CA2472341C - Phosphorus-containing compounds & uses thereof - Google Patents
Phosphorus-containing compounds & uses thereof Download PDFInfo
- Publication number
- CA2472341C CA2472341C CA2472341A CA2472341A CA2472341C CA 2472341 C CA2472341 C CA 2472341C CA 2472341 A CA2472341 A CA 2472341A CA 2472341 A CA2472341 A CA 2472341A CA 2472341 C CA2472341 C CA 2472341C
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- moiety
- compound
- independently
- aliphatic
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- 150000001875 compounds Chemical class 0.000 title claims abstract description 368
- 229910052698 phosphorus Inorganic materials 0.000 title claims abstract description 21
- OAICVXFJPJFONN-UHFFFAOYSA-N Phosphorus Chemical compound [P] OAICVXFJPJFONN-UHFFFAOYSA-N 0.000 title abstract description 15
- 239000011574 phosphorus Substances 0.000 title abstract description 15
- -1 heteroaliphatic Chemical group 0.000 claims abstract description 180
- 125000003118 aryl group Chemical group 0.000 claims abstract description 101
- 125000001931 aliphatic group Chemical group 0.000 claims abstract description 92
- 125000001072 heteroaryl group Chemical group 0.000 claims abstract description 63
- 239000000126 substance Substances 0.000 claims abstract description 42
- 229910052717 sulfur Inorganic materials 0.000 claims abstract description 21
- 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 abstract description 19
- 229910052760 oxygen Inorganic materials 0.000 claims abstract description 17
- 229960002930 sirolimus Drugs 0.000 claims description 109
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- QFJCIRLUMZQUOT-HPLJOQBZSA-N sirolimus Chemical compound C1C[C@@H](O)[C@H](OC)C[C@@H]1C[C@@H](C)[C@H]1OC(=O)[C@@H]2CCCCN2C(=O)C(=O)[C@](O)(O2)[C@H](C)CC[C@H]2C[C@H](OC)/C(C)=C/C=C/C=C/[C@@H](C)C[C@@H](C)C(=O)[C@H](OC)[C@H](O)/C(C)=C/[C@@H](C)C(=O)C1 QFJCIRLUMZQUOT-HPLJOQBZSA-N 0.000 claims description 99
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- 125000001424 substituent group Chemical group 0.000 claims description 36
- 239000003795 chemical substances by application Substances 0.000 claims description 33
- 125000000623 heterocyclic group Chemical group 0.000 claims description 30
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims description 30
- 238000011282 treatment Methods 0.000 claims description 30
- 210000001519 tissue Anatomy 0.000 claims description 28
- 150000003839 salts Chemical class 0.000 claims description 27
- 125000004432 carbon atom Chemical group C* 0.000 claims description 26
- 125000003545 alkoxy group Chemical group 0.000 claims description 25
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims description 24
- 238000004519 manufacturing process Methods 0.000 claims description 22
- 229910052736 halogen Inorganic materials 0.000 claims description 20
- 150000002367 halogens Chemical class 0.000 claims description 20
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- 125000005843 halogen group Chemical group 0.000 claims description 19
- 125000005113 hydroxyalkoxy group Chemical group 0.000 claims description 19
- 229910052757 nitrogen Inorganic materials 0.000 claims description 19
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- 125000001188 haloalkyl group Chemical group 0.000 claims description 17
- 230000001404 mediated effect Effects 0.000 claims description 17
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims description 17
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- 125000002252 acyl group Chemical group 0.000 claims description 16
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- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 16
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims description 16
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- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 14
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims description 14
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- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical group [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims description 13
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- 102000005962 receptors Human genes 0.000 claims description 13
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- 125000004122 cyclic group Chemical group 0.000 claims description 12
- STQGQHZAVUOBTE-VGBVRHCVSA-N daunorubicin Chemical compound O([C@H]1C[C@@](O)(CC=2C(O)=C3C(=O)C=4C=CC=C(C=4C(=O)C3=C(O)C=21)OC)C(C)=O)[C@H]1C[C@H](N)[C@H](O)[C@H](C)O1 STQGQHZAVUOBTE-VGBVRHCVSA-N 0.000 claims description 12
- 125000000325 methylidene group Chemical group [H]C([H])=* 0.000 claims description 12
- HTTJABKRGRZYRN-UHFFFAOYSA-N Heparin Chemical compound OC1C(NC(=O)C)C(O)OC(COS(O)(=O)=O)C1OC1C(OS(O)(=O)=O)C(O)C(OC2C(C(OS(O)(=O)=O)C(OC3C(C(O)C(O)C(O3)C(O)=O)OS(O)(=O)=O)C(CO)O2)NS(O)(=O)=O)C(C(O)=O)O1 HTTJABKRGRZYRN-UHFFFAOYSA-N 0.000 claims description 11
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims description 11
- 150000002576 ketones Chemical group 0.000 claims description 11
- AOJJSUZBOXZQNB-TZSSRYMLSA-N Doxorubicin Chemical compound O([C@H]1C[C@@](O)(CC=2C(O)=C3C(=O)C=4C=CC=C(C=4C(=O)C3=C(O)C=21)OC)C(=O)CO)[C@H]1C[C@H](N)[C@H](O)[C@H](C)O1 AOJJSUZBOXZQNB-TZSSRYMLSA-N 0.000 claims description 10
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- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical group [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims description 10
- 125000002015 acyclic group Chemical group 0.000 claims description 10
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- VOXZDWNPVJITMN-ZBRFXRBCSA-N 17β-estradiol Chemical compound OC1=CC=C2[C@H]3CC[C@](C)([C@H](CC4)O)[C@@H]4[C@@H]3CCC2=C1 VOXZDWNPVJITMN-ZBRFXRBCSA-N 0.000 claims description 9
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- 125000004123 n-propyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])* 0.000 claims description 9
- 230000002829 reductive effect Effects 0.000 claims description 9
- 125000002914 sec-butyl group Chemical group [H]C([H])([H])C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims description 9
- 239000000454 talc Substances 0.000 claims description 9
- 229910052623 talc Inorganic materials 0.000 claims description 9
- 229940033134 talc Drugs 0.000 claims description 9
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 claims description 9
- 238000002560 therapeutic procedure Methods 0.000 claims description 9
- VVIAGPKUTFNRDU-UHFFFAOYSA-N 6S-folinic acid Natural products C1NC=2NC(N)=NC(=O)C=2N(C=O)C1CNC1=CC=C(C(=O)NC(CCC(O)=O)C(O)=O)C=C1 VVIAGPKUTFNRDU-UHFFFAOYSA-N 0.000 claims description 8
- RZVAJINKPMORJF-UHFFFAOYSA-N Acetaminophen Chemical compound CC(=O)NC1=CC=C(O)C=C1 RZVAJINKPMORJF-UHFFFAOYSA-N 0.000 claims description 8
- 201000004624 Dermatitis Diseases 0.000 claims description 8
- NKANXQFJJICGDU-QPLCGJKRSA-N Tamoxifen Chemical compound C=1C=CC=CC=1C(/CC)=C(C=1C=CC(OCCN(C)C)=CC=1)/C1=CC=CC=C1 NKANXQFJJICGDU-QPLCGJKRSA-N 0.000 claims description 8
- SHGAZHPCJJPHSC-YCNIQYBTSA-N all-trans-retinoic acid Chemical compound OC(=O)\C=C(/C)\C=C\C=C(/C)\C=C\C1=C(C)CCCC1(C)C SHGAZHPCJJPHSC-YCNIQYBTSA-N 0.000 claims description 8
- 125000004429 atom Chemical group 0.000 claims description 8
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- VVIAGPKUTFNRDU-ABLWVSNPSA-N folinic acid Chemical compound C1NC=2NC(N)=NC(=O)C=2N(C=O)C1CNC1=CC=C(C(=O)N[C@@H](CCC(O)=O)C(O)=O)C=C1 VVIAGPKUTFNRDU-ABLWVSNPSA-N 0.000 claims description 8
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- NRUKOCRGYNPUPR-QBPJDGROSA-N teniposide Chemical compound COC1=C(O)C(OC)=CC([C@@H]2C3=CC=4OCOC=4C=C3[C@@H](O[C@H]3[C@@H]([C@@H](O)[C@@H]4O[C@@H](OC[C@H]4O3)C=3SC=CC=3)O)[C@@H]3[C@@H]2C(OC3)=O)=C1 NRUKOCRGYNPUPR-QBPJDGROSA-N 0.000 claims description 8
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- SGDBTWWWUNNDEQ-LBPRGKRZSA-N melphalan Chemical compound OC(=O)[C@@H](N)CC1=CC=C(N(CCCl)CCCl)C=C1 SGDBTWWWUNNDEQ-LBPRGKRZSA-N 0.000 claims description 7
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- NWIBSHFKIJFRCO-WUDYKRTCSA-N Mytomycin Chemical compound C1N2C(C(C(C)=C(N)C3=O)=O)=C3[C@@H](COC(N)=O)[C@@]2(OC)[C@@H]2[C@H]1N2 NWIBSHFKIJFRCO-WUDYKRTCSA-N 0.000 claims description 6
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- UODXSCCNACAPCE-UHFFFAOYSA-N draft:flumetramide Chemical compound C1=CC(C(F)(F)F)=CC=C1C1OCC(=O)NC1 UODXSCCNACAPCE-UHFFFAOYSA-N 0.000 claims description 6
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Landscapes
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Applications Claiming Priority (9)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US35325202P | 2002-02-01 | 2002-02-01 | |
| US60/353,252 | 2002-02-01 | ||
| US42692802P | 2002-11-15 | 2002-11-15 | |
| US60/426,928 | 2002-11-15 | ||
| US42838302P | 2002-11-22 | 2002-11-22 | |
| US60/428,383 | 2002-11-22 | ||
| US43393002P | 2002-12-17 | 2002-12-17 | |
| US60/433,930 | 2002-12-17 | ||
| PCT/US2003/003030 WO2003064383A2 (en) | 2002-02-01 | 2003-02-03 | Phosphorus-containing compounds & uses thereof |
Publications (2)
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| CA2472341A1 CA2472341A1 (en) | 2003-08-07 |
| CA2472341C true CA2472341C (en) | 2011-06-21 |
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| CA2472341A Expired - Fee Related CA2472341C (en) | 2002-02-01 | 2003-02-03 | Phosphorus-containing compounds & uses thereof |
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| US20040073294A1 (en) | 2002-09-20 | 2004-04-15 | Conor Medsystems, Inc. | Method and apparatus for loading a beneficial agent into an expandable medical device |
| US7432277B2 (en) | 2002-02-01 | 2008-10-07 | Araid Gene Therapeutics, Inc. | Phosphorus-containing macrocycles |
| AU2003210787B2 (en) | 2002-02-01 | 2009-04-23 | Medinol Ltd. | Phosphorus-containing compounds & uses thereof |
| AU2003231766A1 (en) | 2002-04-26 | 2003-11-10 | Gilead Sciences, Inc. | Non nucleoside reverse transcriptase inhibitors |
| DE60315723T2 (de) * | 2002-07-16 | 2008-06-19 | Biotica Technology Ltd. | Herstellung von Polyketiden und anderen natürlichen Produkten |
| US8980870B2 (en) * | 2002-09-24 | 2015-03-17 | Boehringer Ingelheim International Gmbh | Solid telmisartan pharmaceutical formulations |
| US20040202789A1 (en) * | 2003-03-31 | 2004-10-14 | Council Of Scientific And Industrila Research | Process for preparing thin film solids |
| ATE490788T1 (de) | 2003-04-25 | 2010-12-15 | Gilead Sciences Inc | Antivirale phosphonate analoge |
| KR20060022647A (ko) | 2003-04-25 | 2006-03-10 | 길리애드 사이언시즈, 인코포레이티드 | 키나아제 억제 포스포네이트 유사체 |
| WO2005002626A2 (en) | 2003-04-25 | 2005-01-13 | Gilead Sciences, Inc. | Therapeutic phosphonate compounds |
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| WO2004096285A2 (en) | 2003-04-25 | 2004-11-11 | Gilead Sciences, Inc. | Anti-infective phosphonate conjugates |
| WO2005047898A2 (en) | 2003-10-24 | 2005-05-26 | Gilead Sciences, Inc. | Methods and compositions for identifying therapeutic compounds |
| US7427636B2 (en) | 2003-04-25 | 2008-09-23 | Gilead Sciences, Inc. | Inosine monophosphate dehydrogenase inhibitory phosphonate compounds |
| NZ542343A (en) * | 2003-04-25 | 2009-03-31 | Gilead Sciences Inc | Immunomodulator phosphonate conjugates |
| US7407965B2 (en) | 2003-04-25 | 2008-08-05 | Gilead Sciences, Inc. | Phosphonate analogs for treating metabolic diseases |
| US7452901B2 (en) | 2003-04-25 | 2008-11-18 | Gilead Sciences, Inc. | Anti-cancer phosphonate analogs |
| US7470724B2 (en) | 2003-04-25 | 2008-12-30 | Gilead Sciences, Inc. | Phosphonate compounds having immuno-modulatory activity |
| CA2531454C (en) * | 2003-07-08 | 2011-10-25 | Novartis Ag | Use of rapamycin and rapamycin derivatives for the treatment of bone loss |
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| US20050049693A1 (en) * | 2003-08-25 | 2005-03-03 | Medtronic Vascular Inc. | Medical devices and compositions for delivering biophosphonates to anatomical sites at risk for vascular disease |
| WO2005044279A1 (en) | 2003-10-24 | 2005-05-19 | Gilead Sciences, Inc. | Purine nucleoside phosphonate conjugates |
| US7432273B2 (en) | 2003-10-24 | 2008-10-07 | Gilead Sciences, Inc. | Phosphonate analogs of antimetabolites |
| WO2005049021A1 (en) * | 2003-11-03 | 2005-06-02 | Oy Helsinki Transplantation R & D Ltd | Materials and methods for inhibiting neointimal hyperplasia |
| AR046194A1 (es) | 2003-11-04 | 2005-11-30 | Mayo Foundation | Metodo de tratamiento del linfoma de celulas del manto |
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| US7294123B2 (en) * | 2003-12-17 | 2007-11-13 | Corris Neurovascular, Inc. | Activatable bioactive vascular occlusive device and method of use |
| US20050137568A1 (en) * | 2003-12-17 | 2005-06-23 | Jones Donald K. | Activatable bioactive implantable medical device and method of use |
| EP1557182B1 (en) * | 2003-12-17 | 2010-07-21 | Codman & Shurtleff | Activatable bioactive implantable medical device |
| JP2007515495A (ja) | 2003-12-22 | 2007-06-14 | ギリアード サイエンシーズ， インコーポレイテッド | ４’−置換カルボビル誘導体およびアバカビル誘導体ならびにｈｉｖおよびｈｃｖ抗ウイルス活性を有する関連化合物 |
| US20050187608A1 (en) * | 2004-02-24 | 2005-08-25 | O'hara Michael D. | Radioprotective compound coating for medical devices |
| US7247159B2 (en) | 2004-04-08 | 2007-07-24 | Cordis Neurovascular, Inc. | Activatable bioactive vascular occlusive device |
| BRPI0511262A (pt) * | 2004-05-17 | 2007-11-27 | Novartis Ag | combinação de compostos orgánicos |
| EP1750862B1 (en) | 2004-06-04 | 2011-01-05 | Teva Pharmaceutical Industries Ltd. | Pharmaceutical composition containing irbesartan |
| DE602005027466D1 (de) | 2004-07-27 | 2011-05-26 | Gilead Sciences Inc | Nukleosid phosphonat konjugate als anti hiv mittel |
| US8075904B2 (en) * | 2004-08-11 | 2011-12-13 | California Institute Of Technology | High aspect ratio template and method for producing same for central and peripheral nerve repair |
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| US8367099B2 (en) | 2004-09-28 | 2013-02-05 | Atrium Medical Corporation | Perforated fatty acid films |
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| US9592324B2 (en) | 2006-11-06 | 2017-03-14 | Atrium Medical Corporation | Tissue separating device with reinforced support for anchoring mechanisms |
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| US9000040B2 (en) | 2004-09-28 | 2015-04-07 | Atrium Medical Corporation | Cross-linked fatty acid-based biomaterials |
| US9801982B2 (en) | 2004-09-28 | 2017-10-31 | Atrium Medical Corporation | Implantable barrier device |
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| US20070071754A1 (en) * | 2005-09-26 | 2007-03-29 | Peyman Gholam A | Method to ameliorate inflammation |
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| CN102861332A (zh) | 2005-10-26 | 2013-01-09 | 诺瓦提斯公司 | IL-1β化合物的新用途 |
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