NZ505329A - Two heteroaryl or aryl containing compounds covalently attached via a linker useful as muscarinic receptor antagonists - Google Patents

Two heteroaryl or aryl containing compounds covalently attached via a linker useful as muscarinic receptor antagonists

Info

Publication number
NZ505329A
NZ505329A NZ505329A NZ50532999A NZ505329A NZ 505329 A NZ505329 A NZ 505329A NZ 505329 A NZ505329 A NZ 505329A NZ 50532999 A NZ50532999 A NZ 50532999A NZ 505329 A NZ505329 A NZ 505329A
Authority
NZ
New Zealand
Prior art keywords
nr
covalent bond
xa
optionally attaches
independently
Prior art date
Application number
NZ505329A
Inventor
Mathai Mammen
David Oare
John H Griffin
James Aggen
Original Assignee
Theravance 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
Priority to US8846698P priority Critical
Priority to US9293898P priority
Priority to US12028799P priority
Application filed by Theravance Inc filed Critical Theravance Inc
Priority to PCT/US1999/012733 priority patent/WO1999064043A1/en
Publication of NZ505329A publication Critical patent/NZ505329A/en

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D211/00Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06Heterocyclic 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
    • C07D211/08Heterocyclic 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
    • C07D211/10Heterocyclic 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
    • C07D211/12Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D209/00Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04Indoles; Hydrogenated indoles
    • C07D209/30Indoles; 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
    • C07D209/32Oxygen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D211/00Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06Heterocyclic 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
    • C07D211/36Heterocyclic 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
    • C07D211/40Oxygen atoms
    • C07D211/44Oxygen atoms attached in position 4
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/12Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic 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
    • C07D403/06Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic 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
    • C07D403/12Heterocyclic 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

Abstract

A multibinding compound of formula L-X-L (I) wherein: each L is independently a compound of formula (a), (b), (c), (d), (e), (f), (g) or (h) and X is Xa-Z-(Ya-Z)m-Yb-Z-Xa; m is 0 to 20; each Xa is independently -O-, -S-, -NR-, -C(O)-, -C(O)O-, -C(O)NR-, -C(S)-, -C(S)O-, -C(S)NR- or a covalent bond; each Z is independently optionally substituted alkylene, cycloalkylene, alkenylene, alkynylene, cycloalkenylene or arylene, heteroarylene, heterocyclene, or a covalent bond; Ya and Yb are independently -O-, -C(O)-, -OC(O)-, -C(O)O-, -NR-, -S(O)n-, -C(O)NR'-, -NR'C(O)-, -NR'C(O)NR'-, -NR'C(S)NR'-, -C(=NR')-NR'-, -NR'-C(=NR')-, -OC(O)-NR'-, -NR'-C(O)-O-, -N=C(Xa)-NR'-, -NR'-C(Xa)=N-, -P(O)(OR')-O-, -O-P(O)(OR')-, S(O)nCR'R"-, -S(O)n-NR'-, -NR'-S(O)n-, -S-S- or a covalent bond; A is an aryl or a heteroaryl ring; B is a heterocycloamino group, which optionally attaches X to L; C is an aryl or heteroaryl ring, which optionally attaches the ligand to a linker; GÆ is pyrrolidine, piperidine or a group of formula (2) which optionally attaches L to X; G is aryl, heteroaryl heterocyclic or cycloalkyl, which optionally attaches L to X P is aryl or heteroaryl ring which optionally attaches L to X; S is heterocycloamino which optionally attaches L to X; R20 and R21 are independently hydrogen, alkyl or a covalent bond attaching L to X or together with the nitrogen atom to which they are attached form a heterocycloamino ring, which optionally attaches L to X; R25 and R26 are independently hydrogen, alkyl, aralkyl, or a covalent bond attaching L to X or together with the nitrogen atom to which they are attached form a heterocycloamino group, which optionally attaches L to X; D" is alkylene; D is NR31R32, -N+(R33R34R35) or -OR32; F is -NR40-, -O-, -S- or ûCHR41-; F" is a covalent bond, -OR43, -NR42R43 or -N+R43R44R45 and the rest of the variables are as defined in the specification. The compounds are useful for treating a disease mediated by muscarinic receptor such as chronic obstructive pulmonary disease, chronic bronchitis, irritable bowel syndrome or urinary incontinence.
NZ505329A 1998-06-08 1999-06-07 Two heteroaryl or aryl containing compounds covalently attached via a linker useful as muscarinic receptor antagonists NZ505329A (en)

Priority Applications (4)

Application Number Priority Date Filing Date Title
US8846698P true 1998-06-08 1998-06-08
US9293898P true 1998-07-15 1998-07-15
US12028799P true 1999-02-16 1999-02-16
PCT/US1999/012733 WO1999064043A1 (en) 1998-06-08 1999-06-07 Muscarinic receptor antagonists

Publications (1)

Publication Number Publication Date
NZ505329A true NZ505329A (en) 2003-05-30

Family

ID=27375975

Family Applications (1)

Application Number Title Priority Date Filing Date
NZ505329A NZ505329A (en) 1998-06-08 1999-06-07 Two heteroaryl or aryl containing compounds covalently attached via a linker useful as muscarinic receptor antagonists

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)

Families Citing this family (23)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TW200800953A (en) 2002-10-30 2008-01-01 Theravance Inc Intermediates for preparing substituted 4-amino-1-(pyridylmethyl) piperidine
PE09502004A1 (en) 2003-02-14 2005-01-01 Theravance Inc AS biphenyl derivatives adrenoceptor agonists SS2 and as antagonists of muscarinic
JP4767842B2 (en) 2003-04-01 2011-09-07 セラヴァンス, インコーポレーテッド Diarylmethyl compounds and related compounds having β2 adrenergic receptor agonist activity and muscarinic receptor antagonist activity
EP1626970B1 (en) 2003-05-28 2009-07-08 Theravance, Inc. Azabicycloalkane compounds as muscarinic receptor antagonists
TW200510298A (en) 2003-06-13 2005-03-16 Theravance Inc Substituted pyrrolidine and related compounds
JP2007524641A (en) 2003-07-11 2007-08-30 セラヴァンス, インコーポレーテッド Substituted 4-amino-1-benzylpiperidine compounds
ES2329586T3 (en) 2003-11-21 2009-11-27 Theravance, Inc. Compounds that have agonist activity of the beta2 adrenergic receiver and antagonist of the muscarine receiver.
EP1723109A1 (en) 2004-03-11 2006-11-22 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
WO2005087736A1 (en) 2004-03-11 2005-09-22 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
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
TW200538095A (en) 2004-03-11 2005-12-01 Theravance Inc Biphenyl compounds useful as muscarinic receptor antagonists
EP1723110A1 (en) 2004-03-11 2006-11-22 Theravance, Inc. Biphenyl compounds useful as muscarinic receptor antagonists
WO2005087737A1 (en) 2004-03-11 2005-09-22 Theravance, Inc. Biphenyl compounds useful as muscarinic receptor antagonists
US7642355B2 (en) 2005-03-10 2010-01-05 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
TW200714587A (en) 2005-03-10 2007-04-16 Theravance Inc Biphenyl compounds useful as muscarinic receptor antagonists
US7479562B2 (en) 2005-03-10 2009-01-20 Theravance, Inc. Biphenyl compounds useful as muscarinic receptor antagonists
WO2006099032A1 (en) 2005-03-10 2006-09-21 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

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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 Thomae Gmbh Dr K Substituted 5,11-dihydro-6H-dibenz (b, e) azepin-6-one, process for their preparation and pharmaceutical compositions containing these compounds
US4675326A (en) * 1985-05-08 1987-06-23 Gabriel Amitai Bisquaternary antidotes
US5534520A (en) * 1990-04-10 1996-07-09 Fisher; Abraham Spiro compounds containing five-membered rings
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
WO1999064043A9 (en) 2000-03-02
SG80041A1 (en) 2001-04-17
EP1086066A1 (en) 2001-03-28
AR018629A1 (en) 2001-11-28
EP1086066A4 (en) 2001-08-08
AU4550899A (en) 1999-12-30
CA2315883A1 (en) 1999-12-16
JP2002517464A (en) 2002-06-18
AU763638B2 (en) 2003-07-31
WO1999064043A1 (en) 1999-12-16

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Owner name: THERAVANCE BIOPHARMA R+D IP, LLC, US

Effective date: 20140807

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