AR033375A1 - 4h-benzo[1,4] oxazin-3-onas, composicion farmaceutica que las comprende, uso de las mismas para preparar medicamentos y proceso para preparar una composicion farmaceutica - Google Patents
4h-benzo[1,4] oxazin-3-onas, composicion farmaceutica que las comprende, uso de las mismas para preparar medicamentos y proceso para preparar una composicion farmaceuticaInfo
- Publication number
- AR033375A1 AR033375A1 ARP010102283A ARP010102283A AR033375A1 AR 033375 A1 AR033375 A1 AR 033375A1 AR P010102283 A ARP010102283 A AR P010102283A AR P010102283 A ARP010102283 A AR P010102283A AR 033375 A1 AR033375 A1 AR 033375A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- hydrogen
- heterocyclyl
- group
- nr1r2
- Prior art date
Links
- 239000008194 pharmaceutical composition Substances 0.000 title abstract 4
- 239000003814 drug Substances 0.000 title abstract 2
- 229940079593 drug Drugs 0.000 title 1
- 229910052739 hydrogen Inorganic materials 0.000 abstract 11
- 239000001257 hydrogen Substances 0.000 abstract 11
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 10
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 9
- 125000003118 aryl group Chemical group 0.000 abstract 8
- 125000000623 heterocyclic group Chemical group 0.000 abstract 8
- 125000000008 (C1-C10) alkyl group Chemical group 0.000 abstract 5
- 229910052736 halogen Inorganic materials 0.000 abstract 4
- 150000002367 halogens Chemical class 0.000 abstract 4
- 125000000217 alkyl group Chemical group 0.000 abstract 3
- 125000002877 alkyl aryl group Chemical group 0.000 abstract 2
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical group [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 abstract 2
- RTZKZFJDLAIYFH-UHFFFAOYSA-N ether Substances CCOCC RTZKZFJDLAIYFH-UHFFFAOYSA-N 0.000 abstract 2
- 229910052760 oxygen Inorganic materials 0.000 abstract 2
- 239000001301 oxygen Substances 0.000 abstract 2
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 abstract 1
- MZAGXDHQGXUDDX-JSRXJHBZSA-N (e,2z)-4-ethyl-2-hydroxyimino-5-nitrohex-3-enamide Chemical compound [O-][N+](=O)C(C)C(/CC)=C/C(=N/O)/C(N)=O MZAGXDHQGXUDDX-JSRXJHBZSA-N 0.000 abstract 1
- QRCGFTXRXYMJOS-UHFFFAOYSA-N 4h-1,4-benzoxazin-3-one Chemical compound C1=CC=C2NC(=O)COC2=C1 QRCGFTXRXYMJOS-UHFFFAOYSA-N 0.000 abstract 1
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 abstract 1
- 208000008589 Obesity Diseases 0.000 abstract 1
- 101150023417 PPARG gene Proteins 0.000 abstract 1
- 108090000029 Peroxisome Proliferator-Activated Receptors Proteins 0.000 abstract 1
- 102000003728 Peroxisome Proliferator-Activated Receptors Human genes 0.000 abstract 1
- 239000005557 antagonist Substances 0.000 abstract 1
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 abstract 1
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 abstract 1
- 150000002148 esters Chemical group 0.000 abstract 1
- 238000004519 manufacturing process Methods 0.000 abstract 1
- 125000001160 methoxycarbonyl group Chemical group [H]C([H])([H])OC(*)=O 0.000 abstract 1
- 239000000203 mixture Substances 0.000 abstract 1
- 235000020824 obesity Nutrition 0.000 abstract 1
- 230000003287 optical effect Effects 0.000 abstract 1
- 150000002923 oximes Chemical class 0.000 abstract 1
- 239000000651 prodrug Chemical group 0.000 abstract 1
- 229940002612 prodrug Drugs 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 208000001072 type 2 diabetes mellitus Diseases 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D265/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom and one oxygen atom as the only ring hetero atoms
- C07D265/28—1,4-Oxazines; Hydrogenated 1,4-oxazines
- C07D265/34—1,4-Oxazines; Hydrogenated 1,4-oxazines condensed with carbocyclic rings
- C07D265/36—1,4-Oxazines; Hydrogenated 1,4-oxazines condensed with carbocyclic rings condensed with one six-membered ring
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
- C07F9/02—Phosphorus compounds
- C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
- C07F9/6527—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having nitrogen and oxygen atoms as the only ring hetero atoms
- C07F9/6533—Six-membered rings
- C07F9/65335—Six-membered rings condensed with carbocyclic rings or carbocyclic ring systems
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Molecular Biology (AREA)
- Biochemistry (AREA)
- Obesity (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Pharmacology & Pharmacy (AREA)
- Hematology (AREA)
- General Chemical & Material Sciences (AREA)
- Diabetes (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
4H-benzo[1,4]oxazin-3-ona de Formula (1) o un isomero optico, enantiomero, diastereomero, racemato o mezcla racémica de la misma, éster, forma prodroga, o una sal farmacéuticamente aceptable de la misma, utiles como antagonistas del receptor activado por el proliferador del peroxisoma (PPARg), composiciones farmacéuticas que las comprenden, uso de las mismas para preparar medicamentos para el tratamiento de condiciones tales como la NIDDM y la obesidad, y un proceso para preparar una composicion farmacéutica. A se selecciona entre arilo, heterociclilo y alquilo de C1-10, estando dicho arilo, heterociclilo y alquilo de C1-10 opcionalmente sustituido con uno o más miembros seleccionados del grupo integrado por halogeno, OH, arilo, cicloalquilo de C3-8, alquilo de C1-10 sustituido con un halogeno, C1-10 alquil éter, heterociclilo, carbonilo, oxima, -C(NNR3R4)R1, -COOR1, -CONR1R2, -OC(O)R1, -OC(O)OR1, -OC(O)NR1R2, -NR1R2, -NR3C(O)R1, -NR3C(O)OR1 y -NR3C(O)NR1R2, en los cuales R1 y R2 se seleccionan independientemente entre hidrogeno, alquilo de C1-10, arilo, heterociclilo y alquilarilo, o R1 y R2 pueden tomarse conjuntamente para formar un anillo de entre 5 y 10 miembros; y R3 y R4 se seleccionan independientemente entre hidrogeno, alquilo de C1-10, arilo, heterociclilo y alquilarilo, -C(O)R1 o -C(O)NR1R2; Z1 se selecciona entre hidrogeno, alquilo de C1-6, arilo, heterociclilo, COOR1, CONR1R2, OH, C1-6 alquil éter, OC(O)R1, -OC(O)OR1, -OC(O)NR1R2, -NR1R2, -NR3C(O)R1, -NR3C(O)OR1, -NR3C(O)NR1R2, halogeno, -C(O)R1, -C(NR3)R1, -C(NOR3)R1 y ûC(NNR3R4)R1; Z2 se selecciona entre hidrogeno, halogeno, alquilo de C1-6; Z1 y Z2 pueden formar conjuntamente un anillo aromático condensado; n es un numero entero entre 0 y 3; G se selecciona entre -COOR1, -C(O)COOR1, -CONR1R2, -CF3, -P(O)(OR1)(OR2), -S-R3, y el grupo de formula (2) donde R5 y R6 son independientemente hidrogeno o alquilo de C1-6; R7 es hidrogeno, alquilo de C1-6 o -C(O)R5; R8 se selecciona del grupo integrado por hidrogeno, alquilo de C1-6 y alquilo de C1-6 sustituido; y B es oxígeno o -NR5; E se selecciona entre hidrogeno, alquilo de C1-6 y un grupo de formula (3) y X es hidrogeno u oxígeno, con la restriccion de que cuando E es hidrogeno y G es -COOH, -COOCH3 o un grupo de formula (4) o (5) A se selecciona del grupo integrado por arilo, heterociclilo, alquilo de C1-6 sustituido y alquilo de C7-10, siempre que cuando X es hidrogeno, n es 1 y G es un grupo de formula (6), A se selecciona del grupo integrado por heterociclilo y alquilo de C7-10.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US20386000P | 2000-05-12 | 2000-05-12 | |
| US09/854,302 US6555536B2 (en) | 2000-05-12 | 2001-05-11 | Biologically active 4H-benzo [1,4]oxazin-3-ones |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR033375A1 true AR033375A1 (es) | 2003-12-17 |
Family
ID=26898967
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP010102283A AR033375A1 (es) | 2000-05-12 | 2001-05-14 | 4h-benzo[1,4] oxazin-3-onas, composicion farmaceutica que las comprende, uso de las mismas para preparar medicamentos y proceso para preparar una composicion farmaceutica |
Country Status (12)
| Country | Link |
|---|---|
| US (1) | US6555536B2 (es) |
| EP (1) | EP1280784B1 (es) |
| AR (1) | AR033375A1 (es) |
| AT (1) | ATE365725T1 (es) |
| AU (1) | AU2001263083A1 (es) |
| CY (1) | CY1106863T1 (es) |
| DE (1) | DE60129123T2 (es) |
| DK (1) | DK1280784T3 (es) |
| ES (1) | ES2288957T3 (es) |
| MY (1) | MY141659A (es) |
| PT (1) | PT1280784E (es) |
| WO (1) | WO2001087862A2 (es) |
Families Citing this family (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7041691B1 (en) | 1999-06-30 | 2006-05-09 | Amgen Inc. | Compounds for the modulation of PPARγ activity |
| US6908908B2 (en) * | 2000-05-12 | 2005-06-21 | Ortho-Mcneil Pharmaceutical, Inc. | Biologically active 4H-benzo [1,4] oxazin-3-ones |
| MXPA03011558A (es) * | 2001-06-12 | 2004-03-26 | Wellstat Therapeutics Corp | Compuestos para el tratamiento de desordenes metabolicos. |
| AU2003282920A1 (en) | 2002-10-04 | 2004-05-04 | Bristol-Myers Squibb Company | Hydantoin derivatives as inhibitors of matrix metalloproteinases and/or tnf-alpha converting enzyme (tace) |
| EP1829863A4 (en) * | 2004-11-26 | 2009-04-22 | Takeda Pharmaceutical | ARYLALCANOIC ACID DERIVATIVE |
| NZ570100A (en) * | 2006-02-28 | 2011-01-28 | Wellstat Therapeutics Corp | Compounds for the treatment of metabolic disorders |
| KR20090066289A (ko) | 2006-09-08 | 2009-06-23 | 로드아일랜드하스피틀 | 알코올 유발성 뇌 질환의 치료, 예방 및 역행 |
Family Cites Families (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5089514A (en) | 1990-06-14 | 1992-02-18 | Pfizer Inc. | 3-coxazolyl [phenyl, chromanyl or benzofuranyl]-2-hydroxypropionic acid derivatives and analogs as hypoglycemic agents |
| WO1996004261A1 (en) | 1994-07-29 | 1996-02-15 | Smithkline Beecham Plc | Benzoxazoles and pryridine derivatives useful in the treatment of the type ii diabetes |
| JPH0912575A (ja) * | 1995-06-28 | 1997-01-14 | Sankyo Co Ltd | ベンゾオキサジンおよびベンゾチアジン誘導体 |
| US5696117A (en) * | 1995-11-07 | 1997-12-09 | Ortho Pharmaceutical Corporation | Benzoxazine antimicrobial agents |
| US5707990A (en) | 1996-01-30 | 1998-01-13 | Ortho Pharmaceutical Corporation | 2-substituted amino and thio alkyl benzoxazine antimicrobial agents |
| PL341795A1 (en) * | 1998-05-27 | 2001-05-07 | Reddy Research Foundation | Bicycle compounds, process for obtaining them and pharmacological compositions containing such compounds |
-
2001
- 2001-05-11 EP EP01937335A patent/EP1280784B1/en not_active Expired - Lifetime
- 2001-05-11 MY MYPI20012191A patent/MY141659A/en unknown
- 2001-05-11 PT PT01937335T patent/PT1280784E/pt unknown
- 2001-05-11 AT AT01937335T patent/ATE365725T1/de active
- 2001-05-11 DK DK01937335T patent/DK1280784T3/da active
- 2001-05-11 US US09/854,302 patent/US6555536B2/en not_active Expired - Lifetime
- 2001-05-11 ES ES01937335T patent/ES2288957T3/es not_active Expired - Lifetime
- 2001-05-11 DE DE60129123T patent/DE60129123T2/de not_active Expired - Lifetime
- 2001-05-11 AU AU2001263083A patent/AU2001263083A1/en not_active Abandoned
- 2001-05-11 WO PCT/US2001/015383 patent/WO2001087862A2/en active IP Right Grant
- 2001-05-14 AR ARP010102283A patent/AR033375A1/es unknown
-
2007
- 2007-09-12 CY CY20071101181T patent/CY1106863T1/el unknown
Also Published As
| Publication number | Publication date |
|---|---|
| ES2288957T3 (es) | 2008-02-01 |
| DE60129123D1 (de) | 2007-08-09 |
| ATE365725T1 (de) | 2007-07-15 |
| WO2001087862A2 (en) | 2001-11-22 |
| WO2001087862A3 (en) | 2002-05-30 |
| MY141659A (en) | 2010-05-31 |
| US20020165228A1 (en) | 2002-11-07 |
| US6555536B2 (en) | 2003-04-29 |
| DE60129123T2 (de) | 2008-02-28 |
| CY1106863T1 (el) | 2012-09-26 |
| DK1280784T3 (da) | 2007-10-29 |
| EP1280784A2 (en) | 2003-02-05 |
| PT1280784E (pt) | 2007-09-03 |
| EP1280784B1 (en) | 2007-06-27 |
| AU2001263083A1 (en) | 2001-11-26 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FB | Suspension of granting procedure |