JP2005505531A5 - - Google Patents
Download PDFInfo
- Publication number
- JP2005505531A5 JP2005505531A5 JP2003520734A JP2003520734A JP2005505531A5 JP 2005505531 A5 JP2005505531 A5 JP 2005505531A5 JP 2003520734 A JP2003520734 A JP 2003520734A JP 2003520734 A JP2003520734 A JP 2003520734A JP 2005505531 A5 JP2005505531 A5 JP 2005505531A5
- Authority
- JP
- Japan
- Prior art keywords
- residue
- alkyl
- amino acid
- pharmaceutical composition
- acid
- 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
- 125000000217 alkyl group Chemical group 0.000 claims 19
- 235000001014 amino acid Nutrition 0.000 claims 19
- 150000001413 amino acids Chemical class 0.000 claims 19
- 239000008194 pharmaceutical composition Substances 0.000 claims 16
- 239000003112 inhibitor Substances 0.000 claims 10
- RWRDLPDLKQPQOW-UHFFFAOYSA-N Pyrrolidine Chemical compound C1CCNC1 RWRDLPDLKQPQOW-UHFFFAOYSA-N 0.000 claims 9
- 125000003545 alkoxy group Chemical group 0.000 claims 7
- 102100025012 Dipeptidyl peptidase 4 Human genes 0.000 claims 6
- 101000930822 Giardia intestinalis Dipeptidyl-peptidase 4 Proteins 0.000 claims 6
- PMMYEEVYMWASQN-DMTCNVIQSA-N Hydroxyproline Chemical compound O[C@H]1CN[C@H](C(O)=O)C1 PMMYEEVYMWASQN-DMTCNVIQSA-N 0.000 claims 6
- 125000002252 acyl group Chemical group 0.000 claims 6
- 125000003118 aryl group Chemical group 0.000 claims 6
- 150000001875 compounds Chemical class 0.000 claims 6
- 125000001072 heteroaryl group Chemical group 0.000 claims 6
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 6
- 125000004076 pyridyl group Chemical group 0.000 claims 6
- FSYKKLYZXJSNPZ-UHFFFAOYSA-N sarcosine Chemical compound C[NH2+]CC([O-])=O FSYKKLYZXJSNPZ-UHFFFAOYSA-N 0.000 claims 6
- HXEACLLIILLPRG-YFKPBYRVSA-N L-pipecolic acid Chemical compound [O-]C(=O)[C@@H]1CCCC[NH2+]1 HXEACLLIILLPRG-YFKPBYRVSA-N 0.000 claims 5
- 125000003342 alkenyl group Chemical group 0.000 claims 5
- 230000036772 blood pressure Effects 0.000 claims 5
- 125000004093 cyano group Chemical group *C#N 0.000 claims 5
- 125000000524 functional group Chemical group 0.000 claims 5
- 229910052736 halogen Inorganic materials 0.000 claims 5
- 150000002367 halogens Chemical class 0.000 claims 5
- HXEACLLIILLPRG-RXMQYKEDSA-N l-pipecolic acid Natural products OC(=O)[C@H]1CCCCN1 HXEACLLIILLPRG-RXMQYKEDSA-N 0.000 claims 5
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 5
- 108090000765 processed proteins & peptides Chemical class 0.000 claims 5
- 150000003839 salts Chemical class 0.000 claims 5
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 4
- MTCFGRXMJLQNBG-REOHCLBHSA-N (2S)-2-Amino-3-hydroxypropansäure Chemical compound OC[C@H](N)C(O)=O MTCFGRXMJLQNBG-REOHCLBHSA-N 0.000 claims 3
- OGYGFUAIIOPWQD-UHFFFAOYSA-N 1,3-thiazolidine Chemical compound C1CSCN1 OGYGFUAIIOPWQD-UHFFFAOYSA-N 0.000 claims 3
- 102100036969 Dipeptidyl peptidase 9 Human genes 0.000 claims 3
- 102000004190 Enzymes Human genes 0.000 claims 3
- 108090000790 Enzymes Proteins 0.000 claims 3
- AKCRVYNORCOYQT-YFKPBYRVSA-N N-methyl-L-valine Chemical compound CN[C@@H](C(C)C)C(O)=O AKCRVYNORCOYQT-YFKPBYRVSA-N 0.000 claims 3
- 108010077895 Sarcosine Proteins 0.000 claims 3
- 125000004122 cyclic group Chemical group 0.000 claims 3
- 125000000753 cycloalkyl group Chemical group 0.000 claims 3
- RAXXELZNTBOGNW-UHFFFAOYSA-N imidazole Natural products C1=CNC=N1 RAXXELZNTBOGNW-UHFFFAOYSA-N 0.000 claims 3
- 229940043230 sarcosine Drugs 0.000 claims 3
- 229920006395 saturated elastomer Polymers 0.000 claims 3
- -1 tri Chemical class 0.000 claims 3
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims 2
- 150000008574 D-amino acids Chemical class 0.000 claims 2
- 108010016626 Dipeptides Proteins 0.000 claims 2
- 102100020751 Dipeptidyl peptidase 2 Human genes 0.000 claims 2
- 108090000194 Dipeptidyl-peptidases and tripeptidyl-peptidases Proteins 0.000 claims 2
- 102000003779 Dipeptidyl-peptidases and tripeptidyl-peptidases Human genes 0.000 claims 2
- 101000804945 Homo sapiens Dipeptidyl peptidase 9 Proteins 0.000 claims 2
- 102100040449 Inactive dipeptidyl peptidase 10 Human genes 0.000 claims 2
- 241000124008 Mammalia Species 0.000 claims 2
- 229910004013 NO 2 Inorganic materials 0.000 claims 2
- XSQUKJJJFZCRTK-UHFFFAOYSA-N Urea Chemical class NC(N)=O XSQUKJJJFZCRTK-UHFFFAOYSA-N 0.000 claims 2
- 239000002253 acid Substances 0.000 claims 2
- 150000001370 alpha-amino acid derivatives Chemical class 0.000 claims 2
- 235000008206 alpha-amino acids Nutrition 0.000 claims 2
- 150000001408 amides Chemical class 0.000 claims 2
- 229910052794 bromium Inorganic materials 0.000 claims 2
- 125000002837 carbocyclic group Chemical group 0.000 claims 2
- 229910052801 chlorine Inorganic materials 0.000 claims 2
- 125000000392 cycloalkenyl group Chemical group 0.000 claims 2
- 206010012601 diabetes mellitus Diseases 0.000 claims 2
- 230000000694 effects Effects 0.000 claims 2
- 125000000623 heterocyclic group Chemical group 0.000 claims 2
- 229910052739 hydrogen Inorganic materials 0.000 claims 2
- 229910052740 iodine Inorganic materials 0.000 claims 2
- UUEVFMOUBSLVJW-UHFFFAOYSA-N oxo-[[1-[2-[2-[2-[4-(oxoazaniumylmethylidene)pyridin-1-yl]ethoxy]ethoxy]ethyl]pyridin-4-ylidene]methyl]azanium;dibromide Chemical compound [Br-].[Br-].C1=CC(=C[NH+]=O)C=CN1CCOCCOCCN1C=CC(=C[NH+]=O)C=C1 UUEVFMOUBSLVJW-UHFFFAOYSA-N 0.000 claims 2
- 125000005740 oxycarbonyl group Chemical group [*:1]OC([*:2])=O 0.000 claims 2
- 229910052760 oxygen Inorganic materials 0.000 claims 2
- 235000018102 proteins Nutrition 0.000 claims 2
- 102000004169 proteins and genes Human genes 0.000 claims 2
- 108090000623 proteins and genes Proteins 0.000 claims 2
- 229910052717 sulfur Inorganic materials 0.000 claims 2
- IVBVTDXOGUNDHC-LURJTMIESA-N (2s)-2-amino-1-pyrrolidin-1-ylpropan-1-one Chemical compound C[C@H](N)C(=O)N1CCCC1 IVBVTDXOGUNDHC-LURJTMIESA-N 0.000 claims 1
- NPSLKZBLPSTQGO-DFWYDOINSA-N (2s)-2-aminopentanedioic acid;1,3-thiazolidine Chemical compound C1CSCN1.OC(=O)[C@@H](N)CCC(O)=O NPSLKZBLPSTQGO-DFWYDOINSA-N 0.000 claims 1
- ULFVCDOOHOEPBW-DFWYDOINSA-N (2s)-2-aminopentanedioic acid;pyrrolidine Chemical compound C1CCNC1.OC(=O)[C@@H](N)CCC(O)=O ULFVCDOOHOEPBW-DFWYDOINSA-N 0.000 claims 1
- GAJSPNHIKHRBGQ-NTFOPCPOSA-N (4s)-4-amino-5-oxo-5-(1,3-thiazolidin-2-yl)pentanamide Chemical compound NC(=O)CC[C@H](N)C(=O)C1NCCS1 GAJSPNHIKHRBGQ-NTFOPCPOSA-N 0.000 claims 1
- FAAZAHIRCXGFFM-ZETCQYMHSA-N (4s)-4-amino-5-oxo-5-pyrrolidin-1-ylpentanamide Chemical compound NC(=O)CC[C@H](N)C(=O)N1CCCC1 FAAZAHIRCXGFFM-ZETCQYMHSA-N 0.000 claims 1
- OMGHIGVFLOPEHJ-UHFFFAOYSA-N 2,5-dihydro-1h-pyrrol-1-ium-2-carboxylate Chemical compound OC(=O)C1NCC=C1 OMGHIGVFLOPEHJ-UHFFFAOYSA-N 0.000 claims 1
- 208000010444 Acidosis Diseases 0.000 claims 1
- 239000004475 Arginine Substances 0.000 claims 1
- 102100027936 Attractin Human genes 0.000 claims 1
- 101710134735 Attractin Proteins 0.000 claims 1
- 108090001081 Dipeptidases Proteins 0.000 claims 1
- 102000004860 Dipeptidases Human genes 0.000 claims 1
- 102100036968 Dipeptidyl peptidase 8 Human genes 0.000 claims 1
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 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
- 101100278476 Homo sapiens DPP10 gene Proteins 0.000 claims 1
- 101100010319 Homo sapiens DPP9 gene Proteins 0.000 claims 1
- 101000804947 Homo sapiens Dipeptidyl peptidase 8 Proteins 0.000 claims 1
- 101000967820 Homo sapiens Inactive dipeptidyl peptidase 10 Proteins 0.000 claims 1
- 208000031226 Hyperlipidaemia Diseases 0.000 claims 1
- XUJNEKJLAYXESH-REOHCLBHSA-N L-Cysteine Chemical compound SC[C@H](N)C(O)=O XUJNEKJLAYXESH-REOHCLBHSA-N 0.000 claims 1
- ODKSFYDXXFIFQN-BYPYZUCNSA-P L-argininium(2+) Chemical compound NC(=[NH2+])NCCC[C@H]([NH3+])C(O)=O ODKSFYDXXFIFQN-BYPYZUCNSA-P 0.000 claims 1
- CKLJMWTZIZZHCS-REOHCLBHSA-N L-aspartic acid Chemical compound OC(=O)[C@@H](N)CC(O)=O CKLJMWTZIZZHCS-REOHCLBHSA-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
- KDXKERNSBIXSRK-YFKPBYRVSA-N L-lysine Chemical compound NCCCC[C@H](N)C(O)=O KDXKERNSBIXSRK-YFKPBYRVSA-N 0.000 claims 1
- AYFVYJQAPQTCCC-GBXIJSLDSA-N L-threonine Chemical compound C[C@@H](O)[C@H](N)C(O)=O AYFVYJQAPQTCCC-GBXIJSLDSA-N 0.000 claims 1
- OUYCCCASQSFEME-QMMMGPOBSA-N L-tyrosine Chemical compound OC(=O)[C@@H](N)CC1=CC=C(O)C=C1 OUYCCCASQSFEME-QMMMGPOBSA-N 0.000 claims 1
- KDXKERNSBIXSRK-UHFFFAOYSA-N Lysine Natural products NCCCCC(N)C(O)=O KDXKERNSBIXSRK-UHFFFAOYSA-N 0.000 claims 1
- 239000004472 Lysine Substances 0.000 claims 1
- 206010027417 Metabolic acidosis Diseases 0.000 claims 1
- 108010038807 Oligopeptides Proteins 0.000 claims 1
- 102000015636 Oligopeptides Human genes 0.000 claims 1
- 239000002202 Polyethylene glycol Substances 0.000 claims 1
- 102100023832 Prolyl endopeptidase FAP Human genes 0.000 claims 1
- MTCFGRXMJLQNBG-UHFFFAOYSA-N Serine Natural products OCC(N)C(O)=O MTCFGRXMJLQNBG-UHFFFAOYSA-N 0.000 claims 1
- FZWLAAWBMGSTSO-UHFFFAOYSA-N Thiazole Chemical compound C1=CSC=N1 FZWLAAWBMGSTSO-UHFFFAOYSA-N 0.000 claims 1
- AYFVYJQAPQTCCC-UHFFFAOYSA-N Threonine Natural products CC(O)C(N)C(O)=O AYFVYJQAPQTCCC-UHFFFAOYSA-N 0.000 claims 1
- 239000004473 Threonine Substances 0.000 claims 1
- IYZOCUFCTWMQLC-KBPBESRZSA-N [benzoyl(hydroxy)amino] (2S)-1-[(2S)-2-amino-3-methylbutanoyl]pyrrolidine-2-carboxylate Chemical compound N[C@@H](C(C)C)C(=O)N1[C@H](C(=O)ON(O)C(C2=CC=CC=C2)=O)CCC1 IYZOCUFCTWMQLC-KBPBESRZSA-N 0.000 claims 1
- 230000005856 abnormality Effects 0.000 claims 1
- 150000007513 acids Chemical class 0.000 claims 1
- 239000004480 active ingredient Substances 0.000 claims 1
- 125000001118 alkylidene group Chemical group 0.000 claims 1
- 150000001412 amines Chemical class 0.000 claims 1
- 125000000539 amino acid group Chemical group 0.000 claims 1
- 125000004103 aminoalkyl group Chemical group 0.000 claims 1
- 150000008064 anhydrides Chemical class 0.000 claims 1
- 235000009697 arginine Nutrition 0.000 claims 1
- ODKSFYDXXFIFQN-UHFFFAOYSA-N arginine Natural products OC(=O)C(N)CCCNC(N)=N ODKSFYDXXFIFQN-UHFFFAOYSA-N 0.000 claims 1
- 150000001491 aromatic compounds Chemical class 0.000 claims 1
- 125000004104 aryloxy group Chemical group 0.000 claims 1
- 235000003704 aspartic acid Nutrition 0.000 claims 1
- OQFSQFPPLPISGP-UHFFFAOYSA-N beta-carboxyaspartic acid Natural products OC(=O)C(N)C(C(O)=O)C(O)=O OQFSQFPPLPISGP-UHFFFAOYSA-N 0.000 claims 1
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 claims 1
- 125000004432 carbon atom Chemical group C* 0.000 claims 1
- BVKZGUZCCUSVTD-UHFFFAOYSA-N carbonic acid Chemical compound OC(O)=O BVKZGUZCCUSVTD-UHFFFAOYSA-N 0.000 claims 1
- 125000005243 carbonyl alkyl group Chemical group 0.000 claims 1
- 239000003054 catalyst Substances 0.000 claims 1
- 235000018417 cysteine Nutrition 0.000 claims 1
- XUJNEKJLAYXESH-UHFFFAOYSA-N cysteine Natural products SCC(N)C(O)=O XUJNEKJLAYXESH-UHFFFAOYSA-N 0.000 claims 1
- 108090000212 dipeptidyl peptidase II Proteins 0.000 claims 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 1
- PMMYEEVYMWASQN-UHFFFAOYSA-N dl-hydroxyproline Natural products OC1C[NH2+]C(C([O-])=O)C1 PMMYEEVYMWASQN-UHFFFAOYSA-N 0.000 claims 1
- 150000002148 esters Chemical class 0.000 claims 1
- 108010072257 fibroblast activation protein alpha Proteins 0.000 claims 1
- 235000013922 glutamic acid Nutrition 0.000 claims 1
- 239000004220 glutamic acid Substances 0.000 claims 1
- 125000004404 heteroalkyl group Chemical group 0.000 claims 1
- 125000004356 hydroxy functional group Chemical group O* 0.000 claims 1
- 229960002591 hydroxyproline Drugs 0.000 claims 1
- 201000001421 hyperglycemia Diseases 0.000 claims 1
- 235000018977 lysine Nutrition 0.000 claims 1
- 230000004060 metabolic process Effects 0.000 claims 1
- 125000005429 oxyalkyl group Chemical group 0.000 claims 1
- 230000001575 pathological effect Effects 0.000 claims 1
- 125000003386 piperidinyl group Chemical group 0.000 claims 1
- 229920001223 polyethylene glycol Polymers 0.000 claims 1
- 102000004196 processed proteins & peptides Human genes 0.000 claims 1
- 108010066823 proline dipeptidase Proteins 0.000 claims 1
- QJRYYOWARFCJQZ-UHFFFAOYSA-N pyrrolidine-1-carbonitrile Chemical compound N#CN1CCCC1 QJRYYOWARFCJQZ-UHFFFAOYSA-N 0.000 claims 1
- 125000000719 pyrrolidinyl group Chemical group 0.000 claims 1
- 235000004400 serine Nutrition 0.000 claims 1
- 125000000547 substituted alkyl group Chemical group 0.000 claims 1
- 150000003536 tetrazoles Chemical class 0.000 claims 1
- 125000004001 thioalkyl group Chemical group 0.000 claims 1
- 235000008521 threonine Nutrition 0.000 claims 1
- FGMPLJWBKKVCDB-UHFFFAOYSA-N trans-L-hydroxy-proline Natural products ON1CCCC1C(O)=O FGMPLJWBKKVCDB-UHFFFAOYSA-N 0.000 claims 1
- 235000002374 tyrosine Nutrition 0.000 claims 1
- OUYCCCASQSFEME-UHFFFAOYSA-N tyrosine Natural products OC(=O)C(N)CC1=CC=C(O)C=C1 OUYCCCASQSFEME-UHFFFAOYSA-N 0.000 claims 1
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US09/932,546 US20020006899A1 (en) | 1998-10-06 | 2001-08-17 | Use of dipeptidyl peptidase IV effectors for lowering blood pressure in mammals |
| PCT/EP2002/008210 WO2003015775A1 (en) | 2001-08-17 | 2002-07-23 | New dipeptidyl peptidase iv inhibitors and their uses for lowering blood pressure levels |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2009207484A Division JP2009286799A (ja) | 2001-08-17 | 2009-09-08 | 新規ジペプチジルペプチダーゼｉｖ阻害剤および血圧レベルを低下させるためのそれらの使用 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2005505531A JP2005505531A (ja) | 2005-02-24 |
| JP2005505531A5 true JP2005505531A5 (enExample) | 2006-01-05 |
Family
ID=25462480
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2003520734A Pending JP2005505531A (ja) | 2001-08-17 | 2002-07-23 | 新規ジペプチジルペプチダーゼｉｖ阻害剤および血圧レベルを低下させるためのそれらの使用 |
| JP2009207484A Abandoned JP2009286799A (ja) | 2001-08-17 | 2009-09-08 | 新規ジペプチジルペプチダーゼｉｖ阻害剤および血圧レベルを低下させるためのそれらの使用 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2009207484A Abandoned JP2009286799A (ja) | 2001-08-17 | 2009-09-08 | 新規ジペプチジルペプチダーゼｉｖ阻害剤および血圧レベルを低下させるためのそれらの使用 |
Country Status (9)
| Country | Link |
|---|---|
| US (5) | US20020006899A1 (enExample) |
| EP (1) | EP1416932A1 (enExample) |
| JP (2) | JP2005505531A (enExample) |
| CN (1) | CN1582149A (enExample) |
| CA (1) | CA2423025A1 (enExample) |
| NO (1) | NO20031574L (enExample) |
| RU (1) | RU2305553C2 (enExample) |
| WO (1) | WO2003015775A1 (enExample) |
| ZA (1) | ZA200302126B (enExample) |
Families Citing this family (70)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| BR9813233A (pt) * | 1997-09-29 | 2000-08-22 | Point Therapeutics Inc | Estimulação de células hematopoéticas in 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 |
| IL158923A0 (en) | 2001-06-27 | 2004-05-12 | Smithkline Beecham Corp | Fluoropyrrolidines as dipeptidyl peptidase inhibitors |
| US6710040B1 (en) | 2002-06-04 | 2004-03-23 | Pfizer Inc. | Fluorinated cyclic amides as dipeptidyl peptidase IV inhibitors |
| US7550590B2 (en) * | 2003-03-25 | 2009-06-23 | Takeda Pharmaceutical Company Limited | 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 |
| WO2004104216A2 (en) * | 2003-05-21 | 2004-12-02 | Bayer Healthcare Ag | Diagnostics and therapeutics for diseases associated with dipeptidylpeptidase iv (dpp4) |
| WO2005016911A1 (en) * | 2003-08-13 | 2005-02-24 | Takeda Pharmaceutical Company Limited | 4-pyrimidone derivatives and their use as peptidyl peptidase inhibitors |
| 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 |
| JP2007513058A (ja) * | 2003-09-08 | 2007-05-24 | 武田薬品工業株式会社 | ジペプチジルぺプチダーゼ阻害剤 |
| EP1699777B1 (en) * | 2003-09-08 | 2012-12-12 | Takeda Pharmaceutical Company Limited | Dipeptidyl peptidase inhibitors |
| CN101684089A (zh) * | 2004-02-05 | 2010-03-31 | 杏林制药株式会社 | 双环酯类衍生物 |
| 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 |
| EP1753730A1 (en) * | 2004-06-04 | 2007-02-21 | Takeda Pharmaceutical Company Limited | Dipeptidyl peptidase inhibitors |
| WO2006019965A2 (en) | 2004-07-16 | 2006-02-23 | Takeda San Diego, Inc. | Dipeptidyl peptidase inhibitors |
| JP2008507541A (ja) * | 2004-07-23 | 2008-03-13 | ロイヤルティ，スーザン・マリー | ペプチダーゼ阻害剤 |
| US20060063719A1 (en) * | 2004-09-21 | 2006-03-23 | Point Therapeutics, Inc. | Methods for treating diabetes |
| EP1851216A2 (en) * | 2004-11-30 | 2007-11-07 | F.Hoffmann-La Roche Ag | Substituted benzoquinolizines as dpp-iv inhibitors for the treatment of diabetes |
| US7411093B2 (en) * | 2004-12-20 | 2008-08-12 | Hoffman-La Roche Inc. | Aminocycloalkanes as DPP-IV inhibitors |
| AU2005318597A1 (en) * | 2004-12-20 | 2006-06-29 | F. Hoffmann-La Roche Ag | 4-aminopiperidine derivatives |
| 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 |
| KR20080000665A (ko) * | 2005-04-22 | 2008-01-02 | 알란토스 파마슈티컬즈 홀딩, 인코포레이티드 | 디펩티딜 펩티다아제-ⅳ 억제제 |
| CA2605847C (en) * | 2005-04-26 | 2014-02-04 | Mitsubishi Tanabe Pharma Corporation | Ddp-iv inhibitors for the treatment of postprandial hyperlipidemia |
| WO2007033265A1 (en) * | 2005-09-14 | 2007-03-22 | Takeda Pharmaceutical Company Limited | Dipeptidyl peptidase inhibitors for treating diabetis |
| PT1931350E (pt) * | 2005-09-14 | 2014-02-12 | Takeda Pharmaceutical | Administração de inibidores de dipeptidil peptidase |
| WO2007033350A1 (en) | 2005-09-14 | 2007-03-22 | Takeda Pharmaceutical Company Limited | Dipeptidyl peptidase inhibitors for treating diabetes |
| TW200745080A (en) * | 2005-09-16 | 2007-12-16 | Takeda Pharmaceuticals Co | Polymorphs of tartrate salt of 2-[2-(3-(R)-amino-piperidin-1-yl)-5-fluoro-6-oxo-6H-pyrimidin-1-ylmethyl]-benzonitrile and methods of use therefor |
| EP1924567B1 (en) * | 2005-09-16 | 2012-08-22 | Takeda Pharmaceutical Company Limited | Process for the preparation of pyrimidinedione derivatives |
| TW200745079A (en) * | 2005-09-16 | 2007-12-16 | Takeda Pharmaceuticals Co | 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 and methods of use therefor |
| EP1995237A4 (en) * | 2006-03-08 | 2011-07-06 | Kyorin Seiyaku Kk | PROCESS FOR PREPARING AN AMINOACETYLPYRROLIDINCARBONITRILE DERIVATIVE AND PRODUCTION PRODUCT THEREOF |
| WO2007112347A1 (en) | 2006-03-28 | 2007-10-04 | Takeda Pharmaceutical Company Limited | Dipeptidyl peptidase inhibitors |
| 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 |
| DK1971862T3 (da) * | 2006-04-11 | 2011-02-14 | Arena Pharm Inc | Fremgangsmåder til anvendelse af GPR119-receptor til identificering af forbindelser anvendelige til øgning af knoglemasse hos en person |
| DK2073810T3 (da) * | 2006-09-13 | 2011-10-31 | Takeda Pharmaceutical | Anvendelse af 2-6-(3-aminio-piperidin-l-yl)-3-methyl-2,4-dioxo-3,4-dihydro-2H-pyrimidin-l-ylmethyl-4-fluor-benzonitril til behandling af diabetes, cancer, autoimmune sygdomme og HIV infektion |
| 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 |
| 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 |
| JPWO2008114857A1 (ja) * | 2007-03-22 | 2010-07-08 | 杏林製薬株式会社 | アミノアセチルピロリジンカルボニトリル誘導体の製造方法 |
| CN101652147B (zh) | 2007-04-03 | 2013-07-24 | 田边三菱制药株式会社 | 二肽基肽酶iv抑制化合物和甜味剂的并用 |
| CL2008003653A1 (es) | 2008-01-17 | 2010-03-05 | Mitsubishi Tanabe Pharma Corp | Uso de un inhibidor de sglt derivado de glucopiranosilo y un inhibidor de dppiv seleccionado para tratar la diabetes; y composicion farmaceutica. |
| EP2146210A1 (en) * | 2008-04-07 | 2010-01-20 | Arena Pharmaceuticals, Inc. | Methods of using A G protein-coupled receptor to identify peptide YY (PYY) secretagogues and compounds useful in the treatment of conditions modulated by PYY |
| CN102119139A (zh) * | 2008-08-07 | 2011-07-06 | 杏林制药株式会社 | 二环[2.2.2]辛胺衍生物的制造方法 |
| CN102186474A (zh) * | 2008-08-14 | 2011-09-14 | 杏林制药株式会社 | 稳定的医药组合物 |
| EP2344519B1 (en) | 2008-11-07 | 2016-09-28 | The General Hospital Corporation | C-terminal fragments of glucagon-like peptide-1 (glp-1) |
| US20100144140A1 (en) * | 2008-12-10 | 2010-06-10 | Novellus Systems, Inc. | Methods for depositing tungsten films having low resistivity for gapfill applications |
| AR077642A1 (es) | 2009-07-09 | 2011-09-14 | Arena Pharm Inc | Moduladores del metabolismo y el tratamiento de trastornos relacionados con el mismo |
| MX2012011631A (es) | 2010-04-06 | 2013-01-18 | Arena Pharm Inc | Moduladores del receptor gpr119 y el tratamiento de trastornos relacionados con el mismo. |
| JP5941916B2 (ja) | 2010-09-22 | 2016-06-29 | アリーナ ファーマシューティカルズ， インコーポレイテッド | Ｇｐｒ１１９レセプターのモジュレーターおよびそれに関連する障害の処置 |
| US9040481B2 (en) | 2010-11-02 | 2015-05-26 | The General Hospital Corporation | Methods for treating steatotic disease |
| 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 |
| WO2012145603A1 (en) | 2011-04-22 | 2012-10-26 | Arena Pharmaceuticals, Inc. | Modulators of the gpr119 receptor and the treatment of disorders related thereto |
| WO2012145604A1 (en) | 2011-04-22 | 2012-10-26 | 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 |
| WO2013006692A2 (en) | 2011-07-06 | 2013-01-10 | The General Hospital Corporation | Methods of treatment using a pentapeptide derived from the c-terminus of glucagon-like peptide 1 (glp-1) |
| WO2013055910A1 (en) | 2011-10-12 | 2013-04-18 | Arena Pharmaceuticals, Inc. | Modulators of the gpr119 receptor and the treatment of disorders related thereto |
| WO2014074668A1 (en) | 2012-11-08 | 2014-05-15 | Arena Pharmaceuticals, Inc. | Modulators of gpr119 and the treatment of disorders related thereto |
| RU2563234C2 (ru) * | 2012-12-10 | 2015-09-20 | Федеральное государственное бюджетное научное учреждение "Научно-исследовательский институт фармакологии имени В.В. Закусова" | Средство для предупреждения и коррекции проявлений диабета |
| HRP20171590T1 (hr) | 2013-06-05 | 2017-12-29 | Tricida Inc. | Polimeri koji vežu protone za oralnu primjenu |
| GB201415598D0 (en) | 2014-09-03 | 2014-10-15 | Univ Birmingham | Elavated Itercranial Pressure Treatment |
| PL3229816T3 (pl) | 2014-12-10 | 2020-09-21 | Tricida Inc. | Polimery wiążące protony do podawania doustnego |
| AU2016229982B2 (en) | 2015-03-09 | 2020-06-18 | Intekrin Therapeutics, Inc. | Methods for the treatment of nonalcoholic fatty liver disease and/or lipodystrophy |
| EP3452028A4 (en) | 2016-05-06 | 2020-04-15 | Tricida Inc. | COMPOSITIONS AND METHOD FOR TREATING ACID-BASED DISORDERS |
| 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 |
| AU2018360867B2 (en) | 2017-11-03 | 2024-12-12 | Tricida, Inc. | Compositions for and method of treating acid-base disorders |
| JPWO2019208700A1 (ja) * | 2018-04-26 | 2021-04-30 | ゼリア新薬工業株式会社 | ジペプチド及びこれを含有する医薬組成物 |
Family Cites Families (35)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US2961377A (en) * | 1957-08-05 | 1960-11-22 | Us Vitamin Pharm Corp | Oral anti-diabetic compositions and methods |
| US3174901A (en) * | 1963-01-31 | 1965-03-23 | Jan Marcel Didier Aron Samuel | Process for the oral treatment of diabetes |
| US3879541A (en) * | 1970-03-03 | 1975-04-22 | Bayer Ag | Antihyperglycemic methods and compositions |
| US3960949A (en) * | 1971-04-02 | 1976-06-01 | Schering Aktiengesellschaft | 1,2-Biguanides |
| CH602612A5 (enExample) * | 1974-10-11 | 1978-07-31 | Hoffmann La Roche | |
| DE3508251A1 (de) * | 1985-03-08 | 1986-09-11 | Merck Patent Gmbh, 6100 Darmstadt | Dipeptide |
| US4935493A (en) * | 1987-10-06 | 1990-06-19 | E. I. Du Pont De Nemours And Company | Protease inhibitors |
| US5433955A (en) * | 1989-01-23 | 1995-07-18 | Akzo N.V. | Site specific in vivo activation of therapeutic drugs |
| DD296075A5 (de) * | 1989-08-07 | 1991-11-21 | Martin-Luther-Universitaet Halle-Wittenberg,De | Verfahren zur herstellung neuer inhibitoren der dipeptidyl peptidase iv |
| US5462928A (en) * | 1990-04-14 | 1995-10-31 | New England Medical Center Hospitals, Inc. | Inhibitors of dipeptidyl-aminopeptidase type IV |
| JPH0819154B2 (ja) * | 1991-03-14 | 1996-02-28 | 江崎グリコ株式会社 | ジペプチジルカルボキシペプチダーゼを阻害するペプチド |
| IL106998A0 (en) * | 1992-09-17 | 1993-12-28 | Univ Florida | Brain-enhanced delivery of neuroactive peptides by sequential metabolism |
| IL111785A0 (en) * | 1993-12-03 | 1995-01-24 | Ferring Bv | Dp-iv inhibitors and pharmaceutical compositions containing them |
| US5705483A (en) * | 1993-12-09 | 1998-01-06 | Eli Lilly And Company | Glucagon-like insulinotropic peptides, compositions and methods |
| US5543396A (en) * | 1994-04-28 | 1996-08-06 | Georgia Tech Research Corp. | Proline phosphonate derivatives |
| AU2790895A (en) * | 1994-06-10 | 1996-01-05 | Universitaire Instelling Antwerpen | Purification of serine protease and synthetic inhibitors thereof |
| US5512549A (en) * | 1994-10-18 | 1996-04-30 | Eli Lilly And Company | Glucagon-like insulinotropic peptide analogs, compositions, and methods of use |
| US5614379A (en) * | 1995-04-26 | 1997-03-25 | Eli Lilly And Company | Process for preparing anti-obesity protein |
| DE122010000020I1 (de) * | 1996-04-25 | 2010-07-08 | Prosidion Ltd | Verfahren zur Senkung des Blutglukosespiegels in Säugern |
| US6006753A (en) * | 1996-08-30 | 1999-12-28 | Eli Lilly And Company | Use of GLP-1 or analogs to abolish catabolic changes after surgery |
| US5827898A (en) * | 1996-10-07 | 1998-10-27 | Shaman Pharmaceuticals, Inc. | Use of bisphenolic compounds to treat type II diabetes |
| 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 |
| DE19823831A1 (de) * | 1998-05-28 | 1999-12-02 | Probiodrug Ges Fuer Arzneim | Neue pharmazeutische Verwendung von Isoleucyl Thiazolidid und seinen Salzen |
| DE19828114A1 (de) * | 1998-06-24 | 2000-01-27 | Probiodrug Ges Fuer Arzneim | Produgs instabiler Inhibitoren der Dipeptidyl Peptidase IV |
| DE19828113A1 (de) * | 1998-06-24 | 2000-01-05 | Probiodrug Ges Fuer Arzneim | Prodrugs von Inhibitoren der Dipeptidyl Peptidase IV |
| DE19834591A1 (de) * | 1998-07-31 | 2000-02-03 | Probiodrug Ges Fuer Arzneim | Verfahren zur Steigerung des Blutglukosespiegels in Säugern |
| US6107317A (en) * | 1999-06-24 | 2000-08-22 | Novartis Ag | N-(substituted glycyl)-thiazolidines, pharmaceutical compositions containing them and their use in inhibiting dipeptidyl peptidase-IV |
| US6110949A (en) * | 1999-06-24 | 2000-08-29 | Novartis Ag | N-(substituted glycyl)-4-cyanothiazolidines, pharmaceutical compositions containing them and their use in inhibiting dipeptidyl peptidase-IV |
| US6172081B1 (en) * | 1999-06-24 | 2001-01-09 | Novartis Ag | Tetrahydroisoquinoline 3-carboxamide derivatives |
| AU1916401A (en) * | 1999-11-12 | 2001-06-06 | Guilford Pharmaceuticals Inc. | Dipeptidyl peptidase iv inhibitors and methods of making and using dipeptidyl peptidase iv inhibitors |
| US7064145B2 (en) * | 2000-02-25 | 2006-06-20 | Novo Nordisk A/S | Inhibition of beta cell degeneration |
| US6605589B1 (en) * | 2000-03-31 | 2003-08-12 | Parker Hughes Institute | Cathepsin inhibitors in cancer treatment |
| ES2582376T3 (es) * | 2000-03-31 | 2016-09-12 | Royalty Pharma Collection Trust | Método para la mejora de la señalización de islotes en diabetes mellitus y para su prevención |
| US20020037829A1 (en) * | 2000-08-23 | 2002-03-28 | Aronson Peter S. | Use of DPPIV inhibitors as diuretic and anti-hypertensive agents |
| UA74912C2 (en) * | 2001-07-06 | 2006-02-15 | Merck & Co Inc | Beta-aminotetrahydroimidazo-(1,2-a)-pyrazines and tetratriazolo-(4,3-a)-pyrazines as inhibitors of dipeptylpeptidase for the treatment or prevention of diabetes |
-
2001
- 2001-08-17 US US09/932,546 patent/US20020006899A1/en not_active Abandoned
-
2002
- 2002-04-05 US US10/117,022 patent/US20020110560A1/en not_active Abandoned
- 2002-07-23 RU RU2003110960/15A patent/RU2305553C2/ru active
- 2002-07-23 WO PCT/EP2002/008210 patent/WO2003015775A1/en not_active Ceased
- 2002-07-23 CN CNA028026748A patent/CN1582149A/zh active Pending
- 2002-07-23 EP EP02764760A patent/EP1416932A1/en not_active Withdrawn
- 2002-07-23 JP JP2003520734A patent/JP2005505531A/ja active Pending
- 2002-07-23 CA CA002423025A patent/CA2423025A1/en not_active Abandoned
-
2003
- 2003-03-17 ZA ZA2003/02126A patent/ZA200302126B/en unknown
- 2003-04-08 NO NO20031574A patent/NO20031574L/no not_active Application Discontinuation
-
2004
- 2004-12-22 US US11/022,087 patent/US20050107309A1/en not_active Abandoned
-
2009
- 2009-09-08 JP JP2009207484A patent/JP2009286799A/ja not_active Abandoned
-
2012
- 2012-04-27 US US13/458,484 patent/US20130116290A1/en not_active Abandoned
-
2016
- 2016-02-12 US US15/042,892 patent/US20170007582A1/en not_active Abandoned
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| JP2005505531A5 (enExample) | ||
| RU2003110960A (ru) | Новые ингибиторы дипептидилпептидазы iv и их применение для понижения кровяного давления | |
| RU2003105464A (ru) | Новые ингибиторы дипептидилпептидазы iv и их применение в качестве противораковых агентов | |
| AU2002321135B2 (en) | Dipepitdyl peptidase IV inhibitors and their uses as anti-cancer agents | |
| JP4966659B2 (ja) | 異なる細胞に機能的に影響を及ぼし、免疫性疾患、炎症性疾患、神経疾患、およびその他の疾患を治療するための二重のアラニルアミノペプチダーゼおよびジペプチジルペプチダーゼｉｖの阻害剤 | |
| US7109347B2 (en) | Dipeptidyl peptidase IV inhibitors and their uses as anti-cancer agents | |
| ES2243516T3 (es) | Preparaciones que contienen combinaciones de inhibidores enzimaticos y su utilizacion. | |
| JP3798337B2 (ja) | 新規α−アミノ酸化合物、その調製方法及びそれを含有する医薬組成物 | |
| ZA200402357B (en) | Peptidyl ketones as inhibitors of DPIV. | |
| ZA200302126B (en) | New dipeptidyl peptidase iv inhibitors and their uses for lowering blood pressure levels | |
| US20050107308A1 (en) | Dipeptidyl peptidase IV inhibitors and their uses for lowering blood pressure levels | |
| AU2002321135A1 (en) | Dipepitdyl peptidase IV inhibitors and their uses as anti-cancer agents | |
| KR20020040787A (ko) | 디펩티딜 펩티다제 ⅳ의 국소용 신규 효능제 | |
| JP2007508347A5 (enExample) | ||
| RU2010106877A (ru) | Дипептидные пролекарства и их применение | |
| WO1989012627A1 (en) | S-nitroso derivatives of ace inhibitors and the use thereof | |
| JP2005527504A (ja) | グルタミニルを基礎するｄｐｉｖ阻害剤 | |
| BRPI0612607A2 (pt) | inibidores de alfa proteìna de ativação de fibroblasto | |
| AU2005245962A1 (en) | Bacterial efflux pump inhibitors and methods of treating bacterial infections | |
| KR100341982B1 (ko) | 프롤릴엔도펩티다제억제제 | |
| KR890006572A (ko) | 아미노산 유도체 | |
| JP2006513141A5 (enExample) | ||
| PL181749B1 (pl) | Zwiazek do zapobiegania i leczenia zakrzepicy u ssaków oraz oraz kompozycja farmaceutyczna do zapobiegania i leczenia zakrzepicy u ssaków PL PL PL PL PL PL PL PL | |
| JP2004535459A (ja) | プロリルオリゴペプチダーゼ阻害活性を有する化合物、その製造方法ならびにその使用 | |
| AU2008339610A1 (en) | Methods of peptide modification |