AR038886A1 - Amidas heterociclicas, inhibidores de actividad de glucogeno fosforilasa - Google Patents
Amidas heterociclicas, inhibidores de actividad de glucogeno fosforilasaInfo
- Publication number
- AR038886A1 AR038886A1 ARP030100766A ARP030100766A AR038886A1 AR 038886 A1 AR038886 A1 AR 038886A1 AR P030100766 A ARP030100766 A AR P030100766A AR P030100766 A ARP030100766 A AR P030100766A AR 038886 A1 AR038886 A1 AR 038886A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- hydroxy
- carbamoyl
- thien
- pyrrole
- Prior art date
Links
- 230000000694 effects Effects 0.000 title abstract 3
- 239000003112 inhibitor Substances 0.000 title 1
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract 22
- KAESVJOAVNADME-UHFFFAOYSA-N Pyrrole Chemical compound C=1C=CNC=1 KAESVJOAVNADME-UHFFFAOYSA-N 0.000 abstract 22
- -1 heterocyclic amide Chemical class 0.000 abstract 18
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 abstract 8
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 8
- 229910052757 nitrogen Inorganic materials 0.000 abstract 8
- 125000000229 (C1-C4)alkoxy group Chemical group 0.000 abstract 7
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 abstract 7
- 125000000623 heterocyclic group Chemical group 0.000 abstract 7
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 6
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 abstract 5
- 229910052799 carbon Inorganic materials 0.000 abstract 5
- 125000005843 halogen group Chemical group 0.000 abstract 5
- 229910052739 hydrogen Inorganic materials 0.000 abstract 5
- 239000001257 hydrogen Substances 0.000 abstract 5
- 125000001424 substituent group Chemical group 0.000 abstract 5
- 125000006656 (C2-C4) alkenyl group Chemical group 0.000 abstract 4
- 125000000217 alkyl group Chemical group 0.000 abstract 4
- 125000003118 aryl group Chemical group 0.000 abstract 4
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 abstract 3
- 125000006272 (C3-C7) cycloalkyl group Chemical group 0.000 abstract 3
- 150000001875 compounds Chemical class 0.000 abstract 3
- 125000004130 indan-2-yl group Chemical group [H]C1=C([H])C([H])=C2C(=C1[H])C([H])([H])C([H])(*)C2([H])[H] 0.000 abstract 3
- 229910052760 oxygen Inorganic materials 0.000 abstract 3
- 125000006650 (C2-C4) alkynyl group Chemical group 0.000 abstract 2
- 102000007390 Glycogen Phosphorylase Human genes 0.000 abstract 2
- 108010046163 Glycogen Phosphorylase Proteins 0.000 abstract 2
- 125000001589 carboacyl group Chemical group 0.000 abstract 2
- 125000001028 difluoromethyl group Chemical group [H]C(F)(F)* 0.000 abstract 2
- 125000005842 heteroatom Chemical group 0.000 abstract 2
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 abstract 2
- 229920006395 saturated elastomer Polymers 0.000 abstract 2
- 229910052717 sulfur Inorganic materials 0.000 abstract 2
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 abstract 2
- 125000002861 (C1-C4) alkanoyl group Chemical group 0.000 abstract 1
- OHLUUHNLEMFGTQ-UHFFFAOYSA-N N-methylacetamide Chemical compound CNC(C)=O OHLUUHNLEMFGTQ-UHFFFAOYSA-N 0.000 abstract 1
- 150000001204 N-oxides Chemical class 0.000 abstract 1
- DHKHKXVYLBGOIT-UHFFFAOYSA-N acetaldehyde Diethyl Acetal Natural products CCOC(C)OCC DHKHKXVYLBGOIT-UHFFFAOYSA-N 0.000 abstract 1
- 125000004423 acyloxy group Chemical group 0.000 abstract 1
- 125000005115 alkyl carbamoyl group Chemical group 0.000 abstract 1
- 125000005153 alkyl sulfamoyl group Chemical group 0.000 abstract 1
- 125000004397 aminosulfonyl group Chemical group NS(=O)(=O)* 0.000 abstract 1
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 abstract 1
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 abstract 1
- 125000004432 carbon atom Chemical group C* 0.000 abstract 1
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 125000004216 fluoromethyl group Chemical group [H]C([H])(F)* 0.000 abstract 1
- 125000005549 heteroarylene group Chemical group 0.000 abstract 1
- 230000002401 inhibitory effect Effects 0.000 abstract 1
- 238000004519 manufacturing process Methods 0.000 abstract 1
- 238000000034 method Methods 0.000 abstract 1
- 125000000250 methylamino group Chemical group [H]N(*)C([H])([H])[H] 0.000 abstract 1
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 abstract 1
- 125000004433 nitrogen atom Chemical group N* 0.000 abstract 1
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 abstract 1
- 125000004043 oxo group Chemical group O=* 0.000 abstract 1
- 239000001301 oxygen Substances 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 125000000843 phenylene group Chemical group C1(=C(C=CC=C1)*)* 0.000 abstract 1
- 239000000651 prodrug Substances 0.000 abstract 1
- 229940002612 prodrug Drugs 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 125000004434 sulfur atom Chemical group 0.000 abstract 1
- 125000000876 trifluoromethoxy group Chemical group FC(F)(F)O* 0.000 abstract 1
- 125000004385 trihaloalkyl group Chemical group 0.000 abstract 1
- 125000004953 trihalomethyl group Chemical group 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
- C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D495/04—Ortho-condensed systems
-
- 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
- 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)
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Engineering & Computer Science (AREA)
- Diabetes (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Veterinary Medicine (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Emergency Medicine (AREA)
- Endocrinology (AREA)
- Child & Adolescent Psychology (AREA)
- Urology & Nephrology (AREA)
- Vascular Medicine (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
Los compuestos poseen actividad inhibidora de la actividad de glucógeno fosforilasa y por lo tanto tienen valor en el tratamiento de estados de enfermedad con un aumento en la actividad de la glucógeno fosforilasa. También se describen procesos para la fabricación de dichos derivados de amidas heterocíclicas y composiciones farmacéuticas que los contienen. Reivindicación 1: Un compuesto caracterizado porque responde a la fórmula (1) donde: Z es CH o nitrógeno; R4 y R5 juntos son o bien -S-C(R6)=C(R7)- o -C(R7)=C(R6)-S-; R6 y R7 se seleccionan independientemente entre hidrógeno, halo, nitro, ciano, hidroxi, fluorometilo, difluorometilo, trifluorometilo, trifluorometoxi, carboxi, carbamoilo, alquilo C1-4, alquenilo C2-4, alquinilo C2-4, alcoxi C1-4 y alcanoílo C1-4; A es fenileno o heteroarileno; n es 0, 1 ó 2; R1 se selecciona independientemente entre halo, nitro, ciano, hidroxi, carboxi, carbamoilo, N-alquilcarbamoilo C1-4, N,N-(alquil C1-4)2carbamoilo, sulfamoilo, N-alquilsulfamoilo C1-4, N,N-(alquil C1-4)2sulfamoilo, -S(O)balquilo C1-4 (donde b es 0, 1 ó 2), alquilo C1-4, alquenilo C2-4, alquinilo C2-4, alcoxi C1-4, alcanoilo C1-4, alcanoiloxi C1-4, hidroxi alquilo C1-4, fluorometilo, difluorometilo, trifluorometilo y trifluorometoxi; o, cuando n es 2, los dos grupos R1, junto con los átomos de carbono de A a los cuales están unidos, pueden formar un anillo de 4 a 7 miembros, que contiene opcionalmente 1 ó 2 heteroátomos seleccionados independientemente entre O, S y N, y estando opcionalmente sustituidos por 1 ó 2 grupos metilo; r es 1 ó 2; y cuando r es 1 el grupo de fórmula (2) es un sustituyente en el carbono (2) y cuando el r es 2 (formando así un anillo de 6 miembros) el mismo grupo es un sustituyente en el carbono (2) o en el carbono (3); Y es -NR2R3 o -OR3; R2 y R3 se seleccionan independientemente entre hidrógeno, hidroxi, alcoxi C1-4, alcanoilo C1-4, carbamoilo, cicloalquilo C3-7 (opcionalmente sustituido con 1 ó 2 grupos hidroxi), ciano alquilo C1-4, heterociclilo, arilo, alquilo C1-4 (opcionalmente sustituido por 1 ó 2 grupos R8), -COR8, -SObR8 (donde b es 0, 1 ó 2) y grupos de las fórmulas (3) y (4) donde y es 0 ó 1; t es 0, 1, 2 ó 3 y a es 1 ó 2; con la salvedad de que el grupo hidroxi no es un sustituyente en el carbono del anillo adyacente al oxígeno del anillo; o donde NR2R3 pueden formar un anillo saturado, parcialmente saturado o insaturado de 4 a 7 miembros, que contiene opcionalmente 1, 2 ó 3 heteroátomos adicionales seleccionados independientemente entre N, O y S, donde cualquier -CH2- puede ser opcionalmente reemplazado por -C(=O)-, y cualquier átomo de N o S puede oxidarse opcionalmente para formar un grupo N-óxido ó SO o SO2 respectivamente, y donde el anillo es opcionalmente sustituido por 1 ó 2 sustituyentes independientemente seleccionados entre halo, ciano, alquilo C1-4, hidroxi, alcoxi C1-4 y alquil C1-4 S(O)b- (donde b es 0, 1 ó 2); R8 se selecciona independientemente entre hidrógeno, hidroxi, alquilo C1-4, alquenilo C2-4, alcoxi C1-4, ciano alquilo C1-4, amino alquilo C1-4 (opcionalmente sustituido en el nitrógeno por 1 ó 2 grupos seleccionados entre alquilo C1-4, hidroxi, hidroxi alquilo C1-4, dihidroxi alquilo C1-4, -CO2 alquilo C1-4, arilo y aril alquilo C1-4), halo alquilo C1-4, dihalo alquilo C1-4, trihalo alquilo C1-4, hidroxi alquilo C1-4, dihidroxi alquilo C1-4, alcoxi C1-4 alcoxi C1-4, alcoxi C1-4 alquilo C1-4, hidroxi alcoxi C1-4, acetales cíclicos de 5 y 6 miembros y derivados mono- y di-metilo de los mismos, arilo, heterociclilo, (heterociclil) alquilo C1-4, cicloalquilo C3-7 (opcionalmente sustituido con 1 ó 2 grupos hidroxi, alquilo C1-4 o -C(O)O alquilo C1-4), alcanoilo C1-4, alquil C1-4 S(O)b- (donde b es 0, 1 ó 2), cicloalquil C3-6 S(O)b- (donde b es 0, 1 ó 2), S(O)b- donde b es 0, 1 ó 2 heterociclil S(O)b- (donde b es 0, 1 ó 2), bencil S(O)b- (donde b es 0, 1 ó 2), alquil C1-4 S(O)c alquilo C1-4, (donde c es 0, 1 ó 2), -N(OH)CHO, -C(=N-OH)NH2, -C(=N-OH)NH alquilo C1-4, -C(=N-OH)N(alquil C1-4)2, -C(=N-OH)NH cicloalquilo C3-6, -C(=N-OH)N(cicloalquil C3-6)2, -COCOOR9, -C(O)N(R9)(R10), -NHC(O)R9, -C(O)NHSO2(alquilo C1-4), -NHSO2R9, (R9)(R10)NSO2-, -COCH2OR11, (R9)(R10)N- y -COOR9, -CH2OR9, -CH2COOR9,-CH2OCOR9, -CH2CH(CO2R9)OH, -CH2C(O)NR9R10, -(CH2)wCH(NR9R10)CO2R9' (donde w es 1, 2 ó 3), y -(CH2)wCH(NR9R10)CO(NR9'R10')(donde w es 1, 2 ó 3); R9, R9', R10 y R10' se seleccionan independientemente entre hidrógeno, hidroxi, alquilo C1-4 (opcionalmente sustituido por 1 ó 2 R13), alquenilo C2-4, cicloalquilo C3-7 (opcionalmente sustituido por 1 ó 2 grupos hidroxi), ciano alquilo C1-4, trihaloalquilo, arilo, heterociclilo, heterociclil (alquilo C1-4), y -C(=O)O alquilo C1-4; o R9 y R10 junto con el nitrógeno; a los cuales están unidos, y/o R9' y R10' junto con el nitrógeno al cual están unidos, forman un anillo de 4 a 6 miembros donde el anillo es opcionalmente sustituido en un carbono por 1 ó 2 sustituyentes independientemente seleccionados entre oxo, hidroxi, carboxi, halo, nitro, ciano, carbonilo; alcoxi C1-4 y heterociclilo; o el anillo puede ser opcionalmente sustituido en dos carbonos adyacente por -O-CH2-O- para formar un acetal cíclico donde uno o ambos hidrógenos del grupo -O-CH2-O- pueden ser reemplazados por un metilo; R13 se selecciona entre halo, trihalometilo, y alcoxi C1-4; R11 se selecciona independientemente entre hidrógeno, alquilo C1-4, e hidroxi alquilo C1-4; o una sal aceptable para uso farmacéutico o prodroga del mismo; con la salvedad de que el compuesto de fórmula (1) no es: i) 2,3-dicloro-5-(N-{1-[N-(1,1-dimetiletoxi)carbonilamino]indan-2-il}carbamoil)-4H-tien[3,2-b]pirrol; ii) 5-[N-(1-aminoindan-2-il)carbamoil]-2,3-dicloro-4H-tien[3,2-b]pirrol; iii) 5-[N-(1-acetamidoindan-2-il)carbamoil]-2,3-dicloro-4H-tien[3,2-b]pirrol; iv) 2,3-dicloro-5-{N-[1-(metansulfonamido)indan-2-il]carbamoil}-4H-tien[3,2-b]pirrol; v) 2,3-dicloro-5-{N-[1-(metilamino)indan-2-il]carbamoil}-4H-tien[3,2-b]pirrol; iv) 2,3-dicloro-5-{N-[1-(metilacetamido)indan-2-il]carbamoil}-4H-tien[3,2-b]pirrol; vii) 2,3-dicloro-5-[N-(1-hidroxiindan-2-il)carbamoil]-4H-tien[3,2-b]pirrol; viii) 2-cloro-5-[N-(1-hidroxiindan-2-il)carbamoil-6H-tien[2,3-b]pirrol; ix) 2,3-dicloro-5-[N-(6-fluoro-1-hidroxiindan-2-il)carbamoil-4H-tien[3,2-b]pirrol; x) 2,3-dicloro-5-[N-(1-metoxiindan-2-il)-carbamoil-4H-tien[3,2-b]pirrol; xi) 2,3-dicloro-5-[N-(1-hidroxi-1,2,3,4-tetrahidronaft-2-il)carbamoil]-4H-tien[3,2-b]pirrol.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GBGB0205170.4A GB0205170D0 (en) | 2002-03-06 | 2002-03-06 | Chemical compounds |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR038886A1 true AR038886A1 (es) | 2005-02-02 |
Family
ID=9932334
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP030100766A AR038886A1 (es) | 2002-03-06 | 2003-03-06 | Amidas heterociclicas, inhibidores de actividad de glucogeno fosforilasa |
Country Status (25)
| Country | Link |
|---|---|
| US (1) | US7122567B2 (es) |
| EP (1) | EP1483271B1 (es) |
| JP (1) | JP2005524669A (es) |
| KR (1) | KR20040091101A (es) |
| CN (1) | CN1307183C (es) |
| AR (1) | AR038886A1 (es) |
| AT (1) | ATE346072T1 (es) |
| AU (1) | AU2003209445A1 (es) |
| BR (1) | BR0308145A (es) |
| CA (1) | CA2477125A1 (es) |
| DE (1) | DE60309849T2 (es) |
| DK (1) | DK1483271T3 (es) |
| ES (1) | ES2276092T3 (es) |
| GB (1) | GB0205170D0 (es) |
| IL (1) | IL163802A0 (es) |
| IS (1) | IS7433A (es) |
| MX (1) | MXPA04008611A (es) |
| NO (1) | NO20044033L (es) |
| NZ (1) | NZ534684A (es) |
| PL (1) | PL372772A1 (es) |
| PT (1) | PT1483271E (es) |
| RU (1) | RU2004125145A (es) |
| TW (1) | TW200306176A (es) |
| WO (1) | WO2003074531A1 (es) |
| ZA (1) | ZA200406685B (es) |
Families Citing this family (24)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB0205166D0 (en) | 2002-03-06 | 2002-04-17 | Astrazeneca Ab | Chemical compounds |
| GB0205176D0 (en) | 2002-03-06 | 2002-04-17 | Astrazeneca Ab | Chemical compounds |
| GB0205162D0 (en) | 2002-03-06 | 2002-04-17 | Astrazeneca Ab | Chemical compounds |
| GB0205165D0 (en) | 2002-03-06 | 2002-04-17 | Astrazeneca Ab | Chemical compounds |
| GB0205175D0 (en) | 2002-03-06 | 2002-04-17 | Astrazeneca Ab | Chemical compounds |
| GB0222909D0 (en) | 2002-10-03 | 2002-11-13 | Astrazeneca Ab | Novel process and intermediates |
| GB0222912D0 (en) | 2002-10-03 | 2002-11-13 | Astrazeneca Ab | Novel process and intermediates |
| JP4630267B2 (ja) * | 2002-12-25 | 2011-02-09 | 第一三共株式会社 | ジアミン誘導体 |
| AU2003292828B9 (en) | 2002-12-25 | 2009-10-01 | Daiichi Pharmaceutical Co., Ltd. | Diamine derivatives |
| GB0318463D0 (en) * | 2003-08-07 | 2003-09-10 | Astrazeneca Ab | Chemical compounds |
| GB0319759D0 (en) * | 2003-08-22 | 2003-09-24 | Astrazeneca Ab | Chemical compounds |
| BRPI0418244A (pt) | 2003-12-29 | 2007-04-17 | Sepracor Inc | composto, métodos para aumentar a concentração de d-serina e/ou diminuir a concentração de produtos tóxicos da oxidação de d-serina pela daao em um mamìfero, para tratar a esquizofrenia, para tratar ou prevenir a perda de memória e/ou cognição associadas com o mal de alzheimer, para tratar a ataxia ou para prevenir a perda da função neuronal caracterìstica de doenças neurodegenerativas, para intensificar a aprendizagem, memória e/ou cognição e para tratar dor neuropática, e, composição farmacêutica |
| US7223786B2 (en) | 2004-11-15 | 2007-05-29 | Bristol-Myers Squibb Company | 2-aminonaphthalene derivatives and related glycogen phosphorylase inhibitors |
| US7226942B2 (en) | 2004-11-15 | 2007-06-05 | Bristol-Myers Squibb Company | 2-amino-4-functionalized tetralin derivatives and related glycogen phosphorylase inhibitors |
| WO2006053274A2 (en) * | 2004-11-15 | 2006-05-18 | Bristol-Myers Squibb Company | 2-amino-1-functionalized tetralin derivatives and related glycogen phosphorylase inhibitors |
| WO2006055463A2 (en) * | 2004-11-15 | 2006-05-26 | Bristol-Myers Squibb Company | 2-amino-3-functionalized tetralin derivatives and related glycogen phosphorylase inhibitors |
| TWI281231B (en) * | 2004-12-20 | 2007-05-11 | Hynix Semiconductor Inc | Method for forming storage node of capacitor in semiconductor device |
| ES2566479T3 (es) | 2006-01-06 | 2016-04-13 | Sunovion Pharmaceuticals Inc. | Inhibidores de reabsorción de monoamina con base en tetralona |
| AU2007205114B2 (en) | 2006-01-06 | 2012-11-08 | Sunovion Pharmaceuticals Inc. | Cycloalkylamines as monoamine reuptake inhibitors |
| EP2013835B1 (en) | 2006-03-31 | 2015-11-04 | Sunovion Pharmaceuticals Inc. | Preparation of chiral amides and amines |
| PE20080251A1 (es) | 2006-05-04 | 2008-04-25 | Boehringer Ingelheim Int | Usos de inhibidores de dpp iv |
| US7884124B2 (en) | 2006-06-30 | 2011-02-08 | Sepracor Inc. | Fluoro-substituted inhibitors of D-amino acid oxidase |
| US7902252B2 (en) | 2007-01-18 | 2011-03-08 | Sepracor, Inc. | Inhibitors of D-amino acid oxidase |
| CN103936605B (zh) | 2007-05-31 | 2017-09-01 | 赛诺维信制药公司 | 苯基取代的环烷胺作为一元胺再摄取抑制剂 |
Family Cites Families (82)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE200740C (es) | ||||
| US3706810A (en) | 1970-09-15 | 1972-12-19 | American Cyanamid Co | N-morpholinoalkyl-thieno(3,2-b)pyrrole-5-carboxamides |
| US4720503A (en) | 1985-08-02 | 1988-01-19 | Merck & Co., Inc. | N-substituted fused-heterocyclic carboxamide derivatives as dual cyclooxygenase and lipoxygenase inhibitors |
| US4668769A (en) | 1985-08-02 | 1987-05-26 | Hoover Dennis J | Oxa- and azahomocyclostatine polypeptides |
| US4599198A (en) | 1985-08-02 | 1986-07-08 | Pfizer Inc. | Intermediates in polypeptide synthesis |
| FR2601368B1 (fr) | 1986-07-08 | 1989-04-07 | Synthelabo | Derives de nitrofuranne, leur preparation et leur application en therapeutique. |
| DE3629545A1 (de) | 1986-08-30 | 1988-03-10 | Bayer Ag | Dihydropyridinverbindungen, verfahren zu ihrer herstellung und ihre verwendung |
| US4751231A (en) | 1987-09-16 | 1988-06-14 | Merck & Co., Inc. | Substituted thieno[2,3-b]pyrrole-5-sulfonamides as antiglaucoma agents |
| JPH04179949A (ja) | 1990-11-15 | 1992-06-26 | Fuji Photo Film Co Ltd | 新規な色素形成カプラーおよび該カプラーを用いたハロゲン化銀カラー写真感光材料 |
| JP2668003B2 (ja) | 1992-06-12 | 1997-10-27 | ファイザー インク． | ヒトの心臓キマーゼを含むアンギオテンシンｉキマーゼに関する阻害剤 |
| ES2081747B1 (es) | 1993-09-07 | 1997-01-16 | Esteve Labor Dr | Amidas derivadas de tienopirroles, su preparacion y su aplicacion como medicamentos. |
| ATE243196T1 (de) | 1994-03-09 | 2003-07-15 | Novo Nordisk As | Piperidine und pyrrolidine |
| US5863903A (en) | 1994-03-09 | 1999-01-26 | Novo Nordisk A/S | Use of hydroxy alkyl piperidine and pyrrolidine compounds to treat diabetes |
| FR2723739B1 (fr) | 1994-08-19 | 1997-02-14 | Sanofi Sa | Derives de glycinamide, procedes pour leur preparation et medicaments les contenant. |
| DE4445968A1 (de) | 1994-12-22 | 1996-06-27 | Bayer Ag | Verwendung von Sulfonylguanazinen |
| AP624A (en) | 1995-06-06 | 1997-12-19 | Pfizer | Substituted n-(indole-2-carbonyl)-b- alanimamides and derivatives as antidiabetic agents. |
| ES2164151T3 (es) | 1995-06-06 | 2002-02-16 | Pfizer | N-(indol-2-carbonil)glicinamidas sustituidas y derivados como inhibidores de la glucogeno fosforilasa. |
| CA2342471C (en) | 1995-06-06 | 2002-10-29 | Judith L. Treadway | Heterocyclecarbonylmethyl amine intermediates |
| EP1040827A3 (en) | 1995-09-08 | 2000-10-11 | Novo Nordisk A/S | Use of 2-alkylpyrrolidines for the treatment of diabetes |
| AU2090897A (en) | 1996-02-29 | 1997-09-16 | Mikael Bols | Hydroxyhexahydropyridazines |
| US6069162A (en) | 1996-05-27 | 2000-05-30 | Fujisawa Pharmaceutical Co., Ltd. | Indolyl and benzofuranyl carboxamides as inhibitors of nitric oxide production |
| US5952322A (en) * | 1996-12-05 | 1999-09-14 | Pfizer Inc. | Method of reducing tissue damage associated with non-cardiac ischemia using glycogen phosphorylase inhibitors |
| WO1998027108A2 (en) | 1996-12-16 | 1998-06-25 | Fujisawa Pharmaceutical Co., Ltd. | New amide compounds and their use as nitric oxide synthase inhibitors |
| EP0973738A1 (en) | 1997-03-07 | 2000-01-26 | Novo Nordisk A/S | Novel heterocyclic compounds |
| EP0983239A1 (en) | 1997-05-06 | 2000-03-08 | Novo Nordisk A/S | Novel heterocyclic compounds |
| UA57811C2 (uk) | 1997-11-21 | 2003-07-15 | Пфайзер Продактс Інк. | Фармацевтична композиція, що містить інгібітор альдозоредуктази та інгібітор глікогенфосфорилази (варіанти), комплект, який її включає, та способи лікування ссавців зі станом інсулінорезистентності |
| MY153569A (en) | 1998-01-20 | 2015-02-27 | Mitsubishi Tanabe Pharma Corp | Inhibitors of ?4 mediated cell adhesion |
| US5998463A (en) * | 1998-02-27 | 1999-12-07 | Pfizer Inc | Glycogen phosphorylase inhibitors |
| EP0978279A1 (en) | 1998-08-07 | 2000-02-09 | Pfizer Products Inc. | Inhibitors of human glycogen phosphorylase |
| DE60045474D1 (de) | 1999-01-13 | 2011-02-17 | Univ New York State Res Found | Neues verfahren zum erschaffen von proteinkinase-inhibitoren |
| AU2535700A (en) | 1999-02-12 | 2000-08-29 | Novo Nordisk A/S | Use of pyrrolidine derivatives for the manufacture of a pharmaceutical composition for the treatment or prophylaxis of obesity or appetite regulation |
| US6043091A (en) | 1999-07-19 | 2000-03-28 | Isis Pharmaceuticals Inc. | Antisense modulation of liver glycogen phosphorylase expression |
| JP3795305B2 (ja) | 1999-07-19 | 2006-07-12 | 田辺製薬株式会社 | 医薬組成物 |
| EP1220832A1 (en) | 1999-09-29 | 2002-07-10 | Novo Nordisk A/S | Novel aromatic compounds |
| PT1088824E (pt) * | 1999-09-30 | 2004-04-30 | Pfizer Prod Inc | Pirrolil-amidas biciclicas como inibidores de glicogenio-fosforilase |
| SE9903998D0 (sv) | 1999-11-03 | 1999-11-03 | Astra Ab | New compounds |
| CZ20021548A3 (cs) | 1999-11-05 | 2002-10-16 | Societe De Conseils De Recherches Et D'application | Nové heterocyklické sloučeniny a jejich pouľití jako léků |
| EP1741445B1 (en) | 2000-01-21 | 2013-08-14 | Novartis AG | Combinations comprising dipeptidylpeptidase-IV inhibitors and antidiabetic agents |
| CO5271699A1 (es) | 2000-01-24 | 2003-04-30 | Pfizer Prod Inc | Procedimiento para el tratamiento de cardiomiopatia utilizando inhibidores de la glucogeno fosforilasa |
| US6555569B2 (en) | 2000-03-07 | 2003-04-29 | Pfizer Inc. | Use of heteroaryl substituted N-(indole-2-carbonyl-) amides for treatment of infection |
| US6395767B2 (en) | 2000-03-10 | 2002-05-28 | Bristol-Myers Squibb Company | Cyclopropyl-fused pyrrolidine-based inhibitors of dipeptidyl peptidase IV and method |
| PE20011184A1 (es) | 2000-03-16 | 2001-11-15 | Pfizer Prod Inc | Composiciones farmaceuticas de inhibidores de la glucogeno-fosforilasa |
| AR028253A1 (es) | 2000-03-16 | 2003-04-30 | Pfizer Prod Inc | Inhibidores de la glucogeno fosforilasa |
| EP1136071A3 (en) | 2000-03-22 | 2003-03-26 | Pfizer Products Inc. | Use of glycogen phosphorylase inhibitors |
| EP1145717B1 (en) | 2000-04-13 | 2004-05-12 | Pfizer Products Inc. | Synergistic effect of glyburide and milrinone |
| TR200401029T4 (tr) | 2000-06-09 | 2004-06-21 | Aventis Pharma Deutschland Gmbh | Asilfenil-üre türevleri, imalat yöntemleri ve ilaç maddesi olarak kullanımları |
| US20020013334A1 (en) | 2000-06-15 | 2002-01-31 | Robl Jeffrey A. | HMG-CoA reductase inhibitors and method |
| US20020028826A1 (en) | 2000-06-15 | 2002-03-07 | Robl Jeffrey A. | HMG-CoA reductase inhibitors and method |
| IL144507A0 (en) | 2000-07-31 | 2002-05-23 | Pfizer Prod Inc | Use of glycogen phosphorylase inhibitors to inhibit tumor growth |
| GB0021831D0 (en) * | 2000-09-06 | 2000-10-18 | Astrazeneca Ab | Chemical compounds |
| AU2001288110A1 (en) | 2000-09-27 | 2002-04-08 | Takeda Chemical Industries Ltd. | Spiro compounds |
| HU227197B1 (en) | 2000-10-24 | 2010-10-28 | Richter Gedeon Nyrt | Nmda receptor antagonist carboxylic acid amide derivatives and pharmaceutical compositions containing them |
| US6933317B2 (en) | 2000-11-01 | 2005-08-23 | Shionogi & Co. Ltd. | PGD2 receptor antagonistic pharmaceutical compositions |
| AU2002256053A1 (en) | 2001-04-04 | 2002-10-21 | Genzyme Corporation | Novel bgp compounds for therapy and diagnosis and methods for using same |
| PE20021091A1 (es) | 2001-05-25 | 2003-02-04 | Aventis Pharma Gmbh | Derivados de fenilurea sustituidos con carbonamida y procedimiento para su preparacion |
| US7144863B2 (en) | 2001-06-01 | 2006-12-05 | Eli Lilly And Company | GLP-1 formulations with protracted time action |
| WO2003037864A1 (en) | 2001-10-29 | 2003-05-08 | Japan Tobacco Inc. | Indole compound and medicinal use thereof |
| US20050009815A1 (en) | 2001-11-27 | 2005-01-13 | Devita Robert J. | 4-Aminoquinoline compounds |
| MXPA03000966A (es) | 2002-02-28 | 2003-09-04 | Pfizer Prod Inc | Agentes antidiabeticos. |
| GB0205165D0 (en) | 2002-03-06 | 2002-04-17 | Astrazeneca Ab | Chemical compounds |
| GB0205162D0 (en) | 2002-03-06 | 2002-04-17 | Astrazeneca Ab | Chemical compounds |
| GB0205175D0 (en) | 2002-03-06 | 2002-04-17 | Astrazeneca Ab | Chemical compounds |
| GB0205176D0 (en) | 2002-03-06 | 2002-04-17 | Astrazeneca Ab | Chemical compounds |
| GB0205166D0 (en) | 2002-03-06 | 2002-04-17 | Astrazeneca Ab | Chemical compounds |
| AU2003227360A1 (en) | 2002-04-25 | 2003-11-10 | Yamanouchi Pharmaceutical Co., Ltd. | Novel amide derivatives or salts thereof |
| US7057046B2 (en) | 2002-05-20 | 2006-06-06 | Bristol-Myers Squibb Company | Lactam glycogen phosphorylase inhibitors and method of use |
| GB0222912D0 (en) | 2002-10-03 | 2002-11-13 | Astrazeneca Ab | Novel process and intermediates |
| GB0222909D0 (en) | 2002-10-03 | 2002-11-13 | Astrazeneca Ab | Novel process and intermediates |
| WO2004041780A2 (en) | 2002-11-07 | 2004-05-21 | Pfizer Products Inc. | N-(indole-2-carbonyl) amides as anti-diabetic agents |
| US7098235B2 (en) | 2002-11-14 | 2006-08-29 | Bristol-Myers Squibb Co. | Triglyceride and triglyceride-like prodrugs of glycogen phosphorylase inhibiting compounds |
| JP2004196702A (ja) | 2002-12-18 | 2004-07-15 | Yamanouchi Pharmaceut Co Ltd | 新規なアミド誘導体又はその塩 |
| US7501440B2 (en) | 2003-03-07 | 2009-03-10 | Sanofi-Aventis Deutschland Gmbh | Substituted benzoylureidopyridylpiperidine-and-pyrrolidinecarboxylic acid derivatives, processes for preparing them and their use |
| WO2004092158A1 (en) | 2003-04-17 | 2004-10-28 | Pfizer Products Inc. | Carboxamide derivatives as anti-diabetic agents |
| MXPA05011702A (es) | 2003-04-30 | 2006-01-23 | Pfizer Prod Inc | Agentes antidiabeticos. |
| WO2004113345A1 (ja) | 2003-06-20 | 2004-12-29 | Japan Tobacco Inc. | 縮合ピロール化合物及びその医薬用途 |
| GB0318464D0 (en) | 2003-08-07 | 2003-09-10 | Astrazeneca Ab | Chemical compounds |
| GB0318463D0 (en) | 2003-08-07 | 2003-09-10 | Astrazeneca Ab | Chemical compounds |
| GB0319690D0 (en) | 2003-08-22 | 2003-09-24 | Astrazeneca Ab | Chemical compounds |
| GB0319759D0 (en) | 2003-08-22 | 2003-09-24 | Astrazeneca Ab | Chemical compounds |
| WO2005020985A1 (en) | 2003-08-29 | 2005-03-10 | Astrazeneca Ab | Indolamide derivatives which possess glycogen phosphorylase inhibitory activity |
| WO2005020986A1 (en) | 2003-08-29 | 2005-03-10 | Astrazeneca Ab | Heterocyclic amide derivatives which posses glycogen phosphorylase inhibitory activity |
| GB0320422D0 (en) | 2003-08-30 | 2003-10-01 | Astrazeneca Ab | Chemical compounds |
-
2002
- 2002-03-06 GB GBGB0205170.4A patent/GB0205170D0/en not_active Ceased
-
2003
- 2003-03-04 JP JP2003572999A patent/JP2005524669A/ja not_active Withdrawn
- 2003-03-04 ES ES03743418T patent/ES2276092T3/es not_active Expired - Lifetime
- 2003-03-04 DK DK03743418T patent/DK1483271T3/da active
- 2003-03-04 CN CNB038051249A patent/CN1307183C/zh not_active Expired - Fee Related
- 2003-03-04 NZ NZ534684A patent/NZ534684A/en unknown
- 2003-03-04 MX MXPA04008611A patent/MXPA04008611A/es active IP Right Grant
- 2003-03-04 PT PT03743418T patent/PT1483271E/pt unknown
- 2003-03-04 PL PL03372772A patent/PL372772A1/xx not_active Application Discontinuation
- 2003-03-04 RU RU2004125145/04A patent/RU2004125145A/ru not_active Application Discontinuation
- 2003-03-04 IL IL16380203A patent/IL163802A0/xx unknown
- 2003-03-04 DE DE60309849T patent/DE60309849T2/de not_active Expired - Fee Related
- 2003-03-04 WO PCT/GB2003/000875 patent/WO2003074531A1/en not_active Ceased
- 2003-03-04 AU AU2003209445A patent/AU2003209445A1/en not_active Abandoned
- 2003-03-04 BR BR0308145-1A patent/BR0308145A/pt not_active IP Right Cessation
- 2003-03-04 EP EP03743418A patent/EP1483271B1/en not_active Expired - Lifetime
- 2003-03-04 AT AT03743418T patent/ATE346072T1/de not_active IP Right Cessation
- 2003-03-04 KR KR10-2004-7013865A patent/KR20040091101A/ko not_active Ceased
- 2003-03-04 CA CA002477125A patent/CA2477125A1/en not_active Abandoned
- 2003-03-04 US US10/506,746 patent/US7122567B2/en not_active Expired - Fee Related
- 2003-03-05 TW TW092104655A patent/TW200306176A/zh unknown
- 2003-03-06 AR ARP030100766A patent/AR038886A1/es unknown
-
2004
- 2004-08-23 ZA ZA200406685A patent/ZA200406685B/en unknown
- 2004-09-01 IS IS7433A patent/IS7433A/is unknown
- 2004-09-24 NO NO20044033A patent/NO20044033L/no not_active Application Discontinuation
Also Published As
| Publication number | Publication date |
|---|---|
| TW200306176A (en) | 2003-11-16 |
| ATE346072T1 (de) | 2006-12-15 |
| US20050131052A1 (en) | 2005-06-16 |
| US7122567B2 (en) | 2006-10-17 |
| DE60309849T2 (de) | 2007-06-14 |
| ES2276092T3 (es) | 2007-06-16 |
| GB0205170D0 (en) | 2002-04-17 |
| PT1483271E (pt) | 2007-02-28 |
| BR0308145A (pt) | 2004-12-07 |
| EP1483271B1 (en) | 2006-11-22 |
| NZ534684A (en) | 2006-02-24 |
| KR20040091101A (ko) | 2004-10-27 |
| PL372772A1 (en) | 2005-08-08 |
| DE60309849D1 (de) | 2007-01-04 |
| CN1307183C (zh) | 2007-03-28 |
| RU2004125145A (ru) | 2005-06-10 |
| NO20044033L (no) | 2004-11-25 |
| CA2477125A1 (en) | 2003-09-12 |
| EP1483271A1 (en) | 2004-12-08 |
| MXPA04008611A (es) | 2004-12-06 |
| DK1483271T3 (da) | 2007-02-19 |
| ZA200406685B (en) | 2005-10-31 |
| JP2005524669A (ja) | 2005-08-18 |
| AU2003209445A1 (en) | 2003-09-16 |
| WO2003074531A1 (en) | 2003-09-12 |
| HK1070365A1 (en) | 2005-06-17 |
| CN1639167A (zh) | 2005-07-13 |
| IS7433A (is) | 2004-09-01 |
| IL163802A0 (en) | 2005-12-18 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| AR038886A1 (es) | Amidas heterociclicas, inhibidores de actividad de glucogeno fosforilasa | |
| AR038889A1 (es) | Amidas heterociclicas | |
| AR038888A1 (es) | Amidas heterociclicas | |
| AR038887A1 (es) | Amidas heterociclicas | |
| EA199800404A1 (ru) | Производные 1-(1,2-дизамещенный пиперидинил)-4-замещенного пиперазина | |
| RU2004109812A (ru) | Ингибиторы цистеинпротеазы 2-циано-4-аминопиримидинового строения с ингибирующим действием на катепсин к для лечения воспалительных и других заболеваний | |
| AR046779A1 (es) | Derivados de pirazol, metodos para su preparacion y usos de los mismos en la fabricacion de composiciones farmaceuticas y medicamentos que los contienen con actividad inhibitoria de trk para el tratamiento o profilaxis del cancer. | |
| AR046244A1 (es) | Activadores de glucoquinasa heteroaromaticos de seis miembros 5- sustituidos | |
| AR087046A2 (es) | Compuestos derivados de 4-oxoquinolina | |
| MA27626A1 (fr) | Nouveaux derives de 2-pyridinecarboxamide | |
| TW200800949A (en) | Macrocylic inhibitors of hepatitis C virus | |
| NO974586L (no) | Nye substituerte bifenyl- eller fenylpyridinforbindelser, fremgangsmåte for deres fremstilling og farmasöytiske sammensetninger som inneholder dem | |
| CO5700824A2 (es) | Nuevos compuestos heterociclicos utiles para el tratamiento de desordenes inflamatorios y alergicos: proceso para su preparacion y composiciones farmaceuticas que los contienen | |
| AR038000A1 (es) | Compuesto derivado de tien[2,3-d]pirimidin-2,4(1h,3h)-diona, composicion farmaceutica, proceso para su preparacion y su uso en la fabricacion de un medicamento | |
| CO4950625A1 (es) | Derivados de nicotinamida | |
| NO20025641D0 (no) | Substituerte 1-aminoalkyl-laktamer og deres anvendelse som muscarin-reseptor-antagonister | |
| CO5590957A2 (es) | Amino-1,3,5-triazinas sustituidas en n con radicales biciclicos quirales, procedimiento para su preparacion, composiciones de las mismas y su uso como herbicidas y reguladores del crecimiento de las plantas | |
| AR109868A1 (es) | Derivados heterocíclicos activos como plaguicidas con sustituyentes con azufre e hidroxilamina | |
| TW200716528A (en) | Cyclopropanecarboxamide derivatives | |
| NO20025640D0 (no) | Substituerte 1-aminoalkyl-laktamer og deres anvendelse som muscarin-reseptor-antagonister | |
| UY24482A1 (es) | Quinoxalinadionas | |
| NO952208L (no) | Amin-derivater | |
| CO5690551A2 (es) | Derivados de tetrazol y metodos para el tratamiento con los mismos de trastornos relacionados con el metabolismo | |
| JP2005525364A5 (es) | ||
| RU2009114731A (ru) | Производное пиразолопиримидина |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FB | Suspension of granting procedure |