JP2011518817A5 - - Google Patents
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- Publication number
- JP2011518817A5 JP2011518817A5 JP2011505589A JP2011505589A JP2011518817A5 JP 2011518817 A5 JP2011518817 A5 JP 2011518817A5 JP 2011505589 A JP2011505589 A JP 2011505589A JP 2011505589 A JP2011505589 A JP 2011505589A JP 2011518817 A5 JP2011518817 A5 JP 2011518817A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- hydrogen
- optionally substituted
- group
- compound according
- 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.)
- Withdrawn
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- 229910052739 hydrogen Inorganic materials 0.000 claims 20
- 239000001257 hydrogen Substances 0.000 claims 20
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 17
- 150000001875 compounds Chemical class 0.000 claims 15
- 125000000217 alkyl group Chemical group 0.000 claims 10
- 125000000753 cycloalkyl group Chemical group 0.000 claims 9
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 8
- 125000000623 heterocyclic group Chemical group 0.000 claims 8
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 8
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 claims 6
- 229910052799 carbon Inorganic materials 0.000 claims 6
- 239000000203 mixture Substances 0.000 claims 6
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 5
- 150000001721 carbon Chemical group 0.000 claims 5
- RTZKZFJDLAIYFH-UHFFFAOYSA-N Diethyl ether Chemical compound CCOCC RTZKZFJDLAIYFH-UHFFFAOYSA-N 0.000 claims 4
- 125000002619 bicyclic group Chemical group 0.000 claims 4
- 125000001072 heteroaryl group Chemical group 0.000 claims 4
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 4
- 125000006413 ring segment Chemical group 0.000 claims 4
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims 3
- 125000003342 alkenyl group Chemical group 0.000 claims 3
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims 3
- 125000002837 carbocyclic group Chemical group 0.000 claims 3
- 125000004122 cyclic group Chemical group 0.000 claims 3
- 125000001511 cyclopentyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 3
- 125000002950 monocyclic group Chemical group 0.000 claims 3
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 3
- -1 tetrahydrofuran-3-yl Chemical group 0.000 claims 3
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims 2
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical compound FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 claims 2
- 125000002843 carboxylic acid group Chemical group 0.000 claims 2
- 125000004093 cyano group Chemical group *C#N 0.000 claims 2
- 125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 claims 2
- 230000000694 effects Effects 0.000 claims 2
- 125000004185 ester group Chemical group 0.000 claims 2
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 2
- 229910052731 fluorine Inorganic materials 0.000 claims 2
- 239000011737 fluorine Substances 0.000 claims 2
- 229910052736 halogen Inorganic materials 0.000 claims 2
- 150000002367 halogens Chemical class 0.000 claims 2
- 150000002431 hydrogen Chemical class 0.000 claims 2
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 2
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 2
- 238000004519 manufacturing process Methods 0.000 claims 2
- 125000005010 perfluoroalkyl group Chemical group 0.000 claims 2
- 150000003839 salts Chemical class 0.000 claims 2
- 125000002914 sec-butyl group Chemical group [H]C([H])([H])C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 2
- 125000001424 substituent group Chemical group 0.000 claims 2
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 claims 2
- 150000003568 thioethers Chemical class 0.000 claims 2
- 125000003161 (C1-C6) alkylene group Chemical group 0.000 claims 1
- 125000006591 (C2-C6) alkynylene group Chemical group 0.000 claims 1
- 125000006554 (C4-C8) cycloalkenyl group Chemical group 0.000 claims 1
- 125000001989 1,3-phenylene group Chemical group [H]C1=C([H])C([*:1])=C([H])C([*:2])=C1[H] 0.000 claims 1
- 125000001140 1,4-phenylene group Chemical group [H]C1=C([H])C([*:2])=C([H])C([H])=C1[*:1] 0.000 claims 1
- GVNVAWHJIKLAGL-UHFFFAOYSA-N 2-(cyclohexen-1-yl)cyclohexan-1-one Chemical compound O=C1CCCCC1C1=CCCCC1 GVNVAWHJIKLAGL-UHFFFAOYSA-N 0.000 claims 1
- 125000003903 2-propenyl group Chemical group [H]C([*])([H])C([H])=C([H])[H] 0.000 claims 1
- 208000024827 Alzheimer disease Diseases 0.000 claims 1
- 206010073128 Anaplastic oligodendroglioma Diseases 0.000 claims 1
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical group [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims 1
- ZAMOUSCENKQFHK-UHFFFAOYSA-N Chlorine atom Chemical compound [Cl] ZAMOUSCENKQFHK-UHFFFAOYSA-N 0.000 claims 1
- 208000006545 Chronic Obstructive Pulmonary Disease Diseases 0.000 claims 1
- 101150065749 Churc1 gene Proteins 0.000 claims 1
- 206010009900 Colitis ulcerative Diseases 0.000 claims 1
- 208000011231 Crohn disease Diseases 0.000 claims 1
- 206010012438 Dermatitis atopic Diseases 0.000 claims 1
- 101100508533 Drosophila melanogaster IKKbeta gene Proteins 0.000 claims 1
- 108090000790 Enzymes Proteins 0.000 claims 1
- 102000004190 Enzymes Human genes 0.000 claims 1
- 108090000371 Esterases Proteins 0.000 claims 1
- 201000003741 Gastrointestinal carcinoma Diseases 0.000 claims 1
- 201000010915 Glioblastoma multiforme Diseases 0.000 claims 1
- 208000009329 Graft vs Host Disease Diseases 0.000 claims 1
- 208000022559 Inflammatory bowel disease Diseases 0.000 claims 1
- 208000000172 Medulloblastoma Diseases 0.000 claims 1
- 150000001204 N-oxides Chemical class 0.000 claims 1
- 201000010133 Oligodendroglioma Diseases 0.000 claims 1
- 206010033128 Ovarian cancer Diseases 0.000 claims 1
- 206010061535 Ovarian neoplasm Diseases 0.000 claims 1
- 102100038239 Protein Churchill Human genes 0.000 claims 1
- 201000004681 Psoriasis Diseases 0.000 claims 1
- 206010041848 Squamous cell carcinoma of the cervix Diseases 0.000 claims 1
- 208000034331 Squamous cell carcinoma of the stomach Diseases 0.000 claims 1
- 201000006704 Ulcerative Colitis Diseases 0.000 claims 1
- DGYIJVNZSDYBOE-UHFFFAOYSA-N [CH2]C1=CC=NC=C1 Chemical group [CH2]C1=CC=NC=C1 DGYIJVNZSDYBOE-UHFFFAOYSA-N 0.000 claims 1
- 125000005073 adamantyl group Chemical group C12(CC3CC(CC(C1)C3)C2)* 0.000 claims 1
- 125000004450 alkenylene group Chemical group 0.000 claims 1
- 125000000304 alkynyl group Chemical group 0.000 claims 1
- 150000001370 alpha-amino acid derivatives Chemical class 0.000 claims 1
- 235000008206 alpha-amino acids Nutrition 0.000 claims 1
- 208000006673 asthma Diseases 0.000 claims 1
- 125000004429 atom Chemical group 0.000 claims 1
- 201000008937 atopic dermatitis Diseases 0.000 claims 1
- 230000009702 cancer cell proliferation Effects 0.000 claims 1
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 claims 1
- 125000001951 carbamoylamino group Chemical group C(N)(=O)N* 0.000 claims 1
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 1
- 201000006612 cervical squamous cell carcinoma Diseases 0.000 claims 1
- 229910052801 chlorine Inorganic materials 0.000 claims 1
- 239000000460 chlorine Substances 0.000 claims 1
- 125000000392 cycloalkenyl group Chemical group 0.000 claims 1
- 125000001316 cycloalkyl alkyl group Chemical group 0.000 claims 1
- 125000001995 cyclobutyl group Chemical group [H]C1([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 1
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 1
- 206010012601 diabetes mellitus Diseases 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 201000000496 gastric squamous cell carcinoma Diseases 0.000 claims 1
- 208000005017 glioblastoma Diseases 0.000 claims 1
- 208000024908 graft versus host disease Diseases 0.000 claims 1
- 201000010536 head and neck cancer Diseases 0.000 claims 1
- 208000014829 head and neck neoplasm Diseases 0.000 claims 1
- 206010073071 hepatocellular carcinoma Diseases 0.000 claims 1
- 125000004446 heteroarylalkyl group Chemical group 0.000 claims 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 1
- 208000026278 immune system disease Diseases 0.000 claims 1
- 238000001727 in vivo Methods 0.000 claims 1
- 125000003392 indanyl group Chemical group C1(CCC2=CC=CC=C12)* 0.000 claims 1
- 208000027866 inflammatory disease Diseases 0.000 claims 1
- 230000002401 inhibitory effect Effects 0.000 claims 1
- 201000002313 intestinal cancer Diseases 0.000 claims 1
- 230000003834 intracellular effect Effects 0.000 claims 1
- 208000014018 liver neoplasm Diseases 0.000 claims 1
- 208000020816 lung neoplasm Diseases 0.000 claims 1
- 206010025135 lupus erythematosus Diseases 0.000 claims 1
- 201000001441 melanoma Diseases 0.000 claims 1
- 125000006203 morpholinoethyl group Chemical group [H]C([H])(*)C([H])([H])N1C([H])([H])C([H])([H])OC([H])([H])C1([H])[H] 0.000 claims 1
- 201000006417 multiple sclerosis Diseases 0.000 claims 1
- 125000004108 n-butyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])C([H])([H])* 0.000 claims 1
- 125000004123 n-propyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])* 0.000 claims 1
- 230000001613 neoplastic effect Effects 0.000 claims 1
- 229910052757 nitrogen Inorganic materials 0.000 claims 1
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 1
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims 1
- 125000002868 norbornyl group Chemical group C12(CCC(CC1)C2)* 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 125000003884 phenylalkyl group Chemical group 0.000 claims 1
- 125000004482 piperidin-4-yl group Chemical group N1CCC(CC1)* 0.000 claims 1
- 230000002062 proliferating effect Effects 0.000 claims 1
- 125000004076 pyridyl group Chemical group 0.000 claims 1
- 206010039073 rheumatoid arthritis Diseases 0.000 claims 1
- 239000012453 solvate Substances 0.000 claims 1
- 210000002784 stomach Anatomy 0.000 claims 1
- 125000003107 substituted aryl group Chemical group 0.000 claims 1
- 230000009885 systemic effect Effects 0.000 claims 1
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 1
- 208000001072 type 2 diabetes mellitus Diseases 0.000 claims 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GB0807642.4 | 2008-04-26 | ||
| GB0807642A GB0807642D0 (en) | 2008-04-26 | 2008-04-26 | IKK- serine-threonine protein kinase inhibitors |
| GB0815550.9 | 2008-08-27 | ||
| GB0815550A GB0815550D0 (en) | 2008-08-27 | 2008-08-27 | IKK-beta serine-threonine protein kinase inhibitors |
| PCT/GB2009/001051 WO2009130475A1 (en) | 2008-04-26 | 2009-04-23 | Substituted thiophenecarboxamides as ikk-beta serine-, threonine-protein kinase inhibitors |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2011518817A JP2011518817A (ja) | 2011-06-30 |
| JP2011518817A5 true JP2011518817A5 (https=) | 2012-06-07 |
Family
ID=40786701
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2011505589A Withdrawn JP2011518817A (ja) | 2008-04-26 | 2009-04-23 | ＩＫＫ−βセリン−、スレオニン−プロテインキナーゼ阻害剤としての置換されたチオフェンカルボキシアミド類 |
Country Status (13)
| Country | Link |
|---|---|
| US (1) | US20110046210A1 (https=) |
| EP (1) | EP2285797A1 (https=) |
| JP (1) | JP2011518817A (https=) |
| KR (1) | KR20110020784A (https=) |
| CN (1) | CN102036980A (https=) |
| AU (1) | AU2009239772A1 (https=) |
| BR (1) | BRPI0911480A2 (https=) |
| CA (1) | CA2722660A1 (https=) |
| EA (1) | EA201001708A1 (https=) |
| IL (1) | IL208654A0 (https=) |
| MX (1) | MX2010011643A (https=) |
| WO (1) | WO2009130475A1 (https=) |
| ZA (1) | ZA201008027B (https=) |
Families Citing this family (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2012176930A (ja) * | 2010-10-07 | 2012-09-13 | Santen Pharmaceut Co Ltd | ウレイド基とアミノカルボニル基を置換基として有するチオフェン誘導体を有効成分として含有する新規ｊａｋ３阻害剤 |
| GB201211310D0 (en) | 2012-06-26 | 2012-08-08 | Chroma Therapeutics Ltd | CSF-1R kinase inhibitors |
| PL3222616T3 (pl) | 2012-10-17 | 2019-12-31 | Macrophage Pharma Limited | N-[2-{4-[6-amino-5-(2,4-difluorobenzoilo)-2-oksopirydyn-1(2h)-ylo]-3,5-difluorofenylo}etylo)-L-alaninian tert-butylu lub jego sól, hydrat lub solwat |
| PL2953942T3 (pl) | 2013-02-06 | 2018-03-30 | Bayer Cropscience Aktiengesellschaft | Podstawione halogenem pochodne pirazolu jako środki do zwalczania szkodników |
| GB201713975D0 (en) | 2017-08-31 | 2017-10-18 | Macrophage Pharma Ltd | Medical use |
Family Cites Families (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| SE0102616D0 (sv) * | 2001-07-25 | 2001-07-25 | Astrazeneca Ab | Novel compounds |
| SE0300092D0 (sv) * | 2003-01-15 | 2003-01-15 | Astrazeneca Ab | Novel compounds |
| WO2008002246A1 (en) * | 2006-06-28 | 2008-01-03 | Astrazeneca Ab | A pharmaceutical composition comprising an ikk2 inhibitor and a second active ingrdient. |
| WO2008053182A1 (en) * | 2006-11-01 | 2008-05-08 | Chroma Therapeutics Ltd. | IKK-β SERINE-THREONINE PROTEIN KINASE INHIBITORS |
| JP2010508337A (ja) * | 2006-11-01 | 2010-03-18 | クロマ セラピューティクス リミテッド | Ｉｋｋ−ベータセリン−スレオニンプロテインキナーゼの阻害剤 |
-
2009
- 2009-04-23 MX MX2010011643A patent/MX2010011643A/es not_active Application Discontinuation
- 2009-04-23 EA EA201001708A patent/EA201001708A1/ru unknown
- 2009-04-23 EP EP09733957A patent/EP2285797A1/en not_active Withdrawn
- 2009-04-23 JP JP2011505589A patent/JP2011518817A/ja not_active Withdrawn
- 2009-04-23 AU AU2009239772A patent/AU2009239772A1/en not_active Abandoned
- 2009-04-23 KR KR1020107026507A patent/KR20110020784A/ko not_active Withdrawn
- 2009-04-23 CA CA2722660A patent/CA2722660A1/en not_active Abandoned
- 2009-04-23 US US12/989,271 patent/US20110046210A1/en not_active Abandoned
- 2009-04-23 BR BRPI0911480A patent/BRPI0911480A2/pt not_active IP Right Cessation
- 2009-04-23 CN CN2009801189111A patent/CN102036980A/zh active Pending
- 2009-04-23 WO PCT/GB2009/001051 patent/WO2009130475A1/en not_active Ceased
-
2010
- 2010-10-12 IL IL208654A patent/IL208654A0/en unknown
- 2010-11-09 ZA ZA2010/08027A patent/ZA201008027B/en unknown
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