LV12239B - Benzolsulfonamīda atvasinājumi kā cox-2 inhibitori - Google Patents

Benzolsulfonamīda atvasinājumi kā cox-2 inhibitori Download PDF

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Publication number
LV12239B
LV12239B LVP-98-215A LV980215A LV12239B LV 12239 B LV12239 B LV 12239B LV 980215 A LV980215 A LV 980215A LV 12239 B LV12239 B LV 12239B
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LV
Latvia
Prior art keywords
phenyl
sulfonyl
methyl
phenylisoxazol
group
Prior art date
Application number
LVP-98-215A
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English (en)
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LV12239A (lv
Inventor
John J. Talley
James W. Malecha
Stephen Bertenshaw
Matthew J. Graneto
Jeffery S. Carter
Jinglin Li
Srinivasan Nagarajan
David L. Brown
Jr. Donald J. Rogier
Thomas D. Penning
Ish K. Khanna
Xiangdong Zu
Richard M. Weier
Original Assignee
G.D.Searle & Co.
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Application filed by G.D.Searle & Co. filed Critical G.D.Searle & Co.
Publication of LV12239A publication Critical patent/LV12239A/lv
Publication of LV12239B publication Critical patent/LV12239B/lv

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    • C07D207/30—Heterocyclic 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 two double bonds between ring members or between ring members and non-ring members
    • C07D207/32—Heterocyclic 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 two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
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Claims (39)

1 LV 12239 Izgudrojuma formula 1. Savienojums ar formulu (I)
kurā: A ir ciklisks aizvietotājs no rindas: daļēji nepiesātināta heterocikliska grupa, heteroarilgrupa, cikloalkenilgrupa un arilgrupa, kur A ir neobligāti aizvietots aizvietošanai piemērotā vietā ar vienu vai vairākiem aizvietotājiem no rindas: alkiikarbonilgrupa, formiigrupa, halogēna atoms, alkiigrupa, haiogēnaikilgrupa, oksogrupa, ciāngrupa, nitrogrupa, karboksilgrupa, alkoksigrupa, aminokarbonilgrupa, alkoksikarbonilgrupa, karboksialkilgrupa, ciānalkilgrupa, hidroksiaikiigrupa, halogēnalkilsulfoniloksigrupa, alkoksialkiloksialkilgrupa, karboksialkoksialkiigrupa, cikloalkilalkil-grupa, alkenilgrupa, alkinilgrupa, heterocikliioksigrupa, alkiltio-grupa, cikloalkilgrupa, arilgrupa, heterocikliska grupa, cikloalkenilgrupa, aralkilgrupa, heterociklilakilgrupa, alkiltioalkilgrupa, aril-karbonilgrupa, aralkilkarbonilgrupa, aralkenilgrupa, alkoksialkil-grupa, ariitioalkilgrupa, ariloksialkiigrupa, aralkiltioalkilgrupa, aralkoksiaikilgrupa, aikoksikarbonilalkilgrupa, aminokarbonilalkil-grupa, alkilaminokarbonilgrupa, N-arilaminokarbonilgrupa, N-alkil-N-arilaminokarbonilgrupa, alkilaminokarbonilalkilgrupa, alkilamino-grupa, N-arilaminogrupa, N-aralkilaminogrupa, N-alkil-N-aralkil-aminogrupa, N-alkil-N-arilaminogrupa, aminoalkilgrupa, alkilamino-alkilgrupa, N-arilaminoalkilgrupa, N-aralkilaminoalkilgrupa, N-alkil-N-aralkilaminoalkilgrupa, N-alkil-N-arilaminoalkilgrupa, ariioksi-grupa, aralkoksigrupa, ariltiogrupa, aralkiltiogrupa, alkilsulfinilgrupa, alkilsulfonilgrupa, aminosulfonilgrupa, alkilaminosulfonilgrupa, N-
2 I arilaminosulfonilgrupa, arilsulfonilgrupa un N-alkil-N-arilaminosulfonilgrupa; R1 ir ņemts no rindas: heterocikliska grupa, cikloalkilgrupa, cikloalkenilgrupa, arilgrupa, kur R1 ir neobligāti aizvietots aizvietošanai piemērotā vietā ar vienu vai vairākiem aizvietotājiem no rindas: alkilgrupa, halogēnalkilgrupa, ciāngrupa, karboksilgrupa, alkoksi-karbonilgrupa, hidroksilgrupa, hidroksialkilgrupa, halogēnalkoksi-grupa, aminogrupa, alkiiaminogrupa, arilaminogrupa, nitrogrupa, alkoksialkilgrupa, alkilsulfinilgrupa, halogēna atoms, alkoksigrupa un alkiltiogrupa; R1 ir ūdeņraža atoms vai alkoksikarboniialkilgrupa; R2 ir ņemts no rindas: alkilgrupa, karboksialkilgrupa, acilgrupa, alkoksi-karbonilgrupa, heteroarilkarbonilgrupa, alkoksikarbonilalkilkarbonilgrupa, alkoksikarbonilkarbonilgrupa, aminoskābes atlikums un alkilkarbonil-aminoalkilkarboniigrupa; ar noteikumu, ka A nav tetrazolija vai piridīnija grupa, kā arī A nav indanona grupa, ja R2 ir alkilgrupa vai karboksialkilgrupa, kā arī A nav tienilgrupa, ja R1 ir 4-fluorfenilgrupa, ja R1 ir ūdeņraža atoms un ja R2 ir metilgrupa vai acetilgrupa, kā arī minētā savienojuma farmaceitiski pieņemama sāls. 1 Savienojums pēc 1. punkta, kurā: 2 A ir ņemts no rindas: daļēji nepiesātināta heterocikliska grupa, 5 vai 6 locekļu heteroarilgrupa, C3.8cikloalkenilgrupa un fenilgrupa, kur A ir neobligāti aizvietots aizvietošanai piemērotā vietā ar vienu vai vairākiem aizvietotājiem no rindas: formilgrupa, C-Moalkilkarbonilgrupa, halogēna atoms, C-Moalkilgrupa, C-i-ehalogēnalkilgrupa, oksogrupa, ciāngrupa, nitrogrupa, karboksilgrupa, Ci-ealkoksigrupa, aminokarbonil-grupa, Ci^alkoksikarbonilgrupa, C-Mokarboksialkiigrupa, C-Mociānalkil-grupa, C-i^hidroksialkilgrupa, C-i-6halogēnalkilsulfoniloksigrupa, C-t-ioalk-oksialkiloksialkilgrupa, karboksi-C-Moalkoksialkilgrupa, C3.8cikloalkilalkil-grupa, C2-6alkenilgrupa, C2-6alkinilgrupa, heterocikliloksigrupa, Ci^alkiltio-grupa, C3_8cikloalkilgrupa, fenilgrupa, 5 vai 6 locekļu heterocikliska grupa, C4.8cikloalkenilgrupa, fenil-C-M0alkilgrupa, 5 vai 6 locekļu heterociklil-alkilgrupa, Ci^alkiltioalkilgrupa, fenilkarbonilgrupa, fenil-C-Moalkilkarbonil-grupa, fenil-C2^alkeniigrupa, C-Moalkoksialkilgrupa, feniltio-Ci.i0alkil-grupa, fenoksi-Ci.i0alkilgrupa, fenil-Ci^alkiltioalkilgrupa, fenil-Ci_6alkoksi-alkilgrupa, Ci^alkoksikarbonilalkilgrupa, aminokarbonil-Ci-ioalkilgrupa, Ci. 6alkilaminokarbonilgrupa, N-fenilaminokarbonilgrupa, N-Ci-§alkil-N-fenil-aminokarbonilgrupa, Ci^alkilaminokarbonilalkilgrupa, Ci^alkilamino-grupa, N-fenilaminogrupa, N-fenil-Ci-ealkilaminogrupa, N-Ci^alkil-N-fenil-alkilaminogrupa, N-Ci-ealkil-N-fenilaminogrupa, C-Moaminoalkilgrupa, C^alkil-aminoalkilgrupa, N-fenilamino-C-Moalkilgrupa, N-fenil-Ci^alkil-aminoalkilgrupa, NA^alkil-N-fenilalkilaminoalkilgrupa, N-Cļ-ealkil-N-fenil-aminoalkilgrupa, fenoksigrupa, fenil-C-i^alkoksigrupa, feniltiogrupa, fenil- 3 LV 12239 Ci-i0alkiltio-grupat Ci^alkilsulfinilgrupa, Cļ^alkilsulfonilgrupa, amino-sulfonilgrupa, Ci^alkilaminosulfonilgrupa, N-fenilaminosulfonilgrupa, fenilsulfonilgrupa, N-Ci^alki!-N-fenilaminosulfonilgrupa; R1 ir ņemts no rindas: 5 vai 6 locekļu heterocikliska grupa, C^ciklo-alkiigrupa, C^scikloalkenilgrupa, fenilgrupa, kur R1 ir neobligāti aizvietots aizvietošanai piemērotā vietā ar vienu vai vairākiem aizvietotājiem no rindas: Ci-ioalkil-grupa, Ci-ehalogēnalkilgrupa, ciāngrupa, karboksilgrupa, C-i-ealkoksikarbonilgrupa, hidroksilgrupa, C-i-ehidroksialkilgrupa, Ci^halogēnalkoksigrupa, aminogrupa, C-i^alkilaminogrupa, fenil-aminogrupa, nitrogrupa, C-Moalkoksialkilgrupa, Ci^alkilsulfinil-grupa, halogēna atoms, Ci^alkoksigrupa, Ci^alkiltiogrupa; R2 ir ūdeņraža atoms vai Ci-6alkoksikarbonilalkilgrupa; R3 ir ņemts no rindas: C-Moalkilgrupa, karboksi-Ci.i0alkilgrupa, alkanoilgrupa, aroilgrupa, aminoskābes atlikums, Ci^alkoksikarbonilgrupa, Ci.10alkoksi-alkilkarbonilgrupa, (5 vai 6 locekļu heterocikliska grupa)-CO-, Ci^alkil-karbonilaminoalkilkarbonilgrupa, vai minētā savienojuma farmaceitiski pieņemama sāls.
3. Savienojums pēc 2. punkta, kurā: A ir aizvietotājs no rindas: tienilgrupa, oksazolilgrupa, furanilgrupa, pirolilgrupa, tiazolilgrupa, imidazolilgrupa, benzofuranilgrupa, indenil-grupa, benzotienilgrupa, izoksazoliigrupa, pirazolilgrupa, ciklopenteni-Igrupa, ciklopentadienilgrupa, benzindazolilgrupa, benzopiranopirazolil-grupa, fenilgrupa, piridinilgrupa, kur A ir neobligāti aizvietots aizvietošanai piemērotā vietā ar vienu vai vairākiem aizvietotājiem no rindas: formilgrupa, metilkarbonilgrupa, fluora atoms, hlora atoms, broma atoms, metilgrupa, trifluormetilgrupa, difluormetilgrupa, oksogrupa, ciāngrupa, karboksilgrupa, metoksigrupa, aminokarbonilgrupa, metoksikarbonilgrupa, etoksikarbonilgrupa, karboksipropilgrupa, oksimetilgrupa, ciānmetilgrupa, fenilgrupa, fenilmetilgrupa, metoksikarbonilgrupa, fenilkarbonilgrupa, metoksimetilgrupa, fenoksimetilgrupa, aminokarbonilmetilgrupa, karboksimetilgrupa, fenoksigrupa; R1 ir ņemts no rindas: tienilgrupa, oksazolilgrupa, izoksazoliigrupa, furanil grupa, tiazolilgrupa, piridinilgrupa, fenilgrupa, kur R1 ir neobligāti aizvietots aizvietošanai piemērotā vietā ar vienu vai vairākiem aizvietotājiem no rindas: metilgrupa, trifluormetilgrupa, hidroksilgrupa, oksimetilgrupa, trifluormetoksigrupa, nitrogrupa, metoksimetilgrupa, fluora atoms, hlora atoms, broma atoms, metoksigrupa, metiltiogrupa; R2 ir ūdeņraža atoms vai etoksikarbonilmetiigrupa; R3 ir ņemts no rindas: metilgrupa, karboksimetilgrupa, formilgrupa, metil karbonilgrupa, etilkarbonilgrupa, propilkarbonilgrupa, izopropilkarbonil- 4 I grupa, butilkarbonilgrupa, terc-butilkarbonilgrupa, pentilkarbonilgrupa, hidroksietilkarbonilgrupa, benzilkarbonilgrupa, fenil(hidroksilgrupa)metil-karbonilgrupa, metoksikarbonilgrupa, terc-butoksikarbonilgrupa, metoksi-etilkarbonilgrupa, etoksimetilkarbonilgrupa, metoksimetilkarbonilgrupa, fenilkarbonilgrupa, karboksietilkarbonilgrupa, karboksimetilkarbonilgrupa, karboksi[1,2-bis(hidroksi)etil]karbonilgrupa, metoksikarbonilmetilkarbonil-grupa, metoksikarboniletilkarbonilgrupa, metoksikarbonilkarbonilgrupa, aminometilkarbonilgrupa, terc-butoksikarbonilaminometilkarbonilgrupa, metilkarbonilaminometilkarbonilgrupa, vai minētā savienojuma farmaceitiski pieņemama sāls.
4. Savienojums pēc 3. punkta, kas ņemts no savienojumu un to farmaceitiski pieņemamo sāļu rindas: N-({4-[3-difluormetil-5-(3-fluor-4-metoksifenil)-1H-pirazol-1-i!]fenil}sulfonil)propān- amTds; N-({4-[3-difluormetil-5-(3-fluor-4-metoksifenil)-1H-pirazol-1-il]fenil}sulfonil)butān- amīds; N-({4-[(1,5-dimetil)-3-fenil-1H-pirazol-4-il]fenil}sulfonil)acetamīds; N-({4-[2-(3-piridinil)-4-trifluormetil-1H-imidazol-1-il]fenil}sulfonil)acetamīds; N-({4-[2-(5-metilpiridin-3-il)-4-trifluormetil-1H-imidazol-1-il]fenil}sulfonil)acet- amīds; N-({4-[2-(2-metiipiridin-3-il)-4-trifIuormetil-1H-imidazol-1-il]fenii}sulfonil)acet- amīds; N-({4-[2-(5-metilpiridin-3-il)-4-trifluormetil-1H-imidazol-1-il]fenil}sulfonil)butān- amīds; N-({4-[2-(2-metilpiridin-3-il)-4-trifluormetil-1H-imidazol-1-il]fenil}sulfonil)butān- amīds; N-({4-[2-(3-hlor-5-metilfenil)-4-trifluormetil-1H-imidazol-1-ii]fenii}sulfonil)acet- amīds; N-({4-[3-(3-fluorfenil)-5-metilizoksazol-4-ii]fenil}sulfonil)acetamīds; 2- metil-N-{[4-{5-metil-3'fenilizoksazol-4-il]fenil}sulfonil)propānamīds; N-{[4-(5-metil-3-fenilizoksazol-4-il]fenil}sulfonil)propānamTds; N-{[4-(5-metil-3-fenilizoksazol-4-il]fenil}sulfonil)benzamīds; 2,2-dimetil-N-{[4-(5-metil-3-fenilizoksazol-4-il]fenil}sulfonil)propānamīds; N-{[4-(5-metil-3-fenilizoksazol-4-il]fenil}sulfonil)butānamīds; N-{[4-(5-metil-3-fenilizoksazol-4-il]fenil}sulfonil)pentānamīds; N-{[4-(5-metil-3-fenilizoksazol-4-il]fenil}sulfonil)heksānamīds; 3- metoksi-N-{[4-(5-metil-3-fenilizoksazol-4-il]fenH}sulfonil)propānamīds; 2-etoksi-N-{[4-(5-metil-3-fenilizoksazol-4-il]fenil}sulfonil)propānam7ds; N-{[4-(5-metil-3-fenilizoksazol-4-il]fenil}sulfonil)acetamīds; N-({4-[5-(4-hlorfenil)-3-trifluormetil-1H-pirazol-1-il]fenil}sulfonil)propānamīds; N-({4-[5-(4-hlorfenil)-3-trifluormetil-1H-pirazol-1-il]fenil}sulfonil)butānamīds; N-({4-[5-(4-hlorfenil)-3-trifluormetil-1H-pirazol-1-il]fenil}sulfonil)acetamTds; 5 LV 12239 N-{[4-(3-difIuormetil-6-fIuor-1,5-dihidro-7-metoksi[2]benzoiiopirano[4,3-c]pirazol-1 -il)fenil]sulfonil}acetamīds; N-{[4-(6-fIuor-1t5-ciihidro-7-metoksi-3-trifluonnetii[2]benzotiopirano[4,3-c]pirazol-1 -il)fenil]sulfonil}acetarnīds; N-({4-[3-difluormetiI-5-(3-fiuor-4-metoksifenil)-1H-pirazol-1-il]fenil}sulfonil)acet- amīds; N-{[4-(2-metil-4-feniloksazol-5-il]feniI}sulfonii)acetamīds; ({[4-(5-meĪil-3-fenilizoksazol-4-i!)fenil]sulfonil}amino)oksoetiķskābes metilesteris; 2-metoksi-N~{[4-(5-metil-3-fenilizoksazol-4-il]fenil}sulfonil)acetamīds; N-{[4-(5-difIūOimetil-3-fenilizoksazol-4-il]fenii}suIfonil)propānamīds; N-{[4-(5-difIuormetil-3-feniIizoksazol-4-iI]fenil}sulfoniI)butānamīds; 4-({[4-(5-metil-3-fenilizoksazoi-4-iI)feniI]sulfonil}amino)-4-oksobutānskābe; N-{[4-{5-metil-3-feniiizoksazol-4-il]fenil}sūlfonil)formamTds; N-{[4-(5-metil-3-fenilizoksazol-4-il]fenil}sulfonil)karbamTnskābes 1, 1-dimetiletil- esteris; N-{[4-(5-metil-3-fenilizoksazol-4-il]fenil}sulfoniI)glicTns; 2-amino-N-{[4-{5-metii-3-fenilizoksazol-4-il]fenil}sulfonil)acetamTds; 2- acetilamino-N-{[4-(5-metil-3-fenilizoksazol-4-{l]fenii}sulfonil)acetamTds; 4-({[4-(5-metil-3-fenilizoksazol-4-il)fenii]sulfonil}amino)-4-oksobutānskābes metilesteris; N-{[4-(5-metil-3-fenilizoksazol-4-il]fenil}sulfonil)karbamīnskābes metilesteris; N-acetil-N-{[4-(5-metil-3-fenilizoksazol-4-il]fenil}sulfonil)glicīna etilesteris; N-({4-[5-(4-metilfenil)-3-trifluormetil-1H-pirazol-1-il]fenil}sulfonil)acetamīds; 3- ({[4-{5-metil-3-fenilizoksazol-4-il)fenil]sulfonil}amino)-3-oksopropānskābes metilesteris; 4- [5-(3-brom-5-fluor-4-metoksifenil)-2-(trifluormetil)oksazol-4-il]-N-metilbenzol-sulfonamīds; N-(1,1-dimetiletil)-4-(5-metil-3-fenilizoksazol-4-il]benzolsulfonamīds; 4-[5-(4-fIuorfenil)-3-{trifluormetil)-1H-pirazol-1-il]-N-metilbenzolsulfonamīds; N-metil-4-(5-metil-3-fenilizoksazol-4-il]benzolsulfonamīds; N-{[4-(5-oksimetil-3-feniloksazol-4-il]fenil}sulfonii)acetamīds; N-{[4-(5-acetoksimetil-3-feniloksazol-4-il]fenil}sulfonil)acetamTds; N-[2-({[4-(5-metil-3-feniiizoksazol-4-il)fenil]sulfonil}amino)-2-oksoetil]karbamīn- skābes 1,1 -dimetiletilesteris; N-({4-[2-(3-hlor-4-fluorfenii)ciklopenten-1-il]fenii}sulfonil)acetamTds; 4-[2-(4-fluorfenii)-1 H-pirol-1 -il]-N-metilbenzolsulfonamīds; N-{[4-(3)4-dimetil-1-fenil-1H-pirazol-5-ii)fenil]sulfonil}propānamTds; N-({4-[2-(2-metiIpiridin-3-il)-4-(trifluormetil)imidazol-1-il]fenil}sulfonil)propānamīds; 4-[2-(4-fluorfenil)ciklopenten-1-il]-N-metilbenzolsulfonamTds; N-{[4-(3-fenil-2,3-dihidro-2-oksofuran-4-il)fenil]sulfonil}propānamīds. 6
5. Savienojums ar formulu (II)
kurā: A ir cikla aizvietotājs, kas ņemts no rindas: daļēji nepiesātināta heterocikliska grupa, 5 vai 6 locekļu heteroarilgrupa, C^cikloalkenilgrupa un fenilgrupa, kur A ir neobligāti aizvietots aizvietošanai piemērotā vietā ar vienu vai vairākiem aizvietotājiem no rindas: aciigrupa, halogēna atoms, hidroksilgrupa, C-Moalkilgrupa, Ci^halo-gēnaikiigrupa, oksogrupa, ciāngrupa, nitrogrupa, karboksilgrupa, Ci^alkoksigrupa, aminokarbonilgrupa, Ci^alkoksikarbonilgrupa, karboksi-C-Moalkilgrupa, C-Modānalkilgrupa, C-i-ehidroksialkilgrupa, Ci.ioalkilkarboniloksialkiigrupa, fenilgrupa; R4 ir ņemts no rindas: heterocikliska grupa, cikloalkilgrupa, cikloalkeniigrupa, fenilgrupa, kur R4 ir neobligāti aizvietots aizvietošanai piemērotā vietā ar vienu vai vairākiem aizvietotājiem no rindas: Ci-ioalkilgrupa, Ci^halogēnalkilgrupa, ciāngrupa, karboksilgrupa, C-i-ealkoksikarbonilgrupa, hidroksilgrupa, Ci^hidroksialkilgrupa, Ci^halogēnalkoksigrupa, aminogrupa, Ci^alkilaminogrupa, fenil-aminogrupa, nitrogrupa, C-Moalkoksialkiigrupa, Cļ^alkilsulfinilgrupa, halogēna atoms, Ci^alkoksigrupa, Cļ^alkiltiogrupa; R5 ir ņemts no rindas: ūdeņraža atoms, C-Moalkilgrupa, C-Moaikoksigrupa, CMoalkoksialkiigrupa, fenilgrupa, arii-C-Moalkilgrupa, karboksi-C-M0alkiI-grupa, Ci^alkoksikarbonilalkilgrupa, Ci^alkoksikarbonilgrupa, amino-Ci-ioalkilgrupa, Ci^alkoksikarbonilaminoaikilgrupa,Ci-ioalkilkarbonilamino-alkilgrupa, ar noteikumu, ka A nav tetrazolija vai piridīnija grupa, kā arī A nav tienilgrupa, ja R4 ir 4-fluorfenilgrupa, ja R5 ir metilgrupa, kā arī minētā savienojuma farmaceitiski pieņemama sāls.
6. Savienojums pēc 5. punkta, kurā: A ir cikliska grupa no rindas: tienilgrupa, oksazolilgrupa, furanilgrupa, pirolilgrupa, tiazolilgrupa, imidazolilgrupa, benzofuranilgrupa, indenilgrupa, benzotieniigrupa, izoksazolilgrupa, pirazolilgrupa, ciklopentenilgrupa, ciklopentadienilgrupa, benzindazolilgrupa, benzopiranopirazolilgrupa, fenilgrupa, piridinilgrupa, kur A ir neobligāti aizvietots aizvietošanai piemērotā vietā ar vienu vai vairākiem aizvietotājiem no rindas: 7 LV 12239 acilgrupa, halogēna atoms, hidroksilgrupa, C-Moalkilgrupa, Ci^halo-gēnalkilgrupa, oksogrupa, ciāngrupa, nitrogrupa, karboksilgrupa, Ci-6alkoksigrupa, aminokarbonilgrupa, Ci.6alkoksikarbonilgrupa, karboksi-Ci.i0alkilgrupa, Ci-i0ciānalkilgrupa, Ci.i0alkilkarboniloksi-alkilgrupa, fenilgrupa, Ci^hidroksialkilgrupa; R4 ir ņemts no rindas: 5 vai 6 locekļu heterocikliska grupa, fenilgrupa, kur R4 ir neobligāti aizvietots aizvietošanai piemērotā vietā ar vienu vai vairākiem aizvietotājiem no rindas: Ci-ioalkilgrupa, Ci.6halogēnalkilgrupa, ciāngrupa, karbonilgrupa, Ci-ealkoksikarbonilgrupa, hidroksilgrupa, Ci-ehidroksialkilgrupa, Ci^halogēnalkoksigrupa, aminogrupa, Ci^alkilaminogrupa, fenii-aminogrupa, nitrogrupa, Ci-ioalkoksialkilgrupa, Ci^alkilsulfinilgrupa, halogēna atoms, Ci.6alkoksigrupa, C-t-ealkiltiogrupa; R5 ir ņemts no rindas: ūdeņraža atoms, Ci.i0alkilgrupa, Ci-6alkoksigrupa, Ci-ioalkoksialkilgrupa, fenilgrupa, Ci-6alkoksikarbonilalkilgrupa, Ci-6alk-oksikarbonilgrupa, amino-Ci-ioalkilgrupa, Cļ-ealkoksikarbonilaminoalkil-grupa, Ci-ioalkiikarbonilaminoalkilgrupa, vai minētā savienojuma farmaceitiski pieņemama sāls.
7. Savienojums pēc 6. punkta, kurā: A ir ciklisks aizvietotājs no rindas: tienilgrupa, oksazolilgrupa, furanilgrupa, pirolilgrupa, tiazolilgrupa, imidazolilgrupa, izotiazolilgrupa, izoksazolil-grupa, pirazolilgrupa, ciklopentenilgrupa, ciklopentadienilgrupa, benz-indazolilgrupa, benzopiranopirazolilgrupa, fenilgrupa, piridinilgrupa, kur A ir neobligāti aizvietots aizvietošanai piemērotā vietā ar vienu vai vairākiem aizvietotājiem no rindas: formilgrupa, fluora atoms, hlora atoms, broma atoms, metilgrupa, trifluormetilgrupa, oksogrupa, ciāngrupa, karboksilgrupa, metoksi-grupa, aminokarbonilgrupa, metoksikarbonilgrupa, etoksikarbonil-grupa, karboksimetilgrupa, karboksipropilgrupa, metilkarboniloksi-metilgrupa, oksimetilgrupa; R4 ir ņemts no rindas: tienilgrupa, piridinilgrupa, fenilgrupa, kur R4 ir neobligāti aizvietots aizvietošanai piemērotā vietā ar vienu vai vairākiem aizvietotājiem no rindas: metilgrupa, trifluormetilgrupa, hidroksilgrupa, oksimetilgrupa, trifluormetoksigrupa, nitrogrupa, metoksimetilgrupa, fluora atoms, hlora atoms, broma atoms, metoksigrupa, metiltiogrupa; R5 ir ņemts no rindas: ūdeņraža atoms, metilgrupa, etilgrupa, izopropilgrupa, propilgrupa, terc-butilgrupa, butilgrupa, pentilgrupa, metoksigrupa, terc-butoksigrupa, metoksietilgrupa, etoksimetilgrupa, metoksimetilgrupa, fenilgrupa, karboksietilgrupa, metoksikarbonilmetilgrupa, metoksikarboni-letilgrupa, terc-butoksikarbonilaminometilgrupa, metoksikarbonilgrupa, aminometilgrupa, metil karbonilaminometiigrupa, vai minētā savienojuma farmaceitiski pieņemama sāls. 8 I
8. Savienojums pēc 7. punkta, kas ņemts no savienojumu un to farmaceitiski pieņemamo sāļu rindas: N-({4-[3-difluormetil-5-(3-fluor-4-metoksifenil)-1H-pirazol-1-ii]fenil}sulfonil)propān- amīds; N-({4-[3-difluormetil-5-(3-fIuor-4-metoksifenil)-1 H-pirazol-1-il]fenil}sulfonil)butān-amīds; N-{4-(1,5-dimetii-3-fenil-1 H-pirazol-1-il)fenii]suifonīi}acetamīds; N-({4-[2-(3-piridinil)-4-trifiuormetil-1H-imidazol-1-il]fenil}sulfonil)acetam7ds; N-({4-[2-(5-metilpiridin-3-il)-4-trifluormetil-1H-imidazol-1-il]fenil}sulfonil)-acetamīds; N-({4-[2-(2-metilpiridin-3-il)-4-trifluormetil-1H-imidazol-1-il]fenil}sulfonil)- acetamīds; N-({4-[2-(5-metilpiridin-3-il)-4-trifluormetil-1H-imidazol-1-il]fenil}sulfonil)- butānamīds; N-({4-[2-(2-metilpiridin-3-il)-4-trifluormetil-1 H-imidazol-1-īlļfeniljsulfonil)-butānamīds; N-({4-[2-(3-hlor-5-metilfenil)-4-trifiuormetil-1H-imidazol-1-il]fenil}sulfonil)- acetamīds; N-({4-[3-(3-fIuorfenil)-5-metilizoksazol-4-il]fenil}sulfonil)acetamīds; 2- metii-N-{[4-(5-metil-3-fenilizoksazol-4-il)fenil]sulfonil}propānamīds; N-{[4-(5-metil-3-fenilizoksazol-4-il)fenil]sulfoniI}propānamīds; N-{[4-(5-metil-3-fenilizoksazol-4-ii)feniljsulfonii}benzamīds; 212-dimetil-N-{[4-(5-metil-3-fenilizoksazol-4-ii)fenil]sulfonil}propānamīds; N-{[4-(5-metil-3-feniiizoksazol-4-il)fenil]sulfonil}butānamīds; N-{[4-(5-metii-3-fenilizoksazol-4-il)fenii]sulfonii}pentānamīds; N-{[4-(5-metil-3-feniiizoksazol-4-il)fenil]suifonil}heksānamTds; 3- metoksi-N-{[4-(5-metil-3-fenilizoksazol-4-il)fenil]sulfonil}propānamTds; 2-etoksi-N-{[4-(5-metil-3-fenilizoksazol-4-il)fenii]suifonil}acetamTds; N-{[4-(5-metil-3-fenilizoksazol-4-il)fenil]sulfonil}acetamīds; N-({4-[5-(4-hlorfenil)-3-trifluormetil 1 H-pirazol-1 -il]fenil}sulfonil)propānamīds; N-({4-[5-(4-hiorfenil)-3-trifiuormetil 1 H-pirazoi-1 -il]fenii}sulfonil)butānamīds; N-({4-[5-(4-hlorfenil)-3-trifIuormetil 1 H-pirazol-1 -il]fenil}sulfonil)acetam7ds; N-{[4-(3-difluormetil-6-fluor-1(5-dihidro-7-metoksi[2]benzotiopirano[4l3-c]pirazol-1 -il)fenil]sulfonil}acetamīds; N-{[4-(6-fluor-1,5-dihidro-7-metoksi-3-trifluormetil-[2]benzotiopirano[4,3-c]pirazol-1 -il)fenil]sulfonil}acetamīds; N-({4-[3-difiuormetil-5-(3-fluor-4-metoksifenil)-1H-pirazol-1-il]fenil}sulfonil)acet- amīds; N-{[4-(2-metil-4-feniloksazol-5-il]fenii}sulfonil)acetam7ds; ({[4-(5-metil-3-fenilizoksazol-4-il)fenil]sulfonil}amino)oksoetiķskābes metiiesteris; 2-metoksi-N-{[4-(5-metil-3-fenilizoksazol-4-il]fenil}sulfonil)acetam7ds; N-{[4-(5-difluormetil-3-fenilizoksazol-4-il]fenil}sulfonil)propānamīds; N-{[4-(5-difluormetil-3-fenilizoksazol-4-il]fenii}sulfonil)butānam7ds; 4_({[4-(5-metil-3-fenilizoksazol-4-il)fenii]sulfonil}amino)-4-oksobutānskābe; N-{[4-(5-metil-3-fenilizoksazol-4-il]fenil}sulfonil)formam7ds; 9 LV 12239 N-{[4-(5-metil-3-fenilizoksazol-4-il]fenil}sulfonil)karbamīnskābes 1,1-dimetiletil-esteris; N-{[4-(5-m etil-3-fen i I izoksazo l-4-i l]fen i l}su Ifon il )g I icīns; 2-amino-N-{[4-(5-metil-3-fenilizoksazol-4-il]fenil}sulfonil)acetam7ds; 2- acetilamino-N-{[4-(5-metil-3-fenilizoksazol-4-il]fenil}sulfonil)acetamīds; 4-({[4-(5-metil-3-fenilizoksazol-4-il)fenil]sulfonil}amino)-4-oksobutānskābes metilesteris; N-{[4-(5-metil-3-fenilizoksazol-4-il]fenil}sulfonil)karbamīnskābes metilesteris; N-({4-[5-(4-metilfenil)-3-trifluormetil-1H-pirazol-1-il]fenil}sulfonil)acetamīds; 3- ({[4-(5-metil-3-fenilizoksazol-4-il)fenil]sulfonil}amino)-3-oksopropānskābes metilesteris; N-{[4-(5-oksimetil-3-feniloksazol-4-il]fenil}sulfonil)acetamīds; N-{[4-(5-acetoksimetil-3-feniloksazol-4-il]fenil}sulfonil)acetamīds; N-[2-({[4-(5-metil-3-fenilizoksazol-4-il)fenil]sulfonil}amino)-2-oksoetil]karbamīn-skābes 1,1 -dimetiletilesteris; N-{[4-(3,4-dimetil-1-fenil-1H-pirazol-5-il)fenil]sulfonil}propānamīds; N-({4-[2-(2-metilpiridin-3-il)-4-(trifluormetil)imidazol-1-il]fenil}sulfonil)- propānamīds; N-({4-[2-(3-hlor-4-fluorfeniI)ciklopenten-1-il]fenil}sulfonil)acetamTds; N-{[4-(3-fenil-2,3-dihidro-2-oksofuran-4-il)fenil]sulfonil}propānamīds.
9. Savienojums pēc 5. punkta, kura farmaceitiski pieņemamās sālis ir metālu sālis.
10. Savienojums pēc 9. Punkta, kura farmaceitiski pieņemamās sālis ir sārmmetālu vai sārmzemju metālu sālis.
11. Savienojums pēc 10. punkta, kura farmaceitiski pieņemamās sālis ir nātrija vai kālija sālis.
12. Savienojums pēc 11. punkta, kas ņemts no savienojumu un to farmaceitiski pieņemamo sāļu rindas: N-({4-[3-difluormetil-5-(3-fluor-4-metoksifenil)-1H-pirazol-1-il]fenil}sulfonil)propān-amīda nātrija sāls; N-({4-[3“difluormetil-5-(3-fluor-4-metoksifenil)-1H-pirazol-1-il]fenil}sulfonil)butān-amīda nātrija sāls; N-{4-(1,5-dimetii-3-fenil-1 H-pirazol-1-il)fenil]sulfonil}acetamīda nātrija sāls; N-({4-[2-(3-piridinil)-4-trifluormetil-1H-imidazol-1-il]fenil}sulfonil)acetamīda nātrija sāls; N-({4-[2-(5-metilpiridin-3-il)-4-trifluormetil-1H-imidazol-1-il]fenil}sulfonil)acetamīda nātrija sāls; N-({4-[2-(2-metilpiridin-3-il)-4-trifluormetil-1H-imidazol-1-il]fenil}sulfonil)acetamīda nātrija sāls; N-({4-[2-(5-metilpiridin-3-il)-4-trifluormetil-1H-imidazol-1-il]fenil}sulfonil)butān-amīda nātrija sāls; 10 I N-({4-[2-(2-metilpiridin-3-il)-4-trifluormetil-1H-imidazol-1-il]fenil}sulfonil)butān-amlda nātrija sāls; N-({4-[2-(3-hlor-5-metilfenil)-4-trifluormetil-1H-imidazol-1-il]fenil}sulfonil)acet-amīda nātrija sāls; N-({4-[3-(3-fluorfenil)-5-metilizoksazol-4-il]fenil}sulfonil)acetamīda nātrija sāls; 2- metil-N-{[4-(5-metil-3-feniiizoksazol-4-il)fenil]sulfonil}propānamīda nātrija sāls; N-{[4-(5-metil-3-fenilizoksazol-4-il)fenil]sulfonil}propānamīda nātrija sāls; N-{[4-(5-metii-3-fenilizoksazol-4-il)fenil]sulfonil}benzamīda nātrija sāls; 2,2-dimetil-N-{[4-(5-metil-3-fenilizoksazol-4-il)fenil]sulfonil}propānamīda nātrija sāls; N-{[4-(5-metil-3-fenilizoksazol-4-il)fenil]sulfonil}butānam7da nātrija sāls; N-{[4-(5-metil-3-fenilizoksazol-4-ii)fenil]sulfonil}pentānamTda nātrija sāls; N-{[4-(5-metil-3-fenilizoksazol-4-il)fenil]sulfonil}heksānamTda nātrija sāls; 3- metoksi-N-{[4-(5-metil-3-fenilizoksazol-4-il)fenil]sulfonil}propānamīda nātrija sāls; 2-etoksi-N-{[4-(5-metil-3-fenilizoksazol-4-il)fenil]sulfonil}acetamīda nātrija sāls; N-{[4-(5-metil-3-fenilizoksazol-4-il)fenil]sulfonil}acetam7da nātrija sāls; N-{[4-(5-metil-3-fenilizoksazol-4-il)fenil]sulfonil}acetamīda kālija sāls; N-({4-[5-(4-hlorfenil)-3-trifluormetil-1H-pirazol-1-il]fenil}sulfonil)propānamīda nātrija sāls; N-({4-[5-(4-hlorfenil)-3-trifluormeti-1H-pirazol-1-il]fenil}sulfonil)butānamīda nātrija sāls; N-({4-[5-(4-hlorfenil)-3-trifluormetil-1 H-pirazol-1 -il]fenil}sulfonil)acetamīda nātrija sāls; N-{[4-(3-difluormetil-6-fIuor-1t5-dihidro-7-metoksi[2]benzotiopirano[4,3-c]pirazol-1-il)fenilļsulfonil}acetamīda nātrija sāls; N-{[4-(6-fluor-1,5-dihidro-7-metoksi-3-trifluormetil-[2]benzotiopirano[4,3-c]pirazol- 1- il)fenil]sulfonil}acetamīda nātrija sāls; N-({4-[3-difluormetil-5-(3-fluor-4-metoksifenil)-1H-pirazol-1-il]fenil}sulfonil)acet-amīda nātrija sāls; N-{[4-(2-metil-4-feniloksazol-5-il]fenil}sulfonil)acetamīda nātrija sāls; ({[4-(5-metil-3-fenilizoksazol-4-il)fenil]sulfonil}amino)oksoetiķskābes metilestera nātrija sāls; 2- metoksi-N-{[4-(5-metil-3-fenilizoksazol-4-il]fenil}sulfonil)acetamīda nātrija sāls; N-{[4-(5-difluormetil-3-fenilizoksazol-4-il]fenil}sulfonil)propānamīda nātrija sāls; N-{[4-(5-difluormetil-3-fenilizoksazol-4-il]fenil}sulfonil)butānamīda nātrija sāls; 4- ({[4-(5-metil-3-fenilizoksazol-4-il)fenil]sulfonil}amino)-4-oksobutānskābes nātrija sāls; N-{[4-(5-metil-3-fenilizoksazol-4-il]fenil}sulfonil)formamīda nātrija sāls; N-{[4-(5-metil-3-fenilizoksazol-4-il]fenil}sulfonil)karbamīnskābes 1,1 -dimetiletil-estera nātrija sāls; N-{[4-(5-metil-3-fenilizoksazol-4-il]fenil}sulfonil)glicīna nātrija sāls; 2-amino-N-{[4-(5-metil-3-fenilizoksazol-4-il]fenil}sulfonil)acetam7ds; 2-acetilamino-N-{[4-(5-metil-3-fenilizoksazol-4-il]fenil}sulfonil)acetam7da nātrija sāls; 4-({[4-(5-metil-3-fenilizoksazol-4-il)fenil]sulfonil}amino)-4-oksobutānskābes metilestera nātrija sāls; 11 LV 12239 N-{[4-(5-metil-3-fenilizoksazol-4-il]fenil}sulfonil)karbamīnskābes metilestera nātrija sāls; N-{[4-(5-oksimetil-3-feniloksazol-4-il]fenil}sulfonil)acetamīda nātrija sāls; N-({4-[5-(4-metilfenil)-3-trifluormetil-1 H-pirazol-1 -il]fenil}sulfonil)acetamīda nātrija sāls; 3-({[4-(5-metil-3-fenilizoksazol-4-il)fenil]sulfonil}amino)-3-oksopropānskābes metil-estera nātrija sāls; N-{[4-(5-oksimetil-3-feniloksazol-4-il]fenil}sulfonil)acetamīda nātrija sāls; N-{[4-(5-acetoksimetil-3-feniloksazol-4-il]fenil}sulfonil)acetamīda nātrija sāls; N-{[4-(3,4-dimetil-1-fenil-1H-pirazol-5-il)fenil]sulfonil}propānamīda N-{[4-(5-oksi-metil-3-feniloksazol-4-il]fenil}sulfonil)acetamīda nātrija sāls; N-({4-[2-(2-metilpiridin-3-il)-4-(trifluormetil)imidazol-1-il]fenil}sulfonil)propānamīda nātrija sāls; N-({4-[2-(3-hlor-4-fluorfenil)ciklopenten-1-il]fenil}sulfonil)acetamīda nātrija sāls; N^[4-(3-fenil-2,3-dihidro-2-oksofuran-4-il)fenil]sulfonil}propānamīda nātrija sāls.
13. Savienojums ar formulu (III)
III kurā: R6 ir ņemts no rindas: hidroksilgrupa, Ci.1Qalkilgrupa, karboksilgrupa,, halogēna atoms, karboksi-C^oalkilgrupa, C-i-ealkoksikarbonilgrupa, aril-Ci.ioalkilgrupa, Ci-i0alkoksialkilgrupa, Ci-ioalkoksialkiloksialkilgrupa, aril-Ci-ioalkoksialkilgrupa, Ci^halogēnalkilgrupa, Ci^hidroksialkilgrupa, aril-Ci^hidroksialkilgrupa, Ci-ehalogēnalkilsulfoniloksigrupa, karboksi-C-Moalk-oksialkilgrupa, C3.8cikloalkilalkilgrupa, C^ecikloalkilgrupa; R7 ir viens vai vairāki aizvietotāji no rindas: ūdeņraža atoms, C-M0alkilgrupa, Ci-ehalogēnalkilgrupa, ciāngrupa, karboksilgrupa, Cļ^alkoksikarbonil-grupa, hidroksilgrupa, Ci^hidroksialkilgrupa, C-i-ehalogēnalkoksigrupa, aminogrupa, Ci-ealkilaminogrupa, fenilaminogrupa, nitrogrupa, C-Moalk-oksialkilgrupa, Cļ-ealkilsulfinilgrupa, halogēna atoms, Ci^alkoksigrupa, Ci^alkiltiogrupa; 12 R8 ir ņemts no rindas: ūdeņraža atoms, Ci-ioalkilgrupa, Ci-ealkoksigrupa, Ci-i0alkoksialkilgrupa, fenilgrupa, karboksi-Ci-ioalkilgrupa, Ci-ealkoksikar-bonilalkilgrupa, Ci^alkoksikarbonilgrupa, amino-C-Moalkilgrupa, C-i-ealk-oksikarbonilaminoalkilgrupa, Ci-ioalkilkarbonilaminoalkilgrupa; vai minētā savienojuma farmaceitiski pieņemama sāls.
14. Savienojums pēc 13. punkta, kurā: R6 ir ņemts no rindas: C-Moalkilgrupa, C-i-e halogēnalkilgrupa, Ci^hidroksi-alkilgrupa; R7 ir viens vai vairāki aizvietotāji no rindas: ūdeņraža atoms, Ci.ioalkilgrupa, halogēna atoms, C^alkoksigrupa; R8 ir ņemts no rindas: Ci-i0alkilgrupa, fenilgrupa, amino-Ci-ioalkilgrupa, vai minētā savienojuma farmaceitiski pieņemama sāls.
15. Savienojums pēc 14. punkta, kurā: R6 ir ņemts no rindas: metilgrupa, difluormetilgrupa, oksimetilgrupa; R7 ir viens vai vairāki aizvietotāji no rindas: ūdeņraža atoms, metilgrupa, fluora atoms, hlora atoms, broma atoms, metoksigrupa; R8 ir ņemts no rindas: metilgrupa, etilgrupa, izopropilgrupa, propilgrupa, terc-butilgrupa, butilgrupa, pentilgrupa, fenilgrupa, aminometilgrupa vai minētā savienojuma farmaceitiski pieņemama sāls.
16. Savienojums pēc 15. punkta, kas ņemts no savienojumu un to farmaceitiski pieņemamo sāļu rindas: N-({4-[3-(3-fluorfenil)-5-metilizoksazol-4-il]fenil}sulfonil)acetamīds; 2-metil-N-{[4-(5-metil-3-fenilizoksazo!-4-il]fenil}sulfonil)propānamīds; N-{[4-(5-metil-3-fenilizoksazol-4-iIjfenil}sulfonil)propānamTds; N-{[4-(5-metil-3-fenilizoksazol-4-il]fenil}sulfonil)benzamīds; 2,2-dimetil-N-{[4-(5-metil-3-fenilizoksazol-4-il]fenil}sulfonil)propānamīds; N-{[4-(5-metil-3-fenilizoksazol-4-il]fenil}sulfonil)butānamTds; N-{ļ4-(5-metiI-3-fenilizoksazol-4-il]fenil}sulfonil)pentānamTds; N-{[4-(5-metil-3-fenilizoksazol-4-il]fenil}sulfonil)heksānamīds; N-{[4-(5-metil-3-fenilizoksazol-4-il]fenil}sulfonil)acetamīds; N-{[4-(5-oksimetil-3-fenilizoksazol-4-il]fenil}sulfonil)propānamīds; N-{[4-(5-difluormetil-3-fenilizoksazol-4-il]fenil}sulfonil)propānamīds; N_([4-(5-difluormetil-3-fenilizoksazol-4-il]fenil}sulfonil)butānamīds; N-{[4-(5-metil-3-fenilizoksazol-4-il]fenil}sulfonil)glicīns; N-{[4-(5-oksimetil-3-fenilizoksazol-4-il]fenil}sulfonil)acetamīds. 13 LV 12239
17. Savienojums pēc 13. punkta, kura farmaceitiski pieņemamās sālis ir sārmmetālu sālis vai sārmzemju metālu sālis.
18. Savienojums pēc 17. punkta, kura farmaceitiski pieņemamās sālis ir nātrija vai kālija sālis.
19. Savienojums pēc 18. punkta, kas ņemts no savienojumu un to farmaceitiski pieņemamo sāļu rindas: N-{[4-(5-metil-3-fenilizoksazol-4-ii]fenil}sulfonil)acetamīda kālija sāls; N-({4-[3-{3-fiuorfenil)-5-metilizoksazol-4-il]fenil}sulfonil)acetamīda nātrija sāls; 2-metil-N-{[4-(5-meti!-3-fenilizoksazol-4-il]feni!}sulfonil)propānamīda nātrija sāls; N-{[4-(5-metil-3-fenilizoksazol-4-il]fenil}sulfonil)propānamīda nātrija sāls; N-{[4-(5-metil-3-fenilizoksazol-4-il]fenil}sulfonil)benzamīda nātrija sāls; 2,2-dimetil-N-{[4-(5-metil-3-fenilizoksazol-4-iI]fenil}sulfonil)propānamTda nātrija sāls; N-{[4-(5-metil-3-fenilizoksazol-4-il]fenil}sulfonil)butānamTda nātrija sāls; N-{[4-(5-metil-3-fenilizoksazol-4-il]fenil}sulfonil)pentānamīda nātrija sāls; N-{[4-(5-metil-3-fenilizoksazol-4-il]fenil}sulfonil)heksānamīda nātrija sāls; N-{[4-(2-metil-4-fenilizoksazol-5-il]fenil}sulfonil)acetamīda nātrija sāls; N-{[4-(5-difluormetil-3-fenHizoksazol-4-il]fenil}sulfonil)propānamīda nātrija sāls; N-{[4-(5-difluormetil-3-fenilizoksazol-4-il]fenil}sulfonil)butānamīda nātrija sāls; N-{[4-(5-oksimetil-3-fenilizoksazol-4-il]fenil}sulfonil)propānamTda nātrija sāls; NHJ4-(5-metil-3-fenilizoksazol-4-il]fenil}sulfonil)glicļna nātrija sāls; N-{[4-(5-oksimetil-3-fenilizoksazol-4-il]fenil}sulfonil)acetamīda nātrija sāls.
20. Farmaceitiskā kompozīcija, kas ietver terapeitiski aktīvu daudzumu savienojuma, kurš ņemts no 1. punktā minētajiem savienojumiem, ieskaitot tos, kuros A ir tetrazolija grupa vai A ir indāna grupa, kad R3 ir alkilgrupa vai cikloalkilgrupa, vai arī savienojumu, kurš ņemts no jebkurā no 2. līdz 19. punktam minētajiem savienojumiem.
21. Paņēmiens savienojuma ar formulu (II)
A- R4 II kā arī minētā savienojuma farmaceitiski pieņemamas sāls iegūšanai, kur: A ir ņemts no rindas: daļēji nepiesātināta heterocikliska grupa, 5 vai 6 locekļu heteroarilgrupa, C3^cikloalkenilgrupa un feniigrupa, kur A ir neobligāti aizvietots aizvietošanai piemērotā vietā ar vienu vai vairākiem aizvietotājiem no rindas: acilgrupa, halogēna atoms, hidroksilgrupa, Ci-ioalkilgrupa, Ci^halo-gēnalkilgrupa, oksogrupa, ciāngrupa, nitrogrupa, karboksilgrupa, 14 Ci^alkoksigrupa, aminokarbonilgrupa, C-i-ealkoksikarbonilgrupa, karboksi-Ci-ioalkilgrupa, C-Mociānalkilgrupa, Ci-ehidroksialkilgrupa, Cļ-ioalkilkarboniloksialkiigrupa, fenilgrupa; R4 ir ņemts no rindas: heterocikliska grupa, cikloalkilgrupa, cikloalkenilgrupa, fenilgrupa, kur R4 ir neobligāti aizvietots aizvietošanai piemērotā vietā ar vienu vai vairākiem aizvietotājiem no rindas: C-Moalkilgrupa, C-t-ehalogēnalkilgrupa, ciāngrupa, karboksilgrupa, Ci-ealkoksikarbonilgrupa, hidroksilgrupa, Ci.6hidroksialkilgrupa, Ci^haiogēnalkoksigrupa, aminogrupa, C-i.6alkiIaminogrupa, fenil-aminogrupa, nitrogrupa, C^ioalkoksialkilgrupa, Ci-galkiisulfinilgrupa, halogēna atoms, Ci.6aikoksigrupa, Ci.6alkiltiogrupa; R5 ir ņemts no rindas: ūdeņraža atoms, C-M0aikilgrupa, C-Moalkoksigrupa, Ci-ioalkoksialkiigrupa, fenilgrupa, aril-C-Moalkiigrupa, karboksi-Ci.-ioalkii-grupa, C-i^alkoksikarbonilalkilgrupa, C^alkoksikarbonilgrupa, amino-C-Moaikilgrupa, Ci^alkoksikarbonilaminoaikilgrupa, Ci.ialkilkarbonilamino-alkilgrupa, ar noteikumu, ka A nav tienilgrupa, ja R4 ir 4-fluorfenilgrupa un R5 ir metiigrupa, ietver neaizvietota sulfonamīda apstrādi ar acilējošu aģentu bāzes un šķīdinātāja klātienē.
22. Paņēmiens pēc 21. punkta, kurā acilējošais aģents ņemts no rindas: anhidrīdi, skābju hlorīdi, acilimidazoli, aktivētie esteri.
23. Paņēmiens pēc 22. punkta, kurā acilējošais aģents ņemts no rindas: acetanhidrīds, propionskābes anhidrīds, sviestskābes anhidrīds.
24. Paņēmiens pēc 21. punkta, kurā šķīdinātājs ir tetrahidrofurāns.
25. Paņēmiens savienojuma ar formulu (III)
vai tā farmaceitiski pieņemamu sāļu iegūšanai, kur: 15 LV 12239 R6 ir ņemts no rindas: hidroksilgrupa, C-Moalkilgrupa, karboksiigrupa, halogēna atoms, karboksi-C-Moalkilgrupa, Ci-6alkoksikarbonilgrupa, aril-Ci-ioalkilgrupa, Cļ-ioalkoksialkilgrupa, Ci-ioalkoksialkiloksialkilgrupa, aril-Cļ.ioalkoksialkilgrupa, Ci^halogēnalkiigrupa, C-i-ehidroksialkilgrupa, aril-Ci-ehidroksialkiigrupa, Ci^halogēnalkilsulfoniloksigrupa, karboksi-C-i. ioalkoksialkilgrupa, C3_ecikloalkilalkilgrupa, Cs-ecikloalkilgrupa; R7 ir viens vai vairāki aizvietotāji no rindas: ūdeņraža atoms, C-mo alkilgrupa, Ci-ehalogēnalkilgrupa, ciāngrupa, karboksiigrupa, Ci-ealkoksikarbonil-grupa, hidroksilgrupa, Ci^hidroksialkilgrupa, Ci-ehalogēnalkoksigrupa, aminogrupa, Ci^alkilaminogrupa, fenilaminogrupa, nitrogrupa, Ci_i0alk-oksialkilgrupa, Ci-6alkilsulfinilgrupa, halogēna atoms, Ci^alkoksigrupa, C-i-ealkiltiogrupa; R8 ir ņemts no rindas: ūdeņraža atoms, Ci-ioalkilgrupa, Ci^alkoksigrupa, C-Moaikoksiaikilgrupa, fenilgrupa, karboksi-Ci-ioalkilgrupa, Ci^alkoksi-karbonilalkilgrupa, Ci^alkoksikarbonilgrupa, amino-Ci-i0alkilgrupa, Ci^alkoksikarbonilaminoalkilgrupa, Ci-ioalkilkarbonilaminoalkilgrupa, ietver neaizvietota izoksazolilbenzolsulfonamīda apstrādi ar acilējošu aģentu bāzes un šķīdinātāja klātienē.
26. Paņēmiens savienojuma ar formulu (II) farmaceitiski pieņemamas sāls iegūšanai a A-> R4
o // Ν'* O O II kur: A ir ņemts no rindas: daļēji nepiesātināta heterocikliska grupa, 5 vai 6 locekļu heteroarilgrupa, C^ecikloalkenilgrupa un fenilgrupa, kur A ir neobligāti aizvietots aizvietošanai piemērotā vietā ar vienu vai vairākiem aizvietotājiem no rindas: acilgrupa, halogēna atoms, hidroksilgrupa, Ci-ioalkilgrupa, Ci^halo-gēnalkilgrupa, oksogrupa, ciāngrupa, nitrogrupa, karboksiigrupa, C-i-ealkoksigrupa, aminokarbonilgrupa, Ci^alkoksikarbonilgrupa, karboksi-Ci.-ioalkilgrupa, C-Modānalkilgrupa, C-i-ehidroksialkilgrupa, Ci-ioalkilkarboniloksialkilgrupa, fenilgrupa: 16 ι R4 ir ņemts no rindas: heterocikliska grupa, cikloalkilgrupa, cikloalkenilgrupa, fenilgrupa, kur R4 ir neobligāti aizvietots aizvietošanai piemērotā vietā ar vienu vai vairākiem aizvietotājiem no rindas: Cļ.ioalkilgrupa, Cļ^halogēnalkilgrupa, ciāngrupa, karboksilgrupa, Ci^alkoksikarbonilgrupa, hidroksilgrupa, Ci^hidroksialkilgrupa, Ci^halogēnalkoksigrupa, aminogrupa, C^alkilaminogrupa, fenil-aminogrupa, nitrogrupa, CMoalkoksialkilgrupa, Ci^alkilsulfmilgrupa, halogēna atoms, C-i^alkoksigrupa, Cļ^alkiltiogrupa; R5 ir ņemts no rindas: ūdeņraža atoms, Ci-ioalkilgrupa, Ci.ioalkoksigrupa, C-Moalkoksialkilgrupa, fenilgrupa, aril-Ci-ioalkilgrupa, karboksi-Ci-ioalkil-grupa, Ci-ealkoksikarbonilalkilgrupa, Ci^alkoksikarbonilgrupa, amino-Cļ.ioalkilgrupa, C^alkoksikarbonilaminoalkilgrupa, Ci-ialkilkarbonilamino-alkilgrupa, ietver bis(N-acil)sulfonamīda pagatavošanu, apstrādājot neaizvietotu sulfon-amīdu ar anhidrīda, skābes hlorīda vai karbamilhlorīda pārākumu trešējā amīna kā bāzes klātienē, kam seko minētā bis(N-acil)sulfonamīda apstrāde ar diviem ekvivalentiem stipras bāzes, lai iegūtu sāli,
27. Paņēmiens savienojuma ar formulu (II)
vai tā farmaceitiski pieņemamas sāls iegūšanai, kur: A ir ņemts no rindas: daļēji nepiesātināta heterocikliska grupa, 5 vai 6 locekļu heteroarilgrupa, C^acikloalkenilgrupa un fenilgrupa, kur A ir neobligāti aizvietots aizvietošanai piemērotā vietā ar vienu vai vairākiem aizvietotājiem no rindas: acilgrupa, halogēna atoms, hidroksilgrupa, Ci.i0alkilgrupa, Ci^halo-gēnalkilgrupa, oksogrupa, ciāngrupa, nitrogrupa, karboksilgrupa, Ci-ealkoksigrupa, aminokarbonilgrupa, Cļ^alkoksikarbonilgrupa, karboksi-Ci_ioalkilgrupa, Ci.iociānalkilgrupa, Ci^hidroksialkilgrupa, Ci-ioalkilkarboniloksialkilgrupa, fenilgrupa; R4 ir ņemts no rindas: heterocikliska grupa, cikloalkilgrupa, cikloalkenilgrupa, fenilgrupa, kur R4 ir neobligāti aizvietots aizvietošanai piemērotā vietā ar vienu vai vairākiem aizvietotājiem no rindas: Ci-ioalkilgrupa, Ci^halogēnalkilgrupa, ciāngrupa, karboksilgrupa, Ci^alkoksikarbonilgrupa, hidroksilgrupa, Ci^hidroksialkilgrupa, Ci^halogēnalkoksigrupa, aminogrupa, C-i-ealkilaminogrupa, fenil-aminogrupa, nitrogrupa, C-Moalkoksialkilgrupa, Ci^alkilsulfinilgrupa, halogēna atoms, Ci^alkoksigrupa, C^alkiltiogrupa; 17 LV 12239 R5 ir ņemts no rindas: ūdeņraža atoms, Ci.10alkilgrupa, C^oalkoksigrupa, Ci-ioalkoksialkilgrupa, fenilgrupa, aril-Ci-ioalkilgrupa, karboksi-Ci-i0alkil- grupa, C-i-ealkoksikarbonilalkilgrupa, Ci_6alkoksikarbonilgrupa, amino- Ci-ioalkilgrupa, Ci^alkoksikarbonilaminoalkilgrupa, Ci.ialkilkarbonilamino- alkilgrupa, ar noteikumu, ka nav tienilgrupa, kad R4 ir 4-fluorfenilgrupa un R5 ir metilgrupa, ietver neaizvietota sulfonamīda apstrādi ar acilējošu aģentu skābes klātienē.
28. Paņēmiens pēc 27. punkta, kurā acilējošais aģents ir anhidrīdi vai skābju hlorīdi.
29. Paņēmiens pēc 28. punkta, kurā acilējošais aģents ņemts no rindas: acetilhlorīds, acetanhidrīds, propionskābes anhidrīds, sviestskābes anhidrīds.
30. Paņēmiens pēc 27. punkta, kurā A ir ņemts no rindas: oksazolilgrupa, furanilgrupa, tiazolilgrupa, imidazolilgrupa, benzofuranilgrupa, indenilgrupa, benzotienilgrupa, izoksazolilgrupa, pirazolilgrupa, ciklopentenilgrupa, ciklopentadienilgrupa.benzindazolilgrupa, benzopiranopirazoliigrupa, fenilgrupa, piridinilgrupa.
31. Paņēmiens pēc 30. punkta, kurā A ir ņemts no rindas: imidazolilgrupa, izoksazolilgrupa, pirazolilgrupa.
32. Savienojuma pēc 1. punkta, ieskaitot tos, kuros A ir tetrazolija vai piridīnija grupa, vai A ir indanona grupa, kad R3 ir alkilgrupa vai karboksialkilgrupa, vai savienojuma, kas minēts jebkurā no 1. līdz 19. punktam, pielietojums medikamenta ražošanai, kas paredzēts iekaisuma slimības vai ar iekaisumu saistītu slimīgu stāvokļu ārstēšanai.
33. Pielietojums pēc 32. punkta iekaisumu ārstēšanai.
34. Pielietojums pēc 32. punkta ar iekaisumu saistītu slimīgu stāvokļu ārstēšanai.
35. Pielietojums pēc 34. punkta, kurā ar iekaisumu saistītais slimīgais stāvoklis ir sāpes.
36. Pielietojums pēc 35. punkta, kurā sāpes ir saistītas ar vēzi.
37. Pielietojums pēc 35. punkta, kurā sāpes ir zobu sāpes.
38. Pielietojums pēc 35. punkta, kurā savienojumu ievada intravenozi.
39. Pielietojums pēc 35. punkta, kurā savienojumu ievada intramuskulāri.
LVP-98-215A 1996-04-12 1998-10-12 Benzolsulfonamīda atvasinājumi kā cox-2 inhibitori LV12239B (lv)

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Families Citing this family (279)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2223154A1 (en) 1995-06-02 1996-12-05 G.D. Searle & Co. Heterocyclo substituted hydroxamic acid derivatives as cyclooxygenase-2 and 5-lipoxygenase inhibitors
US5908858A (en) * 1996-04-05 1999-06-01 Sankyo Company, Limited 1,2-diphenylpyrrole derivatives, their preparation and their therapeutic uses
TR199802049T2 (xx) * 1996-04-12 1999-01-18 G.D.Searle & Co. COX-2 Inhibit�rlerinin �nilac� olarak s�bstit�e edilmi� benzens�lfonamid t�revleri.
US8022095B2 (en) 1996-08-16 2011-09-20 Pozen, Inc. Methods of treating headaches using 5-HT agonists in combination with long-acting NSAIDs
US6586458B1 (en) 1996-08-16 2003-07-01 Pozen Inc. Methods of treating headaches using 5-HT agonists in combination with long-acting NSAIDs
BR9807920A (pt) * 1997-04-03 2000-02-22 Searle & Co Processos para tratamento de uma demência em um sujeito e para prevenção de uma demência
US20040072889A1 (en) * 1997-04-21 2004-04-15 Pharmacia Corporation Method of using a COX-2 inhibitor and an alkylating-type antineoplastic agent as a combination therapy in the treatment of neoplasia
RS49982B (sr) 1997-09-17 2008-09-29 Euro-Celtique S.A., Sinergistička analgetička kombinacija analgetičkog opijata i inhibitora ciklooksigenaze-2
NZ333399A (en) 1997-12-24 2000-05-26 Sankyo Co Cyclooxygenase-2 inhibitors (COX-2) for the prevention and treatment of tumors, cachexia and tumor-metastasis
EP1061908A4 (en) * 1998-03-13 2007-01-24 Merck & Co Inc COMBINATION THERAPY AND COMPOSITION FOR ACUTE CORONARY MIXING SYNDROME AND ASSOCIATED CONDITIONS
US6136804A (en) * 1998-03-13 2000-10-24 Merck & Co., Inc. Combination therapy for treating, preventing, or reducing the risks associated with acute coronary ischemic syndrome and related conditions
WO1999063939A2 (en) 1998-06-08 1999-12-16 Advanced Medicine, Inc. Multibinding inhibitors of cyclooxygenase-2
AR024222A1 (es) * 1998-10-16 2002-09-25 Palau Pharma Sa Imidazoles con actividad antiinflamatoria un procedimiento para su preparacion y composiciones farmaceuticas que lo contienen
DE69922688T2 (de) * 1998-11-02 2005-12-01 Merck & Co. Inc. Zusammensetzungen aus einem 5ht1b/1d agonisten und einem selektiven cox-2 hemmer zur behandlung von migräne
AU1398899A (en) * 1998-11-12 2000-06-05 Algos Pharmaceutical Corporation Cox-2 inhibitors in combination with centrally acting analgesics
US20040122011A1 (en) * 1998-12-23 2004-06-24 Pharmacia Corporation Method of using a COX-2 inhibitor and a TACE inhibitors as a combination therapy
US6649645B1 (en) 1998-12-23 2003-11-18 Pharmacia Corporation Combination therapy of radiation and a COX-2 inhibitor for treatment of neoplasia
US20030119895A1 (en) * 1998-12-23 2003-06-26 Pharmacia Corporation Methods using a combination of a 3-heteroaryl-2-indolinone and a cyclooxygenase-2 inhibitor for the treatment of neoplasia
US20030013739A1 (en) * 1998-12-23 2003-01-16 Pharmacia Corporation Methods of using a combination of cyclooxygenase-2 selective inhibitors and thalidomide for the treatment of neoplasia
AU3596500A (en) * 1999-02-19 2000-09-04 Pozen, Inc. Formulation of 5-ht agonists with cox-2 inhibitors
US20010024664A1 (en) * 1999-03-19 2001-09-27 Obukowicz Mark G. Selective COX-2 inhibition from edible plant extracts
US6323226B1 (en) 1999-10-19 2001-11-27 Texas Heart Institute Treatment of heart disease with cox-2 inhibitors
ATE283048T1 (de) * 1999-12-08 2004-12-15 Pharmacia Corp Cyclooxygenase-2 hemmer enthaltende zusammensetzungen mit schnellem wirkungseintritt
EP1239857B1 (en) * 1999-12-22 2006-04-19 Pharmacia Corporation Dual-release compositions of a cyclooxygenase-2- inhibitor
WO2001045703A1 (en) * 1999-12-23 2001-06-28 Nitromed, Inc. Nitrosated and nitrosylated cyclooxygenase-2 inhibitors, compositions and methods of use
AU2001238468B2 (en) 2000-02-16 2006-07-06 The Brigham And Women's Hospital, Inc. Aspirin-triggered lipid mediators
AU2001232175B2 (en) * 2000-03-03 2005-07-07 Pfizer Products Inc. Pyrazole ether derivatives as anti-inflammatory/analgesic agents
US20070072861A1 (en) * 2000-03-27 2007-03-29 Barbara Roniker Method of using cyclooxygenase-2 inhibitors in the prevention of cardiovascular disorders
ES2166710B1 (es) * 2000-04-25 2004-10-16 J. URIACH & CIA, S.A. Nuevos compuestos heterociclicos con actividad antiinflamatoria.
JP2003531202A (ja) * 2000-04-25 2003-10-21 ファルマシア・コーポレーション ３，４−ジ（カルボシクリルまたはヘテロシクリル）チオフェンの位置選択的合成
CA2414674A1 (en) * 2000-07-13 2002-01-24 Pharmacia Corporation Use of cox-2 inhibitors in the treatment and prevention of ocular cox-2 mediated disorders
JP2004510705A (ja) 2000-07-20 2004-04-08 ラウラス　エイエス 方法
US20030219461A1 (en) * 2000-09-12 2003-11-27 Britten Nancy J. Parenteral combination therapy for infective conditions
CA2422064A1 (en) * 2000-09-18 2002-03-21 Merck & Co., Inc. Treatment of inflammation with a combination of a cyclooxygenase-2 inhibitor and an integrin alpha-v antagonist
AU2002213467A1 (en) * 2000-10-11 2002-04-22 Chemocentryx, Inc. Modulation of ccr4 function
JP2004529079A (ja) * 2000-12-15 2004-09-24 ファルマシア・コーポレーション 植物抽出物による選択的ｃｏｘ−２阻害
US20020122836A1 (en) * 2000-12-15 2002-09-05 Pharmacia Corporation Selective COX-2 inhibition from non-edible plant extracts
CA2432642A1 (en) 2000-12-21 2002-08-08 Subhash P. Khanapure Substituted aryl compounds as novel cyclooxygenase-2 selective inhibitors, compositions and methods of use
US7115565B2 (en) * 2001-01-18 2006-10-03 Pharmacia & Upjohn Company Chemotherapeutic microemulsion compositions of paclitaxel with improved oral bioavailability
JP2004522754A (ja) * 2001-02-02 2004-07-29 ファルマシア・コーポレーション 月経困難症の治療および予防のための組み合わせ治療としてシクロオキシゲナーゼ‐２阻害剤および性ステロイドを使用する方法
WO2002078625A2 (en) * 2001-03-28 2002-10-10 Pharmacia Corporation Therapeutic combinations for cardiovascular and inflammatory indications
US7695736B2 (en) * 2001-04-03 2010-04-13 Pfizer Inc. Reconstitutable parenteral composition
ITMI20010733A1 (it) 2001-04-05 2002-10-05 Recordati Chem Pharm Uso di inibitori dell'isoenzina cox-2 per il trattamento dell'incontinenza urinaria
US20030105144A1 (en) * 2001-04-17 2003-06-05 Ping Gao Stabilized oral pharmaceutical composition
US6673818B2 (en) 2001-04-20 2004-01-06 Pharmacia Corporation Fluoro-substituted benzenesulfonyl compounds for the treatment of inflammation
WO2002094264A1 (en) * 2001-05-23 2002-11-28 Tularik Inc. Ccr4 antagonists
US20030153801A1 (en) * 2001-05-29 2003-08-14 Pharmacia Corporation Compositions of cyclooxygenase-2 selective inhibitors and radiation for inhibition or prevention of cardiovascular disease
WO2002096435A2 (en) * 2001-05-31 2002-12-05 Pharmacia Corporation Skin-permeable composition comprising a selective cyclooxygenase-2 inhibitor a monohydric alcohol
US20060167074A1 (en) * 2001-06-19 2006-07-27 Norbert Muller Methods and compositions for the treatment of psychiatric disorders
DE10129320A1 (de) * 2001-06-19 2003-04-10 Norbert Mueller Verwendung von COX-2 Inhibitoren zur Behandlung von Schizophrenie, wahnhaften Störungen, affektiven Störungen oder Ticstörungen
UA80682C2 (en) * 2001-08-06 2007-10-25 Pharmacia Corp Orally deliverable stabilized oral suspension formulation and process for the incresaing physical stability of thixotropic pharmaceutical composition
WO2003013655A2 (en) * 2001-08-10 2003-02-20 Pharmacia Corporation Carbonic anhydrase inhibitors
US20040067992A1 (en) * 2001-08-10 2004-04-08 Pharmacia Corporation Compositions of a cyclooxygenase-2 selective inhibitor and a carbonic anhydrase inhibitor for the treatment of neoplasia
US20030114416A1 (en) * 2001-08-14 2003-06-19 Pharmacia Corporation Method and compositions for the treatment and prevention of pain and inflammation with a cyclooxygenase-2 selective inhibitor and chondroitin sulfate
US20050101563A1 (en) * 2001-08-14 2005-05-12 Pharmacia Corporation Method and compositions for the treatment and prevention of pain and inflammation
AR038957A1 (es) 2001-08-15 2005-02-02 Pharmacia Corp Terapia de combinacion para el tratamiento del cancer
US6777417B2 (en) * 2001-09-10 2004-08-17 Sugen, Inc. 3-(4,5,6,7-tetrahydroindol-2-ylmethylidiene-2-indolinone derivatives as kinase inhibitors
AU2002330042A1 (en) 2001-09-18 2003-04-01 Onconova Therapeutics, Inc. Process for the preparation of 1,5-diarylpyrazoles
US20030114483A1 (en) * 2001-09-18 2003-06-19 Pharmacia Corporation Compositions of chromene cyclooxygenase-2 selective inhibitors and acetaminophen for treatment and prevention of inflammation, inflammation-mediated disorders and pain
JP2005508320A (ja) * 2001-09-18 2005-03-31 オンコノバ・セラピューティックス・インコーポレーテッド １，５−ジアリール−３−置換ピラゾールの調製方法
US20030236308A1 (en) * 2001-09-18 2003-12-25 Pharmacia Corporation Compositions of cyclooxygenase-2 selective inhibitors and acetaminophen for treatment and prevention of inflammation, inflammation-mediated disorders and pain
CA2460939C (en) * 2001-09-19 2008-07-29 Pharmacia Corporation Substituted pyrazolyl compounds for the treatment of inflammation
JP2005509608A (ja) * 2001-10-02 2005-04-14 ファルマシア コーポレイション ベンゼンスルホニル化合物の製造方法
AR037097A1 (es) 2001-10-05 2004-10-20 Novartis Ag Compuestos acilsulfonamidas, composiciones farmaceuticas y el uso de dichos compuestos para la preparacion de un medicamento
AU2002337843A1 (en) * 2001-10-12 2003-04-22 Onconova Therapeutics, Inc. Processes for the preparation of substituted isoxazoles and 2-isoxazolines
US20030162824A1 (en) * 2001-11-12 2003-08-28 Krul Elaine S. Methods of treating or preventing a cardiovascular condition using a cyclooxygenase-1 inhibitor
KR20050044459A (ko) * 2001-11-13 2005-05-12 파마시아 코포레이션 파레콕시브 등의 설폰아미드 선구약물의 경구 투여 형태
ATE424388T1 (de) 2001-12-06 2009-03-15 Merck & Co Inc Mitotische kinesinhemmer
US20040126438A1 (en) * 2001-12-13 2004-07-01 Obukowicz Mark G. Selective cox-2 inhibition from plant extracts
EP1463505A2 (en) * 2001-12-13 2004-10-06 Abbott Laboratories 3-(phenyl-alkoxy)-5-(phenyl)-pyridine derivatives and related compounds as kinase inhibitors for the treatment of cancer
US20040062823A1 (en) * 2001-12-13 2004-04-01 Obukowicz Mark G. Selective cox-2 inhibition from non-edible plant extracts
IL162726A0 (en) * 2002-01-10 2005-11-20 Pharmacia & Upjohn Co Llc Use of cox-2 inhibitors in combination with antiviral agents for the treatment of papilloma virus infections
US20030220374A1 (en) * 2002-01-14 2003-11-27 Pharmacia Corporation Compositions and methods of treatment involving peroxisome proliferator-activated receptor-gamma agonists and cyclooxygenase-2 selective inhibitors
US20030212138A1 (en) * 2002-01-14 2003-11-13 Pharmacia Corporation Combinations of peroxisome proliferator-activated receptor-alpha agonists and cyclooxygenase-2 selective inhibitors and therapeutic uses therefor
TW200403072A (en) * 2002-01-23 2004-03-01 Upjohn Co Combination therapy for the treatment of bacterial infections
US20100311701A1 (en) * 2002-02-15 2010-12-09 Transform Pharmaceuticals, Inc Pharmaceutical Co-Crystal Compositions
US7790905B2 (en) * 2002-02-15 2010-09-07 Mcneil-Ppc, Inc. Pharmaceutical propylene glycol solvate compositions
WO2004026235A2 (en) * 2002-09-20 2004-04-01 Transform Pharmaceuticals, Inc. Pharmaceutical compositions with improved dissolution
US7927613B2 (en) * 2002-02-15 2011-04-19 University Of South Florida Pharmaceutical co-crystal compositions
WO2003074474A2 (en) * 2002-03-01 2003-09-12 University Of South Florida Multiple-component solid phases containing at least one active pharmaceutical ingredient
EP1915992A1 (en) 2002-02-19 2008-04-30 Pharmacia Corporation Use of cyclooxygenase inhibitors and antimuscarinic agents for the treatment of incontinence
US20030232871A1 (en) 2002-03-15 2003-12-18 Sheikh Ahmad Y. Crystalline parecoxib sodium
US8481772B2 (en) 2002-04-01 2013-07-09 University Of Southern California Trihydroxy polyunsaturated eicosanoid derivatives
US7902257B2 (en) * 2002-04-01 2011-03-08 University Of Southern California Trihydroxy polyunsaturated eicosanoid
RU2004132721A (ru) 2002-04-08 2005-06-27 Глэксо Груп Лимитед (GB) (2-алкокси)фенил)циклопент-1-енил)ароматическая карбо- и гетероциклическая карбоновая кислота и ее производные
BR0309337A (pt) * 2002-04-18 2005-02-15 Pharmacia Corp Monoterapia para o tratamento de doença de parkinson com inibidores de ciclooxigenase-2 (cox2)
EP1494664A2 (en) * 2002-04-18 2005-01-12 Pharmacia Corporation Combinations of cox-2 inhibitors and other agents for the treatment of parkinson's disease
AU2003229016A1 (en) * 2002-05-10 2003-11-11 The Trustees Of Columbia University In The City Of New York Genetically engineered cell lines and systems for propagatingvaricella zoster virus and methods of use thereof
CA2489984A1 (en) * 2002-06-21 2003-12-31 Transform Pharmaceuticals, Inc. Pharmaceutical compositions with improved dissolution
AU2003247793A1 (en) * 2002-06-26 2004-01-19 Pharmacia Corporation Stable liquid parenteral parecoxib formulation
CA2489428A1 (en) 2002-06-27 2004-01-08 Nitromed, Inc. Cyclooxygenase-2 selective inhibitors, compositions and methods of use
US7211598B2 (en) 2002-06-28 2007-05-01 Nitromed, Inc. Oxime and/or hydrozone containing nitrosated and/or nitrosylated cyclooxygenase-2 selective inhibitors, compositions and methods of use
US20040063697A1 (en) * 2002-07-02 2004-04-01 Isakson Peter C. Compositions of cyclooxygenase-2 selective inhibitors and thrombolytic agents for the treatment or prevention of a vaso-occlusive event
EP3584235A3 (en) * 2002-08-12 2020-04-22 Brigham and Women's Hospital Resolvins: biotemplates for novel therapeutic interventions
US7759395B2 (en) 2002-08-12 2010-07-20 The Brigham And Women's Hospital, Inc. Use of docosatrienes, resolvins and their stable analogs in the treatment of airway diseases and asthma
UY27939A1 (es) 2002-08-21 2004-03-31 Glaxo Group Ltd Compuestos
KR100484525B1 (ko) * 2002-10-15 2005-04-20 씨제이 주식회사 이소티아졸 유도체, 그 제조방법 및 약제학적 조성물
US20040082543A1 (en) * 2002-10-29 2004-04-29 Pharmacia Corporation Compositions of cyclooxygenase-2 selective inhibitors and NMDA receptor antagonists for the treatment or prevention of neuropathic pain
GB0225548D0 (en) 2002-11-01 2002-12-11 Glaxo Group Ltd Compounds
US20040092566A1 (en) * 2002-11-12 2004-05-13 Graneto Matthew J. Celecoxib prodrug
US20040147581A1 (en) * 2002-11-18 2004-07-29 Pharmacia Corporation Method of using a Cox-2 inhibitor and a 5-HT1A receptor modulator as a combination therapy
US20040126415A1 (en) * 2002-11-21 2004-07-01 Lu Guang Wei Dermal delivery of a water-soluble selective cyclooxygenase-2 inhibitor
US20040127531A1 (en) * 2002-11-21 2004-07-01 Lu Guang Wei Adhesive coated sheet for dermal delivery of a selective cyclooxygenase-2 inhibitor
US20050020658A1 (en) * 2002-11-21 2005-01-27 Katsuyuki Inoo Selective cyclooxygenase-2 inhibitor patch
KR20090118994A (ko) 2002-12-13 2009-11-18 워너-램버트 캄파니 엘엘씨 하부요로증상을 치료하기 위한 알파-2-델타 리간드
US20040235925A1 (en) * 2002-12-17 2004-11-25 Pharmacia Corporation Method for the treatment, prevention, or inhibition of a CNS disorder and/or pain and inflammation using a combination of duloxetine, venlafaxine or atomoxetine and a cyclooxygenase-2 selective inhibitor and compositions thereof
US20040204411A1 (en) * 2002-12-17 2004-10-14 Pharmacia Corporation Method for the treatment, prevention, or inhibition of a CNS disorder and/or pain and inflammation using a combination of reboxetine and a cyclooxygenase-2 selective inhibitor and compositions thereof
PL377427A1 (pl) * 2002-12-19 2006-02-06 Pharmacia Corporation Sposoby i kompozycje do leczenia infekcji wirusem opryszczki z zastosowaniem inhibitorów selektywnych względem cyklooksygenazy-2 lub inhibitorów cyklooksygenazy-2 w połączeniu ze środkami przeciwwirusowymi
US20080153894A1 (en) * 2002-12-19 2008-06-26 Pharmacia Corporation Cyclooxygenase-2 inhibitor and antibacterial agent combination for intramammary treatment of mastitis
US20040171664A1 (en) * 2002-12-20 2004-09-02 Pharmacia Corporation Compositions of cyclooxygenase-2 selective inhibitors and selective serotonin reuptake inhibitors for the treatment or prevention of a vaso-occlusive event
ES2215474B1 (es) * 2002-12-24 2005-12-16 J. URIACH & CIA S.A. Nuevos derivados de fosforamida.
CA2509023C (en) 2002-12-26 2011-05-24 Pozen Inc. Multilayer dosage forms containing nsaids and triptans
US8183290B2 (en) 2002-12-30 2012-05-22 Mcneil-Ppc, Inc. Pharmaceutically acceptable propylene glycol solvate of naproxen
WO2004060367A1 (en) * 2002-12-30 2004-07-22 Fujisawa Pharmaceutical Co., Ltd. Imidazole and triazole derivatives useful as selective cox-1 inhibitors
US20050026902A1 (en) * 2003-01-31 2005-02-03 Timothy Maziasz Methods and compositions for the treatment or prevention of human immunodeficiency virus and related conditions using cyclooxygenase-2 selective inhibitors and antiviral agents
US20040176378A1 (en) * 2003-02-12 2004-09-09 Pharmacia Corporation Compositions of a cyclooxygenase-2 selective inhibitor and an amphetamine for the treatment of reduced blood flow to the central nervous system
WO2004078143A2 (en) * 2003-03-05 2004-09-16 The Brigham And Women's Hospital Inc. Methods for identification and uses of anti-inflammatory receptors for eicosapentaenoic acid analogs
US20050004098A1 (en) * 2003-03-20 2005-01-06 Britten Nancy Jean Dispersible formulation of an anti-inflammatory agent
BRPI0408556A (pt) * 2003-03-20 2006-03-21 Pharmacia Corp formulações dispersìvel de um agente antiinflamatório
US20040214753A1 (en) * 2003-03-20 2004-10-28 Britten Nancy Jean Dispersible pharmaceutical composition for treatment of mastitis and otic disorders
US20050009931A1 (en) * 2003-03-20 2005-01-13 Britten Nancy Jean Dispersible pharmaceutical composition for treatment of mastitis and otic disorders
US20040220155A1 (en) * 2003-03-28 2004-11-04 Pharmacia Corporation Method of providing a steroid-sparing benefit with a cyclooxygenase-2 inhibitor and compositions therewith
US20040214861A1 (en) * 2003-03-28 2004-10-28 Pharmacia Corporation Compositions of a cyclooxygenase-2 selective inhibitors and 5-HT1B1D antagonists for the treatment and prevention of migraine
AU2003238669A1 (en) * 2003-04-04 2004-10-25 Hetero Drugs Limited Novel crystalline forms of parecoxib sodium
DE602004011511T2 (de) * 2003-04-14 2009-01-29 The Institutes for Pharmaceutical Discovery, LLC, Branford N-(((((1,3-thiazol-2-yl)amino)carbonyl)phenyl)sulphonyl)phenylalanin derivate und verwandte verbindungen zur behandlung von diabetes
US20050159403A1 (en) * 2003-04-22 2005-07-21 Pharmacia Corporation Compositions of a cyclooxygenase-2 selective inhibitor and a calcium modulating agent for the treatment of central nervous system damage
WO2004093814A2 (en) * 2003-04-22 2004-11-04 Pharmacia Corporation Compositions of a cyclooxygenase-2 selective inhibitor and a sodium channel blocker
US20050009733A1 (en) * 2003-04-22 2005-01-13 Pharmacia Corporation Compositions of a cyclooxygenase-2 selective inhibitor and a potassium ion channel modulator for the treatment of central nervous system damage
WO2004093895A1 (en) * 2003-04-22 2004-11-04 Pharmacia Corporation Compositions of a cyclooxygenase-2 selective inhibitor and a potassium ion channel modulator for the treatment of pain, inflammation or inflammation mediated disorders
US20060135506A1 (en) * 2003-04-22 2006-06-22 Pharmacia Corporation Compositions of a cyclooxygenase-2 selective inhibitor and a calcium modulating agent for the treatment of pain, inflammation or inflammation mediated disorders
US20040224940A1 (en) * 2003-04-22 2004-11-11 Pharmacia Corporation Compositions of a cyclooxygenase-2 selective inhibitor and a sodium ion channel blocker for the treatment of central nervous system damage
JP2006525329A (ja) 2003-04-30 2006-11-09 ジ インスチチュート フォー ファーマシューティカル ディスカバリー、エルエルシー 置換カルボン酸類
US20040220167A1 (en) * 2003-05-02 2004-11-04 Nasrollah Samiy Methods of treating neuralgic pain
ES2275218T3 (es) 2003-05-07 2007-06-01 Osteologix A/S Sales de estroncio hidrosolubles para el tratamiento de afecciones de cartilagos y/o huesos.
WO2004100895A2 (en) * 2003-05-13 2004-11-25 Pharmacia Corporation Compositions of a cyclooxygenase-2 selective inhibitor and a peroxisome proliferator activated receptor agonist for the treatment of ischemic mediated central nervous system disorders
WO2004103286A2 (en) * 2003-05-14 2004-12-02 Pharmacia Corporation Compositions of a cyclooxygenase-2 selective inhibitor and a cholimergic agent
CA2525280A1 (en) * 2003-05-14 2004-12-02 Pharmacia Corporation Compositions for the treatment of reduced blood flow
EP1628653A2 (en) * 2003-05-14 2006-03-01 Pharmacia Corporation Compositions of a benzenesulfonamide or methylsulfonylbenzene cyclooxygenase-2 selective inhibitor and a cholinergic agent for the treatment of reduced blood flow or trauma to the central nervous system
US20050159419A1 (en) * 2003-05-14 2005-07-21 Pharmacia Corporation Compositions of a cyclooxygenase-2 selective inhibitor and a central nervous system stimulant for the treatment of central nervous system damage
WO2004110456A1 (en) * 2003-05-27 2004-12-23 Pharmacia Corporation Fcompositions of a cyclooxygenase-2 selective inhibitor, a xanthine compound and an alcohol for the treatment of ischemic mediated central nervous system disorders or injury
US20060160776A1 (en) * 2003-05-28 2006-07-20 Pharmacia Corporation Compositions of a cyclooxygenase-2 selective inhibitor and a cannabinoid agent for the treatment of central nervous system damage
UA82698C2 (uk) 2003-05-30 2008-05-12 Ранбакси Лабораториз Лимитед Заміщені похідні піролу та їх використання в якості інгібіторів hmg-co
WO2005016243A2 (en) * 2003-06-09 2005-02-24 Pharmacia Corporation Compositions of a cyclooxygenase-2 selective inhibitor and an antioxidant agent for the treatment of central nervous system disorders
US20050065154A1 (en) * 2003-06-24 2005-03-24 Pharmacia Corporation Treatment of migraine accompanied by nausea with a combination of cyclooxygenase-2 selective inhibitors and anti-nausea agents
US20050101597A1 (en) * 2003-07-10 2005-05-12 Pharmacia Corporation Compositions of a cyclooxygenase-2 selective inhibitior and a non-NMDA glutamate modulator for the treatment of central nervous system damage
US20050080083A1 (en) * 2003-07-10 2005-04-14 Pharmacia Corporation Compositions of a cyclooxygenase-2 selective inhibitor and an angiotensin II receptor antagonist for the treatment of central nervous system damage
US20050070543A1 (en) * 2003-07-11 2005-03-31 Pharmacia Corporation Compositions of a chromene or phenyl acetic acid cyclooxygenase-2 selective inhibitor and an ACE inhibitor for the treatment of central nervous system damage
WO2005018541A2 (en) * 2003-07-11 2005-03-03 Pharmacia Corporation Cox-2 inhibitor and serotonin modulator for treating cns damage
WO2005009342A2 (en) * 2003-07-16 2005-02-03 Pharmacia Corporation Method for the treatment or prevention of dermatological disorders with a cyclooxygenase-2 inhibitor alone and in combination with a dermatological treatment agent and compositions therewith
US20050075341A1 (en) * 2003-07-17 2005-04-07 Pharmacia Corporation Compositions of a cyclooxygenase-2 selective inhibitor and an IKK inhibitor for the treatment of ischemic mediated central nervous system disorders or injury
JPWO2005012268A1 (ja) * 2003-07-30 2006-09-14 塩野義製薬株式会社 イソオキサゾール環を有するスルホンアミド誘導体
AU2004266705A1 (en) * 2003-08-20 2005-03-03 Nitromed, Inc. Nitrosated and nitrosylated cardiovascular compounds, compositions and methods of use
US20050119262A1 (en) * 2003-08-21 2005-06-02 Pharmacia Corporation Method for preventing or treating an optic neuropathy with a cox-2 inhibitor and an intraocular pressure reducing agent
WO2005018563A2 (en) * 2003-08-22 2005-03-03 Pharmacia Corporation Compositions of a cyclooxygenase-2 selective inhibitor and a phosphodiesterase inhibitor for the treatment of ischemic mediated central nervous system disorders or injury
US20050107350A1 (en) * 2003-08-22 2005-05-19 Pharmacia Corporation Method for the treatment or prevention of bone disorders with a cyclooxygenase-2 inhibitor alone and in combination with a bone disorder treatment agent and compositions therewith
US20050085478A1 (en) * 2003-08-22 2005-04-21 Pharmacia Corporation Compositions of a cyclooxygenase-2 selective inhibitor and a low-molecular-weight heparin for the treatment of central nervous system damage
CA2536340A1 (en) * 2003-08-22 2005-03-03 Pharmacia Corporation Compositions of a cyclooxygenase-2 selective inhibitor and a serotonin modulating agent for the treatment of neoplasia
US20050085479A1 (en) * 2003-08-27 2005-04-21 Pharmacia Corporation Mediated central nervous system compositions of a cyclooxygenase-2 selective inhibitor and a corticotropin releasing factor antagonist for the treatment of ischemic disorders or injury
US20050187278A1 (en) * 2003-08-28 2005-08-25 Pharmacia Corporation Treatment or prevention of vascular disorders with Cox-2 inhibitors in combination with cyclic AMP-specific phosphodiesterase inhibitors
AU2004270162B2 (en) * 2003-08-28 2010-05-13 Nicox S.A. Nitrosated ad nitrosylated diuretic compouds, compositions and methods of use
WO2005023189A2 (en) * 2003-09-03 2005-03-17 Pharmacia Corporation Method of cox-2 selective inhibitor and nitric oxide-donating agent
EP1670417A2 (en) * 2003-10-03 2006-06-21 Pharmacia Corporation Compositions of a cyclooxygenase-2 selective inhibitor administered under hypothermic conditions for the treatment of ischenic mediated central nervous system disorders or injury
BRPI0415939A (pt) * 2003-11-12 2007-01-02 Pharmacia & Upjohn Co Llc composições de um inibidor seletivo da ciclooxigenase-2 e um agente de modulação do fator neurotrófico para o tratamento de distúrbios mediados pelo sistema nervoso central
WO2005065684A1 (en) * 2003-12-24 2005-07-21 Pharmacia Corporation Metal salts of parecoxib as prodrugs of the cox-2 inhibitor valdecoxib for the treatment of inflammation, pain and/or fever
EP1708718A1 (en) 2004-01-22 2006-10-11 Pfizer Limited Triazole derivatives which inhibit vasopressin antagonistic activity
EP1755537A4 (en) * 2004-04-14 2009-12-09 Univ Boston METHOD AND COMPOSITIONS FOR PREVENTING OR TREATING PERIODONTOPATHIA
BRPI0510340A (pt) * 2004-04-28 2007-10-30 Pfizer derivados de 3-heterociclil-4-feniltriazol como inibidores do receptor via da vasopressina
RU2007103816A (ru) 2004-07-01 2008-08-10 Мерк энд Ко., Инк. (US) Ингибиторы митотического кинезина
ES2257929B1 (es) * 2004-07-16 2007-05-01 Laboratorios Del Dr. Esteve, S.A. Derivados de pirazolina, procedimiento para su obtencion y utilizacion de los mismos como agentes terapeuticos.
JP2008506768A (ja) * 2004-07-22 2008-03-06 ファルマシア コーポレーション Ｃｏｘ−２選択的阻害剤とｌｔｂ４受容体アンタゴニストを組み合わせて用いる炎症および疼痛を治療するための組成物
WO2006041855A2 (en) 2004-10-04 2006-04-20 Nitromed, Inc. Compositions and methods using apocynin compounds and nitric oxide donors
AU2005304770A1 (en) * 2004-11-08 2006-05-18 Nicox S.A. Nitrosated and nitrosylated compounds, compositions and methods for the treatment of ophthalmic disorders
DE602005013116D1 (de) 2004-12-23 2009-04-16 Glaxo Group Ltd Pyridin-verbindungen für die behandlung von prostaglandin-vermittelten krankheiten
US20080306041A1 (en) * 2005-01-21 2008-12-11 Garvey David S Cardiovascular Compounds Comprising Heterocyclic Nitric Oxide Donor Groups, Compositions and Methods of Use
JP2008530226A (ja) * 2005-02-16 2008-08-07 ニトロメッド インコーポレーティッド 抗微生物化合物の有機酸化窒素供与体塩、組成物、および使用法
US7521435B2 (en) 2005-02-18 2009-04-21 Pharma Diagnostics, N.V. Silicon containing compounds having selective COX-2 inhibitory activity and methods of making and using the same
AU2006218766A1 (en) * 2005-02-28 2006-09-08 Nicox S.A. Cardiovascular compounds comprising nitric oxide enhancing groups, compositions and methods of use
MX2007013304A (es) 2005-04-26 2007-12-13 Pfizer Anticuerpos de p-caderina.
WO2006121887A2 (en) * 2005-05-05 2006-11-16 Cook Biotech Incorporated Implantable materials and methods for inhibiting tissue adhesion formation
ATE550019T1 (de) 2005-05-17 2012-04-15 Merck Sharp & Dohme Cis-4-ä(4-chlorophenyl)sulfonylü-4-(2,5- difluorophenyl)cyclohexanepropansäure zur behandlug von krebs
WO2006123242A1 (en) * 2005-05-18 2006-11-23 Pfizer Limited 1, 2, 4 -triazole derivatives as vasopressin antagonists
US20090048219A1 (en) * 2005-05-23 2009-02-19 Nitromed Inc. Organic nitric oxide donor salts of nonsteroidal antiinflammatory compounds, compositions and methods of use
HUP0500730A2 (en) * 2005-07-29 2007-02-28 Richter Gedeon Vegyuszeti Gyar 1,2-diaryl-heterocyclic compounds, their preparation, pharmaceutical compositions comprising thereof and their use
US20090018091A1 (en) * 2005-08-02 2009-01-15 Nitromed, Inc. Nitric Oxide Enhancing Antimicrobial Compounds, Compositions and Methods of Use
PE20070427A1 (es) * 2005-08-30 2007-04-21 Novartis Ag Compuestos derivados de benzimidazoles sustituidos como inhibidores de tirosina quinasas
MY164457A (en) 2005-09-07 2017-12-15 Amgen Fremont Inc Human monoclonal antibodies to activin receptor-like kinase-1
US8273792B2 (en) * 2005-10-03 2012-09-25 The Brigham And Women's Hospital, Inc. Anti-inflammatory actions of neuroprotectin D1/protectin D1 and it's natural stereoisomers
AU2006299383A1 (en) * 2005-10-04 2007-04-12 Nitromed, Inc. Methods for treating respiratory disorders
WO2007054896A1 (en) 2005-11-08 2007-05-18 Ranbaxy Laboratories Limited Process for (3r, 5r)-7-[2-(4-fluorophenyl)-5-isopropyl-3-phenyl-4- [(4-hydroxy methyl phenyl amino) carbonyl]-pyrrol-1-yl]-3, 5-dihydroxy-heptanoic acid hemi calcium salt
US7838023B2 (en) * 2005-11-16 2010-11-23 Nitromed, Inc. Furoxan compounds, compositions and methods of use
US8636986B2 (en) * 2005-11-18 2014-01-28 The Forsyth Institute Treatment and prevention of bone loss using resolvins
WO2007075541A2 (en) * 2005-12-20 2007-07-05 Nitromed, Inc. Nitric oxide enhancing glutamic acid compounds, compositions and methods of use
NL2000351C2 (nl) 2005-12-22 2007-09-11 Pfizer Prod Inc Estrogeen-modulatoren.
WO2007075542A2 (en) * 2005-12-22 2007-07-05 Nitromed, Inc. Nitric oxide enhancing pyruvate compounds, compositions and methods of use
US20090062302A1 (en) 2006-01-24 2009-03-05 Buser-Doepner Carolyn A Jak2 Tyrosine Kinase Inhibition
GB0603041D0 (en) 2006-02-15 2006-03-29 Angeletti P Ist Richerche Bio Therapeutic compounds
WO2007126609A1 (en) 2006-03-29 2007-11-08 Nitromed, Inc. Nitric oxide enhancing prostaglandin compounds, compositions and methods of use
EP2010528B1 (en) 2006-04-19 2017-10-04 Novartis AG 6-o-substituted benzoxazole and benzothiazole compounds and methods of inhibiting csf-1r signaling
WO2007136790A2 (en) 2006-05-18 2007-11-29 Mannkind Corporation Intracellular kinase inhibitors
WO2008033931A1 (en) * 2006-09-13 2008-03-20 The Institutes For Pharmaceutical Discovery, Llc Para-xylylene carboxylic acids and isothiazolones useful as protein tyrosine phosphatases (ptps) in particular ptp-ib
US8173629B2 (en) 2006-09-22 2012-05-08 Merck Sharp & Dohme Corp. Method of treatment using fatty acid synthesis inhibitors
US20110218176A1 (en) 2006-11-01 2011-09-08 Barbara Brooke Jennings-Spring Compounds, methods, and treatments for abnormal signaling pathways for prenatal and postnatal development
UA94979C2 (uk) 2006-12-22 2011-06-25 Рекордати Айеленд Лимитед КОМБІНОВАНА ТЕРАПІЯ ПОРУШЕНЬ НИЖНІХ СЕЧОВИВІДНИХ ШЛЯХІВ ЛІГАНДАМИ α2δ І НПЗП
RS58936B1 (sr) 2007-01-10 2019-08-30 Msd Italia Srl Indazoli supstituisani amidom kao inhibitori poli(adp-riboza)polimeraze (parp)
KR100843351B1 (ko) * 2007-01-30 2008-07-03 한국과학기술연구원 중추신경계 질환 치료제로 유효한ｎ-벤질-ｎ-(2-디메틸아미노-에틸)-벤젠술폰아미드 화합물
CA2679659C (en) 2007-03-01 2016-01-19 Novartis Ag Pim kinase inhibitors and methods of their use
GB0704407D0 (en) 2007-03-07 2007-04-18 Glaxo Group Ltd Compounds
EP2152700B1 (en) 2007-05-21 2013-12-11 Novartis AG Csf-1r inhibitors, compositions, and methods of use
US8389553B2 (en) 2007-06-27 2013-03-05 Merck Sharp & Dohme Corp. 4-carboxybenzylamino derivatives as histone deacetylase inhibitors
JP2010533205A (ja) 2007-07-12 2010-10-21 トラガラ ファーマシューティカルズ，インク． 癌、腫瘍、および腫瘍関連障害を治療するための方法および組成物
US7943658B2 (en) 2007-07-23 2011-05-17 Bristol-Myers Squibb Company Indole indane amide compounds useful as CB2 agonists and method
MX2010002712A (es) 2007-09-10 2010-06-09 Calcimedica Inc Compuestos que modulan calcio intracelular.
US8598184B2 (en) 2008-03-03 2013-12-03 Tiger Pharmatech Protein kinase inhibitors
GB0813144D0 (en) 2008-07-17 2008-08-27 Glaxo Group Ltd Novel compounds
GB0813142D0 (en) 2008-07-17 2008-08-27 Glaxo Group Ltd Novel compounds
EP2321303B1 (en) 2008-08-27 2019-11-27 Calcimedica, Inc. Compounds that modulate intracellular calcium
EP2177215A1 (en) 2008-10-17 2010-04-21 Laboratorios Del. Dr. Esteve, S.A. Co-crystals of tramadol and NSAIDs
GB0903493D0 (en) 2009-02-27 2009-04-08 Vantia Ltd New compounds
JP5212177B2 (ja) * 2009-02-27 2013-06-19 東レ株式会社 γ−ケトアセタール化合物及びピロール誘導体の製造方法
KR101069175B1 (ko) 2009-04-19 2011-09-30 중앙대학교 산학협력단 신규 아미노설포닐아릴이소옥사졸계 화합물 및 이를 포함하는 다약제내성 억제용 약제학적 조성물
WO2011012622A1 (en) 2009-07-30 2011-02-03 Glaxo Group Limited Benzoxazinone derivatives for the treatment of glytl mediated disorders
WO2011023753A1 (en) 2009-08-27 2011-03-03 Glaxo Group Limited Benzoxazine derivatives as glycine transport inhibitors
CN104945382B (zh) 2009-10-14 2020-02-07 默沙东公司 提高p53活性的取代的哌啶和其用途
GB201000685D0 (en) 2010-01-15 2010-03-03 Glaxo Group Ltd Novel compounds
CN101805290A (zh) * 2010-04-01 2010-08-18 中国人民解放军第四军医大学 氨基磺酰吡唑类化合物及其用途
ES2591004T3 (es) 2010-04-27 2016-11-24 Calcimedica, Inc. Compuestos moduladores del calcio intracelular
CA2797533A1 (en) 2010-04-27 2011-11-10 Calcimedica, Inc. Compounds that modulate intracellular calcium
GB201007791D0 (en) 2010-05-10 2010-06-23 Glaxo Group Ltd Novel compounds
GB201007789D0 (en) 2010-05-10 2010-06-23 Glaxo Group Ltd Novel Compound
US20130072519A1 (en) 2010-05-21 2013-03-21 Edward Lee Conn 2-phenyl benzoylamides
WO2011163330A1 (en) 2010-06-24 2011-12-29 Merck Sharp & Dohme Corp. Novel heterocyclic compounds as erk inhibitors
US9115132B2 (en) 2010-07-09 2015-08-25 Convergence Pharmaceuticals Limited Tetrazole compounds as calcium channel blockers
WO2012018754A2 (en) 2010-08-02 2012-02-09 Merck Sharp & Dohme Corp. RNA INTERFERENCE MEDIATED INHIBITION OF CATENIN (CADHERIN-ASSOCIATED PROTEIN), BETA 1 (CTNNB1) GENE EXPRESSION USING SHORT INTERFERING NUCLEIC ACID (siNA)
US9029341B2 (en) 2010-08-17 2015-05-12 Sirna Therapeutics, Inc. RNA interference mediated inhibition of hepatitis B virus (HBV) gene expression using short interfering nucleic acid (siNA)
EP2606044B1 (en) * 2010-08-20 2014-06-04 Allergan, Inc. Compounds act at multiple prostaglandin receptors giving a general anti-inflammatory response
EP2608669B1 (en) 2010-08-23 2016-06-22 Merck Sharp & Dohme Corp. NOVEL PYRAZOLO[1,5-a]PYRIMIDINE DERIVATIVES AS mTOR INHIBITORS
EP2609095A4 (en) 2010-08-27 2014-06-18 Calcimedica Inc COMPOUNDS MODULATING INTRACELLULAR CALCIUM
EP2613782B1 (en) 2010-09-01 2016-11-02 Merck Sharp & Dohme Corp. Indazole derivatives useful as erk inhibitors
US9242981B2 (en) 2010-09-16 2016-01-26 Merck Sharp & Dohme Corp. Fused pyrazole derivatives as novel ERK inhibitors
US9260471B2 (en) 2010-10-29 2016-02-16 Sirna Therapeutics, Inc. RNA interference mediated inhibition of gene expression using short interfering nucleic acids (siNA)
WO2012087772A1 (en) 2010-12-21 2012-06-28 Schering Corporation Indazole derivatives useful as erk inhibitors
US8933132B2 (en) 2011-01-19 2015-01-13 Convergence Pharmaceuticals Limited Tricyclic substituted benzenesulfonamide piperazine derivatives as CAV2.2 calcium channel blockers
JP2014513923A (ja) 2011-03-04 2014-06-19 ファイザー・インク Ｅｄｎ３様ペプチドおよびその使用
US20140045847A1 (en) 2011-04-21 2014-02-13 Piramal Enterprises Limited Crystalline form of a salt of a morpholino sulfonyl indole derivative and a process for its preparation
EP2770987B1 (en) 2011-10-27 2018-04-04 Merck Sharp & Dohme Corp. Novel compounds that are erk inhibitors
US9221809B2 (en) 2011-10-31 2015-12-29 Merck Sharp & Dohme Corp. Aminopyrimidinones as interleukin receptor-associated kinase inhibitors
US9562015B2 (en) 2011-11-17 2017-02-07 The Regents Of The University Of Colorado, A Body Methods and compositions for enhanced drug delivery to the eye and extended delivery formulations
GB201122113D0 (en) 2011-12-22 2012-02-01 Convergence Pharmaceuticals Novel compounds
EP3453762B1 (en) 2012-05-02 2021-04-21 Sirna Therapeutics, Inc. Short interfering nucleic acid (sina) compositions
MX2015004041A (es) 2012-09-28 2015-07-06 Merck Sharp & Dohme Compuestos novedosos que son inhibidores de erk.
WO2014059333A1 (en) 2012-10-12 2014-04-17 Calcimedica, Inc. Compounds that modulate intracellular calcium
WO2014085216A1 (en) 2012-11-28 2014-06-05 Merck Sharp & Dohme Corp. Compositions and methods for treating cancer
CA2895504A1 (en) 2012-12-20 2014-06-26 Merck Sharp & Dohme Corp. Substituted imidazopyridines as hdm2 inhibitors
EP2951180B1 (en) 2013-01-30 2018-05-02 Merck Sharp & Dohme Corp. 2,6,7,8 substituted purines as hdm2 inhibitors
JP6480909B2 (ja) * 2013-03-15 2019-03-13 ユニバーシティー オブ サウザン カリフォルニア アンギオテンシン関連疾患の処置のための方法、化合物および組成物
WO2015006181A1 (en) 2013-07-11 2015-01-15 Merck Sharp & Dohme Corp. Substituted amidopyrazole inhibitors of interleukin receptor-associated kinases (irak-4)
EP3041938A1 (en) 2013-09-03 2016-07-13 Moderna Therapeutics, Inc. Circular polynucleotides
CN104418818B (zh) * 2013-09-04 2017-01-11 天津汉瑞药业有限公司 帕瑞昔布钠无水化合物
US9611263B2 (en) 2013-10-08 2017-04-04 Calcimedica, Inc. Compounds that modulate intracellular calcium
CN105085425B (zh) * 2014-05-23 2018-01-30 昆药集团股份有限公司 一种制备帕瑞昔布的方法
JO3589B1 (ar) 2014-08-06 2020-07-05 Novartis Ag مثبطات كيناز البروتين c وطرق استخداماتها
GB201417499D0 (en) 2014-10-03 2014-11-19 Convergence Pharmaceuticals Novel use
GB201417500D0 (en) 2014-10-03 2014-11-19 Convergence Pharmaceuticals Novel use
GB201417497D0 (en) 2014-10-03 2014-11-19 Convergence Pharmaceuticals Novel use
CN104557754A (zh) * 2015-01-04 2015-04-29 成都克莱蒙医药科技有限公司 一种帕瑞昔布钠杂质的合成方法
EP3267996B1 (en) 2015-03-12 2020-11-11 Merck Sharp & Dohme Corp. Pyrazolopyrimidine inhibitors of irak4 activity
US10040802B2 (en) 2015-03-12 2018-08-07 Merck Sharp & Dohme Corp. Thienopyrazine inhibitors of IRAK4 activity
EP3268367B8 (en) 2015-03-12 2022-11-16 Merck Sharp & Dohme LLC Carboxamide inhibitors of irak4 activity
WO2017023774A1 (en) * 2015-07-31 2017-02-09 The Johns Hopkins University Prodrugs of glutamine analogs
US9598361B1 (en) * 2016-04-12 2017-03-21 King Saud University Amino substituted acetamide derivative
WO2019094311A1 (en) 2017-11-08 2019-05-16 Merck Sharp & Dohme Corp. Prmt5 inhibitors
CN108299331A (zh) * 2018-03-02 2018-07-20 成都新恒创药业有限公司 一种帕瑞昔布钠光降解杂质及其制备、检测方法和应用
CN108164521B (zh) * 2018-03-02 2020-11-13 成都新恒创药业有限公司 一种帕瑞昔布钠降解杂质及其制备、检测方法和应用
US11981701B2 (en) 2018-08-07 2024-05-14 Merck Sharp & Dohme Llc PRMT5 inhibitors
EP3833668A4 (en) 2018-08-07 2022-05-11 Merck Sharp & Dohme Corp. PRMT5 INHIBITORS
CN110305071A (zh) * 2019-07-23 2019-10-08 成都通德药业有限公司 一种帕瑞昔布钠中间体帕瑞昔布的合成方法
JP2023507634A (ja) 2019-12-17 2023-02-24 メルク・シャープ・アンド・ドーム・エルエルシー Ｐｒｍｔ５阻害剤
US20240165148A1 (en) 2021-03-15 2024-05-23 Saul Yedgar Hyaluronic acid-conjugated dipalmitoyl phosphatidyl ethanolamine in combination with non-steroidal anti-inflammatory drugs (nsaids) for treating or alleviating inflammatory diseases
CN115784991A (zh) * 2022-11-22 2023-03-14 合肥医工医药股份有限公司 N-(苯磺酰基)酰胺衍生物及其制备方法和用途

Family Cites Families (39)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US538738A (en) 1895-05-07 Measuring-faucet
GB911204A (en) 1960-07-28 1962-11-21 Unilever Ltd Bleaching compositions
US4146721A (en) 1969-09-12 1979-03-27 Byk Gulden Lomberg Chemische Fabrik Gmbh Pyrazol-4-acetic acid compounds
US3984431A (en) 1972-03-15 1976-10-05 Claude Gueremy Derivatives of pyrazole-5-acetic acid
DE3321082C2 (de) 1982-06-10 1996-08-22 Kao Corp Bleich-Reinigungsmittel
JPS59145300A (ja) 1983-02-07 1984-08-20 日本パ−オキサイド株式会社 漂白洗剤
JPS6015500A (ja) 1983-07-08 1985-01-26 ライオン株式会社 高嵩密度洗剤組成物
JPS60118606A (ja) 1983-11-28 1985-06-26 Mitsubishi Gas Chem Co Inc 安定化された過炭酸ナトリウム粒状物
US5051518A (en) 1987-05-29 1991-09-24 Ortho Pharmaceutical Corporation Pharmacologically active 2- and 3-substituted (1',5'-diaryl-3-pyrazolyl)-N-hydroxypropanamides
JP2590124B2 (ja) * 1987-08-12 1997-03-12 国際試薬株式会社 水溶性テトラゾリウム化合物およびその化合物を用いる還元性物質の測定方法
JPS6445374U (lv) 1987-09-10 1989-03-20
DE3903993A1 (de) * 1989-02-10 1990-08-16 Basf Ag Diarylsubstituierte heterocyclische verbindungen, ihre herstellung und arzneimittel daraus
JPH04277724A (ja) * 1991-03-06 1992-10-02 Sumitomo Electric Ind Ltd 有機非線形光学材料
GB9113628D0 (en) * 1991-06-25 1991-08-14 Ici Plc Heterocyclic derivatives
US5219856A (en) * 1992-04-06 1993-06-15 E. I. Du Pont De Nemours And Company Angiotensin-II receptor blocking, heterocycle substituted imidazoles
US5334991A (en) 1992-05-15 1994-08-02 Reflection Technology Dual image head-mounted display
JPH05323522A (ja) * 1992-05-20 1993-12-07 Fuji Photo Film Co Ltd 黒白ハロゲン化銀写真感光材料の処理方法
US5604260A (en) * 1992-12-11 1997-02-18 Merck Frosst Canada Inc. 5-methanesulfonamido-1-indanones as an inhibitor of cyclooxygenase-2
CA2152792C (en) * 1993-01-15 2000-02-15 Stephen R. Bertenshaw Novel 3,4-diaryl thiophenes and analogs thereof having use as antiinflammatory agents
US5409944A (en) * 1993-03-12 1995-04-25 Merck Frosst Canada, Inc. Alkanesulfonamido-1-indanone derivatives as inhibitors of cyclooxygenase
CA2161789A1 (en) * 1993-05-13 1994-11-24 Jacques Yves Gauthier 2-substituted-3,4-diarylthiophene derivatives as inhibitors of cyclooxygenase
US5380738A (en) * 1993-05-21 1995-01-10 Monsanto Company 2-substituted oxazoles further substituted by 4-fluorophenyl and 4-methylsulfonylphenyl as antiinflammatory agents
US5474995A (en) * 1993-06-24 1995-12-12 Merck Frosst Canada, Inc. Phenyl heterocycles as cox-2 inhibitors
US5344991A (en) * 1993-10-29 1994-09-06 G.D. Searle & Co. 1,2 diarylcyclopentenyl compounds for the treatment of inflammation
CN1061036C (zh) * 1993-11-30 2001-01-24 G·D·瑟尔公司 用于治疗炎症的取代的吡唑基苯磺酰胺类化合物
US5401765A (en) 1993-11-30 1995-03-28 G. D. Searle 1,4,5-triphenyl pyrazolyl compounds for the treatment of inflammation and inflammation-related disorders
US5434178A (en) 1993-11-30 1995-07-18 G.D. Searle & Co. 1,3,5 trisubstituted pyrazole compounds for treatment of inflammation
US5393790A (en) * 1994-02-10 1995-02-28 G.D. Searle & Co. Substituted spiro compounds for the treatment of inflammation
AU692231B2 (en) * 1994-02-10 1998-06-04 G.D. Searle & Co. Substituted spiro compounds for the treatment of inflammation
US5486534A (en) 1994-07-21 1996-01-23 G. D. Searle & Co. 3,4-substituted pyrazoles for the treatment of inflammation
US5556019A (en) * 1994-07-25 1996-09-17 Sealed Air Corporation Bag separator and dispenser
US5616601A (en) * 1994-07-28 1997-04-01 Gd Searle & Co 1,2-aryl and heteroaryl substituted imidazolyl compounds for the treatment of inflammation
JP3181190B2 (ja) * 1994-12-20 2001-07-03 日本たばこ産業株式会社 オキサゾール誘導体
JP2636819B2 (ja) * 1994-12-20 1997-07-30 日本たばこ産業株式会社 オキサゾール系複素環式芳香族化合物
US5633272A (en) * 1995-02-13 1997-05-27 Talley; John J. Substituted isoxazoles for the treatment of inflammation
US5908858A (en) * 1996-04-05 1999-06-01 Sankyo Company, Limited 1,2-diphenylpyrrole derivatives, their preparation and their therapeutic uses
TR199802049T2 (xx) * 1996-04-12 1999-01-18 G.D.Searle & Co. COX-2 Inhibit�rlerinin �nilac� olarak s�bstit�e edilmi� benzens�lfonamid t�revleri.
JPH1045374A (ja) 1996-08-01 1998-02-17 Nittetsu Mining Co Ltd ドラム缶吊り上げ装置
US20030105144A1 (en) * 2001-04-17 2003-06-05 Ping Gao Stabilized oral pharmaceutical composition

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