AR086750A1 - Ligandos del receptor trpm8 y su uso en diversos tratamientos - Google Patents

Ligandos del receptor trpm8 y su uso en diversos tratamientos

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Publication number
AR086750A1
AR086750A1 ARP120102273A ARP120102273A AR086750A1 AR 086750 A1 AR086750 A1 AR 086750A1 AR P120102273 A ARP120102273 A AR P120102273A AR P120102273 A ARP120102273 A AR P120102273A AR 086750 A1 AR086750 A1 AR 086750A1
Authority
AR
Argentina
Prior art keywords
alkyl
nrara
nra
ora
substituted
Prior art date
Application number
ARP120102273A
Other languages
English (en)
Inventor
B Horne Daniel
R Kaller Matthew
Liu Qingyian
Van Ma Vu
Monenschein Holger
T Nguyen Thomas
J Jr St Jean David
Chenguang Yuan Chester
Biswas Kaustav
Brown James
J Chen Jian
Keshav Gore Vijay
Harried Scott
Zhong Wenge
Original Assignee
Amgen Inc
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Publication date
Application filed by Amgen Inc filed Critical Amgen Inc
Publication of AR086750A1 publication Critical patent/AR086750A1/es

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    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom 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
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Abstract

Compuestos basados en amidas. Composiciones que los contienen. Su uso en el tratamiento del dolor agudo, del dolor en los dientes, de la cefalea en general, de la migraña, de la cefalea combinada, de los síndromes vasculares y no vasculares combinados, de la cefalea provocada por la tensión, de la inflamación en general, de la artritis, de las enfermedades reumáticas, de la osteoartritis, de los trastornos inflamatorios en el intestino, de los trastornos inflamatorios en los ojos, de los trastornos inflamatorios en la vejiga, de la inestabilidad a nivel de la vejiga, de la psoriasis, de las afecciones inflamatorias de la piel, de las afecciones inflamatorias crónicas, del dolor inflamatorio o de la hiperalgesia o la alodinia asociada a él, del dolor neuropático o de la hiperalgesia o la alodinia asociada a él, del dolor provocado por la neuropatía diabética, de la causalgia, del dolor que es mantenido por el sistema nervioso simpático, de los síndromes de diferenciación, del asma, de los daños o las disfunciones en el tejido epitelial, del herpes simple, de las alteraciones en la motilidad de las vísceras en los sistemas respiratorio, genitourinario, gastrointestinal o vascular, de las heridas, de las quemaduras, de las reacciones alérgicas en la piel, del prurito, del vitíligo, de los trastornos gastrointestinales en general, de la úlcera gástrica, de la úlcera duodenal, de la diarrea, de las lesiones gástricas inducidas por agentes necrosantes, de la pérdida de cabello, de la rinitis vasomotora o alérgica o de los trastornos en los bronquios. Reivindicación 1: Un compuesto caracterizado porque que tiene la estructura de formula (1) o cualquier sal farmacéuticamente aceptable del mismo, donde: m es 0, 1, 2 ó 3; n es 0 ó 1; X¹ es C(R⁴) o N; X² es C o N; R¹ se selecciona entre alquilo C₁₋₆ o un anillo saturado, parcialmente saturado o insaturado, monocíclico de 3, 4, 5, 6 ó 7 miembros o bicíclico de 7, 8, 9, 10 u 11 miembros, unido en forma directa, unido por alquilo C₁₋₂ o unido por alquil C₁₋₂-O que contiene 0, 1, 2, 3 ó 4 átomos seleccionados entre N, O y S, pero no contiene más que un átomo de O ó S, donde el alquilo C₁₋₆ y el anillo están sustituidos con 0, 1, 2 ó 3 sustituyentes seleccionados en forma independiente entre halo, oxo, alquilo C₁₋₆, haloalquilo C₁₋₄, ciano, nitro, -C(=O)Rᵃ, -C(=O)ORᵃ, -C(=O)NRᵃRᵃ, -C(=NRᵃ)NRᵃRᵃ, -ORᵃ, -OC(=O)Rᵃ, -OC(=O)NRᵃRᵃ, -OC(=O)N(Rᵃ)S(=O)₂Rᵃ, -O-alquil C₂₋₆-NRᵃRᵃ, O-alquil C₂₋₆-ORᵃ, -SRᵃ, -S(=O)Rᵃ, -S(=O)₂Rᵃ, -S(=O)₂NRᵃRᵃ, -S(=O)₂N(Rᵃ)C(=O)Rᵃ, -S(=O)₂N(Rᵃ)C(=O)ORᵃ, -S(=O)₂N(Rᵃ)C(=O)NRᵃRᵃ, -NRᵃRᵃ, -N(Rᵃ)C(=O)Rᵃ, -N(Rᵃ)C(=O)ORᵃ, -N(Rᵃ)C(=O)NRᵃRᵃ, -N(Rᵃ)C(=NRᵃ)NRᵃRᵃ, -N(Rᵃ)S(=O)₂Rᵃ, -N(Rᵃ)S(=O)₂NRᵃRᵃ, NRᵃ-alquil C₂₋₆-NRᵃRᵃ y NRᵃ-alquil C₂₋₆-ORᵃ, donde el anillo está adicionalmente sustituido con 0 ó 1 anillo saturado, parcialmente saturado o insaturado monocíclico de 3, 4, 5, 6 ó 7 miembros unido en forma directa, unido a través de SO₂, unido a través de C(=O) o unido a través de CH₂ sustituido con 0, 1, 2 ó 3 grupos seleccionados entre halo, alquilo C₁₋₆, haloalquilo C₁₋₄, ciano, nitro, -C(=O)Rᵃ, -C(=O)ORᵃ, -C(=O)NRᵃRᵃ, -C(=NRᵃ)NRᵃRᵃ, -ORᵃ, -OC(=O)Rᵃ, -SRᵃ, -S(=O)Rᵃ, -S(=O)₂Rᵃ, -S(=O)₂NRᵃRᵃ, -NRᵃRᵃ, y -N(Rᵃ)C(=O)Rᵃ; R² se selecciona entre H, halo, ciano, Rᶜ, -C(=O)Rᵇ, -C(=O)ORᵇ, -C(=O)NRᵃRᵃ, -C(=NRᵃ)NRᵃRᵃ, -ORᵃ, -OC(=O)Rᵇ, -OC(=O)NRᵃRᵃ, -O-alquil C₂₋₆-NRᵃRᵃ, O-alquil C₂₋₆-ORᵃ, -SRᵃ, -S(=O)Rᵇ, -S(=O)₂Rᵇ, -S(=O)₂NRᵃRᵃ, -NRᵃRᵃ, -N(Rᵃ)C(=O)Rᵇ, -N(Rᵃ)C(=O)ORᵇ, -N(Rᵃ)C(=O)NRᵃRᵃ, -N(Rᵃ)C(=NRᵃ)NRᵃRᵃ, -N(Rᵃ)S(=O)₂Rᵇ, -N(Rᵃ)S(=O)₂NRᵃRᵃ, NRᵃ-alquil C₂₋₆-NRᵃRᵃ y NRᵃ-alquil C₂₋₆-ORᵃ; o R² es alquilo C₁₋₆ sustituido con 0, 1, 2 ó 3 sustituyentes seleccionados entre haloalquilo C₁₋₄, halo, ciano, nitro, -C(=O)Rᵇ, -C(=O)ORᵇ, -C(=O)NRᵃRᵃ, -C(=NRᵃ)NRᵃRᵃ, -ORᵃ, -OC(=O)Rᵇ, -OC(=O)NRᵃRᵃ, O-alquil C₂₋₆-NRᵃRᵃ, -O-alquil C₂₋₆-ORᵃ, -SRᵃ, -S(=O)Rᵇ, S(=O)₂Rᵇ, S(=O)₂NRᵃRᵃ, -NRᵃRᵃ, -N(Rᵃ)C(=O)Rᵇ, -N(Rᵃ)C(=O)ORᵇ, -N(Rᵃ)C(=O)NRᵃRᵃ, -N(Rᵃ)C(=NRᵃ)NRᵃRᵃ, -N(Rᵃ)S(=O)₂Rᵇ, -N(Rᵃ)S(=O)₂NRᵃRᵃ, NRᵃ-alquil C₂₋₆-NRᵃRᵃ y NRᵃ-alquilo C₂₋₆-ORᵃ, o R² es alquilo C₁₋₆ sustituido con 0, 1, 2 ó 3 sustituyentes halo y adicionalmente sustituido con 0 ó 1 sustituyentes seleccionados entre Rᶜ; R³ es H, alquilo C₁₋₈, haloalquilo C₁₋₄, halo, ciano, -C(=O)Rᵇ, -C(=O)ORᵇ, -C(=O)NRᵃRᵃ, -C(=NRᵃ)NRᵃRᵃ, -ORᵃ, -OC(=O)Rᵇ, -OC(=O)NRᵃRᵃ, -O-alquil C₂₋₆-NRᵃRᵃ, -O-alquil C₂₋₆-ORᵃ, -SRᵃ, -S(=O)Rᵇ, -S(=O)₂Rᵇ, -S(=O)₂NRᵃRᵃ, -NRᵃRᵃ, -N(Rᵃ)C(=O)Rᵇ, -N(Rᵃ)C(=O)ORᵇ, -N(Rᵃ)C(=O)NRᵃRᵃ, -N(Rᵃ)C(=NRᵃ)NRᵃRᵃ, -N(Rᵃ)S(=O)₂Rᵇ, N(Rᵃ)S(=O)₂NRᵃRᵃ, NRᵃ-alquil C₂₋₆-NRᵃRᵃ o NRᵃ-alquil C₂₋₆-ORᵃ; R⁴ es en forma independiente, en cada instancia, H, alquilo C₁₋₆, -haloalquilo C₁₋₃, -O-alquilo C₁₋₆, -O-haloalquilo C₁₋₃, -N(alquil C₁₋₆)alquilo C₁₋₆, -NH-alquilo C₁₋₆, -NC(=O)alquilo C₁₋₆, -N(alquil C₁₋₆)alquilo C₁₋₆, F, Cl, Br, CN, OH o NH₂; o R³ y R⁴ juntos forman un puente insaturado de cuatro átomos que contiene 0 ó 1 átomos de N, donde el puente está sustituido con 0, 1 ó 2 sustituyentes R⁵; R⁵ es en forma independiente, en cada instancia, F, CH₃ o CF₃; R⁶ es F; Rᵃ es en forma independiente, en cada instancia, H o Rᵇ; Rᵇ es en forma independiente, en cada instancia, fenilo, bencilo o alquilo C₁₋₆, donde el fenilo, bencilo y alquilo C₁₋₆ está sustituido con 0, 1, 2 ó 3 sustituyentes seleccionados entre halo, oxo, alquilo C₁₋₄, haloalquilo C₁₋₃, -O-alquilo C₁₋₄, -OH, -NH₂, -O-alquilo C₁₋₄, -O-haloalquilo C₁₋₄, -NH-alquilo C₁₋₄, y -N(alquil C₁₋₄)alquilo C₁₋₄; y Rᶜ es en forma independiente, en cada instancia, un anillo saturado, parcialmente saturado o insaturado monocíclico de 4, 5 ó 6 miembros que contiene 0, 1, 2, 3 ó 4 átomos seleccionados entre N, O y S, donde el alquilo C₁₋₆ y el anillo están sustituidos con 0 ó 1 grupos oxo sustituidos con 0, 1, 2 ó 3 sustituyentes seleccionados entre alquilo C₁₋₈, haloalquilo C₁₋₄, halo y ciano.
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Families Citing this family (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8952009B2 (en) 2012-08-06 2015-02-10 Amgen Inc. Chroman derivatives as TRPM8 inhibitors
ES2895174T3 (es) * 2014-09-29 2022-02-17 Scripps Research Inst Moduladores del receptor de esfingosina-1-fosfato para el tratamiento de trastornos cardiopulmonares
US9765026B2 (en) * 2015-08-28 2017-09-19 Scinopharm Taiwan, Ltd. Forms of apremilast and the process of making the same
CN113398124A (zh) * 2016-06-13 2021-09-17 田边三菱制药株式会社 用于治疗或预防血管舒缩症状的组合物
TWI799426B (zh) 2017-06-22 2023-04-21 英商克拉德夫製藥有限公司 人類ｓｔｉｎｇ之小分子調節劑
WO2018234805A1 (en) * 2017-06-22 2018-12-27 Curadev Pharma Limited SMALL MOLECULAR MODULATORS OF HUMAN STING
TW201929855A (zh) * 2017-12-19 2019-08-01 日商田邊三菱製藥股份有限公司 用於治療或預防血管舒縮症狀的組成物及方法
EP3768659B1 (en) * 2018-03-21 2023-07-19 Piramal Pharma Limited An improved asymmetric synthesis of alpha-(diarylmethyl) alkyl amines
US11279672B2 (en) * 2018-04-18 2022-03-22 Piramal Pharma Limited Asymmetric synthesis of alpha-branched chiral amines
CN110981795B (zh) * 2019-12-18 2021-02-12 武汉世纪久海检测技术有限公司 一种利用2-氰基异烟酸甲酯制备2-氨酰基异烟酸的方法
PE20231383A1 (es) 2020-06-17 2023-09-12 Merck Sharp And Dohme Llc 2-oxoimidazolidin-4-carboxamidas como inhibidores de nav1.8
CN115108980B (zh) * 2022-06-22 2023-06-16 济南大学 一种2-甲基喹啉类化合物的4号位酰基化衍生物的制备方法

Family Cites Families (186)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US2483250A (en) * 1949-09-27 Tt a it tt
DE2417763A1 (de) 1974-04-11 1975-10-30 Bayer Ag Carbonsaeureamide, verfahren zu ihrer herstellung sowie ihre verwendung als arzneimittel
DE2428673A1 (de) 1974-06-14 1976-01-02 Bayer Ag Carbonsaeureamide, verfahren zu ihrer herstellung sowie ihre verwendung als arzneimittel
JPS53141271U (es) 1977-04-14 1978-11-08
PT72878B (en) 1980-04-24 1983-03-29 Merck & Co Inc Process for preparing mannich-base hydroxamic acid pro-drugs for the improved delivery of non-steroidal anti-inflammatory agents
US5081131A (en) 1986-01-13 1992-01-14 American Cyanamid Company Omega-((hetero)alkyl)benz(cd)-indol-2-amines
US5223499A (en) 1989-05-30 1993-06-29 Merck & Co., Inc. 6-amino substituted imidazo[4,5-bipyridines as angiotensin II antagonists
AU640016B2 (en) 1990-05-30 1993-08-12 Imperial Chemical Industries Plc Hydroquinazoline derivatives
US5380721A (en) 1990-09-10 1995-01-10 Sterling Winthrop Inc. Aryl-fused and hetaryl-fused-2,4-diazepine and 2,4-diazocine antiarrhythmic agents
WO1992012973A1 (fr) 1991-01-23 1992-08-06 Nippon Kayaku Kabushiki Kaisha Derive de chromane
ES2036926B1 (es) 1991-08-08 1994-01-16 Uriach & Cia Sa J "procedimiento para la obtencion de derivados de la (2-alquil-3-piridil)metilpiperazina".
JP2600644B2 (ja) 1991-08-16 1997-04-16 藤沢薬品工業株式会社 チアゾリルベンゾフラン誘導体
DE4135474A1 (de) 1991-10-28 1993-04-29 Bayer Ag 2-aminomethyl-chromane
DE4138819A1 (de) 1991-11-26 1993-05-27 Basf Ag Hydroxypyridoncarbonsaeureamide, deren herstellung und verwendung
GB9127041D0 (en) 1991-12-20 1992-02-19 Fujisawa Pharmaceutical Co New use
FR2692895A1 (fr) 1992-06-26 1993-12-31 Adir Nouveaux 1-oxo 2,4,5,6-tétrahydro 2,3,7-triazaphénalènes leurs procédés de préparation et les compositions pharmaceutiques qui les contiennent.
DE4304455A1 (de) 1993-02-15 1994-08-18 Bayer Ag Heterocyclisch substituierte Phenyl-cyclohexan-carbonsäurederivate
JPH07179488A (ja) 1993-11-12 1995-07-18 Tanabe Seiyaku Co Ltd グルコサミン誘導体、その製法及びその合成中間体
JPH07285962A (ja) 1994-04-20 1995-10-31 Nissan Chem Ind Ltd ピリジンカルボン酸アミド誘導体
BR9510360A (pt) 1994-12-23 1997-12-23 Thomae Gmbh Dr K Derivados de piperazina medicamentos contendo esses compostos sua aplicação e processo para sua preparação
US5916906A (en) 1995-03-14 1999-06-29 Shaskan; Edward G. Compositions comprising nicotinylalanine and an inhibitor of glycine conjugation or vitamin B6
US5891872A (en) 1995-04-07 1999-04-06 Schering Corporation Tricyclic compounds
MY114302A (en) 1995-04-19 2002-09-30 Ihara Chemical Ind Co Benzylsulfide derivative, process for its production and pesticide
DE19518681A1 (de) 1995-05-22 1996-11-28 Bayer Ag Verfahren zur Herstellung von 5,6-Dihydro-1,3-oxazinen
DE19523087A1 (de) 1995-06-26 1997-01-02 Bayer Ag 1,3-Oxa(thia)zin-Derivate
IL118631A (en) 1995-06-27 2002-05-23 Tanabe Seiyaku Co History of pyridazinone and processes for their preparation
GB9518552D0 (en) 1995-09-11 1995-11-08 Fujisawa Pharmaceutical Co New heterocyclic compounds
EP0858457A1 (de) 1995-10-20 1998-08-19 Dr. Karl Thomae GmbH 5-gliedrige heterocyclen, diese verbindungen enthaltende arzneimittel und deren verwendung sowie verfahren zu ihrer herstellung
GB9525828D0 (en) 1995-12-18 1996-02-21 Bayer Ag Use of hetarylacetic acid derivatives
US5977090A (en) 1996-09-27 1999-11-02 Guilford Pharmaceuticals Inc. Pharmaceutical compositions and methods of treating compulsive disorders using NAALADase inhibitors
US6268384B1 (en) 1997-08-29 2001-07-31 Vertex Pharmaceuticals Incorporated Compounds possessing neuronal activity
US6075029A (en) 1998-01-02 2000-06-13 Cell Therapeutics, Inc. Xanthine modulators of metabolism of cellular P-450
CA2318184C (en) 1998-01-21 2008-11-18 Banyu Pharmaceutical Co., Ltd. Substituted 5-(2,2-difluoro-1,3-benzodioxol-5-yl) cyclopentenopyridine derivative as selective endothelin antagonists
AU761737B2 (en) 1998-06-03 2003-06-12 Gpi Nil Holdings, Inc. N-oxide of heterocyclic ester, amide, thioester, or ketone hair growth compositions and uses
US5910595A (en) 1998-06-26 1999-06-08 Salsbury Chemicals, Inc. Process for preparing oximidazoles
US6617351B1 (en) 1998-07-31 2003-09-09 Eli Lilly And Company Amide, carbamate, and urea derivatives
US6166028A (en) 1998-12-09 2000-12-26 American Home Products Corporation Diaminopuridine-containing thiourea inhibitors of herpes viruses
WO2000035889A1 (fr) 1998-12-11 2000-06-22 Sankyo Company, Limited Benzylamines substituees
AU3127900A (en) 1998-12-23 2000-07-31 Du Pont Pharmaceuticals Company Thrombin or factor xa inhibitors
US6200993B1 (en) 1999-05-05 2001-03-13 Merck Frosst Canada & Co. Heterosubstituted pyridine derivatives as PDE4 inhibitors
CZ290178B6 (cs) 1999-07-22 2002-06-12 Sankyo Company Limited Deriváty cyklobutenu
GB9919588D0 (en) 1999-08-18 1999-10-20 Hoechst Schering Agrevo Gmbh Fungicidal compounds
BR0013593A (pt) 1999-09-01 2002-05-07 Unilever Nv Método para alvejar manchas de tecido
EP1208188A1 (en) 1999-09-01 2002-05-29 Unilever Plc Composition and method for bleaching a substrate
BR0013592A (pt) 1999-09-01 2002-05-07 Unilever Nv Embalagem comercial para alvejar manchas de tecido em um licor de lavagem aquoso, e, uso da mesma
US7291641B2 (en) 1999-10-11 2007-11-06 Societe De Conseils De Recherches Et D'applications Scientifiques (S.C.R.A.S.) Derivatives of heterocycles with 5 members, their preparation and their use as medicaments
IL139450A0 (en) 1999-11-10 2001-11-25 Pfizer Prod Inc Methods of administering apo b-secretion/mtp inhibitors
CA2325358C (en) 1999-11-10 2005-08-02 Pfizer Products Inc. 7-¬(4'-trifluoromethyl-biphenyl-2-carbonyl)amino|-quinoline-3-carboxylic acid amides, and methods of inhibiting the secretion of apolipoprotein b
EP1457490A1 (en) 1999-11-10 2004-09-15 Takeda Chemical Industries, Ltd. 5-membered N-heterocyclic compounds with hypoglycemic and hypolipidemic activity
TW574193B (en) 1999-12-03 2004-02-01 Astrazeneca Ab Novel phenalkyloxy-phenyl derivatives, pharmaceutical composition containing the same and their uses
BR0016818A (pt) 1999-12-28 2002-10-01 Pfizer Prod Inc Inibidores não-peptidila de adesão celular dependente de vla-4 úteis no tratamento de doenças inflamatórias, auto-imunes e respiratórias
MXPA02007289A (es) 2000-01-28 2003-09-22 Melacure Therapeutics Ab Agonistas y antagonistas novedosos de receptores de melanocortina.
WO2001058869A2 (en) 2000-02-11 2001-08-16 Bristol-Myers Squibb Company Cannabinoid receptor modulators, their processes of preparation, and use of cannabinoid receptor modulators in treating respiratory and non-respiratory diseases
EP1276726A2 (en) 2000-04-27 2003-01-22 Abbott Laboratories Substituted phenyl farnesyltransferase inhibitors
US20020019527A1 (en) 2000-04-27 2002-02-14 Wei-Bo Wang Substituted phenyl farnesyltransferase inhibitors
JP2001354563A (ja) 2000-06-09 2001-12-25 Sankyo Co Ltd 置換ベンジルアミン類を含有する医薬
US6448281B1 (en) 2000-07-06 2002-09-10 Boehringer Ingelheim (Canada) Ltd. Viral polymerase inhibitors
US6417367B1 (en) 2000-08-11 2002-07-09 Pfizer Inc. Methods of making quinoline amides
US20030050211A1 (en) 2000-12-14 2003-03-13 Unilever Home & Personal Care Usa, Division Of Conopco, Inc. Enzymatic detergent compositions
WO2002051396A1 (fr) 2000-12-26 2002-07-04 Sankyo Company, Limited Compositions pharmaceutiques contenant des derives de cyclobutene
JP2002302439A (ja) 2001-01-19 2002-10-18 Sankyo Co Ltd シクロブテン誘導体を含有する回腸型胆汁酸トランスポーター阻害剤
US20040106635A1 (en) 2001-03-29 2004-06-03 Iwao Takamuro Spiroisoquinoline compound, a method for preparing the same and an intermediate thereof
DE10121003A1 (de) 2001-04-28 2002-12-19 Aventis Pharma Gmbh Anthranilsäureamide, Verfahren zur Herstellung, ihrer Verwendung als Medikament sowie sie enthaltende pharmazeutische Zubereitungen
MY130373A (en) 2001-10-29 2007-06-29 Malesci Sas Linear basic compounds having nk-2 antagonist activity and formulations thereof
ATE391505T1 (de) 2001-11-27 2008-04-15 Hoffmann La Roche Benzothiazole derivative
AU2002344567A1 (en) 2001-11-28 2003-06-10 Daiso Co., Ltd. Heterocyclic amide compounds as apolipoprotein b inhibitors
AR037746A1 (es) 2001-12-06 2004-12-01 Novartis Ag Compuestos derivados de amidoacetonitrilo, un procedimiento para su preparacion, un procedimiento para la preparacion de compuestos intermediarios, una composicion para combatir parasitos, un procedimiento para combatir dichos parasitos, y el empleo de dichos derivados para la preparacion de una com
SE0104248D0 (sv) 2001-12-14 2001-12-14 Astrazeneca Ab Method of treatment
ATE392897T1 (de) 2002-02-04 2008-05-15 Hoffmann La Roche Chinolinderivate als npy antagonisten
AU2003240757B2 (en) 2002-03-28 2008-07-03 Merck Serono Sa Thiazolidine carboxamide derivatives as modulators of the prostaglandin F receptor
JP4570878B2 (ja) 2002-04-11 2010-10-27 メルク・シャープ・エンド・ドーム・コーポレイション 選択的糖質コルチコイド受容体モジュレーターとしての１Ｈ−ベンゾ［ｆ］インダゾール−５−イル誘導体
FR2838739B1 (fr) 2002-04-19 2004-05-28 Sanofi Synthelabo Derives de n-[phenyl(piperidin-2-yl)methyl)benzamide, leur preparation et leur application en therapeutique
US20050239656A1 (en) 2002-04-26 2005-10-27 Toru Koyanagi Pyridine compounds or salts thereof and herbicides containing the same
US7375093B2 (en) 2002-07-05 2008-05-20 Intrexon Corporation Ketone ligands for modulating the expression of exogenous genes via an ecdysone receptor complex
FR2842805A1 (fr) 2002-07-29 2004-01-30 Sanofi Synthelabo Derives de n-[phenyl(piperidin-2-yl)methyl]benzamide,leur preparation et leur application et therapeutique
GB0221697D0 (en) 2002-09-18 2002-10-30 Unilever Plc Novel compouds and their uses
CA2499497A1 (en) 2002-09-27 2004-04-08 Merck & Co., Inc. Substituted pyrimidines
JP2004115450A (ja) 2002-09-27 2004-04-15 Tanabe Seiyaku Co Ltd 医薬組成物
WO2004039795A2 (en) 2002-10-29 2004-05-13 Fujisawa Pharmaceutical Co., Ltd. Amide compounds for the treatment of hyperlipidemia
ES2350977T3 (es) 2002-11-05 2011-01-28 Glaxo Group Limited Agentes antibacterianos.
JP4261884B2 (ja) 2002-11-26 2009-04-30 株式会社ネオス 水溶性金属加工油剤組成物
JP2004203871A (ja) 2002-12-13 2004-07-22 Yamanouchi Pharmaceut Co Ltd 医薬組成物
AU2003290333A1 (en) 2002-12-24 2004-07-22 Biofocus Plc Compound libraries of imidazo(1,5-a)pyridin-3-yl derivatives and related heterobicycles for targetting compounds capable of binding to g-protein coupled receptors
WO2004072018A1 (ja) 2003-02-12 2004-08-26 Takeda Pharmaceutical Company Limited アミン誘導体
CA2524352A1 (en) 2003-05-09 2004-11-18 Pharmacia & Upjohn Company Llc Substituted pyrimidine derivatives
EP1660454A1 (en) * 2003-07-07 2006-05-31 Vernalis (R&D) Limited Azacyclic compounds as inhibitors of sensory neurone specific channels
CA2573951A1 (en) 2003-07-18 2005-01-27 Virochem Pharma Inc. Spiro compounds and methods for the modulation of chemokine receptor activity
US7094791B2 (en) 2003-07-31 2006-08-22 Avalon Pharmaceuticals, Inc. Derivatives of 3-hydroxy-pyrrole-2,4-dicarboxylic acid and uses thereof
JP2007504220A (ja) 2003-09-03 2007-03-01 ガラパゴス・エヌブイ イミダゾ［１，５−ａ］ピリジン又はイミダゾ［１，５−ａ］ピペリジン誘導体および５ＨＴ２Ａ受容体関連障害に対する薬剤の製造のためのその使用
GB0320983D0 (en) 2003-09-08 2003-10-08 Biofocus Plc Compound libraries
CA2579609A1 (en) 2003-09-10 2005-03-17 Virochem Pharma Inc. Spirohydantoin compounds and methods for the modulation of chemokine receptor activity
TW200526631A (en) * 2003-10-07 2005-08-16 Renovis Inc Amide derivatives as ion-channel ligands and pharmaceutical compositions and methods of using the same
WO2005042524A1 (en) 2003-10-30 2005-05-12 Virochem Pharma Inc. Pyridine carboxamide and methods for inhibiting hiv integrase
EP1716137A1 (en) 2004-02-04 2006-11-02 Pfizer Products Incorporated Substituted quinoline compounds
GB0403578D0 (en) 2004-02-18 2004-03-24 Biofocus Discovery Ltd Compounds which interact with the G-protein coupled receptor family
EP1720855A4 (en) 2004-03-02 2008-12-17 Smithkline Beecham Corp HEMMER OF ACT ACTIVITY
CN1972914A (zh) 2004-03-31 2007-05-30 詹森药业有限公司 作为组胺h3受体配合体的非咪唑杂环化合物
DE102004022897A1 (de) 2004-05-10 2005-12-08 Bayer Cropscience Ag Azinyl-imidazoazine
US7550499B2 (en) 2004-05-12 2009-06-23 Bristol-Myers Squibb Company Urea antagonists of P2Y1 receptor useful in the treatment of thrombotic conditions
US20090105218A1 (en) 2004-05-29 2009-04-23 7Tm Pharma A/S CRTH2 Receptor Ligands For Therapeutic Use
DE102004039876A1 (de) 2004-06-23 2006-01-26 Lanxess Deutschland Gmbh Herstellung von fluorierten 1,3-Benzodioxanen
DE102004031323A1 (de) 2004-06-29 2006-01-19 Bayer Cropscience Ag Substituierte Pyridazincarboxamide und Derivate hiervon
US7378420B2 (en) 2004-08-30 2008-05-27 Neuromed Pharmaceuticals Ltd. Urea derivatives as calcium channel blockers
AR050926A1 (es) 2004-09-03 2006-12-06 Astrazeneca Ab Derivados de benzamida como inhibidores de la histonadesacetilasa(hdac)
KR100677149B1 (ko) 2004-11-12 2007-02-02 삼성전자주식회사 잉크 조성물
JPWO2006057448A1 (ja) 2004-11-26 2008-06-05 武田薬品工業株式会社 アリールアルカン酸誘導体
WO2006068594A1 (en) * 2004-12-21 2006-06-29 Astrazeneca Ab HETEROCYCLIC MCHr1 ANTAGONISTS AND THEIR USE IN THERAPY
EP1833832A1 (en) 2004-12-31 2007-09-19 GPC Biotech AG Napthyridine compounds as rock inhibitors
US20060173183A1 (en) 2004-12-31 2006-08-03 Alantos Pharmaceuticals, Inc., Multicyclic bis-amide MMP inhibitors
JP2008528580A (ja) 2005-01-27 2008-07-31 アストラゼネカ・アクチエボラーグ Ｐ２ｘ７受容体の阻害剤である新規二環式芳香族化合物
WO2006094246A2 (en) 2005-03-03 2006-09-08 Sirtris Pharmaceuticals, Inc. N-arylmethyl benzamide sirtuin modulators
JP5007788B2 (ja) 2005-05-16 2012-08-22 日産化学工業株式会社 ジヒドロアゾール置換ベンズアミド化合物及び有害生物防除剤
US20070155738A1 (en) 2005-05-20 2007-07-05 Alantos Pharmaceuticals, Inc. Heterobicyclic metalloprotease inhibitors
WO2006130403A1 (en) 2005-06-02 2006-12-07 Bayer Cropscience Ag Phenylalkyl substituted heteroaryl devivatives
CA2611376C (en) 2005-06-13 2013-09-10 Merck Sharp & Dohme Limited Therapeutic agents
CA2613517A1 (en) 2005-06-27 2007-01-04 Exelixis, Inc. Pyrazole based lxr modulators
US7968542B2 (en) 2005-07-15 2011-06-28 Nissan Chemical Industries, Ltd. Thiophene compounds and thrombopoietin receptor activators
CN100494167C (zh) 2005-08-02 2009-06-03 天津大学 抗乙肝病毒的叔胺氧化物及制备方法和制备药物的应用
WO2007017093A1 (en) 2005-08-04 2007-02-15 Bayer Healthcare Ag Substituted 2-benzyloxy-benzoic acid amide derivatives
EP1764098A1 (en) 2005-09-17 2007-03-21 Speedel Experimenta AG Diaminoalcohols derivatives for the treatment of Alzheimer, malaria, HIV
CA2628875A1 (en) 2005-11-10 2007-05-18 Bayer Healthcare Ag Diaryl ureas for treating diabetic neuropathy
DK1948176T3 (da) 2005-11-10 2011-04-18 Bayer Schering Pharma Ag Diarylurinstoffer til behandling af pulmonær hypertension
US7888376B2 (en) 2005-11-23 2011-02-15 Bristol-Myers Squibb Company Heterocyclic CETP inhibitors
DE102005059479A1 (de) 2005-12-13 2007-06-14 Merck Patent Gmbh Hydroxychinolinderivate
JP2009524585A (ja) 2005-12-15 2009-07-02 バイエル・ヘルスケア・アクチェンゲゼルシャフト ウイルス感染を処置するためのジアリールウレア
CA2633411A1 (en) 2005-12-15 2007-06-21 Bayer Healthcare Ag Diaryl ureas for treating inflammatory skin, eye and/or ear diseases
TWI412322B (zh) 2005-12-30 2013-10-21 Du Pont 控制無脊椎害蟲之異唑啉
EP1981882A4 (en) 2006-01-27 2009-11-18 Astrazeneca Ab QUINOLINES SUBSTITUTED BY AN AMIDE
US20100234351A1 (en) 2006-02-23 2010-09-16 Takeda Pharmaceutical Company Limited Fused nitrogen-comprising heterocyclic compound
DE102006012251A1 (de) 2006-03-15 2007-11-08 Grünenthal GmbH Substituierte 4-Amino-chinazolin-Derivate und ihre Verwendung zur Herstellung von Arzneimitteln
PL2010493T3 (pl) 2006-04-12 2016-08-31 Merck Sharp & Dohme Pirydyloamidy jako antagoniści kanałów wapniowych typu t
WO2007139930A2 (en) 2006-05-26 2007-12-06 Bayer Healthcare Llc Drug combinations with substituted diaryl ureas for the treatment of cancer
GB0611152D0 (en) 2006-06-06 2006-07-19 Ucb Sa Therapeutic agents
WO2008003746A1 (en) 2006-07-06 2008-01-10 Bayer Cropscience Sa N-(4-pyridin-2-ylbutyl) carboxamide derivatives, their process of preparation and their use as fungicides
WO2008014602A1 (en) 2006-07-25 2008-02-07 Envivo Pharmaceuticals, Inc. Quinoline derivatives
CA2661459A1 (en) * 2006-08-21 2008-02-28 F. Hoffmann-La Roche Ag Di-aromatic substituted amides as inhibitors for glyt1
US7834023B2 (en) 2006-09-20 2010-11-16 Portola Pharmaceuticals, Inc. Substituted dihydroquinazolines as platelet ADP receptor inhibitors
WO2008056687A1 (fr) 2006-11-09 2008-05-15 Daiichi Sankyo Company, Limited Nouveau dérivé de spiropipéridine
WO2008063669A1 (en) 2006-11-20 2008-05-29 Alantos Pharmaceuticals Holding, Inc. Heterobicyclic matrix metalloprotease inhibitors
AU2007321920A1 (en) 2006-11-20 2008-05-29 Alantos Pharmaceuticals Holding, Inc. Heterotricyclic metalloprotease inhibitors
EP2121621B1 (en) 2006-12-08 2014-05-07 Exelixis Patent Company LLC Lxr and fxr modulators
WO2008080015A2 (en) 2006-12-21 2008-07-03 Plexxikon, Inc. Compounds and methods for kinase modulation, and indications therefor
US20080293711A1 (en) 2007-03-08 2008-11-27 Clark Michael P Chemokine receptor modulators
JP2010523663A (ja) 2007-04-11 2010-07-15 メルク・シャープ・エンド・ドーム・コーポレイション 第３級アミド、スルホンアミド、カルバミン酸及び尿素末端基をもつｃｇｒｐ受容体アンタゴニスト
EP2161996B1 (en) 2007-06-05 2014-07-16 Merck Sharp & Dohme Corp. Heterocyclic carboxamide cgrp receptor antagonists
WO2009007749A2 (en) 2007-07-09 2009-01-15 Astrazeneca Ab Trisubstituted pyrimidine derivatives for the treatment of proliferative diseases
EP2187883A2 (en) 2007-08-10 2010-05-26 Genelabs Technologies, Inc. Nitrogen containing bicyclic chemical entities for treating viral infections
WO2009037570A2 (en) 2007-08-10 2009-03-26 Crystalgenomics, Inc. Pyridine derivatives and methods of use thereof
WO2009038812A1 (en) 2007-09-20 2009-03-26 Amgen Inc. Condensed piperidine derivatives useful as vanilloid receptor ligands
US8476297B2 (en) 2007-12-04 2013-07-02 Amgen Inc. TRP-M8 receptor ligands and their use in treatments
JPWO2009072621A1 (ja) 2007-12-07 2011-04-28 日産化学工業株式会社 置換ジヒドロアゾール化合物及び有害生物防除剤
ES2524883T3 (es) 2008-03-18 2014-12-15 Merck Sharp & Dohme Corp. 4-Hidroxipirimidina-5-carboxamidas sustituidas
EP2272841A1 (en) 2008-03-28 2011-01-12 Banyu Pharmaceutical Co., Ltd. Diarylmethylamide derivative having antagonistic activity on melanin-concentrating hormone receptor
AU2009235406A1 (en) 2008-04-11 2009-10-15 Merck Serono S.A. Sulfonamides
DE102008019838A1 (de) 2008-04-19 2009-12-10 Boehringer Ingelheim International Gmbh Neue Arylsulfonylglycin-Derivate, deren Herstellung und deren Verwendung als Arzneimittel
WO2009152010A1 (en) 2008-06-12 2009-12-17 Merck & Co., Inc. Branched 3- and 6-substituted quinolines as cgrp receptor antagonists
MX2010014441A (es) 2008-06-25 2011-01-21 Bayer Schering Pharma Ag Diaril ureas para tratar la insuficiencia cardiaca.
ES2610882T3 (es) * 2008-08-19 2017-05-03 Janssen Pharmaceutica, N.V. Antagonistas del receptor al mentol frío
CN101343313B (zh) 2008-09-03 2011-11-16 南京农业大学 一种葡萄糖二肽类化合物及其制备方法和用途
TWI389913B (zh) 2008-09-08 2013-03-21 Lg Life Sciences Ltd 并合雜環化合物
EP2337563B1 (en) 2008-09-08 2014-04-09 The Board of Trustees of The Leland Stanford Junior University Modulators of aldehyde dehydrogenase activity and methods of use thereof
WO2010046780A2 (en) 2008-10-22 2010-04-29 Institut Pasteur Korea Anti viral compounds
TW201030001A (en) 2008-11-14 2010-08-16 Amgen Inc Pyridine and pyrimidine derivatives as phosphodiesterase 10 inhibitors
UY32525A (es) 2009-04-03 2010-10-29 Astrazeneca Ab Compuestos que tienen actividad agonista del receptor de glucocorticosteroides
CA2757761A1 (en) * 2009-05-01 2010-11-04 Raqualia Pharma Inc. Sulfamoyl benzoic acid derivatives as trpm8 antagonists
CN105130957A (zh) 2009-05-29 2015-12-09 拉夸里亚创药株式会社 作为钙或钠通道阻滞剂的芳基取代羧酰胺衍生物
WO2010141330A1 (en) 2009-06-02 2010-12-09 Boehringer Ingelheim International Gmbh DERIVATIVES OF 6,7-DIHYDRO-5H-IMIDAZO[1,2-a]IMIDAZOLE-3-CARBOXYLIC ACID AMIDES
TW201103941A (en) * 2009-06-10 2011-02-01 Janssen Pharmaceutica Nv Benzimidazole derivatives useful as TRPM8 channel modulators
CA2769512C (en) 2009-07-29 2019-07-09 Duke University Compositions comprising fp receptor antagonists and their use for inhibiting hair growth
DE102009028929A1 (de) 2009-08-27 2011-07-07 Bayer Schering Pharma Aktiengesellschaft, 13353 Heterocyclisch-substituierte 2-Acetamido-5-Aryl-1,2,4-triazolone und deren Verwendung
UY32940A (es) 2009-10-27 2011-05-31 Bayer Cropscience Ag Amidas sustituidas con halogenoalquilo como insecticidas y acaricidas
CN102811723A (zh) 2010-01-06 2012-12-05 约瑟夫·P·埃里科 靶向药物研发的方法和组合物
WO2011094890A1 (en) 2010-02-02 2011-08-11 Argusina Inc. Phenylalanine derivatives and their use as non-peptide glp-1 receptor modulators
WO2011106632A1 (en) 2010-02-26 2011-09-01 Millennium Pharmaceuticals, Inc. Substituted hydroxamic acids and uses thereof
JPWO2011142359A1 (ja) 2010-05-10 2013-07-22 日産化学工業株式会社 スピロ化合物及びアディポネクチン受容体活性化薬
US8669252B2 (en) 2010-05-17 2014-03-11 Merck Sharp & Dohme Corp. Prolylcarboxypeptidase inhibitors
JP2013528169A (ja) 2010-05-27 2013-07-08 バイエル・クロップサイエンス・アーゲー 殺菌剤としてのピリジニルカルボン酸誘導体
JP2013540145A (ja) 2010-10-21 2013-10-31 ウニベルシテート デス ザールランデス コルチゾール依存性疾患の治療用の選択的ｃｙｐ１１ｂ１阻害剤
MY165612A (en) 2010-11-05 2018-04-18 Senomyx Inc Compounds useful as modulators of trpm8
PT3366688T (pt) 2010-12-08 2022-05-11 Us Health Pirazolopirimidinas substituídas como ativadores de glucocerebrosidase
WO2012082862A2 (en) 2010-12-14 2012-06-21 Beth Israel Deaconess Medical Center Androgen receptor inhibitors and methods of use thereof
WO2012079624A1 (en) 2010-12-15 2012-06-21 Ppg Europe Bv Drier composition and use thereof
US20130324522A1 (en) 2010-12-17 2013-12-05 The Rockefeller University Insect odorant receptor antagonists
MX339873B (es) 2011-02-28 2016-06-15 Genentech Inc Inhibidores de serina/treonina cinasa.
WO2012120398A1 (en) 2011-03-04 2012-09-13 Pfizer Limited Aryl substituted carboxamide derivatives as trpm8 modulators
MX2013015058A (es) 2011-06-24 2014-01-20 Amgen Inc Antagonistas de melastatina 8 de potencial receptor transitorio y su uso en tratamientos.

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