IL113179A - Rapamcin hydroxyesters and pharmaceuticals containing them - Google Patents

Rapamcin hydroxyesters and pharmaceuticals containing them

Info

Publication number: IL113179A
Authority: IL; Israel
Prior art keywords: carbon atoms; alkyl; hydrogen; cr3r4; for10
Prior art date: 1994-04-18

Application number

IL113179A

Other languages

English (en)

Hebrew (he)

Other versions

IL113179A0 (en

Original Assignee

American Home Prod

Priority date (The priority date 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 date listed.)

1994-04-18

Filing date

1995-03-29

Publication date

1998-06-15

Family has litigation

First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=22860462&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=IL113179(A) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.

1995-03-29 Application filed by American Home Prod filed Critical American Home Prod

1995-06-29 Publication of IL113179A0 publication Critical patent/IL113179A0/xx

1998-06-15 Publication of IL113179A publication Critical patent/IL113179A/en

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
125000006241 alcohol protecting group Chemical group 0.000 description 3
210000004027 cell Anatomy 0.000 description 3
239000006071 cream Substances 0.000 description 3
201000010099 disease Diseases 0.000 description 3
208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 3
239000002552 dosage form Substances 0.000 description 3
229940079593 drug Drugs 0.000 description 3
239000003814 drug Substances 0.000 description 3
230000000694 effects Effects 0.000 description 3
239000006260 foam Substances 0.000 description 3
210000002683 foot Anatomy 0.000 description 3
210000002216 heart Anatomy 0.000 description 3
210000000548 hind-foot Anatomy 0.000 description 3
239000003018 immunosuppressive agent Substances 0.000 description 3
229940125721 immunosuppressive agent Drugs 0.000 description 3
230000001404 mediated effect Effects 0.000 description 3
238000007911 parenteral administration Methods 0.000 description 3
239000000725 suspension Substances 0.000 description 3
238000005160 1H NMR spectroscopy Methods 0.000 description 2
208000023275 Autoimmune disease Diseases 0.000 description 2
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
206010062016 Immunosuppression Diseases 0.000 description 2
OKKJLVBELUTLKV-UHFFFAOYSA-N Methanol Chemical compound OC OKKJLVBELUTLKV-UHFFFAOYSA-N 0.000 description 2
206010028980 Neoplasm Diseases 0.000 description 2
DNIAPMSPPWPWGF-UHFFFAOYSA-N Propylene glycol Chemical compound CC(O)CO DNIAPMSPPWPWGF-UHFFFAOYSA-N 0.000 description 2
VYPSYNLAJGMNEJ-UHFFFAOYSA-N Silicium dioxide Chemical compound O=[Si]=O VYPSYNLAJGMNEJ-UHFFFAOYSA-N 0.000 description 2
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
150000001298 alcohols Chemical class 0.000 description 2
230000000259 anti-tumor effect Effects 0.000 description 2
239000008346 aqueous phase Substances 0.000 description 2
210000004369 blood Anatomy 0.000 description 2
239000008280 blood Substances 0.000 description 2
239000002775 capsule Substances 0.000 description 2
150000001718 carbodiimides Chemical class 0.000 description 2
150000001721 carbon Chemical group 0.000 description 2
239000001768 carboxy methyl cellulose Substances 0.000 description 2
239000001913 cellulose Substances 0.000 description 2
229920002678 cellulose Polymers 0.000 description 2
235000010980 cellulose Nutrition 0.000 description 2
238000006243 chemical reaction Methods 0.000 description 2
239000003153 chemical reaction reagent Substances 0.000 description 2
238000007906 compression Methods 0.000 description 2
230000006835 compression Effects 0.000 description 2
230000008878 coupling Effects 0.000 description 2
238000010168 coupling process Methods 0.000 description 2
238000005859 coupling reaction Methods 0.000 description 2
238000010511 deprotection reaction Methods 0.000 description 2
238000010828 elution Methods 0.000 description 2
239000000839 emulsion Substances 0.000 description 2
RTZKZFJDLAIYFH-UHFFFAOYSA-N ether Substances CCOCC RTZKZFJDLAIYFH-UHFFFAOYSA-N 0.000 description 2
239000000796 flavoring agent Substances 0.000 description 2
235000013355 food flavoring agent Nutrition 0.000 description 2
238000009472 formulation Methods 0.000 description 2
230000003463 hyperproliferative effect Effects 0.000 description 2
230000004957 immunoregulator effect Effects 0.000 description 2
230000001939 inductive effect Effects 0.000 description 2
210000004072 lung Anatomy 0.000 description 2
HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 description 2
238000004519 manufacturing process Methods 0.000 description 2
VNWKTOKETHGBQD-UHFFFAOYSA-N methane Natural products C VNWKTOKETHGBQD-UHFFFAOYSA-N 0.000 description 2
201000006417 multiple sclerosis Diseases 0.000 description 2
239000002674 ointment Substances 0.000 description 2
239000003208 petroleum Substances 0.000 description 2
238000002360 preparation method Methods 0.000 description 2
230000035755 proliferation Effects 0.000 description 2
235000019260 propionic acid Nutrition 0.000 description 2
239000000741 silica gel Substances 0.000 description 2
229910002027 silica gel Inorganic materials 0.000 description 2
235000019812 sodium carboxymethyl cellulose Nutrition 0.000 description 2
229920001027 sodium carboxymethylcellulose Polymers 0.000 description 2
239000002904 solvent Substances 0.000 description 2
239000008174 sterile solution Substances 0.000 description 2
239000000126 substance Substances 0.000 description 2
239000000375 suspending agent Substances 0.000 description 2
229960001967 tacrolimus Drugs 0.000 description 2
QJJXYPPXXYFBGM-SHYZHZOCSA-N tacrolimus Natural products CO[C@H]1C[C@H](CC[C@@H]1O)C=C(C)[C@H]2OC(=O)[C@H]3CCCCN3C(=O)C(=O)[C@@]4(O)O[C@@H]([C@H](C[C@H]4C)OC)[C@@H](C[C@H](C)CC(=C[C@@H](CC=C)C(=O)C[C@H](O)[C@H]2C)C)OC QJJXYPPXXYFBGM-SHYZHZOCSA-N 0.000 description 2
125000001981 tert-butyldimethylsilyl group Chemical group [H]C([H])([H])[Si]([H])(C([H])([H])[H])[*]C(C([H])([H])[H])(C([H])([H])[H])C([H])([H])[H] 0.000 description 2
208000019553 vascular disease Diseases 0.000 description 2
CXUAEBDTJFKMBV-UHFFFAOYSA-N 1-(chloromethyl)-2,3,4,5,6-pentamethylbenzene Chemical compound CC1=C(C)C(C)=C(CCl)C(C)=C1C CXUAEBDTJFKMBV-UHFFFAOYSA-N 0.000 description 1
IQFYYKKMVGJFEH-OFKYTIFKSA-N 1-[(2r,4s,5r)-4-hydroxy-5-(tritiooxymethyl)oxolan-2-yl]-5-methylpyrimidine-2,4-dione Chemical compound C1[C@H](O)[C@@H](CO[3H])O[C@H]1N1C(=O)NC(=O)C(C)=C1 IQFYYKKMVGJFEH-OFKYTIFKSA-N 0.000 description 1
NHBKXEKEPDILRR-UHFFFAOYSA-N 2,3-bis(butanoylsulfanyl)propyl butanoate Chemical compound CCCC(=O)OCC(SC(=O)CCC)CSC(=O)CCC NHBKXEKEPDILRR-UHFFFAOYSA-N 0.000 description 1
VPRAWMKVWNGARF-UHFFFAOYSA-N 2-(oxan-2-yloxy)acetic acid 2,4,6-trichlorobenzoyl chloride Chemical compound ClC1=C(C(=O)Cl)C(=CC(=C1)Cl)Cl.O1C(CCCC1)OCC(=O)O VPRAWMKVWNGARF-UHFFFAOYSA-N 0.000 description 1
DEZIVPQYTVAGCL-UHFFFAOYSA-N 2-hydroxyacetic acid;4-methylbenzenesulfonic acid Chemical compound OCC(O)=O.CC1=CC=C(S(O)(=O)=O)C=C1 DEZIVPQYTVAGCL-UHFFFAOYSA-N 0.000 description 1
OJRKHUFDRUZMHQ-UHFFFAOYSA-N 3-hydroxy-2,2-dimethylpropanoic acid;4-methylbenzenesulfonic acid Chemical compound OCC(C)(C)C(O)=O.CC1=CC=C(S(O)(=O)=O)C=C1 OJRKHUFDRUZMHQ-UHFFFAOYSA-N 0.000 description 1
HIQIXEFWDLTDED-UHFFFAOYSA-N 4-hydroxy-1-piperidin-4-ylpyrrolidin-2-one Chemical compound O=C1CC(O)CN1C1CCNCC1 HIQIXEFWDLTDED-UHFFFAOYSA-N 0.000 description 1
206010001052 Acute respiratory distress syndrome Diseases 0.000 description 1
GUBGYTABKSRVRQ-XLOQQCSPSA-N Alpha-Lactose Chemical compound O[C@@H]1[C@@H](O)[C@@H](O)[C@@H](CO)O[C@H]1O[C@@H]1[C@@H](CO)O[C@H](O)[C@H](O)[C@H]1O GUBGYTABKSRVRQ-XLOQQCSPSA-N 0.000 description 1
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238000011725 BALB/c mouse Methods 0.000 description 1
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VEXZGXHMUGYJMC-UHFFFAOYSA-M Chloride anion Chemical compound [Cl-] VEXZGXHMUGYJMC-UHFFFAOYSA-M 0.000 description 1
208000006545 Chronic Obstructive Pulmonary Disease Diseases 0.000 description 1
CMSMOCZEIVJLDB-UHFFFAOYSA-N Cyclophosphamide Chemical compound ClCCN(CCCl)P1(=O)NCCCO1 CMSMOCZEIVJLDB-UHFFFAOYSA-N 0.000 description 1
229920001353 Dextrin Polymers 0.000 description 1
239000004375 Dextrin Substances 0.000 description 1
LVGKNOAMLMIIKO-UHFFFAOYSA-N Elaidinsaeure-aethylester Natural products CCCCCCCCC=CCCCCCCCC(=O)OCC LVGKNOAMLMIIKO-UHFFFAOYSA-N 0.000 description 1
206010014561 Emphysema Diseases 0.000 description 1
108010010803 Gelatin Proteins 0.000 description 1
DGAQECJNVWCQMB-PUAWFVPOSA-M Ilexoside XXIX Chemical compound C[C@@H]1CC[C@@]2(CC[C@@]3(C(=CC[C@H]4[C@]3(CC[C@@H]5[C@@]4(CC[C@@H](C5(C)C)OS(=O)(=O)[O-])C)C)[C@@H]2[C@]1(C)O)C)C(=O)O[C@H]6[C@@H]([C@H]([C@@H]([C@H](O6)CO)O)O)O.[Na+] DGAQECJNVWCQMB-PUAWFVPOSA-M 0.000 description 1
208000022559 Inflammatory bowel disease Diseases 0.000 description 1
GUBGYTABKSRVRQ-QKKXKWKRSA-N Lactose Natural products OC[C@H]1O[C@@H](O[C@H]2[C@H](O)[C@@H](O)C(O)O[C@@H]2CO)[C@H](O)[C@@H](O)[C@H]1O GUBGYTABKSRVRQ-QKKXKWKRSA-N 0.000 description 1
FQISKWAFAHGMGT-SGJOWKDISA-M Methylprednisolone sodium succinate Chemical compound [Na+].C([C@@]12C)=CC(=O)C=C1[C@@H](C)C[C@@H]1[C@@H]2[C@@H](O)C[C@]2(C)[C@@](O)(C(=O)COC(=O)CCC([O-])=O)CC[C@H]21 FQISKWAFAHGMGT-SGJOWKDISA-M 0.000 description 1
229920001273 Polyhydroxy acid Polymers 0.000 description 1
ZLMJMSJWJFRBEC-UHFFFAOYSA-N Potassium Chemical compound [K] ZLMJMSJWJFRBEC-UHFFFAOYSA-N 0.000 description 1
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206010039509 Scab Diseases 0.000 description 1
206010039792 Seborrhoea Diseases 0.000 description 1
UIIMBOGNXHQVGW-UHFFFAOYSA-M Sodium bicarbonate Chemical class [Na+].OC([O-])=O UIIMBOGNXHQVGW-UHFFFAOYSA-M 0.000 description 1
229920002472 Starch Polymers 0.000 description 1
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210000001744 T-lymphocyte Anatomy 0.000 description 1
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Classifications

- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
- C07D498/18—Bridged systems
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/04—Antibacterial agents
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/10—Antimycotics
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- 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
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- 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

Landscapes

Health & Medical Sciences (AREA)
Chemical & Material Sciences (AREA)
Organic Chemistry (AREA)
Veterinary Medicine (AREA)
Life Sciences & Earth Sciences (AREA)
Public Health (AREA)
Chemical Kinetics & Catalysis (AREA)
General Chemical & Material Sciences (AREA)
Medicinal Chemistry (AREA)
Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
General Health & Medical Sciences (AREA)
Pharmacology & Pharmacy (AREA)
Animal Behavior & Ethology (AREA)
Bioinformatics & Cheminformatics (AREA)
Engineering & Computer Science (AREA)
Immunology (AREA)
Oncology (AREA)
Communicable Diseases (AREA)
Cardiology (AREA)
Heart & Thoracic Surgery (AREA)
Rheumatology (AREA)
Urology & Nephrology (AREA)
Transplantation (AREA)
Pain & Pain Management (AREA)
Vascular Medicine (AREA)
Pulmonology (AREA)
Orthopedic Medicine & Surgery (AREA)
Physical Education & Sports Medicine (AREA)
Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
Domestic Plumbing Installations (AREA)

IL113179A 1994-04-18 1995-03-29 Rapamcin hydroxyesters and pharmaceuticals containing them IL113179A (en)

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
US (2)	US5362718A (fr)
EP (3)	EP1266899B1 (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)	DE69529897T3 (fr)
DK (2)	DK0763039T3 (fr)
ES (3)	ES2277975T3 (fr)
FR (1)	FR08C0018I2 (fr)
HK (1)	HK1048816B (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)	PT763039E (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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TWI233359B (en) *	2001-04-06	2005-06-01	Wyeth Corp	Pharmaceutical composition for treating neoplasm
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US5177203A (en) *	1992-03-05	1993-01-05	American Home Products Corporation	Rapamycin 42-sulfonates and 42-(N-carboalkoxy) sulfamates useful as immunosuppressive agents
US5302584A (en) *	1992-10-13	1994-04-12	American Home Products Corporation	Carbamates of rapamycin
US5262423A (en) *	1992-10-29	1993-11-16	American Home Products Corporation	Rapamycin arylcarbonyl and alkoxycarbonyl carbamates as immunosuppressive and antifungal agents
US5260300A (en) *	1992-11-19	1993-11-09	American Home Products Corporation	Rapamycin carbonate esters as immuno-suppressant agents
US5385908A (en) *	1993-11-22	1995-01-31	American Home Products Corporation	Hindered esters of rapamycin
TWI286074B (en)	2000-11-15	2007-09-01	Wyeth Corp	Pharmaceutical composition containing CCI-779 as an antineoplastic agent

1994
- 1994-04-18 US US08/229,261 patent/US5362718A/en not_active Ceased
- 1994-11-08 TW TW083110308A patent/TW275631B/zh not_active IP Right Cessation
1995
- 1995-03-29 IL IL113179A patent/IL113179A/en not_active IP Right Cessation
- 1995-04-13 ZA ZA953090A patent/ZA953090B/xx unknown
- 1995-04-14 EP EP02014322A patent/EP1266899B1/fr not_active Expired - Lifetime
- 1995-04-14 ES ES02014322T patent/ES2277975T3/es not_active Expired - Lifetime
- 1995-04-14 RU RU96122172A patent/RU2134267C1/ru active
- 1995-04-14 EP EP06026307A patent/EP1760083B1/fr not_active Expired - Lifetime
- 1995-04-14 KR KR1019960705839A patent/KR100330800B1/ko not_active Expired - Lifetime
- 1995-04-14 CZ CZ963052A patent/CZ284567B6/cs not_active IP Right Cessation
- 1995-04-14 PT PT95915671T patent/PT763039E/pt unknown
- 1995-04-14 DE DE69529897.6T patent/DE69529897T3/de not_active Expired - Lifetime
- 1995-04-14 BR BR9507323A patent/BR9507323A/pt active IP Right Grant
- 1995-04-14 DK DK95915671T patent/DK0763039T3/da active
- 1995-04-14 SI SI9530648T patent/SI0763039T1/xx unknown
- 1995-04-14 AT AT02014322T patent/ATE350384T1/de active
- 1995-04-14 SK SK1330-96A patent/SK281787B6/sk not_active IP Right Cessation
- 1995-04-14 PT PT02014322T patent/PT1266899E/pt unknown
- 1995-04-14 DK DK02014322T patent/DK1266899T3/da active
- 1995-04-14 MX MX9604694A patent/MX9604694A/es unknown
- 1995-04-14 WO PCT/US1995/004603 patent/WO1995028406A1/fr not_active Ceased
- 1995-04-14 CN CN95193325A patent/CN1059905C/zh not_active Expired - Lifetime
- 1995-04-14 AT AT95915671T patent/ATE234307T1/de active
- 1995-04-14 AT AT06026307T patent/ATE537176T1/de active
- 1995-04-14 DE DE122008000023C patent/DE122008000023I1/de active Pending
- 1995-04-14 SI SI9530730T patent/SI1266899T1/sl unknown
- 1995-04-14 JP JP52710595A patent/JP3725901B2/ja not_active Expired - Lifetime
- 1995-04-14 DE DE69535363T patent/DE69535363T2/de not_active Expired - Lifetime
- 1995-04-14 PL PL95316948A patent/PL183178B1/pl unknown
- 1995-04-14 ES ES95915671.2T patent/ES2191704T7/es active Active
- 1995-04-14 EP EP95915671.2A patent/EP0763039B3/fr not_active Expired - Lifetime
- 1995-04-14 ES ES06026307T patent/ES2375730T3/es not_active Expired - Lifetime
- 1995-04-14 NZ NZ283988A patent/NZ283988A/en not_active IP Right Cessation
- 1995-04-14 HU HU9602893A patent/HU225915B1/hu active Protection Beyond IP Right Term
- 1995-04-14 CA CA002187024A patent/CA2187024C/fr not_active Expired - Lifetime
1998
- 1998-11-24 HK HK03101048.7A patent/HK1048816B/en not_active IP Right Cessation
2003
- 2003-05-13 LV LVP-03-47A patent/LV13038B/en unknown
- 2003-09-12 CY CY0300065A patent/CY2378B1/xx unknown
2008
- 2008-05-15 NL NL300348C patent/NL300348I2/nl unknown
- 2008-05-15 LU LU91438C patent/LU91438I2/fr unknown
- 2008-05-16 FR FR08C0018C patent/FR08C0018I2/fr active Active
- 2008-05-19 CY CY200800012C patent/CY2008012I2/el unknown
2013
- 2013-06-28 US US13/931,400 patent/USRE44768E1/en not_active Expired - Lifetime

Also Published As

Publication number	Publication date
CY2008012I1 (el)	2009-11-04
ATE234307T1 (de)	2003-03-15
EP0763039B3 (fr)	2017-04-05
US5362718A (en)	1994-11-08
PT1266899E (pt)	2007-02-28
CA2187024A1 (fr)	1995-10-26
HK1048816B (en)	2007-04-04
AU2247495A (en)	1995-11-10
HUT77410A (hu)	1998-04-28
CN1149296A (zh)	1997-05-07
CY2378B1 (en)	2004-06-04
DE69535363D1 (de)	2007-02-15
HU225915B1 (en)	2007-12-28
PL316948A1 (en)	1997-02-17
EP0763039A1 (fr)	1997-03-19
IL113179A0 (en)	1995-06-29
HU9602893D0 (en)	1996-12-30
DK0763039T3 (da)	2003-05-05
WO1995028406A1 (fr)	1995-10-26
EP1266899A2 (fr)	2002-12-18
ES2191704T7 (es)	2017-07-10
PL183178B1 (pl)	2002-05-31
JPH09512018A (ja)	1997-12-02
EP1266899B1 (fr)	2007-01-03
DE69529897T3 (de)	2017-08-17
LV13038B (en)	2003-10-20
CZ284567B6 (cs)	1999-01-13
ZA953090B (en)	1996-10-14
PT763039E (pt)	2003-06-30
ATE350384T1 (de)	2007-01-15
SI0763039T1 (en)	2003-08-31
CA2187024C (fr)	2004-08-10
NZ283988A (en)	1998-07-28
BR9507323A (pt)	1997-09-30
EP1760083A1 (fr)	2007-03-07
NL300348I1 (nl)	2008-07-01
CN1059905C (zh)	2000-12-27
EP1266899A3 (fr)	2003-05-28
DK1266899T3 (da)	2007-01-29
RU2134267C1 (ru)	1999-08-10
DE69535363T2 (de)	2007-04-19
MX9604694A (es)	1998-01-31
EP1760083B1 (fr)	2011-12-14
KR100330800B1 (ko)	2002-11-20
DE122008000023I1 (de)	2008-08-14
JP3725901B2 (ja)	2005-12-14
DE69529897D1 (de)	2003-04-17
USRE44768E1 (en)	2014-02-18
CZ305296A3 (en)	1997-08-13
FR08C0018I1 (fr)	2008-07-18
KR970702283A (ko)	1997-05-13
SK281787B6 (sk)	2001-07-10
ATE537176T1 (de)	2011-12-15
EP0763039B1 (fr)	2003-03-12
ES2375730T3 (es)	2012-03-05
DE69529897T2 (de)	2003-11-06
ES2191704T3 (es)	2003-09-16
SI1266899T1 (sl)	2007-04-30
TW275631B (fr)	1996-05-11
ES2277975T3 (es)	2007-08-01
HK1011352A1 (en)	1999-07-09
NL300348I2 (nl)	2008-09-01
CY2008012I2 (el)	2009-11-04
FR08C0018I2 (fr)	2009-10-30
HK1048816A1 (en)	2003-04-17
LU91438I2 (fr)	2008-07-15
SK133096A3 (en)	1997-04-09
AU679854B2 (en)	1997-07-10

Legal Events

Date	Code	Title
1998-11-26	FF	Patent granted
1999-04-11	KB	Patent renewed
2001-07-24	KB	Patent renewed
2005-05-17	KB	Patent renewed
2009-09-15	KB	Patent renewed
2013-04-30	KB	Patent renewed
2015-11-30	EXP	Patent expired

Publication	Publication Date	Title
EP1266899B1 (fr)	2007-01-03	Hydroxyesters de rapamycine, leur procédé de préparation et préparations pharmaceutiques les contenant
US5559122A (en)	1996-09-24	Hindered N-oxide esters of rapamycin
EP0730597B1 (fr)	2001-03-07	Esters heterocycliques de rapamycine et compositions pharmaceutiques les contenant
EP0796260B1 (fr)	2001-06-20	Hydroxylamines et 42-oximes de rapamycine
MXPA96004694A (en)	1998-01-01	Hydroxysteres of rapamycin, process for supreparation and pharmaceutical compositions that loscontie
US5385910A (en)	1995-01-31	Gem-distributed esters of rapamycin
EP0655065B1 (fr)	1996-12-11	27-hydroxyrapamycine et ses derives
AU679854C (en)	1998-04-09	Rapamycin hydroxyesters, process for their preparation and pharmaceutical compositions containing them
HK1011352B (en)	2003-06-13	42-rapamycin hydroxyester, process for its preparation and pharmaceutical compositions containing it
HK1002281B (en)	2001-11-02	Hindered n-oxide esters of rapamycin and their use as medicaments
HK1011354B (en)	2001-06-22	Heterocyclic esters of rapamycin and pharmaceutical compositions containing them
HK1011355B (en)	2002-09-27	Amino alkanoic esters of rapamycin
HK1011355A1 (en)	1999-07-09	Amino alkanoic esters of rapamycin
HK1011030B (en)	2001-11-30	Rapamycin amidino carbamates and pharmaceutical compositions containing them
HK1011030A1 (en)	1999-07-02	Rapamycin amidino carbamates and pharmaceutical compositions containing them