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AR056215A1 - Derivados de indol como inhibidores de la proteina activadora de 5-lipoxigenasa (flap), composiciones farmaceuticas que los comprenden y su uso en el tratamiento de trastornos respiratorios e inflamatorios - Google Patents

Derivados de indol como inhibidores de la proteina activadora de 5-lipoxigenasa (flap), composiciones farmaceuticas que los comprenden y su uso en el tratamiento de trastornos respiratorios e inflamatorios

Info

Publication number
AR056215A1
AR056215A1 ARP060104861A ARP060104861A AR056215A1 AR 056215 A1 AR056215 A1 AR 056215A1 AR P060104861 A ARP060104861 A AR P060104861A AR P060104861 A ARP060104861 A AR P060104861A AR 056215 A1 AR056215 A1 AR 056215A1
Authority
AR
Argentina
Prior art keywords
substituted
unsubstituted
nr9c
alkyl
heteroaryl
Prior art date
Application number
ARP060104861A
Other languages
English (en)
Original Assignee
Amira Pharmaceuticals Inc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=37546284&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=AR056215(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Amira Pharmaceuticals Inc filed Critical Amira Pharmaceuticals Inc
Publication of AR056215A1 publication Critical patent/AR056215A1/es

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    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/425—Thiazoles
    • A61K31/427—Thiazoles not condensed and containing further heterocyclic rings
    • 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
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Abstract

Se describen en la presente, compuestos y composiciones farmacéuticas que contienen tales compuestos que modulan la actividad de la proteína activadora de la 5-lipoxigenasa (FLAP). También se describen en la presente la utilizacion de tales moduladores de FLAP, solos y en combinacion con otros compuestos, para tratar enfermedades respiratorias, cardiovasculares, y otras afecciones o enfermedades leucotrieno-dependientes o mediadas por leucotrienos. Reivindicacion 1: Un compuesto que tiene la estructura de formula (1), en la cual, Z se selecciona de OC(R1)2[C(R2)2]n, [C(R2)2]nC(R1)2O, [C(R2)2]nO[C(R1)2]n, [C(R1)2]nO[C(R2)2]n donde cada R1 es independientemente H, CF3, o un alquilo inferior opcionalmente substituido y dos R1 sobre el mismo carbono pueden unirse para formar un carbonilo (=O); y cada R2 es independientemente H, OH, OMe, CF3, o un alquilo inferior opcionalmente substituido y dos R2 sobre el mismo carbono pueden unirse para formar un carbonilo (=O); m es 0, 1 o 2; cada n es independientemente 0, 1, 2 o 3; Y es H, -L1-(alquilo substituido o no substituido); -L1-(alquenilo substituido o no substituido); -L1-(alquinilo substituido o no substituido); -L1-(cicloalquilo substituido o no substituido); -L1- (heteroarilo substituido o no substituido); -L1-(arilo substituido o no substituido); donde L1 es un enlace, un alquilo substituido o no substituido, alquenilo substituido o no substituido, alquinilo substituido o no substituido, un heteroarilo substituido o no substituido, un cicloalquilo substituido o no substituido, un heteroalquilo substituido o no substituido, un heteroalquenilo substituido o no substituido, o un heteroalquinilo substituido o no substituido, donde cada substituyente es (LsRs)j, donde cada Ls se selecciona independientemente de un enlace, -O-, -C(=O)-, -S-, -S(=O)-, -S(=O)2-, -NHC(O)-, -C(O)NH-, S(=O)2NH-, -NHS(=O)2, -OC(O)NH-, -NHC(O)O-, -OC(O)O-, -NHC(O)NH-, -C(O)O-, - OC(O)-, alquilo C1-6, alquenilo C2-6, fluoroalquilo C1-6, heteroarilo, arilo, o grupo heteroalicíclico; y cada Rs se selecciona independientemente de H, halogeno, -N(R4)2, -CN, -NO2, N3, -S(=O)2NH2, alquilo inferior, cicloalquilo inferior, fluoroalquilo C1-6, heteroarilo o heteroalquilo; donde j s 0, 1, 2 3 o 4; cada R4 se selecciona independientemente H, alquilo inferior substituido o no substituido, cicloalquilo inferior substituido o no substituido, fenilo o bencilo, o dos grupos R4 pueden formar juntos un anillo heterocíclico de 5, 6, 7 u 8 miembros; R6 es H, L2-(alquilo substituido o no substituido), L2-(cicloalquilo substituido o no substituido), L2-(alquenilo substituido o no substituido), L2-(cicloalquenilo substituido o no substituido), L2-(heterociclo substituido o no substituido), L2-(heteroarilo substituido o no substituido), o L2-(arilo substituido o no substituido), donde L2 es un enlace, O, S, -S(=O), -S(=O)2, C(O), -CH(OH), -(alquilo C1-6 substituido o no substituido), o -(alquenilo C2-6 substituido o no substituido); R7 es L3-X-L4-G2 donde L3 es un enlace, alquilo substituido o no substituido, cicloalquilo substituido o no substituido, alquenilo substituido o no substituido, alquinilo substituido o no substituido, arilo substituido o no substituido, heteroarilo substituido o no substituido, heteroalicíclico substituido o no substituido; X es -NR9C(O), -C(O)NR9, -S(=O)2NR9-, -NR9S(=O)2, -OC(O)NR9-, - NR9C(O)O-, -CH=NO-, -ON=CH-, -NR9C(O)NR9-, heteroarilo, arilo, - NR9C(=NR10)NR9-, -NR9C(=NR10), -C(=NR10)NR9-, -OC(=NR10)-, o -C(=NR10)O-; L4 es un alquilo substituido o no substituido, cicloalquilo substituido o no substituido, alquenilo substituido o no substituido, alquinilo substituido o no substituido; G2 es H, -NHS(=O)2R8, S(=O)2N(R9)2, -OR9, -C(=O)CF3, CN, N(R9)2, -N(R9)C(O)R9, -C(=NR10)N(R9)2, -NR9C(=NR10)N(R9)2, -NR9C(=CR10)N(R9)2, -C(O)NR9C(=NR10)N(R9)2, -C(O)NR9C(=CR10)N(R9)2, -CO2R9, -C(O)R9, -CON(R9)2, -SR8, -S(=O)R8, -S(=O)2R8, -L5-(alquilo substituido o no substituido), -L5-(alquenilo substituido o no substituido), -L5-(heteroarilo substituido o no substituido), o -L5-(arilo substituido o no substituido), donde L5 es -OC(O)O-, -NHC(O)NH-, -NHC(O)O, -O(O)CNH-, -NHC(O), -C(O)NH, -C(O)O, u -OC(O); o G2 es W-G5, donde W es arilo substituido o no substituido, grupo heteroalicíclico substituido o no substituido o heteroarilo substituido o no substituido y G5 es H, -NHS(=O)2R8, S(=O)2N(R9)2, OH, -OR8, -C(=O)CF3, CN, N(R9)2, - N(R9)C(O)R9, -C(=NR10)N(R9)2, -NR9C(=NR10)N(R9)2, -NR9C(=CR10)N(R9)2, -C(O)NR9C(=NR10)N(R9)2, -C(O)NR9C(=CR10)N(R9)2, -CO2R9, -C(O)R9, -CON(R9)2, -SR8, -S(=O)R8, -S(=O)2R8, ; cada R8 se selecciona independientemente de alquilo inferior substituido o no substituido, cicloalquilo inferior substituido o no substituido, fenilo o bencilo; cada R9 se selecciona independientemente de H, alquilo inferior substituido o no substituido, cicloalquilo inferior substituido o no substituido, fenilo o bencilo; o dos grupos R9 pueden formar juntos un anillo heterocíclico de 5, 6, 7 u 8 miembros; o R8 y R9 pueden formar juntos un anillo heterocíclico de 5, 6, 7 u 8 miembros y cada R10 se selecciona independientemente de H, -S(=O)2R8, -S(=O)2NH2, -C(O)R8, - CN, -NO2, heteroarilo, o heteroalquilo; o(b) L3-X-L4-G4, donde L3 es un enlace, alquilo substituido o no substituido, cicloalquilo substituido o no substituido, alquenilo substituido o no substituido, alquinilo substituido o no substituido, arilo substituido o no substituido, heteroarilo substituido o no substituido, un grupo heteroalicíclico substituido o no substituido; X es un enlace, O, -C(=O), -CR9(OR9), S, S(=O), -S(=O)2, -NR9, -NR9C(O), -C(O)NR9, -OC(O)NR9-, - NR9C(O)O-, -CH=NO-, - ON=CH-, -NR9C(O)NR9-, heteroarilo, arilo, -NR9C(=NR10)NR9-, -NR9C(=NR10), -C(=NR10)NR9-, -OC(=NR10)-, o -C(=NR10)O-; L4 es un alquilo substituido o no substituido, cicloalquilo substituido o no substituido, alquenilo substituido o no substituido, alquinilo substituido o no substituido; G4 es -C(=NR10)N(R9)2, -NR9C(=NR10)N(R9)2, -NR9C(=CR10)N(R9)2, -L5-(alquilo substituido o no substituido), -L5-(alquenilo substituido o no substituido), -L5-(heteroarilo substituido o no substituido), o -L5- (arilo substituido o no substituido), donde L5 es -NHC(O)O, -O(O)CNH-, -C(O)O, u -OC(O); o G4 es W-G5, donde W es un arilo substituido o no substituido, grupo heteroalicíclico substituido o no substituido o un heteroarilo substituido o no substituido y G5 es es H, halogeno, -NHS(=O)2R8, S(=O)2N(R9)2, OH, -OR8, -C(=O)CF3, CN, N(R9)2, -N(R9)C(O)R9, -C(=NR10)N(R9)2, -NR9C(=NR10)N(R9)2, -NR9C(=CR10)N(R9)2, -C(O)NR9C(=NR10)N(R9)2, -C(O)NR9C(=CR10)N(R9)2, -CO2R9, -C(O)R9, -CON(R9)2, -SR8, - S(=O)R8, -S(=O)2R8, con la condicion que G4 no sea un tetrazol; cada R8 se selecciona independientemente de alquilo inferior substituido o no substituido, cicloalquilo inferior substituido o no substituido, fenilo substituido o no substituido o bencilo substituido o no substituido; cada R9 se selecciona independientemente de H, alquilo inferior substituido o no substituido, cicloalquilo inferior substituido o no substituido, fenilo substituido o no substituido o bencilo substituido o no substituido; o dos grupos R9 pueden formar juntos un anillo heterocíclico de 5, 6, 7 u 8 miembros; o R8 y R9 pueden formar juntos un anillo heterocíclico de 5, 6, 7 u 8 miembros y cada R10 se selecciona independientemente de H, -S(=O)2R8, - S(=O)2NH2, -C(O)R8, -CN, -NO2, heteroarilo, o heteroalquilo; R5 es H, halogeno, alquilo C1-6 substituido o no substituido, O-alquilo C1-6 substituido o no substituido; R11 es L7-L10-G6; donde L7 es un enlace, -O, -S, -S(=O), -S(=O)2, -NH, -C(O), - C(O)NH, -NHC(O), alquilo C1-6 substituido o no substituido, o alquenilo C2-6 substituido o no substituido; L10 es un enlace, alquilo substituido o no substituido, cicloalquilo substituido o no substituido, cicloalquenilo substituido o no substituido, heteroarilo substituido o no substituido, arilo substituido o no substituido, o grupo heteroalicíclico substituido o no substituido; G6 es H, CN, SCN, N3, NO2, halogeno, OR9, -C(O)NHR9, -NHC(O)R9, -C(=O)CF3, -C(=O)R9, -SR8, -S(=O)R8, - S(=O)2R8, N(R9)2, -NHS(=O)2R8, -S(=O)2N(R9)2, -C(O)NHS(=O)2R8, -S(=O)2NHC(O)R9, -C(=NR10)N(R9)2, -NR9C(=NR10)N(R9)2, -NR9C(=CR10)N(R9)2; R12 es H, (alquilo C1-6 substituido o no substituido), (cicloalquilo C3-6 substituido o no substituido); o su metabolito activo, o solvato, o sal aceptable para uso farmacéutico, o profármaco aceptable para uso farmacéutico.
ARP060104861A 2005-11-04 2006-11-06 Derivados de indol como inhibidores de la proteina activadora de 5-lipoxigenasa (flap), composiciones farmaceuticas que los comprenden y su uso en el tratamiento de trastornos respiratorios e inflamatorios AR056215A1 (es)

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Families Citing this family (31)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPH0775490B2 (ja) 1994-01-07 1995-08-16 彦重 藤井 菌糸体の培養方法
US7977359B2 (en) 2005-11-04 2011-07-12 Amira Pharmaceuticals, Inc. 5-lipdxygenase-activating protein (FLAP) inhibitors
GB2431927B (en) 2005-11-04 2010-03-17 Amira Pharmaceuticals Inc 5-Lipoxygenase-activating protein (FLAP) inhibitors
US20070244128A1 (en) * 2005-11-04 2007-10-18 Amira Pharmaceuticals, Inc. 5-lipoxygenase-activating protein (flap) inhibitors
US8399666B2 (en) 2005-11-04 2013-03-19 Panmira Pharmaceuticals, Llc 5-lipoxygenase-activating protein (FLAP) inhibitors
US20070225285A1 (en) * 2005-11-04 2007-09-27 Amira Pharmaceuticals, Inc. 5-lipoxygenase-activating protein (flap) inhibitors
US20070219206A1 (en) * 2005-11-04 2007-09-20 Amira Pharmaceuticals, Inc. 5-lipoxygenase-activating protein (flap) inhibitors
EP2086531A4 (en) * 2006-11-30 2009-09-30 Amira Pharmaceuticals Inc COMPOSITIONS AND TREATMENTS COMPRISING 5-LIPOXYGENASE-ACTIVATING PROTEIN INHIBITORS AND NITRIC OXIDE MODULATORS
TW200920369A (en) 2007-10-26 2009-05-16 Amira Pharmaceuticals Inc 5-lipoxygenase activating protein (flap) inhibitor
SG190667A1 (en) * 2008-05-23 2013-06-28 Panmira Pharmaceuticals Llc 5-lipoxygenase-activating protein inhibitor
US8546431B2 (en) 2008-10-01 2013-10-01 Panmira Pharmaceuticals, Llc 5-lipoxygenase-activating protein (FLAP) inhibitors
EP2379078A4 (en) * 2008-12-23 2012-06-13 Panmira Pharmaceuticals Llc TOPICAL FORMULATIONS OF FLAP INHIBITORS FOR ADMINISTRATION TO AN EYE
EP2381945A4 (en) * 2008-12-23 2012-06-13 Panmira Pharmaceuticals Llc TOPICAL FORMULAS OF FLAP INHIBITORS FOR THE TREATMENT OF DERMATOLOGICAL DISEASES
NZ807894A (en) 2009-04-29 2025-08-29 Amarin Pharmaceuticals Ie Ltd Pharmaceutical compositions comprising epa and a cardiovascular agent and methods of using the same
CN102596193A (zh) * 2009-07-31 2012-07-18 潘米拉制药公司 Dp2受体拮抗的皮肤调配物
CA2779786A1 (en) * 2009-11-03 2011-05-12 Claire Frances Crawford Novel processes
JP5690839B2 (ja) 2009-12-04 2015-03-25 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング ロイコトリエン産生のベンゾイミダゾール阻害薬
US20110301202A1 (en) * 2010-06-04 2011-12-08 Colin Hislop Spla2 inhibitor conjugate compounds and methods of use
CN103180314A (zh) 2010-08-16 2013-06-26 贝林格尔.英格海姆国际有限公司 抑制白三烯产生的*二唑类抑制剂
WO2012027322A1 (en) 2010-08-26 2012-03-01 Boehringer Ingelheim International Gmbh Oxadiazole inhibitors of leukotriene production
CN103261193A (zh) 2010-09-23 2013-08-21 贝林格尔.英格海姆国际有限公司 抑制白三烯生成的*二唑抑制剂
JP5828188B2 (ja) * 2010-09-23 2015-12-02 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング ロイコトリエン産生のオキサジアゾール阻害剤
WO2012058254A1 (en) * 2010-10-29 2012-05-03 Boehringer Ingelheim International Gmbh Benzimidazole inhibitors of leukotriene production
JP5789888B2 (ja) * 2010-11-01 2015-10-07 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング ロイコトリエン生成のベンゾイミダゾールインヒビター
AR089853A1 (es) * 2012-02-01 2014-09-24 Boehringer Ingelheim Int Inhibidores de oxadiazol de la produccion de leucotrienos para terapia de combinacion, composicion farmaceutica, uso
EP2865756A1 (en) 2013-10-22 2015-04-29 Sylentis, S.A.U. siRNA and their use in methods and compositions for inhibiting the expression of the FLAP gene.
US10080748B2 (en) 2014-02-04 2018-09-25 Bioscience Pharma Partners, Llc Use of flap inhibitors to reduce neuroinflammation mediated injury in the central nervous system
CN104277042A (zh) * 2014-10-15 2015-01-14 湖南华腾制药有限公司 一种咪唑并吡啶衍生物的制备方法
ES2902139T3 (es) * 2015-05-04 2022-03-25 Astrazeneca Ab Derivados de pirazol útiles como inhibidores de la proteína activadora de 5-lipoxigenasa (FLAP)
WO2018078097A1 (en) * 2016-10-28 2018-05-03 Astrazeneca Ab Crystalline form of (1r,2r)-2-[4-(3-methy1-1h-pyrazol-5-yl)benzoyl]-n-(4-oxo-4,5,6,7-tetrahydropyrazolo[1,5-a]pyrazin-3-yl)cyclohexanecarboxamide
HRP20230069T1 (hr) * 2017-01-17 2023-03-17 Astrazeneca Ab Selektivni inhibitori jak1

Family Cites Families (208)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR2431491A1 (fr) 1978-07-18 1980-02-15 Delalande Sa Nouveaux derives aminoalkoxy-5 benzofurannes et indoles, leur procede de preparation et leur application en therapeutique
DK151884C (da) * 1979-03-07 1988-06-13 Pfizer Analogifremgangsmaade til fremstilling af 3-(1-imidazolylalkyl)indolderivater eller farmaceutisk acceptable syreadditionssalte deraf
JPS60123485A (ja) * 1983-12-08 1985-07-02 Yoshitomi Pharmaceut Ind Ltd インド−ル−３−カルボキサミド誘導体
IE58870B1 (en) * 1985-03-08 1993-11-17 Leo Pharm Prod Ltd Pyridine derivatives
US5109009A (en) * 1985-03-08 1992-04-28 Leo Pharmaceutical Products Ltd. Quinoline and pyridine compounds and inhibition of 5-lipoxygenases therewith
DE3632411A1 (de) 1986-09-24 1988-04-07 Merck Patent Gmbh Verfahren zur herstellung von ethanderivaten
US5225421A (en) * 1986-12-17 1993-07-06 Merck Frosst Canada, Inc. 3-hetero-substituted-N-benzyl-indoles and medical methods of use therefor
IL84796A (en) * 1986-12-17 1992-03-29 Merck Frosst Canada Inc Substituted n-benzyl-indoles and pharmaceutical compositions containing them
US5081138A (en) * 1986-12-17 1992-01-14 Merck Frosst Canada, Inc. 3-hetero-substituted-n-benzyl-indoles and prevention of leucotriene synthesis therewith
MY103259A (en) * 1987-04-15 1993-05-29 Ici America Inc Aliphatic carboxamides
ES2045420T3 (es) * 1988-04-13 1994-01-16 Ici America Inc Amidas ciclicas.
US5232916A (en) * 1988-06-27 1993-08-03 Merck Frosst Canada, Inc. Quinoline ether alkanoic acids
US5272145A (en) * 1989-08-22 1993-12-21 Merck Frosst Canada, Inc. (Quinolin-2-ylmethoxy)indoles as inhibitors of the biosynthesis of leukotrienes
US5204344A (en) * 1989-08-22 1993-04-20 Merck Frosst Canada, Inc. (Quinolin-2-ylmethoxy)indoles as inhibitors of the biosynthesis of leukotrienes
US5252585A (en) * 1992-02-03 1993-10-12 Merck Frosst Canada, Inc. Fluorinated quinoline indoles as inhibitors of the biosynthesis of leukotrienes
CA1337427C (en) 1989-08-22 1995-10-24 Merck Frosst Canada Incorporated (quinolin-2-ylmethoxy)indoles as inhibitors of the biosynthesis of leukotrienes
NZ234883A (en) 1989-08-22 1995-01-27 Merck Frosst Canada Inc Quinolin-2-ylmethoxy indole derivatives, preparation and pharmaceutical compositions thereof
US5420289A (en) * 1989-10-27 1995-05-30 American Home Products Corporation Substituted indole-, indene-, pyranoindole- and tetrahydrocarbazole-alkanoic acid derivatives as inhibitors of PLA2 and lipoxygenase
PT95692A (pt) * 1989-10-27 1991-09-13 American Home Prod Processo para a preparacao de derivados de acidos indole-,indeno-,piranoindole- e tetra-hidrocarbazole-alcanoicos, ou quais sao uteis como inibidores de pla2 e da lipoxigenase
US5229516A (en) * 1989-10-27 1993-07-20 American Home Products Corporation Substituted indole-, indene-, pyranoindole- and tetrahydrocarbazole-alkanoic acid derivatives as inhibitors of PLA2 and lipoxygenase
CA2032253C (en) 1989-12-15 2000-11-28 John W. Gillard 5-lipoxygenase activating protein
US5093356A (en) * 1990-01-16 1992-03-03 Merck Frosst Canada, Inc. Indenyl hydroxamic acids and hydroxy ureas as inhibitors of 5-lipoxygenase
US5081145A (en) * 1990-02-01 1992-01-14 Merck Frosst Canada, Inc. Indole-2-alkanoic acids compositions of and anti allergic use thereof
US5095031A (en) * 1990-08-20 1992-03-10 Abbott Laboratories Indole derivatives which inhibit leukotriene biosynthesis
JPH0764841B2 (ja) * 1990-10-03 1995-07-12 ファイザー製薬株式会社 インドール誘導体およびその用途
US5182367A (en) * 1990-11-30 1993-01-26 Merck & Co., Inc. 5-lipoxygenase activating protein
CA2060557C (en) * 1991-02-05 2002-06-04 Merck Frosst Canada Incorporated (quinolin-2-ylmethoxy) indoles as inhibitors of the biosynthesis of leukotrienes
GB9108811D0 (en) 1991-04-24 1991-06-12 Erba Carlo Spa N-imidazolyl derivatives of substituted indole
US5202321A (en) * 1991-06-13 1993-04-13 Merck Frosst Canada, Inc. Thiopyrano[2,3,4-c,d]indoles as inhibitors of leukotriene biosynthesis
JPH06100551A (ja) 1991-09-06 1994-04-12 Dainippon Ink & Chem Inc 光学活性な２，５置換テトラヒドロフラン誘導体、その製造方法、その誘導体を含む液晶組成物及び液晶表示素子
US5190968A (en) * 1991-09-30 1993-03-02 Merck Frosst Canada, Inc. (Polycyclic-arylmethoxy) indoles as inhibitors of leukotriene biosynthesis
CA2079374C (en) * 1991-09-30 2003-08-05 Merck Frosst Canada Incorporated (bicyclic-azaarylmethoxy)indoles as inhibitors of leukotriene biosynthesis
US5273980A (en) * 1991-09-30 1993-12-28 Merck Frosst Canada Inc. Bicyclic-azaarylmethoxy) indoles as inhibitors of leukotriene biosynthesis
US5389650A (en) * 1991-09-30 1995-02-14 Merck Frosst Canada, Inc. (Azaarylmethoxy)indoles as inhibitors of leukotriene biosynthesis
US5308850A (en) * 1991-09-30 1994-05-03 Merck Frosst Canada, Inc. (Bicyclic-hetero-arylmethoxy)indoles as inhibitors of leukotriene biosynthesis
US5290798A (en) * 1991-09-30 1994-03-01 Merck Frosst Canada, Inc. (hetero-arylmethoxy)indoles as inhibitors of leukotriene biosynthesis
ZA928276B (en) 1991-10-31 1993-05-06 Daiichi Seiyaku Co Aromatic amidine derivates and salts thereof.
US5254567A (en) * 1991-11-15 1993-10-19 Merck Frosst Canada, Inc. Amorphous (quinolin-2-ylmethoxy)indole compounds which have useful pharmaceutical utility
WO1993016069A1 (en) * 1992-02-13 1993-08-19 Merck Frosst Canada Inc. (azaaromaticalkoxy)indoles as inhibitors of leukotriene biosynthesis
CH683522A5 (de) 1992-03-13 1994-03-31 Hoffmann La Roche Verfahren zur Herstellung von Diarylen.
EP0597112A4 (en) * 1992-03-27 1994-06-22 Kyoto Pharma Ind Novel imidazole derivative, pharmaceutical use thereof, and intermediate therefor.
NZ249729A (en) 1992-05-13 1996-12-20 Syntex Inc Substituted indoles and azaindoles, preparation and pharmaceutical compositions thereof
JPH0658881A (ja) 1992-06-12 1994-03-04 Mitsubishi Rayon Co Ltd 光学活性化合物の絶対配置判定法、絶対配置判定用試薬及び絶対配置判定装置
US5334719A (en) 1992-06-17 1994-08-02 Merck Frosst Canada, Inc. Bicyclic(azaaromatic)indoles as inhibitors of leukotriene bisynthesis
WO1994000446A1 (en) 1992-06-22 1994-01-06 Merck Frosst Canada Inc. Fluorinated quinoline indoles as inhibitors of the biosynthesis of leukotrienes
US5314898A (en) * 1992-06-29 1994-05-24 Merck & Co., Inc. Aryl thiopyrano[4,3,2-cd]indoles as inhibitors of leukotriene biosynthesis
US5314900A (en) 1992-11-19 1994-05-24 Merck Frosst Canada, Inc. Aryl thiopyrano[2,3,4-C,D]indoles as inhibitors of leukotriene biosynthesis
US5288743A (en) 1992-11-20 1994-02-22 Abbott Laboratories Indole carboxylate derivatives which inhibit leukotriene biosynthesis
ZA939516B (en) 1992-12-22 1994-06-06 Smithkline Beecham Corp Endothelin receptor antagonists
JP3457694B2 (ja) 1993-02-04 2003-10-20 第一製薬株式会社 インフルエンザ感染予防・治療薬
US5374635A (en) * 1993-03-29 1994-12-20 Merck Frosst Canada, Inc. Furo[3,2-b]pyridines and thieno[3,2-b]pyridines as inhibitors of leukotriene biosynthesis
IL109311A0 (en) * 1993-04-16 1994-07-31 Lilly Co Eli 1H-indole-3-acetamide sPla2 inhibitors
IL109309A (en) 1993-04-16 2000-06-29 Lilly Co Eli 1-H-indole-3-acetic acid hydrazide SPLA2 inhibitors and pharmaceutical compositions containing them
JPH075651A (ja) 1993-06-14 1995-01-10 Fuji Photo Film Co Ltd ハロゲン化銀カラー写真感光材料の処理方法
DK0703911T3 (da) 1993-06-14 1997-10-06 Pfizer Sekundære aminer som antidiabetiske og antiobesitetsmidler
WO1995006637A1 (en) 1993-09-03 1995-03-09 Smithkline Beecham Plc Indole and indoline derivatives as 5ht1d receptor antagonists
DE4338770A1 (de) * 1993-11-12 1995-05-18 Matthias Dr Lehr Indol-2-alkansäuren und ihre Derivate als Hemmstoffe der Phospholipase A¶2¶
US5399699A (en) * 1994-01-24 1995-03-21 Abbott Laboratories Indole iminooxy derivatives which inhibit leukotriene biosynthesis
US5420282A (en) * 1994-02-15 1995-05-30 Abbott Laboratories Thiopyrano(2,3,4-c,d) indolyloxime ether alkylcarboxylates
US5696076A (en) * 1994-06-22 1997-12-09 Human Genome Sciences, Inc. 5-lipoxygenase-activating protein II
FR2721610B1 (fr) * 1994-06-28 1996-08-23 Adir Nouveaux dérivés (thia)cycloalkyl [b] indoles, leur procédé de préparation et les compositions pharmaceutiques qui les contiennent.
JPH0820532A (ja) 1994-07-05 1996-01-23 Dai Ichi Seiyaku Co Ltd 抗膵炎剤
CN1166169A (zh) 1994-07-27 1997-11-26 三共株式会社 用作毒蕈碱性受体别构效应物的杂环化合物
TW396200B (en) * 1994-10-19 2000-07-01 Sumitomo Chemical Co Liquid crystal composition and liquid crystal element containing such composition
TW321649B (es) 1994-11-12 1997-12-01 Zeneca Ltd
AU4514496A (en) * 1994-12-13 1996-07-03 Smithkline Beecham Corporation Novel compounds
US6069156A (en) * 1995-04-10 2000-05-30 Fujisawa Pharmaceutical Co., Ltd. Indole derivatives as cGMP-PDE inhibitors
US5702637A (en) * 1995-04-19 1997-12-30 Minnesota Mining And Manufacturing Company Liquid crystal compounds having a chiral fluorinated terminal portion
WO1996035670A1 (en) 1995-05-10 1996-11-14 Pfizer Inc. β-ADRENERGIC AGONISTS
JPH092977A (ja) 1995-06-21 1997-01-07 Dai Ichi Seiyaku Co Ltd 経口投与用医薬組成物
EP0880519B1 (en) * 1996-01-22 2002-04-17 Fujisawa Pharmaceutical Co., Ltd. Thiazolylbenzofuran derivatives and pharmaceutical compositions containing them
CA2216537A1 (en) 1996-01-29 1997-08-07 Tadashi Sugawa Process for reduction of carbonyl compounds
US5756531A (en) * 1996-04-30 1998-05-26 Abbott Laboratories Iminoxy derivatives of indole and indene compounds as inhibitors of prostaglandin biosynthesis
US5750558A (en) * 1996-06-06 1998-05-12 Abbott Laboratories Oxime derivatives of indole and indene compounds as inhibitors of prostaglandin biosynthesis
CN1226175A (zh) 1996-07-23 1999-08-18 第一制药株式会社 吸收促进剂
US5877329A (en) * 1996-08-13 1999-03-02 Merck & Co., Inc. Palladium catalyzed indolization
YU22099A (sh) 1996-11-14 2001-09-28 Pfizer Inc. Dobijanje supstituisanih piridina
GB9710523D0 (en) 1997-05-23 1997-07-16 Smithkline Beecham Plc Novel compounds
WO1998056757A1 (fr) 1997-06-11 1998-12-17 Sankyo Company, Limited Derives de benzylamine
GB9716657D0 (en) * 1997-08-07 1997-10-15 Zeneca Ltd Chemical compounds
JPH1180032A (ja) 1997-09-12 1999-03-23 Dai Ichi Seiyaku Co Ltd 複合体
US6548490B1 (en) 1997-10-28 2003-04-15 Vivus, Inc. Transmucosal administration of phosphodiesterase inhibitors for the treatment of erectile dysfunction
RU2225397C2 (ru) * 1997-12-24 2004-03-10 Авентис Фарма Дойчланд Гмбх Производные индола как ингибиторы фактора Ха
AU1689999A (en) 1997-12-25 1999-07-19 Daiichi Pharmaceutical Co., Ltd. Medicinal composition for percutaneous administration
JPH11189531A (ja) 1997-12-26 1999-07-13 Dai Ichi Seiyaku Co Ltd 経粘膜投与用医薬組成物
JPH11193265A (ja) 1997-12-26 1999-07-21 Dai Ichi Seiyaku Co Ltd ３−（７−アミジノ−２−ナフチル）−２−フェニルプロピオン酸誘導体の塩
CA2260499A1 (en) 1998-01-29 1999-07-29 Sumitomo Pharmaceuticals Company Limited Pharmaceutical compositions for the treatment of ischemic brain damage
HUP0100156A3 (en) 1998-02-25 2002-12-28 Genetics Inst Inc Cambridge Indole derivatives as inhibitors of phospholipase a2 and use of them for producing pharmaceutical compositions
US6500853B1 (en) * 1998-02-28 2002-12-31 Genetics Institute, Llc Inhibitors of phospholipase enzymes
ES2272061T5 (es) * 1998-04-15 2012-02-24 Merck Serono Biodevelopment Secuencia genómica de la proteína activadora de 5-lipoxigenasa (flap), marcadores polimórficos de la misma y métodos para la detección de asma.
NZ508790A (en) * 1998-05-22 2003-10-31 Scios Inc Heterocyclic compounds and methods to treat cardiac failure and other disorders
US6867209B1 (en) * 1998-05-22 2005-03-15 Scios, Inc. Indole-type derivatives as inhibitors of p38 kinase
JP2000007590A (ja) 1998-06-23 2000-01-11 Daicel Chem Ind Ltd 置換芳香族化合物の製造方法
EP1131425A2 (en) 1998-11-18 2001-09-12 Incyte Pharmaceuticals, Inc. Inflammation-associated genes
UA73492C2 (en) 1999-01-19 2005-08-15 Aromatic heterocyclic compounds as antiinflammatory agents
JP2000302671A (ja) 1999-04-27 2000-10-31 Hitoshi Sezaki 経口投与用医薬組成物
WO2000071535A1 (en) * 1999-05-21 2000-11-30 Scios Inc. INDOLE-TYPE DERIVATIVES AS INHIBITORS OF p38 KINASE
EP1218356A1 (en) 1999-09-21 2002-07-03 AstraZeneca AB Quinazoline compounds and pharmaceutical compositions containing them
DE19948417A1 (de) * 1999-10-07 2001-04-19 Morphochem Ag Imidazol-Derivate und ihre Verwendung als Arzneimittel
AU7962200A (en) 1999-10-29 2001-05-14 Wakunaga Pharmaceutical Co., Ltd Novel indole derivatives and drugs containing the same as the active ingredient
JP2001139462A (ja) 1999-11-10 2001-05-22 Dai Ichi Seiyaku Co Ltd 新規製剤
EP1232150B1 (en) 1999-11-16 2007-10-10 Boehringer Ingelheim Pharmaceuticals Inc. Urea derivatives as anti-inflammatory agents
WO2001044184A1 (en) 1999-12-16 2001-06-21 Eli Lilly And Company Synthesis of indole-containing spla2 inhibitors
US7345051B2 (en) 2000-01-31 2008-03-18 Genaera Corporation Mucin synthesis inhibitors
GB0003079D0 (en) 2000-02-10 2000-03-29 Glaxo Group Ltd Novel protein
EP1254115A2 (en) * 2000-02-11 2002-11-06 Bristol-Myers Squibb Company Cannabinoid receptor modulators, their processes of preparation, and use of cannabinoid receptor modulators for treating respiratory and non-respiratory diseases
US6436965B1 (en) 2000-03-02 2002-08-20 Merck Frosst Canada & Co. PDE IV inhibiting amides, compositions and methods of treatment
NZ521192A (en) 2000-03-09 2005-01-28 Ono Pharmaceutical Co Indole derivatives, process for preparation of the same and use thereof
WO2003022814A1 (en) 2001-09-07 2003-03-20 Ono Pharmaceutical Co., Ltd. Indole derivatives
US6476037B1 (en) 2000-03-23 2002-11-05 The Regents Of The University Of California L-arginine and phosphodiesterase (PDE) inhibitor synergism
US20010039037A1 (en) * 2000-04-05 2001-11-08 Lee Harland Novel polypeptide
AU2001254790A1 (en) 2000-04-07 2001-10-23 Bayer Aktiengesellschaft Regulation of human cyslt2-like gpcr protein
WO2001096336A2 (en) * 2000-06-14 2001-12-20 Warner-Lambert Company 6,5-fused bicyclic heterocycles
JPWO2002000621A1 (ja) 2000-06-29 2004-04-22 塩野義製薬株式会社 Ｘ型ｓＰＬＡ２阻害作用を有する化合物
DE10037310A1 (de) 2000-07-28 2002-02-07 Asta Medica Ag Neue Indolderivate und deren Verwendung als Arzneimittel
CN1478077A (zh) 2000-10-05 2004-02-25 ����ҩƷ��ҵ��ʽ���� 作为apo b分泌抑制剂的苯甲酰胺化合物
US6787651B2 (en) * 2000-10-10 2004-09-07 Smithkline Beecham Corporation Substituted indoles, pharmaceutical compounds containing such indoles and their use as PPAR-γ binding agents
CN1281605C (zh) 2000-12-22 2006-10-25 惠氏公司 作为5－羟色胺－6配基的杂环基－吲唑或氮杂吲唑化合物
EP1344525A4 (en) 2000-12-22 2005-05-25 Ishihara Sangyo Kaisha ANILINE DERIVATIVES OR ITS SALTS AND CYTOKINE PRODUCTION INHIBITORS CONTAINING THEM
AU2002243692B2 (en) * 2001-01-29 2006-06-08 3-Dimensional Pharmaceuticals, Inc. Substituted indoles and their use as integrin antagonists
JP2002226429A (ja) 2001-02-06 2002-08-14 Fuji Photo Film Co Ltd アクリル酸エステル化合物の製造方法
WO2003022813A1 (en) 2001-09-07 2003-03-20 Ono Pharmaceutical Co., Ltd. Indole derivatives, process for producing the same and drugs containing the same as the active ingredient
EP1427707A1 (en) 2001-09-19 2004-06-16 Pharmacia Corporation Substituted indazole compounds for the treatment of inflammation
DE10147672A1 (de) 2001-09-27 2003-04-10 Bayer Ag Substituierte 2,5-Diamidoindole und ihre Verwendung
EP1314733A1 (en) * 2001-11-22 2003-05-28 Aventis Pharma Deutschland GmbH Indole-2-carboxamides as factor Xa inhibitors
AU2002226401A1 (en) 2001-12-11 2003-06-23 Rhodia Chimie Catalytic pgm mixture for hydrosilylation
USH2153H1 (en) * 2002-04-24 2006-04-04 Smithkline Beecham Corp. Association of asthma with polymorphisms in the cysteinyl leukotriene 2 receptor
WO2003094889A1 (fr) 2002-05-13 2003-11-20 Daiichi Pharmaceutical Co., Ltd. Produit de lyophilisation
PE20040522A1 (es) 2002-05-29 2004-09-28 Novartis Ag Derivados de diarilurea dependientes de la cinasa de proteina
DE10224888A1 (de) * 2002-06-05 2003-12-24 Merck Patent Gmbh Pyridazinderivate
JPWO2004000795A1 (ja) 2002-06-20 2005-10-20 協和醗酵工業株式会社 ビニルパーフルオロアルカンスルホン酸エステル誘導体の製造法
EP1777223A1 (en) * 2002-06-24 2007-04-25 Schering Corporation Indole derivatives useful as histamine H3 antagonists
CA2495903A1 (en) 2002-08-23 2004-03-04 University Of Connecticut Novel biphenyl and biphenyl-like cannabinoids
WO2004017917A2 (en) 2002-08-26 2004-03-04 Merck & Co., Inc. Method for the prevention and/or treatment of atherosclerosis
HRP20050181A2 (en) 2002-08-29 2006-03-31 Merck & Co. Inc. Indoles having anti-diabetic activity
AU2003292508A1 (en) 2002-11-28 2004-06-18 Suven Life Sciences Limited N-arylalkyl-3-aminoalkoxyindoles and their use as 5-ht ligands
US7642277B2 (en) 2002-12-04 2010-01-05 Boehringer Ingelheim International Gmbh Non-nucleoside reverse transcriptase inhibitors
US20040198800A1 (en) * 2002-12-19 2004-10-07 Geoffrey Allan Lipoxygenase inhibitors as hypolipidemic and anti-hypertensive agents
GB0301350D0 (en) 2003-01-21 2003-02-19 Merck Sharp & Dohme Therapeutic agents
JP4513351B2 (ja) 2003-02-12 2010-07-28 チッソ株式会社 結合基にフッ素化されたアルキル基を有する液晶性化合物、液晶組成物および液晶表示素子
WO2004078719A1 (ja) 2003-03-06 2004-09-16 Ono Pharmaceutical Co., Ltd. インドール誘導体化合物およびその化合物を有効成分とする薬剤
EP1479677A1 (en) 2003-05-19 2004-11-24 Aventis Pharma Deutschland GmbH New indole derivatives as factor xa inhibitors
WO2004108671A1 (en) 2003-06-06 2004-12-16 Suven Life Sciences Limited Substituted indoles with serotonin receptor affinity, process for their preparation and pharmaceutical compositions containing them
JP2006528630A (ja) * 2003-07-24 2006-12-21 メルク　エンド　カムパニー　インコーポレーテッド ジフェニル置換シクロアルカン類、そのような化合物を含む組成物、ならびに使用方法
WO2005019381A1 (en) 2003-08-25 2005-03-03 Merck Patent Gmbh Liquid crystalline medium
AU2004270187A1 (en) 2003-09-04 2005-03-17 Aventis Pharmaceuticals Inc. Substituted indoles as inhibitors of poly (ADP-ribose) polymerase (PARP)
AP2006003559A0 (en) 2003-09-05 2006-04-30 Neurogen Corp Ventis Pharmaceuticals Inc Heteroaryl fused pyridines, pyrazines and pyrimidines as CRF 1 receptor ligands
JP4363133B2 (ja) 2003-09-09 2009-11-11 東洋インキ製造株式会社 有機エレクトロルミネッセンス用素子材料およびそれを用いた有機エレクトロルミネッセンス素子
US7268159B2 (en) * 2003-09-25 2007-09-11 Wyeth Substituted indoles
CA2539335A1 (en) * 2003-10-31 2005-05-12 Otsuka Pharmaceutical Co., Ltd. 2,3-dihydro-6-nitroimidazo (2,1-b) oxazole compounds for the treatment of tuberculosis
JP2005170939A (ja) 2003-11-20 2005-06-30 Takeda Chem Ind Ltd 糖尿病の予防・治療剤
WO2005054176A1 (en) 2003-11-25 2005-06-16 Eli Lilly And Company Peroxisome proliferator activated receptor modulators
US20070054902A1 (en) 2003-12-02 2007-03-08 Shionogi & Co., Ltd. Isoxazole derivatives as peroxisome proliferator-activated receptors agonists
EP1708997B1 (en) 2003-12-03 2009-10-21 Merck and Co., Inc. 1-alkyl-3-thio-substituted indole-2-alkynoic acids useful for the treatment for alzheimer's disease and related conditions
US20050137234A1 (en) 2003-12-19 2005-06-23 Syrrx, Inc. Histone deacetylase inhibitors
JP5142450B2 (ja) 2003-12-25 2013-02-13 徹也 西尾 ジアミノ化合物、ビニル化合物、高分子化合物、配向膜、該配向膜を用いた有機半導体装置、導電性高分子、該導電性高分子を使用したエレクトロルミネッセンス素子、液晶配向膜、及び該液晶配向膜を用いた光学素子
US7064203B2 (en) 2003-12-29 2006-06-20 Bristol Myers Squibb Company Di-substituted pyrrolotriazine compounds
WO2005066157A1 (en) 2004-01-02 2005-07-21 Suven Life Sciences 3-(pyrolidin-3-l) indoles as 5-ht6 receptor modulators
JP2005194250A (ja) 2004-01-09 2005-07-21 Sumitomo Chemical Takeda Agro Co Ltd トリアゾール化合物、その製造法および用途
US8158362B2 (en) 2005-03-30 2012-04-17 Decode Genetics Ehf. Methods of diagnosing susceptibility to myocardial infarction and screening for an LTA4H haplotype
WO2005082346A1 (en) 2004-02-26 2005-09-09 Merck & Co, Inc. Use of cysteinyl leukotriene 2 receptor antagonists
WO2005097203A2 (en) 2004-04-01 2005-10-20 Cardiome Pharma Corp. Serum protein conjugates of ion channel modulating compounds and uses thereof
WO2005112921A2 (en) 2004-04-26 2005-12-01 Vanderbilt University Indoleacetic acid and indenacetic acid derivatives as therapeutic agents with reduced gastrointestinal toxicity
CA2564563C (en) * 2004-05-03 2011-07-05 F. Hoffmann-La Roche Ag Indolyl derivatives as liver-x-receptor modulators
JP2008502670A (ja) 2004-06-18 2008-01-31 バイオリポックス エービー 炎症の治療に有用なインドール類
WO2006014262A2 (en) * 2004-07-02 2006-02-09 Merck & Co., Inc. Indoles having anti-diabetic activity
EP1799653B1 (en) 2004-08-20 2013-03-20 Bayer Intellectual Property GmbH Condensed thienopyrimidine derivatives for the treatment of cancer
GB0420719D0 (en) 2004-09-17 2004-10-20 Addex Pharmaceuticals Sa Novel allosteric modulators
WO2006041961A1 (en) 2004-10-05 2006-04-20 GOVERNMENT OF THE UNITED STATES OF AMERICA, as represented by THE SECRETARY, DEPARTMENT OF HEALTHAND HUMAN SERVICES Arylthioindole tubulin polymerization inhibitors and methods of treating or preventing cancer using same
EP1814877B1 (en) 2004-10-18 2009-03-11 Merck & Co., Inc. Diphenyl substituted alkanes as flap inhibitors
US7947694B2 (en) 2005-01-14 2011-05-24 Janssen Pharmaceutica Nv Substituted pyrazolo[3,4-D]pyrimidines as cell cycle kinase inhibitors
EP1838669A1 (en) 2005-01-19 2007-10-03 Biolipox AB Indoles useful in the treatment of inflammation
KR20070114123A (ko) 2005-01-19 2007-11-29 바이올리폭스 에이비 염증 치료에 유용한 인돌
US20100197687A1 (en) 2005-01-19 2010-08-05 Benjamin Pelcman Indoles Useful in the Treatment of Inflammation
US20080249091A1 (en) 2005-01-19 2008-10-09 Benjamin Pelcman Indoles Useful in the Treatment of Inflammation
CA2600860A1 (en) 2005-03-09 2006-09-21 Merck & Co., Inc. Diphenyl substituted cycloalkanes, compositions containing such compounds and methods of use
RU2453540C2 (ru) * 2005-04-21 2012-06-20 Лаборатуар Сероно С.А. 2,3-замещенные пиразинсульфонамиды в качестве ингибиторов crth2
JP5846711B2 (ja) 2005-06-09 2016-01-20 メダ アーベー 炎症性疾患の治療のための方法及び組成物
GB0516156D0 (en) 2005-08-05 2005-09-14 Eisai London Res Lab Ltd JNK inhibitors
EP1947942B1 (en) 2005-08-18 2015-07-29 Accelalox, Inc. Methods for bone treatment by modulating an arachidonic acid metabolic or signaling pathway
US7405302B2 (en) * 2005-10-11 2008-07-29 Amira Pharmaceuticals, Inc. 5-lipoxygenase-activating protein (FLAP) inhibitors
CN101360731B (zh) 2005-10-11 2013-01-30 联邦高等教育系统-匹兹堡大学 作为淀粉样发生蛋白成像剂的同位素标记苯并呋喃化合物
CA2626549A1 (en) 2005-10-21 2007-04-26 University Of Alabama At Birmingham Small molecule inhibitors of hiv-1 capsid assembly
US20070225285A1 (en) 2005-11-04 2007-09-27 Amira Pharmaceuticals, Inc. 5-lipoxygenase-activating protein (flap) inhibitors
UY29896A1 (es) 2005-11-04 2007-06-29 Astrazeneca Ab Nuevos derivados de cromano, composiciones farmacéuticas conteniéndolos, procesos de preparación y aplicaciones
US20070244128A1 (en) * 2005-11-04 2007-10-18 Amira Pharmaceuticals, Inc. 5-lipoxygenase-activating protein (flap) inhibitors
US8399666B2 (en) * 2005-11-04 2013-03-19 Panmira Pharmaceuticals, Llc 5-lipoxygenase-activating protein (FLAP) inhibitors
US7977359B2 (en) 2005-11-04 2011-07-12 Amira Pharmaceuticals, Inc. 5-lipdxygenase-activating protein (FLAP) inhibitors
GB2431927B (en) 2005-11-04 2010-03-17 Amira Pharmaceuticals Inc 5-Lipoxygenase-activating protein (FLAP) inhibitors
NL2000284C2 (nl) 2005-11-04 2007-09-28 Pfizer Ltd Pyrazine-derivaten.
US20070219206A1 (en) 2005-11-04 2007-09-20 Amira Pharmaceuticals, Inc. 5-lipoxygenase-activating protein (flap) inhibitors
UY29892A1 (es) 2005-11-04 2007-06-29 Astrazeneca Ab Nuevos derivados de cromano, composiciones farmaceuticas conteniendolos, procesos de preparacion y aplicaciones
AR059901A1 (es) 2006-03-20 2008-05-07 Bayer Pharmaceuticals Corp Compuestos de tetrahidropiridotienopirimidina utiles para tratar o prevenir trastornos proliferativos celulares.
TW200815377A (en) 2006-04-24 2008-04-01 Astellas Pharma Inc Oxadiazolidinedione compound
CA2656564C (en) 2006-06-29 2015-06-16 Kinex Pharmaceuticals, Llc Biaryl compositions and methods for modulating a kinase cascade
JP2009023986A (ja) 2006-11-08 2009-02-05 Pharma Ip 抗癌剤としてのビアリール誘導体
EP3048099A3 (en) 2006-11-15 2016-09-21 YM BioSciences Australia Pty Ltd Inhibitors of kinase activity
EP2086531A4 (en) 2006-11-30 2009-09-30 Amira Pharmaceuticals Inc COMPOSITIONS AND TREATMENTS COMPRISING 5-LIPOXYGENASE-ACTIVATING PROTEIN INHIBITORS AND NITRIC OXIDE MODULATORS
JP2010518025A (ja) 2007-02-05 2010-05-27 アミラ ファーマシューティカルス，インコーポレーテッド ５−リポキシゲナーゼ活性化タンパク質（ｆｌａｐ）インヒビターとしての逆インドール
US8039505B2 (en) * 2007-04-11 2011-10-18 University Of Utah Research Foundation Compounds for modulating T-cells
WO2009002746A1 (en) 2007-06-22 2008-12-31 Decode Genetics Ehf. Dosing schedules of leukotriene synthesis inhibitors for human therapy
WO2009009041A2 (en) 2007-07-06 2009-01-15 Kinex Pharmaceuticals, Llc Compositions and methods for modulating a kinase cascade
EP2207547A4 (en) 2007-10-05 2010-11-17 Amira Pharmaceuticals Inc PROTEIN INHIBITORS THAT ACTIVATE 5-LIPOXYGENASE
TW200920369A (en) 2007-10-26 2009-05-16 Amira Pharmaceuticals Inc 5-lipoxygenase activating protein (flap) inhibitor
EP2269076A4 (en) 2008-03-14 2011-04-06 Nat Jewish Health METHOD FOR DETERMINING THE RECOMMENDATION FOR TREATMENT WITH LEUKOTRIA MODIFIERS
SG190667A1 (en) * 2008-05-23 2013-06-28 Panmira Pharmaceuticals Llc 5-lipoxygenase-activating protein inhibitor
US8546431B2 (en) * 2008-10-01 2013-10-01 Panmira Pharmaceuticals, Llc 5-lipoxygenase-activating protein (FLAP) inhibitors
EP2379078A4 (en) 2008-12-23 2012-06-13 Panmira Pharmaceuticals Llc TOPICAL FORMULATIONS OF FLAP INHIBITORS FOR ADMINISTRATION TO AN EYE

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CA2628233A1 (en) 2007-05-18
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