EP1140086A1 - N-ureidoalkyl-piperidines utilisees en tant que modulateurs de l'activite des recepteurs des chimiokines - Google Patents

N-ureidoalkyl-piperidines utilisees en tant que modulateurs de l'activite des recepteurs des chimiokines

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Publication number
EP1140086A1
EP1140086A1 EP99964297A EP99964297A EP1140086A1 EP 1140086 A1 EP1140086 A1 EP 1140086A1 EP 99964297 A EP99964297 A EP 99964297A EP 99964297 A EP99964297 A EP 99964297A EP 1140086 A1 EP1140086 A1 EP 1140086A1
Authority
EP
European Patent Office
Prior art keywords
alkyl
occurrence
substituted
cycloalkyl
chr
Prior art date
Legal status (The legal status 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 status listed.)
Withdrawn
Application number
EP99964297A
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German (de)
English (en)
Other versions
EP1140086A4 (fr
Inventor
Soo S. Ko
George V. Delucca
John V. Duncia
Joseph B. Santella, Iii
Dean A. Wacker
Paul S. Watson
Jeffrey G. Varnes
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Bristol Myers Squibb Pharma Co
Original Assignee
DuPont Merck Pharmaceutical Co
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Publication date
Application filed by DuPont Merck Pharmaceutical Co filed Critical DuPont Merck Pharmaceutical Co
Publication of EP1140086A1 publication Critical patent/EP1140086A1/fr
Publication of EP1140086A4 publication Critical patent/EP1140086A4/fr
Withdrawn legal-status Critical Current

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D207/00Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/04Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom 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
    • C07D207/08Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom 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 radicals, substituted by hetero atoms, attached to ring carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D207/00Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/04Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom 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
    • C07D207/06Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom 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 radicals, containing only hydrogen and carbon atoms, attached to ring carbon 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
    • C07D211/08Heterocyclic 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
    • C07D211/14Heterocyclic 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 hydrocarbon or substituted hydrocarbon radicals attached to the ring nitrogen atom
    • 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
    • C07D211/18Heterocyclic 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 substituted hydrocarbon radicals attached to ring carbon atoms
    • 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
    • C07D401/06Heterocyclic 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 carbon chain containing only aliphatic carbon atoms
    • 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
    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • C07D471/10Spiro-condensed systems

Definitions

  • NPY Neuropeptide Y
  • A is lower alkylene and R 4 may be phenyl optionally substituted with halogen.
  • U.S. Pat. No. 5,668,151 discloses Neuropeptide Y (NPY) antagonists comprising 1, 4-dihydropyridines with a piperidinyl or tetrahydropyridinyl-containing moiety attached to the 3-position of the 4-phenyl ring:
  • Q is selected from CH 2 , CHR 5 , CHR 13 , CR 13 R 13 , and CR 5 R 13 ;
  • R 1 and R 2 are independently selected from H, C ⁇ _ 8 alkyl, C 2 - 8 alkenyl, C 2 - 8 alkynyl, (CH 2 ) r c 3 - 6 cycloalkyl, and a
  • R 2 and R 3 join to form a 5, 6, or 7-membered ring substituted with 0-3 R a ;
  • R lla and R lla ' are selected from H, C ⁇ _ 6 alkyl, C 2 -8 alkenyl, C 2 -s alkynyl, a (CH 2 ) r -C3- ⁇ o carbocyclic residue substituted with 0-5 R lle , and a
  • R 15b is selected from C ⁇ _e alkyl, C 2 - 8 alkenyl, C 2 -8 alkynyl, a (CH 2 ) r -C 3 _ 6 carbocyclic residue substituted with 0-3 R 15e , and (CH 2 ) r ⁇ 5-6 membered heterocyclic system containing 1-4 heteroatoms selected from N, O, and S, substituted with 0-2 R 15e ;
  • R 15d at each occurrence, is selected from C 2 _ 8 alkenyl, C _s alkynyl, C ⁇ _ 6 alkyl substituted with 0-3 R 15e , a (CH 2 )r-C 3 _ ⁇ o carbocyclic residue substituted with 0-3 R 15e , and a (CH ) r 5-6 membered heterocyclic system containing 1-4 heteroatoms selected from N, O, and S, substituted with 0-3 R 15e ;
  • R 15e is selected from ⁇ -s alkyl, C 2 - 8 alkenyl, C 2 _ 8 alkynyl, (CH ) r C 3 _ 6 cycloalkyl, Cl, F, Br, I, CN, N0 2 , (CF 2 ) r CF 3 , (CH 2 ) r OC ⁇ _ 5 alkyl, OH, SH,
  • R 13d at each occurrence, is selected from H, C ⁇ _ 6 alkyl, and C 3 - 6 cycloalkyl;
  • R 16d is selected from C 1 - 6 alkyl and phenyl
  • R 16e at each occurrence, is selected from C ⁇ _ 6 alkyl, Cl, F, Br, I, CN, N0 2 , (CF 2 ) r CF 3 , OH, and (CH 2 ) r OCi- 5 alkyl; and
  • R 15e is selected from C - ⁇ alkyl, Cl,
  • the present invention provides novel compounds of formula (I) and pharmaceutically acceptable salt forms thereof, wherein the compound of formula I is selected from:
  • R 6d at each occurrence, is selected from H, C - 5 alkyl, and C 3 - 6 cycloalkyl;
  • R 11 and R 12 join to form C 3 - 7 cycloalkyl
  • J is selected from CH 2 and CHR 5 ;
  • L is selected from CH 2 and CHR 5 ;
  • R 15a and R 15a ' are selected from H, C ⁇ _g alkyl, C 3 _ 6 cycloalkyl, and (CH ) r phenyl substituted with 0-3 R 15e ;
  • R 15b at each occurrence, is selected from H, C ⁇ _ 6 alkyl,
  • R 15e is selected from C ⁇ _ 6 alkyl, Cl,
  • Z is selected from NR la , CHCN, CHN0 2 , and C(CN) 2 ;
  • R lla and R lla ' are selected from H, C _ 6 alkyl, C 2 - 8 alkenyl, C 2 -8 alkynyl, a (CH 2 ) r -C 3 - ⁇ o carbocyclic residue substituted with 0-5 R lle , and a (CH 2 )r-5-10 membered heterocyclic system containing 1-4 heteroatoms selected from N, 0, and S, substituted with 0-3 R lle ;
  • g is selected from 0, 1, 2, 3, and 4;
  • R 6 at each occurrence, is selected from C ⁇ _ 4 alkyl, C 2 _ 8 alkenyl, C 2 _ 8 alkynyl, (CH 2 ) r C 3 _g cycloalkyl, (CF 2 )rCF 3 , CN, (CH 2 ) r OH, (CH 2 ) r OR 6b , (CH 2 ) r C (0) R 6b ,
  • R 6c is selected from C ⁇ _ 6 alkyl, C 3 _g cycloalkyl, Cl, F, Br, I, CN, N0 2 , (CF 2 ) r CF 3 , (CH 2 ) r OC ⁇ _ 5 alkyl, (CH 2 ) r OH, (CH 2 ) r SC ⁇ - 5 alkyl, and (CH 2 ) r NR 6d R 6d ;
  • R 11 is selected from H, C ⁇ _g alkyl, (CH 2 ) r C 3 -g cycloalkyl, (CH 2 ) q OH, (CH 2 ) q OR ll , (CH 2 ) q NR lla R lla ', (CH 2 ) r C (0) R llb , (CH 2 ) r C(0)NR lla R ll ', (CH 2 ) q NR lla C(0)R lla , C _ 6 haloalkyl, (CH 2 ) r phenyl with 0-2 R ll , (CH 2 ) r -5-10 membered heterocyclic system containing 1-4 heteroatoms selected from N, 0, and S, substituted with 0-3 R 15 ;
  • the present invention provides novel compounds of formula (I) , wherein:
  • R 16 at each occurrence, is selected from C ⁇ _ ⁇ alkyl, (CH 2 ) r C 3 - 6 cycloalkyl, CF 3 , Cl, Br, I, F, (CH 2 ) r NR 16a R 16a ', N0 2 , CN, OH, (CH 2 ) r OR 16d ,
  • R 16f at each occurrence, is selected from H, and C ⁇ - 5 alkyl .
  • R 16f at each occurrence, is selected from H, and C ⁇ - 5 alkyl .
  • R 9 is selected from H, C ⁇ _ 6 alkyl, (CH 2 ) r C 3 -g cycloalkyl, F, Cl, CN, (CH 2 ) r OH, (CH 2 ) r OR 9d , (CH 2 ) r NR 9a R 9a ' , (CH 2 ) r OC(0)NHR 9 ⁇ (CH 2 ) r phenyl substituted with 0-5 R 9e , and a heterocyclic system substituted with 0-2 R 9e , wherein the heterocyclic system is selected from pyridyl, thiophenyl, furanyl, oxazolyl, and thiazolyl;
  • R 9a and R 9a ' are selected from H, C ⁇ _ 6 alkyl, C 3 _ 6 cycloalkyl, and (CH 2 ) r phenyl substituted with 0-3 R 9e ;
  • R 1 a and R 14 ' are selected from H, C _ 6 alkyl, C 3 _g cycloalkyl, and (CH 2 ) r Phenyl substituted with 0-3 R 14e , and a (CH 2 ) r -5-6 membered heterocyclic system containing 1-4 heteroatoms selected from N, O, and S, substituted with 0-2 R 15e ;
  • R 14 at each occurrence, is selected from C ⁇ _ 8 alkyl, (CH 2 ) r C 3 _ 6 cycloalkyl, CF 3 , Cl, Br, I, F,
  • R 14e at each occurrence, is selected from C ⁇ _g alkyl, Cl,
  • carbocycles include, but are not limited to, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl, adamantyl, cyclooctyl, ; [3.3.0]bicyclooctane, [4.3.0]bicyclononane, [4.4.0 ] bicyclodecane (decalin) , [2.2.2]bicyclooctane, fluorenyl, phenyl, naphthyl, indanyl, adamantyl, or tetrahydronaphthyl (tetralin) .
  • heterocycle or
  • Displacement of the SMe group with amines yields substituted guanidines 23 (see H. King and I. M. Tonkin J. Chem. Soc . 1946, 1063 and references therein) .
  • reaction of thiourea 21 with amines in the presence of triethanola ine and "lac sulfur" which facilitates the removal of H 2 S yields substituted guanidines 23 (K. Ramadas, Tet. Lett. 1996, 37, 5161 and references therein).
  • alcohol 55 or 58 may be tosylated, mesylated, triflated, or converted to a halogen by methods familiar to one skilled in the art to produce compound 59.
  • carbon homologs of 55 or 58 where OH can be (CH 2 ) r OH and it is also understood that these carbon homologs may have substituents on the methylene groups as well
  • a hydroxyl group may be converted to a bromide by CBr 4 and Ph 3 P (Takano, S. Heterocycles 1991, 32,
  • R 9 is either in its final form or in a suitable protected precursor form.
  • This electrophile can be a carbon-based electrophile, some examples being formaldehyde to introduce a CH 2 OH group, an aldehyde or a ketone which also introduces a one-carbon homologated alcohol, ethylene oxide (or other epoxides) which introduces a -CH 2 CH 2 OH group (a two-carbon homologated alcohol), an alkyl halide, etc., all of which can be later elaborated into R 9 .
  • It can also be an oxygen-based electrophile such as MCPBA, Davis' reagent (Davis, F. A. ; Haque, M.
  • amine 1 might have to be activated with Lewis acids in order to open the epoxide ring (Fujiwara, M. ; Imada, M.; Baba, A.; Matsuda, H. ; etrahedron Lett 1989, 30, 739; Caron, M. ; Sharpless, K. B.; J Org Chem 1985, 50, 1557) or 1 has to be deprotonated and used as a metal amide, for example the lithium amide (Gorzynski-Smith, J.; Synthesis 1984 (8), 629) or MgBr amide (Carre, M. C; Houmounou, J. P.; Caubere, P.; Tetrahedron Lett 1985, 26, 3107) or aluminum amide (Overman, L. E.; Flippin, L. A.; Tetrahedron Lett 1981, 22, 195).
  • Lewis acids for example the lithium amide (Gorzynski-Smith, J.; Synthesis 1984 (8), 629) or M

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

La présente invention concerne des modulateurs de CCR3, de formule (I), ou leurs sels pharmaceutiquement acceptables, utiles dans la prévention de l'asthme et d'autres maladies allergiques.
EP99964297A 1998-12-18 1999-12-17 N-ureidoalkyl-piperidines utilisees en tant que modulateurs de l'activite des recepteurs des chimiokines Withdrawn EP1140086A4 (fr)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US11271798P 1998-12-18 1998-12-18
US112717P 1998-12-18
US16124399P 1999-10-22 1999-10-22
US161243P 1999-10-22
PCT/US1999/030332 WO2000035451A1 (fr) 1998-12-18 1999-12-17 N-ureidoalkyl-piperidines utilisees en tant que modulateurs de l'activite des recepteurs des chimiokines

Publications (2)

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EP1140086A1 true EP1140086A1 (fr) 2001-10-10
EP1140086A4 EP1140086A4 (fr) 2002-04-03

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Country Link
EP (1) EP1140086A4 (fr)
AU (1) AU2057200A (fr)
CA (1) CA2350730A1 (fr)
WO (1) WO2000035451A1 (fr)

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EP1140086A4 (fr) 2002-04-03
WO2000035451A1 (fr) 2000-06-22
AU2057200A (en) 2000-07-03
CA2350730A1 (fr) 2000-06-22

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