JP2006513265A5 - - Google Patents
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- JP2006513265A5 JP2006513265A5 JP2005509979A JP2005509979A JP2006513265A5 JP 2006513265 A5 JP2006513265 A5 JP 2006513265A5 JP 2005509979 A JP2005509979 A JP 2005509979A JP 2005509979 A JP2005509979 A JP 2005509979A JP 2006513265 A5 JP2006513265 A5 JP 2006513265A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- substituted
- unsubstituted
- alkoxy
- 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.)
- Granted
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- 229910052736 halogen Inorganic materials 0.000 claims 120
- 150000002367 halogens Chemical class 0.000 claims 120
- 125000000217 alkyl group Chemical group 0.000 claims 109
- 125000003545 alkoxy group Chemical group 0.000 claims 83
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 57
- 125000001424 substituent group Chemical group 0.000 claims 51
- 229910052739 hydrogen Inorganic materials 0.000 claims 35
- 150000001875 compounds Chemical class 0.000 claims 30
- 239000001257 hydrogen Substances 0.000 claims 30
- 150000002431 hydrogen Chemical class 0.000 claims 18
- 229910052799 carbon Inorganic materials 0.000 claims 16
- -1 cyano, hydroxy Chemical group 0.000 claims 16
- 125000000623 heterocyclic group Chemical group 0.000 claims 16
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 16
- RWRDLPDLKQPQOW-UHFFFAOYSA-N Pyrrolidine Chemical compound C1CCNC1 RWRDLPDLKQPQOW-UHFFFAOYSA-N 0.000 claims 15
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 12
- 125000000753 cycloalkyl group Chemical group 0.000 claims 11
- YNAVUWVOSKDBBP-UHFFFAOYSA-N Morpholine Chemical compound C1COCCN1 YNAVUWVOSKDBBP-UHFFFAOYSA-N 0.000 claims 10
- NQRYJNQNLNOLGT-UHFFFAOYSA-N Piperidine Chemical compound C1CCNCC1 NQRYJNQNLNOLGT-UHFFFAOYSA-N 0.000 claims 10
- 125000004432 carbon atom Chemical group C* 0.000 claims 10
- GLUUGHFHXGJENI-UHFFFAOYSA-N Piperazine Chemical compound C1CNCCN1 GLUUGHFHXGJENI-UHFFFAOYSA-N 0.000 claims 8
- 125000004453 alkoxycarbonyl group Chemical group 0.000 claims 8
- 125000000325 methylidene group Chemical group [H]C([H])=* 0.000 claims 7
- 229910052757 nitrogen Inorganic materials 0.000 claims 7
- 239000008194 pharmaceutical composition Substances 0.000 claims 7
- 125000004043 oxo group Chemical group O=* 0.000 claims 6
- 125000003831 tetrazolyl group Chemical group 0.000 claims 6
- 102000023984 PPAR alpha Human genes 0.000 claims 5
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 5
- 108091008725 peroxisome proliferator-activated receptors alpha Proteins 0.000 claims 5
- 125000000335 thiazolyl group Chemical group 0.000 claims 5
- 241000124008 Mammalia Species 0.000 claims 4
- 125000003118 aryl group Chemical group 0.000 claims 4
- HONIICLYMWZJFZ-UHFFFAOYSA-N azetidine Chemical compound C1CNC1 HONIICLYMWZJFZ-UHFFFAOYSA-N 0.000 claims 4
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 4
- 125000004093 cyano group Chemical group *C#N 0.000 claims 4
- 125000001072 heteroaryl group Chemical group 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
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 4
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 3
- ZAMOUSCENKQFHK-UHFFFAOYSA-N Chlorine atom Chemical compound [Cl] ZAMOUSCENKQFHK-UHFFFAOYSA-N 0.000 claims 3
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical compound FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 claims 3
- 239000000556 agonist Substances 0.000 claims 3
- 125000003342 alkenyl group Chemical group 0.000 claims 3
- 125000004183 alkoxy alkyl group Chemical group 0.000 claims 3
- 125000004414 alkyl thio group Chemical group 0.000 claims 3
- 229910052801 chlorine Inorganic materials 0.000 claims 3
- 239000000460 chlorine Substances 0.000 claims 3
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 3
- 229910052731 fluorine Inorganic materials 0.000 claims 3
- 239000011737 fluorine Substances 0.000 claims 3
- 150000003839 salts Chemical class 0.000 claims 3
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 3
- WKBOTKDWSSQWDR-UHFFFAOYSA-N Bromine atom Chemical compound [Br] WKBOTKDWSSQWDR-UHFFFAOYSA-N 0.000 claims 2
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 2
- 101710198884 GATA-type zinc finger protein 1 Proteins 0.000 claims 2
- 102100039994 Gastric inhibitory polypeptide Human genes 0.000 claims 2
- 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 2
- 102000004877 Insulin Human genes 0.000 claims 2
- 108090001061 Insulin Proteins 0.000 claims 2
- PVNIIMVLHYAWGP-UHFFFAOYSA-N Niacin Chemical compound OC(=O)C1=CC=CN=C1 PVNIIMVLHYAWGP-UHFFFAOYSA-N 0.000 claims 2
- 102000002808 Pituitary adenylate cyclase-activating polypeptide Human genes 0.000 claims 2
- 108010004684 Pituitary adenylate cyclase-activating polypeptide Proteins 0.000 claims 2
- 102100040918 Pro-glucagon Human genes 0.000 claims 2
- GDTBXPJZTBHREO-UHFFFAOYSA-N bromine Substances BrBr GDTBXPJZTBHREO-UHFFFAOYSA-N 0.000 claims 2
- 229910052794 bromium Inorganic materials 0.000 claims 2
- 206010012601 diabetes mellitus Diseases 0.000 claims 2
- 229940125542 dual agonist Drugs 0.000 claims 2
- 125000005842 heteroatom Chemical group 0.000 claims 2
- 239000003112 inhibitor Substances 0.000 claims 2
- 229940125396 insulin Drugs 0.000 claims 2
- 229910052760 oxygen Inorganic materials 0.000 claims 2
- 229940044601 receptor agonist Drugs 0.000 claims 2
- 239000000018 receptor agonist Substances 0.000 claims 2
- 229920006395 saturated elastomer Polymers 0.000 claims 2
- 229910052717 sulfur Inorganic materials 0.000 claims 2
- HSINOMROUCMIEA-FGVHQWLLSA-N (2s,4r)-4-[(3r,5s,6r,7r,8s,9s,10s,13r,14s,17r)-6-ethyl-3,7-dihydroxy-10,13-dimethyl-2,3,4,5,6,7,8,9,11,12,14,15,16,17-tetradecahydro-1h-cyclopenta[a]phenanthren-17-yl]-2-methylpentanoic acid Chemical compound C([C@@]12C)C[C@@H](O)C[C@H]1[C@@H](CC)[C@@H](O)[C@@H]1[C@@H]2CC[C@]2(C)[C@@H]([C@H](C)C[C@H](C)C(O)=O)CC[C@H]21 HSINOMROUCMIEA-FGVHQWLLSA-N 0.000 claims 1
- 125000006700 (C1-C6) alkylthio group Chemical group 0.000 claims 1
- SXKBTDJJEQQEGE-UHFFFAOYSA-N 3-(3,5-dibromo-4-hydroxy-benzoyl)-2-ethyl-benzofuran-6-sulfonic acid [4-(thiazol-2-ylsulfamoyl)-phenyl]-amide Chemical compound CCC=1OC2=CC(S(=O)(=O)NC=3C=CC(=CC=3)S(=O)(=O)NC=3SC=CN=3)=CC=C2C=1C(=O)C1=CC(Br)=C(O)C(Br)=C1 SXKBTDJJEQQEGE-UHFFFAOYSA-N 0.000 claims 1
- MVQVNTPHUGQQHK-UHFFFAOYSA-N 3-pyridinemethanol Chemical compound OCC1=CC=CN=C1 MVQVNTPHUGQQHK-UHFFFAOYSA-N 0.000 claims 1
- 125000001255 4-fluorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C([H])=C1F 0.000 claims 1
- NFFXEUUOMTXWCX-UHFFFAOYSA-N 5-[(2,4-dioxo-1,3-thiazolidin-5-yl)methyl]-2-methoxy-n-[[4-(trifluoromethyl)phenyl]methyl]benzamide Chemical group C1=C(C(=O)NCC=2C=CC(=CC=2)C(F)(F)F)C(OC)=CC=C1CC1SC(=O)NC1=O NFFXEUUOMTXWCX-UHFFFAOYSA-N 0.000 claims 1
- 229940077274 Alpha glucosidase inhibitor Drugs 0.000 claims 1
- 229940123208 Biguanide Drugs 0.000 claims 1
- XNCOSPRUTUOJCJ-UHFFFAOYSA-N Biguanide Chemical compound NC(N)=NC(N)=N XNCOSPRUTUOJCJ-UHFFFAOYSA-N 0.000 claims 1
- 125000006374 C2-C10 alkenyl group Chemical group 0.000 claims 1
- 102000016622 Dipeptidyl Peptidase 4 Human genes 0.000 claims 1
- 229940124213 Dipeptidyl peptidase 4 (DPP IV) inhibitor Drugs 0.000 claims 1
- 101000930822 Giardia intestinalis Dipeptidyl-peptidase 4 Proteins 0.000 claims 1
- 229940122904 Glucagon receptor antagonist Drugs 0.000 claims 1
- 229940089838 Glucagon-like peptide 1 receptor agonist Drugs 0.000 claims 1
- 229940121710 HMGCoA reductase inhibitor Drugs 0.000 claims 1
- 229940122199 Insulin secretagogue Drugs 0.000 claims 1
- 229940122355 Insulin sensitizer Drugs 0.000 claims 1
- 229940122054 Peroxisome proliferator-activated receptor delta agonist Drugs 0.000 claims 1
- 229940080774 Peroxisome proliferator-activated receptor gamma agonist Drugs 0.000 claims 1
- 102000014743 Pituitary Adenylate Cyclase-Activating Polypeptide Receptors Human genes 0.000 claims 1
- 108010064032 Pituitary Adenylate Cyclase-Activating Polypeptide Receptors Proteins 0.000 claims 1
- 102000001494 Sterol O-Acyltransferase Human genes 0.000 claims 1
- 108010054082 Sterol O-acyltransferase Proteins 0.000 claims 1
- 229940100389 Sulfonylurea Drugs 0.000 claims 1
- 239000004480 active ingredient Substances 0.000 claims 1
- 125000002252 acyl group Chemical group 0.000 claims 1
- 239000002404 acyltransferase inhibitor Substances 0.000 claims 1
- 239000003888 alpha glucosidase inhibitor Substances 0.000 claims 1
- 239000002260 anti-inflammatory agent Substances 0.000 claims 1
- 229940124599 anti-inflammatory drug Drugs 0.000 claims 1
- 230000003579 anti-obesity Effects 0.000 claims 1
- 239000003529 anticholesteremic agent Substances 0.000 claims 1
- 229940127226 anticholesterol agent Drugs 0.000 claims 1
- 239000002220 antihypertensive agent Substances 0.000 claims 1
- 229940127088 antihypertensive drug Drugs 0.000 claims 1
- 239000003963 antioxidant agent Substances 0.000 claims 1
- 239000003613 bile acid Substances 0.000 claims 1
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 claims 1
- 239000003795 chemical substances by application Substances 0.000 claims 1
- 230000001906 cholesterol absorption Effects 0.000 claims 1
- 125000006255 cyclopropyl carbonyl group Chemical group [H]C1([H])C([H])([H])C1([H])C(*)=O 0.000 claims 1
- 239000003603 dipeptidyl peptidase IV inhibitor Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 230000009977 dual effect Effects 0.000 claims 1
- 230000000694 effects Effects 0.000 claims 1
- 125000003754 ethoxycarbonyl group Chemical group C(=O)(OCC)* 0.000 claims 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 1
- 108010036598 gastric inhibitory polypeptide receptor Proteins 0.000 claims 1
- 239000003877 glucagon like peptide 1 receptor agonist Substances 0.000 claims 1
- 239000002471 hydroxymethylglutaryl coenzyme A reductase inhibitor Substances 0.000 claims 1
- 201000001421 hyperglycemia Diseases 0.000 claims 1
- 230000002401 inhibitory effect Effects 0.000 claims 1
- 125000003253 isopropoxy group Chemical group [H]C([H])([H])C([H])(O*)C([H])([H])[H] 0.000 claims 1
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 1
- 125000002816 methylsulfanyl group Chemical group [H]C([H])([H])S[*] 0.000 claims 1
- 125000001624 naphthyl group Chemical group 0.000 claims 1
- 229960003512 nicotinic acid Drugs 0.000 claims 1
- 235000001968 nicotinic acid Nutrition 0.000 claims 1
- 239000011664 nicotinic acid Substances 0.000 claims 1
- 229960004738 nicotinyl alcohol Drugs 0.000 claims 1
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 1
- 239000003801 protein tyrosine phosphatase 1B inhibitor Substances 0.000 claims 1
- 238000006467 substitution reaction Methods 0.000 claims 1
- 125000000391 vinyl group Chemical group [H]C([*])=C([H])[H] 0.000 claims 1
- 229920002554 vinyl polymer Polymers 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US43538902P | 2002-12-20 | 2002-12-20 | |
| US46931503P | 2003-05-09 | 2003-05-09 | |
| PCT/US2003/040114 WO2004058266A1 (en) | 2002-12-20 | 2003-12-16 | 3-amino-4-phenylbutanoic acid derivatives as dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2006513265A JP2006513265A (ja) | 2006-04-20 |
| JP2006513265A5 true JP2006513265A5 (enExample) | 2006-08-10 |
| JP4504924B2 JP4504924B2 (ja) | 2010-07-14 |
Family
ID=32685390
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2005509979A Expired - Fee Related JP4504924B2 (ja) | 2002-12-20 | 2003-12-16 | 糖尿病の治療および予防のためのジペプチジルペプチダーゼ阻害薬としての3−アミノ−4−フェニルブタン酸誘導体 |
Country Status (6)
| Country | Link |
|---|---|
| US (1) | US20060052382A1 (enExample) |
| EP (1) | EP1583534A4 (enExample) |
| JP (1) | JP4504924B2 (enExample) |
| AU (1) | AU2003297219A1 (enExample) |
| CA (1) | CA2508947A1 (enExample) |
| WO (1) | WO2004058266A1 (enExample) |
Families Citing this family (86)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP3909056B2 (ja) | 2001-06-27 | 2007-04-25 | スミスクライン ビーチャム コーポレーション | ジペプチジルペプチダーゼ阻害剤としてのフルオロピロリジン類 |
| EP1490335B1 (en) * | 2002-03-25 | 2007-09-19 | Merck & Co., Inc. | Beta-amino heterocyclic dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes |
| WO2004007468A1 (en) | 2002-07-15 | 2004-01-22 | Merck & Co., Inc. | Piperidino pyrimidine dipeptidyl peptidase inhibitors for the treatment of diabetes |
| WO2004032836A2 (en) | 2002-10-07 | 2004-04-22 | Merck & Co., Inc. | Antidiabetic beta-amino heterocylcic dipeptidyl peptidase inhibitors |
| HRP20050343A2 (en) | 2002-10-18 | 2007-03-31 | Merck & Co. Inc. | Beta-amino heterocyclic dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes |
| EP1583534A4 (en) * | 2002-12-20 | 2007-08-29 | Merck & Co Inc | 3-AMINO-4-PHENYLBUTANIC ACID DERIVATIVES AS DIPEPTIDYL-PEPTIDASE INHIBITORS FOR THE TREATMENT OR PREVENTION OF DIABETES |
| CA2512546A1 (en) | 2003-01-17 | 2004-08-05 | Merck & Co., Inc. | 3-amino-4-phenylbutanoic acid derivatives as dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes |
| JP2006516573A (ja) | 2003-01-31 | 2006-07-06 | メルク エンド カムパニー インコーポレーテッド | 糖尿病の治療および予防のためのジペプチジルペプチダーゼ阻害薬としての3−アミノ−4−フェニルブタン酸誘導体 |
| US20040242568A1 (en) | 2003-03-25 | 2004-12-02 | Syrrx, Inc. | Dipeptidyl peptidase inhibitors |
| WO2004103276A2 (en) | 2003-05-14 | 2004-12-02 | Merck & Co., Inc. | 3-amino-4-phenylbutanoic acid derivatives as dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes |
| 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 |
| WO2004110436A1 (en) | 2003-06-06 | 2004-12-23 | Merck & Co., Inc. | Fused indoles as dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes |
| US7456204B2 (en) | 2003-06-17 | 2008-11-25 | Merck & Co., Inc. | Cyclohexylglycine derivatives as dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes |
| CN1882551A (zh) | 2003-07-31 | 2006-12-20 | 麦克公司 | 用作用于治疗或预防糖尿病的二肽基肽酶-iv酶抑制剂的六氢二氮杂吖庚因酮 |
| MXPA06001601A (es) | 2003-08-13 | 2006-08-25 | Takeda Pharmaceutical | Derivados de 4-pirimidona y su uso como inhibidores de dipeptidilpeptidasa. |
| WO2005108382A1 (en) | 2004-05-04 | 2005-11-17 | Merck & Co., Inc. | 1,2,4-oxadiazole derivatives as dipeptidyl peptidase-iv inhibitors for the treatment or prevention of diabetes |
| WO2005116029A1 (en) | 2004-05-18 | 2005-12-08 | Merck & Co., Inc. | Cyclohexylalanine derivatives as dipeptidyl peptidase-iv inhibitors for the treatment or prevention of diabetes |
| US7482336B2 (en) | 2004-06-21 | 2009-01-27 | Merck & Co., Inc. | Aminocyclohexanes as dipeptidyl peptidase-IV inhibitors for the treatment or prevention of diabetes |
| EP1794120B1 (en) | 2004-07-23 | 2012-04-11 | Nuada, LLC | Peptidase inhibitors |
| DE602005022320D1 (de) | 2004-08-23 | 2010-08-26 | Merck Sharp & Dohme | Kondensierte triazolderivate als dipeptidylpeptidase-iv-hemmer zur behandlung bzw. prävention von diabetes |
| US7884104B2 (en) | 2004-10-01 | 2011-02-08 | Merck Sharp & Dohme Corp. | Aminopiperidines as dipeptidyl peptidase-IV inhibitors for the treatment or prevention of diabetes |
| 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 |
| TWI357902B (en) * | 2005-04-01 | 2012-02-11 | Lg Life Science Ltd | Dipeptidyl peptidase-iv inhibiting compounds, meth |
| EP1928237A4 (en) | 2005-09-02 | 2011-03-09 | Abbott Lab | NEW HETEROCYCLES BASED ON IMIDAZO |
| NZ566799A (en) | 2005-09-14 | 2011-04-29 | Takeda Pharmaceutical | Dipeptidyl peptidase inhibitors for treating diabetes |
| WO2007035629A2 (en) | 2005-09-16 | 2007-03-29 | Takeda Pharmaceutical Company Limited | Process for the preparation of pyrimidinedione derivatives |
| WO2007078726A2 (en) * | 2005-12-16 | 2007-07-12 | Merck & Co., Inc. | Pharmaceutical compositions of combinations of dipeptidyl peptidase-4 inhibitors with metformin |
| US20090156465A1 (en) | 2005-12-30 | 2009-06-18 | Sattigeri Jitendra A | Derivatives of beta-amino acid as dipeptidyl peptidase-iv inhibitors |
| WO2007112347A1 (en) | 2006-03-28 | 2007-10-04 | Takeda Pharmaceutical Company Limited | Dipeptidyl peptidase inhibitors |
| NZ571110A (en) * | 2006-04-11 | 2011-03-31 | Arena Pharm Inc | Methods of using GPR119 receptor to identify Glucose-dependent Insulinotropic Peptide (GIP) secretagogue 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 |
| AU2007235876A1 (en) | 2006-04-12 | 2007-10-18 | Probiodrug Ag | Enzyme inhibitors |
| US8278345B2 (en) | 2006-11-09 | 2012-10-02 | Probiodrug Ag | Inhibitors of glutaminyl cyclase |
| 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 |
| ATE554085T1 (de) | 2006-11-30 | 2012-05-15 | Probiodrug Ag | Neue inhibitoren von glutaminylcyclase |
| WO2008128985A1 (en) | 2007-04-18 | 2008-10-30 | Probiodrug Ag | Thiourea derivatives as glutaminyl cyclase inhibitors |
| CN101417999A (zh) * | 2007-10-25 | 2009-04-29 | 上海恒瑞医药有限公司 | 哌嗪类衍生物,其制备方法及其在医药上的应用 |
| CN101468988A (zh) | 2007-12-26 | 2009-07-01 | 上海恒瑞医药有限公司 | 哌嗪类衍生物,其制备方法及其在医药上的应用 |
| JP5640208B2 (ja) * | 2008-01-24 | 2014-12-17 | パナセア バイオテック リミテッド | 新規複素環化合物 |
| 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 |
| US20110230472A1 (en) * | 2008-08-29 | 2011-09-22 | Shionogi & Co., Ltd. | Ring-fused azole derivative having pi3k-inhibiting activity |
| JP5781930B2 (ja) * | 2008-09-12 | 2015-09-24 | カディラ ファーマシューティカルズ リミテッド | 新規なジペプチジルペプチダーゼ(dp−iv)化合物 |
| CN101849944A (zh) * | 2009-03-31 | 2010-10-06 | 江苏恒瑞医药股份有限公司 | 治疗2型糖尿病的药物组合物 |
| CN101899048B (zh) * | 2009-05-27 | 2013-04-17 | 上海恒瑞医药有限公司 | (R)-7-[3-氨基-4-(2,4,5-三氟-苯基)-丁酰]-3-三氟甲基-5,6,7,8-四氢-咪唑并[1,5-a]吡嗪-1-羧酸甲酯的盐 |
| UY32776A (es) | 2009-07-09 | 2011-02-28 | Irm Llc | Compuestos de imidazopirazinas sustituidas para el tratamiento de enfermedades parasitarias,composiciones farmacéuticas que los contienen y aplicación. |
| AR077642A1 (es) | 2009-07-09 | 2011-09-14 | Arena Pharm Inc | Moduladores del metabolismo y el tratamiento de trastornos relacionados con el mismo |
| JP5916387B2 (ja) | 2009-08-03 | 2016-05-11 | 株式会社カネカ | ジペプチジルペプチダーゼ−4阻害剤 |
| PL2475428T3 (pl) | 2009-09-11 | 2015-12-31 | Probiodrug Ag | Pochodne heterocykliczne jako inhibitory cyklazy glutaminowej |
| ES2586231T3 (es) | 2010-03-03 | 2016-10-13 | Probiodrug Ag | Inhibidores de glutaminil ciclasa |
| MX2012010470A (es) | 2010-03-10 | 2012-10-09 | Probiodrug Ag | Inhibidores heterociclicos d ciclasa de glutaminilo (qc, ec .3 2. 5). |
| JP2013523819A (ja) | 2010-04-06 | 2013-06-17 | 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 |
| US8541596B2 (en) | 2010-04-21 | 2013-09-24 | Probiodrug Ag | Inhibitors |
| WO2011146358A1 (en) | 2010-05-21 | 2011-11-24 | Merck Sharp & Dohme Corp. | Substituted seven-membered heterocyclic compounds as dipeptidyl peptidase-iv inhibitors for the treatment of diabetes |
| IN2010DE02164A (enExample) * | 2010-09-13 | 2015-07-24 | Panacea Biotec Ltd | |
| CN103221410B (zh) | 2010-09-22 | 2017-09-15 | 艾尼纳制药公司 | Gpr119受体调节剂和对与其相关的障碍的治疗 |
| WO2012078448A1 (en) | 2010-12-06 | 2012-06-14 | Schering Corporation | Tricyclic heterocycles useful as dipeptidyl peptidase-iv inhibitors |
| EP2686313B1 (en) | 2011-03-16 | 2016-02-03 | Probiodrug AG | Benzimidazole derivatives as inhibitors of glutaminyl cyclase |
| US20140018371A1 (en) | 2011-04-01 | 2014-01-16 | Arena Pharmaceuticals, Inc. | Modulators Of The GPR119 Receptor And The Treatment Of Disorders Related Thereto |
| EP2508506A1 (en) | 2011-04-08 | 2012-10-10 | LEK Pharmaceuticals d.d. | Preparation of sitagliptin intermediates |
| 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 |
| EP2527320A1 (en) | 2011-05-27 | 2012-11-28 | LEK Pharmaceuticals d.d. | Preparation of Sitagliptin Intermediates |
| WO2012170702A1 (en) | 2011-06-08 | 2012-12-13 | Arena Pharmaceuticals, Inc. | Modulators of the gpr119 receptor and the treatment of disorders related thereto |
| JP2014518266A (ja) | 2011-06-29 | 2014-07-28 | メルク・シャープ・アンド・ドーム・コーポレーション | ジペプチジルペプチダーゼ−iv阻害剤の新規結晶形 |
| EP2729468A4 (en) | 2011-07-05 | 2015-03-18 | Merck Sharp & Dohme | Tricyclic heterocycles useful as dipeptidyl peptidase-iv inhibitors |
| EP2736909B1 (en) | 2011-07-27 | 2017-03-29 | Farma GRS, d.o.o. | Process for the preparation of sitagliptin and its pharmaceutically acceptable salts |
| WO2013055910A1 (en) | 2011-10-12 | 2013-04-18 | Arena Pharmaceuticals, Inc. | Modulators of the gpr119 receptor and the treatment of disorders related thereto |
| TWI571466B (zh) | 2011-10-14 | 2017-02-21 | 艾伯維有限公司 | 用於治療癌症及免疫與自體免疫疾病之細胞凋亡誘發劑 |
| EP2814485A4 (en) | 2012-02-17 | 2015-08-26 | Merck Sharp & Dohme | DIPEPTIDYLPEPTIDASE IV INHIBITORS FOR THE TREATMENT OR PREVENTION OF DIABETES |
| EP2874622A4 (en) | 2012-07-23 | 2015-12-30 | Merck Sharp & Dohme | TREATMENT OF DIABETES WITH DIPEPTIDYLPEPTIDASE IV INHIBITORS |
| EP2874626A4 (en) | 2012-07-23 | 2016-03-23 | Merck Sharp & Dohme | TREATMENT OF DIABETES WITH DIPEPTIDYLPEPTIDASE IV INHIBITORS |
| TWI500613B (zh) | 2012-10-17 | 2015-09-21 | Cadila Healthcare Ltd | 新穎之雜環化合物 |
| WO2014074668A1 (en) | 2012-11-08 | 2014-05-15 | Arena Pharmaceuticals, Inc. | Modulators of gpr119 and the treatment of disorders related thereto |
| WO2014127747A1 (zh) * | 2013-02-22 | 2014-08-28 | 成都先导药物开发有限公司 | 一种抑制dpp-iv的化合物及其中间体 |
| CN105669682B (zh) * | 2013-02-22 | 2019-08-30 | 成都先导药物开发股份有限公司 | 一种dpp-iv抑制剂的中间体 |
| JP6574474B2 (ja) | 2014-07-21 | 2019-09-11 | メルク・シャープ・アンド・ドーム・コーポレーションMerck Sharp & Dohme Corp. | キラルジペプチジルペプチダーゼ−iv阻害剤の製造方法 |
| GB201415598D0 (en) | 2014-09-03 | 2014-10-15 | Univ Birmingham | Elavated Itercranial Pressure Treatment |
| CN107683135A (zh) | 2015-03-09 | 2018-02-09 | 因特克林医疗有限公司 | 用于治疗非酒精性脂肪肝疾病和/或脂肪营养不良的方法 |
| CA2994027C (en) * | 2015-07-31 | 2023-10-10 | Merck Patent Gmbh | Bicyclic heterocyclic derivatives |
| AU2018249822A1 (en) | 2017-04-03 | 2019-10-31 | Coherus Biosciences Inc. | PPArgamma agonist for treatment of progressive supranuclear palsy |
| CN110691597A (zh) | 2017-04-24 | 2020-01-14 | 诺华股份有限公司 | 2-氨基-1-(2-(4-氟苯基)-3-(4-氟苯基氨基)-8,8-二甲基-5,6-二氢咪唑并[1,2-a]吡嗪-7(8H)-基)乙酮及其组合的治疗方案 |
| PL3461819T3 (pl) | 2017-09-29 | 2020-11-30 | Probiodrug Ag | Inhibitory cyklazy glutaminylowej |
| JP2025522970A (ja) * | 2022-07-14 | 2025-07-17 | ザ スクリプス リサーチ インスティテュート | 肺疾患の治療のために2型肺胞細胞を増殖させる小分子調整剤 |
| CN119390698B (zh) * | 2024-09-26 | 2025-11-18 | 同济大学 | 一种西格列汀中间体的合成方法 |
| CN119613413B (zh) * | 2024-12-26 | 2026-02-06 | 上海皓元医药股份有限公司 | 一种非唑奈坦的制备方法 |
Family Cites Families (20)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4386090A (en) * | 1980-12-22 | 1983-05-31 | Delalande S.A. | Nitrogen containing 2,3-dihydro naphthalenes, compositions and use |
| IL111785A0 (en) * | 1993-12-03 | 1995-01-24 | Ferring Bv | Dp-iv inhibitors and pharmaceutical compositions containing them |
| US6673927B2 (en) * | 1996-02-16 | 2004-01-06 | Societe De Conseils De Recherches Et D'applications Scientifiques, S.A.S. | Farnesyl transferase inhibitors |
| DE122010000020I1 (de) * | 1996-04-25 | 2010-07-08 | Prosidion Ltd | Verfahren zur Senkung des Blutglukosespiegels in Säugern |
| 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 |
| US6251902B1 (en) * | 1997-06-25 | 2001-06-26 | Pfizer Inc. | Dipeptide derivatives as growth hormone secretagogues |
| FR2780974B1 (fr) * | 1998-07-08 | 2001-09-28 | Sod Conseils Rech Applic | Utilisation de derives d'imidazopyrazines pour preparer un medicament destine a traiter les pathologies qui resultent de la formation de la proteine g heterotrimetrique |
| CO5150173A1 (es) * | 1998-12-10 | 2002-04-29 | Novartis Ag | Compuestos n-(glicilo sustituido)-2-cianopirrolidinas inhibidores de peptidasa de dipeptidilo-iv (dpp-iv) los cuales son efectivos en el tratamiento de condiciones mediadas por la inhibicion de dpp-iv |
| US6395767B2 (en) * | 2000-03-10 | 2002-05-28 | Bristol-Myers Squibb Company | Cyclopropyl-fused pyrrolidine-based inhibitors of dipeptidyl peptidase IV and method |
| GB0010183D0 (en) * | 2000-04-26 | 2000-06-14 | Ferring Bv | Inhibitors of dipeptidyl peptidase IV |
| US6432969B1 (en) * | 2000-06-13 | 2002-08-13 | Novartis Ag | N-(substituted glycyl)-2 cyanopyrrolidines, pharmaceutical compositions containing them and their use in inhibiting dipeptidyl peptidase-IV |
| US7566734B2 (en) * | 2000-08-01 | 2009-07-28 | Societe De Conseils De Recherches Et D'applications Scientifiques, S.A.S. | Imidazolyl derivatives |
| 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 |
| EP1490335B1 (en) * | 2002-03-25 | 2007-09-19 | Merck & Co., Inc. | Beta-amino heterocyclic dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes |
| EP1583534A4 (en) * | 2002-12-20 | 2007-08-29 | Merck & Co Inc | 3-AMINO-4-PHENYLBUTANIC ACID DERIVATIVES AS DIPEPTIDYL-PEPTIDASE INHIBITORS FOR THE TREATMENT OR PREVENTION OF DIABETES |
| US20070099884A1 (en) * | 2003-06-06 | 2007-05-03 | Erondu Ngozi E | Combination therapy for the treatment of diabetes |
| JO2625B1 (en) * | 2003-06-24 | 2011-11-01 | ميرك شارب اند دوم كوربوريشن | Phosphoric acid salts of dipeptidyl betidase inhibitor 4 |
| CN100457108C (zh) * | 2003-09-02 | 2009-02-04 | 默克公司 | 一种二肽基肽酶iv抑制剂的磷酸盐新晶体 |
| WO2005030127A2 (en) * | 2003-09-23 | 2005-04-07 | Merck & Co., Inc. | Novel crystalline form of a phosphoric acid salt of a dipeptidyl peptidase-iv inhibitor |
| US20060270722A1 (en) * | 2005-05-31 | 2006-11-30 | Thornberry Nancy A | Combination of a dipeptidyl peptidase-IV inhibitor and a dual PPAR agonist for the treatment of diabetes and obesity |
-
2003
- 2003-12-16 EP EP03814066A patent/EP1583534A4/en not_active Withdrawn
- 2003-12-16 AU AU2003297219A patent/AU2003297219A1/en not_active Abandoned
- 2003-12-16 WO PCT/US2003/040114 patent/WO2004058266A1/en not_active Ceased
- 2003-12-16 JP JP2005509979A patent/JP4504924B2/ja not_active Expired - Fee Related
- 2003-12-16 US US10/540,283 patent/US20060052382A1/en not_active Abandoned
- 2003-12-16 CA CA002508947A patent/CA2508947A1/en not_active Abandoned
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