SI3004090T1 - Chemical compounds - Google Patents
Chemical compounds Download PDFInfo
- Publication number
- SI3004090T1 SI3004090T1 SI201430531T SI201430531T SI3004090T1 SI 3004090 T1 SI3004090 T1 SI 3004090T1 SI 201430531 T SI201430531 T SI 201430531T SI 201430531 T SI201430531 T SI 201430531T SI 3004090 T1 SI3004090 T1 SI 3004090T1
- Authority
- SI
- Slovenia
- Prior art keywords
- fluoro
- pyrido
- indol
- phenyl
- methylpropyl
- Prior art date
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- 150000001875 compounds Chemical class 0.000 title claims abstract 20
- 150000003839 salts Chemical class 0.000 claims abstract 13
- 239000008194 pharmaceutical composition Substances 0.000 claims abstract 4
- DFBDRVGWBHBJNR-BBNFHIFMSA-N (e)-3-[3,5-difluoro-4-[(1r,3r)-2-(2-fluoro-2-methylpropyl)-3-methyl-1,3,4,9-tetrahydropyrido[3,4-b]indol-1-yl]phenyl]prop-2-enoic acid Chemical compound C1([C@@H]2C3=C(C4=CC=CC=C4N3)C[C@H](N2CC(C)(C)F)C)=C(F)C=C(\C=C\C(O)=O)C=C1F DFBDRVGWBHBJNR-BBNFHIFMSA-N 0.000 claims 4
- -1 2-fluoro-2-methylpropyl Chemical group 0.000 claims 4
- 206010028980 Neoplasm Diseases 0.000 claims 4
- 201000011510 cancer Diseases 0.000 claims 4
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 4
- SMZOUWXMTYCWNB-UHFFFAOYSA-N 2-(2-methoxy-5-methylphenyl)ethanamine Chemical compound COC1=CC=C(C)C=C1CCN SMZOUWXMTYCWNB-UHFFFAOYSA-N 0.000 claims 3
- NIXOWILDQLNWCW-UHFFFAOYSA-N 2-Propenoic acid Natural products OC(=O)C=C NIXOWILDQLNWCW-UHFFFAOYSA-N 0.000 claims 3
- 229910052739 hydrogen Inorganic materials 0.000 claims 3
- 125000000593 indol-1-yl group Chemical group [H]C1=C([H])C([H])=C2N([*])C([H])=C([H])C2=C1[H] 0.000 claims 3
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 2
- 239000003085 diluting agent Substances 0.000 claims 2
- 239000001257 hydrogen Substances 0.000 claims 2
- 239000000203 mixture Substances 0.000 claims 2
- 238000000634 powder X-ray diffraction Methods 0.000 claims 2
- STVQFMFTCUMADM-XGMWYDOHSA-N (e)-3-[3,5-difluoro-4-[(1r,3r)-2-[(2s)-3-fluoro-2-methylpropyl]-3-methyl-1,3,4,9-tetrahydropyrido[3,4-b]indol-1-yl]phenyl]prop-2-enoic acid Chemical compound C1([C@@H]2C3=C(C4=CC=CC=C4N3)C[C@@H](C)N2C[C@@H](CF)C)=C(F)C=C(\C=C\C(O)=O)C=C1F STVQFMFTCUMADM-XGMWYDOHSA-N 0.000 claims 1
- XTDHJGCTXMSPCY-RSEBSXLISA-N (e)-3-[3,5-difluoro-4-[2-[(2s)-3-fluoro-2-methylpropyl]-3,3-dimethyl-4,9-dihydro-1h-pyrido[3,4-b]indol-1-yl]phenyl]prop-2-enoic acid Chemical compound C1=2NC3=CC=CC=C3C=2CC(C)(C)N(C[C@@H](CF)C)C1C1=C(F)C=C(\C=C\C(O)=O)C=C1F XTDHJGCTXMSPCY-RSEBSXLISA-N 0.000 claims 1
- IOPRLAHXDGSIHG-NAUGMMEESA-N (e)-3-[3-fluoro-4-[2-[(2s)-3-fluoro-2-methylpropyl]-3,3-dimethyl-4,9-dihydro-1h-pyrido[3,4-b]indol-1-yl]phenyl]prop-2-enoic acid Chemical compound C1=2NC3=CC=CC=C3C=2CC(C)(C)N(C[C@@H](CF)C)C1C1=CC=C(\C=C\C(O)=O)C=C1F IOPRLAHXDGSIHG-NAUGMMEESA-N 0.000 claims 1
- DFBDRVGWBHBJNR-NYKMLEKOSA-N (e)-3-[4-[(1r,3r)-1-deuterio-2-(2-fluoro-2-methylpropyl)-3-methyl-4,9-dihydro-3h-pyrido[3,4-b]indol-1-yl]-3,5-difluorophenyl]prop-2-enoic acid Chemical compound C1([C@@]2(C3=C(C4=CC=CC=C4N3)C[C@@H](C)N2CC(C)(C)F)[2H])=C(F)C=C(\C=C\C(O)=O)C=C1F DFBDRVGWBHBJNR-NYKMLEKOSA-N 0.000 claims 1
- HYPDMBONKGTBLC-NVEBTIFVSA-N (e)-3-[4-[(1r,3r)-2-(2-fluoro-2-methylpropyl)-3-methyl-1,3,4,9-tetrahydropyrido[3,4-b]indol-1-yl]phenyl]prop-2-enoic acid Chemical compound C1([C@@H]2C3=C(C4=CC=CC=C4N3)C[C@H](N2CC(C)(C)F)C)=CC=C(\C=C\C(O)=O)C=C1 HYPDMBONKGTBLC-NVEBTIFVSA-N 0.000 claims 1
- CLDCRFJRMORRTI-IEGMAYJBSA-N (e)-3-[4-[(1r,3r)-2-[(2s)-3-fluoro-2-methylpropyl]-3-methyl-1,3,4,9-tetrahydropyrido[3,4-b]indol-1-yl]phenyl]prop-2-enoic acid Chemical compound C1([C@@H]2C3=C(C4=CC=CC=C4N3)C[C@@H](C)N2C[C@@H](CF)C)=CC=C(\C=C\C(O)=O)C=C1 CLDCRFJRMORRTI-IEGMAYJBSA-N 0.000 claims 1
- RZLKPYCEHAUODL-SDNWHVSQSA-N (e)-3-[4-[2-(2-fluoro-2-methylpropyl)-3,3-dimethyl-4,9-dihydro-1h-pyrido[3,4-b]indol-1-yl]phenyl]prop-2-enoic acid Chemical compound C1=2NC3=CC=CC=C3C=2CC(C)(C)N(CC(C)(F)C)C1C1=CC=C(\C=C\C(O)=O)C=C1 RZLKPYCEHAUODL-SDNWHVSQSA-N 0.000 claims 1
- WRHLOSDZEZAYKX-WFSDQYTKSA-N (e)-3-[4-[2-[(2s)-3-fluoro-2-methylpropyl]-3,3-dimethyl-4,9-dihydro-1h-pyrido[3,4-b]indol-1-yl]phenyl]prop-2-enoic acid Chemical compound C1=2NC3=CC=CC=C3C=2CC(C)(C)N(C[C@@H](CF)C)C1C1=CC=C(\C=C\C(O)=O)C=C1 WRHLOSDZEZAYKX-WFSDQYTKSA-N 0.000 claims 1
- NIXOWILDQLNWCW-UHFFFAOYSA-M Acrylate Chemical compound [O-]C(=O)C=C NIXOWILDQLNWCW-UHFFFAOYSA-M 0.000 claims 1
- 206010006187 Breast cancer Diseases 0.000 claims 1
- 208000026310 Breast neoplasm Diseases 0.000 claims 1
- 239000003963 antioxidant agent Substances 0.000 claims 1
- 230000003078 antioxidant effect Effects 0.000 claims 1
- 239000002738 chelating agent Substances 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 201000010255 female reproductive organ cancer Diseases 0.000 claims 1
- 125000001153 fluoro group Chemical group F* 0.000 claims 1
- 150000002688 maleic acid derivatives Chemical class 0.000 claims 1
- 239000002184 metal Substances 0.000 claims 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 1
- 230000002265 prevention Effects 0.000 claims 1
- 238000000034 method Methods 0.000 abstract 1
- 230000002062 proliferating effect Effects 0.000 abstract 1
Classifications
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- 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
- A61K31/437—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
-
- 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
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C57/00—Unsaturated compounds having carboxyl groups bound to acyclic carbon atoms
- C07C57/02—Unsaturated compounds having carboxyl groups bound to acyclic carbon atoms with only carbon-to-carbon double bonds as unsaturation
- C07C57/13—Dicarboxylic acids
- C07C57/145—Maleic acid
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B2200/00—Indexing scheme relating to specific properties of organic compounds
- C07B2200/07—Optical isomers
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B2200/00—Indexing scheme relating to specific properties of organic compounds
- C07B2200/13—Crystalline forms, e.g. polymorphs
Landscapes
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Epidemiology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Endocrinology (AREA)
- Reproductive Health (AREA)
- Engineering & Computer Science (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Medicinal Preparation (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Indole Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
Applications Claiming Priority (4)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201361827951P | 2013-05-28 | 2013-05-28 | |
| US201361915685P | 2013-12-13 | 2013-12-13 | |
| PCT/GB2014/051607 WO2014191726A1 (en) | 2013-05-28 | 2014-05-27 | Chemical compounds |
| EP14727036.7A EP3004090B1 (en) | 2013-05-28 | 2014-05-27 | Chemical compounds |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| SI3004090T1 true SI3004090T1 (en) | 2018-01-31 |
Family
ID=50841880
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| SI201430531T SI3004090T1 (en) | 2013-05-28 | 2014-05-27 | Chemical compounds |
Country Status (35)
Families Citing this family (94)
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|---|---|---|---|---|
| JP5977837B2 (ja) | 2011-12-21 | 2016-08-24 | ノヴィラ・セラピューティクス・インコーポレイテッド | Ｂ型肝炎抗ウイルス剤 |
| CN104902885A (zh) | 2012-08-28 | 2015-09-09 | 爱尔兰詹森科学公司 | 氨磺酰基-芳基酰胺和其作为药物用于治疗乙型肝炎的用途 |
| BR112015020242A2 (pt) | 2013-02-28 | 2017-07-18 | Janssen Sciences Ireland Uc | sulfamoil-arilamidas e seu uso como medicamentos para o tratamento da hepatite b |
| JP6419155B2 (ja) | 2013-04-03 | 2018-11-07 | ヤンセン・サイエンシズ・アイルランド・ユーシー | Ｎ−フェニル−カルボキサミド誘導体およびｂ型肝炎を治療するための医薬品としてのその使用 |
| JO3603B1 (ar) | 2013-05-17 | 2020-07-05 | Janssen Sciences Ireland Uc | مشتقات سلفامويل بيرولاميد واستخدامها كادوية لمعالجة التهاب الكبد نوع بي |
| MX366787B (es) | 2013-05-17 | 2019-07-23 | Janssen Sciences Ireland Uc | Derivados de sulfamoiltiofenamida y su uso como medicamentos para tratar la hepatitis b. |
| DK3024819T3 (en) | 2013-07-25 | 2018-06-06 | Janssen Sciences Ireland Uc | GLYOXAMIDE-SUBSTITUTED PYRROLAMIDE DERIVATIVES AND THE USE THEREOF AS MEDICINES FOR TREATING HEPATITIS B |
| EA034448B1 (ru) | 2013-10-23 | 2020-02-10 | Янссен Сайенсиз Айрлэнд Юси | Производные карбоксамида и их применение в качестве медикаментов для лечения гепатита b |
| US10392349B2 (en) | 2014-01-16 | 2019-08-27 | Novira Therapeutics, Inc. | Azepane derivatives and methods of treating hepatitis B infections |
| US9169212B2 (en) | 2014-01-16 | 2015-10-27 | Novira Therapeutics, Inc. | Azepane derivatives and methods of treating hepatitis B infections |
| CN106232136A (zh) | 2014-02-05 | 2016-12-14 | 诺维拉治疗公司 | 用于治疗hbv感染的联合疗法 |
| CA2932551A1 (en) | 2014-02-06 | 2015-08-13 | Janssen Sciences Ireland Uc | Sulphamoylpyrrolamide derivatives and the use thereof as medicaments for the treatment of hepatitis b |
| IL301960B2 (en) | 2014-12-18 | 2024-08-01 | Hoffmann La Roche | Tetrahydro-pyrido[3, 4-b]indole estrogen receptor modulators and their uses |
| WO2016146591A1 (en) * | 2015-03-16 | 2016-09-22 | Astrazeneca Ab | Combination treatment |
| CA2980298A1 (en) | 2015-03-19 | 2016-09-22 | Novira Therapeutics, Inc. | Azocane and azonane derivatives and methods of treating hepatitis b infections |
| JP2018521988A (ja) * | 2015-06-16 | 2018-08-09 | ジエンス ヘンルイ メデイシンカンパニー リミテッドＪｉａｎｇｓｕ Ｈｅｎｇｒｕｉ Ｍｅｄｉｃｉｎｅ Ｃｏ．，Ｌｔｄ． | ピペリジン誘導体およびその製造方法および医薬用途 |
| US10875876B2 (en) | 2015-07-02 | 2020-12-29 | Janssen Sciences Ireland Uc | Cyclized sulfamoylarylamide derivatives and the use thereof as medicaments for the treatment of hepatitis B |
| AU2016301196B2 (en) | 2015-08-06 | 2022-09-08 | Dana-Farber Cancer Institute, Inc. | Tunable endogenous protein degradation |
| CN108430971A (zh) | 2015-09-29 | 2018-08-21 | 诺维拉治疗公司 | 乙型肝炎抗病毒剂的晶体形式 |
| PL3355884T3 (pl) * | 2015-10-01 | 2021-11-29 | Olema Pharmaceuticals, Inc. | Tetrahydro-1H-pirydo[3,4-b]indolowe leki antyestrogenowe |
| CA3011391C (en) * | 2015-11-12 | 2021-02-09 | Zhejiang Hisun Pharmaceutical Co., Ltd. | Acrylic acid derivative, preparation method and use in medicine thereof |
| LT3386500T (lt) | 2015-12-09 | 2022-12-27 | The Board Of Trustees Of The University Of Illinois | Selektyvūs estrogenų receptorių slopintojai benzotiofeno pagrindu |
| JP2019503346A (ja) | 2015-12-22 | 2019-02-07 | ジエンス ヘンルイ メデイシンカンパニー リミテッドＪｉａｎｇｓｕ Ｈｅｎｇｒｕｉ Ｍｅｄｉｃｉｎｅ Ｃｏ．，Ｌｔｄ． | ベンゾピペリジン誘導体、その製造方法及びその医薬用途 |
| WO2017136688A1 (en) * | 2016-02-05 | 2017-08-10 | Inventisbio Inc. | Selective estrogen receptor degraders and uses thereof |
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| CN109640980A (zh) | 2016-04-15 | 2019-04-16 | 诺维拉治疗公司 | 包含壳体装配抑制剂的组合和方法 |
| TW201803870A (zh) | 2016-04-20 | 2018-02-01 | 阿斯特捷利康公司 | 化學化合物 |
| EP3449017B1 (en) * | 2016-04-29 | 2021-12-22 | Board of Regents, The University of Texas System | Targeted measure of transcriptional activity related to hormone receptors |
| WO2017197904A2 (zh) * | 2016-05-08 | 2017-11-23 | 上海诚妙医药科技有限公司 | 帕布昔利布的新晶型及其制备方法及其用途 |
| EP3454862B1 (en) | 2016-05-10 | 2024-09-11 | C4 Therapeutics, Inc. | Spirocyclic degronimers for target protein degradation |
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| TW201835064A (zh) | 2017-02-10 | 2018-10-01 | 美商G1治療公司 | 苯并噻吩雌激素受體調節劑 |
| CN108864080B (zh) * | 2017-05-09 | 2021-10-15 | 南京圣和药业股份有限公司 | 作为选择性雌激素受体下调剂的四环类化合物及其应用 |
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