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 |
| BR112015030315B1 (pt) * | 2013-06-12 | 2022-10-04 | Kaken Pharmaceutical Co., Ltd | Derivado de 4-alquinilimidazol e produto farmacêutico que o compreende e antagonista de receptor de ep4 |
| 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 |
| WO2015179615A1 (en) * | 2014-05-23 | 2015-11-26 | 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 |
| WO2017014323A1 (en) | 2015-07-23 | 2017-01-26 | Takeda Pharmaceutical Company Limited | 1-substituted 1,2,3,4-tetrahydro-1,7-naphthyridin-8-amine derivatives and their use as ep4 receptor antagonists |
| CA3002144C (en) | 2015-10-16 | 2024-01-23 | Eisai R&D Management Co., Ltd. | Ep4 antagonists |
| CR20180323A (es) | 2015-11-20 | 2018-08-06 | Idorsia Pharmaceuticals Ltd | Derivados de indol n-sustituídos como moduladores de los receptores de pge2 |
| AU2018268311B2 (en) | 2017-05-18 | 2022-02-10 | Idorsia Pharmaceuticals Ltd | Pyrimidine derivatives as PGE2 receptor modulators |
| CN110612296A (zh) | 2017-05-18 | 2019-12-24 | 爱杜西亚药品有限公司 | 作为pge2受体调节剂的苯基衍生物 |
| TW201900180A (zh) | 2017-05-18 | 2019-01-01 | 瑞士商愛杜西亞製藥有限公司 | 嘧啶衍生物 |
| 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 |
| MX394108B (es) | 2017-05-18 | 2025-03-21 | Idorsia Pharmaceuticals Ltd | Derivados de indol n-sustituidos. |
| 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 |
| CN117643587A (zh) * | 2018-02-05 | 2024-03-05 | 深圳市原力生命科学有限公司 | 用于治疗癌症的杂二环羧酸 |
| EP4116291A4 (en) * | 2020-03-04 | 2024-03-06 | Wuhan Humanwell Innovative Drug Research and Development Center Limited Company | SYNTHESIS OF A NEW EP4 ANTAGONIST AND USE IN CANCER AND INFLAMMATION |
| WO2022037601A1 (zh) * | 2020-08-18 | 2022-02-24 | 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制备治疗癌症和炎症药物中的用途 |
| KR20230107228A (ko) | 2020-11-13 | 2023-07-14 | 오노 야꾸힝 고교 가부시키가이샤 | Ep4 길항약과 면역 체크포인트 저해 물질의 병용에 의한 암 치료 |
| 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 |
| US7393842B2 (en) | 2001-08-31 | 2008-07-01 | University Of Connecticut | Pyrazole analogs acting on cannabinoid receptors |
| US7119108B1 (en) | 1999-10-18 | 2006-10-10 | University Of Connecticut | Pyrazole derivatives as cannabinoid receptor antagonists |
| 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 |
| ES2393950T3 (es) * | 2003-06-26 | 2013-01-02 | Novartis Ag | Inhibidores de la quinasa P38 con base en heterociclos de 5 miembros |
| RS20060143A (sr) | 2003-09-03 | 2008-06-05 | Pfizer Inc., | Jedinjenja fenil ili piridil amida kao antagonisti prostaglandina e2 |
| WO2005070889A1 (en) | 2004-01-23 | 2005-08-04 | E.I. Dupont De Nemours And Company | Herbicidal amides |
| MXPA06011555A (es) * | 2004-05-04 | 2006-12-15 | Pfizer | Compuestos de metil-aril o heteroaril-amida sustituida. |
| 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 |
| US8952176B2 (en) | 2005-06-07 | 2015-02-10 | Shionogi & Co., Ltd. | Heterocyclic compound having type I 11 β hydroxysteroid dehydrogenase inhibitory activity |
| US20090131470A1 (en) * | 2005-06-11 | 2009-05-21 | 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 |
| WO2007058346A1 (ja) | 2005-11-21 | 2007-05-24 | Shionogi & Co., Ltd. | I型11βヒドロキシステロイド脱水素酵素阻害活性を有するヘテロ環化合物 |
| JP5218737B2 (ja) * | 2006-02-06 | 2013-06-26 | 大正製薬株式会社 | スフィンゴシン−１−リン酸結合阻害物質 |
| US7705035B2 (en) | 2006-06-12 | 2010-04-27 | Merck Frosst Canada Ltd. | Indoline amide derivatives as EP4 receptor ligands |
| WO2008017164A1 (en) | 2006-08-11 | 2008-02-14 | Merck Frosst Canada Ltd. | Thiophenecarboxamide derivatives as ep4 receptor ligands |
| NZ577109A (en) | 2006-12-15 | 2011-12-22 | Glaxo Group Ltd | Benzamide derivatives as ep4 receptor agonists |
| ES2400293T3 (es) | 2007-02-26 | 2013-04-08 | Merck Canada Inc. | Derivados de indol e indolina ciclopropilamida como antagonistas de receptores EP4 |
| US7560936B1 (en) | 2007-04-24 | 2009-07-14 | Integrated Device Technology, Inc. | Method and apparatus for ground bounce and power supply bounce detection |
| AU2008263883B2 (en) | 2007-06-15 | 2014-03-13 | Basf Se | Method for producing difluoromethyl-substituted pyrazole compounds |
| EP2460787A1 (en) | 2007-07-03 | 2012-06-06 | Astellas Pharma Inc. | Amide compounds and their use as PGE2 antagonists. |
| AU2008275891B2 (en) * | 2007-07-19 | 2013-10-10 | H.Lundbeck A/S | 5-membered heterocyclic amides and related compounds |
| AR067744A1 (es) | 2007-07-31 | 2009-10-21 | Bayer Cropscience Sa | Derivados fungicidas de (hetero) aril- metilen -n- cicloalquil carboxamida condensados de 6 elementos con n |
| GB0721611D0 (en) | 2007-11-02 | 2007-12-12 | Glaxo Group Ltd | Novel compounds |
| WO2009137338A1 (en) * | 2008-05-06 | 2009-11-12 | Boehringer Ingelheim International Gmbh | Pyrazole compounds as ccr1 antagonists |
| US8598355B2 (en) * | 2008-05-14 | 2013-12-03 | Astellas Pharma Inc. | Amide compound |
| PL2310360T3 (pl) | 2008-08-01 | 2013-07-31 | Bayer Ip Gmbh | Grzybobójcze pochodne N-cykloalkilo-N-bifenylometylo-karboksamidu |
| US8404736B2 (en) * | 2008-08-14 | 2013-03-26 | Beta Pharma Canada Inc. | Heterocyclic amide derivatives as EP4 receptor antagonists |
| AU2009295308A1 (en) | 2008-09-25 | 2010-04-01 | Merck Canada Inc. | Beta-carboline sulphonylurea derivatives as EP4 receptor antagonists |
-
2011
- 2011-09-12 EP EP16161460.7A patent/EP3061751A1/en not_active Withdrawn
- 2011-09-12 JP JP2013530177A patent/JP5956448B2/ja active Active
- 2011-09-12 ES ES11760631.9T patent/ES2610185T3/es active Active
- 2011-09-12 RS RS20170008A patent/RS55566B1/sr unknown
- 2011-09-12 PE PE2013000320A patent/PE20131343A1/es active IP Right Grant
- 2011-09-12 PL PL11760631T patent/PL2619182T3/pl unknown
- 2011-09-12 LT LTEP11760631.9T patent/LT2619182T/lt unknown
- 2011-09-12 PH PH1/2013/500467A patent/PH12013500467A1/en unknown
- 2011-09-12 CN CN201180045222.XA patent/CN103097358B/zh active Active
- 2011-09-12 HR HRP20170042TT patent/HRP20170042T1/hr unknown
- 2011-09-12 KR KR1020137004494A patent/KR101911105B1/ko active Active
- 2011-09-12 RU RU2013118209A patent/RU2606510C2/ru active
- 2011-09-12 PT PT117606319T patent/PT2619182T/pt unknown
- 2011-09-12 SI SI201131067A patent/SI2619182T1/sl unknown
- 2011-09-12 WO PCT/US2011/051163 patent/WO2012039972A1/en not_active Ceased
- 2011-09-12 HU HUE11760631A patent/HUE031408T2/en unknown
- 2011-09-12 EP EP11760631.9A patent/EP2619182B1/en active Active
- 2011-09-12 ME MEP-2017-3A patent/ME02575B/me unknown
- 2011-09-12 UA UAA201304961A patent/UA113499C2/uk unknown
- 2011-09-12 DK DK11760631.9T patent/DK2619182T3/en active
- 2011-09-12 NZ NZ60662911A patent/NZ606629A/en unknown
- 2011-09-12 BR BR112013002484-4A patent/BR112013002484B1/pt active IP Right Grant
- 2011-09-12 AU AU2011305872A patent/AU2011305872B2/en active Active
- 2011-09-12 MY MYPI2013700146A patent/MY162146A/en unknown
- 2011-09-12 SG SG2013007174A patent/SG188188A1/en unknown
- 2011-09-12 SM SM20170008T patent/SMT201700008T1/it unknown
- 2011-09-12 MX MX2013003162A patent/MX2013003162A/es active IP Right Grant
- 2011-09-12 CA CA2806121A patent/CA2806121C/en active Active
-
2013
- 2013-01-17 IL IL224288A patent/IL224288A/en active IP Right Grant
- 2013-03-12 CL CL2013000675A patent/CL2013000675A1/es unknown
- 2013-03-12 US US13/795,768 patent/US8686018B2/en active Active
-
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