AR070603A1 - Heterociclos de arilmetilideno 1,3 tiazolicos sustituidos,composiciones farmaceuticas que los contienen y usos de los mismos como agentes analgesicos, para prevenir y/o tratar el dolor y la inflamacion - Google Patents
Heterociclos de arilmetilideno 1,3 tiazolicos sustituidos,composiciones farmaceuticas que los contienen y usos de los mismos como agentes analgesicos, para prevenir y/o tratar el dolor y la inflamacionInfo
- Publication number
- AR070603A1 AR070603A1 ARP090100454A ARP090100454A AR070603A1 AR 070603 A1 AR070603 A1 AR 070603A1 AR P090100454 A ARP090100454 A AR P090100454A AR P090100454 A ARP090100454 A AR P090100454A AR 070603 A1 AR070603 A1 AR 070603A1
- Authority
- AR
- Argentina
- Prior art keywords
- nhc
- aromatic
- nr6c
- cycloalkyl
- alkyl
- Prior art date
Links
- 206010061218 Inflammation Diseases 0.000 title 1
- 239000000730 antalgic agent Substances 0.000 title 1
- 230000004054 inflammatory process Effects 0.000 title 1
- 239000008194 pharmaceutical composition Substances 0.000 title 1
- 125000003118 aryl group Chemical group 0.000 abstract 8
- 125000000217 alkyl group Chemical group 0.000 abstract 5
- 150000001413 amino acids Chemical class 0.000 abstract 4
- 210000004899 c-terminal region Anatomy 0.000 abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 2
- 229910052736 halogen Inorganic materials 0.000 abstract 2
- 150000002367 halogens Chemical class 0.000 abstract 2
- 125000006652 (C3-C12) cycloalkyl group Chemical group 0.000 abstract 1
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 abstract 1
- -1 -C2-8 alkenyl Chemical group 0.000 abstract 1
- 125000004649 C2-C8 alkynyl group Chemical group 0.000 abstract 1
- 101100516563 Caenorhabditis elegans nhr-6 gene Proteins 0.000 abstract 1
- 125000003342 alkenyl group Chemical group 0.000 abstract 1
- 125000005119 alkyl cycloalkyl group Chemical group 0.000 abstract 1
- 125000000304 alkynyl group Chemical group 0.000 abstract 1
- 125000003710 aryl alkyl group Chemical group 0.000 abstract 1
- 125000004429 atom Chemical group 0.000 abstract 1
- 125000004432 carbon atom Chemical group C* 0.000 abstract 1
- 125000000623 heterocyclic group Chemical group 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
- 150000003839 salts Chemical class 0.000 abstract 1
- 229910052717 sulfur Inorganic materials 0.000 abstract 1
Classifications
-
- 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
- C07F9/6558—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system
- C07F9/65583—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system each of the hetero rings containing nitrogen as ring hetero atom
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/04—Centrally acting analgesics, e.g. opioids
-
- 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]
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D263/00—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
- C07D263/02—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings
- C07D263/30—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
- C07D263/34—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members 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
- C07D263/46—Sulfur atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D263/00—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
- C07D263/02—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings
- C07D263/30—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
- C07D263/34—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members 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
- C07D263/48—Nitrogen atoms not forming part of a nitro radical
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
- C07D277/02—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
- C07D277/20—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
- C07D277/32—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members 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
- C07D277/54—Nitrogen and either oxygen or sulfur atoms
-
- 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
- C07D417/04—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 directly linked by a ring-member-to-ring-member bond
-
- 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
- C07D417/06—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 carbon chain containing only aliphatic carbon atoms
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Neurology (AREA)
- Biochemistry (AREA)
- Engineering & Computer Science (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Pain & Pain Management (AREA)
- Molecular Biology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Rheumatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Pyridine Compounds (AREA)
Abstract
Reivindicacion 1: Un compuesto que tiene la siguiente estructura: (1) incluyendo estereoisomeros, estereoisomeros E/Z, sus profármacos y sus sales farmacéuticamente aceptables, en donde: A es -O-, -S-, -SO-, -SO2-, >NR6 o >NC(O)R6; Q es O, S o NR6; Z es -F, -Cl, -NO2, -OR2, -C(O)R6, -C(O)(CR6R6)oNH2, -N(R6)2 o -NHC(O)R6; W es CX o N; X es -H, -F, -Cl, -CN, -OH, -alquilo C2-8, -alquenilo C2-8, -alquinilo C2-8, -cicloalquilo C3-12, -Oalquilo C2-4, -Oalquenilo C2-4, -Oalquinilo C2-4, -N(R6)2, -C(NH)N(R6)2, -O(CH2)nOR6, -C(O)R6, -OC(O)R6, -OC(O)OR6, -OC(O)N(R6)2, -C(O)N(R6)2, -C(O)OR6, -SR6, -S(O)R6, -S(O)2R6, -S(O)2N(R6)2, -NHC(O)R6, -NHS(O)2R6, -NHC(NH)N(R6)2, -NR6C(NH)N(R6)2, -NR6C(NCN)N(R6)2, aminoácido unido en posicion N-terminal o aminoácido unido en posicion C-terminal; Y es -cicloalquilo C3-8, heterociclo aromático o no aromático de 3 a 8 miembros, -SR6, -S(O)R6, -S(O)2R6, -N(R6)2, -NHC(O)R6, -NHS(O)2R6, -NHC(NH)N(R6)2, o -NR6C(NCN)N(R6)2; R1 es -H, halogeno, -alquilo C1-8, -alquenilo C2-8 o -alquinilo C2-8; R2 es -H, -alquilo C1-8, -alquenilo C2-8, alquinilo C2-8, cicloalquilo C3-12, -arilo C6-12, arilalquilo C7-14, -(CH2)nOR6, -C(O)R6, C(O)OR6, -C(O)NHR6, -C(O)N(R6)2, -(CR2AR2B)r2OPO(OR6)2, -(CR2AR2B)r3PO(OR6)2, aminoácido unido en posicion N-terminal o aminoácido unido en posicion C-terminal; cada R2A y R2B es, de modo independiente, H o alquilo C1-5; R3, R4 y R5 son cada uno, de modo independiente, -H, -OH, halogeno, -CN, -NO2, -SH, -alquilo C1-8, -alquenilo C2-8, -alquinilo C2-8, -cicloalquilo C3-12, -arilo C6-12, -arilalquilo C7-14, heterociclo aromático o no aromático de 3 a 9 miembros, -OR6, -N(R6)2, -C(NH)N(R6)2, -O(CH2)nOR6, -C(O)R6, -OC(O)R6, -OC(O)OR6, -OC(O)N(R6)2, -C(O)N(R6)2, -C(O)OR6, -SR6, -SOR6, -S(O)2R6, -NHC(O)R6, -NHS(O)2R6, -NHC(NH)N(R6)2, -NR6C(NH)N(R6)2, -NHC(NCN)N(R6)2, -NR6C(NCN)n(R6)2 o -PO(OR6)2 o R3 y R4, junto con los átomos de carbono a los que cada uno está unido, se unen para formar un carbonilo o heterocilo aromático o no aromático de 5 a 6 miembros; cada R6 es, de modo independiente, -H, -alquilo C1-8, alkcicloalquilo, alkheterociclilo, -cicloalquilo C3-12, -arilo C6-12, -arilalquilo C7-14, heterociclo aromático o no aromático de 3 a 9 miembros, -alquenilo C2-8 o -alquinilo C2-8 o dos R6, junto con el átomo al que cada uno está unido, se unen para formar un carbociclo o heterociclo aromático o no aromática de 3 a 7 miembros; n es 1 o 2; o es un numero entero entre 0-3; cada r2 es un numero entero entre 1-3; cada r3 es un numero entero entre 0-2; en donde R3 no es -Br, cuando R5 es -OH; en donde, cuando W es CX, uno de X y R4 no es -H; y en donde la formula (1) excluye compuestos que tienen la estructura (2).
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US2732908P | 2008-02-08 | 2008-02-08 | |
| US13525308P | 2008-07-17 | 2008-07-17 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR070603A1 true AR070603A1 (es) | 2010-04-21 |
Family
ID=40951764
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP090100454A AR070603A1 (es) | 2008-02-08 | 2009-02-10 | Heterociclos de arilmetilideno 1,3 tiazolicos sustituidos,composiciones farmaceuticas que los contienen y usos de los mismos como agentes analgesicos, para prevenir y/o tratar el dolor y la inflamacion |
Country Status (9)
| Country | Link |
|---|---|
| US (1) | US20090275538A1 (es) |
| EP (1) | EP2250167A4 (es) |
| JP (1) | JP2011511014A (es) |
| AR (1) | AR070603A1 (es) |
| AU (1) | AU2009212072A1 (es) |
| CA (1) | CA2714966A1 (es) |
| CL (1) | CL2009000294A1 (es) |
| TW (1) | TW200934774A (es) |
| WO (1) | WO2009097695A1 (es) |
Families Citing this family (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP5914357B2 (ja) | 2010-01-15 | 2016-05-11 | インセルム（インスティチュート ナショナル デ ラ サンテ エ デ ラ リシェルシェ メディカル） | 自閉症の治療のための化合物 |
| EP2732815A1 (en) | 2012-11-16 | 2014-05-21 | Neurochlore | Modulators of intracellular chloride concentration for treating fragile X syndrome |
| WO2016025778A1 (en) | 2014-08-15 | 2016-02-18 | The Johns Hopkins University | Compositions and methods for treating refractory seizures |
| CN111187217A (zh) * | 2020-02-11 | 2020-05-22 | 威海厚普生物科技有限公司 | 高纯度1-甲基-2-硫代乙内酰脲的制备方法 |
| EP4322952A1 (en) | 2021-04-14 | 2024-02-21 | Inserm (Institut National de la Santé et de la Recherche Scientifique) | Methods and pharmaceutical compositions for treating refractory epilepsy |
| CN113813262B (zh) * | 2021-10-26 | 2023-04-11 | 徐州医科大学 | 一种clp257在制备防治焦虑的药物中的应用 |
Family Cites Families (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AR037714A1 (es) * | 2001-12-06 | 2004-12-01 | Maxia Pharmaceuticals Inc | Derivados de tiazolidinona y oxazolidinona 2-sustituidos para la inhibicion de fosfatasas y el tratamiento de cancer |
| US20050019825A9 (en) * | 2002-03-15 | 2005-01-27 | Qing Dong | Common ligand mimics: pseudothiohydantoins |
| US7344850B2 (en) * | 2003-12-30 | 2008-03-18 | Princeton University | Identification of active-site inhibitors of glycosyltransferases using a generalizable high-throughput screen |
| WO2005082363A1 (en) * | 2004-02-20 | 2005-09-09 | Board Of Regents, The University Of Texas System | Thiazolone compounds for treatment of cancer |
| DE102005024012A1 (de) * | 2005-05-20 | 2006-11-23 | Grünenthal GmbH | Verwendung von 2,5-disubstituierten Thiazol-4-on-Derivaten in Arzneimitteln |
| US7438916B2 (en) * | 2005-10-14 | 2008-10-21 | Virginia Tech Intellectual Properties, Inc. | Therapeutic target for protozoal diseases |
| KR100814109B1 (ko) * | 2006-01-09 | 2008-03-14 | 한국생명공학연구원 | 로다닌 유도체, 이의 제조방법 및 이를 유효성분으로함유하는 약학적 조성물 |
-
2009
- 2009-02-08 CL CL2009000294A patent/CL2009000294A1/es unknown
- 2009-02-09 US US12/368,058 patent/US20090275538A1/en not_active Abandoned
- 2009-02-09 JP JP2010545338A patent/JP2011511014A/ja active Pending
- 2009-02-09 WO PCT/CA2009/000158 patent/WO2009097695A1/en active Application Filing
- 2009-02-09 CA CA2714966A patent/CA2714966A1/en not_active Abandoned
- 2009-02-09 AU AU2009212072A patent/AU2009212072A1/en not_active Abandoned
- 2009-02-09 EP EP09707147A patent/EP2250167A4/en not_active Withdrawn
- 2009-02-09 TW TW098104117A patent/TW200934774A/zh unknown
- 2009-02-10 AR ARP090100454A patent/AR070603A1/es unknown
Also Published As
| Publication number | Publication date |
|---|---|
| CA2714966A1 (en) | 2009-08-13 |
| JP2011511014A (ja) | 2011-04-07 |
| TW200934774A (en) | 2009-08-16 |
| AU2009212072A1 (en) | 2009-08-13 |
| EP2250167A4 (en) | 2012-05-16 |
| EP2250167A1 (en) | 2010-11-17 |
| CL2009000294A1 (es) | 2009-10-23 |
| US20090275538A1 (en) | 2009-11-05 |
| WO2009097695A1 (en) | 2009-08-13 |
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