                         SEQUENCE LISTING

<110>  Eli Lilly
 
<120>  FIBROBLAST GROWTH FACTOR RECEPTOR-3 (FGFR-3) INHIBITORS AND 
       METHODS OF TREATMENT

<130>  X18531

<160>  12    

<170>  PatentIn version 3.5

<210>  1
<211>  10
<212>  PRT
<213>  Artificial Sequence

<220>
<223>  Synthetic

<400>  1

Gly Tyr Met Phe Thr Ser Tyr Gly Ile Ser 
1               5                   10  


<210>  2
<211>  17
<212>  PRT
<213>  Artificial Sequence

<220>
<223>  Synthetic

<400>  2

Trp Val Ser Thr Tyr Asn Gly Asp Thr Asn Tyr Ala Gln Lys Phe Gln 
1               5                   10                  15      


Gly 
    


<210>  3
<211>  17
<212>  PRT
<213>  Artificial Sequence

<220>
<223>  Synthetic

<400>  3

Val Leu Gly Tyr Tyr Asp Ser Ile Asp Gly Tyr Tyr Tyr Gly Met Asp 
1               5                   10                  15      


Val 
    


<210>  4
<211>  11
<212>  PRT
<213>  Artificial Sequence

<220>
<223>  Synthetic

<400>  4

Gly Gly Asn Asn Ile Gly Asp Lys Ser Val His 
1               5                   10      


<210>  5
<211>  7
<212>  PRT
<213>  Artificial Sequence

<220>
<223>  Synthetic

<400>  5

Leu Asp Thr Glu Arg Pro Ser 
1               5           


<210>  6
<211>  11
<212>  PRT
<213>  Artificial Sequence

<220>
<223>  Synthetic

<400>  6

Gln Val Trp Asp Ser Gly Ser Asp His Val Val 
1               5                   10      


<210>  7
<211>  126
<212>  PRT
<213>  Artificial Sequence

<220>
<223>  Synthetic

<400>  7

Glu Val Gln Leu Val Gln Ser Gly Ala Glu Val Lys Lys Pro Gly Ala 
1               5                   10                  15      


Ser Val Lys Val Ser Cys Lys Ala Ser Gly Tyr Met Phe Thr Ser Tyr 
            20                  25                  30          


Gly Ile Ser Trp Val Arg Gln Ala Pro Gly Gln Gly Leu Glu Trp Met 
        35                  40                  45              


Gly Trp Val Ser Thr Tyr Asn Gly Asp Thr Asn Tyr Ala Gln Lys Phe 
    50                  55                  60                  


Gln Gly Arg Val Thr Val Thr Thr Asp Thr Ser Thr Ser Thr Ala Tyr 
65                  70                  75                  80  


Met Glu Leu Arg Ser Leu Arg Ser Glu Asp Thr Ala Val Tyr Tyr Cys 
                85                  90                  95      


Ala Arg Val Leu Gly Tyr Tyr Asp Ser Ile Asp Gly Tyr Tyr Tyr Gly 
            100                 105                 110         


Met Asp Val Trp Gly Gln Gly Thr Thr Val Thr Val Ser Ser 
        115                 120                 125     


<210>  8
<211>  109
<212>  PRT
<213>  Artificial Sequence

<220>
<223>  Synthetic

<400>  8

Gln Ser Val Leu Thr Gln Pro Pro Ser Leu Ser Val Ala Pro Gly Lys 
1               5                   10                  15      


Thr Ala Thr Phe Thr Cys Gly Gly Asn Asn Ile Gly Asp Lys Ser Val 
            20                  25                  30          


His Trp Tyr Arg Gln Lys Pro Gly Gln Ala Pro Val Leu Val Met Tyr 
        35                  40                  45              


Leu Asp Thr Glu Arg Pro Ser Gly Ile Pro Glu Arg Met Ser Gly Ser 
    50                  55                  60                  


Asn Phe Gly Asn Thr Ala Thr Leu Thr Ile Thr Arg Val Glu Ala Glu 
65                  70                  75                  80  


Asp Glu Ala Asp Tyr Tyr Cys Gln Val Trp Asp Ser Gly Ser Asp His 
                85                  90                  95      


Val Val Phe Gly Gly Gly Thr Lys Leu Thr Val Leu Gly 
            100                 105                 


<210>  9
<211>  456
<212>  PRT
<213>  Artificial Sequence

<220>
<223>  Synthetic

<400>  9

Glu Val Gln Leu Val Gln Ser Gly Ala Glu Val Lys Lys Pro Gly Ala 
1               5                   10                  15      


Ser Val Lys Val Ser Cys Lys Ala Ser Gly Tyr Met Phe Thr Ser Tyr 
            20                  25                  30          


Gly Ile Ser Trp Val Arg Gln Ala Pro Gly Gln Gly Leu Glu Trp Met 
        35                  40                  45              


Gly Trp Val Ser Thr Tyr Asn Gly Asp Thr Asn Tyr Ala Gln Lys Phe 
    50                  55                  60                  


Gln Gly Arg Val Thr Val Thr Thr Asp Thr Ser Thr Ser Thr Ala Tyr 
65                  70                  75                  80  


Met Glu Leu Arg Ser Leu Arg Ser Glu Asp Thr Ala Val Tyr Tyr Cys 
                85                  90                  95      


Ala Arg Val Leu Gly Tyr Tyr Asp Ser Ile Asp Gly Tyr Tyr Tyr Gly 
            100                 105                 110         


Met Asp Val Trp Gly Gln Gly Thr Thr Val Thr Val Ser Ser Ala Ser 
        115                 120                 125             


Thr Lys Gly Pro Ser Val Phe Pro Leu Ala Pro Ser Ser Lys Ser Thr 
    130                 135                 140                 


Ser Gly Gly Thr Ala Ala Leu Gly Cys Leu Val Lys Asp Tyr Phe Pro 
145                 150                 155                 160 


Glu Pro Val Thr Val Ser Trp Asn Ser Gly Ala Leu Thr Ser Gly Val 
                165                 170                 175     


His Thr Phe Pro Ala Val Leu Gln Ser Ser Gly Leu Tyr Ser Leu Ser 
            180                 185                 190         


Ser Val Val Thr Val Pro Ser Ser Ser Leu Gly Thr Gln Thr Tyr Ile 
        195                 200                 205             


Cys Asn Val Asn His Lys Pro Ser Asn Thr Lys Val Asp Lys Arg Val 
    210                 215                 220                 


Glu Pro Lys Ser Cys Asp Lys Thr His Thr Cys Pro Pro Cys Pro Ala 
225                 230                 235                 240 


Pro Glu Leu Leu Gly Gly Pro Ser Val Phe Leu Phe Pro Pro Lys Pro 
                245                 250                 255     


Lys Asp Thr Leu Met Ile Ser Arg Thr Pro Glu Val Thr Cys Val Val 
            260                 265                 270         


Val Asp Val Ser His Glu Asp Pro Glu Val Lys Phe Asn Trp Tyr Val 
        275                 280                 285             


Asp Gly Val Glu Val His Asn Ala Lys Thr Lys Pro Arg Glu Glu Gln 
    290                 295                 300                 


Tyr Asn Ser Thr Tyr Arg Val Val Ser Val Leu Thr Val Leu His Gln 
305                 310                 315                 320 


Asp Trp Leu Asn Gly Lys Glu Tyr Lys Cys Lys Val Ser Asn Lys Ala 
                325                 330                 335     


Leu Pro Ala Pro Ile Glu Lys Thr Ile Ser Lys Ala Lys Gly Gln Pro 
            340                 345                 350         


Arg Glu Pro Gln Val Tyr Thr Leu Pro Pro Ser Arg Glu Glu Met Thr 
        355                 360                 365             


Lys Asn Gln Val Ser Leu Thr Cys Leu Val Lys Gly Phe Tyr Pro Ser 
    370                 375                 380                 


Asp Ile Ala Val Glu Trp Glu Ser Asn Gly Gln Pro Glu Asn Asn Tyr 
385                 390                 395                 400 


Lys Thr Thr Pro Pro Val Leu Asp Ser Asp Gly Ser Phe Phe Leu Tyr 
                405                 410                 415     


Ser Lys Leu Thr Val Asp Lys Ser Arg Trp Gln Gln Gly Asn Val Phe 
            420                 425                 430         


Ser Cys Ser Val Met His Glu Ala Leu His Asn His Tyr Thr Gln Lys 
        435                 440                 445             


Ser Leu Ser Leu Ser Pro Gly Lys 
    450                 455     


<210>  10
<211>  214
<212>  PRT
<213>  Artificial Sequence

<220>
<223>  Synthetic

<400>  10

Gln Ser Val Leu Thr Gln Pro Pro Ser Leu Ser Val Ala Pro Gly Lys 
1               5                   10                  15      


Thr Ala Thr Phe Thr Cys Gly Gly Asn Asn Ile Gly Asp Lys Ser Val 
            20                  25                  30          


His Trp Tyr Arg Gln Lys Pro Gly Gln Ala Pro Val Leu Val Met Tyr 
        35                  40                  45              


Leu Asp Thr Glu Arg Pro Ser Gly Ile Pro Glu Arg Met Ser Gly Ser 
    50                  55                  60                  


Asn Phe Gly Asn Thr Ala Thr Leu Thr Ile Thr Arg Val Glu Ala Glu 
65                  70                  75                  80  


Asp Glu Ala Asp Tyr Tyr Cys Gln Val Trp Asp Ser Gly Ser Asp His 
                85                  90                  95      


Val Val Phe Gly Gly Gly Thr Lys Leu Thr Val Leu Gly Gln Pro Lys 
            100                 105                 110         


Ala Ala Pro Ser Val Thr Leu Phe Pro Pro Ser Ser Glu Glu Leu Gln 
        115                 120                 125             


Ala Asn Lys Ala Thr Leu Val Cys Leu Ile Ser Asp Phe Tyr Pro Gly 
    130                 135                 140                 


Ala Val Thr Val Ala Trp Lys Ala Asp Ser Ser Pro Val Lys Ala Gly 
145                 150                 155                 160 


Val Glu Thr Thr Thr Pro Ser Lys Gln Ser Asn Asn Lys Tyr Ala Ala 
                165                 170                 175     


Ser Ser Tyr Leu Ser Leu Thr Pro Glu Gln Trp Lys Ser His Arg Ser 
            180                 185                 190         


Tyr Ser Cys Gln Val Thr His Glu Gly Ser Thr Val Glu Lys Thr Val 
        195                 200                 205             


Ala Pro Ala Glu Cys Ser 
    210                 


<210>  11
<211>  795
<212>  PRT
<213>  Homo sapiens

<400>  11

Met Gly Ala Pro Ala Cys Ala Leu Ala Leu Cys Val Ala Val Ala Ile 
1               5                   10                  15      


Val Ala Gly Ala Ser Ser Glu Ser Leu Gly Thr Glu Gln Arg Val Val 
            20                  25                  30          


Gly Arg Ala Ala Glu Val Pro Gly Pro Glu Pro Gly Gln Glu Leu Val 
        35                  40                  45              


Phe Gly Ser Gly Asp Ala Val Glu Leu Ser Cys Pro Pro Pro Gly Gly 
    50                  55                  60                  


Gly Pro Met Gly Pro Thr Val Trp Val Lys Asp Gly Thr Gly Leu Val 
65                  70                  75                  80  


Pro Ser Glu Arg Val Leu Val Gly Pro Gln Arg Leu Val Leu Asn Ala 
                85                  90                  95      


Ser His Glu Asp Ser Gly Ala Tyr Ser Cys Arg Gln Arg Leu Thr Arg 
            100                 105                 110         


Val Leu Cys His Phe Ser Val Arg Val Thr Asp Ala Pro Ser Ser Gly 
        115                 120                 125             


Asp Asp Glu Asp Gly Glu Asp Glu Ala Glu Asp Thr Gly Val Asp Thr 
    130                 135                 140                 


Gly Ala Pro Tyr Trp Thr Arg Pro Glu Arg Met Asp Lys Lys Leu Leu 
145                 150                 155                 160 


Ala Val Pro Ala Ala Asn Thr Val Arg Phe Arg Cys Pro Ala Ala Gly 
                165                 170                 175     


Asn Pro Thr Pro Ser Ile Ser Trp Leu Lys Asn Gly Arg Glu Phe Arg 
            180                 185                 190         


Gly Glu His Arg Ile Gly Gly Ile Lys Leu Arg His Gln Gln Trp Ser 
        195                 200                 205             


Leu Val Met Glu Ser Val Val Pro Ser Asp Arg Gly Asn Tyr Thr Cys 
    210                 215                 220                 


Val Val Glu Asn Lys Phe Gly Ser Ile Arg Gln Thr Tyr Thr Leu Asp 
225                 230                 235                 240 


Val Leu Glu Arg Ser Pro His Arg Pro Ile Leu Gln Ala Gly Leu Pro 
                245                 250                 255     


Ala Asn Gln Thr Ala Val Leu Gly Ser Asp Val Glu Phe His Cys Lys 
            260                 265                 270         


Val Tyr Ser Asp Ala Pro His Ile Gln Trp Leu Lys His Val Glu Val 
        275                 280                 285             


Asn Gly Ser Lys Val Gly Pro Asp Gly Thr Pro Tyr Val Thr Val Leu 
    290                 295                 300                 


Lys Thr Ala Gly Ala Asn Thr Thr Asp Lys Glu Leu Glu Val Leu Ser 
305                 310                 315                 320 


Leu His Asn Val Thr Phe Glu Asp Ala Gly Glu Tyr Thr Cys Leu Ala 
                325                 330                 335     


Gly Asn Ser Ile Gly Phe Ser His His Ser Ala Trp Leu Val Val Leu 
            340                 345                 350         


Pro Ala Glu Glu Glu Leu Val Glu Ala Asp Glu Ala Gly Ser Val Tyr 
        355                 360                 365             


Ala Gly Ile Leu Ser Tyr Gly Val Gly Phe Phe Leu Phe Ile Leu Val 
    370                 375                 380                 


Val Ala Ala Val Thr Leu Cys Arg Leu Arg Ser Pro Pro Lys Lys Gly 
385                 390                 395                 400 


Leu Gly Ser Pro Thr Val His Lys Ile Ser Arg Phe Pro Leu Lys Arg 
                405                 410                 415     


Gln Val Ser Leu Glu Ser Asn Ala Ser Asn Ser Ser Asn Thr Pro Leu 
            420                 425                 430         


Val Arg Ile Ala Arg Leu Ser Ser Gly Glu Gly Pro Thr Leu Ala Asn 
        435                 440                 445             


Val Ser Glu Leu Glu Leu Pro Ala Asp Pro Lys Trp Glu Leu Ser Arg 
    450                 455                 460                 


Ala Arg Leu Thr Leu Gly Lys Pro Leu Gly Glu Gly Cys Phe Gly Gln 
465                 470                 475                 480 


Val Val Met Ala Glu Ala Ile Gly Ile Asp Lys Asp Arg Ala Ala Lys 
                485                 490                 495     


Pro Val Thr Val Ala Val Lys Met Leu Lys Asp Asp Ala Thr Asp Lys 
            500                 505                 510         


Asp Leu Ser Asp Leu Val Ser Glu Met Glu Met Met Lys Met Ile Gly 
        515                 520                 525             


Lys His Lys Asn Ile Ile Asn Leu Leu Gly Ala Cys Thr Gln Gly Gly 
    530                 535                 540                 


Pro Leu Tyr Val Leu Val Glu Tyr Ala Ala Lys Gly Asn Leu Arg Glu 
545                 550                 555                 560 


Phe Leu Arg Ala Arg Arg Pro Pro Gly Leu Asp Tyr Ser Phe Asp Thr 
                565                 570                 575     


Cys Lys Pro Pro Glu Glu Gln Leu Thr Phe Lys Asp Leu Val Ser Cys 
            580                 585                 590         


Ala Tyr Gln Val Ala Arg Gly Met Glu Tyr Leu Ala Ser Lys Cys Ile 
        595                 600                 605             


His Arg Asp Leu Ala Ala Arg Asn Val Leu Val Thr Glu Asp Asn Val 
    610                 615                 620                 


Met Lys Ile Ala Asp Phe Gly Leu Ala Arg Asp Val His Asn Leu Asp 
625                 630                 635                 640 


Tyr Tyr Lys Lys Thr Thr Asn Gly Arg Leu Pro Val Lys Trp Met Ala 
                645                 650                 655     


Pro Glu Ala Leu Phe Asp Arg Val Tyr Thr His Ser Asp Val Ser Phe 
            660                 665                 670         


Gly Val Leu Leu Trp Glu Ile Phe Thr Leu Gly Gly Ser Pro Tyr Pro 
        675                 680                 685             


Gly Ile Pro Val Glu Glu Leu Phe Lys Leu Leu Lys Glu Gly His Arg 
    690                 695                 700                 


Met Asp Lys Pro Ala Asn Cys Thr His Asp Leu Tyr Met Ile Met Arg 
705                 710                 715                 720 


Glu Cys Trp His Ala Ala Pro Ser Arg Pro Thr Phe Lys Leu Val Glu 
                725                 730                 735     


Asp Leu Asp Arg Val Leu Thr Val Thr Ser Thr Asp Glu Tyr Leu Asp 
            740                 745                 750         


Leu Ser Ala Pro Phe Glu Tyr Ser Pro Gly Gly Gln Asp Thr Pro Ser 
        755                 760                 765             


Ser Ser Ser Ser Gly Asp Asp Ser Val Phe Ala His Asp Leu Leu Pro 
    770                 775                 780                 


Pro Ala Pro Pro Ser Ser Gly Gly Ser Arg Thr 
785                 790                 795 


<210>  12
<211>  100
<212>  PRT
<213>  Homo sapiens

<400>  12

Ala Pro Tyr Trp Thr Arg Pro Glu Arg Met Asp Lys Lys Leu Leu Ala 
1               5                   10                  15      


Val Pro Ala Ala Asn Thr Val Arg Phe Arg Cys Pro Ala Ala Gly Asn 
            20                  25                  30          


Pro Thr Pro Ser Ile Ser Trp Leu Lys Asn Gly Arg Glu Phe Arg Gly 
        35                  40                  45              


Glu His Arg Ile Gly Gly Ile Lys Leu Arg His Gln Gln Trp Ser Leu 
    50                  55                  60                  


Val Met Glu Ser Val Val Pro Ser Asp Arg Gly Asn Tyr Thr Cys Val 
65                  70                  75                  80  


Val Glu Asn Lys Phe Gly Ser Ile Arg Gln Thr Tyr Thr Leu Asp Val 
                85                  90                  95      


Leu Glu Arg Ser 
            100 


