JP2006513265A5 - - Google Patents
Download PDFInfo
- Publication number
- 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
Links
- 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 (https=) | 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 (https=) |
| EP (1) | EP1583534A4 (https=) |
| JP (1) | JP4504924B2 (https=) |
| AU (1) | AU2003297219A1 (https=) |
| CA (1) | CA2508947A1 (https=) |
| WO (1) | WO2004058266A1 (https=) |
Families Citing this family (86)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ES2296979T3 (es) | 2001-06-27 | 2008-05-01 | Smithkline Beecham Corporation | Fluoropirrolidinas como inhibidores de dipeptidil peptidasa. |
| ATE373660T1 (de) * | 2002-03-25 | 2007-10-15 | Merck & Co Inc | Heterocyclische beta-aminoverbindungen als inhibitoren der dipeptidylpeptidase zur behandlung bzw. prävention von diabetes |
| US7208498B2 (en) | 2002-07-15 | 2007-04-24 | Merck & Co., Inc. | Piperidino pyrimidine dipeptidyl peptidase inhibitors for the treatment of diabetes |
| ATE370141T1 (de) | 2002-10-07 | 2007-09-15 | Merck & Co Inc | Antidiabetische heterocyclische beta- aminoverbindungen als inhibitoren von dipeptidylpeptidase |
| KR20050067418A (ko) | 2002-10-18 | 2005-07-01 | 머크 앤드 캄파니 인코포레이티드 | 당뇨병을 치료 또는 예방하기 위한 베타-아미노헤테로사이클릭 디펩티딜 펩티다제 억제제 |
| WO2004058266A1 (en) * | 2002-12-20 | 2004-07-15 | Merck & Co., Inc. | 3-amino-4-phenylbutanoic acid derivatives as dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes |
| WO2004064778A2 (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 |
| WO2004069162A2 (en) | 2003-01-31 | 2004-08-19 | Merck & Co., Inc. | 3-amino-4-phenylbutanoic acid derivatives as dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes |
| US7550590B2 (en) | 2003-03-25 | 2009-06-23 | Takeda Pharmaceutical Company Limited | Dipeptidyl peptidase inhibitors |
| WO2004103993A1 (en) | 2003-05-14 | 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 |
| WO2004110436A1 (en) | 2003-06-06 | 2004-12-23 | Merck & Co., Inc. | Fused indoles as dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes |
| CN1809544A (zh) | 2003-06-17 | 2006-07-26 | 麦克公司 | 作为二肽基肽酶抑制剂用于治疗或预防糖尿病的环己基甘氨酸衍生物 |
| AU2004261186A1 (en) | 2003-07-31 | 2005-02-10 | Merck & Co., Inc. | Hexahydrodiazepinones as dipeptidyl peptidase-IV inhibitors for the treatment or prevention of diabetes |
| KR20060041309A (ko) | 2003-08-13 | 2006-05-11 | 다케다 야쿠힌 고교 가부시키가이샤 | ４-피리미돈 유도체 및 펩티딜 펩티다제 저해제로서의 그의용도 |
| CN1950349A (zh) | 2004-05-04 | 2007-04-18 | 默克公司 | 作为用于治疗或预防糖尿病的二肽基肽酶－ⅳ抑制剂的1,2,4－噁二唑衍生物 |
| AU2005247895A1 (en) | 2004-05-18 | 2005-12-08 | Merck & Co., Inc. | Cyclohexylalanine derivatives as dipeptidyl peptidase-IV inhibitors for the treatment or prevention of diabetes |
| AU2005265148B2 (en) | 2004-06-21 | 2011-01-20 | Merck Sharp & Dohme Corp. | Aminocyclohexanes as dipeptidyl peptidase-IV inhibitors for the treatment or prevention of diabetes |
| ATE553077T1 (de) | 2004-07-23 | 2012-04-15 | Nuada Llc | Peptidaseinhibitoren |
| AU2005277283A1 (en) | 2004-08-23 | 2006-03-02 | Merck Sharp & Dohme Corp. | Fused triazole derivatives as dipeptidyl peptidase-IV inhibitors for the treatment or prevention of diabetes |
| AU2005292134B2 (en) | 2004-10-01 | 2010-12-23 | 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 |
| US7709468B2 (en) | 2005-09-02 | 2010-05-04 | Abbott Laboratories | Imidazo based heterocycles |
| GEP20135838B (en) | 2005-09-14 | 2013-06-10 | Takeda Pharmaceutical | Dipeptidyl peptidase inhibitors usage at diabetes treatment |
| CN101360723A (zh) | 2005-09-16 | 2009-02-04 | 武田药品工业株式会社 | 制备嘧啶二酮衍生物的方法 |
| CN101365432B (zh) * | 2005-12-16 | 2011-06-22 | 默沙东公司 | 二肽基肽酶-4抑制剂与二甲双胍的组合的药物组合物 |
| 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 |
| 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 |
| SG10201404220TA (en) | 2006-04-11 | 2014-10-30 | Arena Pharm Inc | Methods of using gpr119 receptor to identify compounds useful for increasing bone mass in an individual |
| AU2007235876A1 (en) | 2006-04-12 | 2007-10-18 | Probiodrug Ag | Enzyme inhibitors |
| EP2089383B1 (en) | 2006-11-09 | 2015-09-16 | Probiodrug AG | 3-hydr0xy-1,5-dihydr0-pyrr0l-2-one derivatives as inhibitors of glutaminyl cyclase for the treatment of ulcer, cancer and other diseases |
| 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 |
| US9126987B2 (en) | 2006-11-30 | 2015-09-08 | Probiodrug Ag | Inhibitors of glutaminyl cyclase |
| JP5667440B2 (ja) | 2007-04-18 | 2015-02-12 | プロビオドルグ エージー | グルタミニルシクラーゼ阻害剤としてのチオ尿素誘導体 |
| 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 |
| EA018612B1 (ru) * | 2008-01-24 | 2013-09-30 | Панацеа Биотек Лимитед | Новые гетероциклические соединения |
| 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 |
| WO2010024258A1 (ja) * | 2008-08-29 | 2010-03-04 | 塩野義製薬株式会社 | Ｐｉ３ｋ阻害活性を有する縮環アゾール誘導体 |
| EP2343973B1 (en) * | 2008-09-12 | 2016-02-17 | Cadila Pharmaceuticals Ltd. | Prodrugs of Sitagliptin |
| 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 |
| TWI421252B (zh) * | 2009-07-09 | 2014-01-01 | Irm Llc | 用於治療寄生蟲疾病之化合物及組合物 |
| AR077642A1 (es) | 2009-07-09 | 2011-09-14 | Arena Pharm Inc | Moduladores del metabolismo y el tratamiento de trastornos relacionados con el mismo |
| US20120189611A1 (en) * | 2009-08-03 | 2012-07-26 | Kaneka Corporation | Dipeptidyl peptidase-4 inhibitor |
| JP5934645B2 (ja) | 2009-09-11 | 2016-06-15 | プロビオドルグ エージー | グルタミニルシクラーゼ阻害剤としてのヘテロ環式誘導体 |
| WO2011107530A2 (en) | 2010-03-03 | 2011-09-09 | Probiodrug Ag | Novel inhibitors |
| JP5688745B2 (ja) | 2010-03-10 | 2015-03-25 | プロビオドルグ エージー | グルタミニルシクラーゼ（ｑｃ、ｅｃ２．３．２．５）の複素環阻害剤 |
| AU2011237775A1 (en) | 2010-04-06 | 2012-11-22 | Arena Pharmaceuticals, Inc. | Modulators of the GPR119 receptor and the treatment of disorders related thereto |
| WO2011131748A2 (en) | 2010-04-21 | 2011-10-27 | Probiodrug Ag | Novel 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 |
| WO2012035549A2 (en) * | 2010-09-13 | 2012-03-22 | Panacea Biotec Ltd | An improved process for the synthesis of beta amino acid derivatives |
| PH12013500547A1 (en) | 2010-09-22 | 2013-06-10 | Arena Pharm Inc | Modulators of the gpr119 receptor and the treatment of disorders related thereto |
| 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 |
| US20140066369A1 (en) | 2011-04-19 | 2014-03-06 | 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 |
| US20140038889A1 (en) | 2011-04-22 | 2014-02-06 | 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 |
| CA2838738A1 (en) | 2011-06-29 | 2013-01-03 | Merck Sharp & Dohme Corp. | Novel crystalline forms of a dipeptidyl peptidase-iv inhibitor |
| EP2729468A4 (en) | 2011-07-05 | 2015-03-18 | Merck Sharp & Dohme | Tricyclic heterocycles useful as dipeptidyl peptidase-iv inhibitors |
| EA024688B1 (ru) | 2011-07-27 | 2016-10-31 | ФАРМА ДжРС, Д.О.О. | Способ получения ситаглиптина и его фармацевтически приемлемых солей |
| 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 |
| WO2013122920A1 (en) | 2012-02-17 | 2013-08-22 | Merck Sharp & Dohme Corp. | Dipeptidyl peptidase-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 |
| US9156848B2 (en) | 2012-07-23 | 2015-10-13 | Merck Sharp & Dohme Corp. | Treating diabetes with dipeptidyl peptidase-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 |
| WO2014127745A1 (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 |
| 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 |
| US9862725B2 (en) | 2014-07-21 | 2018-01-09 | Merck Sharp & Dohme Corp. | Process for preparing chiral dipeptidyl peptidase-IV inhibitors |
| GB201415598D0 (en) | 2014-09-03 | 2014-10-15 | Univ Birmingham | Elavated Itercranial Pressure Treatment |
| EA201791982A1 (ru) | 2015-03-09 | 2020-02-17 | Интекрин Терапьютикс, Инк. | Способы лечения неалкогольной жировой болезни печени и/или липодистрофии |
| 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 |
| TWI791515B (zh) | 2017-04-24 | 2023-02-11 | 瑞士商諾華公司 | 治療療法 |
| ES2812698T3 (es) | 2017-09-29 | 2021-03-18 | Probiodrug Ag | Inhibidores de glutaminil ciclasa |
| WO2024015889A2 (en) * | 2022-07-14 | 2024-01-18 | The Scripps Research Institute | Small molecule regulators of alveolar type 2 cell proliferation for the treatment of pulmonary diseases |
| 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 |
| DE19616486C5 (de) * | 1996-04-25 | 2016-06-30 | Royalty Pharma Collection Trust | 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 |
| WO2002010140A2 (en) * | 2000-08-01 | 2002-02-07 | Societe De Conseils De Recherches Et D'applications Scientifiques (S.C.R.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 |
| ATE373660T1 (de) * | 2002-03-25 | 2007-10-15 | Merck & Co Inc | Heterocyclische beta-aminoverbindungen als inhibitoren der dipeptidylpeptidase zur behandlung bzw. prävention von diabetes |
| WO2004058266A1 (en) * | 2002-12-20 | 2004-07-15 | Merck & Co., Inc. | 3-amino-4-phenylbutanoic acid derivatives as dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes |
| EP1635832A2 (en) * | 2003-06-06 | 2006-03-22 | Merck & Co., Inc. | 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 |
| CA2536251C (en) * | 2003-09-02 | 2009-08-04 | Merck & Co., Inc. | Novel crystalline forms of a phosphoric acid salt of a dipeptidyl peptidase-iv inhibitor |
| 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 WO PCT/US2003/040114 patent/WO2004058266A1/en not_active Ceased
- 2003-12-16 CA CA002508947A patent/CA2508947A1/en not_active Abandoned
- 2003-12-16 AU AU2003297219A patent/AU2003297219A1/en not_active Abandoned
- 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 EP EP03814066A patent/EP1583534A4/en not_active Withdrawn
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| JP2006513265A5 (https=) | ||
| JP2004536115A5 (https=) | ||
| RU2436780C2 (ru) | Производные 5-фенилтиазола и их применение в качестве ингибиторов рi3 киназы | |
| JP2007507551A5 (https=) | ||
| RU2407740C2 (ru) | Гетеробициклические сульфонамидные производные для лечения диабета | |
| PE20040936A1 (es) | Derivados de triazol como inhibidores de 11-beta-hidroxiesteroide deshidrogenasa 1 | |
| PE20241625A1 (es) | Combinaciones farmaceuticas de inhibidores de sos1 para tratar o prevenir cancer | |
| RU2008138649A (ru) | Применение а1-агонистов аденозина и/или двойных а1/а2в-агонистов аденозина для получения лекарственных средств для лечения заболеваний | |
| JP2008513514A5 (https=) | ||
| JP2004528334A5 (https=) | ||
| RU2010110640A (ru) | Соединения и композиции 5-(4-(галогеналкокси)фенил)пиримидин-2-амина в качестве ингибиторов киназ | |
| CN1152870A (zh) | 杂环化合物作为多巴胺d3配位体的用途 | |
| RU2015150946A (ru) | Новые соединения для селективных ингибиторов гистондеацетилазы и фармацевтическая композиция, включающая такие соединения | |
| CA2522435A1 (en) | Inhibitors of akt activity | |
| CA2502269A1 (en) | Beta-amino heterocyclic dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes | |
| RU2009110442A (ru) | Конденсированные производные имидазола для лечения нарушений, опосредованных альдостеронсинтазой, и/или 11-бета-гидроксилазой, и/или ароматазой | |
| JP2011502958A5 (https=) | ||
| RU2009128966A (ru) | Новые производные аминопиримидина в качестве ингибиторов plr1 | |
| CA2511301A1 (en) | Acylsufonamide compounds as inhibitors of rna-dependent rna viral polymerase | |
| JP2010530431A5 (https=) | ||
| JP2006510630A5 (https=) | ||
| CA2375008A1 (en) | Phenoxypropylamine compounds | |
| BR122017003188A2 (pt) | composto 1-{2-[4-(2-amino-5-cloro-3-piridinil)fenóxi]-5-pirimidinil}-3-[2-(metilsulfonil)-5-(trifluorometil)fenil]ureia, sal deste, composição farmacêutica compreendendo-os e uso destes para o tratamento de câncer | |
| RU2000100935A (ru) | Производные ароил-пиперазина, их получение и их использование в качестве антагонистов тахикинина | |
| JP2005507918A5 (https=) |