JP2008545803A5 - - Google Patents
Download PDFInfo
- Publication number
- JP2008545803A5 JP2008545803A5 JP2008516155A JP2008516155A JP2008545803A5 JP 2008545803 A5 JP2008545803 A5 JP 2008545803A5 JP 2008516155 A JP2008516155 A JP 2008516155A JP 2008516155 A JP2008516155 A JP 2008516155A JP 2008545803 A5 JP2008545803 A5 JP 2008545803A5
- Authority
- JP
- Japan
- Prior art keywords
- aryl
- heteroaryl
- formula
- compound
- hal
- 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 32
- 206010028980 Neoplasm Diseases 0.000 claims 10
- 150000003839 salts Chemical class 0.000 claims 10
- 239000000203 mixture Substances 0.000 claims 7
- 239000012453 solvate Substances 0.000 claims 7
- 239000003814 drug Substances 0.000 claims 6
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 4
- 125000003118 aryl group Chemical group 0.000 claims 3
- 201000011510 cancer Diseases 0.000 claims 3
- 125000001072 heteroaryl group Chemical group 0.000 claims 3
- 239000002207 metabolite Substances 0.000 claims 3
- 238000000034 method Methods 0.000 claims 3
- 229910052760 oxygen Inorganic materials 0.000 claims 3
- VIESAWGOYVNHLV-UHFFFAOYSA-N 1,3-dihydropyrrol-2-one Chemical class O=C1CC=CN1 VIESAWGOYVNHLV-UHFFFAOYSA-N 0.000 claims 2
- DTQVDTLACAAQTR-UHFFFAOYSA-N Trifluoroacetic acid Chemical compound OC(=O)C(F)(F)F DTQVDTLACAAQTR-UHFFFAOYSA-N 0.000 claims 2
- 239000002253 acid Substances 0.000 claims 2
- 230000033228 biological regulation Effects 0.000 claims 2
- 125000000753 cycloalkyl group Chemical group 0.000 claims 2
- 229910052736 halogen Inorganic materials 0.000 claims 2
- 150000002367 halogens Chemical class 0.000 claims 2
- 229910052757 nitrogen Inorganic materials 0.000 claims 2
- XDRYMKDFEDOLFX-UHFFFAOYSA-N pentamidine Chemical compound C1=CC(C(=N)N)=CC=C1OCCCCCOC1=CC=C(C(N)=N)C=C1 XDRYMKDFEDOLFX-UHFFFAOYSA-N 0.000 claims 2
- 229960004448 pentamidine Drugs 0.000 claims 2
- 210000002784 stomach Anatomy 0.000 claims 2
- BYEAHWXPCBROCE-UHFFFAOYSA-N 1,1,1,3,3,3-hexafluoropropan-2-ol Chemical compound FC(F)(F)C(O)C(F)(F)F BYEAHWXPCBROCE-UHFFFAOYSA-N 0.000 claims 1
- HBAQYPYDRFILMT-UHFFFAOYSA-N 8-[3-(1-cyclopropylpyrazol-4-yl)-1H-pyrazolo[4,3-d]pyrimidin-5-yl]-3-methyl-3,8-diazabicyclo[3.2.1]octan-2-one Chemical class C1(CC1)N1N=CC(=C1)C1=NNC2=C1N=C(N=C2)N1C2C(N(CC1CC2)C)=O HBAQYPYDRFILMT-UHFFFAOYSA-N 0.000 claims 1
- 208000024893 Acute lymphoblastic leukemia Diseases 0.000 claims 1
- 208000014697 Acute lymphocytic leukaemia Diseases 0.000 claims 1
- 206010000871 Acute monocytic leukaemia Diseases 0.000 claims 1
- 208000010507 Adenocarcinoma of Lung Diseases 0.000 claims 1
- 208000010839 B-cell chronic lymphocytic leukemia Diseases 0.000 claims 1
- 206010006187 Breast cancer Diseases 0.000 claims 1
- 208000026310 Breast neoplasm Diseases 0.000 claims 1
- 206010009944 Colon cancer Diseases 0.000 claims 1
- 206010061968 Gastric neoplasm Diseases 0.000 claims 1
- 229940121710 HMGCoA reductase inhibitor Drugs 0.000 claims 1
- 206010024305 Leukaemia monocytic Diseases 0.000 claims 1
- 239000002841 Lewis acid Substances 0.000 claims 1
- 208000031422 Lymphocytic Chronic B-Cell Leukemia Diseases 0.000 claims 1
- 208000035489 Monocytic Acute Leukemia Diseases 0.000 claims 1
- 102000007399 Nuclear hormone receptor Human genes 0.000 claims 1
- 108020005497 Nuclear hormone receptor Proteins 0.000 claims 1
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims 1
- 208000006664 Precursor Cell Lymphoblastic Leukemia-Lymphoma Diseases 0.000 claims 1
- 206010041067 Small cell lung cancer Diseases 0.000 claims 1
- 239000002671 adjuvant Substances 0.000 claims 1
- 125000000217 alkyl group Chemical group 0.000 claims 1
- 239000004037 angiogenesis inhibitor Substances 0.000 claims 1
- 229940121369 angiogenesis inhibitor Drugs 0.000 claims 1
- 230000001028 anti-proliverative effect Effects 0.000 claims 1
- JHXKRIRFYBPWGE-UHFFFAOYSA-K bismuth chloride Chemical compound Cl[Bi](Cl)Cl JHXKRIRFYBPWGE-UHFFFAOYSA-K 0.000 claims 1
- 239000008280 blood Substances 0.000 claims 1
- 210000004369 blood Anatomy 0.000 claims 1
- 210000004556 brain Anatomy 0.000 claims 1
- 210000000481 breast Anatomy 0.000 claims 1
- 229910052794 bromium Inorganic materials 0.000 claims 1
- XMPZTFVPEKAKFH-UHFFFAOYSA-P ceric ammonium nitrate Chemical compound [NH4+].[NH4+].[Ce+4].[O-][N+]([O-])=O.[O-][N+]([O-])=O.[O-][N+]([O-])=O.[O-][N+]([O-])=O.[O-][N+]([O-])=O.[O-][N+]([O-])=O XMPZTFVPEKAKFH-UHFFFAOYSA-P 0.000 claims 1
- 210000003679 cervix uteri Anatomy 0.000 claims 1
- 239000003795 chemical substances by application Substances 0.000 claims 1
- 229910052801 chlorine Inorganic materials 0.000 claims 1
- 208000032852 chronic lymphocytic leukemia Diseases 0.000 claims 1
- 201000006778 chronic monocytic leukemia Diseases 0.000 claims 1
- 201000010902 chronic myelomonocytic leukemia Diseases 0.000 claims 1
- 208000029742 colonic neoplasm Diseases 0.000 claims 1
- 239000002254 cytotoxic agent Substances 0.000 claims 1
- 229940127089 cytotoxic agent Drugs 0.000 claims 1
- 231100000599 cytotoxic agent Toxicity 0.000 claims 1
- 201000010099 disease Diseases 0.000 claims 1
- 210000000981 epithelium Anatomy 0.000 claims 1
- 210000003238 esophagus Anatomy 0.000 claims 1
- 239000002834 estrogen receptor modulator Substances 0.000 claims 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 1
- 229910052731 fluorine Inorganic materials 0.000 claims 1
- 125000002541 furyl group Chemical group 0.000 claims 1
- 208000005017 glioblastoma Diseases 0.000 claims 1
- 210000003128 head Anatomy 0.000 claims 1
- 239000004030 hiv protease inhibitor Substances 0.000 claims 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 1
- 239000002471 hydroxymethylglutaryl coenzyme A reductase inhibitor Substances 0.000 claims 1
- 230000003463 hyperproliferative effect Effects 0.000 claims 1
- 210000000987 immune system Anatomy 0.000 claims 1
- 230000005764 inhibitory process Effects 0.000 claims 1
- 210000000936 intestine Anatomy 0.000 claims 1
- 229910052740 iodine Inorganic materials 0.000 claims 1
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 1
- 210000003734 kidney Anatomy 0.000 claims 1
- 206010023841 laryngeal neoplasm Diseases 0.000 claims 1
- 210000000867 larynx Anatomy 0.000 claims 1
- 150000007517 lewis acids Chemical class 0.000 claims 1
- 210000004185 liver Anatomy 0.000 claims 1
- 201000005249 lung adenocarcinoma Diseases 0.000 claims 1
- 208000037841 lung tumor Diseases 0.000 claims 1
- 210000004324 lymphatic system Anatomy 0.000 claims 1
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 1
- 230000000394 mitotic effect Effects 0.000 claims 1
- 201000006894 monocytic leukemia Diseases 0.000 claims 1
- 208000025113 myeloid leukemia Diseases 0.000 claims 1
- 210000003739 neck Anatomy 0.000 claims 1
- 201000002528 pancreatic cancer Diseases 0.000 claims 1
- 208000008443 pancreatic carcinoma Diseases 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 1
- 229940096701 plain lipid modifying drug hmg coa reductase inhibitors Drugs 0.000 claims 1
- 230000002265 prevention Effects 0.000 claims 1
- 210000002307 prostate Anatomy 0.000 claims 1
- 125000004076 pyridyl group Chemical group 0.000 claims 1
- 125000000714 pyrimidinyl group Chemical group 0.000 claims 1
- 238000001959 radiotherapy Methods 0.000 claims 1
- 102000027483 retinoid hormone receptors Human genes 0.000 claims 1
- 108091008679 retinoid hormone receptors Proteins 0.000 claims 1
- 239000003419 rna directed dna polymerase inhibitor Substances 0.000 claims 1
- HZXJVDYQRYYYOR-UHFFFAOYSA-K scandium(iii) trifluoromethanesulfonate Chemical compound [Sc+3].[O-]S(=O)(=O)C(F)(F)F.[O-]S(=O)(=O)C(F)(F)F.[O-]S(=O)(=O)C(F)(F)F HZXJVDYQRYYYOR-UHFFFAOYSA-K 0.000 claims 1
- 125000002914 sec-butyl group Chemical group [H]C([H])([H])C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 1
- 239000000849 selective androgen receptor modulator Substances 0.000 claims 1
- 208000000587 small cell lung carcinoma Diseases 0.000 claims 1
- 229910052717 sulfur Inorganic materials 0.000 claims 1
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 claims 1
- 125000001544 thienyl group Chemical group 0.000 claims 1
- 210000001685 thyroid gland Anatomy 0.000 claims 1
- 239000003558 transferase inhibitor Substances 0.000 claims 1
- AHZJKOKFZJYCLG-UHFFFAOYSA-K trifluoromethanesulfonate;ytterbium(3+) Chemical compound [Yb+3].[O-]S(=O)(=O)C(F)(F)F.[O-]S(=O)(=O)C(F)(F)F.[O-]S(=O)(=O)C(F)(F)F AHZJKOKFZJYCLG-UHFFFAOYSA-K 0.000 claims 1
- 210000003932 urinary bladder Anatomy 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| DE102005027170.7 | 2005-06-13 | ||
| DE102005027170A DE102005027170A1 (de) | 2005-06-13 | 2005-06-13 | Substituierte Tetrahydrochinoline |
| PCT/EP2006/004656 WO2007054138A1 (de) | 2005-06-13 | 2006-05-17 | Substituierte tetrahydrochinoline |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2008545803A JP2008545803A (ja) | 2008-12-18 |
| JP2008545803A5 true JP2008545803A5 (enExample) | 2009-07-09 |
| JP5180070B2 JP5180070B2 (ja) | 2013-04-10 |
Family
ID=36699028
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2008516155A Expired - Fee Related JP5180070B2 (ja) | 2005-06-13 | 2006-05-17 | 置換テトラヒドロキノリン |
Country Status (15)
| Country | Link |
|---|---|
| US (1) | US7893082B2 (enExample) |
| EP (1) | EP1891076B1 (enExample) |
| JP (1) | JP5180070B2 (enExample) |
| KR (1) | KR20080030015A (enExample) |
| CN (2) | CN102010416A (enExample) |
| AR (1) | AR054616A1 (enExample) |
| AU (1) | AU2006312800B2 (enExample) |
| BR (1) | BRPI0611613A2 (enExample) |
| CA (1) | CA2611889C (enExample) |
| DE (1) | DE102005027170A1 (enExample) |
| ES (1) | ES2566729T3 (enExample) |
| MX (1) | MX2007015782A (enExample) |
| RU (1) | RU2007147925A (enExample) |
| WO (1) | WO2007054138A1 (enExample) |
| ZA (1) | ZA200800365B (enExample) |
Families Citing this family (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE102005027168A1 (de) * | 2005-06-13 | 2006-12-14 | Merck Patent Gmbh | Tetrahydrochinoline |
| DE102005027169A1 (de) * | 2005-06-13 | 2006-12-14 | Merck Patent Gmbh | Tetrahydrochinolinderivate |
| DE102007013855A1 (de) * | 2007-03-20 | 2008-09-25 | Merck Patent Gmbh | Substituierte Tetrahydrochinoline |
| WO2009052288A1 (en) | 2007-10-19 | 2009-04-23 | Schering Corporation | Spiro-condensed 1, 3, 4-thiadiazole derivatives for inhibiting ksp kinesin activity |
| US8278454B2 (en) * | 2007-12-18 | 2012-10-02 | MERCK Patent Gesellschaft mit beschränkter Haftung | Process for preparing tetrahydroquinoline derivatives |
| US12275729B2 (en) | 2017-11-01 | 2025-04-15 | Merck Sharp & Dohme Llc | Substituted tetrahydroquinolin compounds as indoleamine 2,3-dioxygenase (IDO) inhibitors |
| EP4269392A4 (en) | 2020-12-25 | 2025-01-29 | Toray Industries, Inc. | TETRAHYDROQUINOLINE DERIVATIVE AND MEDICAL USE THEREOF |
| EP4545079A4 (en) | 2022-06-24 | 2026-06-03 | Toray Industries | THERAPEUTIC OR PROPHYLACTIC AGENT FOR AMYOTROPHIC LATERAL SCLEROSIS |
Family Cites Families (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO1998027093A1 (en) * | 1996-12-18 | 1998-06-25 | Eli Lilly And Company | Combinatorial process for preparing hydrofuroquinoline libraries |
| US6288075B1 (en) * | 1998-02-26 | 2001-09-11 | Rhone-Poulenc Rorer S.A. | Thiazolo[5,4,3-ij]quinolines, preparation and medicines containing the same |
| US7250423B2 (en) | 2001-09-24 | 2007-07-31 | Chao-Jun Li | Methods for synthesizing heterocycles and therapeutic use of the heterocycles for cancers |
| WO2005016255A2 (en) | 2003-07-16 | 2005-02-24 | Ligand Pharmaceuticals Incorporated | Substituted tetrahydroquinolines, phenylacetic acids and benzoic acids as hepatocyte nuclear factor 4 (hnf-4 ) modulator compounds |
| DK1761515T3 (da) * | 2003-12-20 | 2009-02-16 | Merck Patent Gmbh | 2-(hetero-)aryl-substituerede tetrahydroquinolinderivater |
| SE0400285D0 (sv) * | 2004-02-10 | 2004-02-10 | Astrazeneca Ab | Pyrroloquinoline and piperidoquinoline derivatives, preparation thereof, compositions containing them and uses thereof |
| RU2384571C2 (ru) * | 2004-04-28 | 2010-03-20 | Такеда Фармасьютикал Компани Лимитед | Конденсированное хинолиновое производное и его применение |
| DE102005027168A1 (de) * | 2005-06-13 | 2006-12-14 | Merck Patent Gmbh | Tetrahydrochinoline |
| DE102005027169A1 (de) * | 2005-06-13 | 2006-12-14 | Merck Patent Gmbh | Tetrahydrochinolinderivate |
| KR20090020702A (ko) * | 2006-06-19 | 2009-02-26 | 메르크 파텐트 게엠베하 | 다형체 및 방법 |
-
2005
- 2005-06-13 DE DE102005027170A patent/DE102005027170A1/de not_active Withdrawn
-
2006
- 2006-05-17 MX MX2007015782A patent/MX2007015782A/es active IP Right Grant
- 2006-05-17 EP EP06840909.3A patent/EP1891076B1/de not_active Expired - Lifetime
- 2006-05-17 US US11/916,952 patent/US7893082B2/en not_active Expired - Fee Related
- 2006-05-17 CN CN2010105171785A patent/CN102010416A/zh active Pending
- 2006-05-17 AU AU2006312800A patent/AU2006312800B2/en not_active Ceased
- 2006-05-17 KR KR1020087000901A patent/KR20080030015A/ko not_active Ceased
- 2006-05-17 CA CA2611889A patent/CA2611889C/en not_active Expired - Fee Related
- 2006-05-17 RU RU2007147925/04A patent/RU2007147925A/ru not_active Application Discontinuation
- 2006-05-17 WO PCT/EP2006/004656 patent/WO2007054138A1/de not_active Ceased
- 2006-05-17 JP JP2008516155A patent/JP5180070B2/ja not_active Expired - Fee Related
- 2006-05-17 BR BRPI0611613-2A patent/BRPI0611613A2/pt not_active IP Right Cessation
- 2006-05-17 CN CNA200680021167XA patent/CN101198613A/zh active Pending
- 2006-05-17 ES ES06840909.3T patent/ES2566729T3/es not_active Expired - Lifetime
- 2006-06-09 AR ARP060102412A patent/AR054616A1/es not_active Application Discontinuation
-
2008
- 2008-01-11 ZA ZA200800365A patent/ZA200800365B/xx unknown
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| KR101937501B1 (ko) | 치환된 2,3-디히드로이미다조[1,2-ｃ]퀴나졸린 염 | |
| JP2007515419A5 (enExample) | ||
| CN103172648B (zh) | 三杂环衍生物、制备方法及应用 | |
| US20110190312A1 (en) | Combinations Comprising Epothilones and Protein Tyrosine Kinase Inhibitors and Pharmaceutical Uses Thereof | |
| CN117064897A (zh) | 用于治疗血液病的化合物和组合物 | |
| CA2550350A1 (en) | 2-(hetero)aryl-substituted tetrahydroquinoline derivatives | |
| KR20170131650A (ko) | 글루타미나제 억제제의 투여 방법 | |
| TW202116356A (zh) | 作為治療劑之微管靶向藥劑之肽結合物 | |
| US9738613B2 (en) | Substituted 1,2,3-triazoles as antitumor agents | |
| JP2017137323A (ja) | 新規抗がん剤 | |
| RU2007106933A (ru) | Ингибиторы hsp90 | |
| US10351586B2 (en) | Cytidine derivative dimers and applications thereof | |
| TW202330015A (zh) | 作為治療劑之肽微管蛋白抑制劑之肽結合物 | |
| US20190330142A1 (en) | Inhibitors of mtor-deptor interactions and methods of use thereof | |
| KR102410362B1 (ko) | 증식성 질환을 위한 조합 치료 | |
| RU2007147925A (ru) | Замещенные тетрагидрохинолины | |
| JP2008179567A (ja) | ピラジン誘導体を有効成分とする抗がん剤 | |
| US11370766B2 (en) | Sulfonyl amidine as indoleamine-2,3-dioxygenase inhibitor, and preparation method therefor and use thereof | |
| JP2023507799A (ja) | 組み合わせ | |
| RU2007103300A (ru) | Тетрагидрохинолины | |
| CA3102434C (en) | Selective a2a receptor antagonist | |
| JP2003535891A (ja) | 置換アクリロイルジスタマイシン誘導体及びアルキル化剤を含む腫瘍に対する併用療法 | |
| RU2375354C2 (ru) | Производные 2-(гетеро)арил-замещенных тетрагидрохинолинов | |
| US10975079B2 (en) | 4-amino-3-phenylamino-6-phenylpyrazolo[3,4-d]pyrimidine derivatives for use as BCRP inhibitors in therapeutic treatments | |
| CN107868081B (zh) | 喹啉衍生物及其制备方法和用途 |