Rgenix, Inc. | Polymorphs and uses thereof |
| TWI767148B (zh) | 2018-10-10 | 2022-06-11 | 美商弗瑪治療公司 | 抑制脂肪酸合成酶(fasn) |
| US10793554B2 (en) | 2018-10-29 | 2020-10-06 | Forma Therapeutics, Inc. | Solid forms of 4-(2-fluoro-4-(1-methyl-1H-benzo[d]imidazol-5-yl)benzoyl)piperazin-1-yl)(1-hydroxycyclopropyl)methanone |
| IL283313B2 (en) * | 2018-11-20 | 2025-08-01 | Regeneron Pharma | Bis-octahydrophenanthrene carboxamide derivatives and protein conjugates thereof for use as lxr agonists |
| CA3121202A1 (en) | 2018-11-30 | 2020-06-04 | Nuvation Bio Inc. | Pyrrole and pyrazole compounds and methods of use thereof |
| MX2021006915A (es) | 2018-12-12 | 2021-08-24 | Chemocentryx Inc | Inhibidores de cxcr7 para el tratamiento de cancer. |
| PT3911647T (pt) | 2019-01-15 | 2024-03-04 | Gilead Sciences Inc | Composto de isoxazole como agonista de fxr e composições farmacêuticas que o contenham |
| JP2022519906A (ja) | 2019-02-19 | 2022-03-25 | ギリアード サイエンシーズ， インコーポレイテッド | Ｆｘｒアゴニストの固体形態 |
| SG11202113155XA (en) | 2019-05-30 | 2021-12-30 | Intercept Pharmaceuticals Inc | Pharmaceutical compositions comprising a fxr agonist and a fibrate for use in the treatment of cholestatic liver disease |
| EP3999101A1 (en) | 2019-07-18 | 2022-05-25 | ENYO Pharma | Method for decreasing adverse-effects of interferon |
| CN110713460A (zh) * | 2019-11-08 | 2020-01-21 | 南通大学 | 一种含吡唑苯基单元的吡唑酰胺衍生物的制备方法及其应用 |
| HUE063556T2 (hu) | 2019-11-26 | 2024-01-28 | Bayer Ag | [(1,5-difenil-1H-1,2,4-triazol-3-il)oxi]ecetsav-származékok és ezek sói, ezeket tartalmazó növényvédõszer haszon- vagy kultúrnövényekhez, eljárás ezek elõállítására és alkalmazásuk széfenerként |
| TWI888447B (zh) | 2019-12-13 | 2025-07-01 | 美商因思博納公司 | 金屬鹽及其用途 |
| EP4075979A1 (de) | 2019-12-19 | 2022-10-26 | Bayer Aktiengesellschaft | 1,5-diphenylpyrazolyl-3-oxyalkylsäuren und 1-phenyl-5-thienylpyrazolyl-3-oxyalkylsäuren und deren verwendung zur bekämpfung unerwünschten pflanzenwachstums |
| WO2021144330A1 (en) | 2020-01-15 | 2021-07-22 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Use of fxr agonists for treating an infection by hepatitis d virus |
| WO2021219527A1 (de) | 2020-04-29 | 2021-11-04 | Bayer Aktiengesellschaft | 1-pyrazinylpyrazolyl-3-oxyalkylsäuren sowie deren derivate und deren verwendung zur bekämpfung unerwünschten pflanzenwachstums |
| US12606542B2 (en) | 2020-11-05 | 2026-04-21 | Bayer Aktiengesellschaft | [(1,5-diheteroaryl-1H-1,2,4-triazol-3-yl)oxy] acetic acid derivatives as safeners for the protection of useful plants and crop plants |
| CA3200680A1 (en) | 2020-11-05 | 2022-05-12 | Bayer Aktiengesellschaft | [(1-phenyl-5-heteroaryl-1h-pyrazol-3-yl)oxy] acetic acid derivatives as safeners for the protection of useful plants and crop plants |
| WO2022096450A1 (de) | 2020-11-05 | 2022-05-12 | Bayer Aktiengesellschaft | Verwendung von [(1,5-diphenyl-1h-pyrazol-3-yl)oxy]essigsäure-derivaten und deren salze sowie diese enthaltende mittel, zur reduktion phytotoxischer wirkungen von agrochemikalien, insbesondere von herbiziden, in nutz- oder kulturpflanzen. |
| KR20230154806A (ko) | 2021-01-14 | 2023-11-09 | 엔요 파마 | Hbv 감염 치료를 위한 fxr 작용제 및 ifn의 상승작용효과 |
| EP4319750A4 (en) | 2021-04-08 | 2025-02-26 | Curis, Inc. | COMBINATION THERAPIES FOR THE TREATMENT OF CANCER |
| CN117320722A (zh) | 2021-04-28 | 2023-12-29 | 埃尼奥制药公司 | 使用fxr激动剂作为联合治疗强烈增强tlr3激动剂的作用 |
Family Cites Families (48)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6492411B1 (en) | 1993-11-30 | 2002-12-10 | G. D. Searle & Co. | Substituted pyrazolyl benzenesulfonamides for the treatment of inflammation |
| US5466823A (en) | 1993-11-30 | 1995-11-14 | G.D. Searle & Co. | Substituted pyrazolyl benzenesulfonamides |
| DE69422306T4 (de) | 1993-11-30 | 2000-09-07 | G.D. Searle & Co., Chicago | Substituierte pyrazolyl-benzolsulfonamide zur behandlung von entzündungen |
| PT839810E (pt) | 1996-11-04 | 2003-01-31 | Bayer Cropscience Sa | 1-poliarilpirazois como pesticidas |
| CN1248916A (zh) | 1997-01-24 | 2000-03-29 | 加利福尼亚大学董事会 | FXR、PPARα和LXRα激活剂恢复屏障功能、促进表皮分化和抑制增生的用途 |
| US20020035156A1 (en) | 1997-04-18 | 2002-03-21 | Barbara Roniker | Combination therapy in the prevention of cardiovascular disorders |
| US6294558B1 (en) | 1999-05-31 | 2001-09-25 | Pfizer Inc. | Sulfonylbenzene compounds as anti-inflammatory/analgesic agents |
| JP4221129B2 (ja) | 1999-02-15 | 2009-02-12 | 富士フイルム株式会社 | 含窒素ヘテロ環化合物、有機発光素子材料、有機発光素子 |
| US6071955A (en) | 1999-02-25 | 2000-06-06 | The Regents Of The University Of California | FXR, PPARA and LXRA activators to treat acne/acneiform conditions |
| YU72201A (sh) | 1999-04-28 | 2005-07-19 | Aventis Pharma Deutschland Gmbh. | Derivati di-aril kiseline kao ppar receptorski ligandi |
| PT1285908E (pt) | 2000-05-29 | 2008-12-04 | Kyorin Seiyaku Kk | Derivados do ácido fenilpropiónico substituídos |
| CN101444496B (zh) | 2001-06-12 | 2011-04-13 | 维尔斯达医疗公司 | 用于治疗代谢失调的化合物 |
| US7482366B2 (en) * | 2001-12-21 | 2009-01-27 | X-Ceptor Therapeutics, Inc. | Modulators of LXR |
| AU2003209388A1 (en) | 2002-01-29 | 2003-09-02 | Merck And Co., Inc. | Substituted imidazoles as cannabinoid receptor modulators |
| US7026346B2 (en) | 2002-04-08 | 2006-04-11 | The Ohio State University Research Foundation | Compounds and methods for inducing apoptosis in proliferating cells |
| WO2003090732A1 (en) * | 2002-04-23 | 2003-11-06 | Chugai Seiyaku Kabushiki Kaisha | Lxr modulators for the treatment of cardiovascular diseases |
| WO2004011446A1 (en) | 2002-07-26 | 2004-02-05 | Bayer Pharmaceuticals Corporation | Indane, dihydrobenzofuran, and tetrahydronaphthalene carboxylic acid derivatives and their use as antidiabetics |
| US7109227B2 (en) | 2002-08-26 | 2006-09-19 | National Health Research Institutes | Imidazolamino compounds |
| EP1398029A1 (en) * | 2002-09-10 | 2004-03-17 | LION Bioscience AG | NR3B1 nuclear receptor binding 3-substituted pyrazole derivatives |
| JP4631259B2 (ja) | 2002-10-03 | 2011-02-16 | コニカミノルタホールディングス株式会社 | 有機エレクトロルミネッセンス素子及び表示装置 |
| WO2004033432A1 (ja) | 2002-10-09 | 2004-04-22 | Ssp Co., Ltd. | 抗真菌活性を有する新規ピラゾール化合物 |
| WO2004056740A1 (en) | 2002-12-20 | 2004-07-08 | Novo Nordisk A/S | Dicarboxylic acid derivatives as ppar-agonists |
| ZA200504898B (en) | 2002-12-20 | 2006-11-29 | Pharmacia Corp | Acyclic pyrazole compounds |
| US7396850B2 (en) | 2003-01-06 | 2008-07-08 | Eli Lilly And Company | Pyrazole derivative as PPAR modulator |
| AU2004210127B2 (en) * | 2003-01-27 | 2009-10-01 | Merck Sharp & Dohme Corp. | Substituted pyrazoles, compositions containing such compounds and methods of use |
| CA2514363A1 (en) | 2003-02-12 | 2004-08-26 | Transtech Pharma, Inc. | Substituted azole derivatives as therapeutic agents |
| WO2004080972A1 (en) | 2003-03-12 | 2004-09-23 | Vertex Pharmaceuticals Incorporated | Pirazole modulators of atp-binding cassette transporters |
| CN100387594C (zh) | 2003-04-03 | 2008-05-14 | 麦克公司 | 二芳基取代的吡唑类代谢型谷氨酸受体-5调节剂 |
| DE10315571A1 (de) | 2003-04-05 | 2004-10-14 | Merck Patent Gmbh | Pyrazolverbindungen |
| DE10315573A1 (de) | 2003-04-05 | 2004-10-14 | Merck Patent Gmbh | Substituierte Pyrazole |
| DE10315569A1 (de) | 2003-04-05 | 2004-10-14 | Merck Patent Gmbh | Substituierte Pyrazolverbindungen |
| MXPA05012679A (es) | 2003-05-27 | 2006-02-08 | Sod Conseils Rech Applic | Nuevos derivados de imidazoles, su preparacion y su uso como medicamento. |
| WO2005012263A1 (en) | 2003-07-24 | 2005-02-10 | Pharmagene Laboratories Limited | 5-ht2b receptor antagonists |
| BRPI0412820A (pt) | 2003-07-25 | 2006-09-26 | Pfizer | compostos de aminopirazol e utilização como inibidores de chk1 |
| CN1889949B (zh) | 2003-10-03 | 2010-06-16 | 俄亥俄州州立大学研究基金会 | PDK-1/Akt信号传导抑制剂 |
| WO2005037199A2 (en) | 2003-10-10 | 2005-04-28 | Bristol-Myers Squibb Company | Pyrazole derivatives as cannabinoid receptor modulators |
| WO2005037763A1 (en) | 2003-10-14 | 2005-04-28 | Eli Lilly And Company | Phenoxyether derivatives as ppar modulators |
| JP2007518686A (ja) | 2003-10-17 | 2007-07-12 | 田辺製薬株式会社 | 高コンダクタンス型カルシウム感受性ｋチャネル開口薬 |
| CA2545942C (en) | 2003-11-14 | 2012-07-10 | Lorus Therapeutics Inc. | Aryl imidazoles and their use as anti-cancer agents |
| TW200526588A (en) | 2003-11-17 | 2005-08-16 | Smithkline Beecham Corp | Chemical compounds |
| ATE386715T1 (de) | 2003-11-25 | 2008-03-15 | Lilly Co Eli | Modulatoren des peroxisomproliferatoraktivierten rezeptors |
| WO2005066137A1 (en) | 2003-12-19 | 2005-07-21 | Neurogen Corporation | 2,5-diaryl-1h-imidazole-4-carboxamides as neurokinin-3 receptor modulators for the treatment of central nervous system and peripheral diseases |
| EP1799673A1 (en) | 2004-10-15 | 2007-06-27 | Memory Pharmaceuticals Corporation | Pyrazole derivatives as phosphodiesterase 4 inhibitors |
| TW200619191A (en) * | 2004-10-27 | 2006-06-16 | Sankyo Co | Phenyl compounds with more than 2 substitutes |
| JP5123668B2 (ja) | 2005-01-10 | 2013-01-23 | エグゼリクシス， インコーポレイテッド | 医薬品としての複素環カルボキサミド化合物 |
| AU2006250354A1 (en) * | 2005-05-23 | 2006-11-30 | Japan Tobacco Inc. | Pyrazole compound and therapeutic agent for diabetes comprising the same |
| BRPI0612287A8 (pt) * | 2005-06-27 | 2019-01-22 | Exelixis Inc | composição para uso farmacêutico no tratamento de doenças através da medicina nuclear e métodos de uso e para modulação de atividade de receptor nuclear |
| US20080090834A1 (en) * | 2006-07-06 | 2008-04-17 | Pfizer Inc | Selective azole pde10a inhibitor compounds |
-
2007
- 2007-12-07 KR KR1020097013701A patent/KR20090094125A/ko not_active Withdrawn
- 2007-12-07 EP EP07865385.4A patent/EP2121621B1/en active Active
- 2007-12-07 US US12/517,800 patent/US7998995B2/en active Active
- 2007-12-07 AU AU2007333194A patent/AU2007333194A1/en not_active Abandoned
- 2007-12-07 JP JP2009540497A patent/JP5399262B2/ja not_active Expired - Fee Related
- 2007-12-07 CN CN2007800511486A patent/CN101679297B/zh not_active Expired - Fee Related
- 2007-12-07 WO PCT/US2007/086787 patent/WO2008073825A1/en not_active Ceased
-
2009
- 2009-07-07 NO NO20092587A patent/NO20092587L/no not_active Application Discontinuation
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| JP2010512342A5 (enExample) | ||
| JP2012520866A5 (enExample) | ||
| JP2022500392A5 (enExample) | ||
| JP2011510080A5 (enExample) | ||
| JP2018518537A5 (enExample) | ||
| US20170217910A1 (en) | Ingenol-3-acylates iii and ingenol-3-carbamates | |
| CN117045653A (zh) | 与毒性醛相关的疾病和治疗 | |
| JP2009197008A5 (enExample) | ||
| RU2019134558A (ru) | Композиции и способы лечения анемии | |
| JP2017504649A5 (enExample) | ||
| RU2015134581A (ru) | Доноры нитроксила с улучшенным терапевтическим индексом | |
| JP2012523395A5 (enExample) | ||
| JP2003515523A5 (enExample) | ||
| CN116615217A (zh) | 炎症性疾病和/或疼痛性疾病的预防或治疗药 | |
| JP2017518360A5 (enExample) | ||
| EP4217359A1 (en) | Hydroxylbenzyl azabicyclo[2.2.1]heptan-1-ane drivatives and medical uses thereof | |
| EP4217344A1 (en) | Arylazabicyclo[2.1.1]hexylmethanol derivatives and medical uses thereof | |
| JP2024096817A (ja) | インドール化合物を用いた疼痛又は間質性膀胱炎の治療方法 | |
| CN106456646B (zh) | 用于治疗或预防肾结石症的可可碱或其衍生物 | |
| TW201628623A (zh) | 尿酸性或痛風性疾病的預防或治療 | |
| JP2022552975A (ja) | 関節リウマチを予防及び／又は治療するためのニコチンアミドモノヌクレオチド（ｎｍｎ）の使用、並びに対応する組成物 | |
| JP5973455B2 (ja) | 脱髄疾患の治療薬及び予防薬 | |
| TWI411435B (zh) | ４－環丙基甲氧基－ｎ－（３，５－二氯－１－氧離子基吡啶－４－基）－５－（甲氧基）吡啶－２－甲醯胺於治療脊髓創傷之用途 | |
| CN117813098A (zh) | 治疗疾病或病症的方法 | |
| JP2025160480A (ja) | 不眠症を治療するためのレンボレキサントの使用 |