JP2009521441A5 - - Google Patents
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- JP2009521441A5 JP2009521441A5 JP2008547342A JP2008547342A JP2009521441A5 JP 2009521441 A5 JP2009521441 A5 JP 2009521441A5 JP 2008547342 A JP2008547342 A JP 2008547342A JP 2008547342 A JP2008547342 A JP 2008547342A JP 2009521441 A5 JP2009521441 A5 JP 2009521441A5
- Authority
- JP
- Japan
- Prior art keywords
- compound
- alkenyl
- compound according
- lower alkyl
- alkyl
- 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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- 150000001875 compounds Chemical class 0.000 claims 65
- 125000000217 alkyl group Chemical group 0.000 claims 27
- 229910052739 hydrogen Inorganic materials 0.000 claims 18
- 239000001257 hydrogen Substances 0.000 claims 18
- 125000003342 alkenyl group Chemical group 0.000 claims 15
- 229910052736 halogen Inorganic materials 0.000 claims 14
- 150000002367 halogens Chemical class 0.000 claims 14
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 11
- ZMZDMBWJUHKJPS-UHFFFAOYSA-M Thiocyanate anion Chemical compound [S-]C#N ZMZDMBWJUHKJPS-UHFFFAOYSA-M 0.000 claims 10
- 150000001540 azides Chemical class 0.000 claims 10
- BWOVZCWSJFYBRM-UHFFFAOYSA-N carbononitridic isocyanate Chemical compound O=C=NC#N BWOVZCWSJFYBRM-UHFFFAOYSA-N 0.000 claims 10
- XLJMAIOERFSOGZ-UHFFFAOYSA-M cyanate Chemical compound [O-]C#N XLJMAIOERFSOGZ-UHFFFAOYSA-M 0.000 claims 10
- ZMZDMBWJUHKJPS-UHFFFAOYSA-N hydrogen thiocyanate Natural products SC#N ZMZDMBWJUHKJPS-UHFFFAOYSA-N 0.000 claims 10
- 150000002540 isothiocyanates Chemical class 0.000 claims 10
- 125000000623 heterocyclic group Chemical group 0.000 claims 9
- 239000000203 mixture Substances 0.000 claims 9
- 125000000304 alkynyl group Chemical group 0.000 claims 7
- 150000002431 hydrogen Chemical class 0.000 claims 7
- 125000003118 aryl group Chemical group 0.000 claims 6
- 108090000765 processed proteins & peptides Proteins 0.000 claims 6
- 102100036968 Dipeptidyl peptidase 8 Human genes 0.000 claims 5
- 101710087011 Dipeptidyl peptidase 8 Proteins 0.000 claims 5
- 102100036969 Dipeptidyl peptidase 9 Human genes 0.000 claims 5
- 101710087005 Dipeptidyl peptidase 9 Proteins 0.000 claims 5
- 125000003710 aryl alkyl group Chemical group 0.000 claims 5
- 125000000392 cycloalkenyl group Chemical group 0.000 claims 5
- 125000000753 cycloalkyl group Chemical group 0.000 claims 5
- 238000000034 method Methods 0.000 claims 5
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims 4
- 102000004245 Proteasome Endopeptidase Complex Human genes 0.000 claims 4
- 108090000708 Proteasome Endopeptidase Complex Proteins 0.000 claims 4
- 235000001014 amino acid Nutrition 0.000 claims 4
- 150000001413 amino acids Chemical class 0.000 claims 4
- 125000004429 atom Chemical group 0.000 claims 4
- 229910052799 carbon Inorganic materials 0.000 claims 4
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 4
- 238000000338 in vitro Methods 0.000 claims 4
- 230000002401 inhibitory effect Effects 0.000 claims 4
- NOESYZHRGYRDHS-UHFFFAOYSA-N insulin Chemical compound N1C(=O)C(NC(=O)C(CCC(N)=O)NC(=O)C(CCC(O)=O)NC(=O)C(C(C)C)NC(=O)C(NC(=O)CN)C(C)CC)CSSCC(C(NC(CO)C(=O)NC(CC(C)C)C(=O)NC(CC=2C=CC(O)=CC=2)C(=O)NC(CCC(N)=O)C(=O)NC(CC(C)C)C(=O)NC(CCC(O)=O)C(=O)NC(CC(N)=O)C(=O)NC(CC=2C=CC(O)=CC=2)C(=O)NC(CSSCC(NC(=O)C(C(C)C)NC(=O)C(CC(C)C)NC(=O)C(CC=2C=CC(O)=CC=2)NC(=O)C(CC(C)C)NC(=O)C(C)NC(=O)C(CCC(O)=O)NC(=O)C(C(C)C)NC(=O)C(CC(C)C)NC(=O)C(CC=2NC=NC=2)NC(=O)C(CO)NC(=O)CNC2=O)C(=O)NCC(=O)NC(CCC(O)=O)C(=O)NC(CCCNC(N)=N)C(=O)NCC(=O)NC(CC=3C=CC=CC=3)C(=O)NC(CC=3C=CC=CC=3)C(=O)NC(CC=3C=CC(O)=CC=3)C(=O)NC(C(C)O)C(=O)N3C(CCC3)C(=O)NC(CCCCN)C(=O)NC(C)C(O)=O)C(=O)NC(CC(N)=O)C(O)=O)=O)NC(=O)C(C(C)CC)NC(=O)C(CO)NC(=O)C(C(C)O)NC(=O)C1CSSCC2NC(=O)C(CC(C)C)NC(=O)C(NC(=O)C(CCC(N)=O)NC(=O)C(CC(N)=O)NC(=O)C(NC(=O)C(N)CC=1C=CC=CC=1)C(C)C)CC1=CN=CN1 NOESYZHRGYRDHS-UHFFFAOYSA-N 0.000 claims 4
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 4
- 230000002797 proteolythic effect Effects 0.000 claims 4
- 150000003839 salts Chemical class 0.000 claims 4
- 102100025012 Dipeptidyl peptidase 4 Human genes 0.000 claims 3
- 102000004190 Enzymes Human genes 0.000 claims 3
- 108090000790 Enzymes Proteins 0.000 claims 3
- 101710178372 Prolyl endopeptidase Proteins 0.000 claims 3
- 102100023832 Prolyl endopeptidase FAP Human genes 0.000 claims 3
- 101710129873 Prolyl endopeptidase FAP Proteins 0.000 claims 3
- 108010072866 Prostate-Specific Antigen Proteins 0.000 claims 3
- 102000007066 Prostate-Specific Antigen Human genes 0.000 claims 3
- QAOWNCQODCNURD-UHFFFAOYSA-L Sulfate Chemical compound [O-]S([O-])(=O)=O QAOWNCQODCNURD-UHFFFAOYSA-L 0.000 claims 3
- 125000004442 acylamino group Chemical group 0.000 claims 3
- 150000001408 amides Chemical class 0.000 claims 3
- 210000004899 c-terminal region Anatomy 0.000 claims 3
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 claims 3
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 3
- 239000000825 pharmaceutical preparation Substances 0.000 claims 3
- 229940127557 pharmaceutical product Drugs 0.000 claims 3
- 229940124530 sulfonamide Drugs 0.000 claims 3
- 150000003456 sulfonamides Chemical class 0.000 claims 3
- BDHFUVZGWQCTTF-UHFFFAOYSA-M sulfonate Chemical compound [O-]S(=O)=O BDHFUVZGWQCTTF-UHFFFAOYSA-M 0.000 claims 3
- 125000002813 thiocarbonyl group Chemical group *C(*)=S 0.000 claims 3
- 102000017927 CHRM1 Human genes 0.000 claims 2
- 101150073075 Chrm1 gene Proteins 0.000 claims 2
- -1 Cyano, isocyanato, thiocyanato, isothiocyanato Chemical group 0.000 claims 2
- 101000930822 Giardia intestinalis Dipeptidyl-peptidase 4 Proteins 0.000 claims 2
- 102000004366 Glucosidases Human genes 0.000 claims 2
- 108010056771 Glucosidases Proteins 0.000 claims 2
- 208000031226 Hyperlipidaemia Diseases 0.000 claims 2
- 102000004877 Insulin Human genes 0.000 claims 2
- 108090001061 Insulin Proteins 0.000 claims 2
- 229940122199 Insulin secretagogue Drugs 0.000 claims 2
- 102000004257 Potassium Channel Human genes 0.000 claims 2
- 229940123796 Prolactin inhibitor Drugs 0.000 claims 2
- 125000003295 alanine group Chemical group N[C@@H](C)C(=O)* 0.000 claims 2
- 150000001412 amines Chemical class 0.000 claims 2
- 125000000539 amino acid group Chemical class 0.000 claims 2
- 210000000227 basophil cell of anterior lobe of hypophysis Anatomy 0.000 claims 2
- 239000003795 chemical substances by application Substances 0.000 claims 2
- 125000004122 cyclic group Chemical group 0.000 claims 2
- 230000001419 dependent effect Effects 0.000 claims 2
- 239000003814 drug Substances 0.000 claims 2
- 230000004153 glucose metabolism Effects 0.000 claims 2
- 239000003112 inhibitor Substances 0.000 claims 2
- 229940125396 insulin Drugs 0.000 claims 2
- XZWYZXLIPXDOLR-UHFFFAOYSA-N metformin Chemical compound CN(C)C(=N)NC(N)=N XZWYZXLIPXDOLR-UHFFFAOYSA-N 0.000 claims 2
- 229960003105 metformin Drugs 0.000 claims 2
- 229910052760 oxygen Inorganic materials 0.000 claims 2
- 125000004437 phosphorous atom Chemical group 0.000 claims 2
- 229910052698 phosphorus Inorganic materials 0.000 claims 2
- 108020001213 potassium channel Proteins 0.000 claims 2
- 239000002464 receptor antagonist Substances 0.000 claims 2
- 229940044551 receptor antagonist Drugs 0.000 claims 2
- 125000001424 substituent group Chemical group 0.000 claims 2
- 229910052717 sulfur Inorganic materials 0.000 claims 2
- 208000001072 type 2 diabetes mellitus Diseases 0.000 claims 2
- 125000005330 8 membered heterocyclic group Chemical group 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
- 102100025892 Complement C1q tumor necrosis factor-related protein 1 Human genes 0.000 claims 1
- 108010067722 Dipeptidyl Peptidase 4 Proteins 0.000 claims 1
- BDAGIHXWWSANSR-UHFFFAOYSA-M Formate Chemical compound [O-]C=O BDAGIHXWWSANSR-UHFFFAOYSA-M 0.000 claims 1
- 101710198884 GATA-type zinc finger protein 1 Proteins 0.000 claims 1
- 108010004460 Gastric Inhibitory Polypeptide Proteins 0.000 claims 1
- 108010088406 Glucagon-Like Peptides Proteins 0.000 claims 1
- DTHNMHAUYICORS-KTKZVXAJSA-N Glucagon-like peptide 1 Chemical compound C([C@@H](C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](C)C(=O)N[C@@H](CC=1C2=CC=CC=C2NC=1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCNC(N)=N)C(N)=O)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CCC(N)=O)NC(=O)CNC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC=1C=CC(O)=CC=1)NC(=O)[C@H](CO)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](CC=1C=CC=CC=1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](C)NC(=O)[C@@H](N)CC=1N=CNC=1)[C@@H](C)O)[C@@H](C)O)C(C)C)C1=CC=CC=C1 DTHNMHAUYICORS-KTKZVXAJSA-N 0.000 claims 1
- 101800000221 Glucagon-like peptide 2 Proteins 0.000 claims 1
- 102400000326 Glucagon-like peptide 2 Human genes 0.000 claims 1
- 208000002705 Glucose Intolerance Diseases 0.000 claims 1
- WHUUTDBJXJRKMK-UHFFFAOYSA-N Glutamic acid Natural products OC(=O)C(N)CCC(O)=O WHUUTDBJXJRKMK-UHFFFAOYSA-N 0.000 claims 1
- 101000983116 Homo sapiens Pancreatic prohormone Proteins 0.000 claims 1
- 206010060378 Hyperinsulinaemia Diseases 0.000 claims 1
- 208000013016 Hypoglycemia Diseases 0.000 claims 1
- 206010022489 Insulin Resistance Diseases 0.000 claims 1
- ONIBWKKTOPOVIA-BYPYZUCNSA-N L-Proline Chemical compound OC(=O)[C@@H]1CCCN1 ONIBWKKTOPOVIA-BYPYZUCNSA-N 0.000 claims 1
- WHUUTDBJXJRKMK-VKHMYHEASA-N L-glutamic acid Chemical compound OC(=O)[C@@H](N)CCC(O)=O WHUUTDBJXJRKMK-VKHMYHEASA-N 0.000 claims 1
- 101710151321 Melanostatin Proteins 0.000 claims 1
- 208000008589 Obesity Diseases 0.000 claims 1
- 102100026844 Pancreatic prohormone Human genes 0.000 claims 1
- 102100040918 Pro-glucagon Human genes 0.000 claims 1
- 102100028427 Pro-neuropeptide Y Human genes 0.000 claims 1
- ONIBWKKTOPOVIA-UHFFFAOYSA-N Proline Natural products OC(=O)C1CCCN1 ONIBWKKTOPOVIA-UHFFFAOYSA-N 0.000 claims 1
- 229940124158 Protease/peptidase inhibitor Drugs 0.000 claims 1
- 241000269821 Scombridae Species 0.000 claims 1
- 108010086019 Secretin Proteins 0.000 claims 1
- 102100037505 Secretin Human genes 0.000 claims 1
- 230000003213 activating effect Effects 0.000 claims 1
- 239000000427 antigen Substances 0.000 claims 1
- 102000036639 antigens Human genes 0.000 claims 1
- 108091007433 antigens Proteins 0.000 claims 1
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 1
- 125000001651 cyanato group Chemical group [*]OC#N 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 150000002148 esters Chemical class 0.000 claims 1
- TWSALRJGPBVBQU-PKQQPRCHSA-N glucagon-like peptide 2 Chemical compound C([C@@H](C(=O)N[C@H](C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC=1C2=CC=CC=C2NC=1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](CC(O)=O)C(O)=O)[C@@H](C)CC)NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCSC)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CO)NC(=O)[C@H](CC=1C=CC=CC=1)NC(=O)[C@H](CO)NC(=O)CNC(=O)[C@H](CC(O)=O)NC(=O)[C@H](C)NC(=O)[C@@H](N)CC=1NC=NC=1)[C@@H](C)O)[C@@H](C)CC)C1=CC=CC=C1 TWSALRJGPBVBQU-PKQQPRCHSA-N 0.000 claims 1
- 235000013922 glutamic acid Nutrition 0.000 claims 1
- 239000004220 glutamic acid Substances 0.000 claims 1
- 201000001421 hyperglycemia Diseases 0.000 claims 1
- 230000003451 hyperinsulinaemic effect Effects 0.000 claims 1
- 201000008980 hyperinsulinism Diseases 0.000 claims 1
- 208000020346 hyperlipoproteinemia Diseases 0.000 claims 1
- 230000002218 hypoglycaemic effect Effects 0.000 claims 1
- BTNMPGBKDVTSJY-UHFFFAOYSA-N keto-phenylpyruvic acid Chemical compound OC(=O)C(=O)CC1=CC=CC=C1 BTNMPGBKDVTSJY-UHFFFAOYSA-N 0.000 claims 1
- 150000002576 ketones Chemical class 0.000 claims 1
- 235000020640 mackerel Nutrition 0.000 claims 1
- AWIJRPNMLHPLNC-UHFFFAOYSA-N methanethioic s-acid Chemical compound SC=O AWIJRPNMLHPLNC-UHFFFAOYSA-N 0.000 claims 1
- URPYMXQQVHTUDU-OFGSCBOVSA-N nucleopeptide y Chemical compound C([C@@H](C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CC=1C=CC(O)=CC=1)C(N)=O)NC(=O)[C@H](CC=1NC=NC=1)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CC=1C=CC(O)=CC=1)NC(=O)[C@H](CC=1C=CC(O)=CC=1)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](C)NC(=O)[C@H]1N(CCC1)C(=O)[C@H](C)NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CCC(O)=O)NC(=O)CNC(=O)[C@H]1N(CCC1)C(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(O)=O)NC(=O)[C@H]1N(CCC1)C(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H]1N(CCC1)C(=O)[C@@H](N)CC=1C=CC(O)=CC=1)C1=CC=C(O)C=C1 URPYMXQQVHTUDU-OFGSCBOVSA-N 0.000 claims 1
- 235000020824 obesity Nutrition 0.000 claims 1
- 239000000813 peptide hormone Substances 0.000 claims 1
- 239000000137 peptide hydrolase inhibitor Substances 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 230000036470 plasma concentration Effects 0.000 claims 1
- 201000009104 prediabetes syndrome Diseases 0.000 claims 1
- 235000013930 proline Nutrition 0.000 claims 1
- 210000002307 prostate Anatomy 0.000 claims 1
- 125000006239 protecting group Chemical group 0.000 claims 1
- 229960002101 secretin Drugs 0.000 claims 1
- OWMZNFCDEHGFEP-NFBCVYDUSA-N secretin human Chemical compound C([C@@H](C(=O)N[C@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CC(C)C)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](CCCNC(N)=N)C(=O)N[C@@H](CCC(O)=O)C(=O)NCC(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)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)N[C@@H](CCC(N)=O)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C(C)C)C(N)=O)[C@@H](C)O)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](N)CC=1NC=NC=1)[C@@H](C)O)C1=CC=CC=C1 OWMZNFCDEHGFEP-NFBCVYDUSA-N 0.000 claims 1
- 239000000758 substrate Substances 0.000 claims 1
- 230000001629 suppression Effects 0.000 claims 1
- 150000007970 thio esters Chemical class 0.000 claims 1
- DUYAAUVXQSMXQP-UHFFFAOYSA-M thioacetate Chemical compound CC([S-])=O DUYAAUVXQSMXQP-UHFFFAOYSA-M 0.000 claims 1
- 0 C*C(CCC1C)N1C(C(*)N(*)I)=S Chemical compound C*C(CCC1C)N1C(C(*)N(*)I)=S 0.000 description 1
- PADUPDZPAMBNNR-UHFFFAOYSA-N CC(B(O)O)NC(C1NCCC1)=S Chemical compound CC(B(O)O)NC(C1NCCC1)=S PADUPDZPAMBNNR-UHFFFAOYSA-N 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US75201705P | 2005-12-19 | 2005-12-19 | |
| US60/752,017 | 2005-12-19 | ||
| PCT/US2006/047853 WO2007100374A2 (en) | 2005-12-19 | 2006-12-15 | Soft protease inhibitors and pro-soft forms thereof |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2009521441A JP2009521441A (ja) | 2009-06-04 |
| JP2009521441A5 true JP2009521441A5 (https=) | 2010-02-12 |
| JP5270369B2 JP5270369B2 (ja) | 2013-08-21 |
Family
ID=38459469
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2008547342A Expired - Fee Related JP5270369B2 (ja) | 2005-12-19 | 2006-12-15 | ソフトプロテアーゼ抑制剤およびそのプロソフト型 |
Country Status (11)
| Country | Link |
|---|---|
| US (5) | US8268880B2 (https=) |
| EP (1) | EP1973548A4 (https=) |
| JP (1) | JP5270369B2 (https=) |
| KR (2) | KR20080077024A (https=) |
| CN (1) | CN101379069A (https=) |
| AU (1) | AU2006339348B2 (https=) |
| BR (1) | BRPI0620027A2 (https=) |
| CA (1) | CA2633803A1 (https=) |
| IL (1) | IL192134A (https=) |
| NO (1) | NO20083216L (https=) |
| WO (1) | WO2007100374A2 (https=) |
Families Citing this family (34)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP5270369B2 (ja) * | 2005-12-19 | 2013-08-21 | タフツ ユニバーシティー／トラスティーズ オブ タフツ カレッジ | ソフトプロテアーゼ抑制剤およびそのプロソフト型 |
| WO2008116054A1 (en) * | 2007-03-20 | 2008-09-25 | Trustees Of Tufts College | Inhibitors of fibroblast activation protein, and methods of use thereof |
| EP2025674A1 (de) | 2007-08-15 | 2009-02-18 | sanofi-aventis | Substituierte Tetrahydronaphthaline, Verfahren zu ihrer Herstellung und ihre Verwendung als Arzneimittel |
| US7838673B2 (en) | 2007-10-16 | 2010-11-23 | Millennium Pharmaceuticals, Inc. | Proteasome inhibitors |
| WO2009051581A1 (en) * | 2007-10-16 | 2009-04-23 | Millennium Pharmaceuticals, Inc. | Proteasome inhibitors |
| CN101896818B (zh) | 2007-12-10 | 2016-01-20 | 霍夫曼-拉罗奇有限公司 | 作为癌症的标记物的Seprase |
| FR2942409B1 (fr) * | 2009-02-20 | 2013-07-26 | Natacha Voillot | Composition pharmaceutique pour la prevention des avortements a repetition. |
| EP2400976B1 (en) * | 2009-02-27 | 2016-12-14 | Trustees Of Tufts College | Soft protease inhibitors, and pro-soft forms thereof |
| WO2011107494A1 (de) | 2010-03-03 | 2011-09-09 | Sanofi | Neue aromatische glykosidderivate, diese verbindungen enthaltende arzneimittel und deren verwendung |
| EP2582709B1 (de) | 2010-06-18 | 2018-01-24 | Sanofi | Azolopyridin-3-on-derivate als inhibitoren von lipasen und phospholipasen |
| US8530413B2 (en) | 2010-06-21 | 2013-09-10 | Sanofi | Heterocyclically substituted methoxyphenyl derivatives with an oxo group, processes for preparation thereof and use thereof as medicaments |
| TW201221505A (en) | 2010-07-05 | 2012-06-01 | Sanofi Sa | Aryloxyalkylene-substituted hydroxyphenylhexynoic acids, process for preparation thereof and use thereof as a medicament |
| TW201215387A (en) | 2010-07-05 | 2012-04-16 | Sanofi Aventis | Spirocyclically substituted 1,3-propane dioxide derivatives, processes for preparation thereof and use thereof as a medicament |
| TW201215388A (en) | 2010-07-05 | 2012-04-16 | Sanofi Sa | (2-aryloxyacetylamino)phenylpropionic acid derivatives, processes for preparation thereof and use thereof as medicaments |
| EP2683699B1 (de) | 2011-03-08 | 2015-06-24 | Sanofi | Di- und trisubstituierte oxathiazinderivate, verfahren zu deren herstellung, ihre verwendung als medikament sowie sie enthaltendes arzneimittel und deren verwendung |
| EP2766349B1 (de) | 2011-03-08 | 2016-06-01 | Sanofi | Mit carbozyklen oder heterozyklen substituierte oxathiazinderivate, verfahren zu deren herstellung, diese verbindungen enthaltende arzneimittel und deren verwendung |
| WO2012120056A1 (de) | 2011-03-08 | 2012-09-13 | Sanofi | Tetrasubstituierte oxathiazinderivate, verfahren zu deren herstellung, ihre verwendung als medikament sowie sie enthaltendes arzneimittel und deren verwendung |
| EP2683704B1 (de) | 2011-03-08 | 2014-12-17 | Sanofi | Verzweigte oxathiazinderivate, verfahren zu deren herstellung, ihre verwendung als medikament sowie sie enthaltendes arzneimittel und deren verwendung |
| US8828994B2 (en) | 2011-03-08 | 2014-09-09 | Sanofi | Di- and tri-substituted oxathiazine derivatives, method for the production thereof, use thereof as medicine and drug containing said derivatives and use thereof |
| PL2753334T3 (pl) * | 2011-08-30 | 2022-12-12 | Trustees Of Tufts College | Aktywowane przez fap inhibitory proteasomu do leczenia guzów litych |
| WO2013037390A1 (en) | 2011-09-12 | 2013-03-21 | Sanofi | 6-(4-hydroxy-phenyl)-3-styryl-1h-pyrazolo[3,4-b]pyridine-4-carboxylic acid amide derivatives as kinase inhibitors |
| WO2013045413A1 (en) | 2011-09-27 | 2013-04-04 | Sanofi | 6-(4-hydroxy-phenyl)-3-alkyl-1h-pyrazolo[3,4-b]pyridine-4-carboxylic acid amide derivatives as kinase inhibitors |
| WO2013078059A1 (en) * | 2011-11-22 | 2013-05-30 | Trustees Of Tufts College | Small molecule enhancer for dendritic cell cancer vaccines |
| WO2014022636A1 (en) * | 2012-08-02 | 2014-02-06 | Trustees Of Tufts College | Broad spectrum inhibitors of the post proline cleaving enzymes for treatment of hepatitis c virus infections |
| US20150297573A1 (en) | 2012-10-24 | 2015-10-22 | INSERM (Institut National de la Santé et de la Recherche Médicale) | TPL2 KINASE INHIBITORS FOR PREVENTING OR TREATING DIABETES AND FOR PROMOTING Beta-CELL SURVIVAL |
| US10426818B2 (en) | 2015-03-24 | 2019-10-01 | Inserm (Institut National De La Sante Et De La Recherche Medicale) | Method and pharmaceutical composition for use in the treatment of diabetes |
| US11583516B2 (en) * | 2016-09-07 | 2023-02-21 | Trustees Of Tufts College | Dash inhibitors, and uses related thereto |
| WO2018144867A1 (en) * | 2017-02-03 | 2018-08-09 | Vanderbilt University | Systems, compositions and methods for treating diabetes |
| US11559537B2 (en) | 2017-04-07 | 2023-01-24 | Trustees Of Tufts College | Combination therapies using caspase-1 dependent anticancer agents and PGE2 antagonists |
| CN108929340B (zh) * | 2017-05-22 | 2019-12-13 | 北京大学 | 脯氨酸硼酸类化合物及其制备方法和用途 |
| MX2020004421A (es) * | 2017-10-30 | 2020-09-25 | Carmentix Pte Ltd | Biomarcadores de parto prematuro. |
| WO2020006367A1 (en) * | 2018-06-29 | 2020-01-02 | Tufts Medical Center, Inc. | Methods and compositions for preventing and treating metabolic syndrome induced by antipsychotic treatment and related diseases and conditions |
| WO2020047185A1 (en) * | 2018-08-31 | 2020-03-05 | Texas Tech University System | Enhancers of neurolysin activity |
| CN117603084A (zh) * | 2023-12-18 | 2024-02-27 | 江苏瑞思坦生物科技有限公司 | 肽酶神经溶素增强剂及其制备方法和应用 |
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| Publication number | Priority date | Publication date | Assignee | Title |
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| JPH03220179A (ja) * | 1990-01-23 | 1991-09-27 | Chisso Corp | 新規な環状ジペプチド誘導体及びその製造法 |
| US6825169B1 (en) * | 1991-10-22 | 2004-11-30 | Trustees Of Tufts College | Inhibitors of dipeptidyl-aminopeptidase type IV |
| MX9206628A (es) | 1991-11-22 | 1993-05-01 | Boehringer Ingelheim Pharma | Ester de prolinaboronato y metodo para su preparacion. |
| WO1995011689A1 (en) * | 1993-10-29 | 1995-05-04 | Trustees Of Tufts College | Use of inhibitors of dipeptidyl-aminopeptidase to block entry of hiv into cells |
| IL111785A0 (en) * | 1993-12-03 | 1995-01-24 | Ferring Bv | Dp-iv inhibitors and pharmaceutical compositions containing them |
| EP2583675A1 (en) * | 1998-02-02 | 2013-04-24 | Trustees Of Tufts College | Use of dipeptidylpeptidase inhibitors to regulate glucose metabolism |
| US6890904B1 (en) * | 1999-05-25 | 2005-05-10 | Point Therapeutics, Inc. | Anti-tumor agents |
| TWI243162B (en) * | 2000-11-10 | 2005-11-11 | Taisho Pharmaceutical Co Ltd | Cyanopyrrolidine derivatives |
| WO2003045228A2 (en) * | 2001-11-26 | 2003-06-05 | Trustees Of Tufts College | Methods for treating autoimmune disorders, and reagents related thereto |
| EP2316470A3 (en) * | 2001-11-26 | 2011-08-24 | Trustees Of Tufts College | Peptidomimetic inhibitors of post-proline cleaving enzymes |
| JP2007511467A (ja) * | 2003-05-14 | 2007-05-10 | タケダ サン ディエゴ インコーポレイテッド | ジペプチジルペプチダーゼインヒビター |
| AU2005216970B2 (en) * | 2004-02-23 | 2011-07-07 | Trustees Of Tufts College | Inhibitors of dipeptidylpeptidase IV for regulating glucose metabolism |
| JP5270369B2 (ja) * | 2005-12-19 | 2013-08-21 | タフツ ユニバーシティー／トラスティーズ オブ タフツ カレッジ | ソフトプロテアーゼ抑制剤およびそのプロソフト型 |
-
2006
- 2006-12-15 JP JP2008547342A patent/JP5270369B2/ja not_active Expired - Fee Related
- 2006-12-15 BR BRPI0620027-3A patent/BRPI0620027A2/pt not_active IP Right Cessation
- 2006-12-15 CN CNA2006800529362A patent/CN101379069A/zh active Pending
- 2006-12-15 KR KR1020087017430A patent/KR20080077024A/ko not_active Ceased
- 2006-12-15 CA CA002633803A patent/CA2633803A1/en not_active Abandoned
- 2006-12-15 EP EP06849964A patent/EP1973548A4/en not_active Withdrawn
- 2006-12-15 KR KR1020147024336A patent/KR20150003157A/ko not_active Ceased
- 2006-12-15 AU AU2006339348A patent/AU2006339348B2/en not_active Ceased
- 2006-12-15 WO PCT/US2006/047853 patent/WO2007100374A2/en not_active Ceased
- 2006-12-15 US US12/096,876 patent/US8268880B2/en not_active Expired - Fee Related
-
2008
- 2008-06-12 IL IL192134A patent/IL192134A/en not_active IP Right Cessation
- 2008-07-18 NO NO20083216A patent/NO20083216L/no not_active Application Discontinuation
-
2012
- 2012-09-14 US US13/617,790 patent/US8563533B2/en not_active Expired - Fee Related
-
2013
- 2013-09-30 US US14/041,201 patent/US8933056B2/en not_active Expired - Fee Related
-
2014
- 2014-12-16 US US14/572,015 patent/US9192646B2/en not_active Expired - Fee Related
-
2015
- 2015-11-04 US US14/932,560 patent/US20160250237A1/en not_active Abandoned
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