JP2010508337A5 - - Google Patents
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- Publication number
- JP2010508337A5 JP2010508337A5 JP2009535117A JP2009535117A JP2010508337A5 JP 2010508337 A5 JP2010508337 A5 JP 2010508337A5 JP 2009535117 A JP2009535117 A JP 2009535117A JP 2009535117 A JP2009535117 A JP 2009535117A JP 2010508337 A5 JP2010508337 A5 JP 2010508337A5
- Authority
- JP
- Japan
- Prior art keywords
- optionally substituted
- alkyl
- hydrogen
- group
- cyclopentyl
- 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- Withdrawn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 description 17
- 239000001257 hydrogen Substances 0.000 claims description 17
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 14
- 125000006413 ring segment Chemical group 0.000 claims description 7
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims description 4
- 125000003118 aryl group Chemical group 0.000 claims description 3
- 125000001072 heteroaryl group Chemical group 0.000 claims description 3
- GVNVAWHJIKLAGL-UHFFFAOYSA-N 2-(cyclohexen-1-yl)cyclohexan-1-one Chemical compound O=C1CCCCC1C1=CCCCC1 GVNVAWHJIKLAGL-UHFFFAOYSA-N 0.000 claims description 2
- 101150065749 Churc1 gene Proteins 0.000 claims description 2
- 102100038239 Protein Churchill Human genes 0.000 claims description 2
- 150000001875 compounds Chemical class 0.000 claims 12
- 125000001511 cyclopentyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 10
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 claims 7
- 125000001951 carbamoylamino group Chemical group C(N)(=O)N* 0.000 claims 5
- -1 chloro, methyl Chemical group 0.000 claims 5
- 239000000203 mixture Substances 0.000 claims 4
- PXBRQCKWGAHEHS-UHFFFAOYSA-N dichlorodifluoromethane Chemical class FC(F)(Cl)Cl PXBRQCKWGAHEHS-UHFFFAOYSA-N 0.000 claims 3
- 125000004185 ester group Chemical group 0.000 claims 3
- 150000002431 hydrogen Chemical class 0.000 claims 3
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 3
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims 2
- RTZKZFJDLAIYFH-UHFFFAOYSA-N Diethyl ether Chemical compound CCOCC RTZKZFJDLAIYFH-UHFFFAOYSA-N 0.000 claims 2
- 150000001204 N-oxides Chemical class 0.000 claims 2
- 125000002527 bicyclic carbocyclic group Chemical group 0.000 claims 2
- 229910052799 carbon Inorganic materials 0.000 claims 2
- 125000002843 carboxylic acid group Chemical group 0.000 claims 2
- 125000000753 cycloalkyl group Chemical group 0.000 claims 2
- 125000000623 heterocyclic group Chemical group 0.000 claims 2
- 125000002950 monocyclic group Chemical group 0.000 claims 2
- 150000003839 salts Chemical class 0.000 claims 2
- 239000012453 solvate Substances 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
- 125000003161 (C1-C6) alkylene 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
- 125000003903 2-propenyl group Chemical group [H]C([*])([H])C([H])=C([H])[H] 0.000 claims 1
- 208000006545 Chronic Obstructive Pulmonary Disease Diseases 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
- 206010015150 Erythema Diseases 0.000 claims 1
- 108090000371 Esterases Proteins 0.000 claims 1
- 208000022559 Inflammatory bowel disease Diseases 0.000 claims 1
- 206010028980 Neoplasm Diseases 0.000 claims 1
- 201000004681 Psoriasis 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
- 239000004480 active ingredient Substances 0.000 claims 1
- 208000006673 asthma Diseases 0.000 claims 1
- 201000008937 atopic dermatitis Diseases 0.000 claims 1
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims 1
- 125000002619 bicyclic group Chemical group 0.000 claims 1
- 125000002618 bicyclic heterocycle group Chemical group 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 1
- 230000010261 cell growth Effects 0.000 claims 1
- 125000004122 cyclic group Chemical group 0.000 claims 1
- 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 1
- WFFUJCYLHAFDIN-QGZVFWFLSA-N cyclopentyl (2r)-2-amino-5-[4-[4-carbamoyl-5-(carbamoylamino)thiophen-2-yl]phenyl]pentanoate Chemical compound C([C@@H](N)C(=O)OC1CCCC1)CCC(C=C1)=CC=C1C1=CC(C(N)=O)=C(NC(N)=O)S1 WFFUJCYLHAFDIN-QGZVFWFLSA-N 0.000 claims 1
- 206010012601 diabetes mellitus Diseases 0.000 claims 1
- 201000010099 disease Diseases 0.000 claims 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 231100000321 erythema Toxicity 0.000 claims 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 1
- 125000001153 fluoro group Chemical group F* 0.000 claims 1
- 206010073071 hepatocellular carcinoma Diseases 0.000 claims 1
- 231100000844 hepatocellular carcinoma Toxicity 0.000 claims 1
- 208000026278 immune system disease Diseases 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
- 230000003834 intracellular effect Effects 0.000 claims 1
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 1
- 206010025135 lupus erythematosus Diseases 0.000 claims 1
- 201000001441 melanoma Diseases 0.000 claims 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 1
- 125000001620 monocyclic carbocycle group Chemical group 0.000 claims 1
- 125000002911 monocyclic heterocycle group Chemical group 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
- 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
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 1
- 230000002062 proliferating effect Effects 0.000 claims 1
- 206010039073 rheumatoid arthritis Diseases 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
- 125000001424 substituent group Chemical group 0.000 claims 1
- 230000009885 systemic effect Effects 0.000 claims 1
- 230000001225 therapeutic effect Effects 0.000 claims 1
- 150000003568 thioethers Chemical class 0.000 claims 1
- 238000002054 transplantation Methods 0.000 claims 1
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GB0621720A GB0621720D0 (en) | 2006-11-01 | 2006-11-01 | Inhibitors of ikk- serine-threonine protein kinase |
| GB0715469A GB0715469D0 (en) | 2007-08-09 | 2007-08-09 | Inhibitors of IKK serine-threonine protein kinase |
| PCT/GB2007/004117 WO2008053185A1 (en) | 2006-11-01 | 2007-10-29 | INHIBITORS OF IKK-β SERINE-THREONINE PROTEIN KINASE |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2010508337A JP2010508337A (ja) | 2010-03-18 |
| JP2010508337A5 true JP2010508337A5 (https=) | 2010-12-16 |
Family
ID=39012039
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2009535117A Withdrawn JP2010508337A (ja) | 2006-11-01 | 2007-10-29 | 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 |
Country Status (5)
| Country | Link |
|---|---|
| US (1) | US8106091B2 (https=) |
| EP (1) | EP2086956B1 (https=) |
| JP (1) | JP2010508337A (https=) |
| AT (1) | ATE524454T1 (https=) |
| WO (1) | WO2008053185A1 (https=) |
Families Citing this family (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB0619753D0 (en) | 2006-10-06 | 2006-11-15 | Chroma Therapeutics Ltd | Enzyme inhibitors |
| GB0803747D0 (en) | 2008-02-29 | 2008-04-09 | Martin | Enzyme and receptor modulation |
| CN102036979A (zh) * | 2008-04-23 | 2011-04-27 | 色品疗法有限公司 | IKK-β丝氨酸苏氨酸蛋白激酶抑制剂 |
| JP2011518817A (ja) * | 2008-04-26 | 2011-06-30 | クロマ セラピューティクス リミテッド | 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 |
| WO2010062829A1 (en) * | 2008-11-28 | 2010-06-03 | Lexicon Pharmaceuticals, Inc. | Tryptophan hydroxylase inhibitors for treating osteoporosis |
| GB0903480D0 (en) | 2009-02-27 | 2009-04-08 | Chroma Therapeutics Ltd | Enzyme Inhibitors |
| GB201211310D0 (en) | 2012-06-26 | 2012-08-08 | Chroma Therapeutics Ltd | CSF-1R kinase inhibitors |
| AR091858A1 (es) * | 2012-07-25 | 2015-03-04 | Sova Pharmaceuticals Inc | INHIBIDORES DE CISTATIONIN-g-LIASA (CSE) |
| HUE046132T2 (hu) | 2012-10-17 | 2020-02-28 | Macrophage Pharma Ltd | N-[2-{4-[6-amino-5-(2,4-difluor-benzoil)-2-oxopiridin-1(2H)-il]-3,5-difluor-fenil}etil]-l-alanin és annak tercbutil-észtere |
| CN107098924A (zh) * | 2017-05-19 | 2017-08-29 | 暨南大学 | 一种芳基硼酸酯修饰的氨基酸衍生物及其制备方法与应用 |
| GB201713975D0 (en) | 2017-08-31 | 2017-10-18 | Macrophage Pharma Ltd | Medical use |
Family Cites Families (2)
| 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 |
-
2007
- 2007-10-29 AT AT07824361T patent/ATE524454T1/de not_active IP Right Cessation
- 2007-10-29 EP EP07824361A patent/EP2086956B1/en not_active Not-in-force
- 2007-10-29 JP JP2009535117A patent/JP2010508337A/ja not_active Withdrawn
- 2007-10-29 WO PCT/GB2007/004117 patent/WO2008053185A1/en not_active Ceased
- 2007-10-29 US US12/447,271 patent/US8106091B2/en not_active Expired - Fee Related
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