AR061905A1 - 3-AZABICICLO VANILOID RECEIVERS LEGANDS [3.1.0] HEXANE, PHARMACEUTICAL COMPOSITIONS CONTAINING THEM, AND PROCESSES FOR THEIR PREPARATION - Google Patents

3-AZABICICLO VANILOID RECEIVERS LEGANDS [3.1.0] HEXANE, PHARMACEUTICAL COMPOSITIONS CONTAINING THEM, AND PROCESSES FOR THEIR PREPARATION

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Publication number
AR061905A1
AR061905A1 ARP070103179A ARP070103179A AR061905A1 AR 061905 A1 AR061905 A1 AR 061905A1 AR P070103179 A ARP070103179 A AR P070103179A AR P070103179 A ARP070103179 A AR P070103179A AR 061905 A1 AR061905 A1 AR 061905A1
Authority
AR
Argentina
Prior art keywords
substituted
unsubstituted
alkyl
cycloalkenyl
occurrence
Prior art date
Application number
ARP070103179A
Other languages
Spanish (es)
Inventor
Atmaram Gharat Laxmikant
Neelima Khairatkar Joshi
Maganbhai Gajera Jitendra
Sabhajit Yadav Pravin
Original Assignee
Glenmark Pharmaceuticals Sa
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
Application filed by Glenmark Pharmaceuticals Sa filed Critical Glenmark Pharmaceuticals Sa
Publication of AR061905A1 publication Critical patent/AR061905A1/en

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic 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
    • C07D401/14—Heterocyclic 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 three or more hetero rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/04—Antipruritics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/12—Keratolytics, e.g. wart or anti-corn preparations
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/14—Drugs for dermatological disorders for baldness or alopecia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/06—Antimigraine agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/22—Anxiolytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/04—Anorexiants; Antiobesity agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links

Abstract

utiles como ligandos de receptores vaniloides, métodos para el tratamiento de enfermedades, condiciones y/o trastornos modulados por receptores vaniloides como dolor, migrana, neuropatías, trastornos gastrointestinales, Crohn, celiaquía, rinitis, alergia, asma, prurito, depresion, artritis, alopecia, ansiedad. Reivindicacion 1: Un Compuesto de la formula general (1) o una prodroga del mismo, una sal farmacéuticamente aceptable del mismo, un N-oxido del mismo, un éster del mismo, un solvato del mismo, un tautomero del mismo, un estereoisomero del mismo o un polimorfo del mismo, en donde: X es O o S; R1 se selecciona de las estructuras del grupo de formulas (2), en donde R1 está unida a la estructura principal a través de cualquier átomo de carbono en el anillo y se substituye opcionalmente con uno o más grupos R; cada ocurrencia de R y R6 se selecciona independientemente de hidrogeno, nitro, ciano, formilo, acetilo, halogeno, -OR7, -SR7, oxo, tio, alquilo substituido o no substituido, alquenilo substituido o no substituido, alquinilo substituido o no substituido, cicloalquilo substituido o no substituido, cicloalquilalquilo substituido o no substituido, cicloalquenilo substituido o no substituido, cicloalquenilalquilo substituido o no substituido, arilo substituido o no substituido, arilalquilo substituido o no substituido, heteroarilo substituido o no substituido, heteroarilalquilo substituido o no substituido, grupo heterocíclico substituido o no substituido, heterociclilalquilo substituido o no substituido, -C(O)R7, -C(O)O-R7, -C(O)NR7R8 , -NR7R8, -S(O)m-R7, S(O)m-NR7R8, y un grupo de proteccion; cada ocurrencia de R7 y R8 se selecciona independientemente de hidrogeno, nitro, halo, ciano, -ORa, -SRa, oxo, tio, alquilo substituido o no substituido, alquenilo substituido o no substituido, alquinilo substituido o no substituido, cicloalquilo substituido o no substituido, cicloalquilalquilo substituido o no substituido, cicloalquenilo substituido o no substituido, cicloalquenilalquilo substituido o no substituido, arilo substituido o no substituido, arilalquilo substituido o no substituido, heteroarilo substituido o no substituido, heteroarilalquilo substituido o no substituido, un grupo heterocíclico substituido o no substituido, heterociclilalquilo substituido o no substituido, -C(O)Ra, -C(O)O-Ra, -C(O)NRaRb, -S(O)m-Ra, -S(O)m-NRaRb, -NRaRb, y un grupo de proteccion, o R7 y R8, cuando ambos están directamente unidos al mismo átomo de nitrogeno, se juntan con el átomo de nitrogeno al cual están unidos para formar un anillo cíclico no saturado o saturado de 3 a 7 miembros opcionalmente substituido, el cual incluye opcionalmente uno o más heteroátomos seleccionados de O, NRa y S; cada ocurrencia de Ra y Rb se selecciona independientemente de hidrogeno, halogeno, nitro, ciano, formilo, acetilo, oxo, tio, -C(O)-Rc, -C(O)ORc, -C(O)NRcRd, -S(O)m-Rc, S(O)m-NRcRd, -NRcRd, -ORc, -SRd, un grupo de proteccion, alquilo substituido o no substituido, alquenilo substituido o no substituido, alquinilo substituido o no substituido, cicloalquilo substituido o no substituido, cicloalquilalquilo substituido o no substituido, cicloalquenilo substituido o no substituido, cicloalquenilalquilo substituido o no substituido, arilo substituido o no substituido, arilalquilo substituido o no substituido, heteroarilo substituido o no substituido, un grupo heterocíclico substituido o no substituido, heterocicliloalquilo substituido o no substituido, y un heteroarilalquilo substituido o no substituido; cada ocurrencia de Rc y Rd se selecciona independientemente de hidrogeno, alquilo substituido o no substituido, alquenilo substituido o no substituido, alquinilo substituido o no substituido, cicloalquilo substituido o no substituido, cicloalquilalquilo substituido o no substituido, cicloalquenilo substituido o no substituido, cicloalquenilalquilo substituido o no substituido, arilo substituido o no substituido, ariloalquilo substituido o no substituido, heteroarilo substituido o no substituido, un grupo heterocíclico substituido o no substituido, heterociclilalquilo substituido o no substituido, o un heteroarilalquilo substituido o no substituido y un grupo de proteccion, o Rc y Rd, cuando ambos se encuentran directamente unidos al mismo átomo de nitrogeno, se unen con el átomo de nitrogeno al cual están unidos para formar un anillo cíclico saturado o no saturado de 3 a 7 miembros substituido opcionalmente, el cual incluye uno o más heteroátomos seleccionados de O, NRe o S; cada ocurrencia de Re se selecciona independientemente de hidrogeno o de alquilo substituido o no substituido, cada ocurrencia de m es 0, 1 o 2; R2 y R3 se seleccionan independientemente de hidrogeno, hidroxi y alquilo C1-6; y cada ocurrencia de R4 y R5 se selecciona independientemente de hidrogeno, halogeno, y alquilo, o cuando R4 y R5 están unidos al mismo átomo de carbono R4 y R5 forman conjuntamente un grupo oxo o un grupo tio.Useful as vanilloid receptor ligands, methods for the treatment of diseases, conditions and / or disorders modulated by vanilloid receptors such as pain, migraine, neuropathies, gastrointestinal disorders, Crohn, celiac disease, rhinitis, allergy, asthma, pruritus, depression, arthritis, alopecia anxiety Claim 1: A Compound of the general formula (1) or a prodrug thereof, a pharmaceutically acceptable salt thereof, an N-oxide thereof, an ester thereof, a solvate thereof, a tautomer thereof, a stereoisomer of the same or a polymorph thereof, where: X is O or S; R1 is selected from the structures of the group of formulas (2), wherein R1 is attached to the main structure through any carbon atom in the ring and is optionally substituted with one or more R groups; Each occurrence of R and R6 is independently selected from hydrogen, nitro, cyano, formyl, acetyl, halogen, -OR7, -SR7, oxo, thio, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted cycloalkylalkyl, substituted or unsubstituted cycloalkenyl, substituted or unsubstituted cycloalkenyl, substituted or unsubstituted aryl, substituted or unsubstituted arylalkyl, substituted or unsubstituted heteroaryl, substituted or unsubstituted heteroaryl, heterocyclic group substituted or unsubstituted, heterocyclyl substituted or unsubstituted alkyl, -C (O) R7, -C (O) O-R7, -C (O) NR7R8, -NR7R8, -S (O) m-R7, S (O) m-NR7R8, and a protection group; each occurrence of R7 and R8 is independently selected from hydrogen, nitro, halo, cyano, -ORa, -SRa, oxo, thio, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted cycloalkyl substituted, substituted or unsubstituted cycloalkylalkyl, substituted or unsubstituted cycloalkenyl, substituted or unsubstituted cycloalkenyl, substituted or unsubstituted aryl, substituted or unsubstituted arylalkyl, substituted or unsubstituted heteroaryl, a substituted or unsubstituted heteroaryl alkyl substituted, substituted or unsubstituted heterocyclylalkyl, -C (O) Ra, -C (O) O-Ra, -C (O) NRaRb, -S (O) m-Ra, -S (O) m-NRaRb, - NRaRb, and a protection group, or R7 and R8, when both are directly attached to the same nitrogen atom, join the nitrogen atom to which they are attached to form an unsaturated or saturated cyclic ring of 3 to 7 opc members ionically substituted, which optionally includes one or more heteroatoms selected from O, NRa and S; Each occurrence of Ra and Rb is independently selected from hydrogen, halogen, nitro, cyano, formyl, acetyl, oxo, thio, -C (O) -Rc, -C (O) ORc, -C (O) NRcRd, -S (O) m-Rc, S (O) m-NRcRd, -NRcRd, -ORc, -SRd, a protection group, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted cycloalkyl or unsubstituted, substituted or unsubstituted cycloalkylalkyl, substituted or unsubstituted cycloalkenyl, substituted or unsubstituted cycloalkenyl, substituted or unsubstituted aryl, substituted or unsubstituted arylalkyl, substituted or unsubstituted heteroaryl, a substituted or unsubstituted heterocyclic group, heterocyclyl or substituted alkyl unsubstituted, and a substituted or unsubstituted heteroarylalkyl; each occurrence of Rc and Rd is independently selected from hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted cycloalkylalkyl, substituted or unsubstituted cycloalkenyl, substituted cycloalkenyl alkyl or unsubstituted, substituted or unsubstituted aryl, substituted or unsubstituted arylalkyl, substituted or unsubstituted heteroaryl, a substituted or unsubstituted heterocyclic group, substituted or unsubstituted heterocyclyl alkyl, or a substituted or unsubstituted heteroarylalkyl and a protecting group, or Rc and Rd, when both are directly attached to the same nitrogen atom, bind with the nitrogen atom to which they are attached to form a 3 to 7-membered saturated or unsaturated cyclic ring optionally substituted, which includes one or more heteroatoms selected from O, NRe or S; each occurrence of Re is independently selected from hydrogen or substituted or unsubstituted alkyl, each occurrence of m is 0, 1 or 2; R2 and R3 are independently selected from hydrogen, hydroxy and C1-6 alkyl; and each occurrence of R4 and R5 is independently selected from hydrogen, halogen, and alkyl, or when R4 and R5 are attached to the same carbon atom R4 and R5 together form an oxo group or a thio group.

ARP070103179A 2006-07-17 2007-07-17 3-AZABICICLO VANILOID RECEIVERS LEGANDS [3.1.0] HEXANE, PHARMACEUTICAL COMPOSITIONS CONTAINING THEM, AND PROCESSES FOR THEIR PREPARATION AR061905A1 (en)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
IN1136MU2006 2006-07-17
US83556006P 2006-08-03 2006-08-03
IN381MU2007 2007-02-27
US89367507P 2007-03-08 2007-03-08
US94771507P 2007-07-03 2007-07-03

Publications (1)

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AR061905A1 true AR061905A1 (en) 2008-10-01

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AR (1) AR061905A1 (en)
WO (1) WO2008010061A2 (en)

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AR067536A1 (en) 2007-07-17 2009-10-14 Hoffmann La Roche METHOD FOR OBTAINING A MONO-PEGILATED ERYTHROPOYETIN IN A SUBSTANTIALLY HOMOGENOUS FORM
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JP2013534229A (en) * 2010-08-20 2013-09-02 グリュネンタール・ゲゼルシャフト・ミト・ベシュレンクテル・ハフツング Substituted cyclic carboxamide derivatives and urea derivatives as vanilloid receptor ligands
KR20170012360A (en) * 2014-06-12 2017-02-02 알로사이트 파마수티컬스 아게 Small molecule lfa-1 inhibitors
KR20220034739A (en) 2019-05-31 2022-03-18 이케나 온콜로지, 인코포레이티드 TEAD inhibitors and uses thereof
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WO2008010061A3 (en) 2008-04-17
WO2008010061A2 (en) 2008-01-24

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