CN104203951B - 肝x受体调节剂 - Google Patents
肝x受体调节剂 Download PDFInfo
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- CN104203951B CN104203951B CN201380014354.5A CN201380014354A CN104203951B CN 104203951 B CN104203951 B CN 104203951B CN 201380014354 A CN201380014354 A CN 201380014354A CN 104203951 B CN104203951 B CN 104203951B
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- 0 C=*=*C=*C(N)=I Chemical compound C=*=*C=*C(N)=I 0.000 description 6
- QKCKRMVNOMERAW-QGZVFWFLSA-N CC(C)[C@H](C(N(CC1)C(C([N+]([O-])=O)=CC2)=CC(F)=C2C(OC)=O)=O)N1C(OC(C)(C)C)=O Chemical compound CC(C)[C@H](C(N(CC1)C(C([N+]([O-])=O)=CC2)=CC(F)=C2C(OC)=O)=O)N1C(OC(C)(C)C)=O QKCKRMVNOMERAW-QGZVFWFLSA-N 0.000 description 1
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- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
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- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
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- C07D487/04—Ortho-condensed systems
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
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- Medicinal Chemistry (AREA)
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- Pharmacology & Pharmacy (AREA)
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- Emergency Medicine (AREA)
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- Orthopedic Medicine & Surgery (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201261612051P | 2012-03-16 | 2012-03-16 | |
| US61/612,051 | 2012-03-16 | ||
| PCT/US2013/031242 WO2013138565A1 (en) | 2012-03-16 | 2013-03-14 | Liver x receptor modulators |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN104203951A CN104203951A (zh) | 2014-12-10 |
| CN104203951B true CN104203951B (zh) | 2016-11-02 |
Family
ID=47997957
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201380014354.5A Expired - Fee Related CN104203951B (zh) | 2012-03-16 | 2013-03-14 | 肝x受体调节剂 |
Country Status (27)
| Country | Link |
|---|---|
| US (4) | US9006244B2 (enExample) |
| EP (1) | EP2825541B1 (enExample) |
| JP (3) | JP6114814B2 (enExample) |
| KR (1) | KR102069912B1 (enExample) |
| CN (1) | CN104203951B (enExample) |
| AU (1) | AU2013232066B2 (enExample) |
| CA (1) | CA2866218C (enExample) |
| CY (1) | CY1118318T1 (enExample) |
| DK (1) | DK2825541T3 (enExample) |
| EA (1) | EA026907B1 (enExample) |
| ES (1) | ES2598653T3 (enExample) |
| HR (1) | HRP20161196T1 (enExample) |
| HU (1) | HUE029402T2 (enExample) |
| IL (1) | IL234265B (enExample) |
| IN (1) | IN2014DN07636A (enExample) |
| LT (1) | LT2825541T (enExample) |
| ME (1) | ME02534B (enExample) |
| MX (1) | MX354818B (enExample) |
| NZ (1) | NZ629122A (enExample) |
| PL (1) | PL2825541T3 (enExample) |
| PT (1) | PT2825541T (enExample) |
| RS (1) | RS55166B1 (enExample) |
| SG (1) | SG11201405328SA (enExample) |
| SI (1) | SI2825541T1 (enExample) |
| SM (1) | SMT201600374B (enExample) |
| WO (1) | WO2013138565A1 (enExample) |
| ZA (1) | ZA201406326B (enExample) |
Families Citing this family (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2825541B1 (en) * | 2012-03-16 | 2016-06-22 | Vitae Pharmaceuticals, Inc. | Liver x receptor modulators |
| BR112014022780A8 (pt) * | 2012-03-16 | 2021-06-15 | Vitae Pharmaceuticals Inc | composto modulador de receptor de fígado x, composição farmacêutica que o compreende e seu uso |
| US10669296B2 (en) | 2014-01-10 | 2020-06-02 | Rgenix, Inc. | LXR agonists and uses thereof |
| WO2015195922A1 (en) * | 2014-06-19 | 2015-12-23 | Vitae Pharmaceuticals, Inc. | Compounds for use in treating acute coronary syndrome and related conditions |
| MX377304B (es) * | 2014-08-07 | 2025-03-07 | Vitae Pharmaceuticals Llc | Derivados de piperazina como moduladores de los receptores x del hígado. |
| US20190125745A1 (en) * | 2014-12-17 | 2019-05-02 | Rgenix, Inc. | Treatment and diagnosis of cancer |
| CN105017262B (zh) * | 2015-07-07 | 2017-05-03 | 广东也乐新材料制造有限公司 | 一种醛基取代多环杂芳烃化合物的合成方法 |
| CN105288658B (zh) * | 2015-10-30 | 2018-08-28 | 中国人民解放军第三军医大学 | miR-18a-5p抑制剂在制备防治骨质疏松药物中的应用 |
| CN109069461A (zh) | 2016-01-11 | 2018-12-21 | 洛克菲勒大学 | 与髓源性抑制细胞相关的病症的治疗方法 |
| EP3713575A4 (en) | 2017-11-21 | 2021-08-25 | Rgenix, Inc. | POLYMORPHS AND THEIR USES |
| HUE067466T2 (hu) | 2019-12-13 | 2024-10-28 | Inspirna Inc | Fémsók és alkalmazásuk |
Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| FR2761073A1 (fr) * | 1997-03-20 | 1998-09-25 | Synthelabo | Derives de pyrazino[1,2-a]indole-1-one, leur preparation et leur application en therapeutique |
| CN101456863A (zh) * | 2007-12-14 | 2009-06-17 | 华北制药集团新药研究开发有限责任公司 | 新的lxr激动剂及其制备方法和用途 |
Family Cites Families (61)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4748247A (en) | 1986-10-21 | 1988-05-31 | American Home Products Corporation | 2-[4-[4-(2-Pyrimidinyl)-1-piperazinyl]alkyl]alkyl]pyrido- and pyrazino-indole-1,3-dione derivatives as histamine H1 antagonists |
| EP0511993A1 (en) | 1990-01-22 | 1992-11-11 | E.I. Du Pont De Nemours And Company | Herbicidal sulfonylureas |
| EP0572863A1 (de) | 1992-06-05 | 1993-12-08 | F. Hoffmann-La Roche Ag | ZNS Pyrazinoindole |
| US5545636A (en) | 1993-12-23 | 1996-08-13 | Eli Lilly And Company | Protein kinase C inhibitors |
| ATE456367T1 (de) | 1993-12-23 | 2010-02-15 | Lilly Co Eli | Proteinkinase c inhibitoren |
| AU3831495A (en) | 1994-10-20 | 1996-05-15 | American Home Products Corporation | Indole derivatives useful as serotonergic agents |
| EP0912175A4 (en) | 1996-06-28 | 1999-09-08 | Merck & Co Inc | FIBRINOGENIC RECEPTOR ANTAGONISTS |
| US5854245A (en) | 1996-06-28 | 1998-12-29 | Merck & Co., Inc. | Fibrinogen receptor antagonists |
| CA2257937A1 (en) | 1996-06-28 | 1998-01-08 | Merck & Co., Inc. | Fibrinogen receptor antagonist prodrugs |
| JP2000513375A (ja) | 1996-06-28 | 2000-10-10 | メルク エンド カンパニー インコーポレーテッド | フィブリノーゲンレセプター拮抗薬プロドラッグ |
| US6177440B1 (en) | 1996-10-30 | 2001-01-23 | Eli Lilly And Company | Substituted tricyclics |
| FR2761070B1 (fr) | 1997-03-20 | 1999-04-23 | Synthelabo | Derives de dihydropyrazino[1,2-a]indole-1-one, leur preparation et leur application en therapeutique |
| DE19802235A1 (de) | 1998-01-22 | 1999-07-29 | Bayer Ag | Mit tricyclischen Indolen substituierte Oxazolidinone |
| ID23219A (id) | 1998-04-17 | 2000-03-30 | Lilly Co Eli | Trisiklik tersubstitusi |
| CA2371472A1 (en) | 1999-05-06 | 2000-11-16 | Neurogen Corporation | Substituted 4-oxo-quinoline-3-carboxamides: gaba brain receptor ligands |
| US7037916B2 (en) | 1999-07-15 | 2006-05-02 | Pharmacopeia Drug Discovery, Inc. | Pyrimidine derivatives as IL-8 receptor antagonists |
| IT1313593B1 (it) | 1999-08-03 | 2002-09-09 | Novuspharma Spa | Derivati di 1,2-diidro-1-oxo-pirazino 1,2-a indolo. |
| WO2001030331A2 (en) | 1999-10-22 | 2001-05-03 | Eli Lilly And Company | Therapeutic compositions including protein kinase c inhibitors |
| JP2003525874A (ja) | 2000-01-06 | 2003-09-02 | メルク フロスト カナダ アンド カンパニー | プロテアーゼ阻害剤としての新規化合物および組成物 |
| AU2001283955B2 (en) | 2000-07-31 | 2006-05-18 | F. Hoffmann-La Roche Ag | Piperazine derivatives |
| WO2002059082A2 (en) | 2000-12-20 | 2002-08-01 | Bristol-Myers Squibb Pharma Company | Aryl and aminoaryl substituted serotonin receptor agonist and antagonist ligands |
| GB0106177D0 (en) * | 2001-03-13 | 2001-05-02 | Hoffmann La Roche | Piperazine derivatives |
| FR2829766A1 (fr) | 2001-09-14 | 2003-03-21 | Lipha | Derives d'oxamates comportant un heterocycle azote diversement substitue |
| BR0215288A (pt) | 2001-12-21 | 2004-12-21 | King Phamaceuticals Res & Dev | Composto, sais farmaceuticamente aceitáveis do mesmo, e, métodos para identificar células tumorais ricas em receptores de p2x7, purinérgicos em um mamìfero, para tratar de uma condição médica em um mamìfero, e para induzir a apoptose em células neoplásticas em um paciente |
| US7919497B2 (en) | 2002-08-02 | 2011-04-05 | Nereus Pharmaceuticals, Inc. | Analogs of dehydrophenylahistins and their therapeutic use |
| DE10320780A1 (de) | 2003-05-09 | 2005-01-20 | Bayer Healthcare Ag | Heterocyclyl-substituierte Dihydrochinazoline |
| US7994196B2 (en) | 2004-02-12 | 2011-08-09 | Mitsubishi Tanabe Pharma Corporation | Indazole compound and pharmaceutical use thereof |
| CA2560311A1 (en) | 2004-04-08 | 2005-10-20 | Novartis Ag | Protein kinase c inhibitors for the treatment of autoimmune diseases and of transplant rejection |
| RU2266906C1 (ru) | 2004-04-29 | 2005-12-27 | Общество с ограниченной ответственностью "Исследовательский Институт Химического Разнообразия" (ООО "Исследовательский Институт Химического Разнообразия") | Анелированные карбамоилазагетероциклы, способы их получения (варианты), фармацевтическая композиция, фокусированная библиотека |
| ITMI20040874A1 (it) | 2004-04-30 | 2004-07-30 | Ist Naz Stud Cura Dei Tumori | Derivati indolici ed azaindolici con azione antitumorale |
| WO2005113526A2 (en) | 2004-05-21 | 2005-12-01 | Pfizer Products Inc. | Metabolites of 4-(3,4-dichloro-phenyl)-2-[2-(4-methyl-piperazin-1-yl)-benzylidene]-thiomorpholin-3-one |
| MX2007006896A (es) * | 2004-12-15 | 2007-06-26 | Hoffmann La Roche | Fenil-metanonas bi- y triciclicas sustituidas como inhibidores del transportador 1 de glicina (glyt-1) para el tratamiento de la enfermedad de alzheimer. |
| CA2593266A1 (en) | 2005-01-03 | 2006-07-13 | Universita Degli Studi Di Siena | Aryl piperazine derivatives for the treatment of neuropsychiatric disorders |
| US7790712B2 (en) | 2005-03-17 | 2010-09-07 | Boehringer Ingelheim Pharmaceutical, Inc. | Substituted [1,4]diazepino[1,2-A]indoles and azepino[1,2-A]indoles as anti-cytokine inhibitors |
| WO2006106423A2 (en) | 2005-04-07 | 2006-10-12 | Pfizer Inc. | Amino sulfonyl derivatives as inhibitors of human 11-.beta.-hydrosysteroid dehydrogenase |
| SI1904477T1 (sl) | 2005-07-14 | 2009-06-30 | Hoffmann La Roche | Derivati indol-3-karbonil-spiro-piperidina kot antagonisti V1A receptorja |
| WO2007035841A1 (en) | 2005-09-21 | 2007-03-29 | Nereus Pharmaceuticals, Inc. | Analogs of dehydrophenylahistins and their therapeutic use |
| EP1779848A1 (en) | 2005-10-28 | 2007-05-02 | Nikem Research S.R.L. | V-ATPase inhibitors for the treatment of inflammatory and autoimmune diseases |
| JP2007137810A (ja) * | 2005-11-17 | 2007-06-07 | Sankyo Co Ltd | インドール化合物を含有する医薬 |
| ATE448230T1 (de) | 2005-12-09 | 2009-11-15 | Hoffmann La Roche | Für die behandlung von obesitas geeignete tricyclische amidderivate |
| US7351706B2 (en) | 2006-01-05 | 2008-04-01 | Hoffmann-La Roche Inc. | Indol-3-yl-carbonyl-spiro-piperidine derivatives |
| FR2897061B1 (fr) * | 2006-02-03 | 2010-09-03 | Sanofi Aventis | Derives de n-heteroaryl-carboxamides tricycliques contenant un motif benzimidazole, leur preparation et leur application en therapeutique. |
| RU2318818C1 (ru) | 2006-04-12 | 2008-03-10 | Общество С Ограниченной Ответственностью "Исследовательский Институт Химического Разнообразия" | Азагетероциклы, комбинаторная библиотека, фокусированная библиотека, фармацевтическая композиция и способ получения (варианты) |
| US8129527B2 (en) | 2006-11-03 | 2012-03-06 | Nereus Pharmacuticals, Inc. | Analogs of dehydrophenylahistins and their therapeutic use |
| TWI539947B (zh) | 2007-04-09 | 2016-07-01 | 米希爾金尼公司 | 組蛋白去乙醯基酶之抑制劑 |
| US20110002855A1 (en) | 2007-06-25 | 2011-01-06 | Neurogen Corporation | Piperazinyl oxoalkyl tetrahydro-beta-carbolines and related analogues |
| EP2205085A1 (en) | 2007-09-25 | 2010-07-14 | Merck Sharp & Dohme Corp. | 2-aryl or heteroaryl indole derivatives |
| JP2011507901A (ja) * | 2007-12-21 | 2011-03-10 | ワイス・エルエルシー | ピラゾロ[1,5−a]ピリミジン化合物 |
| BRPI0907230A2 (pt) | 2008-01-22 | 2019-09-24 | Takeda Pharmaceuticals Co | composto, prodroga do composto, fármaco, método para tratar ou prevenir uma doença associada com as funções de um receptor de crf, e, uso do composto |
| US20090192147A1 (en) | 2008-01-30 | 2009-07-30 | Wyeth | [a]-FUSED INDOLE COMPOUNDS, THEIR USE AS mTOR KINASE AND PI3 KINASE INHIBITORS, AND THEIR SYNTHESES |
| US20100137320A1 (en) | 2008-02-29 | 2010-06-03 | Schering Corporation | Gamma secretase modulators |
| EP2254886B1 (en) | 2008-03-28 | 2016-05-25 | Nerviano Medical Sciences S.r.l. | 3,4-dihydro-2h-pyrazino[1,2-a]indol-1-one derivatives active as kinase inhibitors, process for their preparation and pharmaceutical compositions comprising them |
| TW201031665A (en) | 2009-02-04 | 2010-09-01 | Gruenenthal Gmbh | Substituted indole-compound |
| ES2462290T3 (es) | 2009-06-08 | 2014-05-22 | Grünenthal GmbH | Bencimidazoles, benzotiazoles y benzoxazoles sustituidos |
| WO2011005295A1 (en) | 2009-06-24 | 2011-01-13 | Arena Pharmaceuticals, Inc. | Modulators of the sphingosine-1-phosphate (s1p) receptor useful for the treatment of disorders related thereto |
| CA2772522A1 (en) | 2009-09-11 | 2011-03-17 | Sunovion Pharmaceuticals Inc. | Histamine h3 inverse agonists and antagonists and methods of use thereof |
| US9073926B2 (en) | 2009-12-07 | 2015-07-07 | Boehringer Ingelheim International Gmbh | Heterocyclic compounds containing a pyrrolopyridine or benzimidazole core |
| WO2011109237A2 (en) | 2010-03-02 | 2011-09-09 | Emory University | Uses of noscapine and derivatives in subjects diagnosed with fap |
| US8654867B2 (en) * | 2011-12-07 | 2014-02-18 | Texas Instruments Incorporated | Transformer power combiner with filter response |
| EP2825541B1 (en) * | 2012-03-16 | 2016-06-22 | Vitae Pharmaceuticals, Inc. | Liver x receptor modulators |
| BR112014022780A8 (pt) | 2012-03-16 | 2021-06-15 | Vitae Pharmaceuticals Inc | composto modulador de receptor de fígado x, composição farmacêutica que o compreende e seu uso |
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Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| FR2761073A1 (fr) * | 1997-03-20 | 1998-09-25 | Synthelabo | Derives de pyrazino[1,2-a]indole-1-one, leur preparation et leur application en therapeutique |
| CN101456863A (zh) * | 2007-12-14 | 2009-06-17 | 华北制药集团新药研究开发有限责任公司 | 新的lxr激动剂及其制备方法和用途 |
Non-Patent Citations (2)
| Title |
|---|
| "Streamlined access to 2,3-dihydropyrazino[1,2-a]indole-1,4-diones via Ugi reaction followed by microwave-assisted cyclization";Sergey Tsirulnikov等,;《Tetrahedron Letters》;20090722;第50卷;第5529-5531页 * |
| "海洋来源真菌A-f-11中吲哚二酮哌嗪类抗肿瘤活性成分的研究";赵文英等,;《中国抗生素杂志》;20061231;第31卷(第12期);第749-752,764页 * |
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