JP2016534124A5 - - Google Patents
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- JP2016534124A5 JP2016534124A5 JP2016537878A JP2016537878A JP2016534124A5 JP 2016534124 A5 JP2016534124 A5 JP 2016534124A5 JP 2016537878 A JP2016537878 A JP 2016537878A JP 2016537878 A JP2016537878 A JP 2016537878A JP 2016534124 A5 JP2016534124 A5 JP 2016534124A5
- Authority
- JP
- Japan
- Prior art keywords
- cancer
- compound
- alkyl
- use according
- thiazol
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Pending
Links
- 125000000217 alkyl group Chemical group 0.000 claims description 42
- 125000003118 aryl group Chemical group 0.000 claims description 17
- 229910052739 hydrogen Inorganic materials 0.000 claims description 15
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims description 14
- 229910052736 halogen Inorganic materials 0.000 claims description 11
- 150000002367 halogens Chemical class 0.000 claims description 11
- -1 alkylcyclopropane Chemical group 0.000 claims description 10
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 claims description 9
- FDDDEECHVMSUSB-UHFFFAOYSA-N Sulfanilamide Chemical compound NC1=CC=C(S(N)(=O)=O)C=C1 FDDDEECHVMSUSB-UHFFFAOYSA-N 0.000 claims description 8
- 229960001663 sulfanilamide Drugs 0.000 claims description 8
- 125000003545 alkoxy group Chemical group 0.000 claims description 7
- KXDHJXZQYSOELW-UHFFFAOYSA-M carbamate Chemical compound NC([O-])=O KXDHJXZQYSOELW-UHFFFAOYSA-M 0.000 claims description 7
- 150000001408 amides Chemical class 0.000 claims description 6
- GDTBXPJZTBHREO-UHFFFAOYSA-N bromine Substances BrBr GDTBXPJZTBHREO-UHFFFAOYSA-N 0.000 claims description 4
- WKBOTKDWSSQWDR-UHFFFAOYSA-N bromine atom Chemical compound [Br] WKBOTKDWSSQWDR-UHFFFAOYSA-N 0.000 claims description 4
- 150000001875 compounds Chemical class 0.000 claims 26
- 201000011510 cancer Diseases 0.000 claims 16
- 239000000203 mixture Substances 0.000 claims 15
- 201000010099 disease Diseases 0.000 claims 8
- 238000009472 formulation Methods 0.000 claims 8
- 208000008466 Metabolic Disease Diseases 0.000 claims 7
- 238000004519 manufacturing process Methods 0.000 claims 6
- 125000001997 phenyl group Chemical class [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 6
- JUJWROOIHBZHMG-UHFFFAOYSA-N pyridine Chemical compound C1=CC=NC=C1 JUJWROOIHBZHMG-UHFFFAOYSA-N 0.000 claims 6
- 239000000126 substance Substances 0.000 claims 6
- 206010062060 Hyperlipidaemia Diseases 0.000 claims 4
- 206010020772 Hypertension Diseases 0.000 claims 4
- 206010028980 Neoplasm Diseases 0.000 claims 4
- 101710038873 glc-1 Proteins 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
- 206010003210 Arteriosclerosis Diseases 0.000 claims 3
- 208000006673 Asthma Diseases 0.000 claims 3
- 206010060378 Hyperinsulinaemia Diseases 0.000 claims 3
- 206010022489 Insulin resistance Diseases 0.000 claims 3
- 241001465754 Metazoa Species 0.000 claims 3
- 208000008338 Non-alcoholic Fatty Liver Disease Diseases 0.000 claims 3
- 208000008589 Obesity Diseases 0.000 claims 3
- 208000001072 Type 2 Diabetes Mellitus Diseases 0.000 claims 3
- 239000003814 drug Substances 0.000 claims 3
- 230000003451 hyperinsulinaemic Effects 0.000 claims 3
- 201000008980 hyperinsulinism Diseases 0.000 claims 3
- 235000020824 obesity Nutrition 0.000 claims 3
- RWRDLPDLKQPQOW-UHFFFAOYSA-N pyrrolidine Chemical class C1CCNC1 RWRDLPDLKQPQOW-UHFFFAOYSA-N 0.000 claims 3
- 150000003839 salts Chemical class 0.000 claims 3
- 239000011780 sodium chloride Substances 0.000 claims 3
- 230000004580 weight loss Effects 0.000 claims 3
- 206010006187 Breast cancer Diseases 0.000 claims 2
- 210000004392 Genitalia Anatomy 0.000 claims 2
- 102000004877 Insulin Human genes 0.000 claims 2
- 108090001061 Insulin Proteins 0.000 claims 2
- 206010024324 Leukaemias Diseases 0.000 claims 2
- 206010025323 Lymphomas Diseases 0.000 claims 2
- 206010025650 Malignant melanoma Diseases 0.000 claims 2
- 206010027476 Metastasis Diseases 0.000 claims 2
- 102000015494 Mitochondrial Uncoupling Proteins Human genes 0.000 claims 2
- 108010050258 Mitochondrial Uncoupling Proteins Proteins 0.000 claims 2
- 206010025310 Other lymphomas Diseases 0.000 claims 2
- 206010060862 Prostate cancer Diseases 0.000 claims 2
- 206010039491 Sarcoma Diseases 0.000 claims 2
- 108010021111 Uncoupling Protein 2 Proteins 0.000 claims 2
- 102000008219 Uncoupling Protein 2 Human genes 0.000 claims 2
- 108010021098 Uncoupling Protein 3 Proteins 0.000 claims 2
- 102000008200 Uncoupling Protein 3 Human genes 0.000 claims 2
- 210000001635 Urinary Tract Anatomy 0.000 claims 2
- 230000002058 anti-hyperglycaemic Effects 0.000 claims 2
- 230000037396 body weight Effects 0.000 claims 2
- 201000005216 brain cancer Diseases 0.000 claims 2
- 229910052801 chlorine Inorganic materials 0.000 claims 2
- 230000003247 decreasing Effects 0.000 claims 2
- 239000003603 dipeptidyl peptidase IV inhibitor Substances 0.000 claims 2
- 229940079593 drugs Drugs 0.000 claims 2
- 229910052731 fluorine Inorganic materials 0.000 claims 2
- 230000002496 gastric Effects 0.000 claims 2
- 230000003463 hyperproliferative Effects 0.000 claims 2
- 201000007270 liver cancer Diseases 0.000 claims 2
- 239000000463 material Substances 0.000 claims 2
- 201000001441 melanoma Diseases 0.000 claims 2
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 2
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 2
- 239000008194 pharmaceutical composition Substances 0.000 claims 2
- 150000003222 pyridines Chemical class 0.000 claims 2
- 201000000849 skin cancer Diseases 0.000 claims 2
- 239000002904 solvent Substances 0.000 claims 2
- FZWLAAWBMGSTSO-UHFFFAOYSA-N thiazole Chemical class C1=CSC=N1 FZWLAAWBMGSTSO-UHFFFAOYSA-N 0.000 claims 2
- 150000003557 thiazoles Chemical class 0.000 claims 2
- 201000002510 thyroid cancer Diseases 0.000 claims 2
- ZOBPZXTWZATXDG-UHFFFAOYSA-N 1,3-thiazolidine-2,4-dione Chemical compound O=C1CSC(=O)N1 ZOBPZXTWZATXDG-UHFFFAOYSA-N 0.000 claims 1
- 125000003903 2-propenyl group Chemical group [H]C([*])([H])C([H])=C([H])[H] 0.000 claims 1
- LNGSFISRULVTBP-UHFFFAOYSA-N 4-(4-bromophenyl)-2-(1-propylpyrrolidin-2-yl)-1,3-thiazole Chemical compound CCCN1CCCC1C1=NC(C=2C=CC(Br)=CC=2)=CS1 LNGSFISRULVTBP-UHFFFAOYSA-N 0.000 claims 1
- DLGJFRDAHDCSFE-UHFFFAOYSA-N 4-(4-bromophenyl)-2-pyrrolidin-2-yl-1,3-thiazole Chemical compound C1=CC(Br)=CC=C1C1=CSC(C2NCCC2)=N1 DLGJFRDAHDCSFE-UHFFFAOYSA-N 0.000 claims 1
- SWILVVHJWOGIQP-UHFFFAOYSA-N 4-methyl-N-[4-[4-[(1-methylbenzimidazol-2-yl)methyl]piperazin-1-yl]phenyl]benzenesulfonamide Chemical compound C1=CC(C)=CC=C1S(=O)(=O)NC1=CC=C(N2CCN(CC=3N(C4=CC=CC=C4N=3)C)CC2)C=C1 SWILVVHJWOGIQP-UHFFFAOYSA-N 0.000 claims 1
- 206010012601 Diabetes mellitus Diseases 0.000 claims 1
- 208000004930 Fatty Liver Diseases 0.000 claims 1
- 210000003128 Head Anatomy 0.000 claims 1
- 206010019708 Hepatic steatosis Diseases 0.000 claims 1
- ZJHLLODKYOJMLY-UHFFFAOYSA-N N-(4-formylphenyl)-4-methylbenzenesulfonamide Chemical compound C1=CC(C)=CC=C1S(=O)(=O)NC1=CC=C(C=O)C=C1 ZJHLLODKYOJMLY-UHFFFAOYSA-N 0.000 claims 1
- 230000003542 behavioural Effects 0.000 claims 1
- 229940090129 blood glucose lowering drugs Thiazolidinediones Drugs 0.000 claims 1
- 229910052794 bromium Inorganic materials 0.000 claims 1
- 230000037213 diet Effects 0.000 claims 1
- 235000005911 diet Nutrition 0.000 claims 1
- 238000002651 drug therapy Methods 0.000 claims 1
- 201000010238 heart disease Diseases 0.000 claims 1
- 125000001160 methoxycarbonyl group Chemical group [H]C([H])([H])OC(*)=O 0.000 claims 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 1
- 125000000325 methylidene group Chemical group [H]C([H])=* 0.000 claims 1
- 125000000896 monocarboxylic acid group Chemical group 0.000 claims 1
- 125000004123 n-propyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])* 0.000 claims 1
- 229910052757 nitrogen Inorganic materials 0.000 claims 1
- 230000000849 parathyroid Effects 0.000 claims 1
- 239000000546 pharmaceutic aid Substances 0.000 claims 1
- 238000000554 physical therapy Methods 0.000 claims 1
- GLUUGHFHXGJENI-UHFFFAOYSA-N piperazine Chemical class C1CNCCN1 GLUUGHFHXGJENI-UHFFFAOYSA-N 0.000 claims 1
- 150000004885 piperazines Chemical class 0.000 claims 1
- NQRYJNQNLNOLGT-UHFFFAOYSA-N piperidine Chemical class C1CCNCC1 NQRYJNQNLNOLGT-UHFFFAOYSA-N 0.000 claims 1
- 150000003053 piperidines Chemical class 0.000 claims 1
- 150000003235 pyrrolidines Chemical class 0.000 claims 1
- 231100000240 steatosis hepatitis Toxicity 0.000 claims 1
- 238000001356 surgical procedure Methods 0.000 claims 1
- 238000002560 therapeutic procedure Methods 0.000 claims 1
- PMKIYXFOEJFWIC-UHFFFAOYSA-N thiatetrazole Chemical group N=1N=NSN=1 PMKIYXFOEJFWIC-UHFFFAOYSA-N 0.000 claims 1
- 150000000008 thiatetrazoles Chemical class 0.000 claims 1
- 150000001467 thiazolidinediones Chemical class 0.000 claims 1
- 201000005161 thyroid carcinoma Diseases 0.000 claims 1
- 125000001424 substituent group Chemical group 0.000 description 3
Applications Claiming Priority (7)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US14/013,918 | 2013-08-29 | ||
| US14/013,918 US9085566B2 (en) | 2007-02-02 | 2013-08-29 | Compositions and methods for the treatment of metabolic and related disorders |
| US14/052,074 | 2013-10-11 | ||
| US14/052,074 US9187485B2 (en) | 2007-02-02 | 2013-10-11 | Methods and compositions for the treatment of cancer and related hyperproliferative disorders |
| US14/270,130 | 2014-05-05 | ||
| US14/270,130 US9233941B2 (en) | 2007-02-02 | 2014-05-05 | Methods and compositions for the treatment of body weight related disorders |
| PCT/US2014/053334 WO2015031710A1 (en) | 2013-08-29 | 2014-08-29 | Compositions and methods for the treatment of metabolic and body weight related disorders |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2016534124A JP2016534124A (ja) | 2016-11-04 |
| JP2016534124A5 true JP2016534124A5 (pl) | 2017-10-12 |
Family
ID=52587357
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016537878A Pending JP2016534124A (ja) | 2013-08-29 | 2014-08-29 | 代謝並びに体重関連疾患の処置のための組成物および方法 |
Country Status (6)
| Country | Link |
|---|---|
| EP (1) | EP3039022A4 (pl) |
| JP (1) | JP2016534124A (pl) |
| CN (1) | CN107074839A (pl) |
| AU (1) | AU2014312227A1 (pl) |
| CA (1) | CA2922703A1 (pl) |
| WO (1) | WO2015031710A1 (pl) |
Families Citing this family (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US10328064B2 (en) | 2014-12-23 | 2019-06-25 | Fgh Biotech, Inc. | Compositions of fatostatin based heterocyclic compounds and uses thereof |
| MX2018013221A (es) | 2016-04-29 | 2019-06-24 | Fgh Biotech Inc | Compuestos de pirazol disustituidos para el tratamiento de enfermedades. |
| WO2018049080A1 (en) * | 2016-09-07 | 2018-03-15 | Fgh Biotech, Inc. | Di-substituted pyrazole compounds for the treatment of diseases |
| CN108727295B (zh) * | 2018-06-21 | 2022-04-01 | 济南大学 | 一种2-(3-氨基苯基)-苯并噻唑衍生物及其制备方法和用途 |
| TWI722503B (zh) | 2018-07-24 | 2021-03-21 | 南韓商普洛科技股份有限公司 | 新穎的autotac嵌合化合物及包含其之用於透過經靶定之蛋白質降解來預防、改善或治療疾病的組成物 |
| CN113631163A (zh) * | 2019-01-28 | 2021-11-09 | 卡普勒斯疗法有限责任公司 | 包括噻吩中心环的srebp抑制剂 |
| CN114945365A (zh) * | 2019-11-13 | 2022-08-26 | 卡普勒斯疗法有限责任公司 | 包括噻吩中心环的srebp抑制剂 |
| WO2021154735A1 (en) * | 2020-01-27 | 2021-08-05 | Capulus Therapeutics, Llc | Srebp inhibitors comprising a thiophene central ring |
| TWI794742B (zh) | 2020-02-18 | 2023-03-01 | 美商基利科學股份有限公司 | 抗病毒化合物 |
| US12030903B2 (en) | 2020-02-18 | 2024-07-09 | Gilead Sciences, Inc. | Antiviral compounds |
| TWI775313B (zh) | 2020-02-18 | 2022-08-21 | 美商基利科學股份有限公司 | 抗病毒化合物 |
| CA3216162A1 (en) | 2021-04-16 | 2022-10-20 | Gilead Sciences, Inc. | Methods of preparing carbanucleosides using amides |
Family Cites Families (25)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4153703A (en) * | 1977-06-30 | 1979-05-08 | Uniroyal, Inc. | Method of controlling insects and acarids with certain aryl-substituted thiazoles |
| DK0934937T3 (da) * | 1990-11-30 | 2002-04-02 | Otsuka Pharma Co Ltd | Azolderivater som superoxidradikalinhibitor |
| CA2523808A1 (en) * | 2003-05-16 | 2004-12-23 | Ambit Biosciences Corporation | Pyrrole compounds and uses thereof |
| WO2005044194A2 (en) * | 2003-10-28 | 2005-05-19 | Pharmacia Corporation | TREATMENT OR PREVENTION OF NEOPLASIA BY USE OF AN Hsp90 INHIBITOR |
| TW200633990A (en) * | 2004-11-18 | 2006-10-01 | Takeda Pharmaceuticals Co | Amide compound |
| WO2007005785A1 (en) * | 2005-07-04 | 2007-01-11 | Dr. Reddy's Laboratories Ltd. | Thiazoles derivatives as ampk activator |
| KR100997549B1 (ko) * | 2005-08-15 | 2010-11-30 | 에프. 호프만-라 로슈 아게 | Ｐ2ｘ3 길항제로서의 피페리딘 및 피페라진 유도체 |
| DE602006006712D1 (de) * | 2005-08-18 | 2009-06-18 | Hoffmann La Roche | Thiazolylpiperidin-derivate nützlich als h3 rezeptor modulatoren |
| WO2007052843A1 (ja) * | 2005-11-04 | 2007-05-10 | Takeda Pharmaceutical Company Limited | 複素環アミド化合物およびその用途 |
| CA2630920A1 (en) * | 2005-11-22 | 2007-05-31 | University Of South Florida | Inhibition of cell proliferation |
| SG133452A1 (en) * | 2005-12-30 | 2007-07-30 | Novartis Ag | Peptide deformylase inhibitors for treatment of mycobacterial and other parasitic diseases |
| GB0701426D0 (en) * | 2007-01-25 | 2007-03-07 | Univ Sheffield | Compounds and their use |
| EP2120580B1 (en) * | 2007-02-02 | 2017-12-27 | Baylor College Of Medicine | Compositions and methods for the treatment of metabolic disorders |
| MX2009013003A (es) * | 2007-06-01 | 2010-01-20 | Hoffmann La Roche | Derivados de piperidina-amida. |
| WO2009018844A1 (en) * | 2007-08-09 | 2009-02-12 | Oridis Biomed Forschungs- Und Entwicklungs Gmbh | Thiazole-piperidine derivatives for treatment of hyperproliferative diseases |
| DE102007040243A1 (de) * | 2007-08-25 | 2009-02-26 | Universität des Saarlandes | 17Beta-Hydroxysteriod-Dehydrogenase Typ1 Inhibitoren zur Behandlung hormonabhängiger Erkrankungen |
| WO2009055917A1 (en) * | 2007-11-02 | 2009-05-07 | Methylgene Inc. | Inhibitors of histone deacetylase |
| KR20100014090A (ko) * | 2008-08-01 | 2010-02-10 | 동화약품주식회사 | 벤즈아미딘 유도체 또는 이의 염, 및 비스포스포네이트를 포함하는 골다공증의 예방 또는 치료용 약학 조성물 |
| CA2743497A1 (en) * | 2008-11-19 | 2010-05-27 | Schering Corporation | Inhibitors of diacylglycerol acyltransferase |
| WO2010090716A1 (en) * | 2009-01-30 | 2010-08-12 | Millennium Pharmaceuticals, Inc. | Heteroaryls and their use as pi3k inhibitors |
| CN102802419A (zh) * | 2010-01-07 | 2012-11-28 | 西莱瑟根治疗公司 | 刺猬(hedgehog)抑制剂 |
| EP2523664A4 (en) * | 2010-01-13 | 2013-06-26 | Tempero Pharmaceuticals Inc | COMPOUNDS AND METHODS |
| MX2013002462A (es) * | 2010-09-03 | 2013-07-29 | Piramal Entpr Ltd | Compuestos heterociclicos como inhibidores de dgat1. |
| WO2012129562A2 (en) * | 2011-03-24 | 2012-09-27 | The Scripps Research Institute | Compounds and methods for inducing chondrogenesis |
| US20140364460A1 (en) * | 2012-01-18 | 2014-12-11 | The Trustees Of Columbia University In The City Of New York | USE OF FATOSTATIN FOR TREATING CANCER HAVING A p53 MUTATION |
-
2014
- 2014-08-29 CA CA2922703A patent/CA2922703A1/en not_active Abandoned
- 2014-08-29 EP EP14841043.4A patent/EP3039022A4/en not_active Withdrawn
- 2014-08-29 JP JP2016537878A patent/JP2016534124A/ja active Pending
- 2014-08-29 AU AU2014312227A patent/AU2014312227A1/en not_active Abandoned
- 2014-08-29 CN CN201480058587.XA patent/CN107074839A/zh active Pending
- 2014-08-29 WO PCT/US2014/053334 patent/WO2015031710A1/en active Application Filing
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