TR201907783T4 - Benzosulfonamit türevleri, bileşimleri ve kanser hücrelerinin metastazının önlenmesinde kullanımları. - Google Patents

Benzosulfonamit türevleri, bileşimleri ve kanser hücrelerinin metastazının önlenmesinde kullanımları. Download PDF

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TR201907783T4
TR201907783T4 TR2019/07783T TR201907783T TR201907783T4 TR 201907783 T4 TR201907783 T4 TR 201907783T4 TR 2019/07783 T TR2019/07783 T TR 2019/07783T TR 201907783 T TR201907783 T TR 201907783T TR 201907783 T4 TR201907783 T4 TR 201907783T4
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ethyl
phenylsulfamic acid
phenylsulfamic
ethylthiazol
thiazol
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TR2019/07783T
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Shalwitz Robert
Gene Peters Kevin
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Aerpio Therapeutics Inc
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Abstract

Kanser hücrelerinin metastazının önlenmesi için yöntemler açıklanmaktadır. Açıklanan bileşikler, tümör veya diğer tipteki kanser hücrelerinin yayılmasını önlemek için kullanılabilir.

Claims (10)

ISTEMLER
1. Bir bilesik olup, özelligi; bir gliyoma tasiyan bir insandaki tümör metastazini önlemek, dindirmek, minimize etmek, kontrol etmek ve/veya azaltmak amacina yönelik olmasi, bilesigin, Formül I'e sahip olmasidir: 1m”`x n”`z burada R'nin asagidaki formüle sahip olan ornatilmis veya ornatilmamis bir tiyazolil birimi olmasi: *%IL ag“ %-QI R?, IÜ, ve R4'ün her birinin bagimsiz olarak. asagidakiler olmasidir: i) hidrojen; ii) ornatilmis veya ornatilmamis C1-C6 düz, dalli veya siklik iii) ornatilmis veya ornatilmamis C2-C6 düz, dalli veya siklik alkenil; iv) ornatilmis veya ornatilmamis C2-C6 düz veya dalli alkinil; V) ornatilmis veya ornatilmamis C6 veya Cm aril; vi) ornatilmis veya ornatilmamis Ci-Cg heteroaril; vii) ornatilmis veya ornatilmamis Ci-Cg heterosiklik; veya Viii) R? ve Rß'ün birlikte 5 ila 7 atoma sahip bir doygun veya doymamis halka olusturmalari; burada 1 ila 3 atomun tercihe göre oksijen, nitrojen, ve sülfürden seçilen heteroatomlar olabilmesidir; Z'nin, asagidaki formüle sahip bir birim olmasi: RÃ'in, asagidakilerden seçilmesi: i) hidrojen; ii) hidroksil; iv) ornatilmis veya ornatilmamis C1-C6 düz, dalli veya siklik V) ornatilmis veya ornatilmamis Ci-Cs düz, dalli veya siklik alkoksi; vi) ornatilmis veya ornatilmamis C6 veya Cm aril; Vii) ornatilmis veya ornatilmamis Cy4b heterosiklik; veya viii) ornatilmis veya ornatilmamis Ci-Cg heteroaril; L'nin, asagidaki formüle sahip bir baglantilama birimi olmasi: -[Q]y[C(R5aR5b)]x[Q1]Z[C(RGaR6b)]w- RSa ve Rw'in her birinin bagimsiz olarak asagidakiler olmasi: i) hidrojen; ii) hidroksi; iii) halojen; iv) Cy{b ornatilmis veya ornatilmamis düz veya dalli alkil; V) asagidaki formüle sahip bir birim: Q ve Ql'in her biri bagimsiz olarak asagidakiler olmasi: iv) -NHC(O)-; vi) -NHC(O)O-; viii) -C(O)NHC(O)-; xiv) -NHC(=NH)-; veya R7a ve Rw'in her biri bagimsiz olarak asagidakiler olmasi: 1) hidrojen; veya ii) ornatilmis veya ornatilmamis C1-C6 düz, dalli veya siklik RB'in asagidakiler olmasi: i) hidrojen; ii) ornatilmis veya ornatilmamis C1-C6 düz, dalli veya siklik iii) ornatilmis veya ornatilmamis C6 veya Cm aril; iv) ornatilmis veya ornatilmamis Ci-Cg heteroaril; veya v) ornatilmis veya ornatilmamis Cy4h heterosiklik; R6a ve R%'in her birinin bagimsiz olarak asagidakiler olmasi: i) hidrojen; veya ii) C1-C4 düz veya dalli alkil; n indisinin, (3 veya 1. olmasi; t, vv ve >< indislerinin her birinin bagimsiz olarak 0 ila 4 arasinda olmasi; y ve 2 indislerinin her birinin bagimsiz olarak 0 veya 1 olmasi; veya farmasötik olarak kabul edilebilir bir tuzu olmasidir.
2. Isteni 1'e göre kullanini için Isteni 1'de ortaya konulan sekildeki bir bilesik olup, özelligi; burada kullanimin, terapötik olarak etkili bir miktarda bir kemoterapötik kanser madde veya bir sitotoksik/antineoplastik madde ile kombinasyon halinde olmasidir.
3. Istem Z'ye göre kullanim için, istem 1'de ortaya konulan sekildeki bir bilesik olup, özelligi; burada kemoterapötik kanser maddesi veya sitotoksik/antineoplastik maddesinin, taksol, IL-2, gemsitabin, erlotinib, doksil, irinortekan ve bevacizumab'dan seçilmesidir.
4. Istem 1 ila 3'ün herhangi birine göre kullanim için istem 1'e göre bir bilesik olup, özelligi; burada bilesigin asagidaki formüle sahip olmasidir: ya da bunun farmasötik olarak kabul edilebilir bir tuzu.
5. Istem 1 ila 3'ün herhangi birine göre kullanim için istem 1'e göre bilesik veya farmasötik olarak kabul edilebilir tuzu olup, özelligi; burada bilesigin asagidakilerden seçilmesidir: (S)-4-[2-Benzamido-2-(4-etiltiyazol-2-il)etil]fenilsülfamik asit; (S)-4-{2-(4-etiltiyazol-2-il)-2-[2-(2- florofenil)asetamido]etil}fenil-sülfamik asit; florofenil)asetamido)etil)fenilsülfamik asit; (8)-4-(2-(2- (2,3-Diflorofenil)asetamido)-2-(4-etiltiyazol-2- il)etil)fenilsülfamik asit; (8)-4-(2-(2-(3,4-Diflorofenil)asetamido)-2-(4-etiltiyazol-2- il)etil)fenilsülfamik asit; (8)-4-(2-(2-(2- klorofenil)asetamido)-2-(4-etiltiyazol-2- il)etil)fenilsülfamik asit; (S)-4-(2-(2-(3-klorofenil)asetamido)-2-(4-etiltiyazol-2- il)etil)fenilsülfamik asit; hidroksifenil)asetamido)etil)fenilsülfamik asit; metoksifenil)asetamido)etil)fenilsülfamik asit; metoksifenil)asetamido)etil)fenilsülfamik asit; fenilpropanamido)etil)fenilsülfamik asit; (8)-4-(2-(2-(3,4-Dimetoksifenil)asetamido)-2-(4-etiltiyazol- (S)-4-(2-(2-(2,3-Dimetoksifenil)asetamido)-2-(4-etiltiyazol- (8)-4-(2-(3-(3-klorofenil)propanamido)-2-(4-etiltiyazol-2- il)etil)fenilsülfamik asit; metoksifenil)propanamido)etil)fenilsülfamik asit; metoksifenil)propanamido)etil)fenilsülfamik asit; metoksifenil)propanamido)etil)fenilsülfamik asit; etiltiyazol-Z-il)etil}fenilsülfamik asit; dihidropirimidin-l(2H)-il)asetamit]etil}fenilsülfamik asit; (S)-4-[2-(Benzo[d][l,3]dioksol-S-karboksamido)-2-(4- etiltiyazol-Z-il)etil]-fenilsülfamik asit; 4-(8)-2-(2-(2-klorofenil)asetamido)-2-(2-(tiyofenZ- il)tiyazol-4-il)etil)-fenilsülfamik asit; 4-(S)-2-(2-(3-Metoksifenil)asetamido)-2-(2-(tiyofen2- il)tiyazol-4-il)etil)-fenilsülfamik asit; 4-{(8)-2-(3-fenilpropanamido)-2-[2-(tiyofenZ-il)tiyazol-4- il]etil}fenilsülfamik asit; 4-{(8)-2-(3-(3-klorofenil)propanamido)-2-[2-(tiyofenZ- il)tiyazol-4-il]etil}-fenilsülfamik asit; 4-{(8)-2-[2-(3-florofenil)asetamit]-2-[2-(tiyofen2- il)tiyazol-4-il]etil}-fenilsülfamik asit; (S)-4-{2-[2-(2,5-Dimetiltiyazol-4-il)asetamit]-2-(4- etiltiyazol-Z-il]etil}-fenilsülfamik asit; (S)-4-{2-[2-(2,4-Dimetiltiyazol-5-il)asetamit]-2-(4- metiltiyazol-Z-iletil}-fenilsülfamik asit; il)propanamido]etil}fenilsülfamik asit; il)asetamit]etil}fenilsülfamik asit; feniltiyazol-4-il)etil}fenilsülfamik asit; (tiyofen-2-il)tiyazol-4-il]etil}fenilsülfamik asit; (8)-4-(2-(2,3-Difenilpropanamido)-2-(4-etiltiyazol-2- il)etil)fenilsülfamik asit; (S)-4-{2-(4-etiltiyazol-2-il)-2-[2-(2-metoksifenil)-3- fenilpropanamido]-etil)fenilsülfamik asit; (S)-4-{2-(4-etiltiyazol-2-il)-2-[2-(3-florofenil)-3- fenilpropanamido]-etil}fenilsülfamik asit; (S)-4-{2-(4-etiltiyazol-2-il)-2-[2-(3-metoksifenil)-3- fenilpropanamido]-etil}fenilsülfamik asit; 5-il)-3-fenilpropanamido]etil}fenilsülfamik asit; (8)-4-[2-(4-etiltiyazol-2-il)-2-(4-okso-4-fenilbutanamido)- etil]fenilsülfamik asit; oksoheksanamido)etil)fenilsülfamik asit; (S)-4-{2-[4-(3,4-Dihidro-2H-benzo[b][l,4]dioksepin-7-il)-4- oksobutanamido]-2-(4-etiltiyazol-2-il)etil}fenilsülfamik (S)-4-{2-[4-(2,3-Dimetoksifenil)-4-oksobutanamido]-2-(4- etiltiyazol-Z-il)etil}fenilsülfamik asit; (S)-4-{2-(4-etiltiyazol-2-il)-2-[4-okso-4-(piridin-2- il)butanamido]etil}fenilsülfamik asit; (S)-4-{2-[4-(2,3-Dihidrobenzo[b][1,4]dioksin-6-il)-4- oksobutanamido]-2-(4-etiltiyazol-2-il)etil}fenilsülfamik (S)-4-(2-(4-tert-butoksi-4-oksobutanamido)-2-(4-etiltiyazol- 2-il)etil]fenilsülfamik asit; (8)-4-(2-(4-etoksi-4-oksobutanamido)-2-(4-etiltiyazol-2- il)etil]fenilsülfamik asit; (8)-4-(2-(3-benzilureido)-2-(4-etiltiyazol-2- il)etil)fenilsülfamik asit; 4-{[(S)-2-(2-etiltiyazol-4-il)-2-(3-(R)-1metoksi-l-okso-3- fenilpropan-Z-il)ureido]etil}fenilsülfamik asit; 4-{(8)-2-(3-benzilureido)-2-{2-(tiyofen-Z-il)tiyazol-4- il]etil}fenilsülfamik asit; {4-(S)-[2-fenilmetansülfonilamino-Z-(2-tiy0fen-2-iltiyazol-4- il)etil]-fenilsülfamik asit; 4-{(S)-2-[(2-metiltiyazol-4-il)metilsülfonamido]-2-[2- (tiyofen-Z-il)tiyazol-4-il]etil}fenilsülfamik asit; {4-(S)-[2-fenilmetansülfonilamine-2-(2-etiltiyazol-4- il)etil]fenil}-sülfamik asit; {4-(S)42-(3-Metoksifenil)metansülfonilamino-Z-(2-etiltiyazol- 4-il)etil]fenil} sülfamik asit; sülfoaminofenil)etilsülfamoil]metil}-benzoik asit metil (8)-4-[2-(2-etiltiyazol-4-il)-2(l-metil-lH-imidazol-4- sülfonamido)etil]-fenilsülfamik asit; 4-{(8)-2-[2-(tiyofen-Z-il)tiyazol-4-il]-2-(2,2,2- trifloroetilsülfonamido)-etil}fenilsülfamik asit; {4-(S)42-(feniletansülfonilamino)-2-(2tiyofen-2-iltiyazol-4- il)etil]-fenil}sülfamik asit; {4-(8)-[3-(fenilpropansülfonilamino)-2-(2tiyofen-2-iltiyazol- 4-il)etil]-fenil}sülfamik asit; (S)-{4-[2-(4-metil-3,4-dihidro-2H-benzo[1,4]oksazin-7- sülfonilamino)-2-(2-tiyofen-2-iltiyazol-4- il)etil]fenil}sülfamik asit; 4-{(8)-2-(4-asetamidofenilsülfonamido)-2-[2-(tiyofen-2- il)tiyazol-4-il]etil]fenilsülfamik asit; 4-{(8)-2-(2-siklopropiltiyazol-4-il)-2-[4-(3-metoksifenil)- tiyazol-Z-ilamino] etil }fenilsülfamik asit; (S)-4-(2-(4-((2-Metoksi-2-oksoetil)karbamoil)tiyazol-5- ilamino)2-(2-etiltiyazol-4-il)etil)fenilsülfamik asit; 4-((5)-2-(5-(1-N-(2-Metoksi-2-oksoetil)-1-H-indol-3- il)oksazol-2-ilamino)-2-(2-metiltiyazol-4- il)etil))fenilsülfamik asit; 4-(8)-2-(5-(2-Metoksifenil)oksazol-Z-ilamino)-2-(2- metiltiyazol-4-il)etil)-fenilsülfamik asit; 4-((S)-2-(5-((8)-1-(tert-butoksikarbonil)-2- feniletil)oksazol-Z-ilamino)-2-(2-metiltiyazol-4- il)etil)fenilsülfamik asit; (8)-4-(2-(5-(4-Metoksikarbonil)fenil)oksazol-2-ilamino)2-(2- metiltiyazol-4-il)etil)fenilsülfamik asit; (8)-4-(2-(5-(3-Metoksibenzil)oksazol-2-ilamino)-2-(2- metiltiyazol-4-il)etil)-fenilsülfamik asit; (8)-4-(2-(2-metiltiyazol-4-il)2-(5-feniloksazol-2- ilamino)etil)fenilsülfamik asit; 4-((8)-2-(2-siklopropiltiyazol-4-il)-2-(4-(3- metoksifenil)tiyazol-2-ilamino)-etil)fenilsülfamik asit; (8)-4-(2-(2-siklopropiltiyazol-4-il)-2-(4-(4- florofenil)tiyazol-Z-ilamino)etil)-fenilsülfamik asit; 4-((8)-2-(2-siklopropiltiyazol-4-il)-2-(4-(2- metoksifenil)tiyazol-Z-ilamino)-etil)fenilsülfamik asit; 4-((S)-2-(2-siklopropiltiyazol-4-il)-2-(4-(2,4- diflorofenil)tiyazol-Z-ilamino)-etil)fenilsülfamik asit; (8)-4-(2-(4-(3-metoksibenzil)tiyazol-Z-ilamino)-2-(2- siklopropiltiyazol-4-il)etil)fenilsülfamik asit; sülfoaminofenil)etilamino]-2-metil-2H-[l,2,4]triazol-3- il}karbamik asit metil ester; 4-{(8)-2-[4-(2-Metoksifenil)tiyazol-Z-ilamino)-2-[2-(tiyofen- 2-il)tiyazol-4-il]etil]fenilsülfamik asit; 4-{(5)-2-[5-(3-Metoksifenil)oksazol-Z-ilamino]-2-(2- feniltiyazol-4-il)etil}fenilsülfamik asit; 4-{(S)-2-[4-(2,4-Diflorofenil)tiyazol-Z-ilamino]-2-[2- (tiyofen-Z-il)tiyazol-4-il]etil]fenilsülfamik asit; (S)-4-{2-[4-(etoksikarbonil)tiyazol-Z-ilamino]-2-(2- feniltiyazol-4-il)etil}-fenilsülfamik asit; (S)-4-{2-[4-(2-etoksi-2-oksoetil)tiyazol-Z-ilamino]-2-(2- feniltiyazol-4-il)etil)fenilsülfamik asit; (S)-4-{2-[4-(4-asetamidofenil)tiyazol-2-ilamino]-2-(2- feniltiyazol-4-il)etil}fenilsülfamik asit; (8)-4-[2-(4-feniltiyazol-Z-ilamino)-2-(2-feniltiyazol-4- il)etil]fenilsülfamik asit; (S)-4-{2-[4-(4-(Metoksikarbonil)fenil)tiyazol-2-ilamino]-2- (2-feniltiyazol-4-il)etil}fenilsülfamik asit; 4-{(5)-2-[4-(etoksikarbonil)tiyazol-2-ilamino]-2-[2-(tiyofen- 2-il)tiyazol-4-il]etil}fenilsülfamik asit; (8)-4-[2-(4-(Metoksikarbonil)tiyazol-S-ilamino)-2-(2- feniltiyazol-4-il)etil]-fenilsülfamik asit; (S)-4-[2-(5-feniloksazol-Z-ilamino)]-2-(2-feniltiyazol-4- il)fenilsülfamik asit; (S)-4-{2-[5-(4-asetamidofenil)oksazol-Z-ilamino]-2-(2- feniltiyazol-4-il)etil}fenilsufamik asit; 4-((8)-2-(5-(2,4-Diflorofenil)oksazol-Z-ilamino)-2-(2- feniltiyazol-4-il)etil)fenilsülfamik asit; 4-{(8)-2-[5-(3-Metoksifenil)oksazol-Z-ilamino]-2-[(2-tiyofen- 2-il)tiyazol-4-il]etil]fenilsülfamik asit; (5)-4-[2-(4,6-Dimetilpirimitne-2-ilamino)-2-(2-metiltiyazol- (8)-4-[2-(4-hidroksi-6-metilpirimidin-Z-ilamino)-2-(2- metiltiyazol-4-il)etil]fenilsülfamik asit; 4-{(S)-2-[(8)-2-(tert-butoksikarbonilamino)-3- fenilpropanamido]-2-(4-etiltiyazol-2-il)etil}fenilsülfamik 4-{(S)-2-[(R)-2-(tert-butoksikarbonilamino)-3- fenilpropanamido]-2-(4-etiltiyazol-2-il)etil}fenilsülfamik {l-[l-(S-etiltiyazol-Z-il)-(S)-2-(4- sülfoaminofenil)etilkarbamoil]-(S)-2-feniletil}metil karbamik asit tert-butil ester; {(S)-2-fenil-1-[1-(4-feniltiyazol-2-il)-(8)-2-(4- sülfoaminofenil)etilkarbamoil]etil}karbamik asit tert-butil 4-{(S)-2-(S)-2-(tert-butoksikarbonilamino)-3- fenilpropanamido-2-(2-feniltiyazol-4-il)}fenilsülfamik asit; (metoksikarbonilamino)-3-fenil-propanamido]etil}fenilsülfamik 4-{(S)-2-[(8)-2-(Metoksikarbonilamino)-3-fenilpropanamido]-2- (tiyazol-Z-il)etil}fenilsülfamik asit; 4-{(S)-2-[(8)-2-(Metoksikarbonilamino)-3-fenilpropanamido]-2- (4-metiltiyazol-2-il)etil}fenilsülfamik asit; 4-{(S)-2-[(8)-2-(Metoksikarbonilamino)-3-fenilpropanamido]-2- (4-propiltiyazol-2-il)etil}fenilsülfamik asit; 4-{(8)-2-(4-tert-butiltiyazol-2-il)-2-[(8)-2- (metoksikarbonilamino)-3-fenilpropanamido]etil}fenilsülfamik 4-{(8)-2-(4-siklopropiltiyazol-Z-il)-2-[(8)-2- (metoksikarbonilamino)-3-fenilpropanamido]etil}fenilsülfamik 4-{(8)-2-(4-sikloheksiltiyazol-2-il)-2-[(8)-2- (metoksikarbonilamino)-3-fenil-propanamido]etil }fenilsülfamik asit; 4-{(8)-2-(4,5-Dimetiltiyazol-2-il)-2-[(8)-2- (metoksikarbonilamino)-3-fenil-propanamido]etil}fenilsülfamik 4-{(S)-2-fenil-l-[1-(2-feniltiyaZOl-4-il)-(S)-2-(4- sülfoaminofenil)etilkarbamoil]etil}karbamik asit tert-butil 4-{(8)-2-(4-etil-5-metiltiyazol-2-il)-2-[(S)-2- (metoksikarbonilamino)-3-fenil-propanamido]etil}fenilsülfamik 4-{(S)-2-[(S)-2-(Metoksikarbonilamino)-3-fenilpropanamido]-2- 4-{(S)-2-[(8)-2-(Metoksikarbonilamino)-3-fenilpropanamido)-2- 4-{(8)-2-[4-(2,2-Diflorosiklopropil)tiyazol-Z-il]-2-[(8)-2- (metoksikarbonilamino)-3-fenilpropanamido]etil}fenilsülfamik 4-{(S)-2-[(8)-2-(Metoksikarbonilamino)-3-fenilpropanamido]- 244-(metoksimetil)tiyazol-Z-il]etil}fenilsülfamik asit; 4-{(8)-2-(4-(etoksikarbonilamino)tiyazol-Z-il)-2-[(8)-2- (metoksikarbonilamino)-3-fenilpropanamido]etil}fenilsülfamik 4-{(S)-2-[(8)-2-(Metoksikarbonilamino)-3-fenilpropanamido]-2- (5-feniltiyazo)-2-il))etil}fenilsülfamik asit; 4-{(8)-2-(4-tert-butiltiyazol-2-il)-2-[(8)-2- (metoksikarbonilamino)-3-fenil-propanamido]etil }fenilsülfamik asit; 4-{(8)-2-(4-etil-5-feniltiyazol-2-il)-2-[(8)-2- (metoksikarbonilamino)-3-fenil-propanamido]etil}fenilsülfamik (metoksikarbonilamino)-3-fenilpropanamido]etil}fenilsülfamik 4-{(8)-2-[4-(4-klorofenil)tiyazol-Z-il]-2-[(8)-2- (metoksikarbonilamino)-3-fenilpr0panamido]etil}fenilsülfamik 4-{(S)-2-[(S)-2-(Metoksikarbonilamino)-3-fenilpropanamido]-2- (4-feniltiyazol-2-il)etil}fenilsülfamik asit; 4-{(S)-2-[(8)-2-(Metoksikarbonilamino)-3-fenilpropanamido]-2- 4-(tiyofen-Z-il)tiyazol-2-il]etil}fenilsülfamik asit; 4-{(S)-2-[(8)-2-(Metoksikarbonilamino)-3-fenilpropanamido]-2- 4-(tiyofen-3-il)tiyazol-Z-il]etil}fenil-sülfamik asit; 4-{(S)-2-(4-etiltiyazol-2-il)-2-[(S)-2-(metoksikarbinil)-3- fenilpropiyon-amido]etil}fenilsülfamik asit; 4-{(8)-2-(5,6-Dihidro-4H-siklopenta[d]tiyazol-Z-il)-2-[(8)-2- (metoksi-karbonil)-3-fenilpropanamido]etil}fenilsülfamik 4-{(S)-2-[(S)-2-(Metoksikarbonilamino)-3-fenilpropanamido]-2- (4,5,6,7-tetrahidrobenzo[d]tiyazol-2-il)etil}fenilsülfamik 4-{(8)-2-[4-(S-klorotiyofen-Z-il)tiyazol-Z-il]-2-[(8)-2- (metoksikarbonilamino)-3-fenilpropanamido]etil}fenilsülfamik 4-{(S)-2-[(5)-2-(etoksikarbonilamino)-3-fenilpropanamido]-2- (4-etiltiyazol-2-il)etil}fenilsülfamik asit; 4-{(S)-2-[(8)-2-(Metoksikarbonilamino)-3-fenilpropanamido]-2- (2-etiltiyazol-4-il)etil}fenilsülfamik asit; 4-{(S)-2-[(8)-2-(Metoksikarbonilamino)-3-fenilpropanamido]-2- (2-metil-tiyazol-4-il)etil}fenilsülfamik asit; (metoksikarbonilamino)-3-fenilpropan-amido]etil}fenilsülfamik 4-{(8)-2-(2-lsopropiltiyazol-4-il)-2-[(5)-2- (metoksikarbonilamino)-3-fenil-propan- 4-{(8)-2-(2-siklopropiltiyazol-4-il)-2-[(8)-2- (metoksikarbonilamino)-3-fenilpropanamido]etil}fenilsülfamik 4-{(S)-2-{2-[(4-klorofenilsülfonil)metil]tiyazol-4-il}-2- fenilpropanamido]etil}fenilsülfamik asit; 4-{(8)-2-[2-(tert-butilsülfonilmetil)tiyazol-4-il]-2-[(8)-2- (metoksikarbonilamino)-3-fenilpropanamido]etil}fenilsülfamik 4-{(S)-2-[(8)-2-(Metoksikarbonilamino)-3-fenilpropiyonamido]- 2-(2-fenil-tiyazol-4-il)etil}fenilsülfamik asit; 4-{(S)-2-[(S)-2-(Metoksikarbonilamino)-3-fenilpropanamido]-2- (metoksikarbonilamino)-3-fenilpropanamido]etil}fenilsülfamik 4-{(S)-2-[(S)-2-(Metoksikarbonilamino)-3-fenilpropanamido]-2- 4-{[(8)-2-(2-(Furan-Z-il)tiyazol-4-il]-2-[(S)-2- (metoksikarbonilamino)-3-fenil-propanamido]etil}fenilsülfamik 4-{(S)-2-[(S)-2-(Metoksikarbonilamino)-3-fenilpropanamido]-2- 4-{(S)-2-[(S)-2-(Metoksikarbonilamino)-3-fenilpropanamido]-2- (Z-pirazin-Z-il)tiyazol-4-il}fenilsülfamik asit; 4-{(S)-2-[(8)-2-(Metoksikarbonilamino)-3-fenilpropanamido]- 24-{2-(6-metil-piridin-3-il)tiyazol-4-il}etil}fenilsülfamik 4-[(S)-2-((S)-2-asetamido-3-fenilpropanamido)-2-(4- etiltiyazol-Z-il)etil]-fenilsülfamik asit; 4-[(8)-24(S)-2-asetamido-B-fenilpropanamido)-2-(4-tert- butiltiyazol-Z-il)etil]-fenilsülfamik asit; 4-{(S)-2-((S)-2-asetamido-3-fenilpropanamido)-2-[4-(tiyofen- 3-il)tiyazol-2-il]etil)fenilsülfamik asit; 4-{(S)-2-[(S)-2-(tert-butoksikarbonil)-3-metilbutanamido]-2- (4-etiltiyazol-2-il)etil}fenilsülfamik asit; (S)-4-{2-[2-(tert-butoksikarbonil)asetamit]-2-(4-etiltiyazol- 2-il)etil}fenilsülfamik asit; (metoksikarbonil)asetamido]etil}fenilsülfamik asit; 4-{(8)-2-(4-etiltiyazol-2-il)-2-[(8)-2-(metoksikarbonil)-3- metilbutanamido]-etil}fenilsülfamik asit; 4-{(S)-2-[(8)-2-(tert-butoksikarbonil)-4-metilpentanamido]-2- (4-etiltiyazol-2-il)etil}fenilsülfamik asit; 4-{(8)-2-(4-etiltiyazol-2-il)-2-[(5)-2-(metoksikarbonil)-4- metilpentan-amido]etil}fenilsülfamik asit; (metoksikarbonil)asetamit]-3- fenilpropanamido}etil)fenilsülfamik asit; 4-{(S)-2-[(8)-2-(tert-butoksikarbonil)-4-metilpentanamido]-2- 4-{(S)-2-[(S)-2-(Metoksikarbonil)-4-metilpentanamido]-2-[2- (tiyofen-Z-il)tiyazol-4-il]etil}fenilsülfamik asit; ve (S)-4-{2-[2-(tert-butoksikarbonil)asetamit]-2-(4-etiltiyazol-
6. Istem 1 ila 3'ün herhangi birine göre kullanim için istem 5 l'e göre bilesik veya bir farmasötik olarak kabul edilebilir tuzu olup, özelligi; burada bilesigin asagidakilerden seçilmesidir:
7. Istemler 1 ila 6'nin herhangi birine göre kullanim için Istemler l, 4 veya 5'in herhangi birine göre bir bilesigin bir farmasötik olarak kabul edilebilir tuzu olup, özelligi; burada bilesigin, amonyum, sodyum, lityum, potasyum, 15 kalsiyum, magnezyum, bizmut ve lizinden seçilen bir katyonlu bir tuz biçiminde olmasidir.
8. Istem 1 ila 7'nin herhangi birine göre kullanim için istemler l, 4, 5 veya 6'nin herhangi birine göre bir bilesik olup, özelligi; burada kullanimin, kontrole göre metastazda 20 en az %10'luk bir azalmaya neden olmasidir.
9. Istem 1 ila 7'nin herhangi birine göre kullanim için istemler 1, 4, 5 veya 6'nin herhangi birine göre bir bilesik olup, özelligi; burada kullanimin, kontrole göre metastazda en az yaklasik %50'lik bir azalmaya neden olmasidir.
10. Istem 1 ila 7'nin herhangi birine göre kullanim için istemler l, 4, 5 veya 6'nin herhangi birine göre bilesik kontrole göre metastazda olup, özelligi; burada kullanimin, en az yaklasik o/8O'lik bir azalmaya neden olmasidir.
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