AR039383A1 - Derivados del tropano utiles en terapia - Google Patents

Derivados del tropano utiles en terapia

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Publication number
AR039383A1
AR039383A1 ARP030101205A ARP030101205A AR039383A1 AR 039383 A1 AR039383 A1 AR 039383A1 AR P030101205 A ARP030101205 A AR P030101205A AR P030101205 A ARP030101205 A AR P030101205A AR 039383 A1 AR039383 A1 AR 039383A1
Authority
AR
Argentina
Prior art keywords
alkyl
conr6r7
nr6r7
substituted
atoms
Prior art date
Application number
ARP030101205A
Other languages
English (en)
Original Assignee
Pfizer
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 GBGB0208071.1A external-priority patent/GB0208071D0/en
Priority claimed from GB0301575A external-priority patent/GB0301575D0/en
Application filed by Pfizer filed Critical Pfizer
Publication of AR039383A1 publication Critical patent/AR039383A1/es

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D519/00Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D451/00Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof
    • C07D451/02Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof
    • C07D451/04Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof with hetero atoms directly attached in position 3 of the 8-azabicyclo [3.2.1] octane or in position 7 of the 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring system
    • AHUMAN NECESSITIES
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    • 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
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    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/18Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
    • AHUMAN NECESSITIES
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    • A61P11/00Drugs for disorders of the respiratory system
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    • A61P11/00Drugs for disorders of the respiratory system
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
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    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • A61P31/14Antivirals for RNA viruses
    • A61P31/18Antivirals for RNA viruses for HIV
    • AHUMAN NECESSITIES
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    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Public Health (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Diabetes (AREA)
  • Neurology (AREA)
  • Cardiology (AREA)
  • Pulmonology (AREA)
  • Immunology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Hematology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Virology (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Endocrinology (AREA)
  • Dermatology (AREA)
  • Urology & Nephrology (AREA)
  • Hospice & Palliative Care (AREA)
  • Obesity (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Transplantation (AREA)
  • Child & Adolescent Psychology (AREA)
  • Reproductive Health (AREA)
  • Rheumatology (AREA)
  • AIDS & HIV (AREA)
  • Psychiatry (AREA)
  • Molecular Biology (AREA)

Abstract

Los compuestos de la presente son moduladores, especialmente antagonistas, de la actividad de los receptores CCR5 de quimioquinas. Los moduladores del receptor CCR5 pueden ser útiles para el tratamiento de diversas enfermedades inflamatorias y situaciones con inflamaciones, y para el tratamiento de la infección por el HIV-1 y retrovirus genéticamente relacionados. Reivindicación 1: Un compuesto caracterizado porque es de la fórmula (1) o una de sus sales, solvatos o derivados farmacéuticamente aceptables, en el que: X e Y se seleccionan entre CH2 y NR4 de forma de que X e Y uno de ellos es CH2 y el otro es NR4; R1 y R4 son independientemente R5; COR5; CO2R5; CONR6R7; SO2R5; o (alquilen C1-6)fenilo, en el que el fenilo está sustituido con de 0 a 3 átomos o grupos seleccionados entre alquilo C1-6, alquil(C1-6)-carbonilo, alcoxi C1-6, alcoxi(C1-6)-carbonilo, halógeno, CF3, OH, CN, NR6R7,CO2R7 ó CONR6R7; R2 es un fenilo sustituido con de 0 a 3 átomos o grupos seleccionados entre alquilo C1-6, alquil(C1-6)-carbonilo, alcoxi C1-6, alcoxi(C1-6)-carbonilo, halógeno, CF3, OH, CN, NR6R7, CO2R7 ó CONR6R7; R3 es un alquilo C1-4 sustituido con de 0 a 3 átomos de flúor; R5 es un alquilo C1-6; alquenilo C2-6; alquinilo C2-6; cicloalquilo C3-7; un heterociclo aromático de 5 ó 6 miembros, o un heterociclo saturado de 4 a 7 miembros; en el que dichos alquilo, alquenilo, alquinilo y cicloalquilo están sustituidos con de 0 a 3 átomos o grupos seleccionados entre oxo, halógeno, CF3, OR7, CN, NR6R7, COR7, CO2R7 ó CONR6R7; en el que dichos heterociclos contienen de uno a tres heteroátomos seleccionados entre N, O ó S; y en el que dichos heterociclos están sustituidos con de 0 a 3 átomos o grupos seleccionados entre alquilo C1-6, alquilo(C1-6)-carbonilo, alcoxi C1-6, alcoxi(C1-6)-carbonilo, halógeno, CF3, OH, CN, NR6R7, COR7, CO2R7 ó CONR6R7; R6 es H ó R5; R7 es H o un alquilo C1-6; o, cuando R6 y R7 están ambos unidos al mismo átomo de N, NR6R7 puede representar también un heterociclo de 5 a 7 miembros, saturado, parcialmente insaturado o aromático, que contiene de 0 a 2 heteroátomos adicionales seleccionados entre O, N ó S.
ARP030101205A 2002-04-08 2003-04-07 Derivados del tropano utiles en terapia AR039383A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
GBGB0208071.1A GB0208071D0 (en) 2002-04-08 2002-04-08 Tropane derivatives useful in therapy
GB0301575A GB0301575D0 (en) 2003-01-23 2003-01-23 Tropane derivatives useful in therapy

Publications (1)

Publication Number Publication Date
AR039383A1 true AR039383A1 (es) 2005-02-16

Family

ID=28793308

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP030101205A AR039383A1 (es) 2002-04-08 2003-04-07 Derivados del tropano utiles en terapia

Country Status (41)

Country Link
EP (1) EP1492789B1 (es)
JP (2) JP3793200B2 (es)
KR (1) KR100734685B1 (es)
CN (1) CN1324025C (es)
AP (1) AP1789A (es)
AR (1) AR039383A1 (es)
AT (1) ATE328882T1 (es)
AU (1) AU2003214503B2 (es)
BR (1) BR0309118A (es)
CA (1) CA2481482C (es)
CR (1) CR7514A (es)
CU (1) CU23282A3 (es)
CY (1) CY1106114T1 (es)
DE (1) DE60305903T2 (es)
DK (1) DK1492789T3 (es)
DO (1) DOP2003000624A (es)
EA (1) EA007590B1 (es)
ES (1) ES2263960T3 (es)
GE (1) GEP20074210B (es)
HK (1) HK1076102A1 (es)
HN (1) HN2003000114A (es)
HR (1) HRP20040940A2 (es)
IL (1) IL164261A0 (es)
IS (1) IS2577B (es)
MA (1) MA27190A1 (es)
MX (1) MXPA04009220A (es)
MY (1) MY134223A (es)
NI (1) NI200300053A (es)
NO (1) NO329674B1 (es)
NZ (1) NZ535452A (es)
OA (1) OA12798A (es)
PA (1) PA8570801A1 (es)
PE (1) PE20040082A1 (es)
PL (1) PL372968A1 (es)
PT (1) PT1492789E (es)
RS (1) RS51550B (es)
SI (1) SI1492789T1 (es)
TN (1) TNSN04194A1 (es)
TW (1) TWI280130B (es)
UY (1) UY27752A1 (es)
WO (1) WO2003084954A1 (es)

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JP3793200B2 (ja) * 2002-04-08 2006-07-05 ファイザー・インク Ccr5モジュレータとしてのトロパン誘導体
US6855724B2 (en) 2002-04-08 2005-02-15 Agouron Pharmaceuticals, Inc. Tropane derivatives useful in therapy
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AP2174A (en) * 2003-10-03 2010-11-20 Pfizer Imidazopyridine substituted tropane derivatives with CCR5 receptor antagonist activity for the treatment of HIV and inflamation.
TW200533348A (en) 2004-02-18 2005-10-16 Theravance Inc Indazole-carboxamide compounds as 5-ht4 receptor agonists
US7751601B2 (en) 2004-10-04 2010-07-06 Validity Sensors, Inc. Fingerprint sensing assemblies and methods of making
US8131026B2 (en) 2004-04-16 2012-03-06 Validity Sensors, Inc. Method and apparatus for fingerprint image reconstruction
WO2006064340A2 (en) * 2004-12-13 2006-06-22 Pfizer Limited Process for the preparation of n-acyl beta-aminoaldehydes
WO2008063600A2 (en) * 2006-11-17 2008-05-29 Concert Pharmaceuticals Inc. Triazolyl tropane derivatives
JP5194105B2 (ja) 2007-04-13 2013-05-08 ドン ファ ファーマシューティカル カンパニー リミテッド 1−シクロプロピル−6−フルオロ−7−(8−メトキシイミノ−2,6−ジアザ−スピロ[3.4]オクト−6−イル)−4−オキソ−1,4−ジヒドロ−[1,8]ナフチリジン−3−カルボン酸のアスパラギンサン酸塩、その製造方法、およびそれを含む抗菌用薬学組成物
US7947710B2 (en) 2007-08-27 2011-05-24 Theravance, Inc. Disubstituted alkyl-8-azabicyclo[3.2.1]octane compounds as mu opioid receptor antagonists
CN101712679B (zh) 2008-10-08 2013-04-10 中国科学院上海药物研究所 一种酰胺类化合物、其药物组合物及其制备方法和用途
CA2778206A1 (en) * 2009-11-21 2011-05-26 F. Hoffmann-La Roche Ag Heterocyclic antiviral compounds
JP5731538B2 (ja) 2009-12-23 2015-06-10 アイアンウッド ファーマシューティカルズ インコーポレイテッド Crth2モジュレーター
WO2011121558A1 (en) 2010-04-02 2011-10-06 Phivco-1 Llc Combination therapy comprising a ccr5 antagonist, a hiv-1 protease inhibitor and a pharmacokinetic enhancer
WO2012009134A1 (en) 2010-07-12 2012-01-19 Ironwood Pharmaceuticals, Inc. Crth2 modulators
US20130216552A1 (en) 2010-07-12 2013-08-22 Ironwood Pharmaceuticals, Inc. Crth2 modulators
HUE047354T2 (hu) 2011-05-18 2020-04-28 Vertex Pharmaceuticals Europe Ltd Ivacaftor deuterizált származékai
EP2741777B1 (en) 2011-08-12 2017-01-18 INSERM - Institut National de la Santé et de la Recherche Médicale Methods and pharmaceutical compositions for treatment of pulmonary hypertension
CN106977511B (zh) * 2011-12-19 2019-04-12 中国科学院上海药物研究所 一种氨基丙基取代托烷胺类化合物、其药物组合物及其制备方法和用途
JP6146990B2 (ja) * 2012-11-16 2017-06-14 コンサート ファーマシューティカルズ インコーポレイテッド 重水素化されたcftr増強物質
GB201321748D0 (en) * 2013-12-09 2014-01-22 Ucb Pharma Sa Therapeutic agents
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WO2016160945A1 (en) 2015-03-31 2016-10-06 Concert Pharmaceuticals, Inc. Deuterated vx-661
MA42954A (fr) 2015-09-25 2018-08-01 Vertex Pharmaceuticals Europe Ltd Potentialisateurs cftr deutérés
JP2017105824A (ja) * 2017-02-10 2017-06-15 コンサート ファーマシューティカルズ インコーポレイテッド 重水素化されたcftr増強物質
US11708331B2 (en) 2017-12-01 2023-07-25 Vertex Pharmaceuticals Incorporated Processes for making modulators of cystic fibrosis transmembrane conductance regulator
WO2019183133A1 (en) 2018-03-19 2019-09-26 Emory University Pan-Tropic Entry Inhibitors
JP6654223B2 (ja) * 2018-08-13 2020-02-26 バーテックス ファーマシューティカルズ (ヨーロッパ) リミテッド 重水素化されたcftr増強物質
US11629196B2 (en) 2020-04-27 2023-04-18 Incelldx, Inc. Method of treating SARS-CoV-2-associated hypercytokinemia by administering a human monoclonal antibody (PRO-140) that inhibits CCR5/CCL5 binding interactions

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PE20001420A1 (es) * 1998-12-23 2000-12-18 Pfizer Moduladores de ccr5
WO2001080106A1 (fr) * 2000-04-19 2001-10-25 Satoshi Yamazaki Procede de diffusion d'outil publicitaire et support magnetique pour le logiciel
DE60102233T2 (de) * 2000-05-26 2005-01-27 Pfizer Inc. Triazolyltropanderivate als ccr5-modulatoren
JP3793200B2 (ja) * 2002-04-08 2006-07-05 ファイザー・インク Ccr5モジュレータとしてのトロパン誘導体

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DK1492789T3 (da) 2006-09-11
KR100734685B1 (ko) 2007-07-02
NI200300053A (es) 2005-11-01
CA2481482C (en) 2009-11-10
JP2005532285A (ja) 2005-10-27
NZ535452A (en) 2006-11-30
HN2003000114A (es) 2004-05-05
PE20040082A1 (es) 2004-03-20
CR7514A (es) 2004-11-08
AU2003214503A1 (en) 2003-10-20
HRP20040940A2 (en) 2005-04-30
RS51550B (en) 2011-06-30
HK1076102A1 (en) 2006-01-06
PT1492789E (pt) 2006-09-29
JP4571078B2 (ja) 2010-10-27
AU2003214503B2 (en) 2008-08-07
DE60305903T2 (de) 2007-03-08
WO2003084954A1 (en) 2003-10-16
IL164261A0 (en) 2005-12-18
ATE328882T1 (de) 2006-06-15
BR0309118A (pt) 2005-02-01
AP1789A (en) 2007-10-05
AP2004003147A0 (en) 2004-09-30
CY1106114T1 (el) 2011-06-08
NO329674B1 (no) 2010-11-29
ES2263960T3 (es) 2006-12-16
SI1492789T1 (sl) 2006-10-31
JP2006182784A (ja) 2006-07-13
MY134223A (en) 2007-11-30
CN1646526A (zh) 2005-07-27
MXPA04009220A (es) 2005-09-30
GEP20074210B (en) 2007-10-10
KR20040099420A (ko) 2004-11-26
NO20044615L (no) 2004-10-26
TWI280130B (en) 2007-05-01
EP1492789A1 (en) 2005-01-05
TW200403242A (en) 2004-03-01
RS88804A (en) 2006-12-15
UY27752A1 (es) 2003-11-28
TNSN04194A1 (fr) 2007-03-12
DE60305903D1 (de) 2006-07-20
OA12798A (en) 2006-07-10
JP3793200B2 (ja) 2006-07-05
EP1492789B1 (en) 2006-06-07
IS2577B (is) 2010-02-15
CU23282A3 (es) 2008-06-30
CN1324025C (zh) 2007-07-04
PL372968A1 (en) 2005-08-08
CA2481482A1 (en) 2003-10-16
EA200401167A1 (ru) 2005-04-28
DOP2003000624A (es) 2003-10-15
IS7453A (is) 2004-09-16
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EA007590B1 (ru) 2006-12-29
PA8570801A1 (es) 2004-11-26

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