JP2005511636A5 - - Google Patents
Download PDFInfo
- Publication number
- JP2005511636A5 JP2005511636A5 JP2003546737A JP2003546737A JP2005511636A5 JP 2005511636 A5 JP2005511636 A5 JP 2005511636A5 JP 2003546737 A JP2003546737 A JP 2003546737A JP 2003546737 A JP2003546737 A JP 2003546737A JP 2005511636 A5 JP2005511636 A5 JP 2005511636A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- alkenyl
- alkynyl
- hydrogen
- halogen
- 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.)
- Pending
Links
- 229910052739 hydrogen Inorganic materials 0.000 claims 68
- 239000001257 hydrogen Substances 0.000 claims 68
- 125000000217 alkyl group Chemical group 0.000 claims 66
- 125000003342 alkenyl group Chemical group 0.000 claims 49
- 125000003118 aryl group Chemical group 0.000 claims 39
- 150000002431 hydrogen Chemical class 0.000 claims 38
- 229910052736 halogen Inorganic materials 0.000 claims 37
- 150000002367 halogens Chemical class 0.000 claims 37
- 125000000623 heterocyclic group Chemical group 0.000 claims 35
- 108090000765 processed proteins & peptides Proteins 0.000 claims 34
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 30
- 125000000753 cycloalkyl group Chemical group 0.000 claims 30
- 125000000304 alkynyl group Chemical group 0.000 claims 28
- 210000004899 c-terminal region Anatomy 0.000 claims 28
- 125000003710 aryl alkyl group Chemical group 0.000 claims 26
- 125000000392 cycloalkenyl group Chemical group 0.000 claims 25
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 22
- 125000006239 protecting group Chemical group 0.000 claims 17
- 229940024606 amino acid Drugs 0.000 claims 15
- 125000000539 amino acid group Chemical class 0.000 claims 14
- 150000001413 amino acids Chemical class 0.000 claims 14
- 125000004429 atom Chemical group 0.000 claims 14
- 239000003112 inhibitor Substances 0.000 claims 13
- 125000004093 cyano group Chemical group *C#N 0.000 claims 11
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 11
- 125000001165 hydrophobic group Chemical group 0.000 claims 10
- 150000003839 salts Chemical class 0.000 claims 7
- YCKRFDGAMUMZLT-UHFFFAOYSA-N Fluorine atom Chemical compound [F] YCKRFDGAMUMZLT-UHFFFAOYSA-N 0.000 claims 6
- 108010084214 Peptide PHI Proteins 0.000 claims 6
- 239000000132 Peptide PHI Substances 0.000 claims 6
- 150000001408 amides Chemical class 0.000 claims 6
- 229910052731 fluorine Inorganic materials 0.000 claims 6
- 239000011737 fluorine Substances 0.000 claims 6
- QAOWNCQODCNURD-UHFFFAOYSA-L Sulfate Chemical compound [O-]S([O-])(=O)=O QAOWNCQODCNURD-UHFFFAOYSA-L 0.000 claims 5
- 125000004442 acylamino group Chemical group 0.000 claims 5
- 150000001412 amines Chemical class 0.000 claims 5
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 claims 5
- 125000001316 cycloalkyl alkyl group Chemical group 0.000 claims 5
- 125000004475 heteroaralkyl group Chemical group 0.000 claims 5
- 125000001072 heteroaryl group Chemical group 0.000 claims 5
- DYMRYCZRMAHYKE-UHFFFAOYSA-N n-diazonitramide Chemical compound [O-][N+](=O)N=[N+]=[N-] DYMRYCZRMAHYKE-UHFFFAOYSA-N 0.000 claims 5
- 229910052760 oxygen Inorganic materials 0.000 claims 5
- 125000004437 phosphorous atom Chemical group 0.000 claims 5
- 229910052698 phosphorus Inorganic materials 0.000 claims 5
- 229940124530 sulfonamide Drugs 0.000 claims 5
- 150000003456 sulfonamides Chemical class 0.000 claims 5
- BDHFUVZGWQCTTF-UHFFFAOYSA-M sulfonate Chemical compound [O-]S(=O)=O BDHFUVZGWQCTTF-UHFFFAOYSA-M 0.000 claims 5
- 229910052717 sulfur Inorganic materials 0.000 claims 5
- 125000002813 thiocarbonyl group Chemical group *C(*)=S 0.000 claims 5
- SGAKZYXFPNRMLP-RMYDINGBSA-N 3b3-081716 Chemical compound C([C@@H](C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H]([C@@H](C)CC)C(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCCN)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCC(N)=O)NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](CO)NC(=O)[C@H](CC=1C=CC(O)=CC=1)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](CC(O)=O)NC(=O)[C@H](C)NC(=O)[C@@H](N)CC=1NC=NC=1)C(C)C)[C@@H](C)O)C1=CC=C(O)C=C1 SGAKZYXFPNRMLP-RMYDINGBSA-N 0.000 claims 4
- 208000023275 Autoimmune disease Diseases 0.000 claims 4
- 102000016622 Dipeptidyl Peptidase 4 Human genes 0.000 claims 3
- 101000930822 Giardia intestinalis Dipeptidyl-peptidase 4 Proteins 0.000 claims 3
- 108091005804 Peptidases Proteins 0.000 claims 3
- 108010004684 Pituitary adenylate cyclase-activating polypeptide Proteins 0.000 claims 3
- 102000002808 Pituitary adenylate cyclase-activating polypeptide Human genes 0.000 claims 3
- 239000004365 Protease Substances 0.000 claims 3
- 102100037486 Reverse transcriptase/ribonuclease H Human genes 0.000 claims 3
- 125000004122 cyclic group Chemical group 0.000 claims 3
- 125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 claims 3
- 125000000524 functional group Chemical group 0.000 claims 3
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 3
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 3
- 235000019419 proteases Nutrition 0.000 claims 3
- 125000001424 substituent group Chemical group 0.000 claims 3
- URJOZSLMTIRWFW-QGZVFWFLSA-N (4r)-4-(1,3-benzodioxol-5-yl)-5,6-dimethoxy-4,9-dihydro-1h-benzo[f][2]benzofuran-3-one Chemical compound C1=C2OCOC2=CC([C@H]2C3=C(COC3=O)CC3=CC=C(C(=C32)OC)OC)=C1 URJOZSLMTIRWFW-QGZVFWFLSA-N 0.000 claims 2
- YNXLOPYTAAFMTN-SBUIBGKBSA-N C([C@H](N)C(=O)N1CCC[C@H]1C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CCCCN)C(=O)N1[C@@H](CCC1)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](C)C(=O)N1[C@@H](CCC1)C(=O)NCC(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CC(O)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)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(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CC=1C=CC(O)=CC=1)C(=O)N[C@@H](CC=1C=CC(O)=CC=1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CC=1NC=NC=1)C(=O)N[C@@H](CC=1C=CC(O)=CC=1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C(C)C)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)C1=CC=C(O)C=C1 Chemical compound C([C@H](N)C(=O)N1CCC[C@H]1C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CCCCN)C(=O)N1[C@@H](CCC1)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](C)C(=O)N1[C@@H](CCC1)C(=O)NCC(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CC(O)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)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(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CC=1C=CC(O)=CC=1)C(=O)N[C@@H](CC=1C=CC(O)=CC=1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CC=1NC=NC=1)C(=O)N[C@@H](CC=1C=CC(O)=CC=1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C(C)C)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)C1=CC=C(O)C=C1 YNXLOPYTAAFMTN-SBUIBGKBSA-N 0.000 claims 2
- 102400000320 Glicentin Human genes 0.000 claims 2
- 101800002945 Glicentin Proteins 0.000 claims 2
- 101800000221 Glucagon-like peptide 2 Proteins 0.000 claims 2
- 239000000095 Growth Hormone-Releasing Hormone Substances 0.000 claims 2
- 208000022559 Inflammatory bowel disease Diseases 0.000 claims 2
- 229910003867 O—B—O Inorganic materials 0.000 claims 2
- 102400000978 PACAP-related peptide Human genes 0.000 claims 2
- 101800002869 PACAP-related peptide Proteins 0.000 claims 2
- -1 PG126-158) Chemical compound 0.000 claims 2
- 108010088847 Peptide YY Proteins 0.000 claims 2
- 102100029909 Peptide YY Human genes 0.000 claims 2
- 102100040918 Pro-glucagon Human genes 0.000 claims 2
- 108010086019 Secretin Proteins 0.000 claims 2
- 102100037505 Secretin Human genes 0.000 claims 2
- 102100022831 Somatoliberin Human genes 0.000 claims 2
- 101710142969 Somatoliberin Proteins 0.000 claims 2
- 102000055135 Vasoactive Intestinal Peptide Human genes 0.000 claims 2
- 108010003205 Vasoactive Intestinal Peptide Proteins 0.000 claims 2
- 230000002496 gastric effect Effects 0.000 claims 2
- 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 2
- 230000002401 inhibitory effect Effects 0.000 claims 2
- YLBIOQUUAYXLJJ-WZUUGAJWSA-N peptide histidine methionine Chemical compound C([C@@H](C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCSC)C(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCCN)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCC(N)=O)NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](CC=1C=CC=CC=1)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](CC(O)=O)NC(=O)[C@H](C)NC(=O)[C@@H](N)CC=1N=CNC=1)C(C)C)[C@@H](C)O)C1=CC=C(O)C=C1 YLBIOQUUAYXLJJ-WZUUGAJWSA-N 0.000 claims 2
- 239000000813 peptide hormone Substances 0.000 claims 2
- IVDFJHOHABJVEH-UHFFFAOYSA-N pinacol Chemical compound CC(C)(O)C(C)(C)O IVDFJHOHABJVEH-UHFFFAOYSA-N 0.000 claims 2
- 229960002101 secretin Drugs 0.000 claims 2
- 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 2
- HFDKKNHCYWNNNQ-YOGANYHLSA-N 75976-10-2 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](CCSC)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N1[C@@H](CCC1)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](CCCNC(N)=N)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CC=1C=CC(O)=CC=1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCSC)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H]1N(CCC1)C(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(O)=O)NC(=O)CNC(=O)[C@H]1N(CCC1)C(=O)[C@H](CC=1C=CC(O)=CC=1)NC(=O)[C@@H](NC(=O)[C@H]1N(CCC1)C(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H]1N(CCC1)C(=O)[C@H](C)N)C(C)C)[C@@H](C)O)C1=CC=C(O)C=C1 HFDKKNHCYWNNNQ-YOGANYHLSA-N 0.000 claims 1
- WPWUFUBLGADILS-WDSKDSINSA-N Ala-Pro Chemical compound C[C@H](N)C(=O)N1CCC[C@H]1C(O)=O WPWUFUBLGADILS-WDSKDSINSA-N 0.000 claims 1
- 102400000113 Calcitonin Human genes 0.000 claims 1
- 108060001064 Calcitonin Proteins 0.000 claims 1
- 208000011231 Crohn disease Diseases 0.000 claims 1
- QGWNDRXFNXRZMB-UUOKFMHZSA-N GDP Chemical compound C1=2NC(N)=NC(=O)C=2N=CN1[C@@H]1O[C@H](COP(O)(=O)OP(O)(O)=O)[C@@H](O)[C@H]1O QGWNDRXFNXRZMB-UUOKFMHZSA-N 0.000 claims 1
- 108010004460 Gastric Inhibitory Polypeptide Proteins 0.000 claims 1
- 102400000921 Gastrin Human genes 0.000 claims 1
- 108010052343 Gastrins Proteins 0.000 claims 1
- 101800001226 Glicentin-related polypeptide Proteins 0.000 claims 1
- 102000051325 Glucagon Human genes 0.000 claims 1
- 108060003199 Glucagon Proteins 0.000 claims 1
- 102400000326 Glucagon-like peptide 2 Human genes 0.000 claims 1
- 102400000319 Oxyntomodulin Human genes 0.000 claims 1
- 101800001388 Oxyntomodulin Proteins 0.000 claims 1
- 102000018886 Pancreatic Polypeptide Human genes 0.000 claims 1
- RWCOTTLHDJWHRS-YUMQZZPRSA-N Pro-Pro Chemical compound OC(=O)[C@@H]1CCCN1C(=O)[C@H]1NCCC1 RWCOTTLHDJWHRS-YUMQZZPRSA-N 0.000 claims 1
- 206010040070 Septic Shock Diseases 0.000 claims 1
- 101000983124 Sus scrofa Pancreatic prohormone precursor Proteins 0.000 claims 1
- 206010067584 Type 1 diabetes mellitus Diseases 0.000 claims 1
- 102400000194 Vasostatin-1 Human genes 0.000 claims 1
- 102400000195 Vasostatin-2 Human genes 0.000 claims 1
- UDMBCSSLTHHNCD-KQYNXXCUSA-N adenosine 5'-monophosphate Chemical compound C1=NC=2C(N)=NC=NC=2N1[C@@H]1O[C@H](COP(O)(O)=O)[C@@H](O)[C@H]1O UDMBCSSLTHHNCD-KQYNXXCUSA-N 0.000 claims 1
- 108010087924 alanylproline Proteins 0.000 claims 1
- 125000003545 alkoxy group Chemical group 0.000 claims 1
- 150000001602 bicycloalkyls Chemical group 0.000 claims 1
- 125000005382 boronyl group Chemical group 0.000 claims 1
- BBBFJLBPOGFECG-VJVYQDLKSA-N calcitonin Chemical compound N([C@H](C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC=1NC=NC=1)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](CC=1C=CC(O)=CC=1)C(=O)N1[C@@H](CCC1)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H]([C@@H](C)O)C(=O)NCC(=O)N[C@@H](CO)C(=O)NCC(=O)N[C@@H]([C@@H](C)O)C(=O)N1[C@@H](CCC1)C(N)=O)C(C)C)C(=O)[C@@H]1CSSC[C@H](N)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N[C@@H]([C@@H](C)O)C(=O)N1 BBBFJLBPOGFECG-VJVYQDLKSA-N 0.000 claims 1
- 229960004015 calcitonin Drugs 0.000 claims 1
- 229910052799 carbon Inorganic materials 0.000 claims 1
- 210000004027 cell Anatomy 0.000 claims 1
- AOXOCDRNSPFDPE-UKEONUMOSA-N chembl413654 Chemical compound C([C@H](C(=O)NCC(=O)N[C@H](CC=1C2=CC=CC=C2NC=1)C(=O)N[C@H](CCSC)C(=O)N[C@H](CC(O)=O)C(=O)N[C@H](CC=1C=CC=CC=1)C(N)=O)NC(=O)[C@@H](C)NC(=O)[C@@H](CCC(O)=O)NC(=O)[C@@H](CCC(O)=O)NC(=O)[C@@H](CCC(O)=O)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC=1C2=CC=CC=C2NC=1)NC(=O)[C@H]1N(CCC1)C(=O)CNC(=O)[C@@H](N)CCC(O)=O)C1=CC=C(O)C=C1 AOXOCDRNSPFDPE-UKEONUMOSA-N 0.000 claims 1
- MASNOZXLGMXCHN-ZLPAWPGGSA-N glucagon Chemical compound C([C@@H](C(=O)N[C@H](C(=O)N[C@@H](CCC(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](CCSC)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H]([C@@H](C)O)C(O)=O)C(C)C)NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC=1C=CC(O)=CC=1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](CC=1C=CC(O)=CC=1)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(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](N)CC=1NC=NC=1)[C@@H](C)O)[C@@H](C)O)C1=CC=CC=C1 MASNOZXLGMXCHN-ZLPAWPGGSA-N 0.000 claims 1
- 229960004666 glucagon Drugs 0.000 claims 1
- PXZWGQLGAKCNKD-DPNMSELWSA-N molport-023-276-326 Chemical compound C([C@@H](C(=O)N[C@H](C(=O)N[C@@H](CCC(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](CCSC)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](C)C(O)=O)[C@@H](C)O)C(C)C)NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC=1C=CC(O)=CC=1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](CC=1C=CC(O)=CC=1)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(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](N)CC=1NC=NC=1)[C@@H](C)O)[C@@H](C)O)C1=CC=CC=C1 PXZWGQLGAKCNKD-DPNMSELWSA-N 0.000 claims 1
- 201000006417 multiple sclerosis Diseases 0.000 claims 1
- BPGXUIVWLQTVLZ-OFGSCBOVSA-N neuropeptide y(npy) 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](CCCN=C(N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CC=1C=CC(O)=CC=1)C(O)=O)NC(=O)[C@H](CC=1N=CNC=1)NC(=O)[C@H](CCCN=C(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](CCCN=C(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 BPGXUIVWLQTVLZ-OFGSCBOVSA-N 0.000 claims 1
- 229910052757 nitrogen Inorganic materials 0.000 claims 1
- 239000000816 peptidomimetic Substances 0.000 claims 1
- 230000001817 pituitary effect Effects 0.000 claims 1
- GCYXWQUSHADNBF-AAEALURTSA-N preproglucagon 78-108 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(=O)NCC(O)=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 GCYXWQUSHADNBF-AAEALURTSA-N 0.000 claims 1
- 102000004196 processed proteins & peptides Human genes 0.000 claims 1
- 108010077112 prolyl-proline Proteins 0.000 claims 1
- 230000036303 septic shock Effects 0.000 claims 1
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 claims 1
- 230000017423 tissue regeneration Effects 0.000 claims 1
- 108010059391 vasostatin I Proteins 0.000 claims 1
- 108010077020 vasostatin II Proteins 0.000 claims 1
- WKTRAVJHIBQIPC-RXMQYKEDSA-N CC[C@@H](C)[NH+](C)[O-] Chemical compound CC[C@@H](C)[NH+](C)[O-] WKTRAVJHIBQIPC-RXMQYKEDSA-N 0.000 description 2
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US33369101P | 2001-11-26 | 2001-11-26 | |
| PCT/US2002/038347 WO2003045228A2 (en) | 2001-11-26 | 2002-11-26 | Methods for treating autoimmune disorders, and reagents related thereto |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2010172410A Division JP2010248251A (ja) | 2001-11-26 | 2010-07-30 | 自己免疫疾患の治療方法及びそれに関する試薬 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2005511636A JP2005511636A (ja) | 2005-04-28 |
| JP2005511636A5 true JP2005511636A5 (https=) | 2006-01-19 |
Family
ID=23303859
Family Applications (4)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2003546737A Pending JP2005511636A (ja) | 2001-11-26 | 2002-11-26 | 自己免疫疾患の治療方法及びそれに関する試薬 |
| JP2010172410A Pending JP2010248251A (ja) | 2001-11-26 | 2010-07-30 | 自己免疫疾患の治療方法及びそれに関する試薬 |
| JP2014076508A Pending JP2014122251A (ja) | 2001-11-26 | 2014-04-02 | 自己免疫疾患の治療方法及びそれに関する試薬 |
| JP2016074086A Abandoned JP2016147895A (ja) | 2001-11-26 | 2016-04-01 | 自己免疫疾患の治療方法及びそれに関する試薬 |
Family Applications After (3)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2010172410A Pending JP2010248251A (ja) | 2001-11-26 | 2010-07-30 | 自己免疫疾患の治療方法及びそれに関する試薬 |
| JP2014076508A Pending JP2014122251A (ja) | 2001-11-26 | 2014-04-02 | 自己免疫疾患の治療方法及びそれに関する試薬 |
| JP2016074086A Abandoned JP2016147895A (ja) | 2001-11-26 | 2016-04-01 | 自己免疫疾患の治療方法及びそれに関する試薬 |
Country Status (6)
| Country | Link |
|---|---|
| US (2) | US8410053B2 (https=) |
| EP (2) | EP2769715A3 (https=) |
| JP (4) | JP2005511636A (https=) |
| AU (1) | AU2002360453C1 (https=) |
| CA (1) | CA2466870A1 (https=) |
| WO (1) | WO2003045228A2 (https=) |
Families Citing this family (73)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ATE357509T1 (de) | 1997-09-29 | 2007-04-15 | Point Therapeutics Inc | Stimulierung von hämatopoietischen zellen im vitro |
| US6979697B1 (en) | 1998-08-21 | 2005-12-27 | Point Therapeutics, Inc. | Regulation of substrate activity |
| US6890904B1 (en) * | 1999-05-25 | 2005-05-10 | Point Therapeutics, Inc. | Anti-tumor agents |
| EP2316470A3 (en) | 2001-11-26 | 2011-08-24 | Trustees Of Tufts College | Peptidomimetic inhibitors of post-proline cleaving enzymes |
| US7691967B2 (en) * | 2002-04-30 | 2010-04-06 | Trustees Of Tufts College | Smart pro-drugs of serine protease inhibitors |
| WO2004004661A2 (en) * | 2002-07-09 | 2004-01-15 | Point Therapeutics, Inc. | Boroproline compound combination therapy |
| US7407955B2 (en) | 2002-08-21 | 2008-08-05 | Boehringer Ingelheim Pharma Gmbh & Co., Kg | 8-[3-amino-piperidin-1-yl]-xanthines, the preparation thereof and their use as pharmaceutical compositions |
| CA2518465A1 (en) | 2003-03-25 | 2004-10-14 | Takeda San Diego, Inc. | Dipeptidyl peptidase inhibitors |
| 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 |
| DE10330842A1 (de) | 2003-07-08 | 2005-02-10 | Institut für Medizintechnologie Magdeburg GmbH, IMTM | Verwendung der Inhibitoren von Enzymen mit Aktivitäten der Aminopeptidase N und/oder der Dipeptidylpeptidase IV und pharmazeutischen Zubereitungen daraus zur Therapie und Prävention dermatologischer Erkrankungen mit Hyperproliferation und veränderten Differenzierungszuständen von Fibroblasten |
| US7169926B1 (en) | 2003-08-13 | 2007-01-30 | Takeda Pharmaceutical Company Limited | Dipeptidyl peptidase inhibitors |
| US7678909B1 (en) | 2003-08-13 | 2010-03-16 | Takeda Pharmaceutical Company Limited | Dipeptidyl peptidase inhibitors |
| KR20060041309A (ko) | 2003-08-13 | 2006-05-11 | 다케다 야쿠힌 고교 가부시키가이샤 | ４-피리미돈 유도체 및 펩티딜 펩티다제 저해제로서의 그의용도 |
| EP1699777B1 (en) | 2003-09-08 | 2012-12-12 | Takeda Pharmaceutical Company Limited | Dipeptidyl peptidase inhibitors |
| US7576121B2 (en) | 2003-11-12 | 2009-08-18 | Phenomix Corporation | Pyrrolidine compounds and methods for selective inhibition of dipeptidyl peptidase-IV |
| CN1894261B (zh) * | 2003-11-12 | 2012-12-05 | 芬诺密克斯公司 | 杂环硼酸化合物 |
| US7317109B2 (en) | 2003-11-12 | 2008-01-08 | Phenomix Corporation | Pyrrolidine compounds and methods for selective inhibition of dipeptidyl peptidase-IV |
| SG134333A1 (en) * | 2003-11-12 | 2007-08-29 | Phenomix Corp | Heterocyclic boronic acid compounds |
| AU2005216970B2 (en) * | 2004-02-23 | 2011-07-07 | Trustees Of Tufts College | Inhibitors of dipeptidylpeptidase IV for regulating glucose metabolism |
| US7732446B1 (en) | 2004-03-11 | 2010-06-08 | Takeda Pharmaceutical Company Limited | Dipeptidyl peptidase inhibitors |
| UA85871C2 (uk) | 2004-03-15 | 2009-03-10 | Такеда Фармасьютікал Компані Лімітед | Інгібітори дипептидилпептидази |
| US7687638B2 (en) | 2004-06-04 | 2010-03-30 | Takeda San Diego, Inc. | Dipeptidyl peptidase inhibitors |
| WO2006019965A2 (en) | 2004-07-16 | 2006-02-23 | Takeda San Diego, Inc. | Dipeptidyl peptidase inhibitors |
| US20060063719A1 (en) * | 2004-09-21 | 2006-03-23 | Point Therapeutics, Inc. | Methods for treating diabetes |
| JP2008524331A (ja) | 2004-12-21 | 2008-07-10 | 武田薬品工業株式会社 | ジペプチジルペプチダーゼ阻害剤 |
| DOP2006000008A (es) | 2005-01-10 | 2006-08-31 | Arena Pharm Inc | Terapia combinada para el tratamiento de la diabetes y afecciones relacionadas y para el tratamiento de afecciones que mejoran mediante un incremento de la concentración sanguínea de glp-1 |
| JP2006306770A (ja) * | 2005-04-27 | 2006-11-09 | Nidek Co Ltd | 眼疾患治療剤 |
| US7825139B2 (en) | 2005-05-25 | 2010-11-02 | Forest Laboratories Holdings Limited (BM) | Compounds and methods for selective inhibition of dipeptidyl peptidase-IV |
| MY147393A (en) | 2005-09-14 | 2012-11-30 | Takeda Pharmaceutical | Administration of dipeptidyl peptidase inhibitors |
| CA2622642C (en) | 2005-09-16 | 2013-12-31 | Takeda Pharmaceutical Company Limited | Dipeptidyl peptidase inhibitors |
| WO2007061434A2 (en) * | 2005-11-10 | 2007-05-31 | Nastech Pharmaceutical Company Inc. | A pharmaceutical formulation of glp-1 and its use for treating a metabolic syndrome |
| 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 |
| US7833730B2 (en) | 2006-04-11 | 2010-11-16 | Arena Pharmaceuticals, Inc. | Methods of using GPR119 to identify compounds useful for increasing bone mass in an individual |
| PE20071221A1 (es) | 2006-04-11 | 2007-12-14 | Arena Pharm Inc | Agonistas del receptor gpr119 en metodos para aumentar la masa osea y para tratar la osteoporosis y otras afecciones caracterizadas por masa osea baja, y la terapia combinada relacionada a estos agonistas |
| EP2540725A1 (de) | 2006-05-04 | 2013-01-02 | Boehringer Ingelheim International GmbH | Polymorphe von 1-((4-Methyl-chinazolin-2-yl)methyl)-3-methyl-7-(2-butin-1-yl)-8-(3-(R)-amino-piperidin-1-yl)xanthin |
| EP1852108A1 (en) | 2006-05-04 | 2007-11-07 | Boehringer Ingelheim Pharma GmbH & Co.KG | DPP IV inhibitor formulations |
| PE20080251A1 (es) | 2006-05-04 | 2008-04-25 | Boehringer Ingelheim Int | Usos de inhibidores de dpp iv |
| US8324383B2 (en) | 2006-09-13 | 2012-12-04 | Takeda Pharmaceutical Company Limited | Methods of making polymorphs of benzoate salt of 2-[[6-[(3R)-3-amino-1-piperidinyl]-3,4-dihydro-3-methyl-2,4-dioxo-1(2H)-pyrimidinyl]methyl]-benzonitrile |
| JO3598B1 (ar) | 2006-10-10 | 2020-07-05 | Infinity Discovery Inc | الاحماض والاسترات البورونية كمثبطات اميد هيدروليز الحامض الدهني |
| TW200838536A (en) | 2006-11-29 | 2008-10-01 | Takeda Pharmaceutical | Polymorphs of succinate salt of 2-[6-(3-amino-piperidin-1-yl)-3-methyl-2,4-dioxo-3,4-dihydro-2H-pyrimidin-1-ylmethy]-4-fluor-benzonitrile and methods of use therefor |
| US8093236B2 (en) | 2007-03-13 | 2012-01-10 | Takeda Pharmaceuticals Company Limited | Weekly administration of dipeptidyl peptidase inhibitors |
| WO2009033819A2 (en) * | 2007-09-11 | 2009-03-19 | Mondobiotech Laboratories Ag | Use of a peptide as a therapeutic agent |
| KR20100061481A (ko) * | 2007-09-11 | 2010-06-07 | 몬도바이오테크 래보래토리즈 아게 | 치료제로서의 미니가스트린 |
| WO2009033690A1 (en) * | 2007-09-11 | 2009-03-19 | Mondobiotech Laboratories Ag | Bfgf (119-126) for therapeutic applications |
| WO2009033739A2 (en) * | 2007-09-11 | 2009-03-19 | Mondobiotech Laboratories Ag | Use of a peptide as a therapeutic agent |
| WO2009039982A2 (en) * | 2007-09-11 | 2009-04-02 | Mondobiotech Laboratories Ag | Use of a peptide as a therapeutic agent |
| PE20091730A1 (es) | 2008-04-03 | 2009-12-10 | Boehringer Ingelheim Int | Formulaciones que comprenden un inhibidor de dpp4 |
| EP2108960A1 (en) | 2008-04-07 | 2009-10-14 | Arena Pharmaceuticals, Inc. | Methods of using A G protein-coupled receptor to identify peptide YY (PYY) secretagogues and compounds useful in the treatment of conditons modulated by PYY |
| CA2721060A1 (en) | 2008-04-09 | 2009-10-15 | Infinity Pharmaceuticals, Inc. | Inhibitors of fatty acid amide hydrolase |
| JP5493234B2 (ja) * | 2008-05-15 | 2014-05-14 | 国立大学法人 岡山大学 | Ｐｓｇｌ−１阻害によるメタボリックシンドロームの予防及び治療法 |
| BRPI0916997A2 (pt) | 2008-08-06 | 2020-12-15 | Boehringer Ingelheim International Gmbh | Inibidor de dpp-4 e seu uso |
| US20200155558A1 (en) | 2018-11-20 | 2020-05-21 | Boehringer Ingelheim International Gmbh | Treatment for diabetes in patients with insufficient glycemic control despite therapy with an oral antidiabetic drug |
| AR077642A1 (es) | 2009-07-09 | 2011-09-14 | Arena Pharm Inc | Moduladores del metabolismo y el tratamiento de trastornos relacionados con el mismo |
| KR20240090632A (ko) | 2009-11-27 | 2024-06-21 | 베링거 인겔하임 인터내셔날 게엠베하 | 리나글립틴과 같은 ｄｐｐ－ｉｖ 억제제를 사용한 유전자형 검사된 당뇨병 환자의 치료 |
| RU2015143910A (ru) | 2010-02-03 | 2018-12-28 | Инфинити Фармасьютикалз, Инк. | Ингибиторы амид-гидролазы жирных кислот |
| CA2795513A1 (en) | 2010-04-06 | 2011-10-13 | Arena Pharmaceuticals, Inc. | Modulators of the gpr119 receptor and the treatment of disorders related thereto |
| CN102946875A (zh) | 2010-05-05 | 2013-02-27 | 贝林格尔.英格海姆国际有限公司 | 组合疗法 |
| EP3323818A1 (en) | 2010-09-22 | 2018-05-23 | Arena Pharmaceuticals, Inc. | Modulators of the gpr119 receptor and the treatment of disorders related thereto |
| AR083878A1 (es) | 2010-11-15 | 2013-03-27 | Boehringer Ingelheim Int | Terapia antidiabetica vasoprotectora y cardioprotectora, linagliptina, metodo de tratamiento |
| US20140018371A1 (en) | 2011-04-01 | 2014-01-16 | Arena Pharmaceuticals, Inc. | Modulators Of The GPR119 Receptor And The Treatment Of Disorders Related Thereto |
| WO2012145361A1 (en) | 2011-04-19 | 2012-10-26 | Arena Pharmaceuticals, Inc. | Modulators of the gpr119 receptor and the treatment of disorders related thereto |
| US20140051714A1 (en) | 2011-04-22 | 2014-02-20 | Arena Pharmaceuticals, Inc. | Modulators Of The GPR119 Receptor And The Treatment Of Disorders Related Thereto |
| US20140038889A1 (en) | 2011-04-22 | 2014-02-06 | Arena Pharmaceuticals, Inc. | Modulators Of The GPR119 Receptor And The Treatment Of Disorders Related Thereto |
| WO2012170702A1 (en) | 2011-06-08 | 2012-12-13 | Arena Pharmaceuticals, Inc. | Modulators of the gpr119 receptor and the treatment of disorders related thereto |
| PL2753334T3 (pl) | 2011-08-30 | 2022-12-12 | Trustees Of Tufts College | Aktywowane przez fap inhibitory proteasomu do leczenia guzów litych |
| WO2013055910A1 (en) | 2011-10-12 | 2013-04-18 | Arena Pharmaceuticals, Inc. | Modulators of the gpr119 receptor and the treatment of disorders related thereto |
| JP6224084B2 (ja) | 2012-05-14 | 2017-11-01 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | 糸球体上皮細胞関連障害及び／又はネフローゼ症候群の治療に用いるｄｐｐ−４阻害薬としてのキサンチン誘導体 |
| JP6218811B2 (ja) * | 2012-05-14 | 2017-10-25 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | Ｓｉｒｓ及び／又は敗血症の治療に用いるｄｐｐ−４阻害薬としてのキサンチン誘導体 |
| WO2014074668A1 (en) | 2012-11-08 | 2014-05-15 | Arena Pharmaceuticals, Inc. | Modulators of gpr119 and the treatment of disorders related thereto |
| EA201791982A1 (ru) | 2015-03-09 | 2020-02-17 | Интекрин Терапьютикс, Инк. | Способы лечения неалкогольной жировой болезни печени и/или липодистрофии |
| CN109310697A (zh) | 2016-06-10 | 2019-02-05 | 勃林格殷格翰国际有限公司 | 利格列汀和二甲双胍的组合 |
| JP2020515639A (ja) | 2017-04-03 | 2020-05-28 | コヒラス・バイオサイエンシズ・インコーポレイテッド | 進行性核上性麻痺の処置のためのＰＰＡＲγアゴニスト |
| AU2023219870B1 (en) * | 2023-02-13 | 2024-02-08 | Affiliated Hospital Of Nantong University | Novel use of dpp-4 inhibitor in manufacture of drug for treatment of lupus nephritis |
Family Cites Families (46)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| IT1164225B (it) | 1983-05-13 | 1987-04-08 | Anic Spa | Analoghi retro-invertiti del pentapeptide potenziante la bradichina bpp5a e metodi per la loro preparazione |
| SE8702550D0 (sv) | 1987-06-18 | 1987-06-18 | Anders Grubb | Cysteinproteashemmare |
| US4935493A (en) | 1987-10-06 | 1990-06-19 | E. I. Du Pont De Nemours And Company | Protease inhibitors |
| ZA897515B (en) | 1988-10-07 | 1990-06-27 | Merrell Dow Pharma | Novel peptidase inhibitors |
| IT1227907B (it) | 1988-12-23 | 1991-05-14 | Eniricerche S P A Milano Sclav | Procedimento per la sintesi di peptidi retro-inversi e nuovi intermediin tale procedimento |
| JP2701932B2 (ja) | 1989-04-10 | 1998-01-21 | サントリー株式会社 | タンパク質分解酵素阻害剤 |
| EP0528858B1 (en) * | 1990-04-14 | 1997-01-22 | New England Medical Center Hospitals, Inc. | Inhibitors of dipeptidyl-aminopeptidase type iv |
| US5462928A (en) * | 1990-04-14 | 1995-10-31 | New England Medical Center Hospitals, Inc. | Inhibitors of dipeptidyl-aminopeptidase type IV |
| CA2121369C (en) | 1991-10-22 | 2003-04-29 | William W. Bachovchin | Inhibitors of dipeptidyl-aminopeptidase type iv |
| US6825169B1 (en) * | 1991-10-22 | 2004-11-30 | Trustees Of Tufts College | Inhibitors of dipeptidyl-aminopeptidase type IV |
| DK36392D0 (da) * | 1992-03-19 | 1992-03-19 | Novo Nordisk As | Anvendelse af kemisk forbindelse |
| US5296604A (en) | 1992-05-15 | 1994-03-22 | Miles Inc. | Proline derivatives and compositions for their use as inhibitors of HIV protease |
| IL111785A0 (en) | 1993-12-03 | 1995-01-24 | Ferring Bv | Dp-iv inhibitors and pharmaceutical compositions containing them |
| US5580979A (en) * | 1994-03-15 | 1996-12-03 | Trustees Of Tufts University | Phosphotyrosine peptidomimetics for inhibiting SH2 domain interactions |
| US5543396A (en) | 1994-04-28 | 1996-08-06 | Georgia Tech Research Corp. | Proline phosphonate derivatives |
| US5614649A (en) | 1994-11-14 | 1997-03-25 | Cephalon, Inc. | Multicatalytic protease inhibitors |
| US5834428A (en) * | 1995-04-14 | 1998-11-10 | 1149336 Ontario Inc. | Glucagon-like peptide-2 and its therapeutic use |
| FI974437A7 (fi) | 1995-06-06 | 1997-12-05 | Pfizer | Substituoituja N-(indoli-2-karbonyyli)amideja ja johdannaisia glykogee nifosforylaasi-inhibiittoreina |
| DE122010000020I1 (de) * | 1996-04-25 | 2010-07-08 | Prosidion Ltd | Verfahren zur Senkung des Blutglukosespiegels in Säugern |
| US5783556A (en) * | 1996-08-13 | 1998-07-21 | Genentech, Inc. | Formulated insulin-containing composition |
| TW492957B (en) | 1996-11-07 | 2002-07-01 | Novartis Ag | N-substituted 2-cyanopyrrolidnes |
| US6011155A (en) * | 1996-11-07 | 2000-01-04 | Novartis Ag | N-(substituted glycyl)-2-cyanopyrrolidines, pharmaceutical compositions containing them and their use in inhibiting dipeptidyl peptidase-IV |
| US5952301A (en) * | 1996-12-10 | 1999-09-14 | 1149336 Ontario Inc. | Compositions and methods for enhancing intestinal function |
| WO1999015183A1 (en) * | 1997-09-25 | 1999-04-01 | Proscript Inc. | PROTEASOME INHIBITORS, UBIQUITIN PATHWAY INHIBITORS OR AGENTS THAT INTERFERE WITH THE ACTIVATION OF NF-λB VIA THE UBIQUITIN PROTEASOME PATHWAY TO TREAT INFLAMMATORY AND AUTOIMMUNE DISEASES |
| ATE357509T1 (de) * | 1997-09-29 | 2007-04-15 | Point Therapeutics Inc | Stimulierung von hämatopoietischen zellen im vitro |
| EP2583675A1 (en) * | 1998-02-02 | 2013-04-24 | Trustees Of Tufts College | Use of dipeptidylpeptidase inhibitors to regulate glucose metabolism |
| IL139247A0 (en) * | 1998-05-04 | 2001-11-25 | Point Therapeutics Inc | Hematopoietic stimulation |
| JP2002517401A (ja) * | 1998-06-05 | 2002-06-18 | ポイント セラピューティクス， インコーポレイテッド | 環状ボロプロリン化合物 |
| WO2000010549A1 (en) * | 1998-08-21 | 2000-03-02 | Point Therapeutics, Inc. | Regulation of substrate activity |
| US6979697B1 (en) * | 1998-08-21 | 2005-12-27 | Point Therapeutics, Inc. | Regulation of substrate activity |
| US6890904B1 (en) * | 1999-05-25 | 2005-05-10 | Point Therapeutics, Inc. | Anti-tumor agents |
| DE19940130A1 (de) * | 1999-08-24 | 2001-03-01 | Probiodrug Ges Fuer Arzneim | Neue Effektoren der Dipeptidyl Peptidase IV zur topischen Anwendung |
| JP2003535034A (ja) | 1999-11-12 | 2003-11-25 | ギルフォード ファーマシューティカルズ インコーポレイテッド | ジペプチジルペプチダーゼｉｖ阻害剤並びにジペプチジルペプチダーゼｉｖ阻害剤の製造及び使用法 |
| US6818419B2 (en) * | 2000-01-13 | 2004-11-16 | Tularik Inc. | IRAK-4: compositions and methods of use |
| TW591031B (en) * | 2000-02-29 | 2004-06-11 | Takeda Chemical Industries Ltd | Thienopyridine derivatives, their production and use |
| KR20080067009A (ko) * | 2000-03-31 | 2008-07-17 | 프로시디온 리미티드 | 디펩티딜 펩티다제 ⅳ 효소 활성 억제제를 포함하는약제학적 조성물 |
| EP1142889A1 (en) * | 2000-04-03 | 2001-10-10 | Pfizer Products Inc. | Pyrazole derivatives as anti-inflammatory/analgesic agents |
| GB0010188D0 (en) * | 2000-04-26 | 2000-06-14 | Ferring Bv | Inhibitors of dipeptidyl peptidase IV |
| DE10025464A1 (de) * | 2000-05-23 | 2001-12-06 | Inst Medizintechnologie Magdeb | Kombinierte Verwendung von Enzyminhibitoren zur Therapie von Autoimmunerkrankungen, bei Transplantationen und Tumorerkrankungen sowie Kombinationen von Enzyminhibitoren umfassende pharmazeutische Zubereitungen |
| EP1368349B1 (de) * | 2001-02-24 | 2007-02-14 | Boehringer Ingelheim Pharma GmbH & Co.KG | Xanthinderivate, deren herstellung und deren verwendung als arzneimittel |
| EP2316470A3 (en) * | 2001-11-26 | 2011-08-24 | Trustees Of Tufts College | Peptidomimetic inhibitors of post-proline cleaving enzymes |
| WO2004004661A2 (en) * | 2002-07-09 | 2004-01-15 | Point Therapeutics, Inc. | Boroproline compound combination therapy |
| ATE549028T1 (de) * | 2003-05-15 | 2012-03-15 | Tufts College | Stabile analoga von glp-1 |
| AU2005216970B2 (en) * | 2004-02-23 | 2011-07-07 | Trustees Of Tufts College | Inhibitors of dipeptidylpeptidase IV for regulating glucose metabolism |
| US20060063719A1 (en) * | 2004-09-21 | 2006-03-23 | Point Therapeutics, Inc. | Methods for treating diabetes |
| DE102012201584B4 (de) | 2012-02-03 | 2021-04-01 | Lear Corporation | Sitzschienenanordnung mit wählbaren Endanschlag-Positionen und Verfahren zum Ausbilden einer Sitzschienenanordnung |
-
2002
- 2002-11-26 WO PCT/US2002/038347 patent/WO2003045228A2/en not_active Ceased
- 2002-11-26 US US10/496,627 patent/US8410053B2/en not_active Expired - Fee Related
- 2002-11-26 EP EP14161169.9A patent/EP2769715A3/en not_active Ceased
- 2002-11-26 CA CA002466870A patent/CA2466870A1/en not_active Abandoned
- 2002-11-26 EP EP02795710A patent/EP1487471A4/en not_active Withdrawn
- 2002-11-26 JP JP2003546737A patent/JP2005511636A/ja active Pending
- 2002-11-26 AU AU2002360453A patent/AU2002360453C1/en not_active Ceased
-
2010
- 2010-07-30 JP JP2010172410A patent/JP2010248251A/ja active Pending
-
2012
- 2012-03-14 US US13/420,121 patent/US20120232004A1/en not_active Abandoned
-
2014
- 2014-04-02 JP JP2014076508A patent/JP2014122251A/ja active Pending
-
2016
- 2016-04-01 JP JP2016074086A patent/JP2016147895A/ja not_active Abandoned
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| JP2005511636A5 (https=) | ||
| JP2002501889A5 (https=) | ||
| US7423041B2 (en) | A1 adenosine receptor antagonists | |
| JP2011504935A5 (https=) | ||
| JP2012509892A5 (https=) | ||
| JP2015526448A5 (https=) | ||
| US12583900B2 (en) | Peptide conjugates and methods of use | |
| JP2005041885A5 (https=) | ||
| JP2009542716A5 (https=) | ||
| CA2449441A1 (en) | 3-fluoro-pyrrolidines as antidiabetic agents | |
| KR100931411B1 (ko) | 1ｈ-피라졸 4-카복실아미드, 이의 제조 방법, 및 이의 11베타-하이드록시스테로이드 탈수소효소로서의 용도 | |
| HRP20191614T1 (hr) | Spojevi koji su suagonisti gip i glp-1 | |
| JP2012512903A5 (https=) | ||
| JP2010248251A (ja) | 自己免疫疾患の治療方法及びそれに関する試薬 | |
| EP1857457A3 (en) | Benzimidazole derivative and its use as AII receptor antagonist | |
| TW200538096A (en) | Inhibitors of dipeptidylpeptidase Ⅳ | |
| CA2411778A1 (en) | Organic compounds | |
| CA2409741A1 (en) | Tnf-.alpha. production inhibitors | |
| EP1862458A3 (en) | Therapeutic agents useful for treating pain | |
| HRP20140950T1 (hr) | Novi spojevi i pripravci, te postupci njihove primjene | |
| JP2008505157A5 (https=) | ||
| WO2008021038B1 (en) | Pyridobenzazepine compounds and methods for inhibiting mitotic progression | |
| CA2555961A1 (en) | Lactams as conformationally constrained peptidomimetic inhibitors | |
| CA2571143A1 (fr) | Derives de 2-carbamide-4-phenylthiazole, leur preparation et leur application en therapeutique | |
| KR930701413A (ko) | 벤즈이미다졸 유도체와 이의 제조방법 및 이의 용도 |