AR076830A1 - Compuestos de carboxamidas de imidazol como moduladores de trpv3 - Google Patents
Compuestos de carboxamidas de imidazol como moduladores de trpv3Info
- Publication number
- AR076830A1 AR076830A1 ARP090104861A ARP090104861A AR076830A1 AR 076830 A1 AR076830 A1 AR 076830A1 AR P090104861 A ARP090104861 A AR P090104861A AR P090104861 A ARP090104861 A AR P090104861A AR 076830 A1 AR076830 A1 AR 076830A1
- Authority
- AR
- Argentina
- Prior art keywords
- ring
- heteroaryl
- substituted
- cycloalkyl
- alkenyl
- Prior art date
Links
- 102000003568 TRPV3 Human genes 0.000 title abstract 3
- 101150043371 Trpv3 gene Proteins 0.000 title abstract 3
- NMIZONYLXCOHEF-UHFFFAOYSA-N 1h-imidazole-2-carboxamide Chemical class NC(=O)C1=NC=CN1 NMIZONYLXCOHEF-UHFFFAOYSA-N 0.000 title 1
- 125000001072 heteroaryl group Chemical group 0.000 abstract 7
- 125000000623 heterocyclic group Chemical group 0.000 abstract 6
- 125000003342 alkenyl group Chemical group 0.000 abstract 5
- 125000000217 alkyl group Chemical group 0.000 abstract 5
- 125000003118 aryl group Chemical group 0.000 abstract 5
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 5
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 4
- 125000001188 haloalkyl group Chemical group 0.000 abstract 4
- 229910052739 hydrogen Inorganic materials 0.000 abstract 4
- 239000001257 hydrogen Substances 0.000 abstract 4
- 150000002431 hydrogen Chemical class 0.000 abstract 4
- 125000003710 aryl alkyl group Chemical group 0.000 abstract 3
- 150000001875 compounds Chemical class 0.000 abstract 3
- 125000004966 cyanoalkyl group Chemical group 0.000 abstract 3
- 102000011040 TRPV Cation Channels Human genes 0.000 abstract 2
- 108010062740 TRPV Cation Channels Proteins 0.000 abstract 2
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 2
- 125000004122 cyclic group Chemical group 0.000 abstract 2
- 125000000392 cycloalkenyl group Chemical group 0.000 abstract 2
- 125000001316 cycloalkyl alkyl group Chemical group 0.000 abstract 2
- 230000006806 disease prevention Effects 0.000 abstract 2
- 208000035475 disorder Diseases 0.000 abstract 2
- 229910052736 halogen Inorganic materials 0.000 abstract 2
- 150000002367 halogens Chemical class 0.000 abstract 2
- 125000004446 heteroarylalkyl group Chemical group 0.000 abstract 2
- 125000000592 heterocycloalkyl group Chemical group 0.000 abstract 2
- 238000000034 method Methods 0.000 abstract 2
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 abstract 2
- 230000001052 transient effect Effects 0.000 abstract 2
- 125000002373 5 membered heterocyclic group Chemical group 0.000 abstract 1
- 125000004070 6 membered heterocyclic group Chemical group 0.000 abstract 1
- DGAQECJNVWCQMB-PUAWFVPOSA-M Ilexoside XXIX Chemical compound C[C@@H]1CC[C@@]2(CC[C@@]3(C(=CC[C@H]4[C@]3(CC[C@@H]5[C@@]4(CC[C@@H](C5(C)C)OS(=O)(=O)[O-])C)C)[C@@H]2[C@]1(C)O)C)C(=O)O[C@H]6[C@@H]([C@H]([C@@H]([C@H](O6)CO)O)O)O.[Na+] DGAQECJNVWCQMB-PUAWFVPOSA-M 0.000 abstract 1
- WHXSMMKQMYFTQS-UHFFFAOYSA-N Lithium Chemical compound [Li] WHXSMMKQMYFTQS-UHFFFAOYSA-N 0.000 abstract 1
- ZLMJMSJWJFRBEC-UHFFFAOYSA-N Potassium Chemical compound [K] ZLMJMSJWJFRBEC-UHFFFAOYSA-N 0.000 abstract 1
- 239000003513 alkali Substances 0.000 abstract 1
- 125000004183 alkoxy alkyl group Chemical group 0.000 abstract 1
- 125000003545 alkoxy group Chemical group 0.000 abstract 1
- 125000000304 alkynyl group Chemical group 0.000 abstract 1
- 125000004104 aryloxy group Chemical group 0.000 abstract 1
- 230000015572 biosynthetic process Effects 0.000 abstract 1
- 125000000000 cycloalkoxy group Chemical group 0.000 abstract 1
- 239000000543 intermediate Substances 0.000 abstract 1
- 229910052744 lithium Inorganic materials 0.000 abstract 1
- 229910052757 nitrogen Inorganic materials 0.000 abstract 1
- 125000004433 nitrogen atom Chemical group N* 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 229910052700 potassium Inorganic materials 0.000 abstract 1
- 239000011591 potassium Substances 0.000 abstract 1
- 229940075993 receptor modulator Drugs 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 229910052708 sodium Inorganic materials 0.000 abstract 1
- 239000011734 sodium Substances 0.000 abstract 1
- 238000003786 synthesis reaction Methods 0.000 abstract 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
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- C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
- C07D513/04—Ortho-condensed systems
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Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- General Chemical & Material Sciences (AREA)
- Animal Behavior & Ethology (AREA)
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- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
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- Medicinal Chemistry (AREA)
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- Life Sciences & Earth Sciences (AREA)
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- Psychiatry (AREA)
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- Obesity (AREA)
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- Urology & Nephrology (AREA)
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- Psychology (AREA)
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Abstract
La presente provee un modulador de receptor vaniloide de potencial transitorio (TRPV) de formula (1). En particular, los compuestos aquí descriptos son utiles para el tratamiento o la prevencion de enfermedades, trastornos y/o desordenes modulados por TRPV3. También se proveen los procesos para preparar los compuestos descriptos, los intermediarios usados en su síntesis, sus composiciones farmacéuticas y métodos para el tratamiento o prevencion de enfermedades, trastornos y/o desordenes modulados por TRPV3. Reivindicacion 1: Un compuesto modulador de receptor vaniloide de potencial transitorio (TRPV) caracterizado por estar representado por la formula (1) en donde el anillo de formula (2) es un anillo heterocíclico o heteroaromático de 5 miembros o 6 miembros que contiene uno o dos enlaces dobles, en los que X y Z son elegidos en forma independiente de -N=, y -C(R1)-; e Y es -O-, -S-, =N-, -N(R1)-, -C(R1)=C(R1)-, o -C(R1)=N-; siendo Y -O-, -S- y -N(R1)- cuando el anillo de formula (2) es un anillo de 5 miembros que contiene un doble enlace; y siendo Y -C(R1)=C(R1)- o -C(R1)=N- cuando el anillo de formula (2) es un anillo de 6 miembros que contiene dos enlaces dobles; R1, que puede ser igual o diferente en cada ocurrencia, es independientemente hidrogeno, halogeno, nitro, ciano, alquilo substituido o no substituido, alquenilo, haloalquilo, alcoxi, cicloalquilo, cicloalquiloxi, arilo, ariloxi, arilalquilo, heterociclo, o heteroarilo; R2, que puede ser igual o diferente en cada ocurrencia, se elige en forma independiente del grupo que consiste en nitro, ciano, halogeno, -OR, alquilo substituido o no substituido, alquenilo, haloalquilo, cianoalquilo, cicloalquilo, arilo, anillo heterocíclico, y heteroarilo; R3 y R4, que pueden ser iguales o diferentes, son cada uno, independientemente, hidrogeno, álcali (incluyendo litio, sodio, o potasio), alquilo substituido o no substituido, haloalquilo, cianoalquilo, alquenilo, alquinilo, cicloalquilo, cicloalquenilo, arilo, heteroarilo, heterociclo, -S(O)NR5R6, -S(O)2NR5R6, -S(O)R5 o -S(O)2R5; o R3 y R4, junto con el átomo de nitrogeno al cual están adheridos, pueden formar un anillo cíclico opcionalmente substituido de 4 a 12 miembros; pudiendo el anillo cíclico ser heterociclo o heteroarilo; R se selecciona de hidrogeno, alquilo substituido o no substituido, haloalquilo, cianoalquilo, alquenilo, cicloalquilo, cicloalquilalquilo, alcoxialquilo, arilo, heteroarilo, anillo heterocíclico, arilalquilo, heteroarilalquilo, y heterocicloalquilo; en cada ocurrencia, R5 y R6, que pueden ser iguales o diferentes, son independientemente hidrogeno, alquilo substituido o no substituido, alquenilo, cicloalquilo, cicloalquilalquilo, cicloalquenilo, arilo, arilalquilo, heteroarilo, heteroarilalquilo, heterociclo, o heterocicloalquilo; y m es un entero comprendido en el rango que va de 0 a 5. ambos inclusive; o su sal farmacéuticamente aceptable.
Applications Claiming Priority (8)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| IN2610MU2008 | 2008-12-15 | ||
| US14113308P | 2008-12-29 | 2008-12-29 | |
| IN145MU2009 | 2009-01-22 | ||
| US15024809P | 2009-02-05 | 2009-02-05 | |
| IN1397MU2009 | 2009-06-10 | ||
| US22161509P | 2009-06-30 | 2009-06-30 | |
| IN1730MU2009 | 2009-07-29 | ||
| US23745609P | 2009-08-27 | 2009-08-27 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR076830A1 true AR076830A1 (es) | 2011-07-13 |
Family
ID=42241253
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP090104861A AR076830A1 (es) | 2008-12-15 | 2009-12-15 | Compuestos de carboxamidas de imidazol como moduladores de trpv3 |
Country Status (12)
| Country | Link |
|---|---|
| US (1) | US8318928B2 (es) |
| EP (1) | EP2367825A1 (es) |
| JP (1) | JP2012512151A (es) |
| AR (1) | AR076830A1 (es) |
| AU (1) | AU2009329192A1 (es) |
| CA (1) | CA2746077A1 (es) |
| EA (1) | EA201190004A1 (es) |
| GE (1) | GEP20146099B (es) |
| MX (1) | MX2011006132A (es) |
| NZ (1) | NZ595777A (es) |
| TW (1) | TW201022283A (es) |
| WO (1) | WO2010070452A1 (es) |
Families Citing this family (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2012514577A (ja) * | 2008-12-26 | 2012-06-28 | グレンマーク ファーマシューティカルズ， エセ．アー． | Ｔｒｐｖ３アンタゴニストとしての縮合イミダゾール誘導体 |
| JP2013538800A (ja) * | 2010-08-10 | 2013-10-17 | アッヴィ・インコーポレイテッド | 新規ｔｒｐｖ３モジュレーター |
| WO2012072512A1 (en) * | 2010-11-29 | 2012-06-07 | Glaxo Group Limited | N-cyclobutyl-imidazopyridine or -pyrazolopyridine carboxamides as trpv1 antagonists |
| PH12013501934A1 (en) | 2011-03-18 | 2022-04-08 | Bayer Ip Gmbh | N-(3-carbamoylphenyl)-1h-pyrazole-5-carboxamide derivatives and the use thereof for controlling animal pests |
| US9012651B2 (en) | 2011-03-24 | 2015-04-21 | Abbvie Inc. | TRPV3 modulators |
| US8754101B2 (en) | 2011-04-11 | 2014-06-17 | Glaxo Group Limited | N-cyclobutyl-imidazopyridine-methylamine as TRPV1 antagonists |
| JP2014530911A (ja) | 2011-10-24 | 2014-11-20 | アッヴィ・インコーポレイテッド | Ｔｒｐｖ３モジュレーターとしてのメタノール誘導体 |
| BR112015001201B1 (pt) * | 2012-07-18 | 2022-02-22 | University Of Notre Dame Du Lac | Compostos anti-infecciosos 5,5-heteroaromáticos e composição |
| CN110383066B (zh) * | 2016-12-09 | 2023-03-31 | 戴纳立制药公司 | 化合物、组合物和方法 |
| JP2022500499A (ja) | 2018-09-07 | 2022-01-04 | ピク セラピューティクス， インコーポレイテッド | Ｅｉｆ４ｅ阻害剤およびその使用 |
| NZ790364A (en) | 2020-01-29 | 2025-12-19 | Kamari Pharma Ltd | Compounds and compositions for use in treating skin disorders |
| MX2022010944A (es) | 2020-03-03 | 2022-11-09 | Pic Therapeutics Inc | Inhibidores del factor de iniciacion de traduccion eucariotica 4e (eif4e) y sus usos. |
| WO2023028235A1 (en) | 2021-08-25 | 2023-03-02 | PIC Therapeutics, Inc. | Eif4e inhibitors and uses thereof |
| CN118019739A (zh) | 2021-08-25 | 2024-05-10 | 皮克医疗公司 | Eif4e抑制剂及其用途 |
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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| NO811630L (no) | 1980-05-29 | 1981-11-30 | Bayer Ag | Imidazoazolalkensyreamider, nye mellomprodukter for deres fremstilling, deres fremstilling og deres anvendelse som legemiddel |
| US5204352A (en) | 1987-09-29 | 1993-04-20 | The United States Of America As Represented By The Secretary Of The Army | Compounds exhibiting anti-parasitic activity and a method for their use |
| GB8820231D0 (en) * | 1988-08-25 | 1988-09-28 | Fujisawa Pharmaceutical Co | New benzazole compounds processes for preparation thereof & pharmaceutical composition comprising same |
| JPH02105085A (ja) | 1988-10-14 | 1990-04-17 | Komatsu Ltd | 磁気センサ |
| JPH07242666A (ja) | 1994-03-08 | 1995-09-19 | Fujisawa Pharmaceut Co Ltd | 複素環化合物 |
| WO1999051587A1 (en) | 1998-04-01 | 1999-10-14 | Ono Pharmaceutical Co., Ltd. | Fused thiophene derivatives and drugs containing the same as the active ingredient |
| US20040009537A1 (en) | 2002-01-11 | 2004-01-15 | Jack Roos | Methods of modulating and of identifying agents that modulate intracellular calcium |
| TWI372050B (en) | 2003-07-03 | 2012-09-11 | Astex Therapeutics Ltd | (morpholin-4-ylmethyl-1h-benzimidazol-2-yl)-1h-pyrazoles |
| US20060074124A1 (en) | 2003-09-12 | 2006-04-06 | Andrew Napper | Methods of treating a disorder |
| DE112004003000A5 (de) | 2004-08-18 | 2007-07-26 | Böttcher, Robert, Dr.med. | Einschraubbares enossales Dentalimplantat |
| BRPI0519013A2 (pt) | 2004-12-13 | 2009-11-03 | Lilly Co Eli | composto ou esteroisÈmeros únicos, misturas de esteroisÈmeros, sais, tautÈmeros ou pró-drogas destes farmaceuticamente aceitáveis, composição farmacêutica, e, uso de um composto |
| US7842703B2 (en) | 2005-10-07 | 2010-11-30 | Glenmark Pharmaceuticals S.A. | Substituted benzofused derivatives and their use as vanilloid receptor ligands |
| US7893260B2 (en) | 2005-11-04 | 2011-02-22 | Hydra Biosciences, Inc. | Substituted quinazolin-4-one compounds for antagonizing TRPV3 function |
| WO2008001101A2 (en) | 2006-06-29 | 2008-01-03 | Astex Therapeutics Limited | Pharmaceutical combinations |
| JP5523829B2 (ja) | 2006-06-29 | 2014-06-18 | アステックス、セラピューティックス、リミテッド | 複合薬剤 |
| WO2008012010A1 (en) | 2006-07-27 | 2008-01-31 | Ucb Pharma, S.A. | Fused oxazoles & thiazoles as histamine h3- receptor ligands |
| US7998980B2 (en) | 2006-09-15 | 2011-08-16 | Hydra Biosciences, Inc. | Compounds for modulating TRPV3 function |
| WO2008114006A1 (en) | 2007-03-19 | 2008-09-25 | Astrazeneca Ab | 9-substituted-8-oxo-adenine compounds as toll-like receptor (tlr7) modulators |
| WO2008140750A1 (en) | 2007-05-10 | 2008-11-20 | Hydra Biosciences Inc. | Compounds for modulating trpv3 function |
-
2009
- 2009-12-11 US US12/636,213 patent/US8318928B2/en not_active Expired - Fee Related
- 2009-12-14 TW TW098142756A patent/TW201022283A/zh unknown
- 2009-12-15 GE GEAP200912526A patent/GEP20146099B/en unknown
- 2009-12-15 EP EP09806128A patent/EP2367825A1/en not_active Withdrawn
- 2009-12-15 AR ARP090104861A patent/AR076830A1/es not_active Application Discontinuation
- 2009-12-15 JP JP2011540235A patent/JP2012512151A/ja active Pending
- 2009-12-15 EA EA201190004A patent/EA201190004A1/ru unknown
- 2009-12-15 AU AU2009329192A patent/AU2009329192A1/en not_active Abandoned
- 2009-12-15 MX MX2011006132A patent/MX2011006132A/es unknown
- 2009-12-15 CA CA2746077A patent/CA2746077A1/en not_active Abandoned
- 2009-12-15 WO PCT/IB2009/007951 patent/WO2010070452A1/en not_active Ceased
- 2009-12-15 NZ NZ595777A patent/NZ595777A/xx not_active IP Right Cessation
Also Published As
| Publication number | Publication date |
|---|---|
| US20100152192A1 (en) | 2010-06-17 |
| GEP20146099B (en) | 2014-05-27 |
| AU2009329192A2 (en) | 2012-03-29 |
| TW201022283A (en) | 2010-06-16 |
| AU2009329192A1 (en) | 2011-12-01 |
| NZ595777A (en) | 2013-07-26 |
| EA201190004A1 (ru) | 2012-11-30 |
| US8318928B2 (en) | 2012-11-27 |
| CA2746077A1 (en) | 2010-06-24 |
| MX2011006132A (es) | 2011-09-01 |
| JP2012512151A (ja) | 2012-05-31 |
| EP2367825A1 (en) | 2011-09-28 |
| WO2010070452A1 (en) | 2010-06-24 |
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