JP2012525369A5 - - Google Patents

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Publication number

JP2012525369A5

JP2012525369A5 JP2012507839A JP2012507839A JP2012525369A5 JP 2012525369 A5 JP2012525369 A5 JP 2012525369A5 JP 2012507839 A JP2012507839 A JP 2012507839A JP 2012507839 A JP2012507839 A JP 2012507839A JP 2012525369 A5 JP2012525369 A5 JP 2012525369A5

Authority

JP

Japan

Prior art keywords

composition

use according

group

alkyl

aryl

Prior art date

2010-04-28

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.)

Pending

Links

• Espacenet
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• 239000000203 mixture Substances 0.000 claims 23
• 238000001356 surgical procedure Methods 0.000 claims 10
• 125000000217 alkyl group Chemical group 0.000 claims 7
• UEZVMMHDMIWARA-UHFFFAOYSA-M phosphonate Chemical compound [O-]P(=O)=O UEZVMMHDMIWARA-UHFFFAOYSA-M 0.000 claims 5
• 229940002612 prodrug Drugs 0.000 claims 5
• 239000000651 prodrug Substances 0.000 claims 5
• 125000003118 aryl group Chemical group 0.000 claims 4
• 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 4
• 238000000034 method Methods 0.000 claims 3
• -1 phosphonotetrahydropyran compound Chemical class 0.000 claims 3
• 208000005069 pulmonary fibrosis Diseases 0.000 claims 3
• 230000029663 wound healing Effects 0.000 claims 3
• 206010061218 Inflammation Diseases 0.000 claims 2
• YASAKCUCGLMORW-UHFFFAOYSA-N Rosiglitazone Chemical compound C=1C=CC=NC=1N(C)CCOC(C=C1)=CC=C1CC1SC(=O)NC1=O YASAKCUCGLMORW-UHFFFAOYSA-N 0.000 claims 2
• 125000002252 acyl group Chemical group 0.000 claims 2
• 150000001875 compounds Chemical class 0.000 claims 2
• 238000002316 cosmetic surgery Methods 0.000 claims 2
• 150000005690 diesters Chemical class 0.000 claims 2
• 201000010099 disease Diseases 0.000 claims 2
• 208000035475 disorder Diseases 0.000 claims 2
• 210000002615 epidermis Anatomy 0.000 claims 2
• 125000001072 heteroaryl group Chemical group 0.000 claims 2
• 230000004054 inflammatory process Effects 0.000 claims 2
• ABLZXFCXXLZCGV-UHFFFAOYSA-N phosphonic acid group Chemical group P(O)(O)=O ABLZXFCXXLZCGV-UHFFFAOYSA-N 0.000 claims 2
• 125000001424 substituent group Chemical group 0.000 claims 2
• 125000003107 substituted aryl group Chemical group 0.000 claims 2
• LMBFAGIMSUYTBN-MPZNNTNKSA-N teixobactin Chemical compound C([C@H](C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CO)C(=O)N[C@H](CCC(N)=O)C(=O)N[C@H]([C@@H](C)CC)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CO)C(=O)N[C@H]1C(N[C@@H](C)C(=O)N[C@@H](C[C@@H]2NC(=N)NC2)C(=O)N[C@H](C(=O)O[C@H]1C)[C@@H](C)CC)=O)NC)C1=CC=CC=C1 LMBFAGIMSUYTBN-MPZNNTNKSA-N 0.000 claims 2
• MZOFCQQQCNRIBI-VMXHOPILSA-N (3s)-4-[[(2s)-1-[[(2s)-1-[[(1s)-1-carboxy-2-hydroxyethyl]amino]-4-methyl-1-oxopentan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-3-[[2-[[(2s)-2,6-diaminohexanoyl]amino]acetyl]amino]-4-oxobutanoic acid Chemical compound OC[C@@H](C(O)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(O)=O)NC(=O)CNC(=O)[C@@H](N)CCCCN MZOFCQQQCNRIBI-VMXHOPILSA-N 0.000 claims 1
• VHRSUDSXCMQTMA-PJHHCJLFSA-N 6alpha-methylprednisolone Chemical compound C([C@@]12C)=CC(=O)C=C1[C@@H](C)C[C@@H]1[C@@H]2[C@@H](O)C[C@]2(C)[C@@](O)(C(=O)CO)CC[C@H]21 VHRSUDSXCMQTMA-PJHHCJLFSA-N 0.000 claims 1
• 102000008186 Collagen Human genes 0.000 claims 1
• 108010035532 Collagen Proteins 0.000 claims 1
• 108010008165 Etanercept Proteins 0.000 claims 1
• 102000010834 Extracellular Matrix Proteins Human genes 0.000 claims 1
• 108010037362 Extracellular Matrix Proteins Proteins 0.000 claims 1
• 102000016359 Fibronectins Human genes 0.000 claims 1
• 108010067306 Fibronectins Proteins 0.000 claims 1
• 208000010412 Glaucoma Diseases 0.000 claims 1
• 201000009794 Idiopathic Pulmonary Fibrosis Diseases 0.000 claims 1
• PWKSKIMOESPYIA-BYPYZUCNSA-N L-N-acetyl-Cysteine Chemical compound CC(=O)N[C@@H](CS)C(O)=O PWKSKIMOESPYIA-BYPYZUCNSA-N 0.000 claims 1
• 239000005517 L01XE01 - Imatinib Substances 0.000 claims 1
• 239000005411 L01XE02 - Gefitinib Substances 0.000 claims 1
• BYPFEZZEUUWMEJ-UHFFFAOYSA-N Pentoxifylline Chemical compound O=C1N(CCCCC(=O)C)C(=O)N(C)C2=C1N(C)C=N2 BYPFEZZEUUWMEJ-UHFFFAOYSA-N 0.000 claims 1
• 208000001647 Renal Insufficiency Diseases 0.000 claims 1
• 206010039710 Scleroderma Diseases 0.000 claims 1
• 208000021945 Tendon injury Diseases 0.000 claims 1
• 102000004887 Transforming Growth Factor beta Human genes 0.000 claims 1
• 108090001012 Transforming Growth Factor beta Proteins 0.000 claims 1
• 108060008682 Tumor Necrosis Factor Proteins 0.000 claims 1
• 102000000852 Tumor Necrosis Factor-alpha Human genes 0.000 claims 1
• JXLYSJRDGCGARV-WWYNWVTFSA-N Vinblastine Natural products O=C(O[C@H]1[C@](O)(C(=O)OC)[C@@H]2N(C)c3c(cc(c(OC)c3)[C@]3(C(=O)OC)c4[nH]c5c(c4CCN4C[C@](O)(CC)C[C@H](C3)C4)cccc5)[C@@]32[C@H]2[C@@]1(CC)C=CCN2CC3)C JXLYSJRDGCGARV-WWYNWVTFSA-N 0.000 claims 1
• 206010052428 Wound Diseases 0.000 claims 1
• 208000027418 Wounds and injury Diseases 0.000 claims 1
• 229960004308 acetylcysteine Drugs 0.000 claims 1
• HAMNKKUPIHEESI-UHFFFAOYSA-N aminoguanidine Chemical compound NNC(N)=N HAMNKKUPIHEESI-UHFFFAOYSA-N 0.000 claims 1
• XFILPEOLDIKJHX-QYZOEREBSA-N batimastat Chemical compound C([C@@H](C(=O)NC)NC(=O)[C@H](CC(C)C)[C@H](CSC=1SC=CC=1)C(=O)NO)C1=CC=CC=C1 XFILPEOLDIKJHX-QYZOEREBSA-N 0.000 claims 1
• 229950001858 batimastat Drugs 0.000 claims 1
• 229960003065 bosentan Drugs 0.000 claims 1
• GJPICJJJRGTNOD-UHFFFAOYSA-N bosentan Chemical compound COC1=CC=CC=C1OC(C(=NC(=N1)C=2N=CC=CN=2)OCCO)=C1NS(=O)(=O)C1=CC=C(C(C)(C)C)C=C1 GJPICJJJRGTNOD-UHFFFAOYSA-N 0.000 claims 1
• 230000009787 cardiac fibrosis Effects 0.000 claims 1
• 208000019425 cirrhosis of liver Diseases 0.000 claims 1
• 229920001436 collagen Polymers 0.000 claims 1
• 239000002537 cosmetic Substances 0.000 claims 1
• 230000008021 deposition Effects 0.000 claims 1
• 229960003957 dexamethasone Drugs 0.000 claims 1
• UREBDLICKHMUKA-CXSFZGCWSA-N dexamethasone Chemical compound C1CC2=CC(=O)C=C[C@]2(C)[C@]2(F)[C@@H]1[C@@H]1C[C@@H](C)[C@@](C(=O)CO)(O)[C@@]1(C)C[C@@H]2O UREBDLICKHMUKA-CXSFZGCWSA-N 0.000 claims 1
• 239000003937 drug carrier Substances 0.000 claims 1
• VLCYCQAOQCDTCN-UHFFFAOYSA-N eflornithine Chemical compound NCCCC(N)(C(F)F)C(O)=O VLCYCQAOQCDTCN-UHFFFAOYSA-N 0.000 claims 1
• 229960000403 etanercept Drugs 0.000 claims 1
• 210000002744 extracellular matrix Anatomy 0.000 claims 1
• 229960002584 gefitinib Drugs 0.000 claims 1
• XGALLCVXEZPNRQ-UHFFFAOYSA-N gefitinib Chemical compound C=12C=C(OCCCN3CCOCC3)C(OC)=CC2=NC=NC=1NC1=CC=C(F)C(Cl)=C1 XGALLCVXEZPNRQ-UHFFFAOYSA-N 0.000 claims 1
• 229910052736 halogen Inorganic materials 0.000 claims 1
• 125000005843 halogen group Chemical group 0.000 claims 1
• 229960002411 imatinib Drugs 0.000 claims 1
• KTUFNOKKBVMGRW-UHFFFAOYSA-N imatinib Chemical compound C1CN(C)CCN1CC1=CC=C(C(=O)NC=2C=C(NC=3N=C(C=CN=3)C=3C=NC=CC=3)C(C)=CC=2)C=C1 KTUFNOKKBVMGRW-UHFFFAOYSA-N 0.000 claims 1
• 208000036971 interstitial lung disease 2 Diseases 0.000 claims 1
• 208000011379 keloid formation Diseases 0.000 claims 1
• 201000006370 kidney failure Diseases 0.000 claims 1
• 210000004072 lung Anatomy 0.000 claims 1
• 229960004584 methylprednisolone Drugs 0.000 claims 1
• 229960001476 pentoxifylline Drugs 0.000 claims 1
• 229960003073 pirfenidone Drugs 0.000 claims 1
• ISWRGOKTTBVCFA-UHFFFAOYSA-N pirfenidone Chemical compound C1=C(C)C=CC(=O)N1C1=CC=CC=C1 ISWRGOKTTBVCFA-UHFFFAOYSA-N 0.000 claims 1
• 229960005205 prednisolone Drugs 0.000 claims 1
• OIGNJSKKLXVSLS-VWUMJDOOSA-N prednisolone Chemical compound O=C1C=C[C@]2(C)[C@H]3[C@@H](O)C[C@](C)([C@@](CC4)(O)C(=O)CO)[C@@H]4[C@@H]3CCC2=C1 OIGNJSKKLXVSLS-VWUMJDOOSA-N 0.000 claims 1
• 201000002793 renal fibrosis Diseases 0.000 claims 1
• 229960004586 rosiglitazone Drugs 0.000 claims 1
• 125000000547 substituted alkyl group Chemical group 0.000 claims 1
• ZRKFYGHZFMAOKI-QMGMOQQFSA-N tgfbeta Chemical compound C([C@H](NC(=O)[C@H](C(C)C)NC(=O)CNC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CC(C)C)NC(=O)CNC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](N)CCSC)C(C)C)[C@@H](C)CC)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CC=1C=CC=CC=1)C(=O)N[C@@H](C)C(=O)N1[C@@H](CCC1)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](CC=1C=CC=CC=1)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(C)C)C(=O)N1[C@@H](CCC1)C(=O)N1[C@@H](CCC1)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(O)=O)C1=CC=C(O)C=C1 ZRKFYGHZFMAOKI-QMGMOQQFSA-N 0.000 claims 1
• 210000001519 tissue Anatomy 0.000 claims 1
• 229960003048 vinblastine Drugs 0.000 claims 1
• JXLYSJRDGCGARV-XQKSVPLYSA-N vincaleukoblastine Chemical compound C([C@@H](C[C@]1(C(=O)OC)C=2C(=CC3=C([C@]45[C@H]([C@@]([C@H](OC(C)=O)[C@]6(CC)C=CCN([C@H]56)CC4)(O)C(=O)OC)N3C)C=2)OC)C[C@@](C2)(O)CC)N2CCC2=C1NC1=CC=CC=C21 JXLYSJRDGCGARV-XQKSVPLYSA-N 0.000 claims 1
• 210000001835 viscera Anatomy 0.000 claims 1
• 0 *C(OC(*)=O)OP(CC[C@]([C@@]([C@@]1O)O)O[C@](*)[C@]1N=O)(OC(*)OC(*)=O)=O Chemical compound *C(OC(*)=O)OP(CC[C@]([C@@]([C@@]1O)O)O[C@](*)[C@]1N=O)(OC(*)OC(*)=O)=O 0.000 description 2