AR018629A1 - ANTAGONISTS OF MUSCARINIC RECEIVER, PHARMACEUTICAL COMPOSITION, USE OF SUCH ANTAGONISTS FOR THE MANUFACTURE OF A MEDICINAL PRODUCT, A METHOD FOR IDENTIFYING MULTIMERIC LIGAND COMPOUNDS THAT HAVE MULTIAGLUTINARY MULTIMOTE BIBLETTING AND A BIBLOTTOM BIGO BIG - Google Patents

ANTAGONISTS OF MUSCARINIC RECEIVER, PHARMACEUTICAL COMPOSITION, USE OF SUCH ANTAGONISTS FOR THE MANUFACTURE OF A MEDICINAL PRODUCT, A METHOD FOR IDENTIFYING MULTIMERIC LIGAND COMPOUNDS THAT HAVE MULTIAGLUTINARY MULTIMOTE BIBLETTING AND A BIBLOTTOM BIGO BIG

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Publication number
AR018629A1
AR018629A1 ARP990102700A ARP990102700A AR018629A1 AR 018629 A1 AR018629 A1 AR 018629A1 AR P990102700 A ARP990102700 A AR P990102700A AR P990102700 A ARP990102700 A AR P990102700A AR 018629 A1 AR018629 A1 AR 018629A1
Authority
AR
Argentina
Prior art keywords
antagonists
ligands
multimeric ligand
ligand compounds
muscarinic receptor
Prior art date
Application number
ARP990102700A
Other languages
Spanish (es)
Original Assignee
Advanced Medicine 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 Advanced Medicine Inc filed Critical Advanced Medicine Inc
Publication of AR018629A1 publication Critical patent/AR018629A1/en

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/08—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms
    • C07D211/10—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with radicals containing only carbon and hydrogen atoms attached to ring carbon atoms
    • C07D211/12—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with radicals containing only carbon and hydrogen atoms attached to ring carbon atoms with only hydrogen atoms attached to the ring nitrogen atom
    • 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
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/06—Anti-spasmodics, e.g. drugs for colics, esophagic dyskinesia
    • 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
    • A61P13/00—Drugs for disorders of the urinary system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04—Indoles; Hydrogenated indoles
    • C07D209/30—Indoles; Hydrogenated indoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to carbon atoms of the hetero ring
    • C07D209/32—Oxygen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/36—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D211/40—Oxygen atoms
    • C07D211/44—Oxygen atoms attached in position 4
    • 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
    • C07D401/02—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 two hetero rings
    • C07D401/12—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 two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • 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
    • C07D403/06—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 carbon chain containing only aliphatic carbon atoms
    • 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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Engineering & Computer Science (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pulmonology (AREA)
  • Urology & Nephrology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Hydrogenated Pyridines (AREA)
  • Pyrrole Compounds (AREA)
  • Indole Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Peptides Or Proteins (AREA)

Abstract

Antagonistas de receptores muscarínicos, caracterizado porque comprenden un compuesto multiaglutinante que comprende de 2 a 10 ligandos sujetadoscovalentemente a uno o más enlaces, donde cada uno de dichos ligandos comprenden independientemente entresí, un antagonista de receptor muscarínico o unmodulador alostérico de un receptor muscarínico y sus sales de aceptacion farmacéutica, con la condicion de que por lo menos uno de dichos ligandos sea unantagonista de receptor muscarínico, y con la condicion además de que cuando el compuesto multiaglutinante comprende 2 o tres ligandos, entonces solamente unode los ligandos es 11-acetilo-5, 11-dihidro-6H-pirido[2,3][1,4]-benzodiazepin-6-ona, N-metilquiniclidina, o un compuesto del grupo de fomulas (I) en la cualn(a) es 0 o 1; R(c) es hidrogeno o alquilo; R(d) es hidrogeno y R(e) es -CO2CRf (fenilo)2, donde R(f) es hidrogeno o hidroxi, utiles en el tratamiento yprevencion de enfermedades tales como enfermedad pulmonar obstructiva cronica, bronquitis cronica, síndrome de intestino irritable, incontinencia urinaria ysimilares. Además se describen, composicion farmacéutica, uso de dichos antagonistas para la manufactura de un medicamento, un método para identificarcompuestos de ligandos multiméricos que tiene propiedades multiaglutinantes, una biblioteca de compuestos de ligando multimérico y un método iterativo paraidentificar compuestos de ligando multimérico.Muscarinic receptor antagonists, characterized in that they comprise a multiaglutinating compound comprising from 2 to 10 ligands covalently attached to one or more bonds, where each of said ligands independently comprises, a muscarinic receptor antagonist or an allosteric modulator of a muscarinic receptor and its salts of pharmaceutical acceptance, with the proviso that at least one of said ligands is a muscarinic receptor antagonist, and with the condition that when the multi-binding compound comprises 2 or three ligands, then only one of the ligands is 11-acetyl-5 , 11-dihydro-6H-pyrido [2,3] [1,4] -benzodiazepin-6-one, N-methylquiniclidine, or a compound of the group of formulas (I) in which n (a) is 0 or 1; R (c) is hydrogen or alkyl; R (d) is hydrogen and R (e) is -CO2CRf (phenyl) 2, where R (f) is hydrogen or hydroxy, useful in the treatment and prevention of diseases such as chronic obstructive pulmonary disease, chronic bronchitis, irritable bowel syndrome , urinary incontinence and similar. In addition, pharmaceutical composition, use of said antagonists for the manufacture of a medicament, a method for identifying multimeric ligand compounds having multiagglutinating properties, a library of multimeric ligand compounds and an iterative method for identifying multimeric ligand compounds are described.

ARP990102700A 1998-06-08 1999-06-08 ANTAGONISTS OF MUSCARINIC RECEIVER, PHARMACEUTICAL COMPOSITION, USE OF SUCH ANTAGONISTS FOR THE MANUFACTURE OF A MEDICINAL PRODUCT, A METHOD FOR IDENTIFYING MULTIMERIC LIGAND COMPOUNDS THAT HAVE MULTIAGLUTINARY MULTIMOTE BIBLETTING AND A BIBLOTTOM BIGO BIG AR018629A1 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US8846698P 1998-06-08 1998-06-08
US9293898P 1998-07-15 1998-07-15
US12028799P 1999-02-16 1999-02-16

Publications (1)

Publication Number Publication Date
AR018629A1 true AR018629A1 (en) 2001-11-28

Family

ID=27375975

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP990102700A AR018629A1 (en) 1998-06-08 1999-06-08 ANTAGONISTS OF MUSCARINIC RECEIVER, PHARMACEUTICAL COMPOSITION, USE OF SUCH ANTAGONISTS FOR THE MANUFACTURE OF A MEDICINAL PRODUCT, A METHOD FOR IDENTIFYING MULTIMERIC LIGAND COMPOUNDS THAT HAVE MULTIAGLUTINARY MULTIMOTE BIBLETTING AND A BIBLOTTOM BIGO BIG

Country Status (8)

Country Link
EP (1) EP1086066A4 (en)
JP (1) JP2002517464A (en)
AR (1) AR018629A1 (en)
AU (1) AU763638B2 (en)
CA (1) CA2315883A1 (en)
NZ (1) NZ505329A (en)
SG (1) SG80041A1 (en)
WO (1) WO1999064043A1 (en)

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TW200800953A (en) 2002-10-30 2008-01-01 Theravance Inc Intermediates for preparing substituted 4-amino-1-(pyridylmethyl) piperidine
PE20040950A1 (en) 2003-02-14 2005-01-01 Theravance Inc BIPHENYL DERIVATIVES AS AGONISTS OF ß2-ADRENERGIC RECEPTORS AND AS ANTAGONISTS OF MUSCARINAL RECEPTORS
US7317102B2 (en) 2003-04-01 2008-01-08 Theravance, Inc. Diarylmethyl and related compounds
US7358244B2 (en) 2003-05-28 2008-04-15 Theravance, Inc. Azabicycloalkane compounds
TW200510298A (en) 2003-06-13 2005-03-16 Theravance Inc Substituted pyrrolidine and related compounds
WO2005007645A1 (en) 2003-07-11 2005-01-27 Theravance, Inc. Substituted 4-amino-1-benzylpiperidine compounds
CA2543858C (en) 2003-11-21 2014-04-15 Theravance, Inc. Compounds having beta2 adrenergic receptor agonist and muscarinic receptor antagonist activity
US7456199B2 (en) 2004-03-11 2008-11-25 Theravance, Inc. Biphenyl compounds useful as muscarinic receptor antagonists
US7262205B2 (en) 2004-03-11 2007-08-28 Theravance, Inc. Biphenyl compounds useful as muscarinic receptor antagonists
TW200538095A (en) 2004-03-11 2005-12-01 Theravance Inc Biphenyl compounds useful as muscarinic receptor antagonists
TWI341836B (en) 2004-03-11 2011-05-11 Theravance Inc Biphenyl compounds useful as muscarinic receptor antagonists
EP1723115A1 (en) 2004-03-11 2006-11-22 Theravance, Inc. Biphenyl compounds useful as muscarinic receptor antagonists
WO2005087733A1 (en) 2004-03-11 2005-09-22 Theravance, Inc. Biphenyl compounds useful as muscarinic receptor antagonists
JP2007528415A (en) 2004-03-11 2007-10-11 セラヴァンス， インコーポレーテッド Useful biphenyl compounds as muscarinic receptor antagonists
JP2007528413A (en) 2004-03-11 2007-10-11 セラヴァンス， インコーポレーテッド Useful biphenyl compounds as muscarinic receptor antagonists
WO2006099031A1 (en) 2005-03-10 2006-09-21 Theravance, Inc. Biphenyl compounds useful as muscarinic receptor antagonists
TW200714587A (en) 2005-03-10 2007-04-16 Theravance Inc Biphenyl compounds useful as muscarinic receptor antagonists
EP1856112A1 (en) 2005-03-10 2007-11-21 Theravance, Inc. Biphenyl compounds useful as muscarinic receptor antagonists
EP1866284A1 (en) 2005-03-10 2007-12-19 Theravance, Inc. Biphenyl compounds useful as muscarinic receptor antagonists
US7659403B2 (en) 2005-03-10 2010-02-09 Theravance, Inc. Biphenyl compounds useful as muscarinic receptor antagonists
WO2006138218A1 (en) 2005-06-13 2006-12-28 Theravance, Inc. Biphenyl compounds useful as muscarinic receptor antagonists
GB0602778D0 (en) 2006-02-10 2006-03-22 Glaxo Group Ltd Novel compound
US8389759B2 (en) 2007-03-12 2013-03-05 Nektar Therapeutics Oligomer-anticholinergic agent conjugates
WO2017107877A1 (en) * 2015-12-25 2017-06-29 四川海思科制药有限公司 Biphenyl derivative and preparation method and medical use thereof

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US4587046A (en) * 1982-05-18 1986-05-06 The Regents Of The University Of California Drug-carrier conjugates
DE3402060A1 (en) * 1984-01-21 1985-08-01 Dr. Karl Thomae Gmbh, 7950 Biberach SUBSTITUTED 5,11-DIHYDRO-6H-DIBENZ (B, E) AZEPIN-6-ONE, METHOD FOR THE PRODUCTION THEREOF AND MEDICINAL PRODUCTS CONTAINING THESE COMPOUNDS
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EP0510132B1 (en) * 1990-09-28 1997-05-14 Neorx Corporation Polymeric carriers for release of covalently linked agents

Also Published As

Publication number Publication date
CA2315883A1 (en) 1999-12-16
NZ505329A (en) 2003-05-30
SG80041A1 (en) 2001-04-17
EP1086066A4 (en) 2001-08-08
JP2002517464A (en) 2002-06-18
AU763638B2 (en) 2003-07-31
AU4550899A (en) 1999-12-30
EP1086066A1 (en) 2001-03-28
WO1999064043A9 (en) 2000-03-02
WO1999064043A1 (en) 1999-12-16

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