JP2005513065A5 - - Google Patents
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- Publication number
- JP2005513065A5 JP2005513065A5 JP2003552713A JP2003552713A JP2005513065A5 JP 2005513065 A5 JP2005513065 A5 JP 2005513065A5 JP 2003552713 A JP2003552713 A JP 2003552713A JP 2003552713 A JP2003552713 A JP 2003552713A JP 2005513065 A5 JP2005513065 A5 JP 2005513065A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- alkoxy
- substituted
- unsubstituted
- group
- 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
- 229910052736 halogen Inorganic materials 0.000 claims 81
- 150000002367 halogens Chemical class 0.000 claims 77
- 125000004356 hydroxy functional group Chemical group O* 0.000 claims 70
- 229910052739 hydrogen Inorganic materials 0.000 claims 55
- 229910052799 carbon Inorganic materials 0.000 claims 49
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 39
- -1 azocanyl Chemical group 0.000 claims 35
- 125000000217 alkyl group Chemical group 0.000 claims 31
- 125000002757 morpholinyl group Chemical group 0.000 claims 31
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 29
- 150000001875 compounds Chemical class 0.000 claims 28
- 125000005843 halogen group Chemical group 0.000 claims 28
- 125000004568 thiomorpholinyl group Chemical group 0.000 claims 28
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims 26
- 125000004076 pyridyl group Chemical group 0.000 claims 26
- 125000003545 alkoxy group Chemical group 0.000 claims 25
- 125000000168 pyrrolyl group Chemical group 0.000 claims 25
- 229910052757 nitrogen Inorganic materials 0.000 claims 24
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims 23
- 125000003386 piperidinyl group Chemical group 0.000 claims 23
- 125000000714 pyrimidinyl group Chemical group 0.000 claims 22
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims 19
- 125000003373 pyrazinyl group Chemical group 0.000 claims 18
- 125000002632 imidazolidinyl group Chemical group 0.000 claims 17
- 125000006700 (C1-C6) alkylthio group Chemical group 0.000 claims 16
- XEEYBQQBJWHFJM-UHFFFAOYSA-N Iron Chemical compound [Fe] XEEYBQQBJWHFJM-UHFFFAOYSA-N 0.000 claims 15
- 125000001624 naphthyl group Chemical group 0.000 claims 13
- 125000004193 piperazinyl group Chemical group 0.000 claims 13
- 125000000719 pyrrolidinyl group Chemical group 0.000 claims 12
- 229910052717 sulfur Inorganic materials 0.000 claims 12
- 125000001544 thienyl group Chemical group 0.000 claims 12
- 229910052794 bromium Inorganic materials 0.000 claims 11
- 229910052801 chlorine Inorganic materials 0.000 claims 11
- 125000005495 pyridazyl group Chemical group 0.000 claims 11
- 125000005605 benzo group Chemical group 0.000 claims 10
- 238000000034 method Methods 0.000 claims 10
- 125000003710 aryl alkyl group Chemical group 0.000 claims 8
- 125000004093 cyano group Chemical group *C#N 0.000 claims 8
- 229910052731 fluorine Inorganic materials 0.000 claims 8
- 125000002098 pyridazinyl group Chemical group 0.000 claims 8
- 125000001712 tetrahydronaphthyl group Chemical group C1(CCCC2=CC=CC=C12)* 0.000 claims 8
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims 7
- 125000005046 dihydronaphthyl group Chemical group 0.000 claims 7
- 229910052760 oxygen Inorganic materials 0.000 claims 7
- 125000002541 furyl group Chemical group 0.000 claims 6
- 239000001257 hydrogen Substances 0.000 claims 6
- 150000002431 hydrogen Chemical class 0.000 claims 6
- 125000002183 isoquinolinyl group Chemical group C1(=NC=CC2=CC=CC=C12)* 0.000 claims 6
- 125000002943 quinolinyl group Chemical group N1=C(C=CC2=CC=CC=C12)* 0.000 claims 6
- 125000003039 tetrahydroisoquinolinyl group Chemical group C1(NCCC2=CC=CC=C12)* 0.000 claims 6
- 125000003118 aryl group Chemical group 0.000 claims 5
- 125000003725 azepanyl group Chemical group 0.000 claims 5
- 125000002883 imidazolyl group Chemical group 0.000 claims 5
- 125000004438 haloalkoxy group Chemical group 0.000 claims 4
- 125000001188 haloalkyl group Chemical group 0.000 claims 4
- 125000001072 heteroaryl group Chemical group 0.000 claims 4
- 125000000094 2-phenylethyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])C([H])([H])* 0.000 claims 3
- WEVYAHXRMPXWCK-UHFFFAOYSA-N Acetonitrile Chemical compound CC#N WEVYAHXRMPXWCK-UHFFFAOYSA-N 0.000 claims 3
- 125000004183 alkoxy alkyl group Chemical group 0.000 claims 3
- 125000002490 anilino group Chemical class [H]N(*)C1=C([H])C([H])=C([H])C([H])=C1[H] 0.000 claims 3
- 125000001589 carboacyl group Chemical group 0.000 claims 3
- 239000008194 pharmaceutical composition Substances 0.000 claims 3
- 150000003839 salts Chemical class 0.000 claims 3
- 238000006467 substitution reaction Methods 0.000 claims 3
- 125000006582 (C5-C6) heterocycloalkyl group Chemical group 0.000 claims 2
- 125000001622 2-naphthyl group Chemical group [H]C1=C([H])C([H])=C2C([H])=C(*)C([H])=C([H])C2=C1[H] 0.000 claims 2
- 125000004180 3-fluorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C(F)=C1[H] 0.000 claims 2
- 125000004801 4-cyanophenyl group Chemical group [H]C1=C([H])C(C#N)=C([H])C([H])=C1* 0.000 claims 2
- 125000001255 4-fluorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C([H])=C1F 0.000 claims 2
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims 2
- TVFDJXOCXUVLDH-UHFFFAOYSA-N caesium atom Chemical group [Cs] TVFDJXOCXUVLDH-UHFFFAOYSA-N 0.000 claims 2
- 125000001153 fluoro group Chemical group F* 0.000 claims 2
- 125000004446 heteroarylalkyl group Chemical group 0.000 claims 2
- 125000005885 heterocycloalkylalkyl group Chemical group 0.000 claims 2
- 125000002768 hydroxyalkyl group Chemical group 0.000 claims 2
- 239000013067 intermediate product Substances 0.000 claims 2
- 239000003960 organic solvent Substances 0.000 claims 2
- 239000001301 oxygen Substances 0.000 claims 2
- 125000003854 p-chlorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C([H])=C1Cl 0.000 claims 2
- 125000003884 phenylalkyl group Chemical group 0.000 claims 2
- 150000003461 sulfonyl halides Chemical class 0.000 claims 2
- PTTUMBGORBMNBN-UHFFFAOYSA-N 1,2,3-trifluoro-5-nitrobenzene Chemical compound [O-][N+](=O)C1=CC(F)=C(F)C(F)=C1 PTTUMBGORBMNBN-UHFFFAOYSA-N 0.000 claims 1
- 206010028980 Neoplasm Diseases 0.000 claims 1
- NQRYJNQNLNOLGT-UHFFFAOYSA-N Piperidine Chemical compound C1CCNCC1 NQRYJNQNLNOLGT-UHFFFAOYSA-N 0.000 claims 1
- 125000003342 alkenyl group Chemical group 0.000 claims 1
- 125000006350 alkyl thio alkyl group Chemical group 0.000 claims 1
- 230000033115 angiogenesis Effects 0.000 claims 1
- 206010003246 arthritis Diseases 0.000 claims 1
- 125000002102 aryl alkyloxo group Chemical group 0.000 claims 1
- 125000004104 aryloxy group Chemical group 0.000 claims 1
- 230000015572 biosynthetic process Effects 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- 125000001309 chloro group Chemical group Cl* 0.000 claims 1
- 125000000753 cycloalkyl group Chemical group 0.000 claims 1
- 239000012954 diazonium Substances 0.000 claims 1
- IJGRMHOSHXDMSA-UHFFFAOYSA-O diazynium Chemical compound [NH+]#N IJGRMHOSHXDMSA-UHFFFAOYSA-O 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
- 230000000694 effects Effects 0.000 claims 1
- 239000011737 fluorine Substances 0.000 claims 1
- 150000004820 halides Chemical group 0.000 claims 1
- 125000005114 heteroarylalkoxy group Chemical group 0.000 claims 1
- 125000005553 heteroaryloxy group Chemical group 0.000 claims 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 1
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 1
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 1
- XAEFZNCEHLXOMS-UHFFFAOYSA-M potassium benzoate Chemical compound [K+].[O-]C(=O)C1=CC=CC=C1 XAEFZNCEHLXOMS-UHFFFAOYSA-M 0.000 claims 1
- 230000001105 regulatory effect Effects 0.000 claims 1
- 238000001308 synthesis method Methods 0.000 claims 1
- 238000003786 synthesis reaction Methods 0.000 claims 1
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US34017901P | 2001-12-14 | 2001-12-14 | |
| PCT/US2002/039816 WO2003051825A1 (en) | 2001-12-14 | 2002-12-13 | Human adam-10 inhibitors |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2005513065A JP2005513065A (ja) | 2005-05-12 |
| JP2005513065A5 true JP2005513065A5 (enExample) | 2006-01-05 |
| JP4427328B2 JP4427328B2 (ja) | 2010-03-03 |
Family
ID=23332222
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2003552713A Expired - Fee Related JP4427328B2 (ja) | 2001-12-14 | 2002-12-13 | ヒト−ａｄａｍ−１０インヒビター |
Country Status (9)
| Country | Link |
|---|---|
| US (2) | US7498358B2 (enExample) |
| EP (1) | EP1461313B1 (enExample) |
| JP (1) | JP4427328B2 (enExample) |
| AT (1) | ATE438618T1 (enExample) |
| AU (1) | AU2002346724B2 (enExample) |
| CA (1) | CA2473938C (enExample) |
| DE (1) | DE60233261D1 (enExample) |
| ES (1) | ES2331177T3 (enExample) |
| WO (1) | WO2003051825A1 (enExample) |
Families Citing this family (23)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2003051825A1 (en) * | 2001-12-14 | 2003-06-26 | Exelixis, Inc. | Human adam-10 inhibitors |
| JP4002927B2 (ja) | 2002-05-29 | 2007-11-07 | メルク エンド カムパニー インコーポレーテッド | 炭疸病治療および致死因子阻害に有用な化合物 |
| AU2003237532B2 (en) * | 2002-06-12 | 2009-07-30 | Symphony Evolution, Inc. | Human ADAM-10 inhibitors |
| WO2004089294A2 (en) | 2003-04-04 | 2004-10-21 | Incyte Corporation | Compositions, methods and kits relating to her-2 cleavage |
| GB0311228D0 (en) * | 2003-05-16 | 2003-06-18 | Celltech R&D Ltd | Assay |
| EP1493445A1 (en) * | 2003-07-04 | 2005-01-05 | Max-Planck-Gesellschaft zur Förderung der Wissenschaften e.V. | Inhibition of stress-induced ligand-dependent EGFR activation |
| US7163942B2 (en) * | 2004-04-01 | 2007-01-16 | Pfizer Inc. | Sulfonamide compounds for the treatment of neurodegenerative disorders |
| CA2566191A1 (en) | 2004-05-11 | 2005-12-15 | Merck & Co., Inc. | Process for making n-sulfonated-amino acid derivatives |
| EP1623995A1 (en) | 2004-08-06 | 2006-02-08 | Deutsches Krebsforschungszentrum Stiftung des öffentlichen Rechts | Inhibitors of L1 and ADAM10 for the treatment of carcinomas |
| WO2007084488A2 (en) * | 2006-01-13 | 2007-07-26 | Vanderbilt University | Adam10 and its uses related to infection |
| WO2007103114A2 (en) * | 2006-03-07 | 2007-09-13 | The Brigham & Women's Hospital, Inc. | Notch inhibition in the treatment or prevention of atherosclerosis |
| US9567396B2 (en) | 2006-03-07 | 2017-02-14 | Evonik Degussa Gmbh | Notch inhibition in the prevention of vein graft failure |
| WO2009096198A1 (ja) * | 2008-02-01 | 2009-08-06 | Pharma Ip Limited Liability Intermediary Corporations | 新規ビアリール誘導体 |
| US20120129189A1 (en) * | 2009-07-17 | 2012-05-24 | Chulan Kwon | Methods of Controlling Cell Proliferation |
| EP2493497A4 (en) | 2009-11-01 | 2013-07-24 | Brigham & Womens Hospital | NOTCH INHIBITION IN THE TREATMENT AND PROPHYLAXIS OF ADIPOSITAS AND METABOLISM SYNDROME |
| US8765814B2 (en) | 2010-07-08 | 2014-07-01 | Kaken Pharmaceutical Co., Ltd. | N-hydroxyformamide derivative and medicament containing same |
| EP2637679A4 (en) | 2010-11-09 | 2015-09-23 | Univ Chicago | ROLE OF ADAM10 AND ITS RELEVANCE TO DISEASES AND THERAPEUTICS |
| EP2606884A1 (en) | 2011-12-21 | 2013-06-26 | Ecole Polytechnique Fédérale de Lausanne (EPFL) | Inhibitors of notch signaling pathway and use thereof in treatment of cancers |
| CN112351969A (zh) | 2018-06-21 | 2021-02-09 | 塞莱斯蒂亚生物技术股份公司 | 用于制备氨基二芳基醚和氨基二芳基醚盐酸盐的方法 |
| WO2020016377A1 (en) | 2018-07-19 | 2020-01-23 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Combination for treating cancer |
| CN108947850B (zh) * | 2018-07-23 | 2021-05-18 | 蚌埠中实化学技术有限公司 | 一种3,4,5-三氟苯胺的制备方法 |
| CN113966324B (zh) | 2019-04-10 | 2024-09-03 | 塞莱斯蒂亚生物技术股份公司 | Notch信号传导途径抑制剂及其在癌症治疗的用途 |
| EP4244391A1 (en) | 2020-11-16 | 2023-09-20 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Methods and compositions for predicting and treating uveal melanoma |
Family Cites Families (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5985900A (en) | 1997-04-01 | 1999-11-16 | Agouron Pharmaceuticals, Inc. | Metalloproteinase inhibitors, pharmaceutical compositions containing them and their pharmaceutical uses |
| ID24105A (id) | 1997-07-22 | 2000-07-06 | Shionogi & Co | Komposisi untuk mengobati atau mencegah glomerulopati |
| PL342009A1 (en) | 1998-02-04 | 2001-05-07 | Novartis Ag | Sulphonylamine derivatives capable to inhibit extracellular substance degrading metaloproteinases |
| JPH11246527A (ja) | 1998-03-02 | 1999-09-14 | Shionogi & Co Ltd | Ｍｍｐ−８阻害剤 |
| WO2000015213A1 (en) * | 1998-09-11 | 2000-03-23 | Shionogi & Co., Ltd. | Remedal or preventive agent for congestive heart failure |
| WO2003051825A1 (en) * | 2001-12-14 | 2003-06-26 | Exelixis, Inc. | Human adam-10 inhibitors |
-
2002
- 2002-12-13 WO PCT/US2002/039816 patent/WO2003051825A1/en not_active Ceased
- 2002-12-13 ES ES02784794T patent/ES2331177T3/es not_active Expired - Lifetime
- 2002-12-13 AU AU2002346724A patent/AU2002346724B2/en not_active Ceased
- 2002-12-13 JP JP2003552713A patent/JP4427328B2/ja not_active Expired - Fee Related
- 2002-12-13 AT AT02784794T patent/ATE438618T1/de not_active IP Right Cessation
- 2002-12-13 US US10/498,338 patent/US7498358B2/en not_active Expired - Fee Related
- 2002-12-13 EP EP02784794A patent/EP1461313B1/en not_active Expired - Lifetime
- 2002-12-13 DE DE60233261T patent/DE60233261D1/de not_active Expired - Lifetime
- 2002-12-13 CA CA2473938A patent/CA2473938C/en not_active Expired - Fee Related
-
2009
- 2009-02-02 US US12/322,422 patent/US7951972B2/en not_active Expired - Fee Related
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