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 (25)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JO3296B1 (ar) * | 2012-06-29 | 2018-09-16 | Lilly Co Eli | مركبات فينوكسي إيثيل بيبريدين |
| WO2014200075A1 (ja) | 2013-06-12 | 2014-12-18 | 科研製薬株式会社 | ４－アルキニルイミダゾール誘導体およびそれを有効成分として含有する医薬 |
| 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 |
| KR102535283B1 (ko) * | 2014-05-23 | 2023-05-22 | 에자이 알앤드디 매니지먼트 가부시키가이샤 | 암의 치료를 위한 조합 요법 |
| 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 |
| CA2993312A1 (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 |
| WO2017066633A1 (en) | 2015-10-16 | 2017-04-20 | 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 |
| ES2896476T3 (es) | 2017-05-18 | 2022-02-24 | Idorsia Pharmaceuticals Ltd | Derivados de pirimidina |
| US11325899B2 (en) | 2017-05-18 | 2022-05-10 | Idorsia Pharmaceuticals Ltd | Benzofurane and benzothiophene derivatives as PGE2 receptor modulators |
| AR111808A1 (es) | 2017-05-18 | 2019-08-21 | Idorsia Pharmaceuticals Ltd | Derivados de pirimidina como moduladores del receptor de pge2 |
| HRP20211533T1 (hr) | 2017-05-18 | 2022-01-07 | Idorsia Pharmaceuticals Ltd | Derivati fenila kao modulatori receptora pge2 |
| TWI768043B (zh) | 2017-05-18 | 2022-06-21 | 瑞士商愛杜西亞製藥有限公司 | N-取代吲哚衍生物 |
| 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 |
| 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 |
| CN116801879B (zh) * | 2021-01-28 | 2025-09-26 | 深圳众格生物科技有限公司 | 吡唑酰胺衍生物及其制备方法和应用 |
| CA3230557A1 (en) * | 2021-09-03 | 2023-03-09 | Xuejun Zhang | Ep4 antagonist compound as well as salt, polymorph, and use thereof |
| 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 |
| CN118414328A (zh) | 2021-12-23 | 2024-07-30 | 卫材R&D管理有限公司 | Ep4拮抗剂的结晶盐形式 |
| JP2024544423A (ja) * | 2021-12-30 | 2024-11-29 | 杭州阿諾生物医薬科技有限公司 | 固体医薬組成物 |
| 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 |
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| 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 |
| WO2004037212A2 (en) | 2002-10-24 | 2004-05-06 | 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 |
| CN1832928B (zh) * | 2003-06-26 | 2012-07-04 | 诺瓦提斯公司 | 以5元杂环为基础的p38激酶抑制剂 |
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| 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 |
| KR101024227B1 (ko) | 2005-11-21 | 2011-03-29 | 시오노기세이야쿠가부시키가이샤 | 11-β-히드록시스테로이드 탈수소효소 제 Ⅰ 형에 대한저해 활성을 갖는 헤테로시클릭 화합물 |
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| 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 |
| CA2722811C (en) * | 2008-05-06 | 2016-07-05 | Boehringer Ingelheim International Gmbh | Pyrazole compounds as ccr1 antagonists |
| PL2565191T3 (pl) * | 2008-05-14 | 2015-03-31 | Astellas Pharma Inc | Pochodne kwasu 4-(indol-7-ilokarbonyloaminometylo)cykloheksanokarboksylowego jako antagoniści receptora EP4 użyteczni do leczenia przewlekłej niewydolności nerek lub nefropatii cukrzycowej |
| UA100291C2 (uk) | 2008-08-01 | 2012-12-10 | Байєр Кропсайнс Аг | Фунгіцидні похідні n-циклоалкіл-n-біфенілметилкарбоксаміду |
| CA2733247C (en) * | 2008-08-14 | 2018-04-03 | Beta Pharma Canada Inc. | Heterocyclic amide derivatives as ep4 receptor antagonists |
| WO2010034110A1 (en) | 2008-09-25 | 2010-04-01 | Merck Frosst Canada Ltd. | Beta-carboline sulphonylurea derivatives as ep4 receptor antagonists |
-
2011
- 2011-09-12 KR KR1020137004494A patent/KR101911105B1/ko active Active
- 2011-09-12 EP EP16161460.7A patent/EP3061751A1/en not_active Withdrawn
- 2011-09-12 MY MYPI2013700146A patent/MY162146A/en unknown
- 2011-09-12 ME MEP-2017-3A patent/ME02575B/me unknown
- 2011-09-12 PL PL11760631T patent/PL2619182T3/pl unknown
- 2011-09-12 DK DK11760631.9T patent/DK2619182T3/en active
- 2011-09-12 ES ES11760631.9T patent/ES2610185T3/es active Active
- 2011-09-12 HR HRP20170042TT patent/HRP20170042T1/hr unknown
- 2011-09-12 HU HUE11760631A patent/HUE031408T2/en unknown
- 2011-09-12 SG SG2013007174A patent/SG188188A1/en unknown
- 2011-09-12 NZ NZ60662911A patent/NZ606629A/en unknown
- 2011-09-12 SM SM20170008T patent/SMT201700008T1/it unknown
- 2011-09-12 BR BR112013002484-4A patent/BR112013002484B1/pt active IP Right Grant
- 2011-09-12 CN CN201180045222.XA patent/CN103097358B/zh active Active
- 2011-09-12 UA UAA201304961A patent/UA113499C2/uk unknown
- 2011-09-12 PT PT117606319T patent/PT2619182T/pt unknown
- 2011-09-12 EP EP11760631.9A patent/EP2619182B1/en active Active
- 2011-09-12 WO PCT/US2011/051163 patent/WO2012039972A1/en not_active Ceased
- 2011-09-12 MX MX2013003162A patent/MX2013003162A/es active IP Right Grant
- 2011-09-12 CA CA2806121A patent/CA2806121C/en active Active
- 2011-09-12 RS RS20170008A patent/RS55566B1/sr unknown
- 2011-09-12 SI SI201131067A patent/SI2619182T1/sl unknown
- 2011-09-12 PH PH1/2013/500467A patent/PH12013500467A1/en unknown
- 2011-09-12 AU AU2011305872A patent/AU2011305872B2/en active Active
- 2011-09-12 PE PE2013000320A patent/PE20131343A1/es active IP Right Grant
- 2011-09-12 RU RU2013118209A patent/RU2606510C2/ru active
- 2011-09-12 JP JP2013530177A patent/JP5956448B2/ja active Active
- 2011-09-12 LT LTEP11760631.9T patent/LT2619182T/lt unknown
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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
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2014
- 2014-02-05 US US14/173,170 patent/US9000024B2/en active Active
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2017
- 2017-01-09 SM SM201700008T patent/SMT201700008B/it unknown
- 2017-01-19 CY CY20171100079T patent/CY1118680T1/el unknown