JP2012526096A5 - - Google Patents
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- JP2012526096A5 JP2012526096A5 JP2012509115A JP2012509115A JP2012526096A5 JP 2012526096 A5 JP2012526096 A5 JP 2012526096A5 JP 2012509115 A JP2012509115 A JP 2012509115A JP 2012509115 A JP2012509115 A JP 2012509115A JP 2012526096 A5 JP2012526096 A5 JP 2012526096A5
- Authority
- JP
- Japan
- Prior art keywords
- diabetes
- acceptable salt
- pharmaceutically acceptable
- alkyl
- disease
- 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.)
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- 150000001875 compounds Chemical class 0.000 claims 11
- 150000003839 salts Chemical class 0.000 claims 11
- 229910052739 hydrogen Inorganic materials 0.000 claims 8
- 239000001257 hydrogen Substances 0.000 claims 8
- 239000000203 mixture Substances 0.000 claims 8
- -1 3-oxetanyl Chemical group 0.000 claims 7
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 6
- 150000002431 hydrogen Chemical class 0.000 claims 6
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 5
- 125000004093 cyano group Chemical group *C#N 0.000 claims 5
- 208000001072 type 2 diabetes mellitus Diseases 0.000 claims 5
- 206010012601 diabetes mellitus Diseases 0.000 claims 4
- 208000002705 Glucose Intolerance Diseases 0.000 claims 3
- 206010067584 Type 1 diabetes mellitus Diseases 0.000 claims 3
- 201000010099 disease Diseases 0.000 claims 3
- 208000035475 disorder Diseases 0.000 claims 3
- 229910052736 halogen Inorganic materials 0.000 claims 3
- 150000002367 halogens Chemical class 0.000 claims 3
- 201000009104 prediabetes syndrome Diseases 0.000 claims 3
- GVIYUKXRXPXMQM-BPXGDYAESA-N 221231-10-3 Chemical compound C([C@H](N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H]1C(N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CO)C(=O)N[C@H](C(=O)N[C@@H](CCC(O)=O)C(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CSSC1)C(=O)NCC(=O)N[C@@H](CC=1C=CC=CC=1)C(O)=O)C(C)C)=O)C1=CC=C(O)C=C1 GVIYUKXRXPXMQM-BPXGDYAESA-N 0.000 claims 2
- RKWGIWYCVPQPMF-UHFFFAOYSA-N Chloropropamide Chemical compound CCCNC(=O)NS(=O)(=O)C1=CC=C(Cl)C=C1 RKWGIWYCVPQPMF-UHFFFAOYSA-N 0.000 claims 2
- 206010009900 Colitis ulcerative Diseases 0.000 claims 2
- 108010011459 Exenatide Proteins 0.000 claims 2
- 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 2
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 2
- 208000031226 Hyperlipidaemia Diseases 0.000 claims 2
- 208000035180 MODY Diseases 0.000 claims 2
- 150000001204 N-oxides Chemical class 0.000 claims 2
- 208000008589 Obesity Diseases 0.000 claims 2
- YASAKCUCGLMORW-UHFFFAOYSA-N Rosiglitazone Chemical compound C=1C=CC=NC=1N(C)CCOC(C=C1)=CC=C1CC1SC(=O)NC1=O YASAKCUCGLMORW-UHFFFAOYSA-N 0.000 claims 2
- 201000006704 Ulcerative Colitis Diseases 0.000 claims 2
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- 229960004580 glibenclamide Drugs 0.000 claims 2
- 239000008103 glucose Substances 0.000 claims 2
- ZNNLBTZKUZBEKO-UHFFFAOYSA-N glyburide Chemical compound COC1=CC=C(Cl)C=C1C(=O)NCCC1=CC=C(S(=O)(=O)NC(=O)NC2CCCCC2)C=C1 ZNNLBTZKUZBEKO-UHFFFAOYSA-N 0.000 claims 2
- 201000006950 maturity-onset diabetes of the young Diseases 0.000 claims 2
- 230000002503 metabolic effect Effects 0.000 claims 2
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 2
- 208000010125 myocardial infarction Diseases 0.000 claims 2
- 235000020824 obesity Nutrition 0.000 claims 2
- HYAFETHFCAUJAY-UHFFFAOYSA-N pioglitazone Chemical compound N1=CC(CC)=CC=C1CCOC(C=C1)=CC=C1CC1C(=O)NC(=O)S1 HYAFETHFCAUJAY-UHFFFAOYSA-N 0.000 claims 2
- 208000037803 restenosis Diseases 0.000 claims 2
- XUFXOAAUWZOOIT-SXARVLRPSA-N (2R,3R,4R,5S,6R)-5-[[(2R,3R,4R,5S,6R)-5-[[(2R,3R,4S,5S,6R)-3,4-dihydroxy-6-methyl-5-[[(1S,4R,5S,6S)-4,5,6-trihydroxy-3-(hydroxymethyl)-1-cyclohex-2-enyl]amino]-2-oxanyl]oxy]-3,4-dihydroxy-6-(hydroxymethyl)-2-oxanyl]oxy]-6-(hydroxymethyl)oxane-2,3,4-triol Chemical compound O([C@H]1O[C@H](CO)[C@H]([C@@H]([C@H]1O)O)O[C@H]1O[C@@H]([C@H]([C@H](O)[C@H]1O)N[C@@H]1[C@@H]([C@@H](O)[C@H](O)C(CO)=C1)O)C)[C@@H]1[C@@H](CO)O[C@@H](O)[C@H](O)[C@H]1O XUFXOAAUWZOOIT-SXARVLRPSA-N 0.000 claims 1
- QJLPWVUZFKETMK-LLVKDONJSA-N (5r)-1,5,7,9,11,14-hexahydroxy-3-methyl-8,13-dioxo-5,6-dihydrobenzo[a]tetracene-2-carboxylic acid Chemical compound O=C1C2=C(O)C=C(O)C=C2C(=O)C2=C1C(O)=C1C[C@@H](O)C(C=C(C(=C3O)C(O)=O)C)=C3C1=C2O QJLPWVUZFKETMK-LLVKDONJSA-N 0.000 claims 1
- BOVGTQGAOIONJV-BETUJISGSA-N 1-[(3ar,6as)-3,3a,4,5,6,6a-hexahydro-1h-cyclopenta[c]pyrrol-2-yl]-3-(4-methylphenyl)sulfonylurea Chemical compound C1=CC(C)=CC=C1S(=O)(=O)NC(=O)NN1C[C@H]2CCC[C@H]2C1 BOVGTQGAOIONJV-BETUJISGSA-N 0.000 claims 1
- MVDXXGIBARMXSA-PYUWXLGESA-N 5-[[(2r)-2-benzyl-3,4-dihydro-2h-chromen-6-yl]methyl]-1,3-thiazolidine-2,4-dione Chemical compound S1C(=O)NC(=O)C1CC1=CC=C(O[C@@H](CC=2C=CC=CC=2)CC2)C2=C1 MVDXXGIBARMXSA-PYUWXLGESA-N 0.000 claims 1
- 108010070305 AOD 9604 Proteins 0.000 claims 1
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- 208000024827 Alzheimer disease Diseases 0.000 claims 1
- 206010002383 Angina Pectoris Diseases 0.000 claims 1
- 102000018616 Apolipoproteins B Human genes 0.000 claims 1
- 108010027006 Apolipoproteins B Proteins 0.000 claims 1
- 201000001320 Atherosclerosis Diseases 0.000 claims 1
- 206010007559 Cardiac failure congestive Diseases 0.000 claims 1
- 208000002177 Cataract Diseases 0.000 claims 1
- 208000028698 Cognitive impairment Diseases 0.000 claims 1
- 208000011231 Crohn disease Diseases 0.000 claims 1
- 208000007342 Diabetic Nephropathies Diseases 0.000 claims 1
- 208000032131 Diabetic Neuropathies Diseases 0.000 claims 1
- 206010012689 Diabetic retinopathy Diseases 0.000 claims 1
- 208000005189 Embolism Diseases 0.000 claims 1
- 208000010228 Erectile Dysfunction Diseases 0.000 claims 1
- HTQBXNHDCUEHJF-XWLPCZSASA-N Exenatide Chemical compound C([C@@H](C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CCC(O)=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](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)NCC(=O)NCC(=O)N1[C@@H](CCC1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CO)C(=O)NCC(=O)N[C@@H](C)C(=O)N1[C@@H](CCC1)C(=O)N1[C@@H](CCC1)C(=O)N1[C@@H](CCC1)C(=O)N[C@@H](CO)C(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CCSC)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)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)CNC(=O)[C@@H](N)CC=1NC=NC=1)[C@@H](C)O)[C@@H](C)O)C(C)C)C1=CC=CC=C1 HTQBXNHDCUEHJF-XWLPCZSASA-N 0.000 claims 1
- 102100033839 Glucose-dependent insulinotropic receptor Human genes 0.000 claims 1
- 206010019280 Heart failures Diseases 0.000 claims 1
- 101000996752 Homo sapiens Glucose-dependent insulinotropic receptor Proteins 0.000 claims 1
- 206010060378 Hyperinsulinaemia Diseases 0.000 claims 1
- 206010020772 Hypertension Diseases 0.000 claims 1
- 208000022559 Inflammatory bowel disease Diseases 0.000 claims 1
- 206010022489 Insulin Resistance Diseases 0.000 claims 1
- 206010022562 Intermittent claudication Diseases 0.000 claims 1
- XEEYBQQBJWHFJM-UHFFFAOYSA-N Iron Chemical compound [Fe] XEEYBQQBJWHFJM-UHFFFAOYSA-N 0.000 claims 1
- 208000032382 Ischaemic stroke Diseases 0.000 claims 1
- 208000007976 Ketosis Diseases 0.000 claims 1
- 208000007177 Left Ventricular Hypertrophy Diseases 0.000 claims 1
- 102000016267 Leptin Human genes 0.000 claims 1
- 108010092277 Leptin Proteins 0.000 claims 1
- YSDQQAXHVYUZIW-QCIJIYAXSA-N Liraglutide Chemical compound C([C@@H](C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(O)=O)C(=O)NCC(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCC)C(O)=O)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CC=1C=CC=CC=1)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](CCCNC(N)=N)C(=O)NCC(=O)N[C@@H](CCCNC(N)=N)C(=O)NCC(O)=O)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=1NC=NC=1)[C@@H](C)O)[C@@H](C)O)C(C)C)C1=CC=C(O)C=C1 YSDQQAXHVYUZIW-QCIJIYAXSA-N 0.000 claims 1
- 108010019598 Liraglutide Proteins 0.000 claims 1
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- IBAQFPQHRJAVAV-ULAWRXDQSA-N Miglitol Chemical compound OCCN1C[C@H](O)[C@@H](O)[C@H](O)[C@H]1CO IBAQFPQHRJAVAV-ULAWRXDQSA-N 0.000 claims 1
- 208000001132 Osteoporosis Diseases 0.000 claims 1
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- 208000018262 Peripheral vascular disease Diseases 0.000 claims 1
- QJLPWVUZFKETMK-UHFFFAOYSA-N Pradimicin Q Natural products O=C1C2=C(O)C=C(O)C=C2C(=O)C2=C1C(O)=C1CC(O)C(C=C(C(=C3O)C(O)=O)C)=C3C1=C2O QJLPWVUZFKETMK-UHFFFAOYSA-N 0.000 claims 1
- 206010036618 Premenstrual syndrome Diseases 0.000 claims 1
- 208000006011 Stroke Diseases 0.000 claims 1
- JLRGJRBPOGGCBT-UHFFFAOYSA-N Tolbutamide Chemical compound CCCCNC(=O)NS(=O)(=O)C1=CC=C(C)C=C1 JLRGJRBPOGGCBT-UHFFFAOYSA-N 0.000 claims 1
- 208000032109 Transient ischaemic attack Diseases 0.000 claims 1
- 229930186167 Trestatin Natural products 0.000 claims 1
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- FZNCGRZWXLXZSZ-CIQUZCHMSA-N Voglibose Chemical compound OCC(CO)N[C@H]1C[C@](O)(CO)[C@@H](O)[C@H](O)[C@H]1O FZNCGRZWXLXZSZ-CIQUZCHMSA-N 0.000 claims 1
- IMIPDPVHGGHVNH-YWVHRCQQSA-N [(8r,9s,13s,14s)-13-methyl-17-oxo-7,8,9,11,12,14,15,16-octahydro-6h-cyclopenta[a]phenanthren-3-yl] (z)-octadec-9-enoate Chemical compound C1C[C@]2(C)C(=O)CC[C@H]2[C@@H]2CCC3=CC(OC(=O)CCCCCCC\C=C/CCCCCCCC)=CC=C3[C@H]21 IMIPDPVHGGHVNH-YWVHRCQQSA-N 0.000 claims 1
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- 229960001466 acetohexamide Drugs 0.000 claims 1
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- 125000000217 alkyl group Chemical group 0.000 claims 1
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- OZVBMTJYIDMWIL-AYFBDAFISA-N bromocriptine Chemical compound C1=CC(C=2[C@H](N(C)C[C@@H](C=2)C(=O)N[C@]2(C(=O)N3[C@H](C(N4CCC[C@H]4[C@]3(O)O2)=O)CC(C)C)C(C)C)C2)=C3C2=C(Br)NC3=C1 OZVBMTJYIDMWIL-AYFBDAFISA-N 0.000 claims 1
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Families Citing this family (79)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2399914A4 (en) * | 2009-02-18 | 2012-08-29 | Takeda Pharmaceutical | FUSED HETEROCYCLIC CORE COMPOUND |
| AU2010264720A1 (en) | 2009-06-24 | 2011-12-08 | Boehringer Ingelheim International Gmbh | New compounds, pharmaceutical composition and methods relating thereto |
| AR077214A1 (es) * | 2009-06-24 | 2011-08-10 | Neurocrine Biosciences Inc | Heterociclos nitrogenados y composiciones farmaceuticas que los contienen |
| EP2547339A1 (en) | 2010-03-18 | 2013-01-23 | Boehringer Ingelheim International GmbH | Combination of a gpr119 agonist and the dpp-iv inhibitor linagliptin for use in the treatment of diabetes and related conditions |
| DK2547679T3 (en) | 2010-03-19 | 2016-01-11 | Pfizer | 2,3 dihydro-1H-inden-1-yl-2,7-diazaspiro [3.6] nonane derivatives and their use as antagonists or inverse agonists of ghrelin receptor |
| WO2012025811A1 (en) | 2010-08-23 | 2012-03-01 | Lupin Limited | Indolylpyrimidines as modulators of gpr119 |
| ES2546465T3 (es) | 2010-10-29 | 2015-09-23 | Pfizer Inc | Inhibidores de N1/N2-lactama acetil-CoA carboxilasa |
| WO2012069917A1 (en) | 2010-11-26 | 2012-05-31 | Lupin Limited | Bicyclic gpr119 modulators |
| AU2012245996B2 (en) | 2011-04-22 | 2016-09-01 | Pfizer Inc. | Pyrazolospiroketone derivatives for use as acetyl-CoA carboxylase inhibitors |
| CA2836487A1 (en) | 2011-06-09 | 2012-12-13 | Rhizen Pharmaceuticals Sa | Novel compounds as modulators of gpr-119 |
| JP2014520879A (ja) | 2011-07-15 | 2014-08-25 | ファイザー・インク | Ｇｐｒ１１９調節因子 |
| US8927577B2 (en) | 2011-07-22 | 2015-01-06 | Pfizer Inc. | Quinolinyl glucagon receptor modulators |
| CN103917529B (zh) | 2011-11-11 | 2016-08-17 | 辉瑞大药厂 | 2-硫代嘧啶酮类 |
| EA201400990A1 (ru) | 2012-04-06 | 2015-01-30 | Пфайзер Инк. | Ингибиторы диацилглицеринацилтрансферазы 2 |
| US8889730B2 (en) | 2012-04-10 | 2014-11-18 | Pfizer Inc. | Indole and indazole compounds that activate AMPK |
| WO2013164730A1 (en) | 2012-05-04 | 2013-11-07 | Pfizer Inc. | Heterocyclic substituted hexahydropyrano [3,4-d] [1,3] thiazin- 2 -amine compounds as inhibitors of app, bace1 and bace 2. |
| HK1210825A1 (en) | 2012-07-11 | 2016-05-06 | Elcelyx Therapeutics, Inc. | Compositions comprising statins, biguanides and further agents for reducing cardiometabolic risk |
| EP2897964A1 (en) | 2012-09-20 | 2015-07-29 | Pfizer Inc. | Alkyl-substituted hexahydropyrano [3,4-d][1,3]thiazin-2-amine compounds |
| EP2931731A1 (en) | 2012-12-11 | 2015-10-21 | Pfizer Inc. | Hexahydropyrano [3,4-d][1,3]thiazin-2-amine compounds as inhibitors of bace1 |
| US9403846B2 (en) | 2012-12-19 | 2016-08-02 | Pfizer Inc. | Carbocyclic- and heterocyclic-substituted hexahydropyrano[3,4-d][1,3]thiazin-2-amine compounds |
| EP2956458B1 (en) | 2013-02-13 | 2017-08-09 | Pfizer Inc | Heteroaryl-substituted hexahydropyrano[3,4-d][1,3]thiazin-2-amine compounds |
| US9233981B1 (en) | 2013-02-15 | 2016-01-12 | Pfizer Inc. | Substituted phenyl hexahydropyrano[3,4-d][1,3]thiazin-2-amine compounds |
| EP2813505A1 (en) | 2013-06-14 | 2014-12-17 | Asceneuron SA | Tetraaza-cyclopenta[a]indenyl derivatives |
| CA2926568C (en) | 2013-10-09 | 2017-09-05 | Pfizer Inc. | Antagonists of prostaglandin ep3 receptor |
| LT3119757T (lt) | 2014-03-17 | 2018-07-10 | Pfizer Inc. | Diacilglicerolio aciltransferazės 2 inhibitoriai, skirti panaudoti metabolinių ir susijusių ligų gydyme |
| DK3126330T3 (en) | 2014-04-04 | 2019-04-23 | Pfizer | BICYCLE-FUSED HETEROARYL OR ARYL COMPOUNDS AND USE THEREOF AS IRAC4 INHIBITORS |
| CN106459088A (zh) | 2014-04-10 | 2017-02-22 | 辉瑞公司 | 2‑氨基‑6‑甲基‑4，4a，5，6‑四氢吡喃并[3，4‑d][1，3]噻嗪‑8a(8H)‑基‑1，3‑噻唑‑4‑基酰胺 |
| WO2016092413A1 (en) | 2014-12-10 | 2016-06-16 | Pfizer Inc. | Indole and indazole compounds that activate ampk |
| EP3237401B1 (en) | 2014-12-22 | 2019-03-06 | Pfizer Inc | Antagonists of prostaglandin ep3 receptor |
| AU2016257179A1 (en) | 2015-05-05 | 2017-11-02 | Pfizer Inc. | 2-thiopyrimidinones |
| US10308615B2 (en) | 2015-05-29 | 2019-06-04 | Pfizer Inc. | Heterocyclic compounds as inhibitors of Vanin-1 enzyme |
| CN107787322B (zh) | 2015-06-17 | 2023-07-07 | 辉瑞大药厂 | 三环化合物以及它们作为磷酸二酯酶抑制剂的用途 |
| WO2016203335A1 (en) | 2015-06-18 | 2016-12-22 | Pfizer Inc. | Novel pyrido[2,3-b]pyrazinones as bet-family bromodomain inhibitors |
| WO2017025849A1 (en) | 2015-08-13 | 2017-02-16 | Pfizer Inc. | Bicyclic-fused heteroaryl or aryl compounds |
| HUE053705T2 (hu) | 2015-08-27 | 2021-07-28 | Pfizer | Biciklusos kondenzált heteroaril- vagy aril- vegyületek IRAK4 modulátorokként |
| WO2017037567A1 (en) | 2015-09-03 | 2017-03-09 | Pfizer Inc. | Regulators of frataxin |
| JP2018534251A (ja) | 2015-09-24 | 2018-11-22 | ファイザー・インク | Ｂａｃｅ阻害剤として有用なｎ−［２−（３−アミノ−２，５−ジメチル−１，１−ジオキシド−５，６−ジヒドロ−２ｈ−１，２，４−チアジアジン−５−イル）−１，３−チアゾール−４−イル］アミド |
| WO2017051303A1 (en) | 2015-09-24 | 2017-03-30 | Pfizer Inc. | Tetrahydropyrano[3,4-d][1,3]oxazin derivatives and their use as bace inhibitors |
| JP2018531923A (ja) | 2015-09-24 | 2018-11-01 | ファイザー・インク | Ｎ−［２−（２−アミノ−６，６−二置換−４，４ａ，５，６−テトラヒドロピラノ［３，４−ｄ］［１，３］チアジン−８ａ（８Ｈ）−イル）−１，３−チアゾール−４−イル］アミド |
| SI3397631T1 (sl) | 2015-12-29 | 2022-01-31 | Pfizer Inc. | Substituirani 3-azabiciklo(3.1.0)heksani kot zaviralci ketoheksokinaze |
| WO2018011681A1 (en) | 2016-07-14 | 2018-01-18 | Pfizer Inc. | Novel pyrimidine carboxamides as inhibitors of vanin-1 enzyme |
| AR109179A1 (es) | 2016-08-19 | 2018-11-07 | Pfizer | Inhibidores de diacilglicerol aciltransferasa 2 |
| WO2019133445A1 (en) | 2017-12-28 | 2019-07-04 | Inception Ibd, Inc. | Aminothiazoles as inhibitors of vanin-1 |
| US11254660B2 (en) | 2018-08-31 | 2022-02-22 | Pfizer Inc. | Combinations for treatment of NASH/NAFLD and related diseases |
| WO2020102575A1 (en) | 2018-11-16 | 2020-05-22 | Inception Ibd, Inc. | Heterocyclic aminothiazoles and uses thereof |
| WO2020234726A1 (en) | 2019-05-20 | 2020-11-26 | Pfizer Inc. | Combinations comprising benzodioxol as glp-1r agonists for use in the treatment of nash/nafld and related diseases |
| TW202115086A (zh) | 2019-06-28 | 2021-04-16 | 美商輝瑞大藥廠 | Bckdk抑制劑 |
| WO2020261144A1 (en) | 2019-06-28 | 2020-12-30 | Pfizer Inc. | 5-(thiophen-2-yl)-1h-tetrazole derivatives as bckdk inhibitors useful for treating various diseases |
| TWI771766B (zh) | 2019-10-04 | 2022-07-21 | 美商輝瑞股份有限公司 | 二醯基甘油醯基轉移酶２ 抑制劑 |
| HRP20241159T1 (hr) | 2020-02-07 | 2024-12-06 | Gasherbrum Bio, Inc. | Heterociklički agonisti za glp-1 |
| JP2022058085A (ja) | 2020-02-24 | 2022-04-11 | ファイザー・インク | ジアシルグリセロールアシルトランスフェラーゼ２阻害剤とアセチル－ＣｏＡカルボキシラーゼ阻害剤との組合せ |
| TW202140440A (zh) | 2020-02-28 | 2021-11-01 | 美商克力歐普股份有限公司 | Gpr40激動劑 |
| TW202206429A (zh) | 2020-04-29 | 2022-02-16 | 美商迦舒布魯姆生物有限公司 | 雜環ｇｌｐ—１促效劑 |
| WO2021236617A1 (en) | 2020-05-19 | 2021-11-25 | Kallyope, Inc. | Ampk activators |
| JP7288554B1 (ja) | 2020-06-09 | 2023-06-07 | ファイザー・インク | メラノコルチン４受容体アンタゴニストとしてのスピロ化合物およびそれらの使用 |
| CN116390925A (zh) | 2020-06-26 | 2023-07-04 | 卡尔优普公司 | Ampk活化剂 |
| US20250066337A1 (en) | 2021-08-26 | 2025-02-27 | Pfizer Inc. | Amorphous Form of (S)-2-(5-((3-Ethoxypyridin-2-YL)Oxy)Pyridin-3-YL)-N-(Tetrahydrofuran-3-YL)Pyrimidine-5-Carboxamide |
| CA3240990A1 (en) | 2021-12-01 | 2023-06-08 | Pfizer Inc. | 3-phenyl-1-benzothiophene-2-carboxylic acid derivatives as branched-chain alpha keto acid dehydrogenase kinase inhibitors for the treatment of diabetes, kidney diseases, nash and heart failure |
| JP2024544021A (ja) | 2021-12-06 | 2024-11-26 | ファイザー・インク | メラノコルチン４受容体アンタゴニストおよびそれらの使用 |
| JP2025509281A (ja) | 2022-03-09 | 2025-04-11 | ガシャーブラム・バイオ・インコーポレイテッド | ヘテロ環式ｇｌｐ－１アゴニスト |
| US20250250269A1 (en) | 2022-04-14 | 2025-08-07 | Gasherbrum Bio, Inc. | Heterocyclic glp-1 agonists |
| KR20250075705A (ko) | 2022-10-07 | 2025-05-28 | 화이자 인코포레이티드 | Hsd17b13 억제제 및/또는 분해제 |
| AU2023364628A1 (en) | 2022-10-18 | 2025-04-03 | Pfizer Inc. | Patatin-like phospholipase domain-containing protein 3 (pnpla3) modifiers |
| WO2024118524A1 (en) | 2022-11-28 | 2024-06-06 | Cerevel Therapeutics, Llc | Azaindole compounds and their use as phosphodiesterase inhibitors |
| TW202435857A (zh) | 2022-12-15 | 2024-09-16 | 美商迦舒布魯姆生物有限公司 | 具有glp-1促效劑活性之化合物之鹽及固體形式 |
| EP4634169A1 (en) | 2022-12-16 | 2025-10-22 | Pfizer Inc. | 3-fluoro-4-hydroxybenzmide-containing inhibitors and/or degraders and uses thereof |
| EP4695226A1 (en) | 2023-04-14 | 2026-02-18 | Pfizer Inc. | Glucose-dependent insulinotropic polypeptide receptor antagonists and uses thereof |
| WO2025099566A1 (en) | 2023-11-08 | 2025-05-15 | Pfizer Inc. | A crystalline form of 6-fluoro-3-(2,4,5-trifluoro-3-methoxyphenyl)-1-benzothiophene-2-carboxylic acid |
| TW202539633A (zh) | 2024-02-01 | 2025-10-16 | 美商輝瑞股份有限公司 | 葡萄糖依賴性促胰島素多肽受體拮抗劑及其用途 |
| US20250326741A1 (en) | 2024-04-22 | 2025-10-23 | Pfizer Inc. | Glucose-dependent insulinotropic polypeptide receptor antagonists and uses thereof |
| WO2026013531A1 (en) | 2024-07-10 | 2026-01-15 | Pfizer Inc. | Spiro[2.5]octane compounds |
| WO2026033382A1 (en) | 2024-08-07 | 2026-02-12 | Pfizer Inc. | Heterocyclic glp-1r modulators |
| WO2026042018A1 (en) | 2024-08-21 | 2026-02-26 | Pfizer Inc. | 4-{4-[(1-{[4-(propan-2-yl)phenyl]carbamoyl)-d-prolyl)amino]cyclohexyl}benzoic acid derivatives as gipr antagonists for the treatment of diabetes |
| WO2026078617A1 (en) | 2024-10-11 | 2026-04-16 | Pfizer Inc. | Glucose-dependent insulinotropic polypeptide receptor antagonists and uses thereof |
| WO2026078671A1 (en) | 2024-10-13 | 2026-04-16 | Pfizer Inc. | Heterocyclic compounds as glucose-dependent insulinotropic polypeptide receptor antagonists |
| WO2026078673A1 (en) | 2024-10-13 | 2026-04-16 | Pfizer Inc. | Glucose-dependent insulinotropic polypeptide receptor antagonists and uses thereof |
| WO2026078674A1 (en) | 2024-10-13 | 2026-04-16 | Pfizer Inc. | Heterocyclic derivatives as glucose-dependent insulinotropic polypeptide receptor antagonists and uses thereof |
| WO2026078670A1 (en) | 2024-10-13 | 2026-04-16 | Pfizer Inc. | Heterocyclic derivatives as glucose-dependent insulinotropic polypeptide receptor antagonists |
| WO2026078672A1 (en) | 2024-10-13 | 2026-04-16 | Pfizer Inc. | Glucose-dependent insulinotropic polypeptide receptor antagonists and uses thereof |
Family Cites Families (4)
| Publication number | Priority date | Publication date | Assignee | Title |
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| ES2388315T3 (es) * | 2007-05-04 | 2012-10-11 | Bristol-Myers Squibb Company | Agonistas [6,5]-bicíclicos de receptores GPR119 acoplados a la proteína G |
| AU2008312948C1 (en) * | 2007-10-16 | 2012-08-09 | Daiichi Sankyo Company, Limited | Pyrimidyl indoline compound |
| AR076024A1 (es) * | 2009-04-03 | 2011-05-11 | Schering Corp | Derivados de heterociclos biciclicos puenteados y metodos de uso de los mismos |
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2010
- 2010-04-12 US US13/318,152 patent/US20120052130A1/en not_active Abandoned
- 2010-04-12 EP EP10717259A patent/EP2427448A1/en not_active Withdrawn
- 2010-04-12 JP JP2012509115A patent/JP2012526096A/ja not_active Withdrawn
- 2010-04-12 WO PCT/IB2010/051567 patent/WO2010128414A1/en not_active Ceased
- 2010-04-12 CA CA2759891A patent/CA2759891A1/en not_active Abandoned
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