JP2020520359A5 - - Google Patents
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- Publication number
- JP2020520359A5 JP2020520359A5 JP2019563494A JP2019563494A JP2020520359A5 JP 2020520359 A5 JP2020520359 A5 JP 2020520359A5 JP 2019563494 A JP2019563494 A JP 2019563494A JP 2019563494 A JP2019563494 A JP 2019563494A JP 2020520359 A5 JP2020520359 A5 JP 2020520359A5
- Authority
- JP
- Japan
- Prior art keywords
- pharmaceutically acceptable
- acceptable salt
- cancer
- compound according
- ethylamino
- 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
- 150000001875 compounds Chemical class 0.000 claims 14
- 150000003839 salts Chemical class 0.000 claims 14
- 206010028980 Neoplasm Diseases 0.000 claims 10
- 201000011510 cancer Diseases 0.000 claims 8
- 239000003814 drug Substances 0.000 claims 7
- 239000004480 active ingredient Substances 0.000 claims 5
- 238000011282 treatment Methods 0.000 claims 5
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 4
- 201000001320 Atherosclerosis Diseases 0.000 claims 2
- 208000010061 Autosomal Dominant Polycystic Kidney Diseases 0.000 claims 2
- 201000009273 Endometriosis Diseases 0.000 claims 2
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 2
- 206010035664 Pneumonia Diseases 0.000 claims 2
- 230000001154 acute effect Effects 0.000 claims 2
- 208000022185 autosomal dominant polycystic kidney disease Diseases 0.000 claims 2
- 125000001309 chloro group Chemical group Cl* 0.000 claims 2
- 125000004093 cyano group Chemical group *C#N 0.000 claims 2
- 201000010099 disease Diseases 0.000 claims 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 2
- 229940079593 drug Drugs 0.000 claims 2
- 230000035558 fertility Effects 0.000 claims 2
- 229910052739 hydrogen Inorganic materials 0.000 claims 2
- 239000001257 hydrogen Substances 0.000 claims 2
- 230000004770 neurodegeneration Effects 0.000 claims 2
- 208000015122 neurodegenerative disease Diseases 0.000 claims 2
- 230000002265 prevention Effects 0.000 claims 2
- 208000011580 syndromic disease Diseases 0.000 claims 2
- ZPRQXVPYQGBZON-UHFFFAOYSA-N 2-bromo-1h-indole Chemical compound C1=CC=C2NC(Br)=CC2=C1 ZPRQXVPYQGBZON-UHFFFAOYSA-N 0.000 claims 1
- BBRWMROCLLEJQO-UHFFFAOYSA-N 4-[6-[2-(2,7-dimethylindol-1-yl)ethylamino]pyrimidin-4-yl]benzoic acid Chemical compound CC=1N(C2=C(C=CC=C2C=1)C)CCNC1=CC(=NC=N1)C1=CC=C(C(=O)O)C=C1 BBRWMROCLLEJQO-UHFFFAOYSA-N 0.000 claims 1
- ZAIXSXCCJQKFKG-UHFFFAOYSA-N 4-[6-[2-(2-chloroindol-1-yl)ethylamino]pyrimidin-4-yl]benzoic acid Chemical compound ClC=1N(C2=CC=CC=C2C=1)CCNC1=CC(=NC=N1)C1=CC=C(C(=O)O)C=C1 ZAIXSXCCJQKFKG-UHFFFAOYSA-N 0.000 claims 1
- SXPJRHGUJPJOTF-UHFFFAOYSA-N 4-[6-[2-(2-cyanoindol-1-yl)ethylamino]pyrimidin-4-yl]benzoic acid Chemical compound C(#N)C=1N(C2=CC=CC=C2C=1)CCNC1=CC(=NC=N1)C1=CC=C(C(=O)O)C=C1 SXPJRHGUJPJOTF-UHFFFAOYSA-N 0.000 claims 1
- BTPBTZKFLVYUPZ-UHFFFAOYSA-N 4-[6-[2-(2-methylindol-1-yl)ethylamino]pyrimidin-4-yl]benzoic acid Chemical compound CC=1N(C2=CC=CC=C2C=1)CCNC1=CC(=NC=N1)C1=CC=C(C(=O)O)C=C1 BTPBTZKFLVYUPZ-UHFFFAOYSA-N 0.000 claims 1
- 206010005003 Bladder cancer Diseases 0.000 claims 1
- 206010008342 Cervix carcinoma Diseases 0.000 claims 1
- 208000008839 Kidney Neoplasms Diseases 0.000 claims 1
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 1
- 206010029260 Neuroblastoma Diseases 0.000 claims 1
- 206010033128 Ovarian cancer Diseases 0.000 claims 1
- 206010061535 Ovarian neoplasm Diseases 0.000 claims 1
- 206010038389 Renal cancer Diseases 0.000 claims 1
- 208000007097 Urinary Bladder Neoplasms Diseases 0.000 claims 1
- 208000006105 Uterine Cervical Neoplasms Diseases 0.000 claims 1
- 239000002246 antineoplastic agent Substances 0.000 claims 1
- 125000001246 bromo group Chemical group Br* 0.000 claims 1
- 201000010881 cervical cancer Diseases 0.000 claims 1
- 229940127089 cytotoxic agent Drugs 0.000 claims 1
- 210000000987 immune system Anatomy 0.000 claims 1
- 230000036039 immunity Effects 0.000 claims 1
- 208000028867 ischemia Diseases 0.000 claims 1
- 230000000302 ischemic effect Effects 0.000 claims 1
- 201000010982 kidney cancer Diseases 0.000 claims 1
- 201000005202 lung cancer Diseases 0.000 claims 1
- 208000020816 lung neoplasm Diseases 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 201000001441 melanoma Diseases 0.000 claims 1
- 210000004798 organs belonging to the digestive system Anatomy 0.000 claims 1
- 239000008177 pharmaceutical agent Substances 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 230000000069 prophylactic effect Effects 0.000 claims 1
- 238000011321 prophylaxis Methods 0.000 claims 1
- 238000001959 radiotherapy Methods 0.000 claims 1
- 238000002626 targeted therapy Methods 0.000 claims 1
- 201000005112 urinary bladder cancer Diseases 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EPPCT/EP2017/062008 | 2017-05-18 | ||
| EP2017062008 | 2017-05-18 | ||
| PCT/EP2018/062865 WO2018210995A1 (en) | 2017-05-18 | 2018-05-17 | N-substituted indole derivatives |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2020520359A JP2020520359A (ja) | 2020-07-09 |
| JP2020520359A5 true JP2020520359A5 (enExample) | 2021-07-26 |
| JP7065117B2 JP7065117B2 (ja) | 2022-05-11 |
Family
ID=62186481
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019563494A Active JP7065117B2 (ja) | 2017-05-18 | 2018-05-17 | Ｎ－置換インドール誘導体 |
Country Status (32)
Families Citing this family (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CR20180323A (es) | 2015-11-20 | 2018-08-06 | Idorsia Pharmaceuticals Ltd | Derivados de indol n-sustituídos como moduladores de los receptores de pge2 |
| AR111807A1 (es) | 2017-05-18 | 2019-08-21 | Idorsia Pharmaceuticals Ltd | Derivados de benzofurano y benzotiofeno como moduladores del receptor pge2 |
| HRP20211380T1 (hr) | 2017-05-18 | 2021-11-26 | Idorsia Pharmaceuticals Ltd | Derivati pirimidina kao modulatori receptora pge2 |
| 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 |
| AR111941A1 (es) | 2017-05-18 | 2019-09-04 | Idorsia Pharmaceuticals Ltd | Derivados de pirimidina como moduladores del receptor de pge2 |
| WO2021060281A1 (ja) * | 2019-09-24 | 2021-04-01 | Ａｇｃ株式会社 | プロスタグランジンｅ２レセプターｅｐ２／ｅｐ４デュアルアンタゴニスト |
| CN115697317A (zh) * | 2020-04-08 | 2023-02-03 | 株式会社AskAt | Ep4受体拮抗剂用于治疗肝癌、黑色素瘤、淋巴瘤和白血病的应用 |
| TW202228674A (zh) | 2020-11-13 | 2022-08-01 | 日商小野藥品工業股份有限公司 | 藉由併用ｅｐ４拮抗藥與免疫檢查點抑制物質而進行之癌症治療 |
| WO2025229177A1 (en) | 2024-05-02 | 2025-11-06 | Idorsia Pharmaceuticals Ltd | Crystalline forms of an n-substituted indole derivative |
Family Cites Families (63)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2003528144A (ja) | 2000-03-24 | 2003-09-24 | ファーマジーン ラボラトリーズ リミテッド | 頭痛治療のためのプロスタノイドｅｐ４受容体アンタゴニストの使用およびそのアンタゴニストについてのアッセイ |
| HN2001000224A (es) | 2000-10-19 | 2002-06-13 | Pfizer | Compuestos de imidazol condensado con arilo o heteroarilo como agentes anti - inflamatorios y analgesicos. |
| GB0031295D0 (en) | 2000-12-21 | 2001-01-31 | Glaxo Group Ltd | Naphthalene derivatives |
| GB0031302D0 (en) | 2000-12-21 | 2001-01-31 | Glaxo Group Ltd | Napthalene derivatives |
| GB0103269D0 (en) | 2001-02-09 | 2001-03-28 | Glaxo Group Ltd | Napthalene derivatives |
| BR0309305A (pt) | 2002-04-12 | 2005-02-15 | Pfizer | Compostos de imidazol como agentes antiinflamatórios e analgésicos |
| AU2003216581A1 (en) | 2002-04-12 | 2003-10-27 | Pfizer Inc. | Pyrazole compounds as anti-inflammatory and analgesic agents |
| JP2006506327A (ja) | 2002-05-23 | 2006-02-23 | セラテクノロジーズ インコーポレイティド | プロスタグランジンｅ２の受容体サブタイプｅｐ４のアンタゴニスト・ポリペプチド |
| CA2514220C (en) | 2003-01-29 | 2012-02-28 | Pharmagene Laboratories Limited | Ep4 receptor antagonists |
| AR045507A1 (es) * | 2003-08-26 | 2005-11-02 | Teijin Pharma Ltd | Derivados de pirrolo [3,2-d] pirimidina |
| ES2441206T3 (es) | 2003-09-03 | 2014-02-03 | Raqualia Pharma Inc. | Compuestos de fenil o piridilamida como antagonistas de la prostaglandina E2 |
| GB0324269D0 (en) | 2003-10-16 | 2003-11-19 | Pharmagene Lab Ltd | EP4 receptor antagonists |
| ES2327760T3 (es) | 2004-05-04 | 2009-11-03 | Raqualia Pharma Inc | Compuestos de aril-heteroaril-amida ortosustituidos. |
| WO2005105732A1 (en) | 2004-05-04 | 2005-11-10 | Pfizer Japan Inc. | Substituted methyl aryl or heteroaryl amide compounds |
| HN2005000795A (es) | 2004-10-15 | 2010-08-19 | Aventis Pharma Inc | Pirimidinas como antagonistas del receptor de prostaglandina d2 |
| EP1885722B1 (en) | 2005-05-19 | 2011-11-16 | Merck Canada Inc. | Quinoline derivatives as ep4 antagonists |
| WO2006128129A2 (en) | 2005-05-26 | 2006-11-30 | Synta Pharmaceuticals Corp. | Method for treating cancer |
| JP5244091B2 (ja) | 2006-04-24 | 2013-07-24 | メルク カナダ インコーポレイテッド | Ｅｐ４受容体アンタゴニストとしてのインドールアミド誘導体 |
| EP2035376B1 (en) | 2006-06-12 | 2014-08-27 | Merck Canada Inc. | Indoline amide derivatives as ep4 receptor ligands |
| WO2008008059A1 (en) | 2006-07-12 | 2008-01-17 | Locus Pharmaceuticals, Inc. | Anti-cancer agents ans uses thereof |
| AR061974A1 (es) | 2006-07-14 | 2008-08-10 | Novartis Ag | Derivados de pirimidina como inhibidores de alk, composiciones farmaceuticas y procesos de obtencion |
| WO2008017164A1 (en) | 2006-08-11 | 2008-02-14 | Merck Frosst Canada Ltd. | Thiophenecarboxamide derivatives as ep4 receptor ligands |
| WO2008039882A1 (en) | 2006-09-30 | 2008-04-03 | Sanofi-Aventis U.S. Llc | A combination of niacin and a prostaglandin d2 receptor antagonist |
| JP5301469B2 (ja) | 2007-02-26 | 2013-09-25 | メルク カナダ インコーポレイテッド | Ｅｐ４受容体アンタゴニストとしてのインドール及びインドリンシクロプロピルアミド誘導体 |
| CN101636385B (zh) | 2007-03-26 | 2012-09-05 | 默克弗罗斯特加拿大有限公司 | 作为ep4受体拮抗剂的萘和喹啉磺酰脲衍生物 |
| US8030489B2 (en) | 2007-03-26 | 2011-10-04 | Astellas Pharma Inc. | Ornithine derivative |
| EP2014657A1 (de) | 2007-06-21 | 2009-01-14 | Bayer Schering Pharma Aktiengesellschaft | Diaminopyrimidine als Modulatoren des EP2-Rezeptors |
| EP2460787A1 (en) | 2007-07-03 | 2012-06-06 | Astellas Pharma Inc. | Amide compounds and their use as PGE2 antagonists. |
| KR101612971B1 (ko) | 2008-05-14 | 2016-04-15 | 아스테라스 세이야쿠 가부시키가이샤 | 아미드 화합물 |
| CA2733247C (en) | 2008-08-14 | 2018-04-03 | Beta Pharma Canada Inc. | Heterocyclic amide derivatives as ep4 receptor antagonists |
| WO2010032123A1 (en) | 2008-09-19 | 2010-03-25 | Biotechnology Research Corporation Limited | Triterpenoid compounds and methods of use thereof |
| AU2009295308A1 (en) | 2008-09-25 | 2010-04-01 | Merck Canada Inc. | Beta-carboline sulphonylurea derivatives as EP4 receptor antagonists |
| CN103003264B (zh) | 2010-05-21 | 2014-08-06 | 切米利亚股份公司 | 嘧啶衍生物 |
| LT2619182T (lt) | 2010-09-21 | 2017-01-25 | Eisai R&D Management Co., Ltd. | Farmacinė kompozicija |
| WO2012043634A1 (ja) | 2010-09-29 | 2012-04-05 | 株式会社エヌビィー健康研究所 | ヒトプロスタグランジンｅ２受容体ｅｐ４に対する抗体 |
| EP2649061B1 (en) | 2010-12-10 | 2015-05-13 | Rottapharm Biotech S.r.l. | Pyridine amide derivatives as ep4 receptor antagonists |
| WO2012103071A2 (en) | 2011-01-25 | 2012-08-02 | Eisai R&D Management Co., Ltd. | Compounds and compositions |
| AU2012230229A1 (en) | 2011-03-24 | 2013-10-10 | Noviga Research Ab | Novel pyrimidine derivatives |
| KR101760164B1 (ko) | 2011-07-04 | 2017-07-20 | 로타팜 바이오테크 에스.알.엘 | Ep4 수용체 길항제로서 사이클릭 아민 유도체 |
| EP2554662A1 (en) | 2011-08-05 | 2013-02-06 | M Maria Pia Cosma | Methods of treatment of retinal degeneration diseases |
| US20150004175A1 (en) | 2011-12-13 | 2015-01-01 | Yale University | Compositions and Methods for Reducing CTL Exhaustion |
| IN2014KN02601A (enExample) | 2012-04-24 | 2015-05-08 | Vertex Pharma | |
| TWI572597B (zh) | 2012-06-29 | 2017-03-01 | 美國禮來大藥廠 | 二甲基－苯甲酸化合物 |
| JO3296B1 (ar) | 2012-06-29 | 2018-09-16 | Lilly Co Eli | مركبات فينوكسي إيثيل بيبريدين |
| UA115576C2 (uk) | 2012-12-06 | 2017-11-27 | Байєр Фарма Акцієнгезелльшафт | Похідні бензимідазолу як антагоністи ер4 |
| EP2765128A1 (en) | 2013-02-07 | 2014-08-13 | Almirall, S.A. | Substituted benzamides with activity towards EP4 receptors |
| TW201443004A (zh) | 2013-02-15 | 2014-11-16 | Lilly Co Eli | 苯氧基乙氧基化合物 |
| TWI636046B (zh) | 2013-05-17 | 2018-09-21 | 美國禮來大藥廠 | 苯氧基乙基二氫－１ｈ－異喹啉化合物 |
| RS57406B1 (sr) | 2013-06-12 | 2018-09-28 | Kaken Pharmaceutical Co Ltd | Derivat 4-alkinil imidazola i lekovi koji ga sadrže kao aktivni sastojak |
| JP6417419B2 (ja) | 2013-09-04 | 2018-11-07 | ブリストル−マイヤーズ スクイブ カンパニーＢｒｉｓｔｏｌ−Ｍｙｅｒｓ Ｓｑｕｉｂｂ Ｃｏｍｐａｎｙ | 免疫調節剤として有用な化合物 |
| EA030155B1 (ru) | 2013-09-06 | 2018-06-29 | Ауриген Дискавери Текнолоджиз Лимитед | Производные 1,2,4-оксадиазола в качестве иммуномодуляторов |
| WO2015044900A1 (en) | 2013-09-27 | 2015-04-02 | Aurigene Discovery Technologies Limited | Therapeutic immunomodulating compounds |
| RS57306B1 (sr) | 2013-10-17 | 2018-08-31 | Vertex Pharma | Inhibitori dnk-pk |
| WO2015094902A1 (en) | 2013-12-17 | 2015-06-25 | Eli Lilly And Company | Phenoxyethyl cyclic amine derivatives and their activity as ep4 receptor modulators |
| HRP20190793T1 (hr) | 2013-12-17 | 2019-06-28 | Eli Lilly & Company | Spojevi dimetilbenzojeve kiseline |
| TW201607943A (zh) | 2013-12-19 | 2016-03-01 | 拜耳製藥公司 | 作為ｅｐ４配體之新穎苯并咪唑衍生物 |
| 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 |
| SG11201609770TA (en) | 2014-05-23 | 2016-12-29 | Eisai R&D Man Co Ltd | Combination therapies for the treatment of cancer |
| WO2016021742A1 (en) | 2014-08-07 | 2016-02-11 | Takeda Pharmaceutical Company Limited | Heterocyclic compounds as ep4 receptor antagonists |
| WO2016054807A1 (en) * | 2014-10-10 | 2016-04-14 | Merck Sharp & Dohme Corp. | TrkA KINASE INHIBITORS, COMPOSITIONS AND METHODS THEREOF |
| TWI852872B (zh) | 2015-01-09 | 2024-08-11 | 日商小野藥品工業股份有限公司 | 三環性螺化合物之用途 |
| 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 |
| AU2016338679B2 (en) | 2015-10-16 | 2021-05-06 | Eisai R&D Management Co., Ltd. | EP4 antagonists |
-
2018
- 2018-05-17 SI SI201830413T patent/SI3625224T1/sl unknown
- 2018-05-17 PT PT18725223T patent/PT3625224T/pt unknown
- 2018-05-17 SG SG11201908660R patent/SG11201908660RA/en unknown
- 2018-05-17 EA EA201992679A patent/EA039630B1/ru unknown
- 2018-05-17 UA UAA201911973A patent/UA124748C2/uk unknown
- 2018-05-17 MX MX2019013639A patent/MX394108B/es unknown
- 2018-05-17 US US16/614,268 patent/US20200069686A1/en not_active Abandoned
- 2018-05-17 WO PCT/EP2018/062865 patent/WO2018210995A1/en not_active Ceased
- 2018-05-17 AU AU2018269667A patent/AU2018269667B2/en not_active Ceased
- 2018-05-17 JP JP2019563494A patent/JP7065117B2/ja active Active
- 2018-05-17 PH PH1/2019/502562A patent/PH12019502562B1/en unknown
- 2018-05-17 CA CA3063637A patent/CA3063637A1/en active Pending
- 2018-05-17 KR KR1020197037058A patent/KR102650756B1/ko active Active
- 2018-05-17 ES ES18725223T patent/ES2894124T3/es active Active
- 2018-05-17 LT LTEPPCT/EP2018/062865T patent/LT3625224T/lt unknown
- 2018-05-17 PE PE2019002413A patent/PE20191787A1/es unknown
- 2018-05-17 RS RS20211259A patent/RS62441B1/sr unknown
- 2018-05-17 MA MA49127A patent/MA49127B1/fr unknown
- 2018-05-17 DK DK18725223.4T patent/DK3625224T3/da active
- 2018-05-17 EP EP18725223.4A patent/EP3625224B1/en active Active
- 2018-05-17 CN CN201880031869.9A patent/CN110621666A/zh active Pending
- 2018-05-17 HU HUE18725223A patent/HUE056406T2/hu unknown
- 2018-05-17 HR HRP20211532TT patent/HRP20211532T1/hr unknown
- 2018-05-17 PL PL18725223T patent/PL3625224T3/pl unknown
- 2018-05-17 CR CR20190567A patent/CR20190567A/es unknown
- 2018-05-17 BR BR112019024114-0A patent/BR112019024114A2/pt not_active Application Discontinuation
- 2018-05-17 AR ARP180101311A patent/AR111806A1/es not_active Application Discontinuation
- 2018-05-17 TW TW107116708A patent/TWI768043B/zh not_active IP Right Cessation
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2019
- 2019-09-30 CO CONC2019/0010804A patent/CO2019010804A2/es unknown
- 2019-11-13 IL IL270616A patent/IL270616B/en unknown
- 2019-11-14 CL CL2019003257A patent/CL2019003257A1/es unknown
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2021
- 2021-09-27 CY CY20211100841T patent/CY1124528T1/el unknown
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2022
- 2022-11-27 US US18/058,873 patent/US20230165859A1/en active Pending