KR20170117020A - 질병의 치료를 위한 융합된 비시클릭 화합물 - Google Patents
질병의 치료를 위한 융합된 비시클릭 화합물 Download PDFInfo
- Publication number
- KR20170117020A KR20170117020A KR1020177016606A KR20177016606A KR20170117020A KR 20170117020 A KR20170117020 A KR 20170117020A KR 1020177016606 A KR1020177016606 A KR 1020177016606A KR 20177016606 A KR20177016606 A KR 20177016606A KR 20170117020 A KR20170117020 A KR 20170117020A
- Authority
- KR
- South Korea
- Prior art keywords
- optionally substituted
- alkylene
- compound
- alkyl
- aryl
- 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.)
- Ceased
Links
- 0 Cc1nnc(*)[o]1 Chemical compound Cc1nnc(*)[o]1 0.000 description 17
- RQEQIKJIEDKYNH-UHFFFAOYSA-N CC(C)(CN(C=C1C(N)=O)C(c(cc2)ccc2F)=O)c2c1[nH]nc2 Chemical compound CC(C)(CN(C=C1C(N)=O)C(c(cc2)ccc2F)=O)c2c1[nH]nc2 RQEQIKJIEDKYNH-UHFFFAOYSA-N 0.000 description 1
- NUCLZXYSTWAFHU-UHFFFAOYSA-N CC(C)(CN(C=C1C(OC)=O)C(c(cc2)ccc2F)=O)c2c1[nH]nc2 Chemical compound CC(C)(CN(C=C1C(OC)=O)C(c(cc2)ccc2F)=O)c2c1[nH]nc2 NUCLZXYSTWAFHU-UHFFFAOYSA-N 0.000 description 1
- MZYZIQMPOKAEIS-UHFFFAOYSA-N CC(C)(CN(C=C1C(OC)=O)C(c(cc2F)ccc2F)=O)c2c1[nH]nc2 Chemical compound CC(C)(CN(C=C1C(OC)=O)C(c(cc2F)ccc2F)=O)c2c1[nH]nc2 MZYZIQMPOKAEIS-UHFFFAOYSA-N 0.000 description 1
- VZVVTZZXMVFALF-UHFFFAOYSA-N CC(C)(CN(C=C1C(OC)=O)C(c(cc2F)ccc2F)=O)c2c1[nH]nc2C Chemical compound CC(C)(CN(C=C1C(OC)=O)C(c(cc2F)ccc2F)=O)c2c1[nH]nc2C VZVVTZZXMVFALF-UHFFFAOYSA-N 0.000 description 1
- NLTKYDSJXYSBJZ-UHFFFAOYSA-N CC(C)(c(c(-c(cc1)ccc1F)n[nH]1)c1Br)C#N Chemical compound CC(C)(c(c(-c(cc1)ccc1F)n[nH]1)c1Br)C#N NLTKYDSJXYSBJZ-UHFFFAOYSA-N 0.000 description 1
- BWJHNPHUYJYJAF-UHFFFAOYSA-N CC(C)NC(C(c1c(C(C)(C)C2)[nH]nc1)=CN2C(c(cc1F)ccc1F)=O)=O Chemical compound CC(C)NC(C(c1c(C(C)(C)C2)[nH]nc1)=CN2C(c(cc1F)ccc1F)=O)=O BWJHNPHUYJYJAF-UHFFFAOYSA-N 0.000 description 1
- ZEHIYXOFZUJWAT-UHFFFAOYSA-N CC(C)NC(C(c1c(C(C)(C)C2)[nH]nc1C)=CN2C(c(cc1)ccc1F)=O)=O Chemical compound CC(C)NC(C(c1c(C(C)(C)C2)[nH]nc1C)=CN2C(c(cc1)ccc1F)=O)=O ZEHIYXOFZUJWAT-UHFFFAOYSA-N 0.000 description 1
- UTCNMCLYGAKCOC-UHFFFAOYSA-N CC(C)NC(C(c1c(C(C)(C)C2)[nH]nc1C)=CN2C(c(cc1F)ccc1F)=O)=O Chemical compound CC(C)NC(C(c1c(C(C)(C)C2)[nH]nc1C)=CN2C(c(cc1F)ccc1F)=O)=O UTCNMCLYGAKCOC-UHFFFAOYSA-N 0.000 description 1
- WOYKZRIYRUHHEO-UHFFFAOYSA-N CCOC(C(c1c(C(C)(C)C2)c(C)n[nH]1)=CN2C(c(cc1F)ccc1F)=O)=O Chemical compound CCOC(C(c1c(C(C)(C)C2)c(C)n[nH]1)=CN2C(c(cc1F)ccc1F)=O)=O WOYKZRIYRUHHEO-UHFFFAOYSA-N 0.000 description 1
- ASTFOAVFJIEMJL-UHFFFAOYSA-N CCOC(C(c1c(C(C)(C)C2)cn[nH]1)=CN2C(c(cc1)ccc1F)=O)=O Chemical compound CCOC(C(c1c(C(C)(C)C2)cn[nH]1)=CN2C(c(cc1)ccc1F)=O)=O ASTFOAVFJIEMJL-UHFFFAOYSA-N 0.000 description 1
- VAXDGKRULPIWKT-UHFFFAOYSA-N Oc1n[s]c(I)c1 Chemical compound Oc1n[s]c(I)c1 VAXDGKRULPIWKT-UHFFFAOYSA-N 0.000 description 1
- FNQJDLTXOVEEFB-UHFFFAOYSA-N c(cc1)cc2c1[s]nn2 Chemical compound c(cc1)cc2c1[s]nn2 FNQJDLTXOVEEFB-UHFFFAOYSA-N 0.000 description 1
- DVUBDHRTVYLIPA-UHFFFAOYSA-N c1c(cccc2)[n]2nc1 Chemical compound c1c(cccc2)[n]2nc1 DVUBDHRTVYLIPA-UHFFFAOYSA-N 0.000 description 1
- SIKJAQJRHWYJAI-UHFFFAOYSA-N c1c[nH]c2ccccc12 Chemical compound c1c[nH]c2ccccc12 SIKJAQJRHWYJAI-UHFFFAOYSA-N 0.000 description 1
- FCEHBMOGCRZNNI-UHFFFAOYSA-N c1c[s]c2ccccc12 Chemical compound c1c[s]c2ccccc12 FCEHBMOGCRZNNI-UHFFFAOYSA-N 0.000 description 1
- AWJUIBRHMBBTKR-UHFFFAOYSA-N c1ccc(cncc2)c2c1 Chemical compound c1ccc(cncc2)c2c1 AWJUIBRHMBBTKR-UHFFFAOYSA-N 0.000 description 1
- SMWDFEZZVXVKRB-UHFFFAOYSA-N c1ccc2ncccc2c1 Chemical compound c1ccc2ncccc2c1 SMWDFEZZVXVKRB-UHFFFAOYSA-N 0.000 description 1
- XSCHRSMBECNVNS-UHFFFAOYSA-N c1ccc2nccnc2c1 Chemical compound c1ccc2nccnc2c1 XSCHRSMBECNVNS-UHFFFAOYSA-N 0.000 description 1
- JWVCLYRUEFBMGU-UHFFFAOYSA-N c1ccc2ncncc2c1 Chemical compound c1ccc2ncncc2c1 JWVCLYRUEFBMGU-UHFFFAOYSA-N 0.000 description 1
- HYZJCKYKOHLVJF-UHFFFAOYSA-N c1nc2ccccc2[nH]1 Chemical compound c1nc2ccccc2[nH]1 HYZJCKYKOHLVJF-UHFFFAOYSA-N 0.000 description 1
- FYADHXFMURLYQI-UHFFFAOYSA-N c1ncnnc1 Chemical compound c1ncnnc1 FYADHXFMURLYQI-UHFFFAOYSA-N 0.000 description 1
Classifications
-
- 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
- A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/04—Anorexiants; Antiobesity agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/06—Antihyperlipidemics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Diabetes (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Epidemiology (AREA)
- Child & Adolescent Psychology (AREA)
- Emergency Medicine (AREA)
- Endocrinology (AREA)
- Urology & Nephrology (AREA)
- Vascular Medicine (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201462083031P | 2014-11-21 | 2014-11-21 | |
| US62/083,031 | 2014-11-21 | ||
| PCT/US2015/062017 WO2016081918A1 (en) | 2014-11-21 | 2015-11-20 | Fused bicyclic compounds for the treatment of disease |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| KR20170117020A true KR20170117020A (ko) | 2017-10-20 |
Family
ID=56014622
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| KR1020177016606A Ceased KR20170117020A (ko) | 2014-11-21 | 2015-11-20 | 질병의 치료를 위한 융합된 비시클릭 화합물 |
Country Status (17)
| Country | Link |
|---|---|
| US (5) | US10233187B2 (enExample) |
| EP (1) | EP3221321B1 (enExample) |
| JP (3) | JP7224102B2 (enExample) |
| KR (1) | KR20170117020A (enExample) |
| CN (2) | CN111662297A (enExample) |
| AU (2) | AU2015349687B2 (enExample) |
| CA (1) | CA2968434A1 (enExample) |
| CL (1) | CL2017001289A1 (enExample) |
| CO (1) | CO2017005784A2 (enExample) |
| ES (1) | ES2911293T3 (enExample) |
| IL (1) | IL252309B (enExample) |
| MX (1) | MX370480B (enExample) |
| MY (1) | MY192927A (enExample) |
| RU (1) | RU2706007C2 (enExample) |
| SA (1) | SA517381566B1 (enExample) |
| SG (2) | SG10202010386PA (enExample) |
| WO (1) | WO2016081918A1 (enExample) |
Families Citing this family (24)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2545964A1 (en) | 2011-07-13 | 2013-01-16 | Phenex Pharmaceuticals AG | Novel FXR (NR1H4) binding and activity modulating compounds |
| MY195016A (en) | 2014-08-04 | 2023-01-03 | Nuevolution As | Optionally Fused Heterocyclyl-Substituted Derivatives of Pyrimidine Useful for The Treatment of Inflammatory, Metabolic, Oncologic and Autoimmune Diseases |
| CA2968434A1 (en) * | 2014-11-21 | 2016-05-26 | Akarna Therapeutics, Ltd. | Fused bicyclic compounds for the treatment of disease |
| RU2021107054A (ru) * | 2015-03-26 | 2021-03-31 | Акарна Терапьютикс, Лтд. | Конденсированные бициклические соединения для лечения заболевания |
| MX2018014024A (es) * | 2016-05-25 | 2019-08-29 | Akarna Therapeutics Ltd | Terapias de combinación con moduladores del receptor x farnesoide (fxr). |
| CA2968836C (en) | 2016-06-13 | 2025-09-02 | Gilead Sciences, Inc. | FXR MODULATING COMPOUNDS (NR1H4) |
| NZ748641A (en) | 2016-06-13 | 2020-04-24 | Gilead Sciences Inc | Fxr (nr1h4) modulating compounds |
| ES2982801T3 (es) | 2017-03-28 | 2024-10-17 | Gilead Sciences Inc | Combinaciones terapéuticas para el tratamiento de las enfermedades hepáticas |
| BR112019025228A2 (pt) * | 2017-06-02 | 2020-06-23 | Akarna Therapeutics, Ltd. | Compostos bicíclicos fundidos |
| KR102692309B1 (ko) | 2019-01-15 | 2024-08-07 | 길리애드 사이언시즈, 인코포레이티드 | Fxr (nr1h4) 조정 화합물 |
| WO2020172075A1 (en) | 2019-02-19 | 2020-08-27 | Gilead Sciences, Inc. | Solid forms of fxr agonists |
| CN111825653A (zh) * | 2019-04-19 | 2020-10-27 | 安道麦马克西姆有限公司 | 取代吡唑类化合物的制备及其作为邻氨基苯甲酰胺前体的用途 |
| WO2021014349A1 (en) | 2019-07-23 | 2021-01-28 | Novartis Ag | Treatment comprising fxr agonists |
| TW202114672A (zh) | 2019-07-23 | 2021-04-16 | 瑞士商諾華公司 | 使用fxr促效劑的肝臟疾病之組合治療 |
| KR20220054608A (ko) | 2019-09-03 | 2022-05-03 | 노파르티스 아게 | ActRII 수용체 길항제를 포함하는 간 질환 또는 장애 치료제 |
| JP2022548617A (ja) | 2019-09-19 | 2022-11-21 | ノバルティス アーゲー | Ｆｘｒアゴニストを含む処置 |
| CN114502198A (zh) | 2019-09-30 | 2022-05-13 | 诺华股份有限公司 | 包括使用fxr激动剂的治疗 |
| EP4076454A1 (en) | 2019-12-20 | 2022-10-26 | Novartis AG | Combination treatment of liver diseases using integrin inhibitors |
| AU2020405446A1 (en) | 2019-12-20 | 2022-05-26 | Nuevolution A/S | Compounds active towards nuclear receptors |
| BR112022012205A2 (pt) | 2019-12-20 | 2022-09-13 | Nuevolution As | Compostos ativos para receptores nucleares |
| JP7713954B2 (ja) | 2020-03-31 | 2025-07-28 | ヌエヴォリューション・アクティーゼルスカブ | 核内受容体に対して活性な化合物 |
| CA3174252A1 (en) | 2020-03-31 | 2021-10-07 | Nuevolution A/S | Compounds active towards nuclear receptors |
| UY39391A (es) * | 2020-08-24 | 2022-03-31 | Adama Makhteshim Ltd | Proceso para la preparación de pirazoles sustituidos |
| WO2022101853A1 (en) | 2020-11-16 | 2022-05-19 | Novartis Ag | Method of determining liver fibrosis |
Family Cites Families (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7595311B2 (en) * | 2002-05-24 | 2009-09-29 | Exelixis, Inc. | Azepinoindole derivatives as pharmaceutical agents |
| WO2005009387A2 (en) * | 2003-07-23 | 2005-02-03 | X-Ceptor Therapeutics Inc. | Azepine derivatives as pharmaceutical agents |
| SG146683A1 (en) * | 2003-09-17 | 2008-10-30 | Janssen Pharmaceutica Nv | Fused heterocyclic compounds as serotonin receptor modulators |
| US20090137554A1 (en) * | 2007-10-22 | 2009-05-28 | Wyeth | 1,4,5,6-TETRAHYDRO -PYRROLO[2,3-d]AZEPINES AND -IMIDAZO[4,5-d]AZEPINES AS MODULATORS OF NUCLEAR RECEPTOR ACTIVITY |
| US20090215748A1 (en) * | 2007-12-20 | 2009-08-27 | Wyeth | FXR agonists for treating vitamin D associated diseases |
| JP2012503654A (ja) * | 2008-09-26 | 2012-02-09 | ワイス・エルエルシー | １，２，３，６−テトラヒドロアゼピノ［４，５−ｂ］インドール−５−カルボキシレート核内受容体阻害剤 |
| US8252826B2 (en) * | 2010-03-24 | 2012-08-28 | Hoffmann-La Roche Inc. | Cyclopentyl- and cycloheptylpyrazoles |
| CA2968434A1 (en) * | 2014-11-21 | 2016-05-26 | Akarna Therapeutics, Ltd. | Fused bicyclic compounds for the treatment of disease |
| JP2019520335A (ja) * | 2016-05-25 | 2019-07-18 | アカーナ・セラピューティクス・リミテッドＡｋａｒｎａ Ｔｈｅｒａｐｅｕｔｉｃｓ， Ｌｔｄ． | 疾患治療用の縮合二環式化合物 |
-
2015
- 2015-11-20 CA CA2968434A patent/CA2968434A1/en active Pending
- 2015-11-20 MY MYPI2017701793A patent/MY192927A/en unknown
- 2015-11-20 CN CN202010634386.7A patent/CN111662297A/zh active Pending
- 2015-11-20 ES ES15861717T patent/ES2911293T3/es active Active
- 2015-11-20 WO PCT/US2015/062017 patent/WO2016081918A1/en not_active Ceased
- 2015-11-20 RU RU2017121588A patent/RU2706007C2/ru active
- 2015-11-20 SG SG10202010386PA patent/SG10202010386PA/en unknown
- 2015-11-20 CN CN201580073351.8A patent/CN107207513B/zh not_active Expired - Fee Related
- 2015-11-20 MX MX2017006694A patent/MX370480B/es active IP Right Grant
- 2015-11-20 SG SG11201703953WA patent/SG11201703953WA/en unknown
- 2015-11-20 EP EP15861717.5A patent/EP3221321B1/en not_active Not-in-force
- 2015-11-20 KR KR1020177016606A patent/KR20170117020A/ko not_active Ceased
- 2015-11-20 AU AU2015349687A patent/AU2015349687B2/en not_active Ceased
- 2015-11-20 JP JP2017545870A patent/JP7224102B2/ja active Active
-
2017
- 2017-05-16 IL IL252309A patent/IL252309B/en active IP Right Grant
- 2017-05-19 CL CL2017001289A patent/CL2017001289A1/es unknown
- 2017-05-19 US US15/599,647 patent/US10233187B2/en active Active
- 2017-05-20 SA SA517381566A patent/SA517381566B1/ar unknown
- 2017-06-12 CO CONC2017/0005784A patent/CO2017005784A2/es unknown
-
2019
- 2019-03-15 US US16/354,879 patent/US20190308977A1/en not_active Abandoned
-
2020
- 2020-07-22 JP JP2020125592A patent/JP2021011482A/ja active Pending
- 2020-09-18 US US17/025,724 patent/US20210147426A1/en not_active Abandoned
- 2020-10-08 AU AU2020250270A patent/AU2020250270B2/en not_active Ceased
-
2022
- 2022-09-16 US US17/932,876 patent/US20230183247A1/en not_active Abandoned
- 2022-10-26 JP JP2022171339A patent/JP2023011731A/ja active Pending
-
2024
- 2024-06-27 US US18/757,057 patent/US20250171446A1/en active Pending
Also Published As
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| Publication | Publication Date | Title |
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| JP7224102B2 (ja) | 疾患治療用の縮合二環式化合物 | |
| JP7089566B2 (ja) | 疾患の処置のための縮合二環式化合物 | |
| US20210214362A1 (en) | Fused bicyclic compounds for the treatment of disease | |
| KR20190040140A (ko) | 질환의 치료를 위한 융합된 비시클릭 화합물 | |
| HK40049146A (en) | Fused bicyclic compounds for the treatment of disease | |
| HK1245795B (en) | Fused bicyclic compounds for the treatment of disease | |
| HK1244802B (en) | Fused bicyclic compounds for the treatment of disease |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| PA0105 | International application |
Patent event date: 20170616 Patent event code: PA01051R01D Comment text: International Patent Application |
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| PG1501 | Laying open of application | ||
| A201 | Request for examination | ||
| PA0201 | Request for examination |
Patent event code: PA02012R01D Patent event date: 20201118 Comment text: Request for Examination of Application |
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| E902 | Notification of reason for refusal | ||
| PE0902 | Notice of grounds for rejection |
Comment text: Notification of reason for refusal Patent event date: 20230228 Patent event code: PE09021S01D |
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| E601 | Decision to refuse application | ||
| PE0601 | Decision on rejection of patent |
Patent event date: 20230523 Comment text: Decision to Refuse Application Patent event code: PE06012S01D Patent event date: 20230228 Comment text: Notification of reason for refusal Patent event code: PE06011S01I |