JP2013538825A5 - - Google Patents
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- Publication number
- JP2013538825A5 JP2013538825A5 JP2013530177A JP2013530177A JP2013538825A5 JP 2013538825 A5 JP2013538825 A5 JP 2013538825A5 JP 2013530177 A JP2013530177 A JP 2013530177A JP 2013530177 A JP2013530177 A JP 2013530177A JP 2013538825 A5 JP2013538825 A5 JP 2013538825A5
- Authority
- JP
- Japan
- Prior art keywords
- methyl
- cancer
- hydrogen
- pharmaceutically acceptable
- pharmaceutical composition
- 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
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 45
- 229910052739 hydrogen Inorganic materials 0.000 claims 34
- 239000001257 hydrogen Substances 0.000 claims 34
- 150000001875 compounds Chemical class 0.000 claims 33
- 239000008194 pharmaceutical composition Substances 0.000 claims 31
- 150000003839 salts Chemical class 0.000 claims 28
- 150000002431 hydrogen Chemical class 0.000 claims 22
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 21
- 125000005843 halogen group Chemical group 0.000 claims 20
- 206010028980 Neoplasm Diseases 0.000 claims 19
- 201000011510 cancer Diseases 0.000 claims 19
- 125000004216 fluoromethyl group Chemical group [H]C([H])(F)* 0.000 claims 15
- 241000124008 Mammalia Species 0.000 claims 12
- 125000004785 fluoromethoxy group Chemical group [H]C([H])(F)O* 0.000 claims 10
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 9
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 6
- MYMOFIZGZYHOMD-UHFFFAOYSA-N Dioxygen Chemical group O=O MYMOFIZGZYHOMD-UHFFFAOYSA-N 0.000 claims 5
- 125000001028 difluoromethyl group Chemical group [H]C(F)(F)* 0.000 claims 5
- 201000006417 multiple sclerosis Diseases 0.000 claims 5
- 229910052760 oxygen Inorganic materials 0.000 claims 5
- 239000001301 oxygen Substances 0.000 claims 5
- 206010039073 rheumatoid arthritis Diseases 0.000 claims 5
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 5
- 239000003937 drug carrier Substances 0.000 claims 4
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 3
- 208000000172 Medulloblastoma Diseases 0.000 claims 3
- 125000001309 chloro group Chemical group Cl* 0.000 claims 3
- 239000003814 drug Substances 0.000 claims 3
- 238000004519 manufacturing process Methods 0.000 claims 3
- 206010006187 Breast cancer Diseases 0.000 claims 2
- 208000026310 Breast neoplasm Diseases 0.000 claims 2
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims 2
- 206010008342 Cervix carcinoma Diseases 0.000 claims 2
- 206010009944 Colon cancer Diseases 0.000 claims 2
- 208000001333 Colorectal Neoplasms Diseases 0.000 claims 2
- 206010014733 Endometrial cancer Diseases 0.000 claims 2
- 206010014759 Endometrial neoplasm Diseases 0.000 claims 2
- 208000008839 Kidney Neoplasms Diseases 0.000 claims 2
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 2
- 206010033128 Ovarian cancer Diseases 0.000 claims 2
- 206010061535 Ovarian neoplasm Diseases 0.000 claims 2
- 206010060862 Prostate cancer Diseases 0.000 claims 2
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims 2
- 206010038389 Renal cancer Diseases 0.000 claims 2
- 208000000453 Skin Neoplasms Diseases 0.000 claims 2
- 208000006593 Urologic Neoplasms Diseases 0.000 claims 2
- 208000006105 Uterine Cervical Neoplasms Diseases 0.000 claims 2
- 229910052799 carbon Inorganic materials 0.000 claims 2
- 201000010881 cervical cancer Diseases 0.000 claims 2
- 125000001153 fluoro group Chemical group F* 0.000 claims 2
- 208000005017 glioblastoma Diseases 0.000 claims 2
- 201000010536 head and neck cancer Diseases 0.000 claims 2
- 208000014829 head and neck neoplasm Diseases 0.000 claims 2
- 201000010982 kidney cancer Diseases 0.000 claims 2
- 201000005202 lung cancer Diseases 0.000 claims 2
- 208000020816 lung neoplasm Diseases 0.000 claims 2
- -1 methoxy, difluoromethoxy Chemical group 0.000 claims 2
- 201000000849 skin cancer Diseases 0.000 claims 2
- 125000000876 trifluoromethoxy group Chemical group FC(F)(F)O* 0.000 claims 2
- 125000004786 difluoromethoxy group Chemical group [H]C(F)(F)O* 0.000 claims 1
- 239000000203 mixture Substances 0.000 claims 1
- 239000000825 pharmaceutical preparation Substances 0.000 claims 1
- FQWAIOYNRZLUKT-UHFFFAOYSA-N C[n]1nc(C(F)(F)F)c(C(NC2(CC2)c(cc2)ccc2C(O)=O)=O)c1Oc(cc1)cc(Cl)c1Cl Chemical compound C[n]1nc(C(F)(F)F)c(C(NC2(CC2)c(cc2)ccc2C(O)=O)=O)c1Oc(cc1)cc(Cl)c1Cl FQWAIOYNRZLUKT-UHFFFAOYSA-N 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US38478110P | 2010-09-21 | 2010-09-21 | |
| US61/384,781 | 2010-09-21 | ||
| PCT/US2011/051163 WO2012039972A1 (en) | 2010-09-21 | 2011-09-12 | Pharmaceutical composition |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2013538825A JP2013538825A (ja) | 2013-10-17 |
| JP2013538825A5 true JP2013538825A5 (enExample) | 2014-10-30 |
| JP5956448B2 JP5956448B2 (ja) | 2016-07-27 |
Family
ID=44674894
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2013530177A Active JP5956448B2 (ja) | 2010-09-21 | 2011-09-12 | 医薬組成物 |
Country Status (31)
| Country | Link |
|---|---|
| US (2) | US8686018B2 (enExample) |
| EP (2) | EP3061751A1 (enExample) |
| JP (1) | JP5956448B2 (enExample) |
| KR (1) | KR101911105B1 (enExample) |
| CN (1) | CN103097358B (enExample) |
| AU (1) | AU2011305872B2 (enExample) |
| BR (1) | BR112013002484B1 (enExample) |
| CA (1) | CA2806121C (enExample) |
| CL (1) | CL2013000675A1 (enExample) |
| CY (1) | CY1118680T1 (enExample) |
| DK (1) | DK2619182T3 (enExample) |
| ES (1) | ES2610185T3 (enExample) |
| HR (1) | HRP20170042T1 (enExample) |
| HU (1) | HUE031408T2 (enExample) |
| IL (1) | IL224288A (enExample) |
| LT (1) | LT2619182T (enExample) |
| ME (1) | ME02575B (enExample) |
| MX (1) | MX2013003162A (enExample) |
| MY (1) | MY162146A (enExample) |
| NZ (1) | NZ606629A (enExample) |
| PE (1) | PE20131343A1 (enExample) |
| PH (1) | PH12013500467A1 (enExample) |
| PL (1) | PL2619182T3 (enExample) |
| PT (1) | PT2619182T (enExample) |
| RS (1) | RS55566B1 (enExample) |
| RU (1) | RU2606510C2 (enExample) |
| SG (1) | SG188188A1 (enExample) |
| SI (1) | SI2619182T1 (enExample) |
| SM (2) | SMT201700008T1 (enExample) |
| UA (1) | UA113499C2 (enExample) |
| WO (1) | WO2012039972A1 (enExample) |
Families Citing this family (26)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AR091429A1 (es) * | 2012-06-29 | 2015-02-04 | Lilly Co Eli | Compuestos de fenoxietil piperidina |
| PT3009426T (pt) * | 2013-06-12 | 2018-06-08 | Kaken Pharma Co Ltd | Derivado de 4-alquinilimidazole e medicamento compreendendo o mesmo como ingrediente ativo |
| TW201623277A (zh) | 2014-03-26 | 2016-07-01 | 安斯泰來製藥股份有限公司 | 醯胺化合物 |
| US20170182003A1 (en) * | 2014-05-23 | 2017-06-29 | Eisai R&D Management Co., Ltd. | Combination therapies for the treatment of cancer |
| TWI730959B (zh) | 2015-05-19 | 2021-06-21 | 英商葛蘭素史克智慧財產發展有限公司 | 作為激酶抑制劑之雜環醯胺 |
| EP3325490B1 (en) | 2015-07-23 | 2019-12-18 | Takeda Pharmaceutical Company Limited | 1-substituted 1,2,3,4-tetrahydro-1,7-naphthyridin-8-amine derivatives and their use as ep4 receptor antagonists |
| MX390051B (es) * | 2015-10-16 | 2025-03-20 | Eisai R&D Man Co Ltd | Antagonistas de ep4. |
| CR20180323A (es) | 2015-11-20 | 2018-08-06 | Idorsia Pharmaceuticals Ltd | Derivados de indol n-sustituídos como moduladores de los receptores de pge2 |
| AR111941A1 (es) | 2017-05-18 | 2019-09-04 | Idorsia Pharmaceuticals Ltd | Derivados de pirimidina como moduladores del receptor de pge2 |
| JP7093791B2 (ja) | 2017-05-18 | 2022-06-30 | イドーシア ファーマシューティカルズ リミテッド | Ｐｇｅ２レセプター調節剤としてのベンゾフラン及びベンゾチオフェン誘導体 |
| US20200069686A1 (en) | 2017-05-18 | 2020-03-05 | Idorsia Pharmaceuticals Ltd | N-substituted indole derivatives |
| EP3625223B1 (en) | 2017-05-18 | 2021-08-11 | Idorsia Pharmaceuticals Ltd | Pyrimidine derivatives |
| MX388257B (es) | 2017-05-18 | 2025-03-19 | Idorsia Pharmaceuticals Ltd | Derivados de pirimidina como moduladores del receptor de pge2. |
| CN108929281B (zh) * | 2017-05-27 | 2021-12-24 | 华东师范大学 | 三氮唑类化合物及其合成方法和应用 |
| AU2019214193B2 (en) * | 2018-02-05 | 2022-06-16 | Foshan Ionova Biotherapeutics Co., Inc. | Heterobicyclic carboxylic acids for treating cancer or inflammatory diseases |
| US20230125494A1 (en) * | 2020-03-04 | 2023-04-27 | Wuhan Humanwell Innovative Drug Research and Development Center Limited Company | Synthesis of novel ep4 antagonist and use in cancer and inflammation |
| CN114075140A (zh) * | 2020-08-18 | 2022-02-22 | 武汉人福创新药物研发中心有限公司 | 作为ep4受体拮抗剂的吡唑酰胺衍生物及其在癌症和炎症中的用途 |
| EP4245301A4 (en) | 2020-11-13 | 2024-08-21 | ONO Pharmaceutical Co., Ltd. | TREATMENT OF CANCER BY COMBINED USE OF AN EP4 ANTAGONIST AND AN IMMUNE CHECKPOINT INHIBITOR |
| TWI877433B (zh) | 2020-11-30 | 2025-03-21 | 大陸商杭州阿諾生物醫藥科技有限公司 | 用於治療ｐｉｋ３ｃａ突變癌症的組合療法 |
| CN114790176A (zh) * | 2021-01-25 | 2022-07-26 | 武汉人福创新药物研发中心有限公司 | 咪唑类化合物及其制备方法和用途 |
| EP4286371A4 (en) * | 2021-01-28 | 2025-01-08 | Shenzhen Zhongge Biological Technology Co., Ltd. | Pyrazolamide derivative, preparation method therefor, and application thereof |
| WO2023030492A1 (zh) * | 2021-09-03 | 2023-03-09 | 武汉人福创新药物研发中心有限公司 | 一种ep4拮抗剂化合物及其盐、多晶型和用途 |
| CN115364222A (zh) * | 2021-09-09 | 2022-11-22 | 首都医科大学附属北京地坛医院 | Ep4受体抑制剂治疗肝纤维化的应用 |
| CA3242277A1 (en) | 2021-12-23 | 2023-06-29 | Eisai R&D Management Co., Ltd. | Crystalline salt form of ep4 antagonist |
| US20250381143A1 (en) | 2021-12-30 | 2025-12-18 | Adlai Nortye Biopharma Co., Ltd. | A solid pharmaceutical composition |
| WO2024027599A1 (zh) * | 2022-08-04 | 2024-02-08 | 杭州阿诺生物医药科技有限公司 | 预测直肠癌对an0025联合放疗/放化疗(rt/crt)治疗敏感性的生物标志物 |
Family Cites Families (36)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPH0421671A (ja) * | 1990-05-16 | 1992-01-24 | Mitsubishi Kasei Corp | ４―ピラゾールカルボキサミド類およびこれを有効成分とする殺虫、殺ダニ剤 |
| IL104311A (en) * | 1992-02-05 | 1997-07-13 | Fujisawa Pharmaceutical Co | Pyrazole derivatives, processes for the preparation thereof and pharmaceutical compositions containing the same |
| US6211197B1 (en) * | 1998-10-07 | 2001-04-03 | Merck Frosst Canada & Co. | Prostaglandin receptor ligands |
| US7119108B1 (en) | 1999-10-18 | 2006-10-10 | University Of Connecticut | Pyrazole derivatives as cannabinoid receptor antagonists |
| US7393842B2 (en) | 2001-08-31 | 2008-07-01 | University Of Connecticut | Pyrazole analogs acting on cannabinoid receptors |
| HN2001000224A (es) | 2000-10-19 | 2002-06-13 | Pfizer | Compuestos de imidazol condensado con arilo o heteroarilo como agentes anti - inflamatorios y analgesicos. |
| TW591020B (en) | 2001-06-20 | 2004-06-11 | Wyeth Corp | 6-(aryl-amido or aryl-amidomethyl)-naphthalen-2-yloxy-acidic derivatives as inhibitors of plasminogen activator inhibitor type-1 (PAI-1) |
| US20050113283A1 (en) | 2002-01-18 | 2005-05-26 | David Solow-Cordero | Methods of treating conditions associated with an EDG-4 receptor |
| AU2003285012A1 (en) | 2002-10-24 | 2004-05-13 | Sepracor, Inc. | Compositions comprising zopiclone derivatives and methods of making and using the same |
| FR2847160A1 (fr) | 2002-11-20 | 2004-05-21 | Oreal | Composition capillaire contenant un compose pyrasol-carboxamide, son utilisation pour stimuler la pousse des cheveux et/ou freiner leur chute |
| GB0302094D0 (en) | 2003-01-29 | 2003-02-26 | Pharmagene Lab Ltd | EP4 receptor antagonists |
| HRP20110757T1 (hr) * | 2003-06-26 | 2011-11-30 | Novartis Ag | Inhibitori kinaze p38 bazirani na 5-članom heterociklu |
| RS20060143A (sr) * | 2003-09-03 | 2008-06-05 | Pfizer Inc., | Jedinjenja fenil ili piridil amida kao antagonisti prostaglandina e2 |
| GT200500013A (es) | 2004-01-23 | 2005-08-10 | Amidas herbicidas | |
| CN1950334A (zh) * | 2004-05-04 | 2007-04-18 | 辉瑞有限公司 | 邻位取代的芳基或杂芳基酰胺化合物 |
| JP4054368B2 (ja) | 2004-05-04 | 2008-02-27 | ファイザー株式会社 | 置換メチルアリール又はヘテロアリールアミド化合物 |
| US8952176B2 (en) | 2005-06-07 | 2015-02-10 | Shionogi & Co., Ltd. | Heterocyclic compound having type I 11 β hydroxysteroid dehydrogenase inhibitory activity |
| EP1891048A1 (en) * | 2005-06-11 | 2008-02-27 | Vernalis (R&D) Limited | Pyrazole-substituted benzimidazole derivatives for use in the treatment of cancer and autoimmune disorders |
| CN101273013B (zh) * | 2005-09-27 | 2013-06-12 | 盐野义制药株式会社 | 具有pgd2受体拮抗活性的磺酰胺衍生物 |
| CA2630665C (en) | 2005-11-21 | 2011-03-15 | Shionogi & Co., Ltd. | Heterocyclic compound having inhibitory activity on 11-.beta.-hydroxysteroid dehydrogenase type i |
| EP1988081B1 (en) * | 2006-02-06 | 2012-10-17 | Taisho Pharmaceutical Co., Ltd | Binding inhibitor of sphingosine-1-phosphate |
| US7705035B2 (en) | 2006-06-12 | 2010-04-27 | Merck Frosst Canada Ltd. | Indoline amide derivatives as EP4 receptor ligands |
| CA2660133C (en) | 2006-08-11 | 2015-10-27 | Merck Frosst Canada Ltd. | Thiophenecarboxamide derivatives as ep4 receptor ligands |
| WO2008071736A1 (en) | 2006-12-15 | 2008-06-19 | Glaxo Group Limited | Benzamide derivatives as ep4 receptor agonists |
| US8158671B2 (en) | 2007-02-26 | 2012-04-17 | Merck Canada Inc. | Indole and indoline cyclopropyl amide derivatives as EP4 receptor antagonists |
| US7560936B1 (en) | 2007-04-24 | 2009-07-14 | Integrated Device Technology, Inc. | Method and apparatus for ground bounce and power supply bounce detection |
| MX2009013059A (es) | 2007-06-15 | 2010-01-15 | Basf Se | Procedimientos para la preparacion de compuestos de pirazol sustituidos con difluorometilo. |
| US20110028463A1 (en) | 2007-07-03 | 2011-02-03 | Astellas Pharma Inc. | Amide compounds |
| SG187396A1 (en) | 2007-07-19 | 2013-02-28 | Lundbeck & Co As H | 5-membered heterocyclic amides and related compounds |
| CL2008002241A1 (es) | 2007-07-31 | 2009-12-28 | Bayer Cropscience Sa | Compuestos derivados de (hetero)aril-metilen-n-cicloalquil carboxamida condensados de 6 elementos con n-sustituido; composicion funguicida que comprende uno de dichos compuestos; y metodo para el control hongos fitopatogenos de cultivos agricolas. |
| GB0721611D0 (en) | 2007-11-02 | 2007-12-12 | Glaxo Group Ltd | Novel compounds |
| US8293917B2 (en) * | 2008-05-06 | 2012-10-23 | Boehringer Ingelheim International Gmbh | Pyrazole compounds as CCR1 antagonists |
| SI2565191T1 (sl) | 2008-05-14 | 2014-12-31 | Astellas Pharma Inc. | Derivati 4-(indol-7-ilkarbonilaminometil)cikloheksan karboksilne kisline kot EP4 receptorski antagonisti, uporabni za zdravljenje kronične ledvične odpovedi ali diabetične nefropatije |
| EA018569B1 (ru) | 2008-08-01 | 2013-08-30 | Байер Кропсайенс Аг | Фунгицидные n-циклоалкил-n-бифенилметилкарбоксамидные производные |
| EP2320906B1 (en) * | 2008-08-14 | 2016-02-24 | Beta Pharma Canada Inc. | Heterocyclic amide derivatives as ep4 receptor antagonists |
| CN102224154A (zh) | 2008-09-25 | 2011-10-19 | 默克弗罗斯特加拿大有限公司 | 作为EP4受体拮抗剂的β-咔啉磺酰脲衍生物 |
-
2011
- 2011-09-12 PH PH1/2013/500467A patent/PH12013500467A1/en unknown
- 2011-09-12 PE PE2013000320A patent/PE20131343A1/es active IP Right Grant
- 2011-09-12 WO PCT/US2011/051163 patent/WO2012039972A1/en not_active Ceased
- 2011-09-12 EP EP16161460.7A patent/EP3061751A1/en not_active Withdrawn
- 2011-09-12 PL PL11760631T patent/PL2619182T3/pl unknown
- 2011-09-12 KR KR1020137004494A patent/KR101911105B1/ko active Active
- 2011-09-12 SM SM20170008T patent/SMT201700008T1/it unknown
- 2011-09-12 CA CA2806121A patent/CA2806121C/en active Active
- 2011-09-12 AU AU2011305872A patent/AU2011305872B2/en active Active
- 2011-09-12 BR BR112013002484-4A patent/BR112013002484B1/pt active IP Right Grant
- 2011-09-12 PT PT117606319T patent/PT2619182T/pt unknown
- 2011-09-12 NZ NZ60662911A patent/NZ606629A/en unknown
- 2011-09-12 CN CN201180045222.XA patent/CN103097358B/zh active Active
- 2011-09-12 UA UAA201304961A patent/UA113499C2/uk unknown
- 2011-09-12 RS RS20170008A patent/RS55566B1/sr unknown
- 2011-09-12 MY MYPI2013700146A patent/MY162146A/en unknown
- 2011-09-12 HR HRP20170042TT patent/HRP20170042T1/hr unknown
- 2011-09-12 ES ES11760631.9T patent/ES2610185T3/es active Active
- 2011-09-12 SI SI201131067A patent/SI2619182T1/sl unknown
- 2011-09-12 RU RU2013118209A patent/RU2606510C2/ru active
- 2011-09-12 ME MEP-2017-3A patent/ME02575B/me unknown
- 2011-09-12 JP JP2013530177A patent/JP5956448B2/ja active Active
- 2011-09-12 HU HUE11760631A patent/HUE031408T2/en unknown
- 2011-09-12 LT LTEP11760631.9T patent/LT2619182T/lt unknown
- 2011-09-12 SG SG2013007174A patent/SG188188A1/en unknown
- 2011-09-12 DK DK11760631.9T patent/DK2619182T3/en active
- 2011-09-12 MX MX2013003162A patent/MX2013003162A/es active IP Right Grant
- 2011-09-12 EP EP11760631.9A patent/EP2619182B1/en active Active
-
2013
- 2013-01-17 IL IL224288A patent/IL224288A/en active IP Right Grant
- 2013-03-12 US US13/795,768 patent/US8686018B2/en active Active
- 2013-03-12 CL CL2013000675A patent/CL2013000675A1/es unknown
-
2014
- 2014-02-05 US US14/173,170 patent/US9000024B2/en active Active
-
2017
- 2017-01-09 SM SM201700008T patent/SMT201700008B/it unknown
- 2017-01-19 CY CY20171100079T patent/CY1118680T1/el unknown
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