KR20070085465A - Ｓ１ｐ 수용체 효능제의 투여 용법 - Google Patents
Ｓ１ｐ 수용체 효능제의 투여 용법 Download PDFInfo
- Publication number
- KR20070085465A KR20070085465A KR1020077011969A KR20077011969A KR20070085465A KR 20070085465 A KR20070085465 A KR 20070085465A KR 1020077011969 A KR1020077011969 A KR 1020077011969A KR 20077011969 A KR20077011969 A KR 20077011969A KR 20070085465 A KR20070085465 A KR 20070085465A
- Authority
- KR
- South Korea
- Prior art keywords
- agonist
- alkyl
- receptor
- daily dose
- dose
- 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.)
- Ceased
Links
- 229940044601 receptor agonist Drugs 0.000 title claims abstract description 80
- 239000000018 receptor agonist Substances 0.000 title claims description 21
- 102000011011 Sphingosine 1-phosphate receptors Human genes 0.000 claims abstract description 112
- 108050001083 Sphingosine 1-phosphate receptors Proteins 0.000 claims abstract description 109
- 239000000556 agonist Substances 0.000 claims abstract description 82
- 229940075993 receptor modulator Drugs 0.000 claims abstract description 64
- 125000000217 alkyl group Chemical group 0.000 claims description 101
- 229910052736 halogen Inorganic materials 0.000 claims description 49
- KKGQTZUTZRNORY-UHFFFAOYSA-N fingolimod Chemical group CCCCCCCCC1=CC=C(CCC(N)(CO)CO)C=C1 KKGQTZUTZRNORY-UHFFFAOYSA-N 0.000 claims description 41
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 41
- 150000002367 halogens Chemical class 0.000 claims description 39
- -1 4-cyclohexyl-3-trifluoromethyl-benzyloxyimino Chemical group 0.000 claims description 27
- 239000003814 drug Substances 0.000 claims description 23
- 150000003839 salts Chemical group 0.000 claims description 22
- 125000005843 halogen group Chemical group 0.000 claims description 19
- 125000002252 acyl group Chemical group 0.000 claims description 18
- 229910052799 carbon Inorganic materials 0.000 claims description 18
- 229910052739 hydrogen Inorganic materials 0.000 claims description 17
- 238000000034 method Methods 0.000 claims description 17
- 230000036765 blood level Effects 0.000 claims description 16
- 208000023275 Autoimmune disease Diseases 0.000 claims description 14
- 125000001424 substituent group Chemical group 0.000 claims description 14
- 238000004519 manufacturing process Methods 0.000 claims description 10
- 206010052779 Transplant rejections Diseases 0.000 claims description 9
- 125000004423 acyloxy group Chemical group 0.000 claims description 9
- 238000012423 maintenance Methods 0.000 claims description 9
- 230000002459 sustained effect Effects 0.000 claims description 9
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims description 7
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims description 6
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims description 5
- 230000002401 inhibitory effect Effects 0.000 claims description 4
- 102000005962 receptors Human genes 0.000 claims description 4
- 108020003175 receptors Proteins 0.000 claims description 4
- UKNPZNCFUIYBMA-UHFFFAOYSA-N 5-amino-5-[2-chloro-4-(2-phenylmethoxyphenyl)sulfanylphenyl]pentane-1,3-diol Chemical compound NC(CC(CCO)O)C1=C(C=C(C=C1)SC1=C(C=CC=C1)OCC1=CC=CC=C1)Cl UKNPZNCFUIYBMA-UHFFFAOYSA-N 0.000 claims description 2
- 230000005764 inhibitory process Effects 0.000 claims description 2
- GOJUJUVQIVIZAV-UHFFFAOYSA-N 2-amino-4,6-dichloropyrimidine-5-carbaldehyde Chemical group NC1=NC(Cl)=C(C=O)C(Cl)=N1 GOJUJUVQIVIZAV-UHFFFAOYSA-N 0.000 claims 1
- 238000011292 agonist therapy Methods 0.000 claims 1
- 230000001186 cumulative effect Effects 0.000 abstract description 4
- 150000001875 compounds Chemical class 0.000 description 52
- 125000003545 alkoxy group Chemical group 0.000 description 43
- 229960000556 fingolimod Drugs 0.000 description 39
- 125000003118 aryl group Chemical group 0.000 description 16
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 description 11
- 150000004677 hydrates Chemical class 0.000 description 10
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 description 9
- 125000000623 heterocyclic group Chemical group 0.000 description 9
- 229910052760 oxygen Inorganic materials 0.000 description 9
- 229910052717 sulfur Inorganic materials 0.000 description 9
- 125000000753 cycloalkyl group Chemical group 0.000 description 8
- 229940079593 drug Drugs 0.000 description 8
- 125000001072 heteroaryl group Chemical group 0.000 description 7
- 210000004698 lymphocyte Anatomy 0.000 description 7
- 125000004442 acylamino group Chemical group 0.000 description 6
- 125000002947 alkylene group Chemical group 0.000 description 6
- 210000004369 blood Anatomy 0.000 description 6
- 239000008280 blood Substances 0.000 description 6
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 description 6
- DUYSYHSSBDVJSM-KRWOKUGFSA-N sphingosine 1-phosphate Chemical compound CCCCCCCCCCCCC\C=C\[C@@H](O)[C@@H](N)COP(O)(O)=O DUYSYHSSBDVJSM-KRWOKUGFSA-N 0.000 description 6
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 description 5
- 210000003734 kidney Anatomy 0.000 description 5
- 239000012453 solvate Substances 0.000 description 5
- 241000700159 Rattus Species 0.000 description 4
- 125000003282 alkyl amino group Chemical group 0.000 description 4
- 125000004414 alkyl thio group Chemical group 0.000 description 4
- 238000003556 assay Methods 0.000 description 4
- 150000001721 carbon Chemical group 0.000 description 4
- 210000002216 heart Anatomy 0.000 description 4
- 125000004356 hydroxy functional group Chemical group O* 0.000 description 4
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 description 4
- 230000002035 prolonged effect Effects 0.000 description 4
- 230000004083 survival effect Effects 0.000 description 4
- XOFLBQFBSOEHOG-UUOKFMHZSA-N γS-GTP Chemical compound C1=2NC(N)=NC(=O)C=2N=CN1[C@@H]1O[C@H](COP(O)(=O)OP(O)(=O)OP(O)(O)=S)[C@@H](O)[C@H]1O XOFLBQFBSOEHOG-UUOKFMHZSA-N 0.000 description 4
- 125000004890 (C1-C6) alkylamino group Chemical group 0.000 description 3
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 description 3
- 241000282693 Cercopithecidae Species 0.000 description 3
- IAZDPXIOMUYVGZ-UHFFFAOYSA-N Dimethylsulphoxide Chemical compound CS(C)=O IAZDPXIOMUYVGZ-UHFFFAOYSA-N 0.000 description 3
- 101100236683 Homo sapiens MBTPS1 gene Proteins 0.000 description 3
- 229910019142 PO4 Inorganic materials 0.000 description 3
- ZMANZCXQSJIPKH-UHFFFAOYSA-N Triethylamine Chemical compound CCN(CC)CC ZMANZCXQSJIPKH-UHFFFAOYSA-N 0.000 description 3
- 125000003342 alkenyl group Chemical group 0.000 description 3
- 125000003302 alkenyloxy group Chemical group 0.000 description 3
- 238000004458 analytical method Methods 0.000 description 3
- 125000005842 heteroatom Chemical group 0.000 description 3
- 239000001257 hydrogen Substances 0.000 description 3
- 125000004435 hydrogen atom Chemical class [H]* 0.000 description 3
- 230000007774 longterm Effects 0.000 description 3
- 125000001624 naphthyl group Chemical group 0.000 description 3
- 125000003884 phenylalkyl group Chemical group 0.000 description 3
- VZCYOOQTPOCHFL-UHFFFAOYSA-N trans-butenedioic acid Natural products OC(=O)C=CC(O)=O VZCYOOQTPOCHFL-UHFFFAOYSA-N 0.000 description 3
- 108010052285 Membrane Proteins Proteins 0.000 description 2
- FAPWRFPIFSIZLT-UHFFFAOYSA-M Sodium chloride Chemical compound [Na+].[Cl-] FAPWRFPIFSIZLT-UHFFFAOYSA-M 0.000 description 2
- 102100025750 Sphingosine 1-phosphate receptor 1 Human genes 0.000 description 2
- 101710155454 Sphingosine 1-phosphate receptor 1 Proteins 0.000 description 2
- 125000004453 alkoxycarbonyl group Chemical group 0.000 description 2
- 125000005133 alkynyloxy group Chemical group 0.000 description 2
- 239000011324 bead Substances 0.000 description 2
- 125000000051 benzyloxy group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])O* 0.000 description 2
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 description 2
- 125000006297 carbonyl amino group Chemical group [H]N([*:2])C([*:1])=O 0.000 description 2
- 210000004027 cell Anatomy 0.000 description 2
- 125000004093 cyano group Chemical group *C#N 0.000 description 2
- 150000002148 esters Chemical class 0.000 description 2
- 125000000592 heterocycloalkyl group Chemical group 0.000 description 2
- 210000004185 liver Anatomy 0.000 description 2
- 210000001165 lymph node Anatomy 0.000 description 2
- VZCYOOQTPOCHFL-UPHRSURJSA-N maleic acid Chemical compound OC(=O)\C=C/C(O)=O VZCYOOQTPOCHFL-UPHRSURJSA-N 0.000 description 2
- 125000002757 morpholinyl group Chemical group 0.000 description 2
- 229910052757 nitrogen Inorganic materials 0.000 description 2
- 210000001986 peyer's patch Anatomy 0.000 description 2
- 230000003285 pharmacodynamic effect Effects 0.000 description 2
- 125000000951 phenoxy group Chemical group [H]C1=C([H])C([H])=C(O*)C([H])=C1[H] 0.000 description 2
- 125000000843 phenylene group Chemical group C1(=C(C=CC=C1)*)* 0.000 description 2
- 239000010452 phosphate Substances 0.000 description 2
- 125000003386 piperidinyl group Chemical group 0.000 description 2
- 239000000902 placebo Substances 0.000 description 2
- 229940068196 placebo Drugs 0.000 description 2
- 229940002612 prodrug Drugs 0.000 description 2
- 239000000651 prodrug Substances 0.000 description 2
- 238000000159 protein binding assay Methods 0.000 description 2
- 125000003072 pyrazolidinyl group Chemical group 0.000 description 2
- 125000000168 pyrrolyl group Chemical group 0.000 description 2
- 238000002560 therapeutic procedure Methods 0.000 description 2
- 125000004568 thiomorpholinyl group Chemical group 0.000 description 2
- 238000002054 transplantation Methods 0.000 description 2
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 description 1
- 125000004768 (C1-C4) alkylsulfinyl group Chemical group 0.000 description 1
- 125000004769 (C1-C4) alkylsulfonyl group Chemical group 0.000 description 1
- 125000006376 (C3-C10) cycloalkyl group Chemical group 0.000 description 1
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 description 1
- 125000004502 1,2,3-oxadiazolyl group Chemical group 0.000 description 1
- KIHYPELVXPAIDH-UHFFFAOYSA-N 1-[[4-[n-[[4-cyclohexyl-3-(trifluoromethyl)phenyl]methoxy]-c-methylcarbonimidoyl]-2-ethylphenyl]methyl]azetidine-3-carboxylic acid Chemical class CCC1=CC(C(C)=NOCC=2C=C(C(C3CCCCC3)=CC=2)C(F)(F)F)=CC=C1CN1CC(C(O)=O)C1 KIHYPELVXPAIDH-UHFFFAOYSA-N 0.000 description 1
- JKMHFZQWWAIEOD-UHFFFAOYSA-N 2-[4-(2-hydroxyethyl)piperazin-1-yl]ethanesulfonic acid Chemical compound OCC[NH+]1CCN(CCS([O-])(=O)=O)CC1 JKMHFZQWWAIEOD-UHFFFAOYSA-N 0.000 description 1
- BXIWYZLGTUWLCD-UHFFFAOYSA-N 2-amino-2-tetradecylpropane-1,3-diol Chemical compound CCCCCCCCCCCCCCC(N)(CO)CO BXIWYZLGTUWLCD-UHFFFAOYSA-N 0.000 description 1
- ITJCKQTXCLGXHE-UHFFFAOYSA-N 2-amino-4-(4-heptoxyphenyl)-2-methylbutan-1-ol Chemical compound CCCCCCCOC1=CC=C(CCC(C)(N)CO)C=C1 ITJCKQTXCLGXHE-UHFFFAOYSA-N 0.000 description 1
- BKMMTJMQCTUHRP-UHFFFAOYSA-N 2-aminopropan-1-ol Chemical class CC(N)CO BKMMTJMQCTUHRP-UHFFFAOYSA-N 0.000 description 1
- QPRQEDXDYOZYLA-UHFFFAOYSA-N 2-methyl-1-butanol Substances CCC(C)CO QPRQEDXDYOZYLA-UHFFFAOYSA-N 0.000 description 1
- 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 description 1
- NESAWTWENPISNE-UHFFFAOYSA-N 5-amino-5-[2-chloro-4-(3-phenylmethoxyphenoxy)phenyl]hexane-1,3-diol Chemical compound C1=C(Cl)C(C(N)(CC(O)CCO)C)=CC=C1OC1=CC=CC(OCC=2C=CC=CC=2)=C1 NESAWTWENPISNE-UHFFFAOYSA-N 0.000 description 1
- MIYSLZPNGDBEIR-UHFFFAOYSA-N 5-amino-5-[2-chloro-4-(3-phenylmethoxyphenoxy)phenyl]pentane-1,3-diol Chemical compound C1=C(Cl)C(C(CC(O)CCO)N)=CC=C1OC1=CC=CC(OCC=2C=CC=CC=2)=C1 MIYSLZPNGDBEIR-UHFFFAOYSA-N 0.000 description 1
- 125000003341 7 membered heterocyclic group Chemical group 0.000 description 1
- QTBSBXVTEAMEQO-UHFFFAOYSA-M Acetate Chemical compound CC([O-])=O QTBSBXVTEAMEQO-UHFFFAOYSA-M 0.000 description 1
- 210000001266 CD8-positive T-lymphocyte Anatomy 0.000 description 1
- 0 CNC(*)(OC)O* Chemical compound CNC(*)(OC)O* 0.000 description 1
- OYPRJOBELJOOCE-UHFFFAOYSA-N Calcium Chemical compound [Ca] OYPRJOBELJOOCE-UHFFFAOYSA-N 0.000 description 1
- KRKNYBCHXYNGOX-UHFFFAOYSA-K Citrate Chemical compound [O-]C(=O)CC(O)(CC([O-])=O)C([O-])=O KRKNYBCHXYNGOX-UHFFFAOYSA-K 0.000 description 1
- 229940126062 Compound A Drugs 0.000 description 1
- 229930105110 Cyclosporin A Natural products 0.000 description 1
- 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 1
- 108010036949 Cyclosporine Proteins 0.000 description 1
- VGGSQFUCUMXWEO-UHFFFAOYSA-N Ethene Chemical compound C=C VGGSQFUCUMXWEO-UHFFFAOYSA-N 0.000 description 1
- 239000005977 Ethylene Substances 0.000 description 1
- HKVAMNSJSFKALM-GKUWKFKPSA-N Everolimus Chemical compound C1C[C@@H](OCCO)[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 HKVAMNSJSFKALM-GKUWKFKPSA-N 0.000 description 1
- WSFSSNUMVMOOMR-UHFFFAOYSA-N Formaldehyde Chemical compound O=C WSFSSNUMVMOOMR-UHFFFAOYSA-N 0.000 description 1
- VZCYOOQTPOCHFL-OWOJBTEDSA-N Fumaric acid Chemical compound OC(=O)\C=C\C(O)=O VZCYOOQTPOCHFL-OWOJBTEDSA-N 0.000 description 1
- NLDMNSXOCDLTTB-UHFFFAOYSA-N Heterophylliin A Natural products O1C2COC(=O)C3=CC(O)=C(O)C(O)=C3C3=C(O)C(O)=C(O)C=C3C(=O)OC2C(OC(=O)C=2C=C(O)C(O)=C(O)C=2)C(O)C1OC(=O)C1=CC(O)=C(O)C(O)=C1 NLDMNSXOCDLTTB-UHFFFAOYSA-N 0.000 description 1
- 241000282412 Homo Species 0.000 description 1
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 description 1
- CPELXLSAUQHCOX-UHFFFAOYSA-N Hydrogen bromide Chemical compound Br CPELXLSAUQHCOX-UHFFFAOYSA-N 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
- 206010062016 Immunosuppression Diseases 0.000 description 1
- 208000022559 Inflammatory bowel disease Diseases 0.000 description 1
- 208000005777 Lupus Nephritis Diseases 0.000 description 1
- KDXKERNSBIXSRK-UHFFFAOYSA-N Lysine Natural products NCCCCC(N)C(O)=O KDXKERNSBIXSRK-UHFFFAOYSA-N 0.000 description 1
- 239000004472 Lysine Substances 0.000 description 1
- 241000124008 Mammalia Species 0.000 description 1
- 102000018697 Membrane Proteins Human genes 0.000 description 1
- 241001465754 Metazoa Species 0.000 description 1
- AFVFQIVMOAPDHO-UHFFFAOYSA-N Methanesulfonic acid Chemical compound CS(O)(=O)=O AFVFQIVMOAPDHO-UHFFFAOYSA-N 0.000 description 1
- 150000001204 N-oxides Chemical class 0.000 description 1
- LZAPHMLITWOKCL-UHFFFAOYSA-N NC(CC(CCO)O)(C)C1=C(C=C(C=C1)SC1=C(C=CC=C1)OCC1=CC=CC=C1)Cl Chemical compound NC(CC(CCO)O)(C)C1=C(C=C(C=C1)SC1=C(C=CC=C1)OCC1=CC=CC=C1)Cl LZAPHMLITWOKCL-UHFFFAOYSA-N 0.000 description 1
- IJBMPYLQDRXBRE-UHFFFAOYSA-N OC(CCNCc(cc1)ccc1OCc1cc(-c2ccccc2)c(C(F)(F)F)[s]1)=O Chemical compound OC(CCNCc(cc1)ccc1OCc1cc(-c2ccccc2)c(C(F)(F)F)[s]1)=O IJBMPYLQDRXBRE-UHFFFAOYSA-N 0.000 description 1
- 108091000080 Phosphotransferase Proteins 0.000 description 1
- ZLMJMSJWJFRBEC-UHFFFAOYSA-N Potassium Chemical compound [K] ZLMJMSJWJFRBEC-UHFFFAOYSA-N 0.000 description 1
- 201000004681 Psoriasis Diseases 0.000 description 1
- QAOWNCQODCNURD-UHFFFAOYSA-L Sulfate Chemical compound [O-]S([O-])(=O)=O QAOWNCQODCNURD-UHFFFAOYSA-L 0.000 description 1
- 210000001744 T-lymphocyte Anatomy 0.000 description 1
- YPFDHNVEDLHUCE-UHFFFAOYSA-N Trimethylene glycol Natural products OCCCO YPFDHNVEDLHUCE-UHFFFAOYSA-N 0.000 description 1
- URPMOIWBYMBOHA-MRXNPFEDSA-N [(2r)-2-amino-2-methyl-4-(4-pentoxyphenyl)butyl] dihydrogen phosphate Chemical compound CCCCCOC1=CC=C(CC[C@@](C)(N)COP(O)(O)=O)C=C1 URPMOIWBYMBOHA-MRXNPFEDSA-N 0.000 description 1
- 238000009825 accumulation Methods 0.000 description 1
- 230000004913 activation Effects 0.000 description 1
- 125000001931 aliphatic group Chemical group 0.000 description 1
- 125000004450 alkenylene group Chemical group 0.000 description 1
- 125000004849 alkoxymethyl group Chemical group 0.000 description 1
- 125000004448 alkyl carbonyl group Chemical group 0.000 description 1
- 125000005037 alkyl phenyl group Chemical group 0.000 description 1
- 125000000304 alkynyl group Chemical group 0.000 description 1
- 229910052782 aluminium Inorganic materials 0.000 description 1
- XAGFODPZIPBFFR-UHFFFAOYSA-N aluminium Chemical compound [Al] XAGFODPZIPBFFR-UHFFFAOYSA-N 0.000 description 1
- 150000001412 amines Chemical class 0.000 description 1
- 150000001413 amino acids Chemical class 0.000 description 1
- 125000003277 amino group Chemical group 0.000 description 1
- 206010003246 arthritis Diseases 0.000 description 1
- HONIICLYMWZJFZ-UHFFFAOYSA-N azetidine Chemical compound C1CNC1 HONIICLYMWZJFZ-UHFFFAOYSA-N 0.000 description 1
- 210000003719 b-lymphocyte Anatomy 0.000 description 1
- 229940077388 benzenesulfonate Drugs 0.000 description 1
- WPYMKLBDIGXBTP-UHFFFAOYSA-N benzoic acid Chemical compound OC(=O)C1=CC=CC=C1 WPYMKLBDIGXBTP-UHFFFAOYSA-N 0.000 description 1
- 239000011575 calcium Substances 0.000 description 1
- 229910052791 calcium Inorganic materials 0.000 description 1
- 125000004432 carbon atom Chemical group C* 0.000 description 1
- 210000004970 cd4 cell Anatomy 0.000 description 1
- 238000005119 centrifugation Methods 0.000 description 1
- 229960001265 ciclosporin Drugs 0.000 description 1
- 238000012790 confirmation Methods 0.000 description 1
- 125000000000 cycloalkoxy group Chemical group 0.000 description 1
- 125000001316 cycloalkyl alkyl group Chemical group 0.000 description 1
- 230000016396 cytokine production Effects 0.000 description 1
- 230000003247 decreasing effect Effects 0.000 description 1
- 201000010099 disease Diseases 0.000 description 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 1
- 238000009826 distribution Methods 0.000 description 1
- 230000007783 downstream signaling Effects 0.000 description 1
- 230000000694 effects Effects 0.000 description 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 description 1
- 238000011156 evaluation Methods 0.000 description 1
- 229960005167 everolimus Drugs 0.000 description 1
- 230000005713 exacerbation Effects 0.000 description 1
- 238000002474 experimental method Methods 0.000 description 1
- 235000013861 fat-free Nutrition 0.000 description 1
- 125000000524 functional group Chemical group 0.000 description 1
- 125000002541 furyl group Chemical group 0.000 description 1
- 238000003304 gavage Methods 0.000 description 1
- 125000005059 halophenyl group Chemical group 0.000 description 1
- 230000002489 hematologic effect Effects 0.000 description 1
- 125000003187 heptyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 description 1
- 125000005446 heptyloxy group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])O* 0.000 description 1
- 125000004446 heteroarylalkyl group Chemical group 0.000 description 1
- 125000005343 heterocyclic alkyl group Chemical group 0.000 description 1
- 150000002391 heterocyclic compounds Chemical class 0.000 description 1
- 102000034345 heterotrimeric G proteins Human genes 0.000 description 1
- 108091006093 heterotrimeric G proteins Proteins 0.000 description 1
- 125000003707 hexyloxy group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])O* 0.000 description 1
- 125000002632 imidazolidinyl group Chemical group 0.000 description 1
- 125000002883 imidazolyl group Chemical group 0.000 description 1
- 230000002519 immonomodulatory effect Effects 0.000 description 1
- 230000001506 immunosuppresive effect Effects 0.000 description 1
- 238000001727 in vivo Methods 0.000 description 1
- 238000011534 incubation Methods 0.000 description 1
- 238000001764 infiltration Methods 0.000 description 1
- 230000008595 infiltration Effects 0.000 description 1
- 208000027866 inflammatory disease Diseases 0.000 description 1
- 230000002757 inflammatory effect Effects 0.000 description 1
- 230000003834 intracellular effect Effects 0.000 description 1
- 125000001786 isothiazolyl group Chemical group 0.000 description 1
- 125000003965 isoxazolidinyl group Chemical group 0.000 description 1
- 125000000842 isoxazolyl group Chemical group 0.000 description 1
- 238000004020 luminiscence type Methods 0.000 description 1
- 210000004072 lung Anatomy 0.000 description 1
- 210000003563 lymphoid tissue Anatomy 0.000 description 1
- 238000002483 medication Methods 0.000 description 1
- 239000012528 membrane Substances 0.000 description 1
- 239000002207 metabolite Substances 0.000 description 1
- 229910052751 metal Inorganic materials 0.000 description 1
- 239000002184 metal Substances 0.000 description 1
- 150000002739 metals Chemical class 0.000 description 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 description 1
- 150000007522 mineralic acids Chemical class 0.000 description 1
- 239000000203 mixture Substances 0.000 description 1
- 238000012544 monitoring process Methods 0.000 description 1
- 201000006417 multiple sclerosis Diseases 0.000 description 1
- 230000003287 optical effect Effects 0.000 description 1
- 150000007524 organic acids Chemical class 0.000 description 1
- 235000005985 organic acids Nutrition 0.000 description 1
- 125000000160 oxazolidinyl group Chemical group 0.000 description 1
- 125000002971 oxazolyl group Chemical group 0.000 description 1
- 125000004043 oxo group Chemical group O=* 0.000 description 1
- 125000004430 oxygen atom Chemical group O* 0.000 description 1
- 125000004115 pentoxy group Chemical group [*]OC([H])([H])C([H])([H])C([H])([H])C(C([H])([H])[H])([H])[H] 0.000 description 1
- 210000005105 peripheral blood lymphocyte Anatomy 0.000 description 1
- 230000000144 pharmacologic effect Effects 0.000 description 1
- 230000026731 phosphorylation Effects 0.000 description 1
- 238000006366 phosphorylation reaction Methods 0.000 description 1
- 102000020233 phosphotransferase Human genes 0.000 description 1
- 125000004193 piperazinyl group Chemical group 0.000 description 1
- 229910052700 potassium Inorganic materials 0.000 description 1
- 239000011591 potassium Substances 0.000 description 1
- 238000002360 preparation method Methods 0.000 description 1
- 230000001737 promoting effect Effects 0.000 description 1
- LVTJOONKWUXEFR-FZRMHRINSA-N protoneodioscin Natural products O(C[C@@H](CC[C@]1(O)[C@H](C)[C@@H]2[C@]3(C)[C@H]([C@H]4[C@@H]([C@]5(C)C(=CC4)C[C@@H](O[C@@H]4[C@H](O[C@H]6[C@@H](O)[C@@H](O)[C@@H](O)[C@H](C)O6)[C@@H](O)[C@H](O[C@H]6[C@@H](O)[C@@H](O)[C@@H](O)[C@H](C)O6)[C@H](CO)O4)CC5)CC3)C[C@@H]2O1)C)[C@H]1[C@H](O)[C@H](O)[C@H](O)[C@@H](CO)O1 LVTJOONKWUXEFR-FZRMHRINSA-N 0.000 description 1
- 125000004309 pyranyl group Chemical group O1C(C=CC=C1)* 0.000 description 1
- 125000003373 pyrazinyl group Chemical group 0.000 description 1
- 125000003226 pyrazolyl group Chemical group 0.000 description 1
- 125000002098 pyridazinyl group Chemical group 0.000 description 1
- 125000004076 pyridyl group Chemical group 0.000 description 1
- 125000000719 pyrrolidinyl group Chemical group 0.000 description 1
- 230000009467 reduction Effects 0.000 description 1
- 230000002441 reversible effect Effects 0.000 description 1
- 238000012216 screening Methods 0.000 description 1
- 210000003491 skin Anatomy 0.000 description 1
- 210000000813 small intestine Anatomy 0.000 description 1
- 229910052708 sodium Inorganic materials 0.000 description 1
- 239000011734 sodium Substances 0.000 description 1
- 239000011780 sodium chloride Substances 0.000 description 1
- 150000003410 sphingosines Chemical class 0.000 description 1
- 239000000126 substance Substances 0.000 description 1
- 125000000475 sulfinyl group Chemical group [*:2]S([*:1])=O 0.000 description 1
- 125000000472 sulfonyl group Chemical group *S(*)(=O)=O 0.000 description 1
- 230000001629 suppression Effects 0.000 description 1
- 208000024891 symptom Diseases 0.000 description 1
- 230000002195 synergetic effect Effects 0.000 description 1
- 125000001412 tetrahydropyranyl group Chemical group 0.000 description 1
- 125000003831 tetrazolyl group Chemical group 0.000 description 1
- 125000001113 thiadiazolyl group Chemical group 0.000 description 1
- 125000001984 thiazolidinyl group Chemical group 0.000 description 1
- 125000000335 thiazolyl group Chemical group 0.000 description 1
- 125000001544 thienyl group Chemical group 0.000 description 1
- 125000001425 triazolyl group Chemical group 0.000 description 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/13—Amines
- A61K31/135—Amines having aromatic rings, e.g. ketamine, nortriptyline
- A61K31/137—Arylalkylamines, e.g. amphetamine, epinephrine, salbutamol, ephedrine or methadone
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/13—Amines
- A61K31/135—Amines having aromatic rings, e.g. ketamine, nortriptyline
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/397—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having four-membered rings, e.g. azetidine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/66—Phosphorus compounds
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/12—Drugs for disorders of the urinary system of the kidneys
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/06—Antipsoriatics
-
- 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
- A61P25/00—Drugs for disorders of the nervous system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
-
- 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
- A61P37/00—Drugs for immunological or allergic disorders
-
- 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
-
- 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
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
Landscapes
- Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Organic Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Immunology (AREA)
- Epidemiology (AREA)
- Emergency Medicine (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Rheumatology (AREA)
- Transplantation (AREA)
- Psychiatry (AREA)
- Dermatology (AREA)
- Urology & Nephrology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Physical Education & Sports Medicine (AREA)
- Hospice & Palliative Care (AREA)
- Pain & Pain Management (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Medicinal Preparation (AREA)
- Storage Device Security (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US63148304P | 2004-11-29 | 2004-11-29 | |
| US60/631,483 | 2004-11-29 |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| KR1020137008529A Division KR20130041385A (ko) | 2004-11-29 | 2005-11-28 | Ｓ１ｐ 수용체 효능제의 투여 용법 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| KR20070085465A true KR20070085465A (ko) | 2007-08-27 |
Family
ID=36046868
Family Applications (4)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| KR1020077011969A Ceased KR20070085465A (ko) | 2004-11-29 | 2005-11-28 | Ｓ１ｐ 수용체 효능제의 투여 용법 |
| KR1020137008529A Ceased KR20130041385A (ko) | 2004-11-29 | 2005-11-28 | Ｓ１ｐ 수용체 효능제의 투여 용법 |
| KR1020147018084A Withdrawn KR20140095109A (ko) | 2004-11-29 | 2005-11-28 | Ｓ１ｐ 수용체 효능제의 투여 용법 |
| KR20157005416A Ceased KR20150028858A (ko) | 2004-11-29 | 2005-11-28 | Ｓ１ｐ 수용체 효능제의 투여 용법 |
Family Applications After (3)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| KR1020137008529A Ceased KR20130041385A (ko) | 2004-11-29 | 2005-11-28 | Ｓ１ｐ 수용체 효능제의 투여 용법 |
| KR1020147018084A Withdrawn KR20140095109A (ko) | 2004-11-29 | 2005-11-28 | Ｓ１ｐ 수용체 효능제의 투여 용법 |
| KR20157005416A Ceased KR20150028858A (ko) | 2004-11-29 | 2005-11-28 | Ｓ１ｐ 수용체 효능제의 투여 용법 |
Country Status (21)
| Country | Link |
|---|---|
| US (3) | US20090275553A1 (https=) |
| EP (3) | EP2384749A1 (https=) |
| JP (4) | JP2008521827A (https=) |
| KR (4) | KR20070085465A (https=) |
| CN (2) | CN101068536B (https=) |
| AU (1) | AU2005309378B2 (https=) |
| BR (1) | BRPI0518674A2 (https=) |
| CA (1) | CA2589265A1 (https=) |
| ES (1) | ES2495690T3 (https=) |
| IL (2) | IL183134A0 (https=) |
| MA (1) | MA29034B1 (https=) |
| MX (1) | MX2007006373A (https=) |
| NO (2) | NO20072401L (https=) |
| NZ (2) | NZ590054A (https=) |
| PL (1) | PL1819326T3 (https=) |
| PT (1) | PT1819326E (https=) |
| RU (2) | RU2478384C2 (https=) |
| SG (2) | SG187468A1 (https=) |
| TN (1) | TNSN07209A1 (https=) |
| WO (1) | WO2006058316A1 (https=) |
| ZA (1) | ZA200703328B (https=) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR101347919B1 (ko) * | 2008-12-22 | 2014-01-07 | 노파르티스 아게 | Ｓ１ｐ 수용체 효능제를 위한 투여 요법 |
Families Citing this family (30)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| MX2007001661A (es) | 2004-08-13 | 2007-04-23 | Praecis Pharm Inc | Metodos y composiciones para modular la actividad del receptor de esfingosina -1 fosfato (sip). |
| KR20070085465A (ko) * | 2004-11-29 | 2007-08-27 | 노파르티스 아게 | Ｓ１ｐ 수용체 효능제의 투여 용법 |
| ES2529724T3 (es) * | 2005-09-09 | 2015-02-25 | Novartis Ag | Tratamiento de enfermedades autoinmunes |
| GB0612721D0 (en) * | 2006-06-27 | 2006-08-09 | Novartis Ag | Organic compounds |
| CA2684953C (en) * | 2007-05-04 | 2016-08-09 | Novartis Ag | Use of s1p receptor modulator |
| PL2278960T5 (pl) | 2008-03-17 | 2020-06-29 | Actelion Pharmaceuticals Ltd. | Schemat dawkowania dla selektywnego agonisty receptora sip1 |
| CA2724592A1 (en) * | 2008-05-20 | 2009-11-26 | Kyorin Pharmaceutical Co., Ltd. | Agent for maintenance of induced remission |
| EP2695615A3 (en) | 2008-07-23 | 2014-04-30 | Novartis AG | Sphingosine 1 phosphate receptor modulators and their use to treat muscle inflammation |
| KR101618906B1 (ko) * | 2008-08-18 | 2016-05-09 | 노파르티스 아게 | 말초 신경병증의 치료를 위한 화합물 |
| US20120115840A1 (en) * | 2008-12-18 | 2012-05-10 | Lech Ciszewski | Hemifumarate salt of 1-[4-[1-(4-cyclohexyl-3-trifluoromethyl-benzyloxyimino)-ethyl]-2-ethyl-benzyl]-azetidine-3-carboxylic acid |
| JP2012512884A (ja) | 2008-12-18 | 2012-06-07 | ノバルティス アーゲー | １−（４−｛１−［（ｅ）−４−シクロヘキシル−３−トリフルオロメチル−ベンジルオキシイミノ］−エチル｝−２−エチル−ベンジル）−アゼチジン−３−カルボン酸の新規の多形相 |
| KR20110101159A (ko) * | 2008-12-18 | 2011-09-15 | 노파르티스 아게 | 신규 염 |
| AU2015275246B2 (en) * | 2008-12-22 | 2018-02-01 | Novartis Ag | Dosage regimen for a S1P receptor agonist |
| JP5657565B2 (ja) * | 2008-12-22 | 2015-01-21 | ノバルティス アーゲー | Ｓ１ｐ受容体アゴニストの投与レジメン |
| NZ598534A (en) | 2009-09-29 | 2014-03-28 | Novartis Ag | Dosage regimen of an s1p receptor modulator |
| US20110124605A1 (en) * | 2009-11-20 | 2011-05-26 | Shreeram Aradhye | Use of an S1P Receptor Agonist |
| US8791100B2 (en) | 2010-02-02 | 2014-07-29 | Novartis Ag | Aryl benzylamine compounds |
| BR112012028248A2 (pt) * | 2010-05-06 | 2016-08-02 | Novartis Ag | derivados de sulfeto de diarila, seu uso, e kit |
| JP6111202B2 (ja) | 2011-01-07 | 2017-04-05 | ノバルティス アーゲー | 免疫抑制製剤 |
| BR112014009141A8 (pt) * | 2011-10-21 | 2017-06-20 | Novartis Ag | regime de dosagem para um modulador ou agonista do receptor s1p |
| SMT202000298T1 (it) | 2012-08-17 | 2020-07-08 | Actelion Pharmaceuticals Ltd | Processo per la produzione di (2z,5z)-5-(3-cloro-4((r)-2,3-diidrossipropossi) benziliden)-2-(propilimmino)-3-(o-tolil)tiazolidin-4-one e intermedio usato in detto processo |
| CN102887829B (zh) * | 2012-09-05 | 2014-07-02 | 中国科学院上海药物研究所 | 芬戈莫德粘酸盐及其晶体的制备方法和用途 |
| US10675254B2 (en) | 2013-10-11 | 2020-06-09 | Teikoku Seiyaku Co., Ltd. | Sphingosine-1-phosphate receptor agonist iontophoretic devices and methods of using the same |
| CN105611917A (zh) | 2013-10-11 | 2016-05-25 | 帝国制药美国公司 | 局部鞘氨醇-1-磷酸酯受体激动剂制剂及其使用方法 |
| KR20200013086A (ko) | 2014-12-11 | 2020-02-05 | 액테리온 파마슈티칼 리미티드 | 선택적 s1p1 수용체 효능제에 대한 투약 섭생 |
| MA41139B1 (fr) | 2014-12-11 | 2026-02-27 | Laboratoires Juvise Pharmaceuticals | Combinaison pharmaceutique comprenant du ponesimod et son utilisation dans le traitement de la sclérose en plaque |
| WO2016135644A1 (en) | 2015-02-26 | 2016-09-01 | Novartis Ag | Treatment of autoimmune disease in a patient receiving additionally a beta-blocker |
| US10250466B2 (en) * | 2016-03-29 | 2019-04-02 | Juniper Networks, Inc. | Application signature generation and distribution |
| US11629124B2 (en) | 2017-03-09 | 2023-04-18 | Novartis Ag | Solid forms comprising an oxime ether compound, compositions and methods of use thereof |
| JP7749552B2 (ja) | 2019-10-31 | 2025-10-06 | イドルシア・ファーマシューティカルズ・リミテッド | Ｃｘｃｒ７アンタゴニストのｓ１ｐ１受容体調節剤との合剤 |
Family Cites Families (28)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE69321823T2 (de) * | 1992-10-21 | 1999-06-02 | Taito Co., Ltd., Tokio/Tokyo | 2-amino-1, 3- propandiolverbindung und immunosuppressium |
| EP0778263B1 (en) | 1994-08-22 | 2002-01-09 | Welfide Corporation | Benzene compound and medicinal use thereof |
| WO1997024112A1 (en) * | 1995-12-28 | 1997-07-10 | Yoshitomi Pharmaceutical Industries, Ltd. | External preparation |
| US6476004B1 (en) * | 1996-07-18 | 2002-11-05 | Mitsubishi Pharma Corporation | Pharmaceutical composition |
| KR20000075745A (ko) * | 1997-02-27 | 2000-12-26 | 가마후라 아키오 | 의약 조성물 |
| ES2240868T3 (es) | 1997-04-04 | 2005-10-16 | Mitsubishi Pharma Corporation | Compuesto de 2-aminopropano -1,3-diol, su uso farmaceutico e intermedios en su sintesis. |
| JPH1180026A (ja) * | 1997-09-02 | 1999-03-23 | Yoshitomi Pharmaceut Ind Ltd | 新規免疫抑制剤、その使用方法およびその同定方法 |
| JPH11116479A (ja) * | 1997-10-10 | 1999-04-27 | Sugen Inc | 脳癌のための組み合わせ化学療法処置 |
| CN1328387C (zh) | 2000-07-13 | 2007-07-25 | 三共株式会社 | 氨基醇衍生物 |
| EP1315735A4 (en) | 2000-08-31 | 2005-04-06 | Merck & Co Inc | Phosphate derivatives as immunoregulatory compounds |
| CA2442178A1 (en) | 2001-03-26 | 2002-10-03 | Novartis Ag | 2-amino-propanol derivatives |
| IL157946A0 (en) * | 2001-04-02 | 2004-03-28 | Genentech Inc | Combination therapy |
| EP1381358B1 (en) * | 2001-04-02 | 2006-05-03 | Astrazeneca AB | Solid pharmaceutical composition comprising 4'-cyano-trifluoro-3-(4-fluorophenylsulphonyl) -2-hydroxy-2-methylpropiono- m toluidide and pvp |
| JP2002316985A (ja) | 2001-04-20 | 2002-10-31 | Sankyo Co Ltd | ベンゾチオフェン誘導体 |
| BR0209319A (pt) * | 2001-06-08 | 2004-07-20 | Novartis Ag | Tratamento ou profilaxia de rejeição de enxerto de célula produtora de insulina |
| DE60235900D1 (de) * | 2001-09-27 | 2010-05-20 | Kyorin Seiyaku Kk | Osuppressivum |
| CA2461212C (en) | 2001-09-27 | 2010-08-17 | Kyorin Pharmaceutical Co., Ltd. | Diaryl sulfide derivatives, salts thereof and immunosuppressive agents using the same |
| JP4430941B2 (ja) | 2002-01-18 | 2010-03-10 | メルク エンド カムパニー インコーポレーテッド | Ｅｄｇ受容体作動薬 |
| WO2003061567A2 (en) | 2002-01-18 | 2003-07-31 | Merck & Co., Inc. | Selective s1p1/edg1 receptor agonists |
| ATE448193T1 (de) | 2002-01-18 | 2009-11-15 | Merck & Co Inc | ßN-(BENZYL)AMINOALKYL CARBOXYLATE, PHOSPHINATE, PHOSPHONATE UND TETRAZOLE ALS EDG REZEPTORAGONISTENß |
| EP1575576A2 (en) * | 2002-09-24 | 2005-09-21 | Novartis AG | Organic compounds |
| CL2004001120A1 (es) | 2003-05-19 | 2005-04-15 | Irm Llc | Compuestos derivados de amina sustituidas con heterociclos, inmunosupresores; composicion farmaceutica; y uso para tratar enfermedades mediadas por interacciones de linfocito, tales como enfermedades autoinmunes, inflamatorias, infecciosas, cancer. |
| MY150088A (en) | 2003-05-19 | 2013-11-29 | Irm Llc | Immunosuppressant compounds and compositions |
| UA74941C2 (en) | 2004-04-26 | 2006-02-15 | Fos Internat S A | A metal-thermal process for producing magnesium and vacuum induction furnace for realizing the same |
| WO2005113330A1 (en) | 2004-05-05 | 2005-12-01 | Adler, Richard, S. | Systems and methods for protecting ship from attack on the surface or under water |
| WO2006041015A1 (ja) * | 2004-10-12 | 2006-04-20 | Kyorin Pharmaceutical Co., Ltd. | アミノアルコール誘導体とその付加塩及び免疫抑制剤 |
| KR20070085465A (ko) * | 2004-11-29 | 2007-08-27 | 노파르티스 아게 | Ｓ１ｐ 수용체 효능제의 투여 용법 |
| GT200600350A (es) * | 2005-08-09 | 2007-03-28 | Formulaciones líquidas |
-
2005
- 2005-11-28 KR KR1020077011969A patent/KR20070085465A/ko not_active Ceased
- 2005-11-28 JP JP2007543584A patent/JP2008521827A/ja not_active Withdrawn
- 2005-11-28 US US11/720,205 patent/US20090275553A1/en not_active Abandoned
- 2005-11-28 AU AU2005309378A patent/AU2005309378B2/en not_active Ceased
- 2005-11-28 CN CN2005800409686A patent/CN101068536B/zh not_active Expired - Fee Related
- 2005-11-28 MX MX2007006373A patent/MX2007006373A/es active IP Right Grant
- 2005-11-28 KR KR1020137008529A patent/KR20130041385A/ko not_active Ceased
- 2005-11-28 CN CN2012100846463A patent/CN102600472A/zh active Pending
- 2005-11-28 BR BRPI0518674-9A patent/BRPI0518674A2/pt not_active Application Discontinuation
- 2005-11-28 PL PL05826219T patent/PL1819326T3/pl unknown
- 2005-11-28 SG SG2013002662A patent/SG187468A1/en unknown
- 2005-11-28 NZ NZ590054A patent/NZ590054A/en not_active IP Right Cessation
- 2005-11-28 PT PT58262197T patent/PT1819326E/pt unknown
- 2005-11-28 KR KR1020147018084A patent/KR20140095109A/ko not_active Withdrawn
- 2005-11-28 KR KR20157005416A patent/KR20150028858A/ko not_active Ceased
- 2005-11-28 EP EP10179083A patent/EP2384749A1/en not_active Withdrawn
- 2005-11-28 SG SG200907947-6A patent/SG158096A1/en unknown
- 2005-11-28 RU RU2007124327/15A patent/RU2478384C2/ru not_active IP Right Cessation
- 2005-11-28 WO PCT/US2005/043044 patent/WO2006058316A1/en not_active Ceased
- 2005-11-28 ES ES05826219.7T patent/ES2495690T3/es not_active Expired - Lifetime
- 2005-11-28 EP EP05826219.7A patent/EP1819326B1/en not_active Revoked
- 2005-11-28 CA CA002589265A patent/CA2589265A1/en not_active Abandoned
- 2005-11-28 EP EP10179081A patent/EP2359821A1/en not_active Withdrawn
- 2005-11-28 NZ NZ554720A patent/NZ554720A/en not_active IP Right Cessation
-
2007
- 2007-04-24 ZA ZA200703328A patent/ZA200703328B/xx unknown
- 2007-05-10 IL IL183134A patent/IL183134A0/en unknown
- 2007-05-10 NO NO20072401A patent/NO20072401L/no not_active Application Discontinuation
- 2007-05-22 MA MA29926A patent/MA29034B1/fr unknown
- 2007-05-28 TN TNP2007000209A patent/TNSN07209A1/fr unknown
-
2011
- 2011-11-22 US US13/302,881 patent/US20120071446A1/en not_active Abandoned
-
2012
- 2012-02-27 JP JP2012040574A patent/JP2012107059A/ja not_active Withdrawn
- 2012-10-02 RU RU2012141951/15A patent/RU2012141951A/ru unknown
- 2012-11-06 NO NO20121305A patent/NO20121305L/no not_active Application Discontinuation
- 2012-12-06 IL IL223502A patent/IL223502A0/en unknown
-
2013
- 2013-03-05 JP JP2013043351A patent/JP2013129664A/ja not_active Withdrawn
-
2014
- 2014-10-16 US US14/516,153 patent/US20150087720A1/en not_active Abandoned
- 2014-12-26 JP JP2014266267A patent/JP2015061883A/ja active Pending
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR101347919B1 (ko) * | 2008-12-22 | 2014-01-07 | 노파르티스 아게 | Ｓ１ｐ 수용체 효능제를 위한 투여 요법 |
Also Published As
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| KR20070085465A (ko) | Ｓ１ｐ 수용체 효능제의 투여 용법 | |
| KR101473494B1 (ko) | 액상 제제 | |
| CN1893934B (zh) | 1-磷酸-鞘氨醇（s1p）受体激动剂用于制备治疗脑变性性疾病的药物的应用 | |
| HK1161247A (en) | Dosage regimen of an s1p receptor agonist | |
| HK1109057B (en) | Dosage regimen of an s1p receptor agonist | |
| HK1158943A (en) | Dosage regimen of an s1p receptor agonist | |
| KR20070102538A (ko) | Ｓ1ｐ 수용체 효능제/조절제와 면역억제성 약물의 조합에의한 항림프구 항체 유도 |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| PA0105 | International application |
Patent event date: 20070528 Patent event code: PA01051R01D Comment text: International Patent Application |
|
| PG1501 | Laying open of application | ||
| A201 | Request for examination | ||
| PA0201 | Request for examination |
Patent event code: PA02012R01D Patent event date: 20101129 Comment text: Request for Examination of Application |
|
| E902 | Notification of reason for refusal | ||
| PE0902 | Notice of grounds for rejection |
Comment text: Notification of reason for refusal Patent event date: 20120710 Patent event code: PE09021S01D |
|
| E601 | Decision to refuse application | ||
| PE0601 | Decision on rejection of patent |
Patent event date: 20130130 Comment text: Decision to Refuse Application Patent event code: PE06012S01D Patent event date: 20120710 Comment text: Notification of reason for refusal Patent event code: PE06011S01I |
|
| J201 | Request for trial against refusal decision | ||
| PJ0201 | Trial against decision of rejection |
Patent event date: 20130304 Comment text: Request for Trial against Decision on Refusal Patent event code: PJ02012R01D Patent event date: 20130130 Comment text: Decision to Refuse Application Patent event code: PJ02011S01I Appeal kind category: Appeal against decision to decline refusal Decision date: 20130404 Appeal identifier: 2013101001660 Request date: 20130304 |
|
| A107 | Divisional application of patent | ||
| PA0104 | Divisional application for international application |
Comment text: Divisional Application for International Patent Patent event code: PA01041R01D Patent event date: 20130403 |
|
| J121 | Written withdrawal of request for trial | ||
| PC1202 | Submission of document of withdrawal before decision of registration |
Comment text: [Withdrawal of Procedure relating to Patent, etc.] Withdrawal (Abandonment) Patent event code: PC12021R01D Patent event date: 20130404 |
|
| PJ1201 | Withdrawal of trial |
Patent event code: PJ12011R01D Patent event date: 20130404 Comment text: Written Withdrawal of Request for Trial Appeal identifier: 2013101001660 Request date: 20130304 Appeal kind category: Appeal against decision to decline refusal Decision date: 20130404 |
|
| WITB | Written withdrawal of application |