JP2006515319A5 - - Google Patents
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- Publication number
- JP2006515319A5 JP2006515319A5 JP2005502644A JP2005502644A JP2006515319A5 JP 2006515319 A5 JP2006515319 A5 JP 2006515319A5 JP 2005502644 A JP2005502644 A JP 2005502644A JP 2005502644 A JP2005502644 A JP 2005502644A JP 2006515319 A5 JP2006515319 A5 JP 2006515319A5
- Authority
- JP
- Japan
- Prior art keywords
- aliphatic
- ring
- cycloaliphatic
- compound
- optionally substituted
- 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 53
- 125000001931 aliphatic group Chemical group 0.000 claims 43
- 125000005843 halogen group Chemical group 0.000 claims 19
- 125000001424 substituent group Chemical group 0.000 claims 19
- 125000005842 heteroatom Chemical group 0.000 claims 18
- 125000000623 heterocyclic group Chemical group 0.000 claims 16
- 229910052760 oxygen Inorganic materials 0.000 claims 16
- 229910052717 sulfur Inorganic materials 0.000 claims 15
- 125000001072 heteroaryl group Chemical group 0.000 claims 12
- 229910052757 nitrogen Inorganic materials 0.000 claims 12
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 12
- -1 cycloaliphatic Chemical group 0.000 claims 11
- 239000008194 pharmaceutical composition Substances 0.000 claims 11
- 125000003118 aryl group Chemical group 0.000 claims 10
- 125000000217 alkyl group Chemical group 0.000 claims 7
- 229910052736 halogen Inorganic materials 0.000 claims 7
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 6
- 125000004649 C2-C8 alkynyl group Chemical group 0.000 claims 6
- 125000003342 alkenyl group Chemical group 0.000 claims 6
- 125000000304 alkynyl group Chemical group 0.000 claims 6
- 150000002367 halogens Chemical class 0.000 claims 6
- 125000006413 ring segment Chemical group 0.000 claims 6
- 125000002373 5 membered heterocyclic group Chemical group 0.000 claims 5
- 125000003341 7 membered heterocyclic group Chemical group 0.000 claims 5
- 241000124008 Mammalia Species 0.000 claims 4
- 125000004093 cyano group Chemical group *C#N 0.000 claims 4
- 239000000203 mixture Substances 0.000 claims 4
- 125000003003 spiro group Chemical group 0.000 claims 4
- 125000001963 4 membered heterocyclic group Chemical group 0.000 claims 3
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 3
- 201000010099 disease Diseases 0.000 claims 3
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 3
- 230000002401 inhibitory effect Effects 0.000 claims 3
- 125000004076 pyridyl group Chemical group 0.000 claims 3
- 125000003107 substituted aryl group Chemical group 0.000 claims 3
- MZOFCQQQCNRIBI-VMXHOPILSA-N (3s)-4-[[(2s)-1-[[(2s)-1-[[(1s)-1-carboxy-2-hydroxyethyl]amino]-4-methyl-1-oxopentan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-3-[[2-[[(2s)-2,6-diaminohexanoyl]amino]acetyl]amino]-4-oxobutanoic acid Chemical compound OC[C@@H](C(O)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(O)=O)NC(=O)CNC(=O)[C@@H](N)CCCCN MZOFCQQQCNRIBI-VMXHOPILSA-N 0.000 claims 2
- 208000028006 Corneal injury Diseases 0.000 claims 2
- 102100031111 Disintegrin and metalloproteinase domain-containing protein 17 Human genes 0.000 claims 2
- 101000777461 Homo sapiens Disintegrin and metalloproteinase domain-containing protein 17 Proteins 0.000 claims 2
- 206010020751 Hypersensitivity Diseases 0.000 claims 2
- 206010061218 Inflammation Diseases 0.000 claims 2
- 206010028980 Neoplasm Diseases 0.000 claims 2
- 108060008682 Tumor Necrosis Factor Proteins 0.000 claims 2
- 102000000852 Tumor Necrosis Factor-alpha Human genes 0.000 claims 2
- 150000001408 amides Chemical class 0.000 claims 2
- 125000004429 atom Chemical group 0.000 claims 2
- 229910052799 carbon Inorganic materials 0.000 claims 2
- 125000004432 carbon atom Chemical group C* 0.000 claims 2
- 230000001413 cellular effect Effects 0.000 claims 2
- BFPSDSIWYFKGBC-UHFFFAOYSA-N chlorotrianisene Chemical compound C1=CC(OC)=CC=C1C(Cl)=C(C=1C=CC(OC)=CC=1)C1=CC=C(OC)C=C1 BFPSDSIWYFKGBC-UHFFFAOYSA-N 0.000 claims 2
- 125000002541 furyl group Chemical group 0.000 claims 2
- 229910052739 hydrogen Inorganic materials 0.000 claims 2
- 125000002883 imidazolyl group Chemical group 0.000 claims 2
- 238000001727 in vivo Methods 0.000 claims 2
- 230000004054 inflammatory process Effects 0.000 claims 2
- 125000001786 isothiazolyl group Chemical group 0.000 claims 2
- 125000001715 oxadiazolyl group Chemical group 0.000 claims 2
- 125000002971 oxazolyl group Chemical group 0.000 claims 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 2
- 125000003373 pyrazinyl group Chemical group 0.000 claims 2
- 125000003226 pyrazolyl group Chemical group 0.000 claims 2
- 125000002098 pyridazinyl group Chemical group 0.000 claims 2
- 125000000714 pyrimidinyl group Chemical group 0.000 claims 2
- 125000000168 pyrrolyl group Chemical group 0.000 claims 2
- 125000000472 sulfonyl group Chemical group *S(*)(=O)=O 0.000 claims 2
- 125000001113 thiadiazolyl group Chemical group 0.000 claims 2
- 125000000335 thiazolyl group Chemical group 0.000 claims 2
- 125000001544 thienyl group Chemical group 0.000 claims 2
- 125000004306 triazinyl group Chemical group 0.000 claims 2
- 125000001425 triazolyl group Chemical group 0.000 claims 2
- 125000000069 2-butynyl group Chemical group [H]C([H])([H])C#CC([H])([H])* 0.000 claims 1
- 125000004070 6 membered heterocyclic group Chemical group 0.000 claims 1
- 208000030507 AIDS Diseases 0.000 claims 1
- 206010001052 Acute respiratory distress syndrome Diseases 0.000 claims 1
- 208000024827 Alzheimer disease Diseases 0.000 claims 1
- 206010059245 Angiopathy Diseases 0.000 claims 1
- 201000001320 Atherosclerosis Diseases 0.000 claims 1
- 208000023275 Autoimmune disease Diseases 0.000 claims 1
- 201000006474 Brain Ischemia Diseases 0.000 claims 1
- 206010006895 Cachexia Diseases 0.000 claims 1
- 206010007559 Cardiac failure congestive Diseases 0.000 claims 1
- 206010008120 Cerebral ischaemia Diseases 0.000 claims 1
- 208000006545 Chronic Obstructive Pulmonary Disease Diseases 0.000 claims 1
- 206010011044 Corneal scar Diseases 0.000 claims 1
- 208000011231 Crohn disease Diseases 0.000 claims 1
- 206010014561 Emphysema Diseases 0.000 claims 1
- 206010014989 Epidermolysis bullosa Diseases 0.000 claims 1
- 206010019196 Head injury Diseases 0.000 claims 1
- 206010019280 Heart failures Diseases 0.000 claims 1
- 208000023105 Huntington disease Diseases 0.000 claims 1
- 208000022559 Inflammatory bowel disease Diseases 0.000 claims 1
- 201000009906 Meningitis Diseases 0.000 claims 1
- 206010027476 Metastases Diseases 0.000 claims 1
- 208000019695 Migraine disease Diseases 0.000 claims 1
- 206010029113 Neovascularisation Diseases 0.000 claims 1
- 208000001132 Osteoporosis Diseases 0.000 claims 1
- 208000018737 Parkinson disease Diseases 0.000 claims 1
- 208000013616 Respiratory Distress Syndrome Diseases 0.000 claims 1
- 206010040047 Sepsis Diseases 0.000 claims 1
- 206010040070 Septic Shock Diseases 0.000 claims 1
- 208000006011 Stroke Diseases 0.000 claims 1
- 206010064390 Tumour invasion Diseases 0.000 claims 1
- 208000025865 Ulcer Diseases 0.000 claims 1
- 230000002159 abnormal effect Effects 0.000 claims 1
- 125000000641 acridinyl group Chemical group C1(=CC=CC2=NC3=CC=CC=C3C=C12)* 0.000 claims 1
- 201000000028 adult respiratory distress syndrome Diseases 0.000 claims 1
- 208000026935 allergic disease Diseases 0.000 claims 1
- 230000000172 allergic effect Effects 0.000 claims 1
- 208000030961 allergic reaction Diseases 0.000 claims 1
- 230000007815 allergy Effects 0.000 claims 1
- 206010002026 amyotrophic lateral sclerosis Diseases 0.000 claims 1
- 208000007474 aortic aneurysm Diseases 0.000 claims 1
- 206010003246 arthritis Diseases 0.000 claims 1
- 125000001769 aryl amino group Chemical group 0.000 claims 1
- 125000005129 aryl carbonyl group Chemical group 0.000 claims 1
- 125000004391 aryl sulfonyl group Chemical group 0.000 claims 1
- 208000006673 asthma 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
- 210000004556 brain Anatomy 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- 230000009400 cancer invasion Effects 0.000 claims 1
- 125000000609 carbazolyl group Chemical group C1(=CC=CC=2C3=CC=CC=C3NC12)* 0.000 claims 1
- 210000000170 cell membrane Anatomy 0.000 claims 1
- 206010008118 cerebral infarction Diseases 0.000 claims 1
- 125000000259 cinnolinyl group Chemical group N1=NC(=CC2=CC=CC=C12)* 0.000 claims 1
- 238000003776 cleavage reaction Methods 0.000 claims 1
- 239000002475 cognitive enhancer Substances 0.000 claims 1
- 208000010247 contact dermatitis Diseases 0.000 claims 1
- 125000004122 cyclic group Chemical group 0.000 claims 1
- 125000000753 cycloalkyl 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
- 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
- 125000001511 cyclopentyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 1
- 206010012601 diabetes mellitus Diseases 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 210000004696 endometrium Anatomy 0.000 claims 1
- 239000001257 hydrogen Substances 0.000 claims 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 1
- 125000004356 hydroxy functional group Chemical group O* 0.000 claims 1
- 239000007943 implant Substances 0.000 claims 1
- 125000003406 indolizinyl group Chemical group C=1(C=CN2C=CC=CC12)* 0.000 claims 1
- 125000001041 indolyl group Chemical group 0.000 claims 1
- 230000003993 interaction Effects 0.000 claims 1
- 125000000904 isoindolyl group Chemical group C=1(NC=C2C=CC=CC12)* 0.000 claims 1
- 125000002183 isoquinolinyl group Chemical group C1(=NC=CC2=CC=CC=C12)* 0.000 claims 1
- 208000002780 macular degeneration Diseases 0.000 claims 1
- 230000001404 mediated effect Effects 0.000 claims 1
- 239000012528 membrane Substances 0.000 claims 1
- 230000009401 metastasis Effects 0.000 claims 1
- 206010027599 migraine Diseases 0.000 claims 1
- 125000002950 monocyclic group Chemical group 0.000 claims 1
- 201000006417 multiple sclerosis Diseases 0.000 claims 1
- 208000010125 myocardial infarction Diseases 0.000 claims 1
- 208000004296 neuralgia Diseases 0.000 claims 1
- 208000015122 neurodegenerative disease Diseases 0.000 claims 1
- 208000021722 neuropathic pain Diseases 0.000 claims 1
- 210000000056 organ Anatomy 0.000 claims 1
- 125000004043 oxo group Chemical group O=* 0.000 claims 1
- UUEVFMOUBSLVJW-UHFFFAOYSA-N oxo-[[1-[2-[2-[2-[4-(oxoazaniumylmethylidene)pyridin-1-yl]ethoxy]ethoxy]ethyl]pyridin-4-ylidene]methyl]azanium;dibromide Chemical compound [Br-].[Br-].C1=CC(=C[NH+]=O)C=CN1CCOCCOCCN1C=CC(=C[NH+]=O)C=C1 UUEVFMOUBSLVJW-UHFFFAOYSA-N 0.000 claims 1
- 208000028169 periodontal disease Diseases 0.000 claims 1
- 125000001791 phenazinyl group Chemical group C1(=CC=CC2=NC3=CC=CC=C3N=C12)* 0.000 claims 1
- 125000001484 phenothiazinyl group Chemical group C1(=CC=CC=2SC3=CC=CC=C3NC12)* 0.000 claims 1
- 125000001644 phenoxazinyl group Chemical group C1(=CC=CC=2OC3=CC=CC=C3NC12)* 0.000 claims 1
- 125000004592 phthalazinyl group Chemical group C1(=NN=CC2=CC=CC=C12)* 0.000 claims 1
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 1
- 125000006239 protecting group Chemical group 0.000 claims 1
- 125000001042 pteridinyl group Chemical group N1=C(N=CC2=NC=CN=C12)* 0.000 claims 1
- 125000000561 purinyl group Chemical group N1=C(N=C2N=CNC2=C1)* 0.000 claims 1
- 125000000719 pyrrolidinyl group Chemical group 0.000 claims 1
- 125000002294 quinazolinyl group Chemical group N1=C(N=CC2=CC=CC=C12)* 0.000 claims 1
- 125000002943 quinolinyl group Chemical group N1=C(C=CC2=CC=CC=C12)* 0.000 claims 1
- 125000001567 quinoxalinyl group Chemical group N1=C(C=NC2=CC=CC=C12)* 0.000 claims 1
- 208000037803 restenosis Diseases 0.000 claims 1
- 230000007017 scission Effects 0.000 claims 1
- 230000036303 septic shock Effects 0.000 claims 1
- 208000020431 spinal cord injury Diseases 0.000 claims 1
- 208000024891 symptom Diseases 0.000 claims 1
- 230000009885 systemic effect Effects 0.000 claims 1
- 230000001988 toxicity Effects 0.000 claims 1
- 231100000419 toxicity Toxicity 0.000 claims 1
- 230000004614 tumor growth Effects 0.000 claims 1
- 230000036269 ulceration Effects 0.000 claims 1
- 230000029663 wound healing Effects 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US43493602P | 2002-12-19 | 2002-12-19 | |
| US44363903P | 2003-01-29 | 2003-01-29 | |
| PCT/US2003/040512 WO2004056766A1 (en) | 2002-12-19 | 2003-12-19 | Inhibitors of tace |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2006515319A JP2006515319A (ja) | 2006-05-25 |
| JP2006515319A5 true JP2006515319A5 (https=) | 2007-02-08 |
| JP4580866B2 JP4580866B2 (ja) | 2010-11-17 |
Family
ID=32685351
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2005502644A Expired - Fee Related JP4580866B2 (ja) | 2002-12-19 | 2003-12-19 | Taceのインヒビター |
Country Status (8)
| Country | Link |
|---|---|
| US (2) | US7485664B2 (https=) |
| EP (1) | EP1581488B1 (https=) |
| JP (1) | JP4580866B2 (https=) |
| AT (1) | ATE443044T1 (https=) |
| AU (1) | AU2003297364B2 (https=) |
| CA (1) | CA2510807C (https=) |
| DE (1) | DE60329326D1 (https=) |
| WO (1) | WO2004056766A1 (https=) |
Families Citing this family (15)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20020128476A1 (en) * | 1996-08-08 | 2002-09-12 | Smithkline Beecham Corporation | Inhibitors of cysteine protease |
| ATE443044T1 (de) * | 2002-12-19 | 2009-10-15 | Vertex Pharma | Tace inhibitoren |
| US7488745B2 (en) | 2004-07-16 | 2009-02-10 | Schering Corporation | Compounds for the treatment of inflammatory disorders |
| US7504424B2 (en) | 2004-07-16 | 2009-03-17 | Schering Corporation | Compounds for the treatment of inflammatory disorders |
| ATE478864T1 (de) | 2004-07-16 | 2010-09-15 | Schering Corp | Hydantoinderivate zur behandlung von entzündlichen erkrankungen |
| WO2007016597A2 (en) * | 2005-07-29 | 2007-02-08 | The Regents Of The University Of California | Targeting tnf-alpha converting enzyme (tace)-dependent growth factor shedding in cancer therapy |
| AR059036A1 (es) | 2006-01-17 | 2008-03-12 | Schering Corp | Compuestos para el tratamiento de trastornos inflamatorios |
| TW201024304A (en) | 2008-09-24 | 2010-07-01 | Schering Corp | Compounds for the treatment of inflammatory disorders |
| EP2346857B1 (en) | 2008-09-24 | 2019-11-27 | Merck Sharp & Dohme Corp. | Compounds for the treatment of inflammatory disorders |
| EP2356111A1 (en) | 2008-11-10 | 2011-08-17 | Schering Corporation | Compounds for the treatment of inflammatory disorders |
| US8569336B2 (en) | 2008-11-10 | 2013-10-29 | Ling Tong | Compounds for the treatment of inflammatory disorders |
| DK2597084T3 (en) * | 2010-07-08 | 2016-08-15 | Kaken Pharma Co Ltd | N-HYDROXYFORMAMIDE DERIVATIVE AND MEDICINAL CONTAINING SAME |
| EP2617812B1 (en) | 2010-09-17 | 2019-03-20 | The University of Tokyo | Composition for maintaining platelet function |
| US12213970B2 (en) | 2018-10-29 | 2025-02-04 | Boehringer Ingelheim International Gmbh | Pyridinyl sulfonamide derivatives, pharmaceutical compositions and uses thereof |
| DK3873600T5 (da) | 2018-10-29 | 2024-03-18 | Boehringer Ingelheim Int | Pyridinylsulfonamidderivater, farmaceutiske sammensætninger og anvendelser deraf |
Family Cites Families (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3501489A (en) * | 1966-01-21 | 1970-03-17 | American Home Prod | 1-phenylsulfonyl-2-(2-thiazolin-2-yl-oxy and thiol) pyrrolidines |
| US5734081A (en) * | 1994-08-05 | 1998-03-31 | Warner-Lambert Company | Arylthio compounds |
| US6747027B1 (en) * | 1996-07-22 | 2004-06-08 | Pharmacia Corporation | Thiol sulfonamide metalloprotease inhibitors |
| BR9712792A (pt) * | 1996-08-28 | 1999-12-14 | Procter & Gamble | Inibidores de metaloprotease bidentada. |
| JPH11147876A (ja) * | 1997-09-12 | 1999-06-02 | Kanebo Ltd | テトラヒドロイソキノリン誘導体およびそれを有効成分とする薬剤 |
| JPH11343279A (ja) * | 1998-03-16 | 1999-12-14 | Shionogi & Co Ltd | スルホンアミド誘導体およびそれらを含有するTNF―α産生抑制剤 |
| WO2000023443A1 (en) * | 1998-10-22 | 2000-04-27 | Akzo Nobel N.V. | Tetrahydropyridopyridine derivatives and intermediates for producing the same |
| AR035313A1 (es) | 1999-01-27 | 2004-05-12 | Wyeth Corp | Inhibidores de tace acetilenicos de acido hidroxamico de sulfonamida a base de alfa-aminoacidos, composiciones farmaceuticas y el uso de los mismos para la manufactura de medicamentos. |
| US6313123B1 (en) | 1999-01-27 | 2001-11-06 | American Cyanamid Company | Acetylenic sulfonamide thiol tace inhibitors |
| ATE443044T1 (de) | 2002-12-19 | 2009-10-15 | Vertex Pharma | Tace inhibitoren |
-
2003
- 2003-12-19 AT AT03813772T patent/ATE443044T1/de not_active IP Right Cessation
- 2003-12-19 EP EP03813772A patent/EP1581488B1/en not_active Expired - Lifetime
- 2003-12-19 AU AU2003297364A patent/AU2003297364B2/en not_active Ceased
- 2003-12-19 JP JP2005502644A patent/JP4580866B2/ja not_active Expired - Fee Related
- 2003-12-19 US US10/741,164 patent/US7485664B2/en not_active Expired - Fee Related
- 2003-12-19 CA CA2510807A patent/CA2510807C/en not_active Expired - Fee Related
- 2003-12-19 DE DE60329326T patent/DE60329326D1/de not_active Expired - Lifetime
- 2003-12-19 WO PCT/US2003/040512 patent/WO2004056766A1/en not_active Ceased
-
2008
- 2008-11-12 US US12/269,429 patent/US7919520B2/en not_active Expired - Fee Related
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