JP2009543843A5 - - Google Patents

Info

Publication number

JP2009543843A5

JP2009543843A5 JP2009519955A JP2009519955A JP2009543843A5 JP 2009543843 A5 JP2009543843 A5 JP 2009543843A5 JP 2009519955 A JP2009519955 A JP 2009519955A JP 2009519955 A JP2009519955 A JP 2009519955A JP 2009543843 A5 JP2009543843 A5 JP 2009543843A5

Authority

JP

Japan

Prior art keywords

disease

compound

pharmaceutical composition

group

diseases

Prior art date

2007-07-13

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
• Global Dossier
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• 150000001875 compounds Chemical class 0.000 claims 12
• 239000008194 pharmaceutical composition Substances 0.000 claims 11
• KSGXQBZTULBEEQ-UHFFFAOYSA-N dabigatran etexilate Chemical compound C1=CC(C(N)=NC(=O)OCCCCCC)=CC=C1NCC1=NC2=CC(C(=O)N(CCC(=O)OCC)C=3N=CC=CC=3)=CC=C2N1C KSGXQBZTULBEEQ-UHFFFAOYSA-N 0.000 claims 10
• 229960000288 dabigatran etexilate Drugs 0.000 claims 10
• 239000002253 acid Substances 0.000 claims 8
• 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 8
• 150000003839 salts Chemical class 0.000 claims 8
• 201000010099 disease Diseases 0.000 claims 6
• 201000001474 proteinuria Diseases 0.000 claims 6
• -1 N-hydroxyamidino Chemical group 0.000 claims 5
• 229960003850 dabigatran Drugs 0.000 claims 5
• YBSJFWOBGCMAKL-UHFFFAOYSA-N dabigatran Chemical compound N=1C2=CC(C(=O)N(CCC(O)=O)C=3N=CC=CC=3)=CC=C2N(C)C=1CNC1=CC=C(C(N)=N)C=C1 YBSJFWOBGCMAKL-UHFFFAOYSA-N 0.000 claims 5
• 102000009027 Albumins Human genes 0.000 claims 4
• 108010088751 Albumins Proteins 0.000 claims 4
• AFVFQIVMOAPDHO-UHFFFAOYSA-N Methanesulfonic acid Chemical compound CS(O)(=O)=O AFVFQIVMOAPDHO-UHFFFAOYSA-N 0.000 claims 4
• 206010028980 Neoplasm Diseases 0.000 claims 4
• 208000025747 Rheumatic disease Diseases 0.000 claims 4
• 201000011510 cancer Diseases 0.000 claims 4
• 230000029142 excretion Effects 0.000 claims 4
• 208000017169 kidney disease Diseases 0.000 claims 4
• 230000004770 neurodegeneration Effects 0.000 claims 4
• 208000015122 neurodegenerative disease Diseases 0.000 claims 4
• 201000000596 systemic lupus erythematosus Diseases 0.000 claims 4
• 210000002700 urine Anatomy 0.000 claims 4
• CDPROXZBMHOBTQ-SJORKVTESA-N 2-[[(2r)-3-cyclohexyl-1-[(2s)-2-[3-(diaminomethylideneamino)propylcarbamoyl]piperidin-1-yl]-1-oxopropan-2-yl]amino]acetic acid Chemical compound NC(N)=NCCCNC(=O)[C@@H]1CCCCN1C(=O)[C@H](NCC(O)=O)CC1CCCCC1 CDPROXZBMHOBTQ-SJORKVTESA-N 0.000 claims 2
• 208000024827 Alzheimer disease Diseases 0.000 claims 2
• 208000019838 Blood disease Diseases 0.000 claims 2
• HTTJABKRGRZYRN-UHFFFAOYSA-N Heparin Chemical compound OC1C(NC(=O)C)C(O)OC(COS(O)(=O)=O)C1OC1C(OS(O)(=O)=O)C(O)C(OC2C(C(OS(O)(=O)=O)C(OC3C(C(O)C(O)C(O3)C(O)=O)OS(O)(=O)=O)C(CO)O2)NS(O)(=O)=O)C(C(O)=O)O1 HTTJABKRGRZYRN-UHFFFAOYSA-N 0.000 claims 2
• 102000007625 Hirudins Human genes 0.000 claims 2
• 108010007267 Hirudins Proteins 0.000 claims 2
• 101001098529 Homo sapiens Proteinase-activated receptor 1 Proteins 0.000 claims 2
• 101001113471 Homo sapiens Proteinase-activated receptor 4 Proteins 0.000 claims 2
• 101000713169 Homo sapiens Solute carrier family 52, riboflavin transporter, member 2 Proteins 0.000 claims 2
• 206010058467 Lung neoplasm malignant Diseases 0.000 claims 2
• 206010061902 Pancreatic neoplasm Diseases 0.000 claims 2
• 102100037136 Proteinase-activated receptor 1 Human genes 0.000 claims 2
• 102100023710 Proteinase-activated receptor 4 Human genes 0.000 claims 2
• 108090000190 Thrombin Proteins 0.000 claims 2
• 208000007536 Thrombosis Diseases 0.000 claims 2
• 208000009205 Tinnitus Diseases 0.000 claims 2
• 206010047249 Venous thrombosis Diseases 0.000 claims 2
• 229960003856 argatroban Drugs 0.000 claims 2
• KXNPVXPOPUZYGB-XYVMCAHJSA-N argatroban Chemical compound OC(=O)[C@H]1C[C@H](C)CCN1C(=O)[C@H](CCCN=C(N)N)NS(=O)(=O)C1=CC=CC2=C1NC[C@H](C)C2 KXNPVXPOPUZYGB-XYVMCAHJSA-N 0.000 claims 2
• 210000004781 brain capillary Anatomy 0.000 claims 2
• 238000002512 chemotherapy Methods 0.000 claims 2
• 208000020832 chronic kidney disease Diseases 0.000 claims 2
• 206010012601 diabetes mellitus Diseases 0.000 claims 2
• 230000006806 disease prevention Effects 0.000 claims 2
• 206010014599 encephalitis Diseases 0.000 claims 2
• 208000014951 hematologic disease Diseases 0.000 claims 2
• 208000018706 hematopoietic system disease Diseases 0.000 claims 2
• 229960002897 heparin Drugs 0.000 claims 2
• 229920000669 heparin Polymers 0.000 claims 2
• 229940006607 hirudin Drugs 0.000 claims 2
• WQPDUTSPKFMPDP-OUMQNGNKSA-N hirudin Chemical compound C([C@@H](C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N1[C@@H](CCC1)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CC=1C=CC(OS(O)(=O)=O)=CC=1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(O)=O)NC(=O)[C@H](CC(O)=O)NC(=O)CNC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC=1NC=NC=1)NC(=O)[C@H](CO)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H]1N(CCC1)C(=O)[C@H](CCCCN)NC(=O)[C@H]1N(CCC1)C(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(O)=O)NC(=O)CNC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H]1NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(O)=O)NC(=O)CNC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@H]([C@@H](C)CC)NC(=O)[C@@H]2CSSC[C@@H](C(=O)N[C@@H](CCC(O)=O)C(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(=O)N[C@H](C(NCC(=O)N[C@@H](CCC(N)=O)C(=O)NCC(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCCN)C(=O)N2)=O)CSSC1)C(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H]1NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)CNC(=O)[C@H](CO)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H](NC(=O)[C@H](CC(O)=O)NC(=O)[C@@H](NC(=O)[C@H](CC=2C=CC(O)=CC=2)NC(=O)[C@@H](NC(=O)[C@@H](N)C(C)C)C(C)C)[C@@H](C)O)CSSC1)C(C)C)[C@@H](C)O)[C@@H](C)O)C1=CC=CC=C1 WQPDUTSPKFMPDP-OUMQNGNKSA-N 0.000 claims 2
• 150000004677 hydrates Chemical class 0.000 claims 2
• 229950003291 inogatran Drugs 0.000 claims 2
• 201000005202 lung cancer Diseases 0.000 claims 2
• 208000020816 lung neoplasm Diseases 0.000 claims 2
• 206010025482 malaise Diseases 0.000 claims 2
• 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims 2
• DKWNMCUOEDMMIN-PKOBYXMFSA-N melagatran Chemical compound C1=CC(C(=N)N)=CC=C1CNC(=O)[C@H]1N(C(=O)[C@H](NCC(O)=O)C2CCCCC2)CC1 DKWNMCUOEDMMIN-PKOBYXMFSA-N 0.000 claims 2
• 229960002137 melagatran Drugs 0.000 claims 2
• 229940098779 methanesulfonic acid Drugs 0.000 claims 2
• 230000036542 oxidative stress Effects 0.000 claims 2
• 201000002528 pancreatic cancer Diseases 0.000 claims 2
• 208000008443 pancreatic carcinoma Diseases 0.000 claims 2
• 229940002612 prodrug Drugs 0.000 claims 2
• 239000000651 prodrug Substances 0.000 claims 2
• 206010039073 rheumatoid arthritis Diseases 0.000 claims 2
• 239000012453 solvate Substances 0.000 claims 2
• 229960004072 thrombin Drugs 0.000 claims 2
• 206010043554 thrombocytopenia Diseases 0.000 claims 2
• 231100000886 tinnitus Toxicity 0.000 claims 2
• 229960001522 ximelagatran Drugs 0.000 claims 2
• ZXIBCJHYVWYIKI-PZJWPPBQSA-N ximelagatran Chemical compound C1([C@@H](NCC(=O)OCC)C(=O)N2[C@@H](CC2)C(=O)NCC=2C=CC(=CC=2)C(\N)=N\O)CCCCC1 ZXIBCJHYVWYIKI-PZJWPPBQSA-N 0.000 claims 2
• CXUUEHHEZJCVMT-UHFFFAOYSA-N 2-[[4-[(Z)-N'-hydroxycarbamimidoyl]anilino]methyl]-1-methylbenzimidazole-5-carboxylic acid Chemical compound CN1C(=NC2=C1C=CC(=C2)C(=O)O)CNC2=CC=C(C=C2)C(NO)=N CXUUEHHEZJCVMT-UHFFFAOYSA-N 0.000 claims 1
• HBAQYPYDRFILMT-UHFFFAOYSA-N 8-[3-(1-cyclopropylpyrazol-4-yl)-1H-pyrazolo[4,3-d]pyrimidin-5-yl]-3-methyl-3,8-diazabicyclo[3.2.1]octan-2-one Chemical class C1(CC1)N1N=CC(=C1)C1=NNC2=C1N=C(N=C2)N1C2C(N(CC1CC2)C)=O HBAQYPYDRFILMT-UHFFFAOYSA-N 0.000 claims 1
• JGLMVXWAHNTPRF-CMDGGOBGSA-N CCN1N=C(C)C=C1C(=O)NC1=NC2=CC(=CC(OC)=C2N1C\C=C\CN1C(NC(=O)C2=CC(C)=NN2CC)=NC2=CC(=CC(OCCCN3CCOCC3)=C12)C(N)=O)C(N)=O Chemical compound CCN1N=C(C)C=C1C(=O)NC1=NC2=CC(=CC(OC)=C2N1C\C=C\CN1C(NC(=O)C2=CC(C)=NN2CC)=NC2=CC(=CC(OCCCN3CCOCC3)=C12)C(N)=O)C(N)=O JGLMVXWAHNTPRF-CMDGGOBGSA-N 0.000 claims 1
• 239000003814 drug Substances 0.000 claims 1
• 239000000203 mixture Substances 0.000 claims 1
• 238000003419 tautomerization reaction Methods 0.000 claims 1