JP2015503582A5 - - Google Patents
Download PDFInfo
- Publication number
- JP2015503582A5 JP2015503582A5 JP2014551231A JP2014551231A JP2015503582A5 JP 2015503582 A5 JP2015503582 A5 JP 2015503582A5 JP 2014551231 A JP2014551231 A JP 2014551231A JP 2014551231 A JP2014551231 A JP 2014551231A JP 2015503582 A5 JP2015503582 A5 JP 2015503582A5
- Authority
- JP
- Japan
- Prior art keywords
- composition
- biguanide compound
- metformin
- optionally substituted
- alkyl
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Withdrawn
Links
- 239000000203 mixture Substances 0.000 claims description 112
- 229940123208 Biguanide Drugs 0.000 claims description 46
- -1 biguanide compound Chemical class 0.000 claims description 46
- XZWYZXLIPXDOLR-UHFFFAOYSA-N metformin Chemical compound CN(C)C(=N)NC(N)=N XZWYZXLIPXDOLR-UHFFFAOYSA-N 0.000 claims description 36
- 229910052757 nitrogen Inorganic materials 0.000 claims description 28
- 125000000217 alkyl group Chemical group 0.000 claims description 22
- 229960003105 metformin Drugs 0.000 claims description 22
- 125000005119 alkyl cycloalkyl group Chemical group 0.000 claims description 18
- 125000004433 nitrogen atom Chemical group N* 0.000 claims description 18
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 17
- 238000000034 method Methods 0.000 claims description 17
- OETHQSJEHLVLGH-UHFFFAOYSA-N metformin hydrochloride Chemical compound Cl.CN(C)C(=N)N=C(N)N OETHQSJEHLVLGH-UHFFFAOYSA-N 0.000 claims description 16
- 229960004329 metformin hydrochloride Drugs 0.000 claims description 14
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims description 12
- 239000012729 immediate-release (IR) formulation Substances 0.000 claims description 11
- 125000003226 pyrazolyl group Chemical group 0.000 claims description 11
- 125000000168 pyrrolyl group Chemical group 0.000 claims description 11
- 125000005213 alkyl heteroaryl group Chemical group 0.000 claims description 9
- 125000001072 heteroaryl group Chemical group 0.000 claims description 9
- 150000003839 salts Chemical class 0.000 claims description 9
- 230000009885 systemic effect Effects 0.000 claims description 9
- 239000000883 anti-obesity agent Substances 0.000 claims description 8
- 229940125710 antiobesity agent Drugs 0.000 claims description 8
- 125000004426 substituted alkynyl group Chemical group 0.000 claims description 8
- 125000002877 alkyl aryl group Chemical group 0.000 claims description 7
- 238000009472 formulation Methods 0.000 claims description 7
- 125000005017 substituted alkenyl group Chemical group 0.000 claims description 7
- 125000000547 substituted alkyl group Chemical group 0.000 claims description 7
- 125000003107 substituted aryl group Chemical group 0.000 claims description 7
- 239000003112 inhibitor Substances 0.000 claims description 6
- 230000036470 plasma concentration Effects 0.000 claims description 6
- NOWKCMXCCJGMRR-UHFFFAOYSA-N Aziridine Chemical compound C1CN1 NOWKCMXCCJGMRR-UHFFFAOYSA-N 0.000 claims description 5
- 108010067722 Dipeptidyl Peptidase 4 Proteins 0.000 claims description 5
- 102100025012 Dipeptidyl peptidase 4 Human genes 0.000 claims description 5
- 125000002252 acyl group Chemical group 0.000 claims description 5
- 150000002148 esters Chemical class 0.000 claims description 5
- 125000002883 imidazolyl group Chemical group 0.000 claims description 5
- 125000003387 indolinyl group Chemical group N1(CCC2=CC=CC=C12)* 0.000 claims description 5
- 125000001041 indolyl group Chemical group 0.000 claims description 5
- 125000004193 piperazinyl group Chemical group 0.000 claims description 5
- 125000005936 piperidyl group Chemical group 0.000 claims description 5
- 125000000719 pyrrolidinyl group Chemical group 0.000 claims description 5
- 150000007970 thio esters Chemical class 0.000 claims description 5
- 229940125708 antidiabetic agent Drugs 0.000 claims description 4
- 239000003472 antidiabetic agent Substances 0.000 claims description 4
- 206010012601 diabetes mellitus Diseases 0.000 claims description 3
- 239000008280 blood Substances 0.000 claims description 2
- 210000004369 blood Anatomy 0.000 claims description 2
- 229940093617 glumetza Drugs 0.000 claims description 2
- 230000003111 delayed effect Effects 0.000 claims 6
- DHHVAGZRUROJKS-UHFFFAOYSA-N phentermine Chemical group CC(C)(N)CC1=CC=CC=C1 DHHVAGZRUROJKS-UHFFFAOYSA-N 0.000 claims 6
- 229960003562 phentermine Drugs 0.000 claims 3
- SWLAMJPTOQZTAE-UHFFFAOYSA-N 4-[2-[(5-chloro-2-methoxybenzoyl)amino]ethyl]benzoic acid Chemical class COC1=CC=C(Cl)C=C1C(=O)NCCC1=CC=C(C(O)=O)C=C1 SWLAMJPTOQZTAE-UHFFFAOYSA-N 0.000 claims 1
- 229940077274 Alpha glucosidase inhibitor Drugs 0.000 claims 1
- WQZGKKKJIJFFOK-GASJEMHNSA-N Glucose Natural products OC[C@H]1OC(O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-GASJEMHNSA-N 0.000 claims 1
- 102000000070 Sodium-Glucose Transport Proteins Human genes 0.000 claims 1
- 108010080361 Sodium-Glucose Transport Proteins Proteins 0.000 claims 1
- 229940100389 Sulfonylurea Drugs 0.000 claims 1
- 229940123464 Thiazolidinedione Drugs 0.000 claims 1
- KJADKKWYZYXHBB-XBWDGYHZSA-N Topiramic acid Chemical compound C1O[C@@]2(COS(N)(=O)=O)OC(C)(C)O[C@H]2[C@@H]2OC(C)(C)O[C@@H]21 KJADKKWYZYXHBB-XBWDGYHZSA-N 0.000 claims 1
- 239000003888 alpha glucosidase inhibitor Substances 0.000 claims 1
- 229960004111 buformin Drugs 0.000 claims 1
- XSEUMFJMFFMCIU-UHFFFAOYSA-N buformin Chemical compound CCCC\N=C(/N)N=C(N)N XSEUMFJMFFMCIU-UHFFFAOYSA-N 0.000 claims 1
- 229940047123 bupropion and naltrexone Drugs 0.000 claims 1
- 239000008103 glucose Substances 0.000 claims 1
- 208000018914 glucose metabolism disease Diseases 0.000 claims 1
- MGXWVYUBJRZYPE-YUGYIWNOSA-N incretin Chemical class C([C@@H](C(=O)N[C@@H](CO)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](C)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CC(O)=O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CC=1NC=NC=1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(O)=O)C(=O)N[C@@H](CC=1C=CC=CC=1)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC=1C2=CC=CC=C2NC=1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(O)=O)C(=O)N[C@@H](CC=1C2=CC=CC=C2NC=1)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC=1NC=NC=1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](CCC(N)=O)C(O)=O)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=1C=CC(O)=CC=1)[C@@H](C)O)[C@@H](C)CC)C1=CC=C(O)C=C1 MGXWVYUBJRZYPE-YUGYIWNOSA-N 0.000 claims 1
- 239000000859 incretin Substances 0.000 claims 1
- 229950004994 meglitinide Drugs 0.000 claims 1
- 229960003243 phenformin Drugs 0.000 claims 1
- ICFJFFQQTFMIBG-UHFFFAOYSA-N phenformin Chemical compound NC(=N)NC(=N)NCCC1=CC=CC=C1 ICFJFFQQTFMIBG-UHFFFAOYSA-N 0.000 claims 1
- 229960005385 proguanil Drugs 0.000 claims 1
- SSOLNOMRVKKSON-UHFFFAOYSA-N proguanil Chemical compound CC(C)\N=C(/N)N=C(N)NC1=CC=C(Cl)C=C1 SSOLNOMRVKKSON-UHFFFAOYSA-N 0.000 claims 1
- 229940121377 sodium-glucose co-transporter inhibitor Drugs 0.000 claims 1
- 150000001467 thiazolidinediones Chemical class 0.000 claims 1
- 229960004394 topiramate Drugs 0.000 claims 1
- 229910052760 oxygen Inorganic materials 0.000 description 25
- 229910052717 sulfur Inorganic materials 0.000 description 25
- 150000001875 compounds Chemical class 0.000 description 19
- 239000002552 dosage form Substances 0.000 description 18
- 125000000623 heterocyclic group Chemical group 0.000 description 16
- 125000001624 naphthyl group Chemical group 0.000 description 16
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 description 16
- XUIMIQQOPSSXEZ-UHFFFAOYSA-N Silicon Chemical group [Si] XUIMIQQOPSSXEZ-UHFFFAOYSA-N 0.000 description 15
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical group [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 description 15
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical group [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 description 15
- 239000001301 oxygen Substances 0.000 description 15
- 229910052710 silicon Inorganic materials 0.000 description 15
- 239000010703 silicon Chemical group 0.000 description 15
- 239000011593 sulfur Chemical group 0.000 description 15
- 150000002391 heterocyclic compounds Chemical class 0.000 description 11
- XSQUKJJJFZCRTK-UHFFFAOYSA-N Urea Chemical compound NC(N)=O XSQUKJJJFZCRTK-UHFFFAOYSA-N 0.000 description 10
- 125000005842 heteroatom Chemical group 0.000 description 10
- XNCOSPRUTUOJCJ-UHFFFAOYSA-N Biguanide Chemical compound NC(N)=NC(N)=N XNCOSPRUTUOJCJ-UHFFFAOYSA-N 0.000 description 9
- 125000005037 alkyl phenyl group Chemical group 0.000 description 6
- 125000002720 diazolyl group Chemical group 0.000 description 6
- 125000002541 furyl group Chemical group 0.000 description 6
- 125000000842 isoxazolyl group Chemical group 0.000 description 6
- 239000003446 ligand Substances 0.000 description 6
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 description 6
- 125000002971 oxazolyl group Chemical group 0.000 description 6
- 125000004076 pyridyl group Chemical group 0.000 description 6
- 125000001544 thienyl group Chemical group 0.000 description 6
- 125000001425 triazolyl group Chemical group 0.000 description 6
- KXDHJXZQYSOELW-UHFFFAOYSA-M Carbamate Chemical compound NC([O-])=O KXDHJXZQYSOELW-UHFFFAOYSA-M 0.000 description 5
- 125000003342 alkenyl group Chemical group 0.000 description 5
- 125000000304 alkynyl group Chemical group 0.000 description 5
- 150000001408 amides Chemical class 0.000 description 5
- 239000004202 carbamide Substances 0.000 description 5
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 description 5
- 210000001035 gastrointestinal tract Anatomy 0.000 description 5
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 description 5
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 description 5
- 125000000335 thiazolyl group Chemical group 0.000 description 5
- 208000008589 Obesity Diseases 0.000 description 4
- MUBZPKHOEPUJKR-UHFFFAOYSA-N Oxalic acid Chemical compound OC(=O)C(O)=O MUBZPKHOEPUJKR-UHFFFAOYSA-N 0.000 description 4
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 4
- 238000013265 extended release Methods 0.000 description 4
- 208000008338 non-alcoholic fatty liver disease Diseases 0.000 description 4
- 235000020824 obesity Nutrition 0.000 description 4
- 239000000546 pharmaceutical excipient Substances 0.000 description 4
- 102000005962 receptors Human genes 0.000 description 4
- 108020003175 receptors Proteins 0.000 description 4
- VZCYOOQTPOCHFL-UHFFFAOYSA-N trans-butenedioic acid Natural products OC(=O)C=CC(O)=O VZCYOOQTPOCHFL-UHFFFAOYSA-N 0.000 description 4
- 208000019901 Anxiety disease Diseases 0.000 description 3
- VZCYOOQTPOCHFL-OWOJBTEDSA-N Fumaric acid Chemical compound OC(=O)\C=C\C(O)=O VZCYOOQTPOCHFL-OWOJBTEDSA-N 0.000 description 3
- CKLJMWTZIZZHCS-REOHCLBHSA-N L-aspartic acid Chemical compound OC(=O)[C@@H](N)CC(O)=O CKLJMWTZIZZHCS-REOHCLBHSA-N 0.000 description 3
- OFOBLEOULBTSOW-UHFFFAOYSA-N Malonic acid Chemical compound OC(=O)CC(O)=O OFOBLEOULBTSOW-UHFFFAOYSA-N 0.000 description 3
- KRKNYBCHXYNGOX-UHFFFAOYSA-N citric acid Chemical compound OC(=O)CC(O)(C(O)=O)CC(O)=O KRKNYBCHXYNGOX-UHFFFAOYSA-N 0.000 description 3
- 208000035475 disorder Diseases 0.000 description 3
- 201000009104 prediabetes syndrome Diseases 0.000 description 3
- 208000001072 type 2 diabetes mellitus Diseases 0.000 description 3
- FEWJPZIEWOKRBE-JCYAYHJZSA-N Dextrotartaric acid Chemical compound OC(=O)[C@H](O)[C@@H](O)C(O)=O FEWJPZIEWOKRBE-JCYAYHJZSA-N 0.000 description 2
- 208000032928 Dyslipidaemia Diseases 0.000 description 2
- 206010018429 Glucose tolerance impaired Diseases 0.000 description 2
- DHMQDGOQFOQNFH-UHFFFAOYSA-N Glycine Chemical compound NCC(O)=O DHMQDGOQFOQNFH-UHFFFAOYSA-N 0.000 description 2
- 208000022559 Inflammatory bowel disease Diseases 0.000 description 2
- WHUUTDBJXJRKMK-VKHMYHEASA-N L-glutamic acid Chemical compound OC(=O)[C@@H](N)CCC(O)=O WHUUTDBJXJRKMK-VKHMYHEASA-N 0.000 description 2
- 208000017170 Lipid metabolism disease Diseases 0.000 description 2
- 206010028289 Muscle atrophy Diseases 0.000 description 2
- 208000001280 Prediabetic State Diseases 0.000 description 2
- 239000002253 acid Substances 0.000 description 2
- 235000001014 amino acid Nutrition 0.000 description 2
- 229940024606 amino acid Drugs 0.000 description 2
- 150000001413 amino acids Chemical class 0.000 description 2
- 125000003118 aryl group Chemical group 0.000 description 2
- 235000003704 aspartic acid Nutrition 0.000 description 2
- OQFSQFPPLPISGP-UHFFFAOYSA-N beta-carboxyaspartic acid Natural products OC(=O)C(N)C(C(O)=O)C(O)=O OQFSQFPPLPISGP-UHFFFAOYSA-N 0.000 description 2
- 150000004283 biguanides Chemical class 0.000 description 2
- 230000030136 gastric emptying Effects 0.000 description 2
- 208000004104 gestational diabetes Diseases 0.000 description 2
- 230000037219 healthy weight Effects 0.000 description 2
- 201000001421 hyperglycemia Diseases 0.000 description 2
- 208000006575 hypertriglyceridemia Diseases 0.000 description 2
- 230000000968 intestinal effect Effects 0.000 description 2
- 208000002551 irritable bowel syndrome Diseases 0.000 description 2
- VZCYOOQTPOCHFL-UPHRSURJSA-N maleic acid Chemical compound OC(=O)\C=C/C(O)=O VZCYOOQTPOCHFL-UPHRSURJSA-N 0.000 description 2
- 206010053219 non-alcoholic steatohepatitis Diseases 0.000 description 2
- 201000010065 polycystic ovary syndrome Diseases 0.000 description 2
- 230000000291 postprandial effect Effects 0.000 description 2
- MTCFGRXMJLQNBG-REOHCLBHSA-N (2S)-2-Amino-3-hydroxypropansäure Chemical compound OC[C@H](N)C(O)=O MTCFGRXMJLQNBG-REOHCLBHSA-N 0.000 description 1
- HOMROMWVNDUGRI-RVZXSAGBSA-N (2s)-2-aminopentanedioic acid;(2s)-2,6-diaminohexanoic acid Chemical compound NCCCC[C@H](N)C(O)=O.OC(=O)[C@@H](N)CCC(O)=O HOMROMWVNDUGRI-RVZXSAGBSA-N 0.000 description 1
- HBAQYPYDRFILMT-UHFFFAOYSA-N 8-[3-(1-cyclopropylpyrazol-4-yl)-1H-pyrazolo[4,3-d]pyrimidin-5-yl]-3-methyl-3,8-diazabicyclo[3.2.1]octan-2-one Chemical class C1(CC1)N1N=CC(=C1)C1=NNC2=C1N=C(N=C2)N1C2C(N(CC1CC2)C)=O HBAQYPYDRFILMT-UHFFFAOYSA-N 0.000 description 1
- QTBSBXVTEAMEQO-UHFFFAOYSA-M Acetate Chemical compound CC([O-])=O QTBSBXVTEAMEQO-UHFFFAOYSA-M 0.000 description 1
- 239000004475 Arginine Substances 0.000 description 1
- DCXYFEDJOCDNAF-UHFFFAOYSA-N Asparagine Natural products OC(=O)C(N)CC(N)=O DCXYFEDJOCDNAF-UHFFFAOYSA-N 0.000 description 1
- BVKZGUZCCUSVTD-UHFFFAOYSA-M Bicarbonate Chemical compound OC([O-])=O BVKZGUZCCUSVTD-UHFFFAOYSA-M 0.000 description 1
- 102000017002 Bile acid receptors Human genes 0.000 description 1
- 108070000005 Bile acid receptors Proteins 0.000 description 1
- 208000020925 Bipolar disease Diseases 0.000 description 1
- 206010065687 Bone loss Diseases 0.000 description 1
- 208000032841 Bulimia Diseases 0.000 description 1
- 206010006550 Bulimia nervosa Diseases 0.000 description 1
- FERIUCNNQQJTOY-UHFFFAOYSA-M Butyrate Chemical compound CCCC([O-])=O FERIUCNNQQJTOY-UHFFFAOYSA-M 0.000 description 1
- FERIUCNNQQJTOY-UHFFFAOYSA-N Butyric acid Natural products CCCC(O)=O FERIUCNNQQJTOY-UHFFFAOYSA-N 0.000 description 1
- BVKZGUZCCUSVTD-UHFFFAOYSA-L Carbonate Chemical compound [O-]C([O-])=O BVKZGUZCCUSVTD-UHFFFAOYSA-L 0.000 description 1
- KRKNYBCHXYNGOX-UHFFFAOYSA-K Citrate Chemical compound [O-]C(=O)CC(O)(CC([O-])=O)C([O-])=O KRKNYBCHXYNGOX-UHFFFAOYSA-K 0.000 description 1
- 208000015943 Coeliac disease Diseases 0.000 description 1
- 206010009900 Colitis ulcerative Diseases 0.000 description 1
- 229940126062 Compound A Drugs 0.000 description 1
- 208000011231 Crohn disease Diseases 0.000 description 1
- 208000032131 Diabetic Neuropathies Diseases 0.000 description 1
- 208000008279 Dumping Syndrome Diseases 0.000 description 1
- 102100025101 GATA-type zinc finger protein 1 Human genes 0.000 description 1
- 101710198884 GATA-type zinc finger protein 1 Proteins 0.000 description 1
- DTHNMHAUYICORS-KTKZVXAJSA-N Glucagon-like peptide 1 Chemical compound C([C@@H](C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](C)C(=O)N[C@@H](CC=1C2=CC=CC=C2NC=1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCNC(N)=N)C(N)=O)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CCC(N)=O)NC(=O)CNC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC=1C=CC(O)=CC=1)NC(=O)[C@H](CO)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](CC=1C=CC=CC=1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](C)NC(=O)[C@@H](N)CC=1N=CNC=1)[C@@H](C)O)[C@@H](C)O)C(C)C)C1=CC=CC=C1 DTHNMHAUYICORS-KTKZVXAJSA-N 0.000 description 1
- 208000002705 Glucose Intolerance Diseases 0.000 description 1
- WHUUTDBJXJRKMK-UHFFFAOYSA-N Glutamic acid Natural products OC(=O)C(N)CCC(O)=O WHUUTDBJXJRKMK-UHFFFAOYSA-N 0.000 description 1
- 239000004471 Glycine Substances 0.000 description 1
- NLDMNSXOCDLTTB-UHFFFAOYSA-N Heterophylliin A Natural products O1C2COC(=O)C3=CC(O)=C(O)C(O)=C3C3=C(O)C(O)=C(O)C=C3C(=O)OC2C(OC(=O)C=2C=C(O)C(O)=C(O)C=2)C(O)C1OC(=O)C1=CC(O)=C(O)C(O)=C1 NLDMNSXOCDLTTB-UHFFFAOYSA-N 0.000 description 1
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 description 1
- CPELXLSAUQHCOX-UHFFFAOYSA-N Hydrogen bromide Chemical compound Br CPELXLSAUQHCOX-UHFFFAOYSA-N 0.000 description 1
- 208000031226 Hyperlipidaemia Diseases 0.000 description 1
- 206010020710 Hyperphagia Diseases 0.000 description 1
- 206010061598 Immunodeficiency Diseases 0.000 description 1
- 208000029462 Immunodeficiency disease Diseases 0.000 description 1
- 206010022489 Insulin Resistance Diseases 0.000 description 1
- XUJNEKJLAYXESH-REOHCLBHSA-N L-Cysteine Chemical compound SC[C@H](N)C(O)=O XUJNEKJLAYXESH-REOHCLBHSA-N 0.000 description 1
- ONIBWKKTOPOVIA-BYPYZUCNSA-N L-Proline Chemical compound OC(=O)[C@@H]1CCCN1 ONIBWKKTOPOVIA-BYPYZUCNSA-N 0.000 description 1
- QNAYBMKLOCPYGJ-REOHCLBHSA-N L-alanine Chemical compound C[C@H](N)C(O)=O QNAYBMKLOCPYGJ-REOHCLBHSA-N 0.000 description 1
- ODKSFYDXXFIFQN-BYPYZUCNSA-P L-argininium(2+) Chemical compound NC(=[NH2+])NCCC[C@H]([NH3+])C(O)=O ODKSFYDXXFIFQN-BYPYZUCNSA-P 0.000 description 1
- DCXYFEDJOCDNAF-REOHCLBHSA-N L-asparagine Chemical compound OC(=O)[C@@H](N)CC(N)=O DCXYFEDJOCDNAF-REOHCLBHSA-N 0.000 description 1
- LEVWYRKDKASIDU-IMJSIDKUSA-N L-cystine Chemical compound [O-]C(=O)[C@@H]([NH3+])CSSC[C@H]([NH3+])C([O-])=O LEVWYRKDKASIDU-IMJSIDKUSA-N 0.000 description 1
- ZDXPYRJPNDTMRX-VKHMYHEASA-N L-glutamine Chemical compound OC(=O)[C@@H](N)CCC(N)=O ZDXPYRJPNDTMRX-VKHMYHEASA-N 0.000 description 1
- HNDVDQJCIGZPNO-YFKPBYRVSA-N L-histidine Chemical compound OC(=O)[C@@H](N)CC1=CN=CN1 HNDVDQJCIGZPNO-YFKPBYRVSA-N 0.000 description 1
- AGPKZVBTJJNPAG-WHFBIAKZSA-N L-isoleucine Chemical compound CC[C@H](C)[C@H](N)C(O)=O AGPKZVBTJJNPAG-WHFBIAKZSA-N 0.000 description 1
- ROHFNLRQFUQHCH-YFKPBYRVSA-N L-leucine Chemical compound CC(C)C[C@H](N)C(O)=O ROHFNLRQFUQHCH-YFKPBYRVSA-N 0.000 description 1
- FFEARJCKVFRZRR-BYPYZUCNSA-N L-methionine Chemical compound CSCC[C@H](N)C(O)=O FFEARJCKVFRZRR-BYPYZUCNSA-N 0.000 description 1
- COLNVLDHVKWLRT-QMMMGPOBSA-N L-phenylalanine Chemical compound OC(=O)[C@@H](N)CC1=CC=CC=C1 COLNVLDHVKWLRT-QMMMGPOBSA-N 0.000 description 1
- AYFVYJQAPQTCCC-GBXIJSLDSA-N L-threonine Chemical compound C[C@@H](O)[C@H](N)C(O)=O AYFVYJQAPQTCCC-GBXIJSLDSA-N 0.000 description 1
- QIVBCDIJIAJPQS-VIFPVBQESA-N L-tryptophane Chemical compound C1=CC=C2C(C[C@H](N)C(O)=O)=CNC2=C1 QIVBCDIJIAJPQS-VIFPVBQESA-N 0.000 description 1
- OUYCCCASQSFEME-QMMMGPOBSA-N L-tyrosine Chemical compound OC(=O)[C@@H](N)CC1=CC=C(O)C=C1 OUYCCCASQSFEME-QMMMGPOBSA-N 0.000 description 1
- ROHFNLRQFUQHCH-UHFFFAOYSA-N Leucine Natural products CC(C)CC(N)C(O)=O ROHFNLRQFUQHCH-UHFFFAOYSA-N 0.000 description 1
- OFOBLEOULBTSOW-UHFFFAOYSA-L Malonate Chemical compound [O-]C(=O)CC([O-])=O OFOBLEOULBTSOW-UHFFFAOYSA-L 0.000 description 1
- 208000001145 Metabolic Syndrome Diseases 0.000 description 1
- 208000029725 Metabolic bone disease Diseases 0.000 description 1
- 208000019022 Mood disease Diseases 0.000 description 1
- 208000021384 Obsessive-Compulsive disease Diseases 0.000 description 1
- 206010049088 Osteopenia Diseases 0.000 description 1
- 208000001132 Osteoporosis Diseases 0.000 description 1
- 206010033307 Overweight Diseases 0.000 description 1
- 229910019142 PO4 Inorganic materials 0.000 description 1
- 208000032395 Post gastric surgery syndrome Diseases 0.000 description 1
- ONIBWKKTOPOVIA-UHFFFAOYSA-N Proline Natural products OC(=O)C1CCCN1 ONIBWKKTOPOVIA-UHFFFAOYSA-N 0.000 description 1
- XBDQKXXYIPTUBI-UHFFFAOYSA-M Propionate Chemical compound CCC([O-])=O XBDQKXXYIPTUBI-UHFFFAOYSA-M 0.000 description 1
- MTCFGRXMJLQNBG-UHFFFAOYSA-N Serine Natural products OCC(N)C(O)=O MTCFGRXMJLQNBG-UHFFFAOYSA-N 0.000 description 1
- 206010049416 Short-bowel syndrome Diseases 0.000 description 1
- 206010041250 Social phobia Diseases 0.000 description 1
- QAOWNCQODCNURD-UHFFFAOYSA-L Sulfate Chemical compound [O-]S([O-])(=O)=O QAOWNCQODCNURD-UHFFFAOYSA-L 0.000 description 1
- LSNNMFCWUKXFEE-UHFFFAOYSA-N Sulfurous acid Chemical compound OS(O)=O LSNNMFCWUKXFEE-UHFFFAOYSA-N 0.000 description 1
- FEWJPZIEWOKRBE-UHFFFAOYSA-N Tartaric acid Natural products [H+].[H+].[O-]C(=O)C(O)C(O)C([O-])=O FEWJPZIEWOKRBE-UHFFFAOYSA-N 0.000 description 1
- AYFVYJQAPQTCCC-UHFFFAOYSA-N Threonine Natural products CC(O)C(N)C(O)=O AYFVYJQAPQTCCC-UHFFFAOYSA-N 0.000 description 1
- 239000004473 Threonine Substances 0.000 description 1
- QIVBCDIJIAJPQS-UHFFFAOYSA-N Tryptophan Natural products C1=CC=C2C(CC(N)C(O)=O)=CNC2=C1 QIVBCDIJIAJPQS-UHFFFAOYSA-N 0.000 description 1
- 206010067584 Type 1 diabetes mellitus Diseases 0.000 description 1
- 201000006704 Ulcerative Colitis Diseases 0.000 description 1
- 201000000690 abdominal obesity-metabolic syndrome Diseases 0.000 description 1
- 235000004279 alanine Nutrition 0.000 description 1
- 208000022531 anorexia Diseases 0.000 description 1
- 230000003178 anti-diabetic effect Effects 0.000 description 1
- 230000003579 anti-obesity Effects 0.000 description 1
- 230000036506 anxiety Effects 0.000 description 1
- ODKSFYDXXFIFQN-UHFFFAOYSA-N arginine Natural products OC(=O)C(N)CCCNC(N)=N ODKSFYDXXFIFQN-UHFFFAOYSA-N 0.000 description 1
- 235000009697 arginine Nutrition 0.000 description 1
- 235000009582 asparagine Nutrition 0.000 description 1
- 229960001230 asparagine Drugs 0.000 description 1
- 229940009098 aspartate Drugs 0.000 description 1
- 238000007681 bariatric surgery Methods 0.000 description 1
- 239000002775 capsule Substances 0.000 description 1
- 230000000723 chemosensory effect Effects 0.000 description 1
- 235000009508 confectionery Nutrition 0.000 description 1
- XUJNEKJLAYXESH-UHFFFAOYSA-N cysteine Natural products SCC(N)C(O)=O XUJNEKJLAYXESH-UHFFFAOYSA-N 0.000 description 1
- 235000018417 cysteine Nutrition 0.000 description 1
- 229960003067 cystine Drugs 0.000 description 1
- 206010061428 decreased appetite Diseases 0.000 description 1
- 238000004090 dissolution Methods 0.000 description 1
- 229940079593 drug Drugs 0.000 description 1
- 239000003814 drug Substances 0.000 description 1
- 208000024732 dysthymic disease Diseases 0.000 description 1
- 235000005686 eating Nutrition 0.000 description 1
- 230000019439 energy homeostasis Effects 0.000 description 1
- 239000002702 enteric coating Substances 0.000 description 1
- 238000009505 enteric coating Methods 0.000 description 1
- 235000013305 food Nutrition 0.000 description 1
- 239000001530 fumaric acid Substances 0.000 description 1
- 235000011087 fumaric acid Nutrition 0.000 description 1
- 230000004153 glucose metabolism Effects 0.000 description 1
- 229930195712 glutamate Natural products 0.000 description 1
- 235000013922 glutamic acid Nutrition 0.000 description 1
- 239000004220 glutamic acid Substances 0.000 description 1
- ZDXPYRJPNDTMRX-UHFFFAOYSA-N glutamine Natural products OC(=O)C(N)CCC(N)=O ZDXPYRJPNDTMRX-UHFFFAOYSA-N 0.000 description 1
- 108091005708 gustatory receptors Proteins 0.000 description 1
- HNDVDQJCIGZPNO-UHFFFAOYSA-N histidine Natural products OC(=O)C(N)CC1=CN=CN1 HNDVDQJCIGZPNO-UHFFFAOYSA-N 0.000 description 1
- QAOWNCQODCNURD-UHFFFAOYSA-M hydrogensulfate Chemical compound OS([O-])(=O)=O QAOWNCQODCNURD-UHFFFAOYSA-M 0.000 description 1
- 230000007813 immunodeficiency Effects 0.000 description 1
- 230000001939 inductive effect Effects 0.000 description 1
- 239000004615 ingredient Substances 0.000 description 1
- 210000000936 intestine Anatomy 0.000 description 1
- 229960000310 isoleucine Drugs 0.000 description 1
- AGPKZVBTJJNPAG-UHFFFAOYSA-N isoleucine Natural products CCC(C)C(N)C(O)=O AGPKZVBTJJNPAG-UHFFFAOYSA-N 0.000 description 1
- 239000011976 maleic acid Substances 0.000 description 1
- 229930182817 methionine Natural products 0.000 description 1
- 230000036651 mood Effects 0.000 description 1
- 201000000585 muscular atrophy Diseases 0.000 description 1
- 235000020830 overeating Nutrition 0.000 description 1
- 235000006408 oxalic acid Nutrition 0.000 description 1
- 208000019906 panic disease Diseases 0.000 description 1
- 208000033808 peripheral neuropathy Diseases 0.000 description 1
- COLNVLDHVKWLRT-UHFFFAOYSA-N phenylalanine Natural products OC(=O)C(N)CC1=CC=CC=C1 COLNVLDHVKWLRT-UHFFFAOYSA-N 0.000 description 1
- NBIIXXVUZAFLBC-UHFFFAOYSA-K phosphate Chemical compound [O-]P([O-])([O-])=O NBIIXXVUZAFLBC-UHFFFAOYSA-K 0.000 description 1
- 239000010452 phosphate Substances 0.000 description 1
- ACVYVLVWPXVTIT-UHFFFAOYSA-M phosphinate Chemical compound [O-][PH2]=O ACVYVLVWPXVTIT-UHFFFAOYSA-M 0.000 description 1
- 208000028173 post-traumatic stress disease Diseases 0.000 description 1
- 235000019614 sour taste Nutrition 0.000 description 1
- 239000011975 tartaric acid Substances 0.000 description 1
- 235000002906 tartaric acid Nutrition 0.000 description 1
- 229940095064 tartrate Drugs 0.000 description 1
- LMBFAGIMSUYTBN-MPZNNTNKSA-N teixobactin Chemical compound C([C@H](C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CO)C(=O)N[C@H](CCC(N)=O)C(=O)N[C@H]([C@@H](C)CC)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CO)C(=O)N[C@H]1C(N[C@@H](C)C(=O)N[C@@H](C[C@@H]2NC(=N)NC2)C(=O)N[C@H](C(=O)O[C@H]1C)[C@@H](C)CC)=O)NC)C1=CC=CC=C1 LMBFAGIMSUYTBN-MPZNNTNKSA-N 0.000 description 1
- OUYCCCASQSFEME-UHFFFAOYSA-N tyrosine Natural products OC(=O)C(N)CC1=CC=C(O)C=C1 OUYCCCASQSFEME-UHFFFAOYSA-N 0.000 description 1
- 235000019583 umami taste Nutrition 0.000 description 1
- 230000004580 weight loss Effects 0.000 description 1
Applications Claiming Priority (7)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US13/345,135 | 2012-01-06 | ||
| US13/345,135 US20120177730A1 (en) | 2011-01-07 | 2012-01-06 | Chemosensory Receptor Ligand-Based Therapies |
| USPCT/US2012/020548 | 2012-01-06 | ||
| PCT/US2012/020548 WO2012094636A2 (en) | 2011-01-07 | 2012-01-06 | Chemosensory receptor ligand-based therapies |
| US201261649171P | 2012-05-18 | 2012-05-18 | |
| US61/649,171 | 2012-05-18 | ||
| PCT/US2012/046335 WO2013103384A1 (en) | 2012-01-06 | 2012-07-11 | Biguanide compositions and methods of treating metabolic disorders |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2017079805A Division JP2017141289A (ja) | 2012-01-06 | 2017-04-13 | ビグアナイド組成物および代謝障害を治療する方法 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2015503582A JP2015503582A (ja) | 2015-02-02 |
| JP2015503582A5 true JP2015503582A5 (https=) | 2015-09-03 |
Family
ID=48745353
Family Applications (4)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2014551231A Withdrawn JP2015503582A (ja) | 2012-01-06 | 2012-07-11 | ビグアナイド組成物および代謝障害を治療する方法 |
| JP2017079805A Pending JP2017141289A (ja) | 2012-01-06 | 2017-04-13 | ビグアナイド組成物および代謝障害を治療する方法 |
| JP2019165827A Active JP7335056B2 (ja) | 2012-01-06 | 2019-09-12 | ビグアナイド組成物および代謝障害を治療する方法 |
| JP2021120385A Pending JP2021169522A (ja) | 2012-01-06 | 2021-07-21 | ビグアナイド組成物および代謝障害を治療する方法 |
Family Applications After (3)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2017079805A Pending JP2017141289A (ja) | 2012-01-06 | 2017-04-13 | ビグアナイド組成物および代謝障害を治療する方法 |
| JP2019165827A Active JP7335056B2 (ja) | 2012-01-06 | 2019-09-12 | ビグアナイド組成物および代謝障害を治療する方法 |
| JP2021120385A Pending JP2021169522A (ja) | 2012-01-06 | 2021-07-21 | ビグアナイド組成物および代謝障害を治療する方法 |
Country Status (15)
| Country | Link |
|---|---|
| US (2) | US10154972B2 (https=) |
| EP (1) | EP2800561B1 (https=) |
| JP (4) | JP2015503582A (https=) |
| KR (4) | KR20200137035A (https=) |
| CN (2) | CN104254325A (https=) |
| AU (2) | AU2012363873B2 (https=) |
| BR (1) | BR112014016808B1 (https=) |
| CA (1) | CA2862533C (https=) |
| EA (1) | EA201491335A1 (https=) |
| ES (1) | ES2832773T3 (https=) |
| IL (1) | IL233506B (https=) |
| MX (2) | MX2014008190A (https=) |
| SG (2) | SG11201403839SA (https=) |
| WO (1) | WO2013103384A1 (https=) |
| ZA (1) | ZA201405046B (https=) |
Families Citing this family (29)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US11759441B2 (en) | 2011-01-07 | 2023-09-19 | Anji Pharmaceuticals Inc. | Biguanide compositions and methods of treating metabolic disorders |
| US9211263B2 (en) | 2012-01-06 | 2015-12-15 | Elcelyx Therapeutics, Inc. | Compositions and methods of treating metabolic disorders |
| US9480663B2 (en) | 2011-01-07 | 2016-11-01 | Elcelyx Therapeutics, Inc. | Biguanide compositions and methods of treating metabolic disorders |
| HUE051738T2 (hu) | 2011-01-07 | 2021-03-29 | Anji Pharma Us Llc | Kemoszenzoros receptorligandum-alapú terápiák |
| US11974971B2 (en) | 2011-01-07 | 2024-05-07 | Anji Pharmaceuticals Inc. | Compositions and methods for treating metabolic disorders |
| US8796338B2 (en) | 2011-01-07 | 2014-08-05 | Elcelyx Therapeutics, Inc | Biguanide compositions and methods of treating metabolic disorders |
| US9572784B2 (en) | 2011-01-07 | 2017-02-21 | Elcelyx Therapeutics, Inc. | Compositions comprising statins, biguanides and further agents for reducing cardiometabolic risk |
| EA033067B1 (ru) | 2012-01-06 | 2019-08-30 | Элселикс Терапьютикс, Инк. | Способ лечения метаболических расстройств у пациента, имеющего противопоказание к назначению бигуанидного соединения |
| KR20200137035A (ko) | 2012-01-06 | 2020-12-08 | 앤지 파마 유에스 엘엘씨 | 바이구아나이드 조성물 및 대사 장애를 치료하는 방법 |
| US20140010783A1 (en) * | 2012-07-06 | 2014-01-09 | Hoffmann-La Roche Inc. | Antiviral compounds |
| KR101994145B1 (ko) * | 2013-01-28 | 2019-07-01 | 한올바이오파마주식회사 | Ν１-고리아민-ν５-치환된 바이구아나이드 유도체를 유효성분으로 함유하는 시차증후군의 예방 또는 치료용 약학 조성물 |
| MX2015010892A (es) * | 2013-03-05 | 2015-12-03 | Hoffmann La Roche | Compuestos antivirales. |
| WO2014135483A1 (en) * | 2013-03-05 | 2014-09-12 | F. Hoffmann-La Roche Ag | Antiviral compounds |
| KR102088001B1 (ko) * | 2013-05-23 | 2020-03-12 | 이뮤노메트테라퓨틱스 인코포레이티드 | N1-고리아민-n5-치환된 바이구아나이드 유도체를 유효성분으로 함유하는 섬유화 예방 또는 치료용 약학 조성물 |
| CN106458868A (zh) * | 2014-04-17 | 2017-02-22 | 伊谬诺米特医疗有限公司 | 胍化合物及其用途 |
| CN107205968B (zh) * | 2014-08-14 | 2021-08-20 | 威斯康星州医药大学股份有限公司 | 修饰的线粒体-二甲双胍化合物及其合成和使用方法 |
| US10426745B2 (en) | 2015-03-06 | 2019-10-01 | The University Of North Carolina At Chapel Hill | Polymeric metformin and its use as a therapeutic agent and as a delivery vehicle |
| CZ307146B6 (cs) * | 2015-03-31 | 2018-02-07 | Kkcg Se | Trifenylfosfoniové analogy biguanidu, způsob jejich přípravy a jejich použití jako léčiva |
| WO2018058109A1 (en) * | 2016-09-26 | 2018-03-29 | Nusirt Sciences, Inc. | Compositions and methods for treating metabolic disorders |
| WO2018132768A1 (en) * | 2017-01-13 | 2018-07-19 | Sanna Pietro P | Methods and compositions for treating hpa hyperactivity |
| JP7527275B2 (ja) * | 2018-09-28 | 2024-08-02 | ソシエテ・デ・プロデュイ・ネスレ・エス・アー | メトホルミンの作用を増強する化合物 |
| CN114340615A (zh) | 2019-08-12 | 2022-04-12 | 麻省理工学院 | 用于施用治疗剂的制品和方法 |
| JP7093473B2 (ja) * | 2019-12-13 | 2022-06-29 | 住友ファーマ株式会社 | 製造性及び溶出性に優れた小型錠剤 |
| US12029718B2 (en) | 2021-11-09 | 2024-07-09 | Cct Sciences, Llc | Process for production of essentially pure delta-9-tetrahydrocannabinol |
| US20250042925A1 (en) * | 2021-12-02 | 2025-02-06 | The Medical College Of Wisconsin, Inc. | Improved Compositions and Methods for Targeting Mitochondria in Cancer Cells |
| CN114681438B (zh) * | 2022-05-17 | 2024-03-19 | 中国医学科学院基础医学研究所 | 二甲双胍及其它含胍化合物在逆转Gal-10结晶趋势并缓解相关疾病中应用 |
| CN121846068A (zh) | 2023-08-22 | 2026-04-14 | 雅研(天津)生物医药科技中心(有限合伙) | 盐酸二甲双胍肠溶制剂 |
| CN119499203A (zh) | 2023-08-22 | 2025-02-25 | 雅研(天津)生物医药科技中心(有限合伙) | 一种盐酸二甲双胍肠溶片 |
| US12303604B1 (en) | 2024-10-16 | 2025-05-20 | Currax Pharmaceuticals Llc | Pharmaceutical formulations comprising naltrexone and/or bupropion |
Family Cites Families (203)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3536809A (en) | 1969-02-17 | 1970-10-27 | Alza Corp | Medication method |
| US3598123A (en) | 1969-04-01 | 1971-08-10 | Alza Corp | Bandage for administering drugs |
| US3845770A (en) | 1972-06-05 | 1974-11-05 | Alza Corp | Osmatic dispensing device for releasing beneficial agent |
| US3916899A (en) | 1973-04-25 | 1975-11-04 | Alza Corp | Osmotic dispensing device with maximum and minimum sizes for the passageway |
| JPS58403B2 (ja) | 1975-07-24 | 1983-01-06 | 武田薬品工業株式会社 | Ｌ− アスコルビンサンセイザイノ セイゾウホウ |
| US4008719A (en) | 1976-02-02 | 1977-02-22 | Alza Corporation | Osmotic system having laminar arrangement for programming delivery of active agent |
| US4166452A (en) | 1976-05-03 | 1979-09-04 | Generales Constantine D J Jr | Apparatus for testing human responses to stimuli |
| US4256108A (en) | 1977-04-07 | 1981-03-17 | Alza Corporation | Microporous-semipermeable laminated osmotic system |
| US4265874A (en) | 1980-04-25 | 1981-05-05 | Alza Corporation | Method of delivering drug with aid of effervescent activity generated in environment of use |
| IE58110B1 (en) | 1984-10-30 | 1993-07-14 | Elan Corp Plc | Controlled release powder and process for its preparation |
| US4775536A (en) | 1986-02-24 | 1988-10-04 | Bristol-Myers Company | Enteric coated tablet and process for making |
| US5068110A (en) | 1987-09-29 | 1991-11-26 | Warner-Lambert Company | Stabilization of enteric coated dosage form |
| US5073543A (en) | 1988-07-21 | 1991-12-17 | G. D. Searle & Co. | Controlled release formulations of trophic factors in ganglioside-lipsome vehicle |
| US5135757A (en) | 1988-09-19 | 1992-08-04 | Edward Mendell Co., Inc. | Compressible sustained release solid dosage forms |
| IT1229203B (it) | 1989-03-22 | 1991-07-25 | Bioresearch Spa | Impiego di acido 5 metiltetraidrofolico, di acido 5 formiltetraidrofolico e dei loro sali farmaceuticamente accettabili per la preparazione di composizioni farmaceutiche in forma a rilascio controllato attive nella terapia dei disturbi mentali organici e composizioni farmaceutiche relative. |
| US5007790A (en) | 1989-04-11 | 1991-04-16 | Depomed Systems, Inc. | Sustained-release oral drug dosage form |
| US5120548A (en) | 1989-11-07 | 1992-06-09 | Merck & Co., Inc. | Swelling modulated polymeric drug delivery device |
| US5733566A (en) | 1990-05-15 | 1998-03-31 | Alkermes Controlled Therapeutics Inc. Ii | Controlled release of antiparasitic agents in animals |
| US5580578A (en) | 1992-01-27 | 1996-12-03 | Euro-Celtique, S.A. | Controlled release formulations coated with aqueous dispersions of acrylic polymers |
| US5591767A (en) | 1993-01-25 | 1997-01-07 | Pharmetrix Corporation | Liquid reservoir transdermal patch for the administration of ketorolac |
| FR2704146B1 (fr) | 1993-04-19 | 1995-07-13 | Cripdom | Microcapsules d'acide acétylsalicylique à libération contrôlée. |
| US5424286A (en) | 1993-05-24 | 1995-06-13 | Eng; John | Exendin-3 and exendin-4 polypeptides, and pharmaceutical compositions comprising same |
| US5773025A (en) | 1993-09-09 | 1998-06-30 | Edward Mendell Co., Inc. | Sustained release heterodisperse hydrogel systems--amorphous drugs |
| US5589194A (en) | 1993-09-20 | 1996-12-31 | Minnesota Mining And Manufacturing Company | Method of encapsulation and microcapsules produced thereby |
| GB9412394D0 (en) | 1994-06-21 | 1994-08-10 | Danbiosyst Uk | Colonic drug delivery composition |
| IT1270594B (it) | 1994-07-07 | 1997-05-07 | Recordati Chem Pharm | Composizione farmaceutica a rilascio controllato di moguisteina in sospensione liquida |
| FR2725623A1 (fr) | 1994-10-18 | 1996-04-19 | Flamel Tech Sa | Microcapsules medicamenteuses et/ou nutritionnelles pour administration per os |
| JPH08143476A (ja) | 1994-11-18 | 1996-06-04 | Japan Tobacco Inc | 薬物放出制御膜及び固形製剤 |
| GB2338235B (en) | 1997-04-15 | 2001-11-14 | Csir | Appetite suppressing plant extracts |
| ATE355840T1 (de) | 1997-06-18 | 2007-03-15 | Smithkline Beecham Plc | Behandlung der diabetes mit thiazolidindione und metformin |
| US5891919A (en) | 1997-09-19 | 1999-04-06 | Burlington Bio-Medical & Scientific Corp. | Denatonium capsaicinate and methods of producing the same |
| AU766219B2 (en) | 1998-02-02 | 2003-10-09 | 1149336 Ontario Inc. | Method of regulating glucose metabolism, and reagents related thereto |
| EP1063973B1 (en) * | 1998-03-19 | 2016-11-16 | Bristol-Myers Squibb Company | Biphasic controlled release delivery system for high solubility pharmaceuticals and method |
| US6099859A (en) | 1998-03-20 | 2000-08-08 | Andrx Pharmaceuticals, Inc. | Controlled release oral tablet having a unitary core |
| US6191162B1 (en) | 1998-05-28 | 2001-02-20 | Medical Research Institute | Method of reducing serum glucose levels |
| US6538194B1 (en) | 1998-05-29 | 2003-03-25 | Catalysts & Chemicals Industries Co., Ltd. | Photoelectric cell and process for producing metal oxide semiconductor film for use in photoelectric cell |
| US6099862A (en) | 1998-08-31 | 2000-08-08 | Andrx Corporation | Oral dosage form for the controlled release of a biguanide and sulfonylurea |
| HK1040910B (en) * | 1998-11-12 | 2009-06-26 | Smithkline Beecham Plc | Pharmaceutical composition for modified release of an insulin sensitiser and metformin |
| US20040081697A1 (en) | 1998-11-12 | 2004-04-29 | Smithkline Beecham P.L.C. | Pharmaceutical composition for modified release of an insulin sensitiser and another antidiabetic agent |
| TW514510B (en) | 1999-06-11 | 2002-12-21 | Tanita Seisakusho Kk | Method and apparatus for measuring distribution of body fat |
| ITMI991316A1 (it) | 1999-06-14 | 2000-12-14 | Cip Ninety Two 92 S A | Composizioni farmaceutiche orali a rilascio modificato di mesalazina |
| DE19940944B4 (de) | 1999-08-31 | 2006-10-12 | Grünenthal GmbH | Retardierte, orale, pharmazeutische Darreichungsformen |
| AR028299A1 (es) | 1999-09-17 | 2003-05-07 | Novartis Ag | Una composicion farmaceutica que comprende nateglinida, un proceso para su preparacion y el uso de dicha composicion para la preparacion de un medicamento para el tratamiento de desordenes metabolicos, especialmente diabetes, o de una enfermedad o condicion asociada con diabetes. |
| US6530886B1 (en) | 1999-10-08 | 2003-03-11 | Tanita Corporation | Method and apparatus for measuring subcutaneous fat using ultrasonic wave |
| IL132313A0 (en) | 1999-10-11 | 2001-03-19 | Yeda Res & Dev | Leptin assay |
| US6586438B2 (en) | 1999-11-03 | 2003-07-01 | Bristol-Myers Squibb Co. | Antidiabetic formulation and method |
| AR030920A1 (es) | 1999-11-16 | 2003-09-03 | Smithkline Beecham Plc | Composiciones farmaceuticas para el tratamiento de la diabetes mellitus y condiciones asociadas con la diabetes mellitus, y procedimientos para preparar dichas composiciones |
| US6676966B1 (en) | 2000-05-09 | 2004-01-13 | Intellipharmaceutics Corp. | Extended release metformin hydrochloride formulations |
| TW515705B (en) | 2000-05-31 | 2003-01-01 | Yamato Scale Co Ltd | Visceral fat meter |
| US6451808B1 (en) | 2000-10-17 | 2002-09-17 | Depomed, Inc. | Inhibition of emetic effect of metformin with 5-HT3 receptor antagonists |
| US6790459B1 (en) | 2000-11-03 | 2004-09-14 | Andrx Labs, Llc | Methods for treating diabetes via administration of controlled release metformin |
| US6689385B2 (en) | 2000-11-03 | 2004-02-10 | Chronorx Llc | Formulations for the treatment of insulin resistance and type 2 diabetes mellitus |
| US20110217394A1 (en) | 2000-12-05 | 2011-09-08 | Brett Justin West | Iridoid Based Formulations |
| ATE508738T1 (de) | 2001-01-12 | 2011-05-15 | Sun Pharma Advanced Res Co Ltd | System zur beabstandeten abgabe von arzneimitteln |
| KR100380147B1 (ko) | 2001-01-18 | 2003-04-11 | 주식회사 엘지생명과학 | 류마티스성 자가면역 항체의 검출방법 및 검출키트 |
| WO2002078617A2 (en) | 2001-03-28 | 2002-10-10 | University Of South Florida | Materials and methods for treatment of cancer and identification of anti-cancer compounds |
| US7883856B2 (en) | 2001-04-05 | 2011-02-08 | Senomyx Inc. | Identification of bitter ligands that specifically activate human T2R receptors and related assays for identifying human bitter taste modulators |
| US8030008B2 (en) | 2001-04-05 | 2011-10-04 | Senomyx, Inc. | Identification of bitter ligands that specifically activate human T2R receptors and related assays for identifying human bitter taste modulators |
| RU2324475C2 (ru) | 2001-04-10 | 2008-05-20 | Сан Фармасьютикал Индастриз Лимитед | Состав, выделяемый в импульсном режиме в заданное время |
| JP4848558B2 (ja) * | 2001-05-08 | 2011-12-28 | トーアエイヨー株式会社 | 塩酸メトホルミン含有速放性錠剤 |
| FR2825023B1 (fr) | 2001-05-23 | 2005-04-15 | Flamel Tech Sa | Forme pharmaceutique orale antidiabetique "une prise par jour"comprenant une biguanide et au moins un autre principe actif |
| WO2003004009A1 (en) | 2001-07-02 | 2003-01-16 | Geneva Pharmaceuticals, Inc. | Pharmaceutical composition |
| US20030007420A1 (en) | 2001-07-05 | 2003-01-09 | Koninklijke Philips Electronics N.V. | Dial face of watch graphically represents calendar |
| 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 |
| US6642003B2 (en) | 2001-08-02 | 2003-11-04 | Cedars-Sinai Medical Center | Human glucose-dependent insulin-secreting cell line |
| US20040202718A1 (en) | 2001-09-28 | 2004-10-14 | Tyebji Ziauddin Z. | Dosage form for treatment of diabetes mellitus |
| FR2830447B1 (fr) | 2001-10-09 | 2004-04-16 | Flamel Tech Sa | Forme galenique orale microparticulaire pour la liberation retardee et controlee de principes actifs pharmaceutiques |
| PL369328A1 (en) | 2001-11-06 | 2005-04-18 | Ranbaxy Laboratories Limited | Controlled release tablets of metformin |
| US6709251B2 (en) | 2001-11-16 | 2004-03-23 | Mgs Enterprises, Inc. | Self-contained frameless rotating mold support |
| ITFI20010230A1 (it) | 2001-11-29 | 2003-05-29 | Menarini Int Operations Lu Sa | Composizioni farmaceutiche per il trattamento del diabete mellito di tipo ii |
| US20030113366A1 (en) * | 2001-12-14 | 2003-06-19 | Macgregor Alexander | Reverse-micellar delivery system for controlled transportation and enhanced absorption of agents |
| US7183321B2 (en) | 2001-12-17 | 2007-02-27 | Bristol-Myers Squibb Company | Antidiabetic formulation and method |
| AU2003211131A1 (en) * | 2002-02-14 | 2003-09-04 | Sonus Pharmaceuticals, Inc. | Metformin salts of lipophilic acids |
| US20030171407A1 (en) | 2002-03-07 | 2003-09-11 | Upsher-Smith Laboratories, Inc. | Composition for reducing blood glucose and cholesterol |
| US6830759B2 (en) | 2002-06-28 | 2004-12-14 | Ajinomoto Co., Inc. | Antidiabetic preparation for oral administration |
| US20060019346A1 (en) | 2002-07-29 | 2006-01-26 | Senomyx, Inc. | Identification of a novel bitter taste receptor T2R76 that specifically responds to brucine and prop bitter ligands |
| AU2003261298A1 (en) * | 2002-08-02 | 2004-02-23 | Penwest Pharmaceuticals Company | Sustained release formulations of metformin |
| CN1413582A (zh) * | 2002-11-29 | 2003-04-30 | 贵州圣济堂制药有限公司 | 盐酸二甲双胍肠溶片及其制备方法 |
| DE60320682T2 (de) | 2002-12-18 | 2009-06-10 | Givaudan S.A. | Chimäre alpha q-gustducin g-proteine |
| DE10308504A1 (de) | 2003-02-26 | 2004-09-09 | Basf Ag | Enzymatische Herstellung von (Meth)acrylsäureestern |
| US7135575B2 (en) | 2003-03-03 | 2006-11-14 | Array Biopharma, Inc. | P38 inhibitors and methods of use thereof |
| EP1635832A2 (en) | 2003-06-06 | 2006-03-22 | Merck & Co., Inc. | Combination therapy for the treatment of diabetes |
| CN1805738A (zh) | 2003-06-16 | 2006-07-19 | 兰贝克赛实验室有限公司 | 持续释放的二甲双胍片剂 |
| WO2005009351A2 (en) | 2003-07-17 | 2005-02-03 | Santé International, Inc. | Dietary supplement for promoting control of blood-sugar levels and associated pathology in type 2 diabetics |
| AU2003269484A1 (en) | 2003-09-11 | 2005-03-29 | Biocon Limited | Salt of atorvastatin with metformin |
| EA200600598A1 (ru) | 2003-09-19 | 2006-08-25 | Пенвест Фармасьютикалз Ко. | Лекарственные формы замедленного высвобождения |
| EP1677759A1 (en) * | 2003-10-31 | 2006-07-12 | Alza Corporation | Compositions and dosage forms for enhanced absorption of gabapentin and pregabalin |
| CN1901881A (zh) | 2003-10-31 | 2007-01-24 | 阿尔扎公司 | 用于增强的吸收的组合物和剂型 |
| US7442720B2 (en) | 2003-12-19 | 2008-10-28 | Omega Bio-Pharma (I.P.3) Limited | Compositions and methods for treating diabetes |
| WO2005060942A1 (en) | 2003-12-19 | 2005-07-07 | Aurobindo Pharma Ltd | Extended release pharmaceutical composition of metformin |
| EP1591114A1 (en) | 2004-03-12 | 2005-11-02 | Fournier Laboratories Ireland Limited | Use of metformin and orlistat for the treatment or prevention of obesity |
| CN1561980A (zh) * | 2004-03-26 | 2005-01-12 | 贵州圣济堂制药有限公司 | 盐酸二甲双胍肠溶缓释制剂及其制备方法 |
| KR20070053659A (ko) | 2004-04-20 | 2007-05-25 | 도이체스 인스티튜트 퓌어 에른에룬그스포슝 | 쓴맛 수용체의 작용제 및 그의 용도 |
| DE102004036437A1 (de) | 2004-07-27 | 2006-03-23 | Röhm GmbH & Co. KG | Multipartikuläre Arzneiform für wenig lösliche Wirkstoffe, sowie ein Verfahren zur Herstellung der Arzneiform |
| US20060024335A1 (en) | 2004-07-29 | 2006-02-02 | Roger Stier E | Oral compositions which mask the bitter taste of a bitter-tasting agent |
| CN101014360A (zh) | 2004-08-03 | 2007-08-08 | 埃米斯菲尔技术公司 | 抗糖尿病口服胰岛素－双胍组合物 |
| WO2006053771A2 (en) | 2004-11-18 | 2006-05-26 | Deutsches Institut Für Ernährungsforschung Potsdam-Rehbrücke Stiftung Des Öffentlichen Rechts | Agonists of bitter taste receptors and uses thereof |
| TW200640497A (en) | 2005-01-21 | 2006-12-01 | Pharmanova Inc | Pharmaceutical formulations and methods of use |
| WO2006082523A2 (en) | 2005-01-25 | 2006-08-10 | Aurobindo Pharma Limited | Pharmaceutical sustained release composition of metformin |
| US20070032420A1 (en) | 2005-02-09 | 2007-02-08 | Entelos, Inc. | Treating diabetes with glucagon-like peptide-1 secretagogues |
| US20060222709A1 (en) * | 2005-03-18 | 2006-10-05 | Agi Therapeutics Research Ltd. | Metformin methods and formulations for treating chronic constipation |
| WO2006104401A1 (en) | 2005-03-26 | 2006-10-05 | Protemix Corporation Limited | Copper antagonist compositions |
| EP2258382A3 (en) | 2005-03-31 | 2014-05-14 | Amylin Pharmaceuticals, LLC | Amylin and amylin agonists for treating psychiatric diseases and disorders |
| WO2006109175A2 (en) | 2005-04-11 | 2006-10-19 | Aurobindo Pharma Limited | Solid dosage form of an antidiabetic drug |
| BRPI0610034A2 (pt) | 2005-04-28 | 2011-10-18 | Ajinomoto Kk | composto, agente de icremento do transporte de açúcar, agente hipoglicêmico, agente para prevenção e/ou tratamento de uma doença, medicamento, composição farmacêutica , uso do composto, e, método de preparação para o composto |
| US20060269617A1 (en) | 2005-05-26 | 2006-11-30 | Suracell, Inc. | Supplement compositions and method of use for enhancement of insulin sensitivity |
| US7797782B2 (en) | 2005-06-21 | 2010-09-21 | Goody Products, Inc. | Handle having a ribbed gel grip |
| WO2007002026A2 (en) | 2005-06-22 | 2007-01-04 | Senomyx, Inc. | Identification of human t2r recepors that are activated by bitter molecules in coffee (chlorogenic lactones) and related assays for identifying human bitter taste modulators |
| CN1891229B (zh) * | 2005-07-07 | 2010-05-05 | 北京华安佛医药研究中心有限公司 | 预防或治疗代谢综合征的药物制剂 |
| US7700299B2 (en) | 2005-08-12 | 2010-04-20 | Hoffmann-La Roche Inc. | Method for predicting the response to a treatment |
| CA2620370A1 (en) | 2005-08-30 | 2007-03-22 | Nicholas Piramal India Limited | Extended release pharmaceutical composition of metformin and a process for producing it |
| FR2891459B1 (fr) | 2005-09-30 | 2007-12-28 | Flamel Technologies Sa | Microparticules a liberation modifiee d'au moins un principe actif et forme galenique orale en comprenant |
| KR100831771B1 (ko) * | 2005-10-27 | 2008-05-27 | 주식회사종근당 | 서방출과 ｐＨ 의존성 속방출을 나타내는 약제학적 조성물 |
| US20070104805A1 (en) | 2005-11-01 | 2007-05-10 | Udell Ronald G | Compositions of Hoodia Gordonii and Pinolenic Acid Derivatives |
| GB0526291D0 (en) | 2005-12-23 | 2006-02-01 | Prosidion Ltd | Therapeutic method |
| JP2007215162A (ja) | 2006-01-11 | 2007-08-23 | Canon Inc | 情報処理装置及びその制御方法、プログラム、記憶媒体 |
| US20070196399A1 (en) | 2006-02-21 | 2007-08-23 | Shin-Etsu Chemical Co., Ltd. | Enteric-coated preparation covered with enteric coating material for site-specific delivery of drug to site within the small intestine |
| US20070207227A1 (en) | 2006-02-23 | 2007-09-06 | Conopco, Inc., D/B/A Unilever, A Corporation Of New York | Appetite suppressant compositions |
| WO2007116404A2 (en) | 2006-04-10 | 2007-10-18 | Bar-Ilan University | Cucurbitacin glucosides and use thereof in treating cancer |
| PE20110235A1 (es) | 2006-05-04 | 2011-04-14 | Boehringer Ingelheim Int | Combinaciones farmaceuticas que comprenden linagliptina y metmorfina |
| CA2551706A1 (en) | 2006-06-27 | 2007-12-27 | Innovative Life Sciences Corporation | Herbal product comprising cinnamon and bitter melon |
| CN100596277C (zh) | 2006-07-10 | 2010-03-31 | 博仲盛景医药技术（北京）有限公司 | 一种促进肠胃蠕动的药物组合物 |
| CA2660464A1 (en) | 2006-08-17 | 2008-02-21 | Unilever Plc | Processes for production of hoodia plant extracts containing steroidal glycosides |
| MX2009001866A (es) | 2006-08-24 | 2009-03-02 | Unilever Nv | Proceso para la preparacion de una composicion que comprende glucosidos esteroides. |
| WO2008030429A2 (en) | 2006-09-05 | 2008-03-13 | Senomyx, Inc. | Novel haplotype of human t2r receptor ht2r50 and its use in assays for identifying human bitter taste modulators |
| US20080107787A1 (en) | 2006-11-02 | 2008-05-08 | The Coca-Cola Company | Anti-Diabetic Composition with High-Potency Sweetener |
| DK2089005T3 (da) | 2006-11-09 | 2010-07-19 | Orexigen Therapeutics Inc | Lagdelte farmaceutiske formuleringer omfattende et hurtigt opløsende mellemlag |
| WO2008058355A2 (en) | 2006-11-16 | 2008-05-22 | Walter Santos Junior | Descriptive report of patent of invention of the medicament 'atorvastatin + metformin' in combined form for cardiovascular diseases |
| BRMU8602999U (pt) | 2006-11-16 | 2008-07-08 | Walter Junior Santos | medicamento "rosuvastatina + metformina" em forma combinada para doenças cardiovasculares |
| CN101190179B (zh) * | 2006-11-20 | 2010-05-12 | 北京利龄恒泰药业有限公司 | 一种治疗糖尿病的肠溶药物组合物及其制备方法 |
| CN105152983A (zh) | 2007-01-29 | 2015-12-16 | 韩诺生物制药株式会社 | N,n-二甲基亚氨基二碳亚氨酸二酰胺乙酸盐、其制备方法和包含其的药物组合物 |
| CA2681092A1 (en) | 2007-03-15 | 2008-09-18 | Nectid, Inc. | Anti-diabetic combinations comprising a slow release biguanide composition and an immediate release dipeptidyl peptidase iv inhibitor composition |
| US20080064701A1 (en) | 2007-04-24 | 2008-03-13 | Ramesh Sesha | Anti-diabetic combinations |
| US20070172525A1 (en) | 2007-03-15 | 2007-07-26 | Ramesh Sesha | Anti-diabetic combinations |
| EP1975611A1 (en) | 2007-03-29 | 2008-10-01 | Deutsches Institut für Ernährungsforschung Potsdam -Rehbrücke-Stiftung des öffentlichen Rechts- Vertreten durch den Stiftungsvorstand | Agonists of bitter taste receptors and uses thereof |
| EP1975612A1 (en) | 2007-03-29 | 2008-10-01 | Deutsches Institut für Ernährungsforschung Potsdam -Rehbrücke-Stiftung des öffentlichen Rechts- Vertreten durch den Stiftungsvorstand | Agonists of bitter taste receptors and uses thereof |
| AU2008279447A1 (en) * | 2007-07-19 | 2009-01-29 | Metabolex, Inc. | N-azacyclic substituted pyrrole, pyrazole, imidazole, triazole and tetrazole derivatives as agonists of the RUP3 or GPR119 receptor for the treatment of diabetes and metabolic disorders |
| EP2023144A1 (en) | 2007-08-01 | 2009-02-11 | Sanofi-Aventis | Novel AS160-like protein, test systems, methods and uses involving it for the identification of diabetes type 2 therapeutics |
| US20090042813A1 (en) | 2007-08-10 | 2009-02-12 | Sergey Michailovich Melnikov | Hoodia extract oil compositions comprising medium chain triglycerides |
| US8076491B2 (en) | 2007-08-21 | 2011-12-13 | Senomyx, Inc. | Compounds that inhibit (block) bitter taste in composition and use thereof |
| WO2009053980A2 (en) | 2007-10-24 | 2009-04-30 | Arava Hoodia Growers A. C. S. Ltd. | An improved appetite suppressant |
| WO2009095993A1 (ja) | 2008-01-29 | 2009-08-06 | Nakamori Pharmaceutical Co., Ltd. | 医薬組成物 |
| MX2010009731A (es) | 2008-03-04 | 2010-09-30 | Merck Sharp & Dohme | Composiciones farmaceuticas de una combinacion de metformina y un inhibidor de dipeptidil peptidasa-iv. |
| US9844224B2 (en) | 2008-05-23 | 2017-12-19 | Givaudan Sa | Bitter alkaloid containing consumables comprising bitter blockers |
| CN101590007A (zh) * | 2008-05-27 | 2009-12-02 | 北京瑞伊人科技发展有限公司 | 一种盐酸二甲双胍/伏格列波糖降糖口服制剂组合物及其制备 |
| CN101695575A (zh) | 2008-05-29 | 2010-04-21 | 北京奥萨医药研究中心有限公司 | 含有他汀类降脂药物、双胍类降糖药物和烟酸的药物组合物 |
| WO2009149577A1 (en) | 2008-06-13 | 2009-12-17 | Givaudan Sa | Methods of identifying modulators of the bitter taste receptor tas2r44 |
| CN101339178B (zh) | 2008-08-07 | 2013-05-01 | 贵州天安药业股份有限公司 | 盐酸二甲双胍肠溶片的质量控制方法 |
| JP5539881B2 (ja) | 2008-08-29 | 2014-07-02 | サントリーホールディングス株式会社 | 新規エピガロカテキンガレート４量体、およびそれらを含む血管内皮機能改善剤 |
| US8557530B2 (en) | 2008-08-29 | 2013-10-15 | Givaudan Sa | Use of a TAS2R7 nucleic acid sequence to identify modulators |
| WO2010045417A2 (en) | 2008-10-16 | 2010-04-22 | Metabolous Pharmaceuticals, Inc. | Combination therapies for the treatment of obesity |
| WO2010045656A2 (en) | 2008-10-17 | 2010-04-22 | Nectid, Inc. | Novel sglt2 inhibitor dosage forms |
| WO2010060198A1 (en) | 2008-11-26 | 2010-06-03 | West Central Envirotech Inc. | Composition and method for controlling insects |
| AU2009326965A1 (en) | 2008-12-12 | 2011-06-23 | Poxel | Tetrahydrotriazine compounds for treating diseases associated with AMPK activity |
| CN102272129B (zh) | 2009-01-03 | 2014-10-08 | 静冈县公立大学法人 | 硫酸化c-糖苷及其分离方法以及合成方法 |
| TW201036975A (en) * | 2009-01-07 | 2010-10-16 | Boehringer Ingelheim Int | Treatment for diabetes in patients with inadequate glycemic control despite metformin therapy |
| BRPI1013856A2 (pt) | 2009-04-20 | 2016-04-05 | Elcelyx Therapeutics Inc | terapias à base de ligantes de receptores quimiossensíveis |
| US8828953B2 (en) | 2009-04-20 | 2014-09-09 | NaZura BioHealth, Inc. | Chemosensory receptor ligand-based therapies |
| US9901551B2 (en) | 2009-04-20 | 2018-02-27 | Ambra Bioscience Llc | Chemosensory receptor ligand-based therapies |
| US20100331419A1 (en) * | 2009-06-25 | 2010-12-30 | Aronne Louis J | Combination Therapies for the Treatment of Obesity |
| US20100331420A1 (en) | 2009-06-26 | 2010-12-30 | Aronne Louis J | Combination Therapies for the Treatment of Obesity |
| TW201105336A (en) | 2009-07-01 | 2011-02-16 | Kissei Pharmaceutical | Combined medicine of pyrazole derivative and biguanide drug |
| EP2283830A1 (en) | 2009-07-23 | 2011-02-16 | Actogenix N.V. | Aqueous enteric capsule coating |
| US8709745B2 (en) | 2009-07-28 | 2014-04-29 | Deutsches Institut Für Ernährungsforschung Potsdam-Rehbrücke | Methods for isolating ligands of the human bitter taste receptor TAS2R49 |
| WO2011041632A2 (en) | 2009-10-01 | 2011-04-07 | Metabolous Pharmaceuticals, Inc. | Combination therapies for the treatment of obesity |
| EP2488180A4 (en) | 2009-10-12 | 2013-03-27 | Ipca Lab Ltd | PHARMACEUTICAL COMPOSITIONS FOR THE TREATMENT / PROPHYLAXIS OF NON-ALCOHOLIC FAT TREATMENTS |
| CA2777938C (en) | 2009-10-21 | 2017-11-14 | Wisconsin Alumni Research Foundation | Method of preventing type 1 diabetes |
| CA2778015C (en) * | 2009-10-26 | 2016-08-02 | Warner Chilcott Company, Llc | Bisphosphonate compounds for treating bone metabolism disorders |
| CA2779906A1 (en) | 2009-12-04 | 2011-06-09 | Colgate-Palmolive Company | Oral compositions containing extracts of garcinia mangostana l. and related methods |
| EP2345646A1 (en) | 2010-01-14 | 2011-07-20 | InterMed Discovery GmbH | Use of tricyclic sesquiterpene lactones in the treatment of obesity and related diseases and non-therapeutic treatable conditions |
| CN101785763B (zh) * | 2010-02-04 | 2011-11-23 | 贵州天安药业股份有限公司 | 一种盐酸二甲双胍肠溶缓释片及其制备方法 |
| US20130273154A1 (en) | 2011-03-02 | 2013-10-17 | Joseph M. Fayad | Oral formulations Mimetic of Roux-en-Y gastric bypass actions on the ileal brake; Compositions, Methods of Treatment, Diagnostics and Systems for treatment of metabolic syndrome manifestations including insulin resistance, fatty liver disease, hpperlipidemia, and type 2 diabetes |
| US20140294951A1 (en) * | 2011-10-26 | 2014-10-02 | Joseph M. Fayad | Oral formulations mimetic of Roux-en-Y gastric bypass actions on the ileal brake; Compositions, methods of treatment, diagnostics and systems for treatment of metabolic syndrome manifestations including insulin resistance, fatty liver disease, hyperlipidemia, and T2D |
| CA2792862C (en) * | 2010-03-10 | 2018-03-06 | Incube Labs, Llc | Therapeutic agent preparations for delivery into a lumen of the intestinal tract using a swallowable drug delivery device |
| US8276242B2 (en) | 2010-04-09 | 2012-10-02 | Girard Mylene | Adjustable handle assembly with locking mechanism |
| US8581001B2 (en) * | 2010-04-16 | 2013-11-12 | Codman & Shurtleff | Metformin-cysteine prodrug |
| US20110293753A1 (en) | 2010-05-28 | 2011-12-01 | Louis Bellafiore | Tocotrienol Compositions |
| TWI436768B (zh) | 2010-06-09 | 2014-05-11 | Poxel | 第２型糖尿病之治療 |
| GB201009873D0 (en) | 2010-06-14 | 2010-07-21 | Univ Leuven Kath | Method for hydrogenation of isoalpha-acids (isohumulones) to hexahydro-iso-alpha-acids (hexahydro-isohumulones) by using heterogeneous ruthenium |
| WO2011159100A2 (ko) | 2010-06-15 | 2011-12-22 | 한올바이오파마주식회사 | 항암 활성을 나타내는 약제학적 조성물 |
| US20140235558A1 (en) | 2010-06-15 | 2014-08-21 | Hanall Biopharma Co., Ltd. | Pharmaceutical composition having activity of anticancer |
| KR101275258B1 (ko) | 2010-06-15 | 2013-06-17 | 한올바이오파마주식회사 | 항암 활성을 나타내는 약제학적 조성물 |
| CN103068380A (zh) | 2010-06-17 | 2013-04-24 | 加州理工学院 | 用于调节激素的方法和系统以及相关的方法、剂和组合物 |
| EP2397039A1 (en) | 2010-06-21 | 2011-12-21 | Abbott Laboratories | Compositions for delaying progression of diabetes using Salacia oblonga extract |
| KR20130093012A (ko) | 2010-06-24 | 2013-08-21 | 베링거 인겔하임 인터내셔날 게엠베하 | 당뇨병 요법 |
| US9056134B2 (en) | 2010-07-21 | 2015-06-16 | Nucitec S.A. De C.V. | Single daily dosage form for prevention and treatment of metabolic syndrome |
| CN101978956B (zh) * | 2010-10-13 | 2012-03-28 | 北京京丰制药有限公司 | 盐酸二甲双胍肠溶片及其制备方法 |
| EA201370099A1 (ru) | 2010-10-19 | 2013-11-29 | Элселикс Терапьютикс, Инк. | Терапия на основе лигандов хемосенсорных рецепторов |
| JP2014505011A (ja) | 2010-10-19 | 2014-02-27 | エルセリクス セラピューティクス インコーポレイテッド | 化学感覚受容体リガンドに基づく治療法 |
| EP2629773A2 (en) | 2010-10-19 | 2013-08-28 | Elcelyx Therapeutics, Inc. | Chemosensory receptor ligand-based therapies |
| CN103402358A (zh) | 2010-10-19 | 2013-11-20 | 埃尔舍利克斯治疗公司 | 以化学感应受体配体为基础的治疗 |
| WO2012054528A2 (en) | 2010-10-19 | 2012-04-26 | Elcelyx Therapeutics, Inc. | Chemosensory receptor ligand-based therapies |
| US9211263B2 (en) | 2012-01-06 | 2015-12-15 | Elcelyx Therapeutics, Inc. | Compositions and methods of treating metabolic disorders |
| HUE051738T2 (hu) | 2011-01-07 | 2021-03-29 | Anji Pharma Us Llc | Kemoszenzoros receptorligandum-alapú terápiák |
| US9572784B2 (en) | 2011-01-07 | 2017-02-21 | Elcelyx Therapeutics, Inc. | Compositions comprising statins, biguanides and further agents for reducing cardiometabolic risk |
| US8796338B2 (en) | 2011-01-07 | 2014-08-05 | Elcelyx Therapeutics, Inc | Biguanide compositions and methods of treating metabolic disorders |
| US9480663B2 (en) | 2011-01-07 | 2016-11-01 | Elcelyx Therapeutics, Inc. | Biguanide compositions and methods of treating metabolic disorders |
| US11974971B2 (en) | 2011-01-07 | 2024-05-07 | Anji Pharmaceuticals Inc. | Compositions and methods for treating metabolic disorders |
| CN102188429A (zh) * | 2011-05-20 | 2011-09-21 | 吴四清 | 一种治疗糖尿病的药物组合物 |
| CN102357088A (zh) | 2011-10-26 | 2012-02-22 | 河北山姆士药业有限公司 | 盐酸二甲双胍肠溶片 |
| EA033067B1 (ru) | 2012-01-06 | 2019-08-30 | Элселикс Терапьютикс, Инк. | Способ лечения метаболических расстройств у пациента, имеющего противопоказание к назначению бигуанидного соединения |
| KR20200137035A (ko) | 2012-01-06 | 2020-12-08 | 앤지 파마 유에스 엘엘씨 | 바이구아나이드 조성물 및 대사 장애를 치료하는 방법 |
| CN105101956B (zh) | 2013-01-05 | 2018-12-07 | 埃尔舍利克斯治疗公司 | 包含双胍的延迟释放组合物 |
-
2012
- 2012-07-11 KR KR1020207034195A patent/KR20200137035A/ko not_active Ceased
- 2012-07-11 CN CN201280070968.0A patent/CN104254325A/zh active Pending
- 2012-07-11 SG SG11201403839SA patent/SG11201403839SA/en unknown
- 2012-07-11 CA CA2862533A patent/CA2862533C/en active Active
- 2012-07-11 CN CN201910957458.9A patent/CN110693868A/zh active Pending
- 2012-07-11 MX MX2014008190A patent/MX2014008190A/es active IP Right Grant
- 2012-07-11 KR KR1020147021875A patent/KR102035879B1/ko active Active
- 2012-07-11 AU AU2012363873A patent/AU2012363873B2/en active Active
- 2012-07-11 BR BR112014016808-3A patent/BR112014016808B1/pt active IP Right Grant
- 2012-07-11 JP JP2014551231A patent/JP2015503582A/ja not_active Withdrawn
- 2012-07-11 ES ES12738330T patent/ES2832773T3/es active Active
- 2012-07-11 EP EP12738330.5A patent/EP2800561B1/en active Active
- 2012-07-11 SG SG10201911743TA patent/SG10201911743TA/en unknown
- 2012-07-11 KR KR1020197030360A patent/KR20190120430A/ko not_active Ceased
- 2012-07-11 WO PCT/US2012/046335 patent/WO2013103384A1/en not_active Ceased
- 2012-07-11 EA EA201491335A patent/EA201491335A1/ru unknown
- 2012-07-11 KR KR1020237020116A patent/KR20230095124A/ko not_active Ceased
-
2014
- 2014-07-02 MX MX2020003112A patent/MX2020003112A/es unknown
- 2014-07-03 IL IL233506A patent/IL233506B/en active IP Right Grant
- 2014-07-10 ZA ZA2014/05046A patent/ZA201405046B/en unknown
-
2016
- 2016-10-31 US US15/339,346 patent/US10154972B2/en active Active
-
2017
- 2017-04-13 JP JP2017079805A patent/JP2017141289A/ja active Pending
-
2018
- 2018-02-22 AU AU2018201308A patent/AU2018201308A1/en not_active Abandoned
- 2018-12-17 US US16/223,002 patent/US11065215B2/en active Active
-
2019
- 2019-09-12 JP JP2019165827A patent/JP7335056B2/ja active Active
-
2021
- 2021-07-21 JP JP2021120385A patent/JP2021169522A/ja active Pending
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| JP2015503582A5 (https=) | ||
| ES3031577T3 (en) | Treatment of type 2 diabetes with 2-[(4-{6-[(4-cyano-2-fluorobenzyl)oxy]pyridin-2-yl} piperidin-1-yl)methyl]-1-[(2s)-oxetan-2-ylmethyl]-1h-benzimidazole-6-carboxylic acid or a pharmaceutically salt thereof | |
| JP2022001592A (ja) | 代謝障害を治療するための組成物および方法 | |
| CN103998035B (zh) | 包含格列酮和nrf2激活剂的药物组合物 | |
| ES2832773T3 (es) | Composiciones de biguanida y métodos de tratamiento de trastornos metabólicos | |
| CN110051638B (zh) | 包含双胍的延迟释放组合物 | |
| CA2724133C (en) | Medicine consisting of concomitant use or combination of dpp-iv inhibitor and other diabetic medicine | |
| JP2023096079A (ja) | 化合物の製剤およびそれらの使用 | |
| MX2011008530A (es) | Formulaciones farmaceuticas de liberacion controlada de nitazoxanida. | |
| JP6986445B2 (ja) | １５−ｈｅｐｅを含む組成物、およびそれを用いて線維症を処置または防止する方法 | |
| TWI842924B (zh) | Gpr119致效劑及dpp-4抑制劑的藥物組合及藥物套組 | |
| EP2872127A1 (en) | Compositions comprising statins, biguanides and further agents for reducing cardiometabolic risk | |
| WO2014017833A1 (en) | Composite formulation for oral administration comprising metformin and rosuvastatin | |
| KR20100135700A (ko) | 지방성 간 질환의 치료용 의약 조성물 | |
| US9815777B2 (en) | Metformin salts to treat Type2 diabetes | |
| US20240180871A1 (en) | Modified-release silodosin compositions and use thereof in methods for male contraception | |
| WO2018016596A1 (ja) | ＰＰＡＲαアゴニストを含有する、肺高血圧症の予防又は治療剤 | |
| KR20250171978A (ko) | 엠파글리플로진 및 메트포르민을 포함하는 약제학적 복합제제 | |
| HK40021394A (en) | Compositions and methods for treating metabolic disorders | |
| US10772882B2 (en) | Pulmonary hypertension preventative or therapeutic agent containing crude drug | |
| HK40078244A (en) | Treatment of type 2 diabetes or obesity or overweight with 2-[(4-{6-[(4-cyano-2-fluorobenzyl)oxy]pyridin-2-yl} piperidin-1-yl)methyl]-1-[(2s)-oxetan-2-ylmethyl]-1h-benzimidazole-6-carboxylic acid or a pharmaceutically salt thereof | |
| HK40012109A (en) | Delayed-release composition comprising biguanide | |
| HK40012109B (zh) | 包含双胍的延迟释放组合物 | |
| RU2020143179A (ru) | Фармацевтическая комбинация, композиция и состав, содержащие активатор глюкокиназы и ингибитор альфа-глюкозидазы, способы приготовления и их применение |