JP2008545803A5 - - Google Patents
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- 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 |
|---|---|---|---|
| DE102005027170A DE102005027170A1 (de) | 2005-06-13 | 2005-06-13 | Substituierte Tetrahydrochinoline |
| DE102005027170.7 | 2005-06-13 | ||
| 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 (https=) | 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 (https=) |
| EP (1) | EP1891076B1 (https=) |
| JP (1) | JP5180070B2 (https=) |
| KR (1) | KR20080030015A (https=) |
| CN (2) | CN102010416A (https=) |
| AR (1) | AR054616A1 (https=) |
| AU (1) | AU2006312800B2 (https=) |
| BR (1) | BRPI0611613A2 (https=) |
| CA (1) | CA2611889C (https=) |
| DE (1) | DE102005027170A1 (https=) |
| ES (1) | ES2566729T3 (https=) |
| MX (1) | MX2007015782A (https=) |
| RU (1) | RU2007147925A (https=) |
| WO (1) | WO2007054138A1 (https=) |
| ZA (1) | ZA200800365B (https=) |
Families Citing this family (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE102005027169A1 (de) * | 2005-06-13 | 2006-12-14 | Merck Patent Gmbh | Tetrahydrochinolinderivate |
| DE102005027168A1 (de) * | 2005-06-13 | 2006-12-14 | Merck Patent Gmbh | Tetrahydrochinoline |
| DE102007013855A1 (de) * | 2007-03-20 | 2008-09-25 | Merck Patent Gmbh | Substituierte Tetrahydrochinoline |
| AR068888A1 (es) | 2007-10-19 | 2009-12-16 | Schering Corp | Derivados de 1, 3, 4 - tiadiazol, una composicion farmaceutica que los comprende y su uso en la preparacion de medicamentos para el tratamiento de enfermedades mediadas por la inhibicion de la quinesina ksp. |
| CA2709571C (en) * | 2007-12-18 | 2014-03-11 | Merck Patent Gmbh | Process for preparing tetrahydroquinoline derivatives |
| EP3703692B1 (en) * | 2017-11-01 | 2025-07-23 | Merck Sharp & Dohme LLC | Novel substituted tetrahydroquinolin compounds as indoleamine 2,3-dioxygenase (ido) inhibitors |
| IL303307A (en) | 2020-12-25 | 2023-07-01 | Toray Industries | Tetrahydroquinoline derivative and its medical use |
| JPWO2023249106A1 (https=) | 2022-06-24 | 2023-12-28 |
Family Cites Families (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2001508050A (ja) * | 1996-12-18 | 2001-06-19 | イーライ・リリー・アンド・カンパニー | ヒドロフロキノリンライブラリーを作製するためのコンビネーション法 |
| 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 |
| ATE507220T1 (de) * | 2003-12-20 | 2011-05-15 | Merck Patent Gmbh | Tetrahydropyranochinolinderivate |
| SE0400285D0 (sv) * | 2004-02-10 | 2004-02-10 | Astrazeneca Ab | Pyrroloquinoline and piperidoquinoline derivatives, preparation thereof, compositions containing them and uses thereof |
| JP4361566B2 (ja) * | 2004-04-28 | 2009-11-11 | 武田薬品工業株式会社 | 縮合キノリン誘導体およびその使用 |
| DE102005027169A1 (de) * | 2005-06-13 | 2006-12-14 | Merck Patent Gmbh | Tetrahydrochinolinderivate |
| DE102005027168A1 (de) * | 2005-06-13 | 2006-12-14 | Merck Patent Gmbh | Tetrahydrochinoline |
| ES2537759T3 (es) * | 2006-06-19 | 2015-06-11 | Merck Patent Gmbh | Compuestos enriquecidos enantioméricamente y proceso |
-
2005
- 2005-06-13 DE DE102005027170A patent/DE102005027170A1/de not_active Withdrawn
-
2006
- 2006-05-17 CA CA2611889A patent/CA2611889C/en not_active Expired - Fee Related
- 2006-05-17 JP JP2008516155A patent/JP5180070B2/ja not_active Expired - Fee Related
- 2006-05-17 CN CN2010105171785A patent/CN102010416A/zh active Pending
- 2006-05-17 KR KR1020087000901A patent/KR20080030015A/ko not_active Ceased
- 2006-05-17 US US11/916,952 patent/US7893082B2/en not_active Expired - Fee Related
- 2006-05-17 CN CNA200680021167XA patent/CN101198613A/zh active Pending
- 2006-05-17 BR BRPI0611613-2A patent/BRPI0611613A2/pt not_active IP Right Cessation
- 2006-05-17 WO PCT/EP2006/004656 patent/WO2007054138A1/de not_active Ceased
- 2006-05-17 ES ES06840909.3T patent/ES2566729T3/es active Active
- 2006-05-17 RU RU2007147925/04A patent/RU2007147925A/ru not_active Application Discontinuation
- 2006-05-17 AU AU2006312800A patent/AU2006312800B2/en not_active Ceased
- 2006-05-17 EP EP06840909.3A patent/EP1891076B1/de not_active Not-in-force
- 2006-05-17 MX MX2007015782A patent/MX2007015782A/es active IP Right Grant
- 2006-06-09 AR ARP060102412A patent/AR054616A1/es not_active Application Discontinuation
-
2008
- 2008-01-11 ZA ZA200800365A patent/ZA200800365B/xx unknown
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