CO5190712A1 - ANTAGONISTS OF IL-8 RECEIVERS OF IL-8 RECEIVERS - Google Patents

ANTAGONISTS OF IL-8 RECEIVERS OF IL-8 RECEIVERS

Info

Publication number
CO5190712A1
CO5190712A1 CO00044229A CO00044229A CO5190712A1 CO 5190712 A1 CO5190712 A1 CO 5190712A1 CO 00044229 A CO00044229 A CO 00044229A CO 00044229 A CO00044229 A CO 00044229A CO 5190712 A1 CO5190712 A1 CO 5190712A1
Authority
CO
Colombia
Prior art keywords
cr8r8
alkyl
alkenyl
optionally substituted
heteroaryl
Prior art date
Application number
CO00044229A
Other languages
Spanish (es)
Inventor
Deborah L Bryan
John G Gleason
Gregory M Benson
Original Assignee
Smithkline Beecham Corp
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 Smithkline Beecham Corp filed Critical Smithkline Beecham Corp
Publication of CO5190712A1 publication Critical patent/CO5190712A1/en

Links

Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/13—Amines
    • A61K31/155—Amidines (), e.g. guanidine (H2N—C(=NH)—NH2), isourea (N=C(OH)—NH2), isothiourea (—N=C(SH)—NH2)
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • 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
    • A61P1/02—Stomatological preparations, e.g. drugs for caries, aphtae, periodontitis
    • 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
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/20—Antivirals for DNA viruses
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/20—Antivirals for DNA viruses
    • A61P31/22—Antivirals for DNA viruses for herpes viruses
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00—Antiparasitic agents
    • A61P33/02—Antiprotozoals, e.g. for leishmaniasis, trichomoniasis, toxoplasmosis
    • A61P33/06—Antimalarials
    • 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
    • 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
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
    • Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
    • Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change

Abstract

1. - Compuesto administrable en mamíferos para tratar una enfermedad mediada por quimioquina, seleccionada del grupo constituido por malaria, restinosis, angiogénesis, aterosclerosis, osteoporosis, gingivitis, liberación hematopoyética indeseada de células madre, y enfermedades causadas por virus respiratorios, herpesvirus, y virus de la hepatitis, donde la quimioquina se une a un receptor a o ß de la IL-8, dicho compuesto de fórmula <EMI FILE="00044229_1" ID="1" IMF=JPEG >donde:Z es ciano, OR11, C(O)NR15R16, R18, C(O)R11, C(O)OR11, o S(O)2R17;R es cualquier resto funcional que tiene un hidrógeno ionizable y un pKa de 10 o menos;R1 se selecciona, independientemente, entre hidrógeno; halógeno; nitro; ciano; alquilo C1-10 halosustituido; alquilo C1-10; alquenilo C2-10; alcoxi C1-10; alcoxi C1-10 halosustituido; azida; (CR8R8)qS(O)tR4; hidroxi; hidroxi-alquilo C1-4; arilo; aril-alquilo C1-4; ariloxi; aril-alquiloxi C1-4; heteroarilo; heteroarilalquilo; radical heterocíclico; heterociclil-alquilo C1-4; heteroaril-alquiloxi C1-4; aril-alquenilo C2-10; heteroaril-alquenilo C2-10; heterociclil-alquenilo C2-10; (CR8R8)qNR4R5; alquenil C2-10-C(O)NR4R5; (CR8R8)qC(O)NR4R5;(CR8R8)qC(O)NR4R10; S(O)3H; S(O)3R8; (CR8R8)qC(O)R11; alquenil C2-10-C(O)R11; alquenil C2-10-C(O)OR11; (CR8R8)qC(O)OR12; (CR8R8)qOC(O)R11; (CR8R8)qNR4C(O)R11; (CR8R8)qNHS(O)2R19; (CR8R8)qS(O)2NR4R5; o dos restos R1 juntos pueden formar O-(CH2)sO- o un anillo saturado o insaturado de 5 a 6 miembros, y donde los restos que contienen arilo, heteroarilo y radical heterocíclico pueden estar opcionalmente sustituidos;m es un número entero que tiene un valor de 1 a 3;q es 0, o un número entero que tiene un valor de 1 a 10; s es un número entero que tiene un valor de 1 a 3;t es 0, o un número entero que tiene un valor de 1 ó 2;v es 0, o un número entero que tiene un valor de 1 a 4;R4 y R5 son, independientemente, hidrógeno, alquilo C1-4 opcionalmente sustituido, arilo opcionalmente sustituido, (aril opcionalmente sustituido)-alquilo C1-4, heteroarilo opcionalmente sustituido, (heteroaril opcionalmente sustituido)-alquilo C1-4, radical heterocíclico, heterociclil-alquilo C1-4, o R4 y R5 junto con el nitrógeno al que están unidos, forman un anillo de 5 a 7 miembros que puede contener opcionalmente un heteroátomo adicional seleccionado entre oxígeno, nitrógeno o azufre;HET es un resto heteroarilo opcionalmente sustituido; ...1. - Compound manageable in mammals to treat a chemokine-mediated disease, selected from the group consisting of malaria, restinosis, angiogenesis, atherosclerosis, osteoporosis, gingivitis, unwanted hematopoietic stem cell release, and diseases caused by respiratory viruses, herpesviruses, and viruses of hepatitis, where chemokine binds to an α-β receptor of IL-8, said compound of formula <EMI FILE = "00044229_1" ID = "1" MFI = JPEG> where: Z is cyano, OR11, C ( O) NR15R16, R18, C (O) R11, C (O) OR11, or S (O) 2R17; R is any functional moiety that has an ionizable hydrogen and a pKa of 10 or less; R1 is independently selected from hydrogen; halogen; nitro; cyano; C1-10 alkyl halosubstituted; C1-10 alkyl; C2-10 alkenyl; C1-10 alkoxy; C1-10 alkoxy halosubstituted; azide; (CR8R8) qS (O) tR4; hydroxy; hydroxyC 1-4 alkyl; aryl; arylC 1-4 alkyl; aryloxy; C 1-4 aryl-alkyloxy; heteroaryl; heteroarylalkyl; heterocyclic radical; heterocyclylC 1-4 alkyl; heteroaryl-C1-4 alkyloxy; C2-10 aryl-alkenyl; C2-10 heteroaryl-alkenyl; C2-10 heterocyclyl-alkenyl; (CR8R8) qNR4R5; C2-10-C alkenyl (O) NR4R5; (CR8R8) qC (O) NR4R5; (CR8R8) qC (O) NR4R10; S (O) 3H; S (O) 3R8; (CR8R8) qC (O) R11; C2-10-C (O) R11 alkenyl; C2-10-C (O) alkenyl OR11; (CR8R8) qC (O) OR12; (CR8R8) qOC (O) R11; (CR8R8) qNR4C (O) R11; (CR8R8) qNHS (O) 2R19; (CR8R8) qS (O) 2NR4R5; or two R1 moieties together can form O- (CH2) sO- or a saturated or unsaturated ring of 5 to 6 members, and where the moieties containing aryl, heteroaryl and heterocyclic radical can be optionally substituted; m is an integer having a value from 1 to 3; q is 0, or an integer that has a value from 1 to 10; s is an integer that has a value of 1 to 3; t is 0, or an integer that has a value of 1 or 2; v is 0, or an integer that has a value of 1 to 4; R4 and R5 are, independently, hydrogen, optionally substituted C1-4 alkyl, optionally substituted aryl, (optionally substituted aryl) -C1-4 alkyl, optionally substituted heteroaryl, (optionally substituted heteroaryl) -C 1-4 alkyl, heterocyclyl radical, heterocyclyl-alkyl C1-4, or R4 and R5 together with the nitrogen to which they are attached, form a 5- to 7-membered ring that may optionally contain an additional heteroatom selected from oxygen, nitrogen or sulfur; HET is an optionally substituted heteroaryl moiety; ...

CO00044229A 1999-06-16 2000-06-14 ANTAGONISTS OF IL-8 RECEIVERS OF IL-8 RECEIVERS CO5190712A1 (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US13967799P 1999-06-16 1999-06-16

Publications (1)

Publication Number Publication Date
CO5190712A1 true CO5190712A1 (en) 2002-08-29

Family

ID=22487800

Family Applications (1)

Application Number Title Priority Date Filing Date
CO00044229A CO5190712A1 (en) 1999-06-16 2000-06-14 ANTAGONISTS OF IL-8 RECEIVERS OF IL-8 RECEIVERS

Country Status (9)

Country Link
EP (1) EP1185270A4 (en)
JP (1) JP2003501472A (en)
AU (1) AU5748300A (en)
CO (1) CO5190712A1 (en)
EC (1) ECSP003527A (en)
HK (1) HK1044475A1 (en)
PE (1) PE20010321A1 (en)
UY (1) UY26207A1 (en)
WO (1) WO2000076517A1 (en)

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6642215B2 (en) * 2001-05-24 2003-11-04 Leo Pharma A/S Method of modulating NF-kB activity
CA2565519A1 (en) 2004-05-12 2005-12-01 Schering Corporation Cxcr1 and cxcr2 chemokine antagonists
EP3355876A2 (en) * 2015-09-30 2018-08-08 Instituto de Medicina Molecular Methods for attenuating parasite virulence

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE2928485A1 (en) * 1979-07-14 1981-01-29 Bayer Ag USE OF UREA DERIVATIVES AS A MEDICINAL PRODUCT IN THE TREATMENT OF FATTY METABOLISM DISORDERS
ES2060682T3 (en) * 1988-03-30 1994-12-01 Warner Lambert Co N - ((FENIL (2,6-DISUBSTITUTED)) - N'-ARIL) UREAS AS ANTI-HYPERCHOLESTEROLEMIC AND ANTIATHEROSCLEROTIC AGENTS.
US5780483A (en) * 1995-02-17 1998-07-14 Smithkline Beecham Corporation IL-8 receptor antagonists
WO1998006399A1 (en) * 1996-08-15 1998-02-19 Smithkline Beecham Corporation Il-8 receptor antagonists

Also Published As

Publication number Publication date
ECSP003527A (en) 2002-01-25
PE20010321A1 (en) 2001-05-18
UY26207A1 (en) 2000-12-29
EP1185270A1 (en) 2002-03-13
AU5748300A (en) 2001-01-02
WO2000076517A1 (en) 2000-12-21
EP1185270A4 (en) 2004-02-11
JP2003501472A (en) 2003-01-14
HK1044475A1 (en) 2002-10-25

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