JP2010521443A5 - - Google Patents
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- JP2010521443A5 JP2010521443A5 JP2009553202A JP2009553202A JP2010521443A5 JP 2010521443 A5 JP2010521443 A5 JP 2010521443A5 JP 2009553202 A JP2009553202 A JP 2009553202A JP 2009553202 A JP2009553202 A JP 2009553202A JP 2010521443 A5 JP2010521443 A5 JP 2010521443A5
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- JP
- Japan
- Prior art keywords
- optionally substituted
- groups
- compound
- independently
- alkyl
- 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.)
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- 125000001424 substituent group Chemical group 0.000 claims 85
- 150000001875 compounds Chemical class 0.000 claims 84
- 229910052739 hydrogen Inorganic materials 0.000 claims 63
- 239000001257 hydrogen Substances 0.000 claims 63
- 125000000217 alkyl group Chemical group 0.000 claims 53
- 229910052736 halogen Inorganic materials 0.000 claims 41
- 150000002367 halogens Chemical class 0.000 claims 39
- 125000003342 alkenyl group Chemical group 0.000 claims 34
- 125000000304 alkynyl group Chemical group 0.000 claims 32
- 150000002431 hydrogen Chemical class 0.000 claims 32
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 30
- -1 1,3-dihydroindol-2-one-yl Chemical group 0.000 claims 26
- 125000002947 alkylene group Chemical group 0.000 claims 18
- 125000000623 heterocyclic group Chemical group 0.000 claims 18
- 125000001072 heteroaryl group Chemical group 0.000 claims 17
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 16
- 230000007812 deficiency Effects 0.000 claims 13
- 150000003839 salts Chemical class 0.000 claims 13
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 12
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims 12
- 125000003118 aryl group Chemical group 0.000 claims 12
- 125000006647 (C3-C15) cycloalkyl group Chemical group 0.000 claims 10
- 125000004450 alkenylene group Chemical group 0.000 claims 10
- 125000000753 cycloalkyl group Chemical group 0.000 claims 9
- 239000002671 adjuvant Substances 0.000 claims 7
- 239000003085 diluting agent Substances 0.000 claims 7
- 125000005843 halogen group Chemical group 0.000 claims 7
- 229910052757 nitrogen Chemical group 0.000 claims 7
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 7
- 239000000546 pharmaceutical excipient Substances 0.000 claims 7
- 125000004419 alkynylene group Chemical group 0.000 claims 6
- 239000003814 drug Substances 0.000 claims 6
- 239000008194 pharmaceutical composition Substances 0.000 claims 5
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims 4
- 238000000034 method Methods 0.000 claims 4
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 4
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 claims 4
- 229940124597 therapeutic agent Drugs 0.000 claims 4
- 239000002131 composite material Substances 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
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 3
- 238000004519 manufacturing process Methods 0.000 claims 3
- 208000024891 symptom Diseases 0.000 claims 3
- 125000003161 (C1-C6) alkylene group Chemical group 0.000 claims 2
- 125000001255 4-fluorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C([H])=C1F 0.000 claims 2
- 125000004199 4-trifluoromethylphenyl group Chemical group [H]C1=C([H])C(=C([H])C([H])=C1*)C(F)(F)F 0.000 claims 2
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical group [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims 2
- 206010009900 Colitis ulcerative Diseases 0.000 claims 2
- 241000124008 Mammalia Species 0.000 claims 2
- 206010028980 Neoplasm Diseases 0.000 claims 2
- 201000004681 Psoriasis Diseases 0.000 claims 2
- 201000006704 Ulcerative Colitis Diseases 0.000 claims 2
- 229910052799 carbon Inorganic materials 0.000 claims 2
- 210000003169 central nervous system Anatomy 0.000 claims 2
- 125000001153 fluoro group Chemical group F* 0.000 claims 2
- 125000005842 heteroatom Chemical group 0.000 claims 2
- 230000002757 inflammatory effect Effects 0.000 claims 2
- 206010025135 lupus erythematosus Diseases 0.000 claims 2
- 125000000040 m-tolyl group Chemical group [H]C1=C([H])C(*)=C([H])C(=C1[H])C([H])([H])[H] 0.000 claims 2
- 201000008482 osteoarthritis Diseases 0.000 claims 2
- 230000001575 pathological effect Effects 0.000 claims 2
- 125000003367 polycyclic group Chemical group 0.000 claims 2
- 239000000651 prodrug Substances 0.000 claims 2
- 229940002612 prodrug Drugs 0.000 claims 2
- 201000003651 pulmonary sarcoidosis Diseases 0.000 claims 2
- 206010039073 rheumatoid arthritis Diseases 0.000 claims 2
- 239000012453 solvate Substances 0.000 claims 2
- LMBFAGIMSUYTBN-MPZNNTNKSA-N teixobactin Chemical compound C([C@H](C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CO)C(=O)N[C@H](CCC(N)=O)C(=O)N[C@H]([C@@H](C)CC)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CO)C(=O)N[C@H]1C(N[C@@H](C)C(=O)N[C@@H](C[C@@H]2NC(=N)NC2)C(=O)N[C@H](C(=O)O[C@H]1C)[C@@H](C)CC)=O)NC)C1=CC=CC=C1 LMBFAGIMSUYTBN-MPZNNTNKSA-N 0.000 claims 2
- 125000004182 2-chlorophenyl group Chemical group [H]C1=C([H])C(Cl)=C(*)C([H])=C1[H] 0.000 claims 1
- 125000004179 3-chlorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C(Cl)=C1[H] 0.000 claims 1
- 125000004861 4-isopropyl phenyl group Chemical group [H]C1=C([H])C(=C([H])C([H])=C1*)C([H])(C([H])([H])[H])C([H])([H])[H] 0.000 claims 1
- 125000004863 4-trifluoromethoxyphenyl group Chemical group [H]C1=C([H])C(OC(F)(F)F)=C([H])C([H])=C1* 0.000 claims 1
- 125000002373 5 membered heterocyclic group Chemical group 0.000 claims 1
- FCSKOFQQCWLGMV-UHFFFAOYSA-N 5-{5-[2-chloro-4-(4,5-dihydro-1,3-oxazol-2-yl)phenoxy]pentyl}-3-methylisoxazole Chemical compound O1N=C(C)C=C1CCCCCOC1=CC=C(C=2OCCN=2)C=C1Cl FCSKOFQQCWLGMV-UHFFFAOYSA-N 0.000 claims 1
- 125000004070 6 membered heterocyclic group Chemical group 0.000 claims 1
- 206010001052 Acute respiratory distress syndrome Diseases 0.000 claims 1
- 208000024827 Alzheimer disease Diseases 0.000 claims 1
- 206010002556 Ankylosing Spondylitis Diseases 0.000 claims 1
- WKBOTKDWSSQWDR-UHFFFAOYSA-N Bromine atom Chemical compound [Br] WKBOTKDWSSQWDR-UHFFFAOYSA-N 0.000 claims 1
- 206010006458 Bronchitis chronic Diseases 0.000 claims 1
- 208000006545 Chronic Obstructive Pulmonary Disease Diseases 0.000 claims 1
- UDMBCSSLTHHNCD-UHFFFAOYSA-N Coenzym Q(11) Natural products C1=NC=2C(N)=NC=NC=2N1C1OC(COP(O)(O)=O)C(O)C1O UDMBCSSLTHHNCD-UHFFFAOYSA-N 0.000 claims 1
- 206010010741 Conjunctivitis Diseases 0.000 claims 1
- 208000011231 Crohn disease Diseases 0.000 claims 1
- 201000004624 Dermatitis Diseases 0.000 claims 1
- 206010012438 Dermatitis atopic Diseases 0.000 claims 1
- 206010014561 Emphysema Diseases 0.000 claims 1
- 102000004190 Enzymes Human genes 0.000 claims 1
- 108090000790 Enzymes Proteins 0.000 claims 1
- 208000001640 Fibromyalgia Diseases 0.000 claims 1
- 201000005569 Gout Diseases 0.000 claims 1
- 206010061218 Inflammation Diseases 0.000 claims 1
- 208000022559 Inflammatory bowel disease Diseases 0.000 claims 1
- 208000011200 Kawasaki disease Diseases 0.000 claims 1
- 208000018737 Parkinson disease Diseases 0.000 claims 1
- 208000029082 Pelvic Inflammatory Disease Diseases 0.000 claims 1
- 201000001263 Psoriatic Arthritis Diseases 0.000 claims 1
- 208000036824 Psoriatic arthropathy Diseases 0.000 claims 1
- 206010063837 Reperfusion injury Diseases 0.000 claims 1
- 208000013616 Respiratory Distress Syndrome Diseases 0.000 claims 1
- 206010039085 Rhinitis allergic Diseases 0.000 claims 1
- 206010039710 Scleroderma Diseases 0.000 claims 1
- 208000006045 Spondylarthropathies Diseases 0.000 claims 1
- 206010052779 Transplant rejections Diseases 0.000 claims 1
- 208000024780 Urticaria Diseases 0.000 claims 1
- UDMBCSSLTHHNCD-KQYNXXCUSA-N adenosine 5'-monophosphate Chemical compound C1=NC=2C(N)=NC=NC=2N1[C@@H]1O[C@H](COP(O)(O)=O)[C@@H](O)[C@H]1O UDMBCSSLTHHNCD-KQYNXXCUSA-N 0.000 claims 1
- 229950006790 adenosine phosphate Drugs 0.000 claims 1
- 201000010105 allergic rhinitis Diseases 0.000 claims 1
- 206010003246 arthritis Diseases 0.000 claims 1
- 208000006673 asthma Diseases 0.000 claims 1
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims 1
- 201000008937 atopic dermatitis Diseases 0.000 claims 1
- 208000010668 atopic eczema Diseases 0.000 claims 1
- 125000003785 benzimidazolyl group Chemical group N1=C(NC2=C1C=CC=C2)* 0.000 claims 1
- 125000000499 benzofuranyl group Chemical group O1C(=CC2=C1C=CC=C2)* 0.000 claims 1
- 125000001164 benzothiazolyl group Chemical group S1C(=NC2=C1C=CC=C2)* 0.000 claims 1
- 125000004196 benzothienyl group Chemical group S1C(=CC2=C1C=CC=C2)* 0.000 claims 1
- 125000003354 benzotriazolyl group Chemical group N1N=NC2=C1C=CC=C2* 0.000 claims 1
- 125000004541 benzoxazolyl group Chemical group O1C(=NC2=C1C=CC=C2)* 0.000 claims 1
- 230000000903 blocking effect Effects 0.000 claims 1
- 208000025698 brain inflammatory disease Diseases 0.000 claims 1
- GDTBXPJZTBHREO-UHFFFAOYSA-N bromine Substances BrBr GDTBXPJZTBHREO-UHFFFAOYSA-N 0.000 claims 1
- 229910052794 bromium Inorganic materials 0.000 claims 1
- 206010006451 bronchitis Diseases 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- 239000000969 carrier Substances 0.000 claims 1
- 230000004663 cell proliferation Effects 0.000 claims 1
- 208000026106 cerebrovascular disease Diseases 0.000 claims 1
- 208000007451 chronic bronchitis Diseases 0.000 claims 1
- 230000003920 cognitive function Effects 0.000 claims 1
- 125000004122 cyclic group Chemical group 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
- 206010014599 encephalitis Diseases 0.000 claims 1
- 201000001564 eosinophilic gastroenteritis Diseases 0.000 claims 1
- 238000006735 epoxidation reaction Methods 0.000 claims 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 1
- 125000002541 furyl group Chemical group 0.000 claims 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 1
- 125000002883 imidazolyl group Chemical group 0.000 claims 1
- 125000005945 imidazopyridyl group Chemical group 0.000 claims 1
- 125000001041 indolyl group Chemical group 0.000 claims 1
- 230000004054 inflammatory process Effects 0.000 claims 1
- 230000003834 intracellular effect Effects 0.000 claims 1
- 208000002551 irritable bowel syndrome Diseases 0.000 claims 1
- 230000000302 ischemic effect Effects 0.000 claims 1
- 125000000959 isobutyl group Chemical group [H]C([H])([H])C([H])(C([H])([H])[H])C([H])([H])* 0.000 claims 1
- 230000000366 juvenile effect Effects 0.000 claims 1
- 208000032839 leukemia Diseases 0.000 claims 1
- 206010027175 memory impairment Diseases 0.000 claims 1
- 125000002950 monocyclic group Chemical group 0.000 claims 1
- 208000001725 mucocutaneous lymph node syndrome Diseases 0.000 claims 1
- 201000006417 multiple sclerosis Diseases 0.000 claims 1
- 201000008383 nephritis Diseases 0.000 claims 1
- 125000003261 o-tolyl group Chemical group [H]C1=C([H])C(*)=C(C([H])=C1[H])C([H])([H])[H] 0.000 claims 1
- 210000000056 organ Anatomy 0.000 claims 1
- 239000007800 oxidant agent Substances 0.000 claims 1
- 229910052760 oxygen Inorganic materials 0.000 claims 1
- 239000001301 oxygen Substances 0.000 claims 1
- 125000001037 p-tolyl group Chemical group [H]C1=C([H])C(=C([H])C([H])=C1*)C([H])([H])[H] 0.000 claims 1
- 125000004585 polycyclic heterocycle group Chemical group 0.000 claims 1
- 230000002062 proliferating effect Effects 0.000 claims 1
- 125000004076 pyridyl group Chemical group 0.000 claims 1
- 206010039083 rhinitis Diseases 0.000 claims 1
- 201000000980 schizophrenia Diseases 0.000 claims 1
- 201000005671 spondyloarthropathy Diseases 0.000 claims 1
- 125000001544 thienyl group Chemical group 0.000 claims 1
- 238000002054 transplantation Methods 0.000 claims 1
- 125000001425 triazolyl group Chemical group 0.000 claims 1
- 208000019553 vascular disease Diseases 0.000 claims 1
Applications Claiming Priority (4)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US90680407P | 2007-03-12 | 2007-03-12 | |
| US94352007P | 2007-06-12 | 2007-06-12 | |
| GBGB0722769.7A GB0722769D0 (en) | 2007-11-21 | 2007-11-21 | New compounds |
| PCT/GB2008/000854 WO2008110793A1 (en) | 2007-03-12 | 2008-03-12 | Piperidinones useful in the treatment of inflammation |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2010521443A JP2010521443A (ja) | 2010-06-24 |
| JP2010521443A5 true JP2010521443A5 (enExample) | 2012-05-24 |
Family
ID=38925771
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2009553202A Pending JP2010521443A (ja) | 2007-03-12 | 2008-03-12 | 炎症の治療において有用なピペリジノン類 |
Country Status (9)
| Country | Link |
|---|---|
| US (1) | US20100168167A1 (enExample) |
| EP (1) | EP2134686A1 (enExample) |
| JP (1) | JP2010521443A (enExample) |
| CN (1) | CN101679255A (enExample) |
| AR (1) | AR065708A1 (enExample) |
| CA (1) | CA2680412A1 (enExample) |
| GB (1) | GB0722769D0 (enExample) |
| TW (1) | TW200902000A (enExample) |
| WO (1) | WO2008110793A1 (enExample) |
Families Citing this family (17)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2296653B1 (en) | 2008-06-03 | 2016-01-27 | Intermune, Inc. | Compounds and methods for treating inflammatory and fibrotic disorders |
| WO2010029299A1 (en) * | 2008-09-12 | 2010-03-18 | Biolipox Ab | Pyrimidinone derivaties for use as medicaments |
| GB0907551D0 (en) * | 2009-05-01 | 2009-06-10 | Univ Dundee | Treatment or prophylaxis of proliferative conditions |
| WO2011114103A1 (en) * | 2010-03-18 | 2011-09-22 | Biolipox Ab | Pyrimidinones for use as medicaments |
| JO2998B1 (ar) * | 2010-06-04 | 2016-09-05 | Amgen Inc | مشتقات بيبيريدينون كمثبطات mdm2 لعلاج السرطان |
| MX352672B (es) | 2011-09-27 | 2017-12-04 | Amgen Inc | Compuestos heterocíclicos como inhibidores de mdm2 para el tratamiento del cáncer. |
| AR092742A1 (es) | 2012-10-02 | 2015-04-29 | Intermune Inc | Piridinonas antifibroticas |
| US9771326B2 (en) | 2012-11-20 | 2017-09-26 | Biogen Ma Inc. | S1P and/or ATX modulating agents |
| US11407721B2 (en) | 2013-02-19 | 2022-08-09 | Amgen Inc. | CIS-morpholinone and other compounds as MDM2 inhibitors for the treatment of cancer |
| WO2014134201A1 (en) | 2013-02-28 | 2014-09-04 | Amgen Inc. | A benzoic acid derivative mdm2 inhibitor for the treatment of cancer |
| WO2014151863A1 (en) | 2013-03-14 | 2014-09-25 | Amgen Inc. | Heteroaryl acid morpholinone compounds as mdm2 inhibitors for the treatment of cancer |
| MA53572A1 (fr) | 2013-06-10 | 2021-10-29 | Amgen Inc | Procédés de production et formes cristallines d'un inhibiteur mdm2 |
| RU2692485C2 (ru) | 2014-04-02 | 2019-06-25 | Интермьюн, Инк. | Противофиброзные пиридиноны |
| KR20200118827A (ko) | 2018-02-02 | 2020-10-16 | 마베릭스 온콜로지, 잉크. | 젬시타빈 모노포스페이트의 소분자 약물 컨쥬게이트 |
| CN116693540A (zh) * | 2023-05-23 | 2023-09-05 | 江苏八巨药业有限公司 | 一种西他列汀中间体的合成方法 |
| CN117180247B (zh) * | 2023-09-13 | 2026-05-26 | 山东第一医科大学第一附属医院(山东省千佛山医院) | 2-氨基-6-甲基苯酚衍生物作为铁死亡抑制剂在制备防治骨关节炎的药物中的应用 |
| CN118063332A (zh) * | 2024-02-29 | 2024-05-24 | 浙江鼎龙科技股份有限公司 | 一种2-羟基-4-乙基苯胺及其盐酸盐的制备方法 |
Family Cites Families (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DD90770A (enExample) * | ||||
| EP0299549A3 (en) * | 1987-07-09 | 1989-02-08 | Duphar International Research B.V | Tertiary 2,5-dialkyl-3-phenyl-piperidine derivatives having opiate-antagonistic activity |
| US6162927A (en) * | 1994-08-19 | 2000-12-19 | Abbott Laboratories | Endothelin antagonists |
| US7208517B1 (en) * | 1994-08-19 | 2007-04-24 | Abbott Labortories | Endothelin antagonists |
| WO2000014083A1 (en) * | 1998-09-09 | 2000-03-16 | Inflazyme Pharmaceuticals Ltd. | SUBSTITUTED η-PHENYL-Δ-LACTONES AND ANALOGS THEREOF AND USES RELATED THERETO |
| US6770658B2 (en) * | 1998-09-09 | 2004-08-03 | Inflazyme Pharmaceuticals Ltd. | Substituted γ-phenyl-Δ-lactams and uses related thereto |
| CA2402384A1 (en) * | 2000-03-16 | 2001-09-20 | Inflazyme Pharmaceuticals Ltd. | Benzylated pde4 inhibitors |
| US20020055457A1 (en) * | 2000-08-07 | 2002-05-09 | Janus Todd J. | Methods of treating cancer and the pain associated therewith using endothelin antagonists |
| US20040224316A1 (en) * | 2000-08-10 | 2004-11-11 | Tully Timothy P. | Augmented cognitive training |
| WO2005115389A2 (en) * | 2004-05-25 | 2005-12-08 | Pfizer Products Inc. | Specific ppar agonists for treating negative energy balance |
| US8865707B2 (en) * | 2005-12-30 | 2014-10-21 | Merck Sharp & Dohme Corp. | Cholesteryl ester transfer protein inhibitors |
| US7829713B2 (en) * | 2006-02-28 | 2010-11-09 | Helicon Therapeutics, Inc. | Therapeutic piperazines |
-
2007
- 2007-11-21 GB GBGB0722769.7A patent/GB0722769D0/en not_active Ceased
-
2008
- 2008-03-12 CN CN200880015373A patent/CN101679255A/zh active Pending
- 2008-03-12 JP JP2009553202A patent/JP2010521443A/ja active Pending
- 2008-03-12 US US12/530,578 patent/US20100168167A1/en not_active Abandoned
- 2008-03-12 EP EP08718700A patent/EP2134686A1/en not_active Withdrawn
- 2008-03-12 WO PCT/GB2008/000854 patent/WO2008110793A1/en not_active Ceased
- 2008-03-12 TW TW097108639A patent/TW200902000A/zh unknown
- 2008-03-12 CA CA002680412A patent/CA2680412A1/en not_active Abandoned
- 2008-03-12 AR ARP080101018A patent/AR065708A1/es unknown
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