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AR038420A1 - Compuesto de amida, procedimiento para la preparacion del mismo, su uso para la fabricacion de un medicamento y composicion farmaceutica que lo comprende - Google Patents

Compuesto de amida, procedimiento para la preparacion del mismo, su uso para la fabricacion de un medicamento y composicion farmaceutica que lo comprende

Info

Publication number
AR038420A1
AR038420A1 ARP030100474A ARP030100474A AR038420A1 AR 038420 A1 AR038420 A1 AR 038420A1 AR P030100474 A ARP030100474 A AR P030100474A AR P030100474 A ARP030100474 A AR P030100474A AR 038420 A1 AR038420 A1 AR 038420A1
Authority
AR
Argentina
Prior art keywords
methyl
pyrazol
carboxamide
phenyl
alkyl
Prior art date
Application number
ARP030100474A
Other languages
English (en)
Original Assignee
Glaxo Group Ltd
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
Priority claimed from GB0203680A external-priority patent/GB0203680D0/en
Priority claimed from GB0203677A external-priority patent/GB0203677D0/en
Priority claimed from GB0203673A external-priority patent/GB0203673D0/en
Priority claimed from GB0209032A external-priority patent/GB0209032D0/en
Priority claimed from GB0209003A external-priority patent/GB0209003D0/en
Priority claimed from GB0209035A external-priority patent/GB0209035D0/en
Priority claimed from GB0221318A external-priority patent/GB0221318D0/en
Application filed by Glaxo Group Ltd filed Critical Glaxo Group Ltd
Publication of AR038420A1 publication Critical patent/AR038420A1/es

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/08Drugs for disorders of the alimentary tract or the digestive system for nausea, cinetosis or vertigo; Antiemetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/14Prodigestives, e.g. acids, enzymes, appetite stimulants, antidyspeptics, tonics, antiflatulents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/06Antiasthmatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/08Bronchodilators
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/10Drugs for disorders of the urinary system of the bladder
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/02Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/04Antipruritics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/06Antipsoriatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/04Centrally acting analgesics, e.g. opioids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/06Antimigraine agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D215/00Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/16Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms 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
    • C07D215/38Nitrogen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pulmonology (AREA)
  • Dermatology (AREA)
  • Pain & Pain Management (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Endocrinology (AREA)
  • Nutrition Science (AREA)
  • Urology & Nephrology (AREA)
  • Reproductive Health (AREA)
  • Rheumatology (AREA)
  • Hospice & Palliative Care (AREA)
  • Otolaryngology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Quinoline Compounds (AREA)
  • Other In-Based Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

Uso del compuesto de la fórmula (1) o una de sus sales o solvatos farmacéuticamente aceptables para la fabricación de un medicamento para el tratamiento o profilaxis de trastornos en los que es beneficioso el antagonismo del receptor vainilloide (VR1). Procedimiento para preparar tales compuestos y composición farmacéutica que los comprende. Reivindicación 1:Un compuesto de amida caracterizado porque responde a la fórmula (1) o una de sus sales o solvatos farmacéuticamente aceptables, en la que, P se selecciona entre fenilo, heteroarilo o heterociclilo; R1 y R2 se seleccionan independientemente entre halo, alquilo, alcoxi, cicloalquilo, aralquilo, aralcoxi, cicloalquilalquilo, cicloalquilalcoxi, -CN, -NO2, -OH, =O, -OCF3, -CF3, -NR4R5, S(O)mR6, -S(O)2NR4R5, -OS(O)2R6, -OS(O)2CF3, -O(CH2)nNR4R5, -C(O)CF3, -C(O)alquilo, -C(O)cicloalquilo, -C(O)aralquilo, -C(O)Ar, -C(O)(CH2)nOR6, -C(O)(CH2)nNR4R5, -C(O)alcoxi, -C(O)NR4R5, -(CH2)nC(O)alcoxi, -(CH2)nOC(O)R6, -O(CH2)nOR6, -(CH2)nOR6, -(CH2)nR4R5, -(CH2)nC(O)NR4R5, -(CH2)nN(R4)C(O)R6, -(CH2)nS(O)2NR4R5, -(CH2)nN(R4)S(O)2R6, -ZAr, -(CH2)nS(O)2R6, -(OCH2)nS(O)2R6, -N(R4)S(O)2R6, -N(R4)C(O)R6, -(CH2)nN(R4)S(O)2R6, -(CH2)nN(R4)C(O)R6 o -(CH2)nC(O)alquilo; R3 se selecciona entre alquilo, alcoxi, -CF3, halo, -O(CH2)nOR6, -O(CH2)nNR4R5, fenilo, ciclohexilo, benzo[1,3]dioxiolilo, morfolinilo, piridilo, pirimidinilo, pirazinilo, piperazinilo, piperidinilo, piridizinilo, tienilo, furilo, pirazolilo, pirrolilo, triazolilo, indanilo, imidazolilo, oxazolilo, tiazolilo, oxadiazolilo, isotiazolilo, isoxazolilo o tiadiazolilo; donde dichos grupos alquilo, alcoxi, fenilo, ciclohexilo, benzo[1,3]dioxolilo, morfolinilo, piridilo, pirimidinilo, pirazinilo, piperazinilo, piperidinilo, piridizinilo, tienilo, furilo, pirazolilo, pirrolilo, triazolilo, indanilo, imidazolilo, oxazolilo, tiazolilo, oxadiazolilo, isotiazolilo, isoxazolilo o tiadiazolilo pueden estar opcionalmente sustituidos con uno o más grupos, que pueden ser iguales o diferentes, seleccionados de R2; R4 y R5 pueden ser iguales o diferentes y representa -H o alquilo o R4 y R5 junto con el átomo de nitrógeno al que están unidos forman un anillo heterocíclico; R6 es -H, alquilo o arilo; R7 es -H, alquilo o arilo; R8 se selecciona entre -H, alquilo, hidroxialquilo, cicloalquilo, aralquilo, alcoxialquilo, cicloalquilalquilo, heterociclilalquilo, -S(O)mR6, -C(O)CF3, -C(O)alquilo, -C(O)cicloalquilo, -C(O)aralquilo, -C(O)Ar, -C(O)(CH2)nOR6, -C(O)(CH2)nNR4R5, -C(O)alcoxi, -C(O)NR4R5, -(CH2)nC(O)alcoxi, -(CH2)nOC(O)R6, -O(CH2)nOR6, -(CH2)nOR6, -(CH2)nR4R5, -(CH2)nC(O)NR4R5, -(CH2)nN(R4)C(O)R6, -(CH2)nS(O)2NR4R5, -(CH2)nN(R4)S(O)2R6, -(CH2)nS(O)2R6, -(CH2)nS(O)2R6, -(CH2)nN(R4)S(O)2R6, -(CH2)nN(R4)C(O)R6 o -(CH2)nC(O)alquilo; o cuando X es NR8 e Y es C(R9)2, R8 se puede combinar con R1 para formar un grupo de benzoquinuclidina; R9 es -H o R1; Ar es arilo o heteroarilo, cada uno de los cuales puede estar opcionalmente sustituido con R2; Z es un enlace, O, S, NR7 o CH2; m es 0, 1 o 2; n es un número entero de 1 a 6; q y r se seleccionan independientemente entre 0, 1, 2 o 3; s es 0, 1, 2, o 3; y X e Y se seleccionan entre las combinaciones (Tabla 1) con la condición de que dicho compuesto de la fórmula (1) no es un compuesto seleccionado entre: N-{3-[(N,N-dimetilamino)metil]-1,2,3,4-tetrahidro-7-quinolinil}-4-bifenilcarboxamida; N-{3-[(N,N-dimetilamino)metil]-1-formil-1,2,3,4-tetrahidro-7-quinolinil}-4-bifenilcarboxamida, N-{1-acetil-3-[(N,N-dimetilamino)metil]-1,2,3,4-tetrahidro-7-quinolinil}-4-bifenilcarboxamida, N-{3-[(N,N-dimetilamino)metil]-1-metilsulfonil-1,2,3,4-tetrahidro-7-quinolinil}-4-bifenilcarboxamida; 5-amino-N-isoquinolin-5-il-1-[3-(trifluorometil)fenil]-1H-pirazol-3-carboxamida, 5-metil-N-quinolin-8-il-1-[3-(trifluorometil)fenil]-1H-pirazol-3-carboxamida, 5-metil-N-quinolin-7-il-1-[3-trilfuorometil)fenil]-1H-pirazol-3-carboxamida; 5-metil-N-quinolin-3-il-1-[3-(trifluorometil)fenil]-1H-pirazol-3-carboxamida, N-isoquinolin-5-il-5-metil-1-[3-(trifluorometil)fenil]-1H-pirazol-3-carboxamida, 5-metil-N-quinolin-5-il-1-[3-(trifluorometil)fenil]-1H-pirazol-3-carboxamida, 1-(3-clorofenil)-N-isoquinolin-5-il-5-metil-1H-pirazol-3-carboxamida, N-isoquinolin-5-il-1-(3-metoxifenil)-5-metil-1H-pirazol-3-carboxamida, 1-(3-fluorofenil)-N-isoquinolin-5-il-5-metil-1H-pirazol-3-carboxamida, 1-(2-cloro-5-trifluorometilfenil)-N-isoquinolin-5-il-5-metil-1H-pirazol-3-carboxamida, 5-metil-N-(3-metilisoquinolin-5-il)-1-[3-(trifluorometil)fenil]-1H-pirazol-3-carboxamida, y 5-metil-N-(1,2,3,4-tetrahidroisoquinolin-5-il)-1-[3-(trifluorometil)fenil]-1H-pirazol-3-carboxamida.
ARP030100474A 2002-02-15 2003-02-13 Compuesto de amida, procedimiento para la preparacion del mismo, su uso para la fabricacion de un medicamento y composicion farmaceutica que lo comprende AR038420A1 (es)

Applications Claiming Priority (7)

Application Number Priority Date Filing Date Title
GB0203680A GB0203680D0 (en) 2002-02-15 2002-02-15 Novel compounds
GB0203677A GB0203677D0 (en) 2002-02-15 2002-02-15 Novel compounds
GB0203673A GB0203673D0 (en) 2002-02-15 2002-02-15 Novel compounds
GB0209032A GB0209032D0 (en) 2002-04-19 2002-04-19 Novel compounds
GB0209003A GB0209003D0 (en) 2002-04-19 2002-04-19 Novel compounds
GB0209035A GB0209035D0 (en) 2002-04-19 2002-04-19 Novel compounds
GB0221318A GB0221318D0 (en) 2002-09-13 2002-09-13 Novel compounds

Publications (1)

Publication Number Publication Date
AR038420A1 true AR038420A1 (es) 2005-01-12

Family

ID=27739514

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP030100474A AR038420A1 (es) 2002-02-15 2003-02-13 Compuesto de amida, procedimiento para la preparacion del mismo, su uso para la fabricacion de un medicamento y composicion farmaceutica que lo comprende

Country Status (10)

Country Link
US (1) US7538121B2 (es)
EP (2) EP2033953A1 (es)
JP (1) JP2005526723A (es)
AR (1) AR038420A1 (es)
AT (1) ATE416168T1 (es)
AU (1) AU2003245773A1 (es)
DE (1) DE60325025D1 (es)
ES (1) ES2316777T3 (es)
TW (1) TW200403223A (es)
WO (1) WO2003068749A1 (es)

Families Citing this family (95)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2033951A3 (en) 2002-02-01 2009-12-23 Euro-Celtique S.A. 2-Piperazine-pyridines useful for treating pain
US6974818B2 (en) 2002-03-01 2005-12-13 Euro-Celtique S.A. 1,2,5-thiadiazol-3-YL-piperazine therapeutic agents useful for treating pain
JP2005526137A (ja) 2002-05-17 2005-09-02 ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプ アミノテトラリン−誘動尿素のバニロイドvr1受容体調節剤
CA2491079C (en) 2002-06-28 2011-10-04 Donald J. Kyle Therapeutic piperazine derivatives useful for treating pain
US7262194B2 (en) 2002-07-26 2007-08-28 Euro-Celtique S.A. Therapeutic agents useful for treating pain
GB0221157D0 (en) * 2002-09-12 2002-10-23 Glaxo Group Ltd Novel treatment
US7157462B2 (en) 2002-09-24 2007-01-02 Euro-Celtique S.A. Therapeutic agents useful for treating pain
GB0226724D0 (en) 2002-11-15 2002-12-24 Merck Sharp & Dohme Therapeutic agents
JP4422034B2 (ja) 2002-12-06 2010-02-24 バイエル・ヘルスケア・アクチェンゲゼルシャフト テトラヒドロ−ナフタレン誘導体
CA2508845C (en) * 2002-12-09 2012-02-21 Bayer Healthcare Ag Tetrahydro-naphthalene derivatives as vanilloid receptor antagonists
EP1575918A2 (en) * 2002-12-19 2005-09-21 Neurogen Corporation Substituted biaryl-4-carboxylic acid arylamide analogues as capsaicin receptor modulators
SE0301446D0 (sv) 2003-05-16 2003-05-16 Astrazeneca Ab New Compounds
WO2004103954A1 (ja) * 2003-05-20 2004-12-02 Ajinomoto Co., Inc. アミド誘導体
PL1632477T3 (pl) * 2003-06-12 2017-07-31 Astellas Pharma Inc. Pochodna benzamidu lub jej sól
TWI287010B (en) 2003-06-12 2007-09-21 Euro Celtique Sa Therapeutic agents useful for treating pain
ES2358426T3 (es) * 2003-07-23 2011-05-10 Synta Pharmaceuticals Corporation Compuestos para la inflamación y usos inmunorrelacionados.
ES2327684T3 (es) 2003-07-24 2009-11-02 Euro-Celtique S.A. Compuestos heteroaril-tetrahidropiridilo utiles para el tratamiento o la prevencion del dolor.
GB0319150D0 (en) 2003-08-14 2003-09-17 Glaxo Group Ltd Novel compounds
GB0319151D0 (en) * 2003-08-14 2003-09-17 Glaxo Group Ltd Novel compounds
ES2360152T3 (es) 2003-09-22 2011-06-01 Euro-Celtique S.A. Compuestos de fenil-carboxamida útiles para el tratamiento del dolor.
WO2005030753A2 (en) * 2003-09-22 2005-04-07 Euro-Celtique S.A. Therapeutic agents useful for treating pain
US7615557B2 (en) 2003-10-01 2009-11-10 Xention Limited Tetrahydro-naphthalene and urea derivatives
CA2541299A1 (en) * 2003-10-07 2005-04-14 Renovis, Inc. Amide compounds as ion channel ligands and uses thereof
GB2413129A (en) * 2003-10-07 2005-10-19 Renovis Inc Aromatic amide compounds as ion channel ligands and uses thereof
BRPI0415179A (pt) 2003-10-07 2006-11-28 Renovis Inc derivados de amida como ligandos de canal de ìon e composições farmacêuticas e métodos de empregar as mesmas
US7544803B2 (en) 2004-01-23 2009-06-09 Amgen Inc. Vanilloid receptor ligands and their use in treatments
WO2005072681A2 (en) * 2004-01-23 2005-08-11 Amgen Inc. Vanilloid receptor ligands and their use in treatments of inflammatory and neurotic pain.
EP1768959A2 (en) 2004-06-28 2007-04-04 Janssen Pharmaceutica N.V. Hetero isonipecotic modulators of vanilloid vr1 receptor
US20060035939A1 (en) * 2004-07-14 2006-02-16 Japan Tobacco Inc. 3-Aminobenzamide compounds and inhibitors of vanilloid receptor subtype 1 (VR1) activity
EP2314585B1 (en) * 2004-07-15 2012-09-12 Japan Tobacco, Inc. Condensed benzamide compounds as inhibitors of vanilloid receptor subtype 1 (VR1) activity
WO2006058338A2 (en) * 2004-11-29 2006-06-01 Janssen Pharmaceutica N.V. 4 - piperidinecarboxamide derivatives as modulators of vanilloid vr1 receptor
FR2880625B1 (fr) * 2005-01-07 2007-03-09 Sanofi Aventis Sa Derives de n-(heteroaryl)-1h-indole-2-carboxamides, leur preparation et leur application en therapeutique
KR20060087386A (ko) 2005-01-28 2006-08-02 주식회사 대웅제약 신규 벤조이미다졸 유도체 및 이를 함유하는 약제학적조성물
FR2888848B1 (fr) * 2005-07-22 2007-09-28 Sanofi Aventis Sa Derives de n-(arylalkyl)-1h-pyrrrolopyridine-2-carboxamides, leur preparation et leur application en therapeutique
EP1908753B1 (en) * 2005-07-22 2014-12-17 Mochida Pharmaceutical Co., Ltd. Novel heterocyclidene acetamide derivative
FR2888847B1 (fr) 2005-07-22 2007-08-31 Sanofi Aventis Sa Derives de n-(heteriaryl)-1-heteorarylalkyl-1h-indole-2- carboxamides, leur preparation et application en therapeutique
US7429605B2 (en) 2005-08-04 2008-09-30 Hoffmann-La Roche Inc. Phenylpyridine derivatives
WO2007022946A1 (de) 2005-08-21 2007-03-01 Abbott Gmbh & Co. Kg Heterocyclische verbindungen und ihre verwendung als bindungspartner für 5-ht5-rezeptoren
DE102005059479A1 (de) * 2005-12-13 2007-06-14 Merck Patent Gmbh Hydroxychinolinderivate
AR058705A1 (es) 2005-12-23 2008-02-20 Astrazeneca Ab Compuestos de bencimidazol como inhibidores del receptor vaniloide 1 (vr1)
US7906508B2 (en) * 2005-12-28 2011-03-15 Japan Tobacco Inc. 3,4-dihydrobenzoxazine compounds and inhibitors of vanilloid receptor subtype 1 (VRI) activity
JP4086895B2 (ja) 2005-12-28 2008-05-14 日本たばこ産業株式会社 3,4−ジヒドロベンゾオキサジン化合物及びバニロイド受容体1型(vr1)活性阻害剤
US8546579B2 (en) 2006-03-16 2013-10-01 Evotec (Us) Inc. Bicycloheteroaryl compounds as P2X7 modulators and uses thereof
KR20090008286A (ko) * 2006-03-27 2009-01-21 네르비아노 메디칼 사이언시스 에스.알.엘. 키나제 억제제로서의 피리딜- 및 피리미디닐-치환된 피롤-,티오펜- 및 푸란- 유도체
CA2656875C (en) * 2006-07-11 2011-09-06 Pfizer Inc. Substituted n-bicyclicalkyl bicyclic carboxyamide compounds
TWI433839B (zh) 2006-08-11 2014-04-11 Neomed Inst 新穎的苯并咪唑衍生物290
ATE478847T1 (de) 2006-09-15 2010-09-15 Pfizer Substituierte pyridylmethylbicyclocarboxyamidverbindungen
EP2222631B1 (en) 2006-10-23 2011-08-17 Pfizer Inc. Substituted phenylmethyl bicyclocarboxyamide compounds
WO2008057300A2 (en) * 2006-10-27 2008-05-15 Redpoint Bio Corporation Trpvi antagonists and uses thereof
EP2091944B1 (en) * 2006-11-17 2011-05-18 Pfizer Inc. Substituted bicyclocarboxyamide compounds
FR2910473B1 (fr) 2006-12-26 2009-02-13 Sanofi Aventis Sa Derives de n-(amino-heteroaryl)-1h-pyrrolopyridine-2- carboxamides, leur preparation et leur application en therapeutique.
US8455513B2 (en) * 2007-01-10 2013-06-04 Aerie Pharmaceuticals, Inc. 6-aminoisoquinoline compounds
FR2911604B1 (fr) * 2007-01-19 2009-04-17 Sanofi Aventis Sa Derives de n-(heteroaryl-1h-indole-2-carboxamides, leur preparation et leur application en therapeutique
FR2911605B1 (fr) 2007-01-19 2009-04-17 Sanofi Aventis Sa Derives de pyrrolopyridine-2-carbowamides, leur preparation et leur application en therapeutique
PE20081692A1 (es) * 2007-01-24 2008-12-18 Mochida Pharm Co Ltd Nuevo derivado de heterocicliden acetamida
US20080186971A1 (en) * 2007-02-02 2008-08-07 Tarari, Inc. Systems and methods for processing access control lists (acls) in network switches using regular expression matching logic
AR066146A1 (es) 2007-04-27 2009-07-29 Shionogi & Co Antagonistas de trpvi y usos de los mismos
JP5372913B2 (ja) 2007-04-27 2013-12-18 パーデュー、ファーマ、リミテッド、パートナーシップ 疼痛治療に有効な治療薬
WO2009079008A1 (en) * 2007-12-19 2009-06-25 Yangbo Feng Benzopyrans and analogs as rho kinase inhibitors
EP2234486A4 (en) * 2007-12-19 2011-09-14 Scripps Research Inst BENZIMIDAZOLE AND ANALOGUE AS RHO-KINASEHEMMER
JP2011507850A (ja) * 2007-12-21 2011-03-10 ザ スクリプス リサーチ インスティチュート Rhoキナーゼインヒビターとしてのアニリドおよびアナログ
FR2926554B1 (fr) 2008-01-22 2010-03-12 Sanofi Aventis Derives de carboxamides azabicycliques, leur preparation et leur application en therapeutique
FR2926553B1 (fr) * 2008-01-23 2010-02-19 Sanofi Aventis Derives d'indole-2-carboxamides et d'azaindole-2- carboxamides substitues par un groupe silanyle, leur preparation et leur application en therapeutique
CA2719515C (en) 2008-04-18 2013-11-05 Daewoong Pharmaceutical Co., Ltd. A novel benzoxazine benzimidazole derivative, a pharmaceutical composition comprising the same, and a use thereof
US8450344B2 (en) 2008-07-25 2013-05-28 Aerie Pharmaceuticals, Inc. Beta- and gamma-amino-isoquinoline amide compounds and substituted benzamide compounds
EP3354643B1 (en) 2009-05-01 2020-10-28 Aerie Pharmaceuticals, Inc. Dual mechanism inhibitors for the treatment of disease
US8686009B2 (en) * 2009-06-25 2014-04-01 Alkermes Pharma Ireland Limited Prodrugs of NH-acidic compounds
EP4124616A1 (en) 2009-06-25 2023-02-01 Alkermes Pharma Ireland Limited Heterocyclic compounds for the treatment of neurological and psychological disorders
EP2563759B1 (en) 2010-04-27 2022-04-06 Calcimedica, Inc. Compounds that modulate intracellular calcium
NZ604423A (en) 2010-06-24 2015-01-30 Alkermes Pharma Ireland Ltd Prodrugs of nh-acidic compounds: ester, carbonate, carbamate and phosphonate derivatives
KR101293384B1 (ko) 2010-10-13 2013-08-05 주식회사 대웅제약 신규 피리딜 벤조옥사진 유도체, 이를 포함하는 약학 조성물 및 이의 용도
WO2012129156A1 (en) 2011-03-18 2012-09-27 Alkermes, Inc. Pharmaceutical compositions comprising sorbitan esters
UA113288C2 (xx) 2011-06-22 2017-01-10 Trpv1 антагоністи, що містять дигідроксизамісник, і їх застосування
WO2013088255A1 (en) 2011-12-15 2013-06-20 Alkermes Pharma Ireland Limited Prodrugs of secondary amine compounds
FR2984318B1 (fr) 2011-12-16 2014-06-27 Oreal Coupleur de structure 7 amino-1,2,3,4-tetrahydroquinoleines cationiques, composition tinctoriale en comprenant, procedes et utilisations
FR2984323B1 (fr) * 2011-12-16 2019-08-30 L'oreal Coupleur de structure 7 amino-1,2,3,4-tetrahydroquinoleines, composition tinctoriale en comprenant, procedes et utilisations
ES2765036T3 (es) 2012-03-19 2020-06-05 Alkermes Pharma Ireland Ltd Composiciones farmacéuticas que comprenden esteres de ácidos grasos
AU2013235523B9 (en) 2012-03-19 2018-01-04 Alkermes Pharma Ireland Limited Pharmaceutical compositions comprising glycerol esters
JP6333802B2 (ja) 2012-03-19 2018-05-30 アルカームス ファーマ アイルランド リミテッド ベンジルアルコールを含む医薬組成物
CA2885196C (en) 2012-09-19 2021-06-22 Alkermes Pharma Ireland Limited Pharmaceutical compositions having improved storage stability
CA2894399A1 (en) 2012-12-06 2014-06-12 Quanticel Pharmaceuticals, Inc. Histone demethylase inhibitors
HUE061618T2 (hu) 2013-03-15 2023-07-28 Aerie Pharmaceuticals Inc Vegyület szemrendellenességek kezelésére
CN110368360A (zh) 2014-03-20 2019-10-25 奥克梅斯制药爱尔兰有限公司 具有增加的注射速度的阿立哌唑制剂
JP6633618B2 (ja) * 2014-08-21 2020-01-22 ブリストル−マイヤーズ スクイブ カンパニーBristol−Myers Squibb Company 強力なrock阻害剤としてのタイドバックのベンズアミド誘導体
JP2017214290A (ja) * 2014-09-12 2017-12-07 田辺三菱製薬株式会社 芳香族カルボン酸アミド化合物
MX2019002396A (es) 2016-08-31 2019-07-08 Aerie Pharmaceuticals Inc Composiciones oftalmicas.
WO2018085348A1 (en) * 2016-11-03 2018-05-11 Actavalon, Inc. Substituted quinolines and methods for treating cancer
US9840468B1 (en) 2016-12-30 2017-12-12 Aerie Pharmaceuticals, Inc. Methods for the preparation of 6-aminoisoquinoline
IT201700028127A1 (it) * 2017-03-14 2018-09-14 Fondazione St Italiano Tecnologia Composti e composizioni per il trattamento della fibrosi cistica
CA3057872A1 (en) 2017-03-31 2018-10-04 Aerie Pharmaceuticals, Inc. Aryl cyclopropyl-amino-isoquinolinyl amide compounds
FR3072286B1 (fr) 2017-10-13 2022-08-12 Oreal 7-amino-1,2,3,4-tetrahydroquinoleines particuliers, procede et composition
CN112423754A (zh) 2018-03-05 2021-02-26 奥克梅斯制药爱尔兰有限公司 阿立哌唑的给药策略
AU2019337703B2 (en) 2018-09-14 2023-02-02 Aerie Pharmaceuticals, Inc. Aryl cyclopropyl-amino-isoquinolinyl amide compounds
CN112574106B (zh) * 2020-11-11 2022-04-12 苏州康润医药有限公司 7-氨基-5-溴喹啉的合成方法
DE102022104759A1 (de) 2022-02-28 2023-08-31 SCi Kontor GmbH Co-Kristall-Screening Verfahren, insbesondere zur Herstellung von Co-Kristallen

Family Cites Families (56)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3200123A (en) * 1962-01-26 1965-08-10 Richardson Merreil Inc Imidazoquinolines
US3424760A (en) 1966-03-07 1969-01-28 Robins Co Inc A H 3-ureidopyrrolidines
US3424761A (en) 1966-03-07 1969-01-28 Robins Co Inc A H 3-ureidopyrrolidines
JPS4824396B1 (es) * 1970-09-09 1973-07-20
DE2502588A1 (de) 1975-01-23 1976-07-29 Troponwerke Dinklage & Co Basisch substituierte derivate des 7-amino-2-chinolons, verfahren zu ihrer herstellung sowie ihre verwendung als arzneimittel
US4456604A (en) 1981-05-26 1984-06-26 Merck & Co., Inc. 1-(3-Halo-2-pyridinyl) piperazine
EP0130795B1 (en) 1983-07-05 1988-11-23 Pfizer Inc. Carboxylic acid derivatives useful for inhibiting the degradation of cartilage
US4803162A (en) * 1984-05-15 1989-02-07 Fluorodiagnostic Limited Partners Composition, article and process for detecting a microorganism
DE3766472D1 (de) 1986-10-28 1991-01-10 Smith Kline French Lab Tetrahydroisochinolin-2-yl-derivate von carbonsaeuren als thromboxan a2-antagonisten.
DE3701277A1 (de) * 1987-01-17 1988-07-28 Boehringer Mannheim Gmbh Neue tricyclische benzimidazole, verfahren zu ihrer herstellung und verwendung als arzneimittel
DE68918991T2 (de) 1988-06-17 1995-04-27 Procter & Gamble Anwendung von Vanillin-Derivaten zur Herstellung eines Arzneimittels zur Behandlung von Herpes simplex-Infektion.
HU206082B (en) 1988-12-23 1992-08-28 Sandoz Ag Process for producing capsaicin derivatives and pharmaceutical compositions comprising such compounds
CA2017383A1 (en) 1989-06-08 1990-12-08 Raymond R. Martodam Use of vanilloids for the treatment of respiratory diseases or disorders
AU9079491A (en) 1990-11-27 1992-06-25 Procter & Gamble Company, The Combinations of vanilloid compounds and phosphonate antiviral compounds for treatment of herpes infections
US5342851A (en) 1992-10-07 1994-08-30 Mcneil-Ppc, Inc. Substituted thiazole derivatives useful as platelet aggregation inhibitors
DE4234295A1 (de) 1992-10-12 1994-04-14 Thomae Gmbh Dr K Carbonsäurederivate, diese Verbindungen enthaltende Arzneimittel und Verfahren zu ihrer Herstellung
WO1994014801A1 (en) 1992-12-29 1994-07-07 Smithkline Beecham Plc Heterocyclic urea derivatives as 5ht2c and 5ht2b antagonists
WO1997006158A1 (en) 1995-08-10 1997-02-20 Astra Aktiebolag Bicyclic amidine derivatives useful in therapy
PT1221440E (pt) 1994-06-15 2007-07-20 Otsuka Pharma Co Ltd Derivados benzo-heterocíclicos úteis como moduladores da vasopressina ou oxitocina
GB9416972D0 (en) 1994-08-23 1994-10-12 Smithkline Beecham Plc Carbon side chain/indole/indolene
WO1996040640A1 (en) * 1995-06-07 1996-12-19 Pfizer Inc. BIPHENYL-2-CARBOXYLIC ACID-TETRAHYDRO-ISOQUINOLIN-6-YL AMIDE DERIVATIVES, THEIR PREPARATION AND THEIR USE AS INHIBITORS OF MICROSOMAL TRIGLYCERIDE TRANSFER PROTEIN AND/OR APOLIPOPROTEIN B (Apo B) SECRETION
TW280869B (en) 1995-07-17 1996-07-11 Philips Electronics Nv IDDQ-testing of bias generator circuit
US6323227B1 (en) 1996-01-02 2001-11-27 Aventis Pharmaceuticals Products Inc. Substituted N-[(aminoiminomethyl or aminomethyl)phenyl]propyl amides
GB9605883D0 (en) 1996-03-20 1996-05-22 Smithkline Beecham Plc Novel compounds
EP0891355A1 (en) 1996-04-03 1999-01-20 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
PL329803A1 (en) 1996-05-11 1999-04-12 Smithkline Beecham Plc Derivatives of tetrahydroisoquinoline as modulators od dopamine d receptors
BR9709906A (pt) * 1996-06-17 1999-08-10 Smithkline Beecham Plc Derivados de benzamida substituídos e o uso dos mesmos como anticonvulsivantes
US5854245A (en) 1996-06-28 1998-12-29 Merck & Co., Inc. Fibrinogen receptor antagonists
BR9809047A (pt) * 1997-03-18 2000-08-01 Smithkline Beecham Plc Derivados de isoquinolina substituìda e o uso dos mesmos como anticonvulsivantes
AUPO622597A0 (en) * 1997-04-15 1997-05-08 Fujisawa Pharmaceutical Co., Ltd. New heterocyclic compounds
NZ500252A (en) 1997-04-18 2001-07-27 Smithkline Beecham P 6-(4-Methyl-piperazin-1-yl)-1H-indole derivatives useful as 5HT1A, 5HT1B and 5HT1D receptor antagonists
AU7526798A (en) 1997-04-18 1998-11-27 Smithkline Beecham Plc Acetamide and urea derivatives, process for their preparation and their use in the treatment of cns disorders
JP2001508402A (ja) * 1997-06-13 2001-06-26 スミスクライン・ビーチャム・パブリック・リミテッド・カンパニー 置換ベンズアミド誘導体およびそれらの抗痙攣薬としての使用
EP1025087A1 (en) * 1997-10-24 2000-08-09 Smithkline Beecham Plc Substituted isoquinoline derivatives and their use as anticonvulsants
JP3013989B2 (ja) * 1998-03-26 2000-02-28 日本たばこ産業株式会社 アミド誘導体及びノシセプチンアンタゴニスト
US6399656B1 (en) 1998-07-28 2002-06-04 Smithkline Beecham Corporation Compounds and methods
GB9817424D0 (en) 1998-08-11 1998-10-07 Smithkline Beecham Plc Novel compounds
BR9914370A (pt) 1998-10-08 2001-11-27 Smithkline Beecham Plc Derivados de tetraidrobenzazepina úteis comomoduladores de receptores para a dopamina d3(agentes antipsicóticos)
EP1177188B1 (en) * 1999-05-12 2005-10-12 Ortho-McNeil Pharmaceutical, Inc. Pyrazole carboxamides useful for the treatment of obesity and other disorders
AU778063C (en) * 1999-06-02 2005-12-15 Astrazeneca Ab Metabotropic glutamate receptor antagonists and their use for treating central nervous system diseases
US7115750B1 (en) 1999-09-20 2006-10-03 Takeda Pharmaceutical Company Limited Melanin concentrating hormone antagonist
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
US6531478B2 (en) * 2000-02-24 2003-03-11 Cheryl P. Kordik Amino pyrazole derivatives useful for the treatment of obesity and other disorders
JP2002241274A (ja) * 2000-04-28 2002-08-28 Takeda Chem Ind Ltd メラニン凝集ホルモン拮抗剤
CN1324845A (zh) 2000-05-24 2001-12-05 上海博德基因开发有限公司 一种新的多肽——人蛋白合成起始因子2β亚单位16.5和编码这种多肽的多核苷酸
BR0112631A (pt) * 2000-07-20 2003-09-23 Neurogen Corp Composto ou um sal farmaceuticamente aceitável do mesmo, composição farmacêutica, pacote, métodos de reduzir a condutáncia de cálcio de um receptor de capsaicina e de tratar um mamìfero e uso de um composto
ES2266227T3 (es) 2000-08-21 2007-03-01 Pacific Corporation Nuevos compuestos de (tio)urea y composiciones farmaceuticas que los contienen.
US6500840B2 (en) 2000-08-21 2002-12-31 Pharmacia & Upjohn Company Quinuclidine-substituted heteroaryl moieties for treatment of disease
WO2002016317A1 (en) 2000-08-21 2002-02-28 Pacific Corporation Novel thiocarbamic acid derivatives and the pharmaceutical compositions containing the same
AU2001280229B2 (en) 2000-08-21 2006-12-07 Pacific Corporation Novel thiourea derivatives and the pharmaceutical compositions containing the same
UY26942A1 (es) 2000-09-20 2002-04-26 Abbott Lab N-acilsulfonamidas promotoras de la apoptosis
SK286759B6 (sk) * 2001-07-02 2009-05-07 N.V. Organon Tetrahydrochinolínové deriváty, farmaceutický prostriedok s ich obsahom a ich použitie
JP4408618B2 (ja) * 2001-10-25 2010-02-03 武田薬品工業株式会社 キノリン化合物
EP1450801A4 (en) * 2001-11-27 2010-10-27 Merck Sharp & Dohme 2-AMINOQUINOLINE COMPOUNDS
JP2005518365A (ja) * 2001-11-27 2005-06-23 メルク エンド カムパニー インコーポレーテッド 4−アミノキノリン化合物
DE60325834D1 (de) * 2002-02-20 2009-03-05 Abbott Lab Kondensierte azabicyclischeverbindungen als inhibitoren des vanilloid-rezeptors 1 (vr1)

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TW200403223A (en) 2004-03-01
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US7538121B2 (en) 2009-05-26
ATE416168T1 (de) 2008-12-15
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