IL113179A - Rapamcin hydroxyesters and pharmaceuticals containing them - Google Patents
Rapamcin hydroxyesters and pharmaceuticals containing themInfo
- Publication number
- IL113179A IL113179A IL113179A IL11317995A IL113179A IL 113179 A IL113179 A IL 113179A IL 113179 A IL113179 A IL 113179A IL 11317995 A IL11317995 A IL 11317995A IL 113179 A IL113179 A IL 113179A
- Authority
- IL
- Israel
- Prior art keywords
- carbon atoms
- alkyl
- hydrogen
- cr3r4
- for10
- Prior art date
Links
- 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 title claims description 69
- ZAHRKKWIAAJSAO-UHFFFAOYSA-N rapamycin Natural products COCC(O)C(=C/C(C)C(=O)CC(OC(=O)C1CCCCN1C(=O)C(=O)C2(O)OC(CC(OC)C(=CC=CC=CC(C)CC(C)C(=O)C)C)CCC2C)C(C)CC3CCC(O)C(C3)OC)C ZAHRKKWIAAJSAO-UHFFFAOYSA-N 0.000 title claims description 65
- 229960002930 sirolimus Drugs 0.000 title claims description 65
- 239000008194 pharmaceutical composition Substances 0.000 title claims description 5
- 150000001875 compounds Chemical class 0.000 claims abstract description 96
- 229910052739 hydrogen Inorganic materials 0.000 claims abstract description 95
- 239000001257 hydrogen Substances 0.000 claims abstract description 79
- 125000000217 alkyl group Chemical group 0.000 claims abstract description 70
- 150000002431 hydrogen Chemical class 0.000 claims abstract description 59
- 125000003342 alkenyl group Chemical group 0.000 claims abstract description 56
- 125000000304 alkynyl group Chemical group 0.000 claims abstract description 56
- 125000000753 cycloalkyl group Chemical group 0.000 claims abstract description 44
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims abstract description 33
- 125000000532 dioxanyl group Chemical group 0.000 claims abstract description 32
- 150000003839 salts Chemical class 0.000 claims abstract description 27
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims abstract description 18
- 125000004276 dioxalanyl group Chemical group 0.000 claims abstract description 15
- 125000004849 alkoxymethyl group Chemical group 0.000 claims abstract description 10
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims abstract description 10
- 125000002603 chloroethyl group Chemical group [H]C([*])([H])C([H])([H])Cl 0.000 claims abstract description 10
- 125000001181 organosilyl group Chemical group [SiH3]* 0.000 claims abstract description 10
- 125000001412 tetrahydropyranyl group Chemical group 0.000 claims abstract description 10
- 125000002221 trityl group Chemical group [H]C1=C([H])C([H])=C([H])C([H])=C1C([*])(C1=C(C(=C(C(=C1[H])[H])[H])[H])[H])C1=C([H])C([H])=C([H])C([H])=C1[H] 0.000 claims abstract description 10
- 125000003884 phenylalkyl group Chemical group 0.000 claims abstract description 9
- 125000005346 substituted cycloalkyl group Chemical group 0.000 claims abstract description 9
- 230000000843 anti-fungal effect Effects 0.000 claims abstract description 5
- 230000001028 anti-proliverative effect Effects 0.000 claims abstract description 4
- 229940121375 antifungal agent Drugs 0.000 claims abstract description 4
- 230000003110 anti-inflammatory effect Effects 0.000 claims abstract description 3
- 125000004432 carbon atom Chemical group C* 0.000 claims description 263
- -1 -(CR3R4)fOR10 Chemical group 0.000 claims description 26
- 238000000034 method Methods 0.000 claims description 19
- 229910052799 carbon Inorganic materials 0.000 claims description 18
- 239000002253 acid Substances 0.000 claims description 9
- 241000124008 Mammalia Species 0.000 claims description 7
- 206010039073 rheumatoid arthritis Diseases 0.000 claims description 6
- 238000002054 transplantation Methods 0.000 claims description 5
- AEMRFAOFKBGASW-UHFFFAOYSA-N Glycolic acid Chemical compound OCC(O)=O AEMRFAOFKBGASW-UHFFFAOYSA-N 0.000 claims description 4
- RBNPOMFGQQGHHO-UHFFFAOYSA-N glyceric acid Chemical compound OCC(O)C(O)=O RBNPOMFGQQGHHO-UHFFFAOYSA-N 0.000 claims description 4
- 208000037803 restenosis Diseases 0.000 claims description 4
- 206010017533 Fungal infection Diseases 0.000 claims description 3
- 208000031888 Mycoses Diseases 0.000 claims description 3
- 206010035664 Pneumonia Diseases 0.000 claims description 3
- 239000003937 drug carrier Substances 0.000 claims description 3
- PTBDIHRZYDMNKB-UHFFFAOYSA-N 2,2-Bis(hydroxymethyl)propionic acid Chemical compound OCC(C)(CO)C(O)=O PTBDIHRZYDMNKB-UHFFFAOYSA-N 0.000 claims description 2
- 229960004275 glycolic acid Drugs 0.000 claims description 2
- 208000024908 graft versus host disease Diseases 0.000 claims description 2
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims description 2
- 125000004429 atom Chemical group 0.000 claims 2
- 125000005587 carbonate group Chemical group 0.000 claims 2
- JGOQLTUMDGDSPK-UHFFFAOYSA-N 2,2-dimethyl-3-(oxan-2-yloxy)propanoic acid Chemical compound OC(=O)C(C)(C)COC1CCCCO1 JGOQLTUMDGDSPK-UHFFFAOYSA-N 0.000 claims 1
- JWBQDXPJNGBSDC-UHFFFAOYSA-N 2-(oxan-2-yloxy)acetic acid Chemical compound OC(=O)COC1CCCCO1 JWBQDXPJNGBSDC-UHFFFAOYSA-N 0.000 claims 1
- RDFQSFOGKVZWKF-UHFFFAOYSA-N 3-hydroxy-2,2-dimethylpropanoic acid Chemical compound OCC(C)(C)C(O)=O RDFQSFOGKVZWKF-UHFFFAOYSA-N 0.000 claims 1
- ULMZOZMSDIOZAF-UHFFFAOYSA-N 3-hydroxy-2-(hydroxymethyl)propanoic acid Chemical compound OCC(CO)C(O)=O ULMZOZMSDIOZAF-UHFFFAOYSA-N 0.000 claims 1
- 230000001506 immunosuppresive effect Effects 0.000 abstract description 12
- 239000002246 antineoplastic agent Substances 0.000 abstract description 2
- IAZDPXIOMUYVGZ-UHFFFAOYSA-N Dimethylsulphoxide Chemical compound CS(C)=O IAZDPXIOMUYVGZ-UHFFFAOYSA-N 0.000 description 81
- XEKOWRVHYACXOJ-UHFFFAOYSA-N Ethyl acetate Chemical compound CCOC(C)=O XEKOWRVHYACXOJ-UHFFFAOYSA-N 0.000 description 32
- 239000000203 mixture Substances 0.000 description 31
- 238000010998 test method Methods 0.000 description 29
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 description 26
- 239000012634 fragment Substances 0.000 description 24
- 239000000243 solution Substances 0.000 description 24
- 230000000144 pharmacologic effect Effects 0.000 description 23
- 239000007787 solid Substances 0.000 description 23
- UHOVQNZJYSORNB-UHFFFAOYSA-N Benzene Chemical compound C1=CC=CC=C1 UHOVQNZJYSORNB-UHFFFAOYSA-N 0.000 description 21
- ZMANZCXQSJIPKH-UHFFFAOYSA-N Triethylamine Chemical compound CCN(CC)CC ZMANZCXQSJIPKH-UHFFFAOYSA-N 0.000 description 21
- 238000005481 NMR spectroscopy Methods 0.000 description 17
- 235000019439 ethyl acetate Nutrition 0.000 description 16
- VHYFNPMBLIVWCW-UHFFFAOYSA-N 4-Dimethylaminopyridine Chemical compound CN(C)C1=CC=NC=C1 VHYFNPMBLIVWCW-UHFFFAOYSA-N 0.000 description 14
- 238000004992 fast atom bombardment mass spectroscopy Methods 0.000 description 14
- 229910052757 nitrogen Inorganic materials 0.000 description 13
- 238000003818 flash chromatography Methods 0.000 description 12
- 239000007788 liquid Substances 0.000 description 12
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 12
- 239000003795 chemical substances by application Substances 0.000 description 11
- 206010061218 Inflammation Diseases 0.000 description 10
- OAYLNYINCPYISS-UHFFFAOYSA-N ethyl acetate;hexane Chemical compound CCCCCC.CCOC(C)=O OAYLNYINCPYISS-UHFFFAOYSA-N 0.000 description 10
- 230000004054 inflammatory process Effects 0.000 description 10
- 239000002244 precipitate Substances 0.000 description 10
- 239000004480 active ingredient Substances 0.000 description 9
- 239000012267 brine Substances 0.000 description 9
- HPALAKNZSZLMCH-UHFFFAOYSA-M sodium;chloride;hydrate Chemical compound O.[Na+].[Cl-] HPALAKNZSZLMCH-UHFFFAOYSA-M 0.000 description 9
- 238000001644 13C nuclear magnetic resonance spectroscopy Methods 0.000 description 8
- 208000009386 Experimental Arthritis Diseases 0.000 description 8
- 230000008859 change Effects 0.000 description 8
- 229920006395 saturated elastomer Polymers 0.000 description 8
- 229960000549 4-dimethylaminophenol Drugs 0.000 description 7
- 239000000706 filtrate Substances 0.000 description 7
- 229910052943 magnesium sulfate Inorganic materials 0.000 description 7
- 239000000047 product Substances 0.000 description 7
- 230000004083 survival effect Effects 0.000 description 7
- 238000003828 vacuum filtration Methods 0.000 description 7
- 239000003921 oil Substances 0.000 description 6
- OZGSEIVTQLXWRO-UHFFFAOYSA-N 2,4,6-trichlorobenzoyl chloride Chemical compound ClC(=O)C1=C(Cl)C=C(Cl)C=C1Cl OZGSEIVTQLXWRO-UHFFFAOYSA-N 0.000 description 5
- 150000008064 anhydrides Chemical class 0.000 description 5
- 235000019198 oils Nutrition 0.000 description 5
- 229910000030 sodium bicarbonate Inorganic materials 0.000 description 5
- 229930105110 Cyclosporin A Natural products 0.000 description 4
- PMATZTZNYRCHOR-CGLBZJNRSA-N Cyclosporin A Chemical compound CC[C@@H]1NC(=O)[C@H]([C@H](O)[C@H](C)C\C=C\C)N(C)C(=O)[C@H](C(C)C)N(C)C(=O)[C@H](CC(C)C)N(C)C(=O)[C@H](CC(C)C)N(C)C(=O)[C@@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)N(C)C(=O)[C@H](C(C)C)NC(=O)[C@H](CC(C)C)N(C)C(=O)CN(C)C1=O PMATZTZNYRCHOR-CGLBZJNRSA-N 0.000 description 4
- 108010036949 Cyclosporine Proteins 0.000 description 4
- 241000700159 Rattus Species 0.000 description 4
- 239000000969 carrier Substances 0.000 description 4
- 229960001265 ciclosporin Drugs 0.000 description 4
- XBDQKXXYIPTUBI-UHFFFAOYSA-N dimethylselenoniopropionate Natural products CCC(O)=O XBDQKXXYIPTUBI-UHFFFAOYSA-N 0.000 description 4
- 150000002148 esters Chemical class 0.000 description 4
- 125000002887 hydroxy group Chemical group [H]O* 0.000 description 4
- 238000000338 in vitro Methods 0.000 description 4
- 238000001727 in vivo Methods 0.000 description 4
- 230000005764 inhibitory process Effects 0.000 description 4
- 239000012074 organic phase Substances 0.000 description 4
- 239000000843 powder Substances 0.000 description 4
- 125000006239 protecting group Chemical group 0.000 description 4
- 238000000746 purification Methods 0.000 description 4
- QTBSBXVTEAMEQO-UHFFFAOYSA-N Acetic acid Chemical compound CC(O)=O QTBSBXVTEAMEQO-UHFFFAOYSA-N 0.000 description 3
- 208000016683 Adult T-cell leukemia/lymphoma Diseases 0.000 description 3
- FAPWRFPIFSIZLT-UHFFFAOYSA-M Sodium chloride Chemical class [Na+].[Cl-] FAPWRFPIFSIZLT-UHFFFAOYSA-M 0.000 description 3
- 238000005917 acylation reaction Methods 0.000 description 3
- 201000006966 adult T-cell leukemia Diseases 0.000 description 3
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- 239000006071 cream Substances 0.000 description 3
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- 238000005160 1H NMR spectroscopy Methods 0.000 description 2
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- FQQYOXPFBMYCPO-AURGRMCHSA-N 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](O)[C@H](O)/C(C)=C/[C@@H](C)C(=O)C1 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](O)[C@H](O)/C(C)=C/[C@@H](C)C(=O)C1 FQQYOXPFBMYCPO-AURGRMCHSA-N 0.000 description 2
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical group [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 description 2
- 201000004624 Dermatitis Diseases 0.000 description 2
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 description 2
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- DNIAPMSPPWPWGF-UHFFFAOYSA-N Propylene glycol Chemical compound CC(O)CO DNIAPMSPPWPWGF-UHFFFAOYSA-N 0.000 description 2
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- 230000006052 T cell proliferation Effects 0.000 description 2
- QJJXYPPXXYFBGM-LFZNUXCKSA-N Tacrolimus Chemical compound C1C[C@@H](O)[C@H](OC)C[C@@H]1\C=C(/C)[C@@H]1[C@H](C)[C@@H](O)CC(=O)[C@H](CC=C)/C=C(C)/C[C@H](C)C[C@H](OC)[C@H]([C@H](C[C@H]2C)OC)O[C@@]2(O)C(=O)C(=O)N2CCCC[C@H]2C(=O)O1 QJJXYPPXXYFBGM-LFZNUXCKSA-N 0.000 description 2
- 206010052779 Transplant rejections Diseases 0.000 description 2
- DPXJVFZANSGRMM-UHFFFAOYSA-N acetic acid;2,3,4,5,6-pentahydroxyhexanal;sodium Chemical compound [Na].CC(O)=O.OCC(O)C(O)C(O)C(O)C=O DPXJVFZANSGRMM-UHFFFAOYSA-N 0.000 description 2
- 230000010933 acylation Effects 0.000 description 2
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- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 description 2
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- A61P31/04—Antibacterial agents
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- A61P35/00—Antineoplastic agents
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
- A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US08/229,261 US5362718A (en) | 1994-04-18 | 1994-04-18 | Rapamycin hydroxyesters |
Publications (2)
Publication Number | Publication Date |
---|---|
IL113179A0 IL113179A0 (en) | 1995-06-29 |
IL113179A true IL113179A (en) | 1998-06-15 |
Family
ID=22860462
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
IL113179A IL113179A (en) | 1994-04-18 | 1995-03-29 | Rapamcin hydroxyesters and pharmaceuticals containing them |
Country Status (30)
Country | Link |
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US (2) | US5362718A (fr) |
EP (3) | EP1760083B1 (fr) |
JP (1) | JP3725901B2 (fr) |
KR (1) | KR100330800B1 (fr) |
CN (1) | CN1059905C (fr) |
AT (3) | ATE350384T1 (fr) |
BR (1) | BR9507323A (fr) |
CA (1) | CA2187024C (fr) |
CY (2) | CY2378B1 (fr) |
CZ (1) | CZ284567B6 (fr) |
DE (3) | DE69535363T2 (fr) |
DK (2) | DK1266899T3 (fr) |
ES (3) | ES2375730T3 (fr) |
FR (1) | FR08C0018I2 (fr) |
HK (2) | HK1011352A1 (fr) |
HU (1) | HU225915B1 (fr) |
IL (1) | IL113179A (fr) |
LU (1) | LU91438I2 (fr) |
LV (1) | LV13038B (fr) |
MX (1) | MX9604694A (fr) |
NL (1) | NL300348I2 (fr) |
NZ (1) | NZ283988A (fr) |
PL (1) | PL183178B1 (fr) |
PT (2) | PT1266899E (fr) |
RU (1) | RU2134267C1 (fr) |
SI (2) | SI0763039T1 (fr) |
SK (1) | SK281787B6 (fr) |
TW (1) | TW275631B (fr) |
WO (1) | WO1995028406A1 (fr) |
ZA (1) | ZA953090B (fr) |
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TWI256395B (en) * | 1999-09-29 | 2006-06-11 | Wyeth Corp | Regioselective synthesis of rapamycin derivatives |
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WO2002013802A2 (fr) | 2000-08-11 | 2002-02-21 | Wyeth | Procede de traitement d'un carcinome a recepteur d'oestrogene |
JP2004509898A (ja) | 2000-09-19 | 2004-04-02 | ワイス | 水溶性ラパマイシンエステル |
US6399625B1 (en) | 2000-09-27 | 2002-06-04 | Wyeth | 1-oxorapamycins |
US20070276473A1 (en) * | 2000-09-29 | 2007-11-29 | Llanos Gerard H | Medical Devices, Drug Coatings and Methods for Maintaining the Drug Coatings Thereon |
CA2424029C (fr) | 2000-09-29 | 2008-01-29 | Cordis Corporation | Dispositifs medicaux enrobes |
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US6399626B1 (en) * | 2000-10-02 | 2002-06-04 | Wyeth | Hydroxyesters of 7-desmethylrapamycin |
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TWI286074B (en) | 2000-11-15 | 2007-09-01 | Wyeth Corp | Pharmaceutical composition containing CCI-779 as an antineoplastic agent |
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1994
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1995
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