ES2393824T3 - Derivados de piridin-2-il-amino-1,2,4-tiadiazol como activadores de glucoquinasa para el tratamiento de diabetes mellitus - Google Patents
Derivados de piridin-2-il-amino-1,2,4-tiadiazol como activadores de glucoquinasa para el tratamiento de diabetes mellitus Download PDFInfo
- Publication number
- ES2393824T3 ES2393824T3 ES08834504T ES08834504T ES2393824T3 ES 2393824 T3 ES2393824 T3 ES 2393824T3 ES 08834504 T ES08834504 T ES 08834504T ES 08834504 T ES08834504 T ES 08834504T ES 2393824 T3 ES2393824 T3 ES 2393824T3
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- Prior art keywords
- alkyl
- ring
- independently selected
- optionally substituted
- nitrogen atoms
- 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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- BOQQUDFKYXJRGO-UHFFFAOYSA-N 5-pyridin-2-yl-1,2,4-thiadiazol-3-amine Chemical class NC1=NSC(C=2N=CC=CC=2)=N1 BOQQUDFKYXJRGO-UHFFFAOYSA-N 0.000 title 1
- 102000030595 Glucokinase Human genes 0.000 title 1
- 108010021582 Glucokinase Proteins 0.000 title 1
- 239000012190 activator Substances 0.000 title 1
- 206010012601 diabetes mellitus Diseases 0.000 title 1
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 19
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 abstract 10
- 125000004433 nitrogen atom Chemical group N* 0.000 abstract 6
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 abstract 3
- 125000000217 alkyl group Chemical group 0.000 abstract 3
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 3
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 2
- 125000005842 heteroatom Chemical group 0.000 abstract 2
- 229910052760 oxygen Inorganic materials 0.000 abstract 2
- 229910052717 sulfur Inorganic materials 0.000 abstract 2
- 125000006274 (C1-C3)alkoxy group Chemical group 0.000 abstract 1
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 abstract 1
- 125000003118 aryl group Chemical group 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 abstract 1
- 125000001072 heteroaryl group Chemical group 0.000 abstract 1
- 239000001257 hydrogen Substances 0.000 abstract 1
- 229910052739 hydrogen Inorganic materials 0.000 abstract 1
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 abstract 1
- 125000004170 methylsulfonyl group Chemical group [H]C([H])([H])S(*)(=O)=O 0.000 abstract 1
- 125000001624 naphthyl group Chemical group 0.000 abstract 1
- 229910052757 nitrogen Inorganic materials 0.000 abstract 1
- 125000004430 oxygen atom Chemical group O* 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
- C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
- C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D213/72—Nitrogen atoms
- C07D213/75—Amino or imino radicals, acylated by carboxylic or carbonic acids, or by sulfur or nitrogen analogues thereof, e.g. carbamates
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
- C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Diabetes (AREA)
- Public Health (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- General Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Obesity (AREA)
- Hematology (AREA)
- Endocrinology (AREA)
- Emergency Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Pyridine Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Abstract
Un compuesto de fórmula general I o una sal del mismo, en la que: R13 es un polihidroxi-alquilo (C2-6), metoxi (polihidroxi-alquilo (C3-6) ) o polihidroxi-cicloalquilo (C5-6); L es O o S; D2 es N o CH; R2 es Ar1, hetAr1, hetAr2 o hetAr3; Ar1 es fenilo o naftilo, cada uno de los cuales está opcionalmente sustituido con uno o más grupos seleccionados independientemente de entre alquilo (C1-6), F, Br, CF3, OH, CN, SO2Me, C (>=O) NH (alquilo C1-3) N (alquilo) 2 y C (>=O) NH (alquilo C1-3) hetCyc1; HetAr1 es un grupo heteroarilo de 5-6 miembros que tiene 1-3 átomos de nitrógeno en el anillo y opcionalmente sustituido con uno o más grupos seleccionados independientemente de entre (alquilo C1-6), Cl, CF3 y (alquilo C1-6) OH; HetAr2 es un sistema anillo heteroarilo bicíclico parcialmente insaturado 5, 6 o 6, 6 que tiene 1-2 átomos de nitrógeno en el anillo y que tiene opcionalmente un átomo de oxígeno en el anillo; HetAr3 es un anillo heteroarilo bicíclico de 9-10 miembros que tiene 1-3 átomos de nitrógeno en el anillo; R3 es Cl, Br, CF3, arilo, hetAra, SR6 u OR6; HetAra es un heteroarilo de 6 miembros que tiene 1-2 átomos de nitrógeno en el anillo; R6 es Ar2, hetAr4, (alquilo C1-6), - (alquilo C1-6) OH, polihidroxi (alquilo C1-6), -CH (R9) -Ar3, -CH (R10) -hetAr5, hetAr6, cicloalquilo (C5-6) sustituido con 1 a 4 OH, (alcoxi C1-3) (alquilo C1-6) o ciclopropil (alquilo C1-6); Ar2 es fenilo opcionalmente sustituido con uno o más grupos seleccionados independientemente de entre alquilo (C1-6), F, Br, Cl, CF3, CN, OH, O- (alquilo C1-6), C (>=O) OH, C (>=O) O (alquilo C1-6), C (>=O) NH (alquilo C1-3) N (alquilo C1-3) 2 y C (>=O) NH (alquilo C1-3) hetCyc2; HetAr4 es un anillo heteroarilo de 5-6 miembros que tiene 1-3 átomos de nitrógeno y opcionalmente sustituido con uno o más grupos seleccionados independientemente de entre alquilo (C1-6), F, Br, Cl, CF3, CN, OH, O- (alquilo C1-6), C (>=O) OH, C (>=O) O (alquilo C1-6), C (>=O) NH (alquilo C1-3) N (alquilo C1-3) 2 y C (>=O) NH (alquilo C1-3) hetCyc2; Ar3 es fenilo opcionalmente sustituido con uno o más grupos seleccionados independientemente de entre F, Cl, Br y alquilo (C1-6); HetAr5 es un heteroarilo de 5-6-miembros que tiene 1-2 átomos de nitrógeno en el anillo; HetAr6 es un anillo heteroaromático bicíclico de 9-10 miembros que tiene 2-3 heteroátomos seleccionados independientemente de entre N, S y O (a condición de que el anillo no contenga un enlace O-O) que está opcionalmente sustituido con uno o más grupos seleccionados independientemente de entre alquilo (C1-6), F, Br, Cl, CF3, CN, OH, -O- (alquilo C1-6), C (>=O) OH, C (>=O) O (alquilo C1-6) y C (>=O) NH (alquilo C1-3) N (alquilo C1-3) 2; R9 y R10 son independientemente hidrógeno, alquilo (C1-6), alquilo (C1-6) OH o CF3; y HetCyc1 y hetCyc2 son independientemente un anillo heterocíclico de 5-7 miembros que tiene 1-2 heteroátomos en el anillo seleccionados independientemente de entre N y O
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US97422507P | 2007-09-21 | 2007-09-21 | |
| US974225P | 2007-09-21 | ||
| PCT/US2008/076401 WO2009042435A1 (en) | 2007-09-21 | 2008-09-15 | Pyridin-2 -yl-amino-i, 2, 4 -thiadiazole derivatives as glucokinase activators for the treatment of diabetes mellitus |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ES2393824T3 true ES2393824T3 (es) | 2012-12-28 |
Family
ID=40250949
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ES08834504T Active ES2393824T3 (es) | 2007-09-21 | 2008-09-15 | Derivados de piridin-2-il-amino-1,2,4-tiadiazol como activadores de glucoquinasa para el tratamiento de diabetes mellitus |
| ES13186328.4T Active ES2569734T3 (es) | 2007-09-21 | 2008-09-15 | Derivados de piridin-2-il-tiourea y de piridin-2-il-amina como intermedios para la preparación de piridin-2-il-amino-1,2,4-tiadiazoles activadores de la glucocinasa |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ES13186328.4T Active ES2569734T3 (es) | 2007-09-21 | 2008-09-15 | Derivados de piridin-2-il-tiourea y de piridin-2-il-amina como intermedios para la preparación de piridin-2-il-amino-1,2,4-tiadiazoles activadores de la glucocinasa |
Country Status (28)
| Country | Link |
|---|---|
| US (3) | US8212045B2 (es) |
| EP (4) | EP3078662A1 (es) |
| JP (1) | JP5722037B2 (es) |
| KR (1) | KR101566042B1 (es) |
| CN (1) | CN101868459B (es) |
| AR (1) | AR068628A1 (es) |
| AU (1) | AU2008305294B2 (es) |
| BR (1) | BRPI0816881A2 (es) |
| CA (1) | CA2699718C (es) |
| CO (1) | CO6270223A2 (es) |
| CR (2) | CR11383A (es) |
| DK (1) | DK2209778T3 (es) |
| EA (1) | EA019104B1 (es) |
| ES (2) | ES2393824T3 (es) |
| HR (1) | HRP20120814T1 (es) |
| IL (1) | IL204264A (es) |
| MA (1) | MA31779B1 (es) |
| MX (1) | MX2010002772A (es) |
| MY (1) | MY180558A (es) |
| NZ (1) | NZ583538A (es) |
| PL (1) | PL2209778T3 (es) |
| PT (1) | PT2209778E (es) |
| SI (1) | SI2209778T1 (es) |
| TN (1) | TN2010000100A1 (es) |
| TW (1) | TWI423799B (es) |
| UA (1) | UA101166C2 (es) |
| WO (1) | WO2009042435A1 (es) |
| ZA (2) | ZA201002206B (es) |
Families Citing this family (21)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2131656A4 (en) * | 2006-11-15 | 2011-12-07 | Forest Lab Holdings Ltd | phthalazine |
| ES2393824T3 (es) | 2007-09-21 | 2012-12-28 | Array Biopharma, Inc. | Derivados de piridin-2-il-amino-1,2,4-tiadiazol como activadores de glucoquinasa para el tratamiento de diabetes mellitus |
| WO2011107494A1 (de) | 2010-03-03 | 2011-09-09 | Sanofi | Neue aromatische glykosidderivate, diese verbindungen enthaltende arzneimittel und deren verwendung |
| JP5909482B2 (ja) | 2010-03-31 | 2016-04-26 | ザ スクリプス リサーチ インスティテュート | 細胞の再プログラム |
| US8530413B2 (en) | 2010-06-21 | 2013-09-10 | Sanofi | Heterocyclically substituted methoxyphenyl derivatives with an oxo group, processes for preparation thereof and use thereof as medicaments |
| TW201221505A (en) | 2010-07-05 | 2012-06-01 | Sanofi Sa | Aryloxyalkylene-substituted hydroxyphenylhexynoic acids, process for preparation thereof and use thereof as a medicament |
| TW201215388A (en) | 2010-07-05 | 2012-04-16 | Sanofi Sa | (2-aryloxyacetylamino)phenylpropionic acid derivatives, processes for preparation thereof and use thereof as medicaments |
| TW201215387A (en) | 2010-07-05 | 2012-04-16 | Sanofi Aventis | Spirocyclically substituted 1,3-propane dioxide derivatives, processes for preparation thereof and use thereof as a medicament |
| JP2013536233A (ja) | 2010-08-23 | 2013-09-19 | アムジエン・インコーポレーテツド | グルコキナーゼ調節タンパク質と相互作用する糖尿病治療用の化合物 |
| EP2684878A4 (en) | 2011-03-09 | 2014-08-27 | Daiichi Sankyo Co Ltd | DIPYRIDYLAMINDERIVAT |
| WO2012138776A1 (en) | 2011-04-05 | 2012-10-11 | Amgen Inc. | Benzodioxepine and benzodioxine compounds that interact with glucokinase regulatory protein for the treatment of diabetes |
| WO2013037390A1 (en) | 2011-09-12 | 2013-03-21 | Sanofi | 6-(4-hydroxy-phenyl)-3-styryl-1h-pyrazolo[3,4-b]pyridine-4-carboxylic acid amide derivatives as kinase inhibitors |
| WO2013045413A1 (en) | 2011-09-27 | 2013-04-04 | Sanofi | 6-(4-hydroxy-phenyl)-3-alkyl-1h-pyrazolo[3,4-b]pyridine-4-carboxylic acid amide derivatives as kinase inhibitors |
| WO2013123444A1 (en) | 2012-02-17 | 2013-08-22 | Amgen Inc. | Sulfonyl compounds that interact with glucokinase regulatory protein |
| WO2013173382A1 (en) | 2012-05-15 | 2013-11-21 | Amgen Inc. | Benzothiophene sulfonamides and other compounds that interact with glucokinase regulatory protein |
| CN104736518B (zh) * | 2012-05-18 | 2017-10-13 | 安进股份有限公司 | 制备噻二唑的方法 |
| EP2917213A1 (en) * | 2012-11-09 | 2015-09-16 | Array Biopharma, Inc. | Crystalline forms of (1s)-1-[5-({3-[(2-methylpyridin-3-yl)oxy]-5-(pyridin-2-ylsulfanyl)pyridin-2-yl}amino)-1,2,4-thiadiazol-3-yl]ethane-1,2-diol |
| WO2016059647A2 (en) * | 2014-10-13 | 2016-04-21 | SHRI CHHATRAPTI SHIVAJI COLLEGE Maharashtra, India) | Triaminotriazine picolinonitrile derivatives as potent reverse transcriptase inhibitor of hiv-1 |
| GB201714777D0 (en) | 2017-09-14 | 2017-11-01 | Univ London Queen Mary | Agent |
| AU2018359224B2 (en) | 2017-10-30 | 2023-10-05 | Neuropore Therapies, Inc. | Substituted phenyl sulfonyl phenyl triazole thiones and uses thereof |
| DK3804716T3 (da) | 2018-05-31 | 2025-03-03 | Hua Medicine Shanghai Ltd | Farmaceutisk kombination, sammensætning og kombinationspræparat omfattende glucokinase-aktivator og sglt-2-inhibitor og fremgangsmåder til fremstilling og anvendelser deraf |
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