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AR046321A1 - Compuestos de lactamas macrociclicas, procedimientos de preparacion y composiciones farmaceuticas. - Google Patents

Compuestos de lactamas macrociclicas, procedimientos de preparacion y composiciones farmaceuticas.

Info

Publication number
AR046321A1
AR046321A1 ARP040104052A ARP040104052A AR046321A1 AR 046321 A1 AR046321 A1 AR 046321A1 AR P040104052 A ARP040104052 A AR P040104052A AR P040104052 A ARP040104052 A AR P040104052A AR 046321 A1 AR046321 A1 AR 046321A1
Authority
AR
Argentina
Prior art keywords
alkyl
diyl
cycloalkyl
hydrogen
tetrahydro
Prior art date
Application number
ARP040104052A
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English (en)
Original Assignee
Novartis Ag
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 Novartis Ag filed Critical Novartis Ag
Publication of AR046321A1 publication Critical patent/AR046321A1/es

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D245/00Heterocyclic compounds containing rings of more than seven members having two nitrogen atoms as the only ring hetero atoms
    • C07D245/02Heterocyclic compounds containing rings of more than seven members having two nitrogen atoms as the only ring hetero atoms not condensed with other rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • 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
    • A61P25/28Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/04Antineoplastic agents specific for metastasis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D255/00Heterocyclic compounds containing rings having three nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D249/00 - C07D253/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D255/00Heterocyclic compounds containing rings having three nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D249/00 - C07D253/00
    • C07D255/02Heterocyclic compounds containing rings having three nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D249/00 - C07D253/00 not condensed with other rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D273/00Heterocyclic compounds containing rings having nitrogen and oxygen atoms as the only ring hetero atoms, not provided for by groups C07D261/00 - C07D271/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D281/00Heterocyclic compounds containing rings of more than six members having one nitrogen atom and one sulfur atom as the only ring hetero atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/08Bridged systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D513/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/02Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
    • C07D513/08Bridged systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Epidemiology (AREA)
  • Psychiatry (AREA)
  • Hospice & Palliative Care (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen- Or Sulfur-Containing Heterocyclic Ring Compounds With Rings Of Six Or More Members (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Other In-Based Heterocyclic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)

Abstract

El presente se refiere a su preparación, y composiciones farmacéuticas que los comprenden. Reivindicación 1: Un compuesto de la fórmula (1), en donde: R1 es CH(Re)C(=O)N(Ra)Rb o (CH2)kN(Rc)Rd, en donde K es 0, 1 ó 2; Ra y Rb, independientemente, son hidrógeno o un grupo alquilo C1-8 opcionalmente sustituido, cicloalquilo C3-7, cicloalquilo C3-7-alquilo C1-4, arilo, arilalquilo C1-4, heteroarilo o heteroarilalquilo C1-4; Rc y Rd, independientemente, son hidrógeno o un grupo alquilo C1-8 opcionalmente sustituido, cicloalquilo C3-7, cicloalquilo C3-7-alquilo C1-4, arilo, arilalquilo C1-4, heteroarilo, heteroarilalquilo C1-4, croman-4-ilo, isocroman-4-ilo, tiocroman-4-ilo, isotiocroman-4-ilo, 1,1-dioxo-1l*6*-tiocroman-4-ilo, 2,2-dioxo- 2l*6*-isotiocroman-4-ilo, 1,2,3,4-tetrahidro-quinolin-4-ilo, 1,2,3,4-tetrahidro-isoquinolin-4-ilo, 1,2,3,4-tetrahidro-naftalen-1-ilo, 1,1-dioxo-1,2,3,4-tetrahidro-1l*6*-benzo[e][1,2]tiazin-4-ilo, 2,2-dioxo-1,2,3,4-tetrahidro-2l*6*benzo[c][1,2]tiazin- 4-ilo, 1,1-dioxo-3,4-dihidro-1H-1l*6*[c][1,2]oxatiin-4-ilo, 2,2-dioxo-3,4-dihidro-2H-2l*6*[e][1,2]oxatiin-4-ilo, 2,3,4,5-tetrahidro-benzo[b]oxepin-5-ilo o 1,2,3,4-tetrahidro-benzo[c]oxepin-5-ilo, o Ra y Rb, o Rc y Rd junto con el átomo de nitrógeno al cual están unidos, forman un grupo pirrolidinilo opcionalmente sustituido, 1-piperidinilo, 4-morfolinilo o piperazinilo; y Re es alquilo C1-8 opcionalmente sustituido, alcoxi C1-4-alquilo C1-4, cicloalquilo C3-7 o cicloalquilo C3-7-alquilo C1-4; R2 es hidrógeno o alquilo C1-4; R3 es hidrógeno, alquilo C1-6 o un grupo alquilo C1-6OC(=O)NH, cicloalquilo C3-7OC(=O)NH, cicloalquilo C3-7-alquilo C1-4OC(=O)NH, arilalquilo C1-4OC(=O)NH, heteroarilalquilo C1-4OC(=O)NH, alquilo C1-4OC(=O)NH, cicloalquilo C3-7OC(=O)NH, ariloOC(=O)NH, arilalquilo C1-4OC(=O)NH, heteroariloOC(=O)NH, o heteroarilalquilo C1-4OC(=O)NH; U es un enlace CF2, CF2CF2, CHF, CHFCHF, cicloprop-1,2-ileno, alquilenoxi C1-3, alquileno C1-8, NRg o un anillo aromático o heteroaromático, cuyo anillo está opcionalmente sustituido con halógeno, alcoxi C1-4, hidroxi o alquilo C1-4, en donde Z y V están en la posición orto o meta uno con respecto del otro, en donde Rg es hidrógeno, alquilo C1-8 o cicloalquilo C3-7; V es CH=CH, cicloprop-1,2-ileno, CH2CH(OH), CH(OH)CH2 o CRhRhCRhRh, en donde cada Rh, independientemente, es hidrógeno, flúor o alquilo C1-4; W es alquileno C1-6, O, S, S(=O)2, C(=O), C(=O)O, OC(=O), C(Rf)C(=O), C(=O)NRf o NRf, en donde Rf es hidrógeno o alquilo C1-4; X es un grupo alcanililideno C1-4 opcionalmente sustituido, alquileno C1-4, cicloalquileno C3-7, piperidin-diilo, pirrolidin-diilo, benzotiazol-4,6-diilo, benzoxazol-4,6-diilo, 1H-benzotriazol-4,6-diilo, imidazol[1,2-a]piridin-6,8- diilo, benzo-[1,2,5]oxadiazol-4,6-diilo, benzo[1,2,5]tiadiazol-4,6-diilo, 1H-indazol-1,6-diilo, 1H-bencimidazol-4,6-diilo o 1H-indazol-1,6-diilo o un anillo aromático o heteroaromático opcionalmente sustituido, en donde Y y C(=O)NR2 están en la posición meta uno con respecto del otro; Y es un enlace, O, S(=O)2, S(=O)2NRg, N(Rg)S(=O)2, NRg, C(Rg)OH, C(=O)NRg, N(Rg)C(=O), C(=O)N(Rg)O o ON(Rg)C(=O), en donde Rg es hidrógeno, alquilo C1-8 o cicloalquilo C3-7; Z es O, CH2, CF2, CHF, cicloprop- 1,2-ileno o un enlace; y n es de 0 a 5, el número de átomos de anillo incluidos en el anillo macrocíclico siendo 14, 15, 16 o 17, en forma de base libre o en forma de sal de adición de ácido.
ARP040104052A 2003-11-05 2004-11-04 Compuestos de lactamas macrociclicas, procedimientos de preparacion y composiciones farmaceuticas. AR046321A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
GBGB0325830.8A GB0325830D0 (en) 2003-11-05 2003-11-05 Organic compounds

Publications (1)

Publication Number Publication Date
AR046321A1 true AR046321A1 (es) 2005-11-30

Family

ID=29725994

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP040104052A AR046321A1 (es) 2003-11-05 2004-11-04 Compuestos de lactamas macrociclicas, procedimientos de preparacion y composiciones farmaceuticas.

Country Status (15)

Country Link
US (2) US7612055B2 (es)
EP (1) EP1682521A1 (es)
JP (1) JP4628366B2 (es)
KR (1) KR20060110289A (es)
CN (1) CN1902182A (es)
AR (1) AR046321A1 (es)
AU (1) AU2004291276B2 (es)
BR (1) BRPI0416276A (es)
CA (1) CA2544751A1 (es)
GB (1) GB0325830D0 (es)
MX (1) MXPA06005032A (es)
PE (1) PE20051006A1 (es)
RU (1) RU2006119504A (es)
TW (1) TW200530203A (es)
WO (1) WO2005049585A1 (es)

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CN103370331B (zh) 2011-02-08 2017-02-15 默克专利股份有限公司 用于治疗关节病的氨基他汀衍生物
PH12013501934A1 (en) 2011-03-18 2022-04-08 Bayer Ip Gmbh N-(3-carbamoylphenyl)-1h-pyrazole-5-carboxamide derivatives and the use thereof for controlling animal pests
EP2877485B1 (de) 2012-07-24 2018-03-14 Merck Patent GmbH Hydroxystatin-derivate zur behandlung von arthrose
US9663475B2 (en) 2013-02-25 2017-05-30 Merck Patent Gmbh 2 amino-3,4-dihydrcquinazoline derivatives and the use thereof as cathepsin D inhibitors
CN105451754A (zh) 2013-08-06 2016-03-30 默克专利股份有限公司 在关节病的情况下胃酶抑素的关节内施用
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GB0500683D0 (en) * 2005-01-13 2005-02-23 Novartis Ag Organic compounds
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Also Published As

Publication number Publication date
CN1902182A (zh) 2007-01-24
RU2006119504A (ru) 2007-12-27
JP4628366B2 (ja) 2011-02-09
WO2005049585A1 (en) 2005-06-02
GB0325830D0 (en) 2003-12-10
US7612055B2 (en) 2009-11-03
BRPI0416276A (pt) 2007-01-23
EP1682521A1 (en) 2006-07-26
US20070072792A1 (en) 2007-03-29
AU2004291276B2 (en) 2009-03-12
CA2544751A1 (en) 2005-06-02
TW200530203A (en) 2005-09-16
US20100022500A1 (en) 2010-01-28
JP2007510002A (ja) 2007-04-19
AU2004291276A1 (en) 2005-06-02
MXPA06005032A (es) 2006-07-06
KR20060110289A (ko) 2006-10-24
PE20051006A1 (es) 2005-12-28

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