JP2011500683A5 - - Google Patents
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- Publication number
- JP2011500683A5 JP2011500683A5 JP2010529955A JP2010529955A JP2011500683A5 JP 2011500683 A5 JP2011500683 A5 JP 2011500683A5 JP 2010529955 A JP2010529955 A JP 2010529955A JP 2010529955 A JP2010529955 A JP 2010529955A JP 2011500683 A5 JP2011500683 A5 JP 2011500683A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- aryl
- hydrogen
- amino
- alkoxy
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Granted
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- 125000000217 alkyl group Chemical group 0.000 claims 99
- 125000003118 aryl group Chemical group 0.000 claims 59
- 229910052739 hydrogen Inorganic materials 0.000 claims 48
- 239000001257 hydrogen Substances 0.000 claims 45
- 150000002431 hydrogen Chemical class 0.000 claims 39
- -1 heteroaliphatic Chemical group 0.000 claims 38
- 125000003545 alkoxy group Chemical group 0.000 claims 35
- 239000000126 substance Substances 0.000 claims 35
- 125000001424 substituent group Chemical group 0.000 claims 32
- 125000000623 heterocyclic group Chemical group 0.000 claims 27
- 229910052736 halogen Inorganic materials 0.000 claims 26
- 239000003814 drug Substances 0.000 claims 25
- 229940124597 therapeutic agent Drugs 0.000 claims 25
- 150000002367 halogens Chemical group 0.000 claims 24
- 125000001072 heteroaryl group Chemical group 0.000 claims 24
- 150000001875 compounds Chemical class 0.000 claims 23
- 125000000753 cycloalkyl group Chemical group 0.000 claims 20
- 239000005557 antagonist Substances 0.000 claims 19
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 17
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 17
- 125000003342 alkenyl group Chemical group 0.000 claims 16
- 125000000304 alkynyl group Chemical group 0.000 claims 16
- 125000004043 oxo group Chemical group O=* 0.000 claims 16
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 15
- 125000002723 alicyclic group Chemical group 0.000 claims 13
- 125000001931 aliphatic group Chemical group 0.000 claims 13
- 125000002877 alkyl aryl group Chemical group 0.000 claims 13
- 125000005213 alkyl heteroaryl group Chemical group 0.000 claims 13
- 150000002148 esters Chemical class 0.000 claims 13
- 125000005842 heteroatom Chemical group 0.000 claims 12
- 150000003839 salts Chemical class 0.000 claims 12
- 125000004093 cyano group Chemical group *C#N 0.000 claims 11
- 229910052757 nitrogen Inorganic materials 0.000 claims 11
- RTZKZFJDLAIYFH-UHFFFAOYSA-N Diethyl ether Chemical compound CCOCC RTZKZFJDLAIYFH-UHFFFAOYSA-N 0.000 claims 10
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 10
- 229910052717 sulfur Inorganic materials 0.000 claims 10
- 125000005843 halogen group Chemical group 0.000 claims 9
- 125000004104 aryloxy group Chemical group 0.000 claims 8
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 claims 8
- 229910052760 oxygen Inorganic materials 0.000 claims 8
- 125000000446 sulfanediyl group Chemical group *S* 0.000 claims 8
- 229910052794 bromium Inorganic materials 0.000 claims 7
- 125000004181 carboxyalkyl group Chemical group 0.000 claims 7
- 229910052731 fluorine Inorganic materials 0.000 claims 7
- 229910052740 iodine Inorganic materials 0.000 claims 7
- 229920006395 saturated elastomer Polymers 0.000 claims 7
- 206010012689 Diabetic retinopathy Diseases 0.000 claims 6
- ZRALSGWEFCBTJO-UHFFFAOYSA-N Guanidine Chemical group NC(N)=N ZRALSGWEFCBTJO-UHFFFAOYSA-N 0.000 claims 6
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 6
- 229910052799 carbon Inorganic materials 0.000 claims 6
- 229910052801 chlorine Inorganic materials 0.000 claims 6
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 6
- 125000000472 sulfonyl group Chemical group *S(*)(=O)=O 0.000 claims 6
- 150000001408 amides Chemical class 0.000 claims 5
- 125000004429 atom Chemical group 0.000 claims 5
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 claims 5
- BVKZGUZCCUSVTD-UHFFFAOYSA-N carbonic acid Chemical compound OC(O)=O BVKZGUZCCUSVTD-UHFFFAOYSA-N 0.000 claims 5
- 125000002485 formyl group Chemical group [H]C(*)=O 0.000 claims 5
- SNOOUWRIMMFWNE-UHFFFAOYSA-M sodium;6-[(3,4,5-trimethoxybenzoyl)amino]hexanoate Chemical compound [Na+].COC1=CC(C(=O)NCCCCCC([O-])=O)=CC(OC)=C1OC SNOOUWRIMMFWNE-UHFFFAOYSA-M 0.000 claims 5
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 4
- KXDAEFPNCMNJSK-UHFFFAOYSA-N Benzamide Chemical compound NC(=O)C1=CC=CC=C1 KXDAEFPNCMNJSK-UHFFFAOYSA-N 0.000 claims 4
- 239000004215 Carbon black (E152) Substances 0.000 claims 4
- 125000004453 alkoxycarbonyl group Chemical group 0.000 claims 4
- 125000004414 alkyl thio group Chemical group 0.000 claims 4
- 125000002947 alkylene group Chemical group 0.000 claims 4
- 125000001589 carboacyl group Chemical group 0.000 claims 4
- 125000000392 cycloalkenyl group Chemical group 0.000 claims 4
- 229930195733 hydrocarbon Natural products 0.000 claims 4
- 150000002430 hydrocarbons Chemical group 0.000 claims 4
- 238000001802 infusion Methods 0.000 claims 4
- 125000002950 monocyclic group Chemical group 0.000 claims 4
- 125000000547 substituted alkyl group Chemical group 0.000 claims 4
- 125000003396 thiol group Chemical group [H]S* 0.000 claims 4
- 125000006272 (C3-C7) cycloalkyl group Chemical group 0.000 claims 3
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims 3
- 108010064593 Intercellular Adhesion Molecule-1 Proteins 0.000 claims 3
- 102100037877 Intercellular adhesion molecule 1 Human genes 0.000 claims 3
- CHJJGSNFBQVOTG-UHFFFAOYSA-N N-methyl-guanidine Chemical group CNC(N)=N CHJJGSNFBQVOTG-UHFFFAOYSA-N 0.000 claims 3
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical compound [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims 3
- 125000002252 acyl group Chemical group 0.000 claims 3
- 125000003275 alpha amino acid group Chemical group 0.000 claims 3
- 150000001409 amidines Chemical group 0.000 claims 3
- 125000004103 aminoalkyl group Chemical group 0.000 claims 3
- BWOVZCWSJFYBRM-UHFFFAOYSA-N carbononitridic isocyanate Chemical group O=C=NC#N BWOVZCWSJFYBRM-UHFFFAOYSA-N 0.000 claims 3
- 239000003795 chemical substances by application Substances 0.000 claims 3
- 125000004122 cyclic group Chemical group 0.000 claims 3
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 3
- SWSQBOPZIKWTGO-UHFFFAOYSA-N dimethylaminoamidine Chemical group CN(C)C(N)=N SWSQBOPZIKWTGO-UHFFFAOYSA-N 0.000 claims 3
- 125000001183 hydrocarbyl group Chemical group 0.000 claims 3
- 125000005010 perfluoroalkyl group Chemical group 0.000 claims 3
- 239000008194 pharmaceutical composition Substances 0.000 claims 3
- BDHFUVZGWQCTTF-UHFFFAOYSA-M sulfonate Chemical compound [O-]S(=O)=O BDHFUVZGWQCTTF-UHFFFAOYSA-M 0.000 claims 3
- 125000004916 (C1-C6) alkylcarbonyl group Chemical group 0.000 claims 2
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims 2
- 125000006374 C2-C10 alkenyl group Chemical group 0.000 claims 2
- 125000005865 C2-C10alkynyl group Chemical group 0.000 claims 2
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 2
- 125000004648 C2-C8 alkenyl group Chemical group 0.000 claims 2
- 125000004649 C2-C8 alkynyl group Chemical group 0.000 claims 2
- SIKJAQJRHWYJAI-UHFFFAOYSA-N Indole Chemical group C1=CC=C2NC=CC2=C1 SIKJAQJRHWYJAI-UHFFFAOYSA-N 0.000 claims 2
- JTNFLOSMZURXJM-UHFFFAOYSA-N NS(S)(=O)=O Chemical compound NS(S)(=O)=O JTNFLOSMZURXJM-UHFFFAOYSA-N 0.000 claims 2
- KAESVJOAVNADME-UHFFFAOYSA-N Pyrrole Chemical group C=1C=CNC=1 KAESVJOAVNADME-UHFFFAOYSA-N 0.000 claims 2
- 125000003668 acetyloxy group Chemical group [H]C([H])([H])C(=O)O[*] 0.000 claims 2
- 239000002253 acid Substances 0.000 claims 2
- 239000000443 aerosol Substances 0.000 claims 2
- 125000004450 alkenylene group Chemical group 0.000 claims 2
- 125000005037 alkyl phenyl group Chemical group 0.000 claims 2
- 125000003710 aryl alkyl group Chemical group 0.000 claims 2
- VCJIGSOOIYBSFA-UHFFFAOYSA-N azido formate Chemical compound [N-]=[N+]=NOC=O VCJIGSOOIYBSFA-UHFFFAOYSA-N 0.000 claims 2
- 125000002619 bicyclic group Chemical group 0.000 claims 2
- 239000013078 crystal Substances 0.000 claims 2
- 125000000000 cycloalkoxy group Chemical group 0.000 claims 2
- 238000002405 diagnostic procedure Methods 0.000 claims 2
- 125000005982 diphenylmethyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])(*)C1=C([H])C([H])=C([H])C([H])=C1[H] 0.000 claims 2
- 239000006260 foam Substances 0.000 claims 2
- 238000009472 formulation Methods 0.000 claims 2
- 125000004404 heteroalkyl group Chemical group 0.000 claims 2
- 125000002768 hydroxyalkyl group Chemical group 0.000 claims 2
- 239000007943 implant Substances 0.000 claims 2
- 239000012948 isocyanate Substances 0.000 claims 2
- 150000002513 isocyanates Chemical class 0.000 claims 2
- 239000002502 liposome Substances 0.000 claims 2
- 239000007788 liquid Substances 0.000 claims 2
- 239000000203 mixture Substances 0.000 claims 2
- 239000002105 nanoparticle Substances 0.000 claims 2
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 2
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims 2
- 125000004193 piperazinyl group Chemical group 0.000 claims 2
- 229920000642 polymer Polymers 0.000 claims 2
- 239000000843 powder Substances 0.000 claims 2
- 239000012453 solvate Substances 0.000 claims 2
- 239000007921 spray Substances 0.000 claims 2
- 125000005346 substituted cycloalkyl group Chemical group 0.000 claims 2
- 125000004001 thioalkyl group Chemical group 0.000 claims 2
- 125000002088 tosyl group Chemical group [H]C1=C([H])C(=C([H])C([H])=C1C([H])([H])[H])S(*)(=O)=O 0.000 claims 2
- VEEGZPWAAPPXRB-BJMVGYQFSA-N (3e)-3-(1h-imidazol-5-ylmethylidene)-1h-indol-2-one Chemical compound O=C1NC2=CC=CC=C2\C1=C/C1=CN=CN1 VEEGZPWAAPPXRB-BJMVGYQFSA-N 0.000 claims 1
- 125000004739 (C1-C6) alkylsulfonyl group Chemical group 0.000 claims 1
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 1
- GZTFUVZVLYUPRG-IZZDOVSWSA-N (e)-3-(4-tert-butylphenyl)-n-(2,3-dihydro-1,4-benzodioxin-6-yl)prop-2-enamide Chemical compound C1=CC(C(C)(C)C)=CC=C1\C=C\C(=O)NC1=CC=C(OCCO2)C2=C1 GZTFUVZVLYUPRG-IZZDOVSWSA-N 0.000 claims 1
- WBYWAXJHAXSJNI-VOTSOKGWSA-M .beta-Phenylacrylic acid Natural products [O-]C(=O)\C=C\C1=CC=CC=C1 WBYWAXJHAXSJNI-VOTSOKGWSA-M 0.000 claims 1
- 125000004607 1,2,3,4-tetrahydroquinolinyl group Chemical group N1(CCCC2=CC=CC=C12)* 0.000 claims 1
- 101710175516 14 kDa zinc-binding protein Proteins 0.000 claims 1
- OVSKIKFHRZPJSS-UHFFFAOYSA-N 2,4-D Chemical compound OC(=O)COC1=CC=C(Cl)C=C1Cl OVSKIKFHRZPJSS-UHFFFAOYSA-N 0.000 claims 1
- SCVJRXQHFJXZFZ-KVQBGUIXSA-N 2-amino-9-[(2r,4s,5r)-4-hydroxy-5-(hydroxymethyl)oxolan-2-yl]-3h-purine-6-thione Chemical compound C1=2NC(N)=NC(=S)C=2N=CN1[C@H]1C[C@H](O)[C@@H](CO)O1 SCVJRXQHFJXZFZ-KVQBGUIXSA-N 0.000 claims 1
- 239000005541 ACE inhibitor Substances 0.000 claims 1
- 101710129690 Angiotensin-converting enzyme inhibitor Proteins 0.000 claims 1
- 101710145634 Antigen 1 Proteins 0.000 claims 1
- 201000004569 Blindness Diseases 0.000 claims 1
- 101710086378 Bradykinin-potentiating and C-type natriuretic peptides Proteins 0.000 claims 1
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims 1
- WBYWAXJHAXSJNI-SREVYHEPSA-N Cinnamic acid Chemical compound OC(=O)\C=C/C1=CC=CC=C1 WBYWAXJHAXSJNI-SREVYHEPSA-N 0.000 claims 1
- 229940124073 Complement inhibitor Drugs 0.000 claims 1
- 206010012688 Diabetic retinal oedema Diseases 0.000 claims 1
- 206010015943 Eye inflammation Diseases 0.000 claims 1
- 102000008394 Immunoglobulin Fragments Human genes 0.000 claims 1
- 108010021625 Immunoglobulin Fragments Proteins 0.000 claims 1
- 108010064600 Intercellular Adhesion Molecule-3 Proteins 0.000 claims 1
- 102100037872 Intercellular adhesion molecule 2 Human genes 0.000 claims 1
- 101710148794 Intercellular adhesion molecule 2 Proteins 0.000 claims 1
- 102100037871 Intercellular adhesion molecule 3 Human genes 0.000 claims 1
- 208000001344 Macular Edema Diseases 0.000 claims 1
- 206010025415 Macular oedema Diseases 0.000 claims 1
- 201000010183 Papilledema Diseases 0.000 claims 1
- 229940123924 Protein kinase C inhibitor Drugs 0.000 claims 1
- 208000007135 Retinal Neovascularization Diseases 0.000 claims 1
- 206010038886 Retinal oedema Diseases 0.000 claims 1
- 125000002777 acetyl group Chemical group [H]C([H])([H])C(*)=O 0.000 claims 1
- 125000002070 alkenylidene group Chemical group 0.000 claims 1
- 125000004390 alkyl sulfonyl group Chemical group 0.000 claims 1
- 230000003281 allosteric effect Effects 0.000 claims 1
- 229940121369 angiogenesis inhibitor Drugs 0.000 claims 1
- 239000004037 angiogenesis inhibitor Substances 0.000 claims 1
- 229940044094 angiotensin-converting-enzyme inhibitor Drugs 0.000 claims 1
- 210000002159 anterior chamber Anatomy 0.000 claims 1
- 239000003242 anti bacterial agent Substances 0.000 claims 1
- 230000000181 anti-adherent effect Effects 0.000 claims 1
- 230000002424 anti-apoptotic effect Effects 0.000 claims 1
- 230000003110 anti-inflammatory effect Effects 0.000 claims 1
- 239000003963 antioxidant agent Substances 0.000 claims 1
- 230000003078 antioxidant effect Effects 0.000 claims 1
- 125000005098 aryl alkoxy carbonyl group Chemical group 0.000 claims 1
- 125000005161 aryl oxy carbonyl group Chemical group 0.000 claims 1
- 125000004391 aryl sulfonyl group Chemical group 0.000 claims 1
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims 1
- 230000008721 basement membrane thickening Effects 0.000 claims 1
- 125000003236 benzoyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C(*)=O 0.000 claims 1
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims 1
- 125000002837 carbocyclic group Chemical group 0.000 claims 1
- 150000003857 carboxamides Chemical class 0.000 claims 1
- 229930016911 cinnamic acid Natural products 0.000 claims 1
- 235000013985 cinnamic acid Nutrition 0.000 claims 1
- 239000004074 complement inhibitor Substances 0.000 claims 1
- 239000006071 cream Substances 0.000 claims 1
- 125000006254 cycloalkyl carbonyl group Chemical group 0.000 claims 1
- 201000011190 diabetic macular edema Diseases 0.000 claims 1
- 238000003745 diagnosis Methods 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 230000001497 fibrovascular Effects 0.000 claims 1
- 125000002541 furyl group Chemical group 0.000 claims 1
- 239000000499 gel Substances 0.000 claims 1
- 125000005223 heteroarylcarbonyl group Chemical group 0.000 claims 1
- 125000005143 heteroarylsulfonyl group Chemical group 0.000 claims 1
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims 1
- 125000004470 heterocyclooxy group Chemical group 0.000 claims 1
- 125000004415 heterocyclylalkyl group Chemical group 0.000 claims 1
- 150000004677 hydrates Chemical class 0.000 claims 1
- 125000002632 imidazolidinyl group Chemical group 0.000 claims 1
- 125000002883 imidazolyl group Chemical group 0.000 claims 1
- PZOUSPYUWWUPPK-UHFFFAOYSA-N indole Chemical group CC1=CC=CC2=C1C=CN2 PZOUSPYUWWUPPK-UHFFFAOYSA-N 0.000 claims 1
- RKJUIXBNRJVNHR-UHFFFAOYSA-N indolenine Chemical group C1=CC=C2CC=NC2=C1 RKJUIXBNRJVNHR-UHFFFAOYSA-N 0.000 claims 1
- 125000003387 indolinyl group Chemical group N1(CCC2=CC=CC=C12)* 0.000 claims 1
- 125000001041 indolyl group Chemical group 0.000 claims 1
- 238000002347 injection Methods 0.000 claims 1
- 239000007924 injection Substances 0.000 claims 1
- 238000003780 insertion Methods 0.000 claims 1
- 230000037431 insertion Effects 0.000 claims 1
- 230000003993 interaction Effects 0.000 claims 1
- 125000004594 isoindolinyl group Chemical group C1(NCC2=CC=CC=C12)* 0.000 claims 1
- 150000003951 lactams Chemical class 0.000 claims 1
- 125000005647 linker group Chemical group 0.000 claims 1
- 239000006194 liquid suspension Substances 0.000 claims 1
- 208000018769 loss of vision Diseases 0.000 claims 1
- 231100000864 loss of vision Toxicity 0.000 claims 1
- 210000004698 lymphocyte Anatomy 0.000 claims 1
- 201000010230 macular retinal edema Diseases 0.000 claims 1
- 239000011159 matrix material Substances 0.000 claims 1
- 238000000034 method Methods 0.000 claims 1
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 1
- WBYWAXJHAXSJNI-UHFFFAOYSA-N methyl p-hydroxycinnamate Natural products OC(=O)C=CC1=CC=CC=C1 WBYWAXJHAXSJNI-UHFFFAOYSA-N 0.000 claims 1
- 125000000325 methylidene group Chemical group [H]C([H])=* 0.000 claims 1
- 239000011859 microparticle Substances 0.000 claims 1
- 125000002757 morpholinyl group Chemical group 0.000 claims 1
- 239000006199 nebulizer Substances 0.000 claims 1
- IQZPDFORWZTSKT-UHFFFAOYSA-N nitrosulphonic acid Chemical compound OS(=O)(=O)[N+]([O-])=O IQZPDFORWZTSKT-UHFFFAOYSA-N 0.000 claims 1
- 239000002674 ointment Substances 0.000 claims 1
- 230000003287 optical effect Effects 0.000 claims 1
- 239000001301 oxygen Substances 0.000 claims 1
- 125000003386 piperidinyl group Chemical group 0.000 claims 1
- 230000002980 postoperative effect Effects 0.000 claims 1
- 239000000651 prodrug Substances 0.000 claims 1
- 229940002612 prodrug Drugs 0.000 claims 1
- 125000006239 protecting group Chemical group 0.000 claims 1
- 239000003881 protein kinase C inhibitor Substances 0.000 claims 1
- 125000000719 pyrrolidinyl group Chemical group 0.000 claims 1
- 125000001422 pyrrolinyl group Chemical group 0.000 claims 1
- 150000003254 radicals Chemical class 0.000 claims 1
- 210000001525 retina Anatomy 0.000 claims 1
- 201000011195 retinal edema Diseases 0.000 claims 1
- 230000002207 retinal effect Effects 0.000 claims 1
- 208000032253 retinal ischemia Diseases 0.000 claims 1
- 239000007787 solid Substances 0.000 claims 1
- 239000000243 solution Substances 0.000 claims 1
- 150000003431 steroids Chemical class 0.000 claims 1
- 238000007920 subcutaneous administration Methods 0.000 claims 1
- 125000003107 substituted aryl group Chemical group 0.000 claims 1
- 239000011593 sulfur Substances 0.000 claims 1
- 239000000725 suspension Substances 0.000 claims 1
- 238000013268 sustained release Methods 0.000 claims 1
- 239000012730 sustained-release form Substances 0.000 claims 1
- 238000012385 systemic delivery Methods 0.000 claims 1
- 230000001225 therapeutic effect Effects 0.000 claims 1
- 125000001984 thiazolidinyl group Chemical group 0.000 claims 1
- 125000000858 thiocyanato group Chemical group *SC#N 0.000 claims 1
- 125000004568 thiomorpholinyl group Chemical group 0.000 claims 1
- 238000011200 topical administration Methods 0.000 claims 1
- 230000000699 topical effect Effects 0.000 claims 1
- APEJMQOBVMLION-VOTSOKGWSA-N trans-cinnamamide Chemical compound NC(=O)\C=C\C1=CC=CC=C1 APEJMQOBVMLION-VOTSOKGWSA-N 0.000 claims 1
- 238000012384 transportation and delivery Methods 0.000 claims 1
- 125000005389 trialkylsiloxy group Chemical group 0.000 claims 1
- 125000004665 trialkylsilyl group Chemical group 0.000 claims 1
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 1
- GBXQPDCOMJJCMJ-UHFFFAOYSA-M trimethyl-[6-(trimethylazaniumyl)hexyl]azanium;bromide Chemical compound [Br-].C[N+](C)(C)CCCCCC[N+](C)(C)C GBXQPDCOMJJCMJ-UHFFFAOYSA-M 0.000 claims 1
- 230000004393 visual impairment Effects 0.000 claims 1
- 238000005406 washing Methods 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US99957107P | 2007-10-19 | 2007-10-19 | |
| US60/999,571 | 2007-10-19 | ||
| PCT/US2008/011878 WO2009054914A1 (en) | 2007-10-19 | 2008-10-17 | Compositions and methods for treatment of diabetic retinopathy |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2014144595A Division JP2014221808A (ja) | 2007-10-19 | 2014-07-14 | 糖尿病性網膜症の治療のための組成物及び方法 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2011500683A JP2011500683A (ja) | 2011-01-06 |
| JP2011500683A5 true JP2011500683A5 (enExample) | 2011-11-17 |
| JP5808037B2 JP5808037B2 (ja) | 2015-11-10 |
Family
ID=40579823
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2010529955A Expired - Fee Related JP5808037B2 (ja) | 2007-10-19 | 2008-10-17 | 糖尿病性網膜症の治療のための組成物及び方法 |
| JP2014144595A Pending JP2014221808A (ja) | 2007-10-19 | 2014-07-14 | 糖尿病性網膜症の治療のための組成物及び方法 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2014144595A Pending JP2014221808A (ja) | 2007-10-19 | 2014-07-14 | 糖尿病性網膜症の治療のための組成物及び方法 |
Country Status (9)
| Country | Link |
|---|---|
| US (3) | US20090155176A1 (enExample) |
| EP (3) | EP3167886B1 (enExample) |
| JP (2) | JP5808037B2 (enExample) |
| CN (1) | CN101873797A (enExample) |
| AU (1) | AU2008317473B2 (enExample) |
| CA (3) | CA2702984C (enExample) |
| ES (2) | ES2830024T3 (enExample) |
| MX (1) | MX2010004281A (enExample) |
| WO (1) | WO2009054914A1 (enExample) |
Families Citing this family (44)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU2004287875B2 (en) | 2003-11-05 | 2011-06-02 | Bausch + Lomb Ireland Limited | Modulators of cellular adhesion |
| SI1881823T1 (sl) * | 2005-05-17 | 2015-04-30 | Sarcode Bioscience Inc. | Sestavki in postopki za zdravljenje bolezni oäśesa |
| CA2702984C (en) | 2007-10-19 | 2017-04-11 | Sarcode Corporation | Compositions and methods for treatment of diabetic retinopathy |
| EP3632444A3 (en) * | 2008-04-15 | 2020-08-26 | SARcode Bioscience Inc. | Topical lfa-1 antagonists for use in localized treatment of immune related disorders |
| WO2009139817A2 (en) * | 2008-04-15 | 2009-11-19 | Sarcode Corporation | Crystalline pharmaceutical and methods of preparation and use thereof |
| CN102065694A (zh) * | 2008-04-15 | 2011-05-18 | 萨可德公司 | 用于局部治疗免疫相关疾病的雾化的lfa-1拮抗剂 |
| EP2276508A4 (en) * | 2008-04-15 | 2011-12-28 | Sarcode Bioscience Inc | ADMINISTRATION OF LFA-1 ANTAGONISTS TO THE GASTROINTESTINAL SYSTEM |
| US8378105B2 (en) * | 2009-10-21 | 2013-02-19 | Sarcode Bioscience Inc. | Crystalline pharmaceutical and methods of preparation and use thereof |
| ES2752008T3 (es) * | 2009-10-30 | 2020-04-02 | Intratus Inc | Métodos y composiciones para la liberación sostenida de fármacos |
| US20110189174A1 (en) * | 2010-02-01 | 2011-08-04 | Afshin Shafiee | Compositions and methods for treating, reducing, ameliorating, alleviating, or inhibiting progression of, pathogenic ocular neovascularization |
| US8598156B2 (en) | 2010-03-25 | 2013-12-03 | Glaxosmithkline Llc | Chemical compounds |
| TW201206908A (en) * | 2010-05-05 | 2012-02-16 | Glaxo Wellcome Mfg Pte Ltd | Pharmaceutical compositions and methods of making same |
| HK1204988A1 (en) * | 2012-02-22 | 2015-12-11 | Stealth Peptides International, Inc. | Methods and compositions for preventing or treating ophthalmic conditions |
| CA2875053C (en) | 2012-06-05 | 2020-07-14 | Olatec Industries Llc | Pharmaceutical composition for treating inflammation and pain |
| SI2861566T1 (sl) | 2012-06-13 | 2017-03-31 | F. Hoffmann-La Roche Ag | Novi diazaspirocikloalkan in azaspirocikloalkan |
| EP2877465A4 (en) | 2012-07-25 | 2016-05-11 | Sarcode Bioscience Inc | LFA-1 HEMMER AND POLYMORPH THEREOF |
| PL2900669T3 (pl) | 2012-09-25 | 2020-01-31 | F. Hoffmann-La Roche Ag | Pochodne heksahydropirolo[3,4-C]pirolu i związki pokrewne jako inhibitory autotaksyny (ATX) oraz inhibitory produkcji kwasu lizofosfatydowego (LPA) do leczenia np. chorób nerek |
| AR095079A1 (es) | 2013-03-12 | 2015-09-16 | Hoffmann La Roche | Derivados de octahidro-pirrolo[3,4-c]-pirrol y piridina-fenilo |
| AU2014356583B2 (en) | 2013-11-26 | 2019-02-28 | F. Hoffmann-La Roche Ag | New octahydro-cyclobuta (1,2-c;3,4-c')dipyrrol-2-yl |
| JP6272604B2 (ja) * | 2013-12-27 | 2018-01-31 | 日本サプリメント株式会社 | 糖取り込み促進剤 |
| CR20160418A (es) | 2014-03-26 | 2016-11-07 | Hoffmann La Roche | Nuevos compuestos biciclicos de 7 eslabones |
| MA50635A (fr) | 2014-03-26 | 2020-08-12 | Hoffmann La Roche | Nouveaux composés bicycliques comme inhibiteurs de la production d'autotaxin (atx) et de l'acide lysophosphatidique |
| WO2016159351A1 (ja) * | 2015-04-03 | 2016-10-06 | 参天製薬株式会社 | 涙腺ドラッグデリバリーシステム |
| EP3344619B1 (en) | 2015-09-04 | 2020-10-28 | H. Hoffnabb-La Roche Ag | Phenoxymethyl derivatives |
| WO2017050747A1 (en) | 2015-09-24 | 2017-03-30 | F. Hoffmann-La Roche Ag | New bicyclic compounds as dual atx/ca inhibitors |
| AU2016328437A1 (en) | 2015-09-24 | 2018-01-25 | F. Hoffmann-La Roche Ag | Bicyclic compounds as ATX inhibitors |
| MA42918A (fr) | 2015-09-24 | 2018-08-01 | Hoffmann La Roche | Composés bicycliques utilisés en tant qu'inhibiteurs d'atx |
| BR112018006080A2 (pt) | 2015-09-24 | 2018-10-09 | F. Hoffmann-La Roche Ag | novos compostos bicíclicos como inibidores de dupla ação de atx/ca |
| RU2019132254A (ru) | 2017-03-16 | 2021-04-16 | Ф. Хоффманн-Ля Рош Аг | Гетероциклические соединения, пригодные в качестве дуальных ингибиторов atx/ca |
| EP3596060B1 (en) * | 2017-03-16 | 2023-09-20 | F. Hoffmann-La Roche AG | New bicyclic compounds as atx inhibitors |
| RU2764243C2 (ru) | 2017-09-22 | 2022-01-14 | ДЖУБИЛАНТ ЭПИПЭД ЭлЭлСи | Гетероциклические соединения в качестве ингибиторов PAD |
| CN111225915B (zh) | 2017-10-18 | 2023-03-07 | 朱比兰特埃皮帕德有限公司 | 作为pad抑制剂的咪唑并吡啶化合物 |
| US11629135B2 (en) | 2017-11-06 | 2023-04-18 | Jubilant Prodell Llc | Pyrimidine derivatives as inhibitors of PD1/PD-L1 activation |
| RS65576B1 (sr) | 2017-11-24 | 2024-06-28 | Jubilant Episcribe Llc | Heterociklična jedinjenja kao inhibitori prmt5 |
| CN112105610B (zh) | 2018-03-13 | 2024-01-26 | 朱比连特普罗德尔有限责任公司 | 作为pd1/pd-l1相互作用/活化的抑制剂的双环化合物 |
| MX2020010999A (es) | 2018-04-18 | 2021-01-20 | Constellation Pharmaceuticals Inc | Moduladores de enzimas modificadoras de metilo, composiciones y usos de estos. |
| EP3797108B1 (en) | 2018-05-21 | 2022-07-20 | Constellation Pharmaceuticals, Inc. | Modulators of methyl modifying enzymes, compositions and uses thereof |
| KR102554417B1 (ko) | 2018-06-18 | 2023-07-11 | 삼성전자주식회사 | 이미지 센서 |
| EP3990433B1 (en) | 2019-06-25 | 2026-05-20 | Translatum Medicus Inc. | PROCESSES FOR THE MANUFACTURE OF 2-((1-BENZYL-1H-INDAZOL-3-YL)METHOXY)-2-METHYLPROPANOIC ACID AND ITS DERIVATIVES |
| PE20220562A1 (es) | 2019-07-24 | 2022-04-13 | Constellation Pharmaceuticals Inc | Formas cristalinas de 7-cloro-2-(4-(3-metoxiazetidin-1-il)ciclohexil)-2,4-dimetil-n-((6-metil-4-(metiltio)-2-oxo-1,2-dihidropiridin-3-il)metil)benzo[d][1,3]dioxol-5-carboxamida |
| MX2022015327A (es) * | 2020-06-05 | 2023-02-22 | Occurx Pty Ltd | Compuestos y metodos para el tratamiento de trastornos oculares. |
| CN116635032A (zh) * | 2020-10-21 | 2023-08-22 | 阿祖拉眼科有限公司 | 用于治疗眼部病症的化合物和方法 |
| EP4589369A4 (en) * | 2022-09-15 | 2026-08-12 | Nof Corp | CONTACT LENS SOLUTION |
| WO2026052060A1 (zh) * | 2024-09-06 | 2026-03-12 | 上海翊石医药科技有限公司 | 一类苯甲酰基甘氨酸衍生物及其制备方法和应用 |
Family Cites Families (166)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6872A (en) | 1849-11-13 | Means of changing the combination in bevolving tumbler-locks | ||
| US735A (en) | 1838-05-10 | Rtjftjg porter | ||
| US3773919A (en) | 1969-10-23 | 1973-11-20 | Du Pont | Polylactide-drug mixtures |
| US3989816A (en) | 1975-06-19 | 1976-11-02 | Nelson Research & Development Company | Vehicle composition containing 1-substituted azacycloheptan-2-ones |
| US4316893A (en) * | 1975-06-19 | 1982-02-23 | Nelson Research & Development Co. | Vehicle composition containing 1-substituted azacycloalkan-2-ones |
| US4405616A (en) | 1975-06-19 | 1983-09-20 | Nelson Research & Development Company | Penetration enhancers for transdermal drug delivery of systemic agents |
| IE52535B1 (en) | 1981-02-16 | 1987-12-09 | Ici Plc | Continuous release pharmaceutical compositions |
| US4557934A (en) | 1983-06-21 | 1985-12-10 | The Procter & Gamble Company | Penetrating topical pharmaceutical compositions containing 1-dodecyl-azacycloheptan-2-one |
| US4568343A (en) * | 1984-10-09 | 1986-02-04 | Alza Corporation | Skin permeation enhancer compositions |
| US4713244A (en) | 1985-08-16 | 1987-12-15 | Bausch & Lomb Incorporated | Sustained-release formulation containing an amino acid polymer with a lower alkyl (C1 -C4) polar solvent |
| US4931279A (en) * | 1985-08-16 | 1990-06-05 | Bausch & Lomb Incorporated | Sustained release formulation containing an ion-exchange resin |
| US4668506A (en) * | 1985-08-16 | 1987-05-26 | Bausch & Lomb Incorporated | Sustained-release formulation containing and amino acid polymer |
| US5023252A (en) | 1985-12-04 | 1991-06-11 | Conrex Pharmaceutical Corporation | Transdermal and trans-membrane delivery of drugs |
| US5001139A (en) * | 1987-06-12 | 1991-03-19 | American Cyanamid Company | Enchancers for the transdermal flux of nivadipine |
| US4992445A (en) | 1987-06-12 | 1991-02-12 | American Cyanamid Co. | Transdermal delivery of pharmaceuticals |
| GB2209937B (en) * | 1987-09-21 | 1991-07-03 | Depiopharm S A | Water insoluble polypeptides |
| ATE114972T1 (de) | 1987-11-02 | 1994-12-15 | Baylor College Medicine | Verwendung von icam-1 oder ihre funktionelle derivate zur behandlung unspezifischer entzündungen. |
| DE68907066T2 (de) | 1988-01-29 | 1993-12-16 | Koken Kk | Verbesserte Formulierungen mit kontrollierter Abgabe. |
| DE3802996A1 (de) * | 1988-02-02 | 1989-08-10 | Cassella Ag | Verwendung von 2-oxo-pyrrolidin-1-acetamid zur bestimmung der glomerulaeren filtrationsrate beim menschen |
| US5424399A (en) * | 1988-06-28 | 1995-06-13 | The Children's Medical Center Corporation | Human CR3α/β heterodimers |
| ATE123810T1 (de) | 1988-08-23 | 1995-06-15 | Dana Farber Cancer Inst Inc | Alpha-subeinheit des lfa-1-leukocyt-adhäsions- rezeptors. |
| EP0362531B1 (en) | 1988-09-01 | 1999-11-10 | Bayer Corporation | A human rhinovirus receptor protein that inhibits virus infectivity |
| KR900701846A (ko) | 1988-09-28 | 1990-12-04 | 원본미기재 | 세포간 점착분자 및 이의 결합 리간드 |
| US5149780A (en) | 1988-10-03 | 1992-09-22 | The Scripps Research Institute | Peptides and antibodies that inhibit integrin-ligand binding |
| EP0462184A4 (en) | 1989-03-09 | 1992-01-08 | Dana Farber Cancer Institute | Method of treating viral infections using lfa-1 |
| AU5553290A (en) | 1989-04-28 | 1990-11-29 | Baylor College Of Medicine | Dissemination of hiv-1 infected cells |
| US5135916A (en) | 1989-06-12 | 1992-08-04 | Oklahoma Medical Research Foundation | Inhibition of complement mediated inflammatory response |
| CH679207A5 (enExample) * | 1989-07-28 | 1992-01-15 | Debiopharm Sa | |
| WO1991019511A1 (en) | 1990-06-18 | 1991-12-26 | The General Hospital Corporation | CONTROLLING CELLULAR IMMUNE/INFLAMMATORY RESPONSES WITH β2 INTEGRINS |
| CA2046830C (en) | 1990-07-19 | 1999-12-14 | Patrick P. Deluca | Drug delivery system involving inter-action between protein or polypeptide and hydrophobic biodegradable polymer |
| US5318965A (en) | 1990-08-24 | 1994-06-07 | Abbott Laboratories | Quinobenzoxazine, antineoplastic agents |
| JPH06500555A (ja) | 1990-08-27 | 1994-01-20 | カイロン コーポレイション | 病気の処置のためのペプチドの薬物 |
| US5288854A (en) * | 1990-11-28 | 1994-02-22 | Center For Blood Research, Inc. | Functional derivatives of ICAM-1 which are substantially capable of binding to LFA-1 but are substantially incapable of binding to MAC-1 |
| CH683149A5 (fr) | 1991-07-22 | 1994-01-31 | Debio Rech Pharma Sa | Procédé pour la préparation de microsphères en matériau polymère biodégradable. |
| AU2777092A (en) * | 1991-10-04 | 1993-05-03 | United States Of America, Represented By The Secretary, Department Of Health And Human Services, The | Treatment of ocular inflammation by blockage of cell adhesion molecules |
| US6764681B2 (en) * | 1991-10-07 | 2004-07-20 | Biogen, Inc. | Method of prophylaxis or treatment of antigen presenting cell driven skin conditions using inhibitors of the CD2/LFA-3 interaction |
| US6162432A (en) | 1991-10-07 | 2000-12-19 | Biogen, Inc. | Method of prophylaxis or treatment of antigen presenting cell driven skin conditions using inhibitors of the CD2/LFA-3 interaction |
| WO1993017047A1 (en) * | 1992-02-28 | 1993-09-02 | Board Of Regents, The University Of Texas System | Compositions and methods for the treatment of thermal injury |
| GB9211268D0 (en) | 1992-05-28 | 1992-07-15 | Ici Plc | Salts of basic peptides with carboxyterminated polyesters |
| US5298492A (en) | 1992-08-04 | 1994-03-29 | Schering Corporation | Diamino acid derivatives as antihypertensives |
| CA2140933A1 (en) | 1992-08-21 | 1994-02-22 | Paula M. Jardieu | Method for treating an lfa-1 mediated disorder |
| DK0661989T3 (da) * | 1992-09-21 | 1998-03-02 | Upjohn Co | Proteinsammensætninger med vedvarende frigivelse |
| WO1994011400A1 (en) | 1992-11-18 | 1994-05-26 | Helsinki University Licensing Ltd. Oy | Peptides from human icam-2 and from human icam-1 and their analogs for use in therapy and diagnosis |
| US5672659A (en) | 1993-01-06 | 1997-09-30 | Kinerton Limited | Ionic molecular conjugates of biodegradable polyesters and bioactive polypeptides |
| PL174772B1 (pl) | 1993-01-06 | 1998-09-30 | Kinerton Ltd | Kompozycja farmaceutyczna zawierająca jonowy konjugat cząsteczkowy |
| US5424289A (en) * | 1993-07-30 | 1995-06-13 | Alza Corporation | Solid formulations of therapeutic proteins for gastrointestinal delivery |
| US5397791A (en) * | 1993-08-09 | 1995-03-14 | Merck & Co., Inc. | Fibrinogen receptor antagonists |
| DE59409322D1 (de) | 1993-12-03 | 2000-06-08 | Hoffmann La Roche | Essigsäurederivate als Arzneimittel |
| US5470953A (en) | 1993-12-23 | 1995-11-28 | Icos Corporation | Human β2 integrin α subunit |
| US5627264A (en) | 1994-03-03 | 1997-05-06 | Alexion Pharmaceuticals, Inc. | Chimeric complement inhibitor proteins |
| EP0762886A4 (en) | 1994-04-19 | 1999-03-31 | Univ Kansas | ICAM-1 / LFA-1 SHORT CHAIN PEPTIDES AND METHODS FOR USE THEREOF |
| US5849327A (en) | 1994-07-29 | 1998-12-15 | Advanced Polymer Systems, Inc. | Delivery of drugs to the lower gastrointestinal tract |
| US5585359A (en) | 1994-09-29 | 1996-12-17 | Merck & Co., Inc. | Inhibitors of farnesyl-protein transferase |
| ATE170179T1 (de) * | 1994-11-02 | 1998-09-15 | Merck Patent Gmbh | Adhäsionsrezeptor-antagonisten |
| US20020028798A1 (en) | 1995-12-12 | 2002-03-07 | Omeros Medical Systems | Irrigation solution and method for inhibition of pain and inflammation |
| US5612052A (en) * | 1995-04-13 | 1997-03-18 | Poly-Med, Inc. | Hydrogel-forming, self-solvating absorbable polyester copolymers, and methods for use thereof |
| US5747035A (en) * | 1995-04-14 | 1998-05-05 | Genentech, Inc. | Polypeptides with increased half-life for use in treating disorders involving the LFA-1 receptor |
| JP3133073B2 (ja) | 1995-05-29 | 2001-02-05 | ファイザー・インコーポレーテッド | 成長ホルモンの放出を促進するジペプチド類 |
| US5877224A (en) * | 1995-07-28 | 1999-03-02 | Rutgers, The State University Of New Jersey | Polymeric drug formulations |
| US5843884A (en) | 1995-11-15 | 1998-12-01 | Oklahoma Medical Research Foundation | C9 complement inhibitor |
| US5863910A (en) * | 1996-01-12 | 1999-01-26 | Bolonick; Joel | Treatment of chronic inflammatory disorders of the gastrointestinal tract |
| US5980945A (en) | 1996-01-16 | 1999-11-09 | Societe De Conseils De Recherches Et D'applications Scientifique S.A. | Sustained release drug formulations |
| US5840332A (en) | 1996-01-18 | 1998-11-24 | Perio Products Ltd. | Gastrointestinal drug delivery system |
| JP2000505068A (ja) | 1996-03-13 | 2000-04-25 | トラスティーズ・オブ・ザ・ユニバーシティ・オブ・ペンシルベニア | 補体活性化を阻害する新規ペプチド類 |
| IL126422A (en) | 1996-04-23 | 2004-02-19 | Kinerton Ltd | Biodegradable acidic polylactic polymers and methods for their preparation |
| HRP970493A2 (en) | 1996-09-23 | 1998-08-31 | Wienman E. Phlips | Oral delayed immediate release medical formulation and method for preparing the same |
| CA2217134A1 (en) * | 1996-10-09 | 1998-04-09 | Sumitomo Pharmaceuticals Co., Ltd. | Sustained release formulation |
| PT944619E (pt) * | 1996-11-27 | 2007-01-31 | Bristol Myers Squibb Pharma Co | Novos antagonistas dos receptores da integrina |
| US5968895A (en) | 1996-12-11 | 1999-10-19 | Praecis Pharmaceuticals, Inc. | Pharmaceutical formulations for sustained drug delivery |
| US5893985A (en) * | 1997-03-14 | 1999-04-13 | The Lincoln Electric Company | Plasma arc torch |
| AR012443A1 (es) | 1997-04-16 | 2000-10-18 | Uriach & Cia Sa J | Nuevas carboxamidas como inhibidores de la agregacion plaquetaria, procedimiento para su preparacion, composiciones farmaceuticas que loscontienen y uso de los mismos en la manufactura de medicamentos |
| ES2306482T3 (es) | 1997-08-28 | 2008-11-01 | Novartis Ag | Antagonistas de antigeno-1 funcion con funcion de linfocito. |
| US6541606B2 (en) * | 1997-12-31 | 2003-04-01 | Altus Biologics Inc. | Stabilized protein crystals formulations containing them and methods of making them |
| US7166568B1 (en) | 1998-02-09 | 2007-01-23 | Oklahoma Medical Research Foundation | Compositions and methods to inhibit formation of the C5b-9 complex of complement |
| CA2325986A1 (en) | 1998-03-27 | 1999-10-07 | Genentech, Inc. | Antagonists for treatment of cd11/cd18 adhesion receptor mediated disorders |
| US6331640B1 (en) | 1998-10-13 | 2001-12-18 | Hoffmann-La Roche Inc. | Diaminopropionic acid derivatives |
| CA2352389C (en) | 1998-11-27 | 2009-01-20 | Kanji Takada | An oral formulation for gastrointestinal drug delivery |
| IT1304152B1 (it) | 1998-12-10 | 2001-03-08 | Mediolanum Farmaceutici Srl | Composizioni comprendenti un peptide ed acido polilattico-glicolicoatte alla preparazione di impianti sottocutanei aventi un prolungato |
| US6867203B2 (en) | 1998-12-29 | 2005-03-15 | Abbott Laboratories | Cell adhesion-inhibiting antiinflammatory and immune-suppressive compounds |
| US6670321B1 (en) | 1998-12-30 | 2003-12-30 | The Children's Medical Center Corporation | Prevention and treatment for retinal ischemia and edema |
| NZ511219A (en) | 1999-01-05 | 2003-05-30 | Univ Southern Australia | Novel agents and methods for treatment and diagnosis of ocular disorders |
| WO2000044731A1 (en) | 1999-01-27 | 2000-08-03 | G.D. Searle & Co. | Novel hydroxyamidino carboxylate derivatives useful as nitric oxide synthase inhibitors |
| EP1028114A1 (en) * | 1999-02-13 | 2000-08-16 | Aventis Pharma Deutschland GmbH | Novel guanidine derivatives as inhibitors of cell adhesion |
| CO5140104A1 (es) | 1999-02-16 | 2002-03-22 | Novartis Ag | Derivados de mevinolina y preparacion farmaceuticas que los contienen |
| US20010006656A1 (en) * | 1999-02-17 | 2001-07-05 | University Of Washington | Methods and compositions for inhibiting inflammation associated with pulmonary disease |
| MX339071B (es) | 1999-03-31 | 2016-05-09 | Janssen Pharmaceutica Nv | Almidon pregelatinizado en una formulacion de liberacion controlada. |
| WO2000072883A2 (en) | 1999-06-02 | 2000-12-07 | Aviana Biopharm | Pharmaceutical transdermal compositions |
| WO2001001964A2 (en) | 1999-06-23 | 2001-01-11 | Sedum Laboratories, Inc. | Ionically formulated biomolecule microcarriers |
| JP4303438B2 (ja) | 1999-08-18 | 2009-07-29 | ソシエテ・ドゥ・コンセイユ・ドゥ・ルシェルシュ・エ・ダプリカーション・シャンティフィック・エス・ア・エス | ペプチドの持続放出製剤 |
| ECSP003707A (es) | 1999-10-13 | 2002-05-23 | Novartis Ag | Diazepanes |
| US6605597B1 (en) | 1999-12-03 | 2003-08-12 | Cv Therapeutics, Inc. | Partial or full A1agonists-N-6 heterocyclic 5′-thio substituted adenosine derivatives |
| US6294522B1 (en) | 1999-12-03 | 2001-09-25 | Cv Therapeutics, Inc. | N6 heterocyclic 8-modified adenosine derivatives |
| EP1237575B1 (en) | 1999-12-14 | 2008-08-06 | Genentech, Inc. | Tnf-alpha antagonist and lfa-1 antagonist for treating rheumatoid arthritis |
| US7521061B2 (en) * | 1999-12-31 | 2009-04-21 | Rutgers, The State University Of New Jersey | Pharmaceutical formulation for regulating the timed release of biologically active compounds based on a polymer matrix |
| WO2001049249A2 (en) | 1999-12-31 | 2001-07-12 | Rutgers, The State University | Pharmaceutical formulation for regulating the timed release of biologically active compounds based on a polymer matrix |
| JP4917726B2 (ja) | 1999-12-31 | 2012-04-18 | ルトガーズ、ザ ステイト ユニバーシティ オブ ニュージャージー | ポリマー混合物および活性化合物からなる徐放用医薬製剤 |
| DE60110396T2 (de) | 2000-01-14 | 2006-01-19 | Larson, Richard S., Albuquerque | Peptidische inhibitoren der lfa-1/icam-1 interaktion |
| US20030064105A1 (en) * | 2000-08-25 | 2003-04-03 | Myung-Jin Kim | Lipophilic-coated microparticle containing a protein drug and formulation comprising same |
| US6515124B2 (en) | 2000-02-09 | 2003-02-04 | Hoffman-La Roche Inc. | Dehydroamino acids |
| EP1296943A1 (fr) | 2000-05-05 | 2003-04-02 | Societe De Conseils De Recherches Et D'applications Scientifiques S.A. (S.C.R.A.S.) | Derives d'aminoacides et leur application a titre de medicaments |
| GB0011817D0 (en) | 2000-05-16 | 2000-07-05 | Pharmacia & Upjohn Spa | Antagonists of integrin receptors |
| US6521619B2 (en) | 2000-06-29 | 2003-02-18 | Icos Corporation | Aryl phenylcyclopropyl sulfide derivatives and their use as cell adhesion inhibiting anti-inflammatory and immune suppressive agents |
| AU2001268718B2 (en) | 2000-06-29 | 2006-01-05 | Abbott Laboratories | Aryl phenylheterocyclyl sulfide derivatives and their use as cell adhesion-inhibiting anti-inflammatory and immune-suppressive agents |
| AR030817A1 (es) | 2000-10-02 | 2003-09-03 | Novartis Ag | Derivados de diazacicloalcanodiona |
| GB0025208D0 (en) | 2000-10-13 | 2000-11-29 | Euro Celtique Sa | Delayed release pharmaceutical formulations |
| US6653478B2 (en) | 2000-10-27 | 2003-11-25 | Ortho-Mcneil Pharmaceutical, Inc. | Substituted benzimidazol-2-ones as vasopressin receptor antagonists and neuropeptide Y modulators |
| DE10055857A1 (de) | 2000-11-10 | 2002-08-22 | Creative Peptides Sweden Ab Dj | Neue pharmazeutische Depotformulierung |
| GB0028367D0 (en) | 2000-11-21 | 2001-01-03 | Celltech Chiroscience Ltd | Chemical compounds |
| IL155683A0 (en) | 2000-11-28 | 2003-11-23 | Genentech Inc | Lfa-1 antagonist compounds |
| AU2002227128A1 (en) * | 2000-12-01 | 2002-06-11 | Bristol-Myers Squibb Company | Hydantoin compounds useful as anti-inflammatory agents |
| WO2002050080A1 (en) | 2000-12-19 | 2002-06-27 | Boehringer Ingelheim Pharmaceuticals, Inc. | Small molecules useful in the treatment of inflammatory disease |
| WO2002058672A2 (en) | 2001-01-26 | 2002-08-01 | Debio Recherche Pharmaceutique S.A. | Microparticles of biodegradable polymer encapsulating a biologically active substance |
| DE60216830T2 (de) | 2001-02-06 | 2007-06-14 | Pfizer Products Inc., Groton | Pharmazeutische Zusammensetzungen zur Behandlung von Störungen des ZNS oder anderen Erkrankungen |
| US20030044406A1 (en) * | 2001-03-02 | 2003-03-06 | Christine Dingivan | Methods of preventing or treating inflammatory or autoimmune disorders by administering CD2 antagonists in combination with other prophylactic or therapeutic agents |
| JP2005511477A (ja) | 2001-03-19 | 2005-04-28 | プラエシス ファーマシューティカルズ インコーポレーテッド | 持続放出のための医薬調合物 |
| US6391290B1 (en) | 2001-03-21 | 2002-05-21 | Schering-Plough Healthcare Products, Inc. | Skin care compositions |
| WO2002089767A1 (en) * | 2001-05-03 | 2002-11-14 | Massachusetts Eye And Ear Infirmary | Implantable drug delivery device and use thereof |
| US6872382B1 (en) * | 2001-05-21 | 2005-03-29 | Alcon, Inc. | Use of selective PDE IV inhibitors to treat dry eye disorders |
| KR20040000507A (ko) | 2001-05-24 | 2004-01-03 | 야마노우치세이야쿠 가부시키가이샤 | 3-퀴놀린-2(1ｈ)-일리덴인돌린-2-온 유도체 |
| JP4583751B2 (ja) | 2001-06-06 | 2010-11-17 | アベンティス・フアーマ・リミテッド | 炎症性疾患の治療に使用するための置換されたテトラヒドロイソキノリン |
| AU2002320352A1 (en) | 2001-07-24 | 2003-02-17 | Biogen Idec Ma Inc. | Methods for treating or preventing sclerotic disorders using cd2-binding agents |
| DE60234264D1 (de) | 2001-10-01 | 2009-12-17 | Bristol Myers Squibb Co | Spiro-hydantoin-verbindungen, die sich als entzündungshemmende mittel eignen |
| HRP20040406A2 (en) * | 2001-11-09 | 2005-02-28 | Eyetech Pharmaceuticals | Methods for treating ocular neovascular diseases |
| IL162293A0 (en) | 2001-12-19 | 2005-11-20 | Alza Corp | Formulation and dosage form for increasing oral bioavailability of hydrophilic macromolecules |
| KR20040091100A (ko) | 2002-03-04 | 2004-10-27 | 소시에떼 더 콘세이유 더 레세르세 에 다플리까띠옹 시엔띠피끄, 에스.아.에스. | 운반체 펩타이드를 함유하는 서방형 의약 조성물 |
| WO2003103587A2 (en) * | 2002-06-06 | 2003-12-18 | Dana-Farber Cancer Institute | Compounds or agents that inhibit and induce the formation of focal microvessel dilatations |
| WO2004014365A1 (en) * | 2002-08-13 | 2004-02-19 | Warner-Lambert Company Llc | Phthalimide derivatives as matrix metalloproteinase inhibitors |
| JP2006502183A (ja) | 2002-09-20 | 2006-01-19 | アルコン，インコーポレイテッド | ドライアイ障害の処置のためのサイトカイン合成インヒビターの使用 |
| US7785578B2 (en) | 2002-10-11 | 2010-08-31 | Aciont, Inc. | Non-invasive ocular drug delivery |
| JP2007524349A (ja) * | 2003-01-16 | 2007-08-30 | ザ・トラスティーズ・オブ・ザ・ユニバーシティ・オブ・ペンシルバニア | ＩＣＡＭ−１のｓｉＲＮＡ阻害のための組成物及び方法 |
| JP4709552B2 (ja) * | 2003-02-19 | 2011-06-22 | 邦康 早田 | Ｌｆａ−１抑制剤、及びその用途 |
| EP1622609A4 (en) * | 2003-04-29 | 2008-09-03 | Smithkline Beecham Corp | METHODS OF TREATING DEGENERATIVE DISEASES / LESIONS |
| WO2005010024A2 (en) | 2003-07-22 | 2005-02-03 | Science & Technology Corporation @ Unm | Potent peptide inhibitors and methods of use |
| US7544699B2 (en) | 2003-08-08 | 2009-06-09 | Transtech Pharma, Inc. | Aryl and heteroaryl compounds, compositions, and methods of use |
| WO2005014532A1 (en) | 2003-08-08 | 2005-02-17 | Transtech Pharma, Inc. | Aryl and heteroaryl compounds, compositions and methods of use |
| SG146624A1 (en) * | 2003-09-11 | 2008-10-30 | Kemia Inc | Cytokine inhibitors |
| US7199125B2 (en) | 2003-10-02 | 2007-04-03 | Bristol-Myers Squibb Company | Spiro-cyclic compounds useful as anti-inflammatory agents |
| GB0323684D0 (en) | 2003-10-09 | 2003-11-12 | Jagotec Ag | Improvements in or relating to organic compounds |
| WO2005042710A1 (en) | 2003-10-28 | 2005-05-12 | The Government Of The United States Of America, As Represented By The Secretary, Department Of Health And Human Services | Use of statin to kill ebv-transformed b cells |
| AU2004287875B2 (en) * | 2003-11-05 | 2011-06-02 | Bausch + Lomb Ireland Limited | Modulators of cellular adhesion |
| WO2005065668A2 (en) * | 2003-12-29 | 2005-07-21 | Qlt Usa, Inc. | Topical compositions comprising halo-deoxyadenosines for treatment of skin disorders |
| KR100799802B1 (ko) * | 2004-02-04 | 2008-01-31 | 화이자 프로덕츠 인크. | 치환된 퀴놀린 화합물 |
| UA86051C2 (en) | 2004-02-04 | 2009-03-25 | Пфайзер Продактс Инк. | Substituted quinoline compounds |
| EP1740561A2 (en) | 2004-04-28 | 2007-01-10 | ICOS Corporation | Arylphenylamino-and arylphenylether-sulfide derivatives, useful for the treatment of inflammatory and immune diseases, and pharmaceutical compositions containing them |
| GT200500139A (es) | 2004-06-08 | 2005-07-25 | Metodo para la preparacion de acidos hidroxamicos | |
| EP1756163A2 (en) * | 2004-06-09 | 2007-02-28 | Genentech, Inc. | Method of treating granuloma annulare or sarcoid |
| US7375237B2 (en) | 2004-08-18 | 2008-05-20 | Bristol-Myers Squibb Company | Pyrrolizine compounds useful as anti-inflammatory agents |
| FI20041129A0 (fi) * | 2004-08-30 | 2004-08-30 | Ctt Cancer Targeting Tech Oy | Tioksotiatsolidinoniyhdisteitä lääkkeinä käytettäviksi |
| TW200616634A (en) | 2004-10-01 | 2006-06-01 | Bristol Myers Squibb Co | Crystalline forms and process for preparing spiro-hydantoin compounds |
| US20060089590A1 (en) | 2004-10-27 | 2006-04-27 | John Higuchi | Methods and devices for sustained in-vivo release of an active agent |
| US7186727B2 (en) | 2004-12-14 | 2007-03-06 | Bristol-Myers Squibb Company | Pyridyl-substituted spiro-hydantoin compounds and use thereof |
| US20060142319A1 (en) | 2004-12-14 | 2006-06-29 | Bang-Chi Chen | Pyridyl-substituted spiro-hydantoin crystalline forms and process |
| SI1881823T1 (sl) * | 2005-05-17 | 2015-04-30 | Sarcode Bioscience Inc. | Sestavki in postopki za zdravljenje bolezni oäśesa |
| US20060286108A1 (en) | 2005-06-16 | 2006-12-21 | Bell Katherine A | Topical compositions for the treatment of chronic wounds |
| DE102005029746B4 (de) * | 2005-06-24 | 2017-10-26 | Boehringer Ingelheim International Gmbh | Zerstäuber |
| US8097237B2 (en) * | 2005-08-23 | 2012-01-17 | Stc.Unm | Non-invasive diagnostic agents of cancer and methods of diagnosing cancer, especially leukemia and lymphoma |
| JP2007099641A (ja) * | 2005-09-30 | 2007-04-19 | Tsumura & Co | インドールキノキサリン類化合物、その製造方法およびそれを用いた医薬組成物 |
| US20080262070A1 (en) * | 2005-10-06 | 2008-10-23 | Karl Baumann | Pharmaceutically Active Tetrahydro-Pyrrolizinone Compounds |
| GB0520378D0 (en) | 2005-10-06 | 2005-11-16 | Novartis Ag | Organic compounds |
| EP1951665A1 (en) | 2005-11-14 | 2008-08-06 | Dominion Pharmakine S.L. | Novel inhibitors of the lfa-1/icam-1 interaction, and uses thereof |
| WO2007076358A1 (en) * | 2005-12-23 | 2007-07-05 | Alcon, Inc. | PHARMACEUTICAL FORMULATION FOR DELIVERY OF RECEPTOR TYROSINE KINASE INHIBITING (RTKi) COMPOUNDS TO THE EYE |
| CA2702984C (en) | 2007-10-19 | 2017-04-11 | Sarcode Corporation | Compositions and methods for treatment of diabetic retinopathy |
| WO2009139817A2 (en) | 2008-04-15 | 2009-11-19 | Sarcode Corporation | Crystalline pharmaceutical and methods of preparation and use thereof |
| EP3632444A3 (en) | 2008-04-15 | 2020-08-26 | SARcode Bioscience Inc. | Topical lfa-1 antagonists for use in localized treatment of immune related disorders |
| EP2276508A4 (en) | 2008-04-15 | 2011-12-28 | Sarcode Bioscience Inc | ADMINISTRATION OF LFA-1 ANTAGONISTS TO THE GASTROINTESTINAL SYSTEM |
| US8378105B2 (en) * | 2009-10-21 | 2013-02-19 | Sarcode Bioscience Inc. | Crystalline pharmaceutical and methods of preparation and use thereof |
-
2008
- 2008-10-17 CA CA2702984A patent/CA2702984C/en active Active
- 2008-10-17 US US12/288,330 patent/US20090155176A1/en not_active Abandoned
- 2008-10-17 JP JP2010529955A patent/JP5808037B2/ja not_active Expired - Fee Related
- 2008-10-17 EP EP16204718.7A patent/EP3167886B1/en active Active
- 2008-10-17 EP EP20189143.9A patent/EP3797775A1/en not_active Withdrawn
- 2008-10-17 CN CN200880117716A patent/CN101873797A/zh active Pending
- 2008-10-17 AU AU2008317473A patent/AU2008317473B2/en not_active Ceased
- 2008-10-17 MX MX2010004281A patent/MX2010004281A/es active IP Right Grant
- 2008-10-17 WO PCT/US2008/011878 patent/WO2009054914A1/en not_active Ceased
- 2008-10-17 ES ES16204718T patent/ES2830024T3/es active Active
- 2008-10-17 EP EP08842113.6A patent/EP2209371B1/en not_active Not-in-force
- 2008-10-17 CA CA3105972A patent/CA3105972A1/en not_active Abandoned
- 2008-10-17 CA CA2958665A patent/CA2958665C/en active Active
- 2008-10-17 ES ES08842113.6T patent/ES2630406T3/es active Active
-
2014
- 2014-07-14 JP JP2014144595A patent/JP2014221808A/ja active Pending
-
2015
- 2015-03-17 US US14/659,789 patent/US10960087B2/en active Active
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2021
- 2021-02-22 US US17/181,187 patent/US20210338839A1/en not_active Abandoned
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