AR080373A1 - Antagonistas de ccr3 de arilsulfamida isotopicamente enriquecida - Google Patents

Antagonistas de ccr3 de arilsulfamida isotopicamente enriquecida

Info

Publication number
AR080373A1
AR080373A1 ARP110100657A ARP110100657A AR080373A1 AR 080373 A1 AR080373 A1 AR 080373A1 AR P110100657 A ARP110100657 A AR P110100657A AR P110100657 A ARP110100657 A AR P110100657A AR 080373 A1 AR080373 A1 AR 080373A1
Authority
AR
Argentina
Prior art keywords
heterocyclyl
nr1br1c
nrbrc
heteroaryl
nrfrg
Prior art date
Application number
ARP110100657A
Other languages
English (en)
Original Assignee
Axikin 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
Application filed by Axikin Pharmaceuticals Inc filed Critical Axikin Pharmaceuticals Inc
Publication of AR080373A1 publication Critical patent/AR080373A1/es

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/22—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with hetero atoms directly attached to ring nitrogen atoms
    • C07D295/26—Sulfur atoms
    • 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
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • 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
    • A61P17/06—Antipsoriatics
    • 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
    • A61P17/10—Anti-acne agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • 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
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B59/00—Introduction of isotopes of elements into organic compounds ; Labelled organic compounds per se
    • C07B59/002—Heterocyclic compounds

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Pulmonology (AREA)
  • Rheumatology (AREA)
  • Dermatology (AREA)
  • Immunology (AREA)
  • Cardiology (AREA)
  • Pain & Pain Management (AREA)
  • Oncology (AREA)
  • Hematology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

Arilsulfonamidas isotopicamente enriquecidas, por ejemplo, de la formula 1, que son de utilidad para modular la actividad de CCR3 y sus composiciones farmacéuticas. También, métodos de uso para tratar, prevenir o mejorar uno o varios síntomas de un trastorno, enfermedad o condicion patologica mediados por CCR3. 1. Reivindicacion 1: Un compuesto caracterizado por la formula (1) o un enantiomero, una mezcla de enantiomeros, una mezcla de dos o más diastereomeros, un tautomero o una mezcla de dos o más tautomeros de ellos; o una de sus sales, solvatos, hidratos o profármacos farmacéuticamente aceptables; en donde: R1, R2, R3, R4, R5 y R8 son cada uno, de modo independiente (a) hidrogeno, deuterio, halo, ciano, nitro o guanidina; (b) alquilo C1-6, alquenilo C2-6, alquinilo C2-6, cicloalquilo C3-7, arilo C6-14, aralquilo C7-15, heteroarilo o heterociclilo; o (c) -C(O)R1a, -C(O)OR1a, -C(O)NR1bR1c, -C(NR1a)NR1bR1c, -OR1a, -OC(O)R1a, -OC(O)OR1a, -OC(O)NR1bR1c, -OC(=NR1a)NR1bR1c, -OS(O)R1a, -OS(O)2R1a, -OS(O)NR1bR1c, -OS(O)2NR1bR1c, -NR1bR1c, -NR1aC(O)R1d, -NR1aC(O)OR1d, -NR1aC(O)NR1bR1c, - NR1aC(=NR1d)NR1bR1c, -NR1aS(O)R1d, -NR1aS(O)2R1d, -NR1aS(O)NR1bR1c, -NR1aS(O)2NR1bR1c, -SR1a, -S(O)R1a, -S(O)2R1a, -S(O)NR1bR1c o -S(O)2NR1bR1c; R6, R7 y R9 son cada uno, de modo independiente (a) hidrogeno o deuterio; R10 y R11 son cada uno, de modo independiente (a) hidrogeno; o (b) alquilo C1-6, alquenilo C2-6, alquinilo C2-6, cicloalquilo C3-7, arilo C6-14, aralquilo C7-15, heteroarilo o heterociclilo; o R10 y R11 se unen para formar heterociclilo; R12 es (a) hidrogeno; (b) alquilo C1-6, alquenilo C2-6, alquinilo C2-6, cicloalquilo C3-7, arilo C6-14, aralquilo C7-15, heteroarilo o heterociclilo; o (c) -C(O)R1a, -C(O)OR1a, -C(O)NR1bR1c, -C(NR1a)NR1bR1c, -S(O)R1a, -S(O)2R1a, -S(O)NR1bR1c o -S(O)2NR1bR1c; L es alquileno C1-6; X es O o S; y cada R1a, R1b, R1c y R1d es, de modo independiente, hidrogeno, deuterio, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, cicloalquilo C3-7, arilo C6-14, heteroarilo o heterociclilo; o cada par de R1b y R1c junto con el átomo de N al que están unidos forman, de modo independiente, heteroarilo o heterociclilo; en donde el compuesto está isotopicamente enriquecido; en donde cada alquilo, alquileno, alquenilo, alquinilo, cicloalquilo, arilo, aralquilo, heterociclilo y heteroarilo en R1, R2, R3, R4, R5, R8, R10, R11, R12, R1a, R1b, R1c, R1d o L está opcionalmente sustituido con uno o varios sustituyentes Q, en donde cada Q está seleccionado, de modo independiente, de (a) deuterio, ciano, halo y nitro; (b) alquilo C1-6, alquenilo C2-6, alquinilo C2-6, cicloalquilo C3-7, arilo C6-14, aralquilo C7-15, heteroarilo y heterociclilo, cada uno de los cuales está también opcionalmente sustituido con uno o varios, en una forma de realizacion, uno, dos, tres o cuatro sustituyentes Qa y (c) -C(O)Ra, -C(O)ORa, -C(O)NRbRc, -C(NRa)NRbRc, -ORa, -OC(O)Ra, -OC(O)ORa, -OC(O)NRbRc, -OC(=NRa)NRbRc, -OS(O)Ra, -OS(O)2Ra, -OS(O)NRbRc, -OS(O)2NRbRc, -NRbRc, -NRaC(O)Rd, -NRaC(O)ORd, -NRaC(O)NRbRc, -NRaC(=NRd)NRbRc, -NRaS(O)Rd, -NRaS(O)2Rd, -NRaS(O)NRbRc, -NRaS(O)2NRbRc, -SRa, -S(O)Ra, -S(O)2Ra, -S(O)NRbRc y -S(O)2NRbRc, en donde cada Ra, Rb, Rc y Rd es, de modo independiente, (i) hidrogeno o deuterio; (ii) alquilo C1-6, alquenilo C2-6, alquinilo C2-6, cicloalquilo C3-7, arilo C6-14, aralquilo C7-15, heteroarilo o heterociclilo, cada uno opcionalmente sustituido con uno o varios, en una forma de realizacion, uno, dos, tres o cuatro, sustituyentes Qa; o (iii) cada par de Rb y Rc junto con el átomo de N al que están unidos forman heterociclilo, opcionalmente sustituido con uno o varios, en una forma de realizacion, uno, dos, tres o cuatro, sustituyentes Qa; en donde cada Qa está seleccionado, de modo independiente, del grupo que consiste en (a) deuterio, ciano, halo y nitro; (b) alquilo C1-6, alquenilo C2-6, alquinilo C2- 6, cicloalquilo C3-7, arilo C6-14, aralquilo C7-15, heteroarilo y heterociclilo; y (c) -C(O)Re, -C(O)ORe, -C(O)NRfRg, -ORe, -OC(O)Re, -OC(O)ORe, -OC(O)NRfRg, -OC(=NRe)NRfRg, -OS(O)Re, -OS(O)2Re, -OS(O)NRfRg, -OS(O)2NRfRg, -NRfRg, -NReC(O)Rh, -NReC(O)ORf, -NReC(O)NRfRg, -NReC(=NRh)NRfRg, -NReS(O)Rh, -NReS(O)2Rh, -NRes(O)NRfRg, -NReS(O)2NRfRg, -SRe, -S(O)Re, -S(O)2Re, -S(O)NRfRg y -S(O)2NRfRg, en donde cada Re, Rf, Rg y Rh es, de modo independiente, (i) hidrogeno o deuterio; (ii) alquilo C1-6, alquenilo C2-6, alquinilo C2-6, cicloalquilo C3-7, arilo C6-14, aralquilo C7-15, heteroarilo o heterociclilo; o (iii) cada par de Rf y Rg junto con el átomo de N al que están unidos forman heterociclilo.
ARP110100657A 2010-03-02 2011-03-02 Antagonistas de ccr3 de arilsulfamida isotopicamente enriquecida AR080373A1 (es)

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US30981510P 2010-03-02 2010-03-02

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US (1) US8999995B2 (es)
EP (1) EP2542542B1 (es)
AR (1) AR080373A1 (es)
AU (1) AU2011223873B2 (es)
CA (1) CA2791964A1 (es)
DK (1) DK2542542T3 (es)
ES (1) ES2542404T3 (es)
HK (1) HK1180334A1 (es)
HU (1) HUE025699T2 (es)
TW (1) TWI485139B (es)
WO (1) WO2011109345A1 (es)

Families Citing this family (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN103298786B (zh) * 2010-10-11 2016-01-20 埃克希金医药品有限公司 芳基磺酰胺盐ccr3拮抗剂
CN104781240A (zh) * 2012-09-07 2015-07-15 埃克希金医药品有限公司 同位素富集的芳基磺酰胺ccr3拮抗剂

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EP2542542B1 (en) 2015-04-22
US8999995B2 (en) 2015-04-07
US20110218207A1 (en) 2011-09-08
EP2542542A1 (en) 2013-01-09
HUE025699T2 (en) 2016-04-28
AU2011223873A1 (en) 2012-09-20
AU2011223873B2 (en) 2015-06-25
ES2542404T3 (es) 2015-08-05
CA2791964A1 (en) 2011-09-09
TW201136899A (en) 2011-11-01
WO2011109345A1 (en) 2011-09-09
TWI485139B (zh) 2015-05-21
DK2542542T3 (en) 2015-07-20
HK1180334A1 (en) 2013-10-18

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