AR051294A1 - Derivados heterociclicos y su uso como inhibidores de la estearoil-coa desaturasa - Google Patents
Derivados heterociclicos y su uso como inhibidores de la estearoil-coa desaturasaInfo
- Publication number
- AR051294A1 AR051294A1 ARP050103902A ARP050103902A AR051294A1 AR 051294 A1 AR051294 A1 AR 051294A1 AR P050103902 A ARP050103902 A AR P050103902A AR P050103902 A ARP050103902 A AR P050103902A AR 051294 A1 AR051294 A1 AR 051294A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- independently selected
- rings
- group
- independently
- Prior art date
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- 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
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/4965—Non-condensed pyrazines
- A61K31/497—Non-condensed pyrazines containing further heterocyclic rings
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- 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
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/50—Pyridazines; Hydrogenated pyridazines
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/18—Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
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- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
- A61P15/08—Drugs for genital or sexual disorders; Contraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/04—Antipruritics
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/06—Antipsoriatics
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- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
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- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P31/16—Antivirals for RNA viruses for influenza or rhinoviruses
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- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
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- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D235/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
- C07D235/02—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
- C07D235/04—Benzimidazoles; Hydrogenated benzimidazoles
- C07D235/06—Benzimidazoles; Hydrogenated benzimidazoles with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 2
- C07D235/08—Radicals containing only hydrogen and carbon atoms
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- 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
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Abstract
Métodos para tratar una enfermedad o afeccion medida por la SCD en un mamífero, preferentemente un ser humano. Los métodos comprenden, por ejemplo, administrar a un mamífero que lo necesita un compuesto de formula (1). Se revelan también composiciones farmacéuticas que comprenden los compuestos de formula (1). Reivindicacion 10: Un compuesto de formula (1) caracterizado porque: x y y son cada uno en forma independiente 1, 2 o 3; J y K son cada uno en forma independiente N o C(R11); L es N o C(R4); M es -N= o -C(R4)=; W es un enlace directo, -N(R1)C(O)-, -C(O)N(R1)-, -OC(O)N(R1)-, -N(R1)C(O)N(R1)-, -O-, -N(R1)-, -S(O)t (donde t es 0, 1 o 2), -N(R1)S(O)p- (donde p es 1 o 2), -S(O)pN(R1)- (donde p es 1 o 2), -C(O)-, -OS(O)2N(R1)- , -OC(O)-, -C(O)O-, -N(R1)C(O)O- o -C(R1)2-; V es -N(R1)-, -N(R1)C(O)-, -C(O)-, -C(O)O-, -C(S)-, -C(O)N(R1)-, -S(O)p- 8donde p es 1 o 2), -S(O)pN(R1)- (donde p es 1 o 2), o -C(R10)H-; cada R1 se selecciona en forma independiente el grupo formado por H, C1-12 alquilo, C2-12 hidroxialquilo, C4-12 cicloalquilalquilo y C7-19 aralquilo; R2 se selecciona del grupo formado por C1-12 alquilo, C2-12 alquenilo, C2-12 hidroxialquilo, C2-12 hidroxialquenilo, C2-12alcoxialquilo, C3-12 cicloalquilo, C4-12 cicloalquilalquilo, arilo, C7-19 aralquilo, C3-12 heterociclilo, C3-12 heterociclilalquilo, C1-12 heteroarilo, y C3-12 heteroarilalquilo; o R2 es una estructura de anillos multiples que tiene entre 2 y 4 anillos en donde los anillos se seleccionan en forma independiente del grupo formado por cicloalquilo, heterociclilo, arilo y heteroarilo y donde algunos o todos los anillos pueden estar fusionados entre sí; R3 se selecciona del grupo formado por C1-12 alquilo, C2-12 alquenilo, C2-12 hidroxialquilo, C2-12 hidroxialquenilo, C2-12 alcoxialquilo, C3-12 cicloalquilo, C4-12 cicloalquilalquilo, arilo, C7-19 aralquilo, C3-12 heterociclilo, C3-12 heterociclilalquilo, C1-12 heteroarilo y C3-12 heteroarilalquilo; o R3 es una estructura de anillos multiples que tiene entre 2 y 4 anillos en donde los anillos se seleccionan en forma independiente del grupo formado por cicloalquilo, heterociclilo, arilo y heteroarilo y donde algunos o todos los anillos pueden estar fusionados entre sí; cada R4 se selecciona en forma independiente entre H, F, Cl, C1-12 alquilo, C1-12 alcoxi, haloalquilo, ciano, nitro o -N(R9)2; R5, R5a, R6, R6a, R7, R7a, R8 y R8a se seleccionan cada uno en forma independiente entre H o C1-3 alquilo; o R5 y R5a juntos, R6 y R6a juntos, o R7 y R7a juntos, o R8 y R8a juntos constituyen un grupo oxo, con la salvedad de que cuando V es -CO-, R6 y R6a juntos o R8 y R8a juntos formen un grupo oxo, mientras los restantes R5, R5a, R6, R6a, R7, R7a, R8 y R8a se seleccionan cada uno en forma independiente entre H o alquilo C1-3; o uno de R5, R5a, R6 y R6a junto con uno de R7, R7a, R8 y R8a forma un enlace directo o un puente alquileno, mientras los restantes R5, R5a, R6, R6a, R7, R7a, R8 y R8a se seleccionan cada uno en forma independiente entre H o C1-3 alquilo; cada R9 se selecciona en forma independiente entre H o C1-6 alquilo; R10 es H o C1-3 alquilo; y R11 se selecciona en forma independiente entre H, F, Cl, C1-12 alquilo o C1-12 alcoxi; en forma de uno de sus estereoisomeros, enantiomeros o tautomeros, en forma de mezcla de estereoisomeros, en forma de sal aceptable para uso farmacéutico, o como prodroga del mismo.
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US61164604P | 2004-09-20 | 2004-09-20 |
Publications (1)
Publication Number | Publication Date |
---|---|
AR051294A1 true AR051294A1 (es) | 2007-01-03 |
Family
ID=35623357
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
ARP050103902A AR051294A1 (es) | 2004-09-20 | 2005-09-20 | Derivados heterociclicos y su uso como inhibidores de la estearoil-coa desaturasa |
Country Status (11)
Country | Link |
---|---|
US (2) | US7547698B2 (es) |
EP (1) | EP1804792A1 (es) |
JP (2) | JP5080256B2 (es) |
CN (1) | CN101083986A (es) |
AR (1) | AR051294A1 (es) |
AU (1) | AU2005286790A1 (es) |
BR (1) | BRPI0515477A (es) |
CA (1) | CA2580781A1 (es) |
MX (1) | MX2007003329A (es) |
TW (1) | TW200626148A (es) |
WO (1) | WO2006034312A1 (es) |
Families Citing this family (45)
Publication number | Priority date | Publication date | Assignee | Title |
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US7517884B2 (en) | 1998-03-30 | 2009-04-14 | Kalypsys Inc. | Sulfonyl-substituted bicyclic compounds as modulators of PPAR |
US20050119251A1 (en) * | 2001-12-21 | 2005-06-02 | Jian-Min Fu | Nicotinamide derivatives and their use as therapeutic agents |
BRPI0515500A (pt) | 2004-09-20 | 2008-07-29 | Xenon Pharmaceuticals Inc | derivados piridazina para inibição de estearoil-coa-desaturase |
US7919496B2 (en) | 2004-09-20 | 2011-04-05 | Xenon Pharmaceuticals Inc. | Heterocyclic derivatives for the treatment of diseases mediated by stearoyl-CoA desaturase enzymes |
WO2006034446A2 (en) * | 2004-09-20 | 2006-03-30 | Xenon Pharmaceuticals Inc. | Pyridine derivatives for inhibiting human stearoyl-coa-desaturase |
BRPI0515489A (pt) | 2004-09-20 | 2008-07-29 | Xenon Pharmaceuticals Inc | derivados heterocìclicos e sua utilização como inibidores de estearoil-coa desaturase |
JP5043668B2 (ja) | 2004-09-20 | 2012-10-10 | ゼノン・ファーマシューティカルズ・インコーポレイテッド | 複素環誘導体および治療薬としてのそれらの使用 |
AU2005329423A1 (en) | 2004-09-20 | 2006-09-28 | Xenon Pharmaceuticals Inc. | Heterocyclic derivatives and their use as stearoyl-CoA desaturase inhibitors |
EP1799668A1 (en) * | 2004-09-20 | 2007-06-27 | Xenon Pharmaceuticals Inc. | Heterocyclic derivatives and their use as mediators of stearoyl-coa desaturase |
AR051092A1 (es) * | 2004-09-20 | 2006-12-20 | Xenon Pharmaceuticals Inc | Derivados heterociclicos y su uso como inhibidores de la estearoil-coa |
AU2005307006B2 (en) | 2004-10-29 | 2012-05-03 | Kalypsys, Inc. | Sulfonyl-substituted bicyclic compounds as modulators of PPAR |
CN101208089A (zh) | 2005-06-03 | 2008-06-25 | 泽农医药公司 | 氨基噻唑衍生物作为人硬酯酰-CoA去饱和酶抑制剂 |
JP2008545760A (ja) * | 2005-06-09 | 2008-12-18 | メルク フロスト カナダ リミテツド | ステアロイル−コエンザイムaデルタ−9デサチュラーゼのインヒビターとしてのアザシクロヘキサン誘導体 |
NZ566831A (en) | 2005-10-25 | 2011-09-30 | Kalypsys Inc | Salts of modulators of PPAR and methods of treating metabolic disorders |
WO2007071023A1 (en) | 2005-12-20 | 2007-06-28 | Merck Frosst Canada Ltd. | Heteroaromatic compounds as inhibitors of stearoyl-coenzyme a delta-9 desaturase |
BRPI0712902A2 (pt) | 2006-06-05 | 2018-10-30 | Novartis Ag | compostos orgânicos |
JP2010501567A (ja) | 2006-08-24 | 2010-01-21 | ノバルティス アクチエンゲゼルシャフト | 代謝系、心血管系および他の障害の処置のためのステアロイル−CoA不飽和化酵素(SCD)阻害剤としての2−(ピラジン−2−イル)−チアゾールおよび2−(1H−ピラゾール−3−イル)チアゾール誘導体ならびに関連化合物 |
WO2008044767A1 (fr) * | 2006-10-13 | 2008-04-17 | Takeda Pharmaceutical Company Limited | Dérivé d'amine aromatique et utilisation de celui-ci |
TW200826936A (en) | 2006-12-01 | 2008-07-01 | Merck Frosst Canada Ltd | Azacycloalkane derivatives as inhibitors of stearoyl-coenzyme a delta-9 desaturase |
AR064965A1 (es) | 2007-01-26 | 2009-05-06 | Merck Frosst Canada Inc | Derivados de azacicloalcanos como inhibidores de estearoil - coenzima a delta -9 desaturasa |
US8575167B2 (en) | 2007-02-06 | 2013-11-05 | Takeda Pharmaceutical Company Limited | Spiro compounds having stearoyl-CoA desaturase action |
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-
2005
- 2005-09-20 CA CA002580781A patent/CA2580781A1/en not_active Abandoned
- 2005-09-20 US US11/575,643 patent/US7547698B2/en not_active Expired - Fee Related
- 2005-09-20 AU AU2005286790A patent/AU2005286790A1/en not_active Abandoned
- 2005-09-20 AR ARP050103902A patent/AR051294A1/es unknown
- 2005-09-20 EP EP05808906A patent/EP1804792A1/en not_active Withdrawn
- 2005-09-20 MX MX2007003329A patent/MX2007003329A/es unknown
- 2005-09-20 BR BRPI0515477-4A patent/BRPI0515477A/pt not_active IP Right Cessation
- 2005-09-20 TW TW094132549A patent/TW200626148A/zh unknown
- 2005-09-20 WO PCT/US2005/033738 patent/WO2006034312A1/en active Application Filing
- 2005-09-20 CN CNA2005800396667A patent/CN101083986A/zh active Pending
- 2005-09-20 JP JP2007532629A patent/JP5080256B2/ja not_active Expired - Fee Related
-
2009
- 2009-05-06 US US12/436,665 patent/US20110009414A9/en not_active Abandoned
-
2012
- 2012-06-13 JP JP2012133967A patent/JP2012193188A/ja not_active Withdrawn
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JP2008513498A (ja) | 2008-05-01 |
US7547698B2 (en) | 2009-06-16 |
CA2580781A1 (en) | 2006-03-30 |
AU2005286790A1 (en) | 2006-03-30 |
US20070219211A1 (en) | 2007-09-20 |
BRPI0515477A (pt) | 2008-07-22 |
US20110009414A9 (en) | 2011-01-13 |
JP2012193188A (ja) | 2012-10-11 |
CN101083986A (zh) | 2007-12-05 |
JP5080256B2 (ja) | 2012-11-21 |
EP1804792A1 (en) | 2007-07-11 |
MX2007003329A (es) | 2007-06-05 |
WO2006034312A1 (en) | 2006-03-30 |
US20090291957A1 (en) | 2009-11-26 |
TW200626148A (en) | 2006-08-01 |
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