AR065495A1 - Metodos para usar derivados de bencimidazol para tratar o prevenir dolor, diabetes, complicacion diabetica composiciones. - Google Patents
Metodos para usar derivados de bencimidazol para tratar o prevenir dolor, diabetes, complicacion diabetica composiciones.Info
- Publication number
- AR065495A1 AR065495A1 ARP080100805A ARP080100805A AR065495A1 AR 065495 A1 AR065495 A1 AR 065495A1 AR P080100805 A ARP080100805 A AR P080100805A AR P080100805 A ARP080100805 A AR P080100805A AR 065495 A1 AR065495 A1 AR 065495A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- alkoxy
- aryl
- independently selected
- halo
- Prior art date
Links
- 239000000203 mixture Substances 0.000 title abstract 6
- 208000002249 Diabetes Complications Diseases 0.000 title abstract 2
- 206010012655 Diabetic complications Diseases 0.000 title abstract 2
- 206010012601 diabetes mellitus Diseases 0.000 title abstract 2
- 208000002193 Pain Diseases 0.000 title 1
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 27
- 125000005843 halogen group Chemical group 0.000 abstract 11
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 abstract 8
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 abstract 8
- 229910052739 hydrogen Inorganic materials 0.000 abstract 8
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 abstract 8
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 abstract 7
- 125000003710 aryl alkyl group Chemical group 0.000 abstract 7
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 7
- 229910052757 nitrogen Inorganic materials 0.000 abstract 7
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 abstract 6
- 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 abstract 6
- 125000001424 substituent group Chemical group 0.000 abstract 6
- 125000000217 alkyl group Chemical group 0.000 abstract 5
- 239000001257 hydrogen Substances 0.000 abstract 5
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 5
- 229910052799 carbon Inorganic materials 0.000 abstract 4
- 150000001875 compounds Chemical class 0.000 abstract 4
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 4
- 125000001153 fluoro group Chemical group F* 0.000 abstract 4
- 125000001072 heteroaryl group Chemical group 0.000 abstract 4
- 125000000876 trifluoromethoxy group Chemical group FC(F)(F)O* 0.000 abstract 4
- -1 C1-6-thio alkyl Chemical group 0.000 abstract 3
- 102000004877 Insulin Human genes 0.000 abstract 3
- 108090001061 Insulin Proteins 0.000 abstract 3
- 229940125396 insulin Drugs 0.000 abstract 3
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 abstract 3
- 125000003161 (C1-C6) alkylene group Chemical group 0.000 abstract 2
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 abstract 2
- 125000006528 (C2-C6) alkyl group Chemical group 0.000 abstract 2
- 239000012190 activator Substances 0.000 abstract 2
- 125000003545 alkoxy group Chemical group 0.000 abstract 2
- 239000000883 anti-obesity agent Substances 0.000 abstract 2
- 229940125708 antidiabetic agent Drugs 0.000 abstract 2
- 239000003472 antidiabetic agent Substances 0.000 abstract 2
- 229940125710 antiobesity agent Drugs 0.000 abstract 2
- 125000004429 atom Chemical group 0.000 abstract 2
- 150000002148 esters Chemical class 0.000 abstract 2
- 125000005842 heteroatom Chemical group 0.000 abstract 2
- 125000000592 heterocycloalkyl group Chemical group 0.000 abstract 2
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 abstract 2
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 abstract 2
- 230000001575 pathological effect Effects 0.000 abstract 2
- 125000000951 phenoxy group Chemical group [H]C1=C([H])C([H])=C(O*)C([H])=C1[H] 0.000 abstract 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 2
- 150000003839 salts Chemical class 0.000 abstract 2
- 239000012453 solvate Substances 0.000 abstract 2
- SWLAMJPTOQZTAE-UHFFFAOYSA-N 4-[2-[(5-chloro-2-methoxybenzoyl)amino]ethyl]benzoic acid Chemical compound COC1=CC=C(Cl)C=C1C(=O)NCCC1=CC=C(C(O)=O)C=C1 SWLAMJPTOQZTAE-UHFFFAOYSA-N 0.000 abstract 1
- 229940077274 Alpha glucosidase inhibitor Drugs 0.000 abstract 1
- 206010056997 Impaired fasting glucose Diseases 0.000 abstract 1
- 229940122199 Insulin secretagogue Drugs 0.000 abstract 1
- 229940122355 Insulin sensitizer Drugs 0.000 abstract 1
- 102000004882 Lipase Human genes 0.000 abstract 1
- 108090001060 Lipase Proteins 0.000 abstract 1
- 239000004367 Lipase Substances 0.000 abstract 1
- 108010047068 Melanin-concentrating hormone receptor Proteins 0.000 abstract 1
- 102000003728 Peroxisome Proliferator-Activated Receptors Human genes 0.000 abstract 1
- 108090000029 Peroxisome Proliferator-Activated Receptors Proteins 0.000 abstract 1
- 229940100389 Sulfonylurea Drugs 0.000 abstract 1
- 239000000556 agonist Substances 0.000 abstract 1
- 125000004450 alkenylene group Chemical group 0.000 abstract 1
- 239000003888 alpha glucosidase inhibitor Substances 0.000 abstract 1
- 125000002102 aryl alkyloxo group Chemical group 0.000 abstract 1
- 125000003118 aryl group Chemical group 0.000 abstract 1
- 125000003236 benzoyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C(*)=O 0.000 abstract 1
- 125000004432 carbon atom Chemical group C* 0.000 abstract 1
- 239000003937 drug carrier Substances 0.000 abstract 1
- 125000000623 heterocyclic group Chemical group 0.000 abstract 1
- 229940088597 hormone Drugs 0.000 abstract 1
- 239000005556 hormone Substances 0.000 abstract 1
- 239000003112 inhibitor Substances 0.000 abstract 1
- 235000019421 lipase Nutrition 0.000 abstract 1
- 229950004994 meglitinide Drugs 0.000 abstract 1
- 102000006953 melanin-concentrating hormone receptor activity proteins Human genes 0.000 abstract 1
- 239000002660 neuropeptide Y receptor antagonist Substances 0.000 abstract 1
- 229910052760 oxygen Inorganic materials 0.000 abstract 1
- 229940002612 prodrug Drugs 0.000 abstract 1
- 239000000651 prodrug Substances 0.000 abstract 1
- 102000004169 proteins and genes Human genes 0.000 abstract 1
- 108090000623 proteins and genes Proteins 0.000 abstract 1
- 239000002464 receptor antagonist Substances 0.000 abstract 1
- 229940044551 receptor antagonist Drugs 0.000 abstract 1
- 231100000489 sensitizer Toxicity 0.000 abstract 1
- YROXIXLRRCOBKF-UHFFFAOYSA-N sulfonylurea Chemical class OC(=N)N=S(=O)=O YROXIXLRRCOBKF-UHFFFAOYSA-N 0.000 abstract 1
- 229910052717 sulfur Inorganic materials 0.000 abstract 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/4164—1,3-Diazoles
- A61K31/4184—1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
- A61K31/437—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- 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
- A61P3/04—Anorexiants; Antiobesity agents
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
Landscapes
- Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Organic Chemistry (AREA)
- General Chemical & Material Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Diabetes (AREA)
- Epidemiology (AREA)
- Obesity (AREA)
- Hematology (AREA)
- Vascular Medicine (AREA)
- Rheumatology (AREA)
- Urology & Nephrology (AREA)
- Cardiology (AREA)
- Emergency Medicine (AREA)
- Endocrinology (AREA)
- Pain & Pain Management (AREA)
- Child & Adolescent Psychology (AREA)
- Heart & Thoracic Surgery (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Abstract
Reivindicacion 1: Un método para tratar una condicion patologica en un paciente, que comprende la administracion al paciente de una cantidad efectiva de uno o varios compuestos que tienen la formula (1), o una de sus sales, solvatos, ésteres oprodrogas farmacéuticamente aceptables, en donde: la línea punteada representa un enlace opcional y adicional; M1 es C(R3); X es un enlace o alquileno C1-6; Y es -C(O)-, -C(S)-, -(CH2)q-, -C(O)NR4-, -C(O)CH2-, -SO2- o -C(=N-CN)-NH-, de modo que,cuando M1 es N, Y no es -C(O)NR4- o -C(=N-CN)-NH-; Z es un enlace, alquileno C1-6, alquenileno C1-6, -C(O)-, -CH(CN)-, o -CH2C(O)NR4-; R1 como en formulas (2) Q es -N(R8)-, -S- u -O-; R es H, OH, alquilo C1-6, haloalquilo C1-6, alcoxi C1-6, alcoxiC1-6-alquilo C1-6, alcoxi C1-6-alcoxi C1-6, alcoxi C1-6-alquil C1-6-SO0-2, R32-arilalcoxi C1-6-, R32-arilalquilo C1-6, R32-arilo, R32-ariloxi, R32-heteroarilo, cicloalquilo C3-6, cicloalquil C3-6-alquilo C1-6, cicloalquil C3-6-alcoxi C1-6,cicloalquil C3-6-oxi-, R37-hetero-cicloalquilo, N(R30)(R31)-alquilo C1-6, -N(R30)(R31), -NH-alquil C1-6-O-alquilo C1-6, -NHC(O)NH(R29); R29-S(O)0-2-, haloalquil C1-6-S(O)0-2-, N(R30)(R31)-alquil C1-6-S(O)0-2- o benzoílo; R2 es un anillo heteroarilode seis miembros que tiene 1 o 2 heteroátomos seleccionados, de modo independiente, de N o N-O, siendo los demás átomos del anillo restante carbono; un anillo heteroarilo de cinco miembros que tiene 1, 2 o 3 heteroátomos seleccionados, de modoindependiente, de N, O o S, siendo los demás átomos del anillo restante carbono; R32-quinolilo; R32-arilo; heterocicloalquilo; formulas (3) en donde dicho anillo heteroarilo de seis miembros o dicho anillo heteroarilo de cinco miembros estáopcionalmente sustituido con R6; R3 es H, halo, alquilo C1-6, -OH o alcoxi C1-6; R4 está seleccionado, de modo independiente, del grupo que consiste en hidrogeno, alquilo C1-6, cicloalquilo C3-6, cicloalquil C3-6-alquilo C1-6, R33-arilo, R33-arilalquilo C1-6, y R32-heteroarilo; R5 es hidrogeno, alquilo C1-6, -C(O)R20, -C(O)2R20, -C(O)N(R20)2, alquil C1-6-SO2-, o alquil C1-6-SO2-NH-; R6 es 1 a 3 sustituyentes seleccionados, de modo independiente, del grupo que consiste en -OH, halo,alquilo C1-6, alcoxi C1-6, alquil C1-6-tio, -CF3, -NR4R5, fenilo, R33-fenilo, NO2, -CO2R4, -CON(R4)2, formulas (4), R7 es -N(R29)-, -O- o -SO0-2-; R8 es H, alquilo C1-6, haloalquilo C1-6, alcoxi C1-6-alquilo C1-6, R32-arilalquilo C1-6, R32-arilo,R32-heteroarilo, cicloalquilo C3-6, cicloalquil C3-6-alquilo C1-6, R37-heterocicloalquilo, N(R30)(R31)-alquilo C1-6, R29-S(O)2-, haloalquil C1-6-S(O)2-, R29-S(O)0-1-alquilo C2-6, haloalquil C1-6-S(O)0-1-alquilo C2-6; R12 está seleccionado, de modoindependiente, del grupo que consiste en alquilo C1-6, hidroxilo, alcoxi C1-6, o fluoro, siempre que, cuando R12 es hidroxi o fluoro, luego R12 no esté unido a un carbono adyacente a un nitrogeno; o R12 forma un puente de alquilo C1 a C2 de unanillo carbono a otro anillo carbono; R13 está seleccionado, de modo independiente, del grupo que consiste en alquilo C1-6, hidroxilo, alcoxi C1-6, o fluoro, siempre que, cuando R13 es hidroxi o fluoro, entonces R13 no esté unido a un carbonoadyacente a un nitrogeno; o forma un puente de alquilo C1 a C2 de un anillo carbono a otro anillo carbono; o R13 es =O; R20 está seleccionado, de modo independiente, del grupo que consiste en hidrogeno, alquilo C1-6, o arilo, en donde dicho grupoarilo está opcionalmente sustituido con de 1 a 3 grupos seleccionados, de modo independiente, de halo, -CF3, -OCF3, hidroxilo, o metoxi; o cuando dos grupos R20 están presentes, dichos dos grupos R20 tomados junto con el nitrogeno al que estánunidos, forman un anillo heterocíclico de cinco o seis miembros; R22 es alquilo C1-6, R34-arilo o heterocicloalquilo; R24 es H, alquilo C1-6, -SO2R22 o R34-arilo; R25 está seleccionado, de modo independiente, del grupo que consiste en alquilo C1-6,halo, -CF3, -OH, alcoxi C1-6, alquil C1-6-C(O)-, aril-C(O)-, N(R4)(R5)-C(O)-, N(R4)(R5)-S(O)1-2-, halo-alquil C1-6- o halo-alcoxi C1-6-alquilo C1-6; R29 es H, alquilo C1-6, cicloalquilo C3-6, R35-arilo o R35-arilalquilo C1-6; R30 es H, alquilo C1-6,R35-arilo o R35-arilalquilo C1-6; R31 es H, alquilo C1-6, R35-arilo, R35-arilalquilo C1-6, R35-heteroarilo, alquil C1-6-C(O)-, R35-aril-C(O)-, N(R4)(R5)-C(O)-, alquil C1-6-S(O)2- o R35-aril-S(O)2-; o R30 y R31 juntos son -(CH2)4-5-, -(CH2)2-O-(CH2)2- o -(CH2)2-N(R38)-(CH2)2- y forman un anillo con el nitrogeno al que están unidos; R32 es 1 a 3 sustituyentes seleccionados, de modo independiente, del grupo que consiste en H, -OH, halo, alquilo C1-6, alcoxi C1-6, R35-aril-O-, -SR22, -CF3, -OCF3, -OCHF2, -NR4R5, fenilo, R33-fenilo, NO2, -CO2R4, -CON(R4)2, -S(O)2R22, -S(O)2N(R20)2, -N(R24)S(O)2R22, -CN, hidroxi-alquilo C1-6, - OCH2CH2OR22, y R35-arilalquil C1-6-O-, o dos grupos R32 en átomos de carbono adyacentes forman juntos un grupo -OCH2O-u -O(CH2)2O-; R33 es 1 a 3 sustituyentes seleccionados, de modo independiente, del grupo que consiste en alquilo C1-6, halo, -CN, -NO2, -CF3, -OCF3, -OCHF2 y -O- alquilo C1-6; R34 es 1 a 3 sustituyentes seleccionados, de modo independiente, delgrupo que consiste en H, halo, -CF3, -OCF3, -OH y -OCH3; R35 es 1 a 3 sustituyentes seleccionados, de modo independiente, de hidrogeno, halo, alquilo C1-6, hidroxi, alcoxi C1-6, fenoxi, -CF3, -N(R36)2, -COOR20 y -NO2; R36 está seleccionado, de modoindependiente, del grupo que consiste en H y alquilo C1-6; R37 es 1 a 3 sustituyentes seleccionados, de modo independiente, de hidrogeno, halo, alquilo C1-6, hidroxi, alcoxi C1-6, fenoxi, -CF3, -N(R36)2, -COOR20, -C(O)N(R29)2 y -NO2, o R37 es uno odos grupos =O; R38 es H, alquilo C1-6, R35-arilo, R35-arilalquilo C1-6, alquil C1-6-SO2 o haloalquil C1-6-SO2-; a es 0, 1 o 2; b es 0, 1 o 2; k es 0, 1, 2, 3 o 4; k1 es 0,1, 2 o 3; k2 es 0, 1 o 2; n es 2; p es 1, 2 o 3; q es un numero entero que vade 1 a 5; y r es un numero entero que va de 0 a 3, de modo que: (i) cuando M2 es N, p no es 1; (ii) cuando r es 0, M2 es C; y (iii) la suma de p y r es 3, en donde la condicion patologica es diabetes, una complicacion diabética, tolerancia a glucosaalterada o glucosa en ayunas alterada. Reivindicacion 26: El método de acuerdo con la reivindicacion 1, en donde uno o varios compuestos de la formula (1) están seleccionados de formulas (5), o una de sus sales, solvatos, ésteres o prodrogasfarmacéuticamente aceptables. Reivindicacion 56: Una composicion que comprende un compuesto de acuerdo con la reivindicacion 1, un agente antidiabético adicional que no es un compuesto de la formula (1), y un portador farmacéuticamente aceptable. Reivindicacion 57: La composicion de acuerdo con la reivindicacion 55, en donde el agente antidiabético adicional está seleccionado de una sulfonilurea, un sensibilizante de insulina, un inhibidor de alfa-glucosidasa, un secretagogo de insulina,un agente antiobesidad, una meglitinida, insulina o una composicion con contenido de insulina. Reivindicacion 59: La composicion de acuerdo con la reivindicacion 57, en donde el sensibilizante de insulina es un activador de PPAR. Reivindicacion61: La composicion de acuerdo con la reivindicacion 59, en donde el agente antiobesidad está seleccionado de: un antagonista de neuropéptido Y, un agonista de MCR4, un antagonista de receptor MCH, una hormona de proteína, un activador de AMPquinasa, y un inhibidor de lipasa.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US90445307P | 2007-03-02 | 2007-03-02 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR065495A1 true AR065495A1 (es) | 2009-06-10 |
Family
ID=39386454
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP080100805A AR065495A1 (es) | 2007-03-02 | 2008-02-27 | Metodos para usar derivados de bencimidazol para tratar o prevenir dolor, diabetes, complicacion diabetica composiciones. |
Country Status (18)
| Country | Link |
|---|---|
| US (1) | US20100144591A1 (es) |
| EP (1) | EP2114402A2 (es) |
| JP (1) | JP2010520201A (es) |
| KR (1) | KR20090127902A (es) |
| CN (1) | CN101674827A (es) |
| AR (1) | AR065495A1 (es) |
| AU (1) | AU2008223513A1 (es) |
| BR (1) | BRPI0808707A2 (es) |
| CA (1) | CA2679809A1 (es) |
| CL (1) | CL2008000593A1 (es) |
| EC (1) | ECSP099612A (es) |
| IL (1) | IL200639A0 (es) |
| MX (1) | MX2009009416A (es) |
| PE (1) | PE20090111A1 (es) |
| RU (1) | RU2009136263A (es) |
| TW (1) | TW200843756A (es) |
| WO (1) | WO2008108958A2 (es) |
| ZA (1) | ZA200906062B (es) |
Families Citing this family (23)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2698071A1 (en) * | 2007-08-27 | 2009-03-05 | Wyeth Llc | Imidazopyridine analogs and their use as agonists of the wnt-beta-catenin cellular messaging system |
| WO2010036613A1 (en) * | 2008-09-26 | 2010-04-01 | Merck Sharp & Dohme Corp. | Novel cyclic benzimidazole derivatives useful anti-diabetic agents |
| JP5642661B2 (ja) * | 2009-03-05 | 2014-12-17 | 塩野義製薬株式会社 | Ｎｐｙｙ５受容体拮抗作用を有するピペリジンおよびピロリジン誘導体 |
| US8829020B2 (en) | 2009-07-16 | 2014-09-09 | Mallinckrodt Llc | Compounds and compositions for use in phototherapy and in treatment of ocular neovascular disease and cancers |
| AU2010322478B2 (en) * | 2009-11-18 | 2013-11-14 | Glaxosmithkline Intellectual Property (No. 3) Limited | Benzoimidazole compounds and uses thereof |
| CN102781940B (zh) | 2009-12-30 | 2016-09-07 | 艾科尔公司 | 取代的咪唑并吡啶基-氨基吡啶化合物 |
| WO2012020725A1 (ja) * | 2010-08-10 | 2012-02-16 | 塩野義製薬株式会社 | Ｎｐｙ ｙ５受容体拮抗作用を有するヘテロ環誘導体 |
| JP5790440B2 (ja) | 2010-12-01 | 2015-10-07 | 住友化学株式会社 | ピリミジン化合物およびその有害生物防除用途 |
| US8889704B2 (en) * | 2011-02-25 | 2014-11-18 | Array Biopharma Inc. | Triazolopyridine compounds as PIM kinase inhibitors |
| JP2014114212A (ja) * | 2011-03-29 | 2014-06-26 | Dainippon Sumitomo Pharma Co Ltd | 新規ベンズイミダゾール誘導体 |
| WO2012158117A1 (en) * | 2011-05-17 | 2012-11-22 | Astrazeneca Ab | Combination therapies for treating pain |
| WO2012177852A1 (en) | 2011-06-24 | 2012-12-27 | Arqule, Inc | Substituted imidazopyridinyl compounds |
| CN103748093B (zh) | 2011-06-24 | 2016-06-01 | 艾科尔公司 | 被取代的咪唑并吡啶基-氨基吡啶化合物 |
| US9527839B2 (en) | 2012-08-22 | 2016-12-27 | Merck Sharp & Dohme Corp. | Benzimidazole tetrahydropyran derivatives |
| US9090618B2 (en) | 2012-12-27 | 2015-07-28 | Purdue Pharma L.P. | Substituted benzimidazole-type piperidine compounds and uses thereof |
| EP2968285A4 (en) * | 2013-03-13 | 2016-12-21 | Flatley Discovery Lab | COMPOUNDS AND METHODS FOR THE TREATMENT OF CYSTIC FIBROSIS |
| JP6539274B2 (ja) | 2013-08-12 | 2019-07-03 | ファーマシューティカル マニュファクチュアリング リサーチ サービシズ，インコーポレーテッド | 押出成形された即放性乱用抑止性丸剤 |
| WO2015095391A1 (en) | 2013-12-17 | 2015-06-25 | Pharmaceutical Manufacturing Research Services, Inc. | Extruded extended release abuse deterrent pill |
| US9492444B2 (en) | 2013-12-17 | 2016-11-15 | Pharmaceutical Manufacturing Research Services, Inc. | Extruded extended release abuse deterrent pill |
| EP3169315B1 (en) | 2014-07-17 | 2020-06-24 | Pharmaceutical Manufacturing Research Services, Inc. | Immediate release abuse deterrent liquid fill dosage form |
| US20160106737A1 (en) | 2014-10-20 | 2016-04-21 | Pharmaceutical Manufacturing Research Services, Inc. | Extended Release Abuse Deterrent Liquid Fill Dosage Form |
| CN104860919B (zh) * | 2015-03-26 | 2017-11-10 | 天津药物研究院有限公司 | 含哌啶的苯并咪唑衍生物及其制备方法和用途 |
| JP6850730B2 (ja) * | 2015-11-12 | 2021-03-31 | 学校法人 聖マリアンナ医科大学 | 緑内障予防治療剤 |
Family Cites Families (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6211199B1 (en) * | 1995-11-17 | 2001-04-03 | Aventis Pharmaceuticals Inc. | Substituted 4-(1H-benzimidazol-2-yl-amino)piperidines useful for the treatment of allergic diseases |
| EP1474132A1 (en) * | 2002-01-11 | 2004-11-10 | Abbott Laboratories | Histamine-3 receptor ligands for diabetic conditions |
| PE20040464A1 (es) * | 2002-04-18 | 2004-07-24 | Schering Corp | Benzimidazolonas sustituidas y derivados como antagonistas de histamina h3 |
| US7105505B2 (en) * | 2002-04-18 | 2006-09-12 | Schering Corporation | Benzimidazole derivatives useful as histamine H3 antagonists |
| EP1931665A1 (en) * | 2005-09-20 | 2008-06-18 | Schering Corporation | 1-[[1-[(2-amin0-6-methyl-4-pyridinyl)methyl]-4-flu0r0-4-piperidinyl,]carbonyl]-4-[2-(2-pyridinyl)-3h-imidaz0[4, 5-b]pyridin-3-yl]piperidine useful as histamine h3 antagonist |
| KR20080081321A (ko) * | 2005-12-21 | 2008-09-09 | 쉐링 코포레이션 | Ｈ3 길항제/역 작용제 및 식욕 억제제의 조합물 |
-
2008
- 2008-02-27 CN CN200880014373A patent/CN101674827A/zh active Pending
- 2008-02-27 KR KR1020097020505A patent/KR20090127902A/ko not_active Withdrawn
- 2008-02-27 BR BRPI0808707-5A patent/BRPI0808707A2/pt not_active Application Discontinuation
- 2008-02-27 CA CA002679809A patent/CA2679809A1/en not_active Abandoned
- 2008-02-27 AU AU2008223513A patent/AU2008223513A1/en not_active Abandoned
- 2008-02-27 RU RU2009136263/15A patent/RU2009136263A/ru unknown
- 2008-02-27 CL CL200800593A patent/CL2008000593A1/es unknown
- 2008-02-27 US US12/527,500 patent/US20100144591A1/en not_active Abandoned
- 2008-02-27 AR ARP080100805A patent/AR065495A1/es not_active Application Discontinuation
- 2008-02-27 EP EP08714248A patent/EP2114402A2/en not_active Withdrawn
- 2008-02-27 JP JP2009551714A patent/JP2010520201A/ja not_active Withdrawn
- 2008-02-27 WO PCT/US2008/002594 patent/WO2008108958A2/en not_active Ceased
- 2008-02-27 TW TW097106891A patent/TW200843756A/zh unknown
- 2008-02-27 MX MX2009009416A patent/MX2009009416A/es unknown
- 2008-02-28 PE PE2008000405A patent/PE20090111A1/es not_active Application Discontinuation
-
2009
- 2009-08-30 IL IL200639A patent/IL200639A0/en unknown
- 2009-09-01 ZA ZA200906062A patent/ZA200906062B/xx unknown
- 2009-09-01 EC EC2009009612A patent/ECSP099612A/es unknown
Also Published As
| Publication number | Publication date |
|---|---|
| EP2114402A2 (en) | 2009-11-11 |
| RU2009136263A (ru) | 2011-04-10 |
| WO2008108958A8 (en) | 2009-08-13 |
| BRPI0808707A2 (pt) | 2014-09-09 |
| ECSP099612A (es) | 2009-10-30 |
| AU2008223513A1 (en) | 2008-09-12 |
| MX2009009416A (es) | 2009-09-11 |
| CA2679809A1 (en) | 2008-09-12 |
| WO2008108958A3 (en) | 2009-05-07 |
| TW200843756A (en) | 2008-11-16 |
| US20100144591A1 (en) | 2010-06-10 |
| IL200639A0 (en) | 2010-05-17 |
| ZA200906062B (en) | 2010-05-26 |
| CL2008000593A1 (es) | 2008-09-05 |
| PE20090111A1 (es) | 2009-02-26 |
| KR20090127902A (ko) | 2009-12-14 |
| CN101674827A (zh) | 2010-03-17 |
| WO2008108958A2 (en) | 2008-09-12 |
| JP2010520201A (ja) | 2010-06-10 |
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Legal Events
| Date | Code | Title | Description |
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| FA | Abandonment or withdrawal |