CN104284893B - 用于治疗皮肤疾病、病症以及病状的肝x受体(lxr)调节剂 - Google Patents
用于治疗皮肤疾病、病症以及病状的肝x受体(lxr)调节剂 Download PDFInfo
- Publication number
- CN104284893B CN104284893B CN201380018482.7A CN201380018482A CN104284893B CN 104284893 B CN104284893 B CN 104284893B CN 201380018482 A CN201380018482 A CN 201380018482A CN 104284893 B CN104284893 B CN 104284893B
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- CN
- China
- Prior art keywords
- alkyl
- aryl
- compound
- heteroalkyl
- another embodiment
- 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.)
- Expired - Fee Related
Links
- 0 CCC(C)C(*)=C(c1ccc(*)cc1C)NI Chemical compound CCC(C)C(*)=C(c1ccc(*)cc1C)NI 0.000 description 9
- DHBVOSREBCFKBO-UHFFFAOYSA-N CC(OCNC)=O Chemical compound CC(OCNC)=O DHBVOSREBCFKBO-UHFFFAOYSA-N 0.000 description 1
Classifications
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/415—1,2-Diazoles
- A61K31/4155—1,2-Diazoles non condensed and containing further heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/04—Antipruritics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/06—Antipsoriatics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/16—Emollients or protectives, e.g. against radiation
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
- C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
- C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
- C07D231/12—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
- C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
- C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
- C07D231/14—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D231/16—Halogen atoms or nitro radicals
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
- C07D405/04—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
- C07D409/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
- C07D417/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Engineering & Computer Science (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Dermatology (AREA)
- Epidemiology (AREA)
- Toxicology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201261606160P | 2012-03-02 | 2012-03-02 | |
| US61/606,160 | 2012-03-02 | ||
| PCT/US2013/028438 WO2013130892A1 (en) | 2012-03-02 | 2013-02-28 | Liver x receptor (lxr) modulators for the treatment of dermal diseases, disorders and conditions |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN104284893A CN104284893A (zh) | 2015-01-14 |
| CN104284893B true CN104284893B (zh) | 2017-04-19 |
Family
ID=49083313
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201380018482.7A Expired - Fee Related CN104284893B (zh) | 2012-03-02 | 2013-02-28 | 用于治疗皮肤疾病、病症以及病状的肝x受体(lxr)调节剂 |
Country Status (25)
| Country | Link |
|---|---|
| US (5) | US8987318B2 (https=) |
| EP (2) | EP2820013B9 (https=) |
| JP (2) | JP6378630B2 (https=) |
| KR (1) | KR102112879B1 (https=) |
| CN (1) | CN104284893B (https=) |
| AU (1) | AU2013225840B2 (https=) |
| BR (1) | BR112014021515A2 (https=) |
| CA (1) | CA2866113C (https=) |
| CY (1) | CY1120742T1 (https=) |
| DK (1) | DK2820013T3 (https=) |
| ES (1) | ES2691079T3 (https=) |
| HR (1) | HRP20181623T1 (https=) |
| HU (1) | HUE040231T2 (https=) |
| IL (1) | IL234413B (https=) |
| LT (1) | LT2820013T (https=) |
| MX (1) | MX361349B (https=) |
| NZ (1) | NZ629636A (https=) |
| PL (1) | PL2820013T3 (https=) |
| PT (1) | PT2820013T (https=) |
| RS (1) | RS57863B9 (https=) |
| SG (2) | SG11201405378VA (https=) |
| SI (1) | SI2820013T1 (https=) |
| SM (1) | SMT201800630T1 (https=) |
| TR (1) | TR201815013T4 (https=) |
| WO (1) | WO2013130892A1 (https=) |
Families Citing this family (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DK2820013T3 (en) | 2012-03-02 | 2018-10-29 | Ralexar Therapeutics Inc | Liver X Receptor (LXR) modulators for the treatment of dermal diseases, disorders and conditions |
| 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 |
| CN104151300B (zh) * | 2013-05-15 | 2018-07-13 | 中国医学科学院医药生物技术研究所 | 一组2,3-二取代的苯并喹唑啉类的肝x受体的激动剂及用途 |
| 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 |
| PT3041835T (pt) | 2013-09-04 | 2020-07-13 | Ellora Therapeutics Inc | Moduladores de recetor de fígado x (lxr) |
| US10669296B2 (en) | 2014-01-10 | 2020-06-02 | Rgenix, Inc. | LXR agonists and uses thereof |
| US20190365784A1 (en) | 2015-12-30 | 2019-12-05 | Raúl Enrique MASSONE | Use of brassinosteroid analogs for the treatment of dermal disorders by selectively modulating liver x receptors (lxr) and dermal disease treatment by brassinosteroid analogs acting as selective liver x receptor (lxr) modulators |
| CA3010883A1 (en) | 2016-01-11 | 2017-07-20 | The Rockefeller University | Methods for the treatment of myeloid derived suppressor cells related disorders |
| EP3713575A4 (en) | 2017-11-21 | 2021-08-25 | Rgenix, Inc. | POLYMORPHS AND THEIR USES |
| CN114126618A (zh) | 2019-07-15 | 2022-03-01 | 诺华股份有限公司 | 用肝脏x受体激动剂治疗睑板腺功能障碍的方法 |
| HUE067466T2 (hu) | 2019-12-13 | 2024-10-28 | Inspirna Inc | Fémsók és alkalmazásuk |
| WO2022249006A1 (en) * | 2021-05-24 | 2022-12-01 | Novartis Ag | Use of 1,2,4-oxadiazole derivatives as liver x receptor agonists |
Citations (4)
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| CN101248048A (zh) * | 2005-06-27 | 2008-08-20 | 埃克塞利希斯股份有限公司 | 吡唑基lxr调节剂 |
| WO2009011850A2 (en) * | 2007-07-16 | 2009-01-22 | Abbott Laboratories | Novel therapeutic compounds |
| WO2009140089A2 (en) * | 2008-05-13 | 2009-11-19 | Boehringer Ingelheim International Gmbh | Sulfone compounds which modulate the cb2 receptor |
| WO2012027710A2 (en) * | 2010-08-27 | 2012-03-01 | Calcimedica Inc. | Compounds that modulate intracellular calcium |
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| JP2004509161A (ja) | 2000-09-18 | 2004-03-25 | グラクソ グループ リミテッド | Lxrのアゴニストとして有用な置換アミノプロポキシアリール誘導体 |
| AUPR738301A0 (en) | 2001-08-30 | 2001-09-20 | Starpharma Limited | Chemotherapeutic agents |
| US7482366B2 (en) | 2001-12-21 | 2009-01-27 | X-Ceptor Therapeutics, Inc. | Modulators of LXR |
| MXPA04011690A (es) | 2002-05-24 | 2005-03-31 | Pharmacia Corp | Moduladores de receptor x de higado de sulfona. |
| MXPA04011691A (es) | 2002-05-24 | 2005-09-12 | Pharmacia Corp | Moduladores del receptor x anilino hepaticos. |
| ATE496893T1 (de) | 2002-12-20 | 2011-02-15 | X Ceptor Therapeutics Inc | Isochinolinonderivate und deren verwendung als medikamente |
| JP2006193426A (ja) | 2003-09-05 | 2006-07-27 | Sankyo Co Ltd | 置換された縮環ピリミジン−4(3h)−オン化合物 |
| WO2005113499A1 (ja) | 2004-05-20 | 2005-12-01 | Sankyo Company, Limited | インドール化合物 |
| TW200606133A (en) | 2004-06-30 | 2006-02-16 | Sankyo Co | Substituted benzene compounds |
| JP2008509138A (ja) | 2004-08-03 | 2008-03-27 | ワイス | 心臓血管疾患の治療に有用なインダゾール類 |
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| WO2006109633A1 (ja) | 2005-04-07 | 2006-10-19 | Daiichi Sankyo Company, Limited | 置換インドール化合物 |
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| RU2008123388A (ru) | 2005-11-14 | 2009-12-27 | Айрм Ллк (Bm) | Соединения и композиции в качестве модуляторов lxr |
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| KR20090094125A (ko) | 2006-12-08 | 2009-09-03 | 엑셀리시스, 인코포레이티드 | Lxr 및 fxr 조절자 |
| US8338437B2 (en) * | 2007-02-28 | 2012-12-25 | Methylgene Inc. | Amines as small molecule inhibitors |
| BRPI0811091A8 (pt) | 2007-05-18 | 2015-09-29 | Wyeth Corp | Composto, composição farmacêutica, métodos para prevenir ou tratar uma doença, distúrbio ou condição, para aumentar níveis de colesterol hdl no soro em um indivíduo, para reduzir níveis de colestetol ldl no soro em um indivíduo, para aumentar o transporte invertido de colesterol em um indivíduo, e para reduzir a absorção do colesterol em um indivíduo, e, uso de um composto |
| MX2010001742A (es) | 2007-08-13 | 2010-03-10 | Hoffmann La Roche | Nuevos derivados de piperazina-amida. |
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| US20100120778A1 (en) | 2008-11-07 | 2010-05-13 | Wyeth | Quinoxaline-based lxr modulators |
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| WO2010096170A2 (en) | 2009-02-19 | 2010-08-26 | President And Fellows Of Harvard College | Inhibition of trna synthetases and therapeutic applications thereof |
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| KR101676704B1 (ko) | 2009-05-28 | 2016-11-16 | 엑셀리시스 페이턴트 컴퍼니 엘엘씨 | Lxr 조절자 |
| EP2501696B1 (en) | 2009-10-15 | 2016-12-28 | Guerbet | Imaging agents and their use for the diagnostic in vivo of neurodegenerative diseases, notably alzheimer's disease and derivative diseases |
| GB0919757D0 (en) | 2009-11-12 | 2009-12-30 | Johnson Matthey Plc | Polymorphs of bromfenac sodium and methods for preparing bromfenac sodium polymorphs |
| US8906943B2 (en) | 2010-08-05 | 2014-12-09 | John R. Cashman | Synthetic compounds and methods to decrease nicotine self-administration |
| US20130137865A1 (en) * | 2010-08-11 | 2013-05-30 | Taisho Pharmaceutical Co., Ltd. | Heteroaryl-pyrazole derivative |
| TW201242953A (en) | 2011-03-25 | 2012-11-01 | Bristol Myers Squibb Co | Imidazole prodrug LXR modulators |
| DK2820013T3 (en) | 2012-03-02 | 2018-10-29 | Ralexar Therapeutics Inc | Liver X Receptor (LXR) modulators for the treatment of dermal diseases, disorders and conditions |
| EP3626309B1 (en) | 2012-08-13 | 2023-03-08 | The Rockefeller University | Lxrbeta agonist for the treatment of cancer |
| 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 |
| PT3041835T (pt) | 2013-09-04 | 2020-07-13 | Ellora Therapeutics Inc | Moduladores de recetor de fígado x (lxr) |
-
2013
- 2013-02-28 DK DK13754329.4T patent/DK2820013T3/en active
- 2013-02-28 BR BR112014021515-4A patent/BR112014021515A2/pt active Search and Examination
- 2013-02-28 RS RS20181179 patent/RS57863B9/sr unknown
- 2013-02-28 LT LTEP13754329.4T patent/LT2820013T/lt unknown
- 2013-02-28 CN CN201380018482.7A patent/CN104284893B/zh not_active Expired - Fee Related
- 2013-02-28 JP JP2014560060A patent/JP6378630B2/ja not_active Expired - Fee Related
- 2013-02-28 SG SG11201405378VA patent/SG11201405378VA/en unknown
- 2013-02-28 WO PCT/US2013/028438 patent/WO2013130892A1/en not_active Ceased
- 2013-02-28 HU HUE13754329A patent/HUE040231T2/hu unknown
- 2013-02-28 HR HRP20181623TT patent/HRP20181623T1/hr unknown
- 2013-02-28 MX MX2014010537A patent/MX361349B/es active IP Right Grant
- 2013-02-28 PL PL13754329T patent/PL2820013T3/pl unknown
- 2013-02-28 AU AU2013225840A patent/AU2013225840B2/en not_active Ceased
- 2013-02-28 SM SM20180630T patent/SMT201800630T1/it unknown
- 2013-02-28 TR TR2018/15013T patent/TR201815013T4/tr unknown
- 2013-02-28 SG SG10201607345YA patent/SG10201607345YA/en unknown
- 2013-02-28 KR KR1020147027825A patent/KR102112879B1/ko not_active Expired - Fee Related
- 2013-02-28 NZ NZ629636A patent/NZ629636A/en not_active IP Right Cessation
- 2013-02-28 EP EP13754329.4A patent/EP2820013B9/en active Active
- 2013-02-28 EP EP18182346.9A patent/EP3441390A1/en not_active Withdrawn
- 2013-02-28 PT PT13754329T patent/PT2820013T/pt unknown
- 2013-02-28 CA CA2866113A patent/CA2866113C/en not_active Expired - Fee Related
- 2013-02-28 ES ES13754329.4T patent/ES2691079T3/es active Active
- 2013-02-28 SI SI201331198T patent/SI2820013T1/sl unknown
-
2014
- 2014-09-01 IL IL234413A patent/IL234413B/en active IP Right Grant
- 2014-09-02 US US14/474,490 patent/US8987318B2/en not_active Expired - Fee Related
-
2015
- 2015-02-12 US US14/621,255 patent/US9637481B2/en not_active Expired - Fee Related
-
2017
- 2017-04-03 US US15/477,140 patent/US20170334897A1/en not_active Abandoned
-
2018
- 2018-04-18 US US15/956,389 patent/US20180370959A1/en not_active Abandoned
- 2018-08-02 JP JP2018145589A patent/JP6800922B2/ja not_active Expired - Fee Related
- 2018-10-08 CY CY181101037T patent/CY1120742T1/el unknown
-
2020
- 2020-05-13 US US15/931,403 patent/US20210101895A1/en not_active Abandoned
Patent Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101248048A (zh) * | 2005-06-27 | 2008-08-20 | 埃克塞利希斯股份有限公司 | 吡唑基lxr调节剂 |
| WO2009011850A2 (en) * | 2007-07-16 | 2009-01-22 | Abbott Laboratories | Novel therapeutic compounds |
| WO2009140089A2 (en) * | 2008-05-13 | 2009-11-19 | Boehringer Ingelheim International Gmbh | Sulfone compounds which modulate the cb2 receptor |
| WO2012027710A2 (en) * | 2010-08-27 | 2012-03-01 | Calcimedica Inc. | Compounds that modulate intracellular calcium |
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