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CASI Pharmaceuticals, Inc. – ‘10-K’ for 12/31/20 – ‘EX-101.DEF’

On:  Tuesday, 3/30/21, at 5:28pm ET   ·   For:  12/31/20   ·   Accession #:  1558370-21-3735   ·   File #:  0-20713

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  As Of               Filer                 Filing    For·On·As Docs:Size             Issuer                      Filing Agent

 3/30/21  CASI Pharmaceuticals, Inc.        10-K       12/31/20  109:13M                                    Toppan Merrill Bridge/FA

Annual Report   —   Form 10-K
Filing Table of Contents

Document/Exhibit                   Description                      Pages   Size 

 1: 10-K        Annual Report                                       HTML   1.49M 
 2: EX-4.1      Instrument Defining the Rights of Security Holders  HTML     40K 
 7: EX-10.29    Material Contract                                   HTML     45K 
 8: EX-10.30    Material Contract                                   HTML    283K 
 3: EX-10.4     Material Contract                                   HTML    249K 
 4: EX-10.5     Material Contract                                   HTML    249K 
 5: EX-10.6     Material Contract                                   HTML    240K 
 6: EX-10.8     Material Contract                                   HTML    444K 
 9: EX-21       Subsidiaries List                                   HTML     28K 
10: EX-23.1     Consent of Expert or Counsel                        HTML     28K 
11: EX-31.1     Certification -- §302 - SOA'02                      HTML     32K 
12: EX-31.2     Certification -- §302 - SOA'02                      HTML     32K 
13: EX-32.1     Certification -- §906 - SOA'02                      HTML     30K 
14: EX-32.2     Certification -- §906 - SOA'02                      HTML     30K 
21: R1          Document and Entity Information                     HTML     91K 
22: R2          Condensed Consolidated Balance Sheets               HTML    120K 
23: R3          Condensed Consolidated Balance Sheets               HTML     50K 
                (Parenthetical)                                                  
24: R4          Condensed Consolidated Statements of Operations     HTML    116K 
                and Comprehensive Loss                                           
25: R5          Condensed Consolidated Statements of Stockholders'  HTML     69K 
                Equity                                                           
26: R6          Condensed Consolidated Statements of Cash Flows     HTML    151K 
27: R7          Description of Business                             HTML     72K 
28: R8          Summary of Significant Accounting Policies          HTML     65K 
29: R9          Investment in Equity Securities, at Fair Value and  HTML     80K 
                Long-Term Investments                                            
30: R10         Inventories                                         HTML     40K 
31: R11         Leases                                              HTML     72K 
32: R12         Property, Plant and Equipment                       HTML     50K 
33: R13         Intangible Assets                                   HTML     61K 
34: R14         Assets Held for Sale                                HTML     37K 
35: R15         Grants                                              HTML     30K 
36: R16         Bank Borrowings                                     HTML     30K 
37: R17         Note Payable                                        HTML     31K 
38: R18         Redeemable Noncontrolling Interest                  HTML     51K 
39: R19         Stockholders' Equity                                HTML     59K 
40: R20         Net Loss Per Share                                  HTML     48K 
41: R21         Employee Benefit Plan                               HTML     31K 
42: R22         Stock-Based Compensation                            HTML    155K 
43: R23         Income Taxes                                        HTML     94K 
44: R24         Fair Value Measurements                             HTML     92K 
45: R25         Related Party Transactions                          HTML     38K 
46: R26         Acrotech License Arrangements                       HTML     31K 
47: R27         Commitments and Contingencies                       HTML     33K 
48: R28         Subsequent Events                                   HTML     36K 
49: R29         Summary of Significant Accounting Policies          HTML    118K 
                (Policies)                                                       
50: R30         Investment in Equity Securities, at Fair Value and  HTML     68K 
                Long-Term Investments (Tables)                                   
51: R31         Inventories (Tables)                                HTML     40K 
52: R32         Leases (Tables)                                     HTML     71K 
53: R33         Property, Plant and Equipment (Tables)              HTML     47K 
54: R34         Intangible Assets (Tables)                          HTML     63K 
55: R35         Assets Held for Sale (Tables)                       HTML     35K 
56: R36         Redeemable Noncontrolling Interest (Tables)         HTML     47K 
57: R37         Stockholders' Equity (Tables)                       HTML     47K 
58: R38         Net Loss Per Share (Tables)                         HTML     46K 
59: R39         Stock-Based Compensation (Tables)                   HTML    155K 
60: R40         Income Taxes (Tables)                               HTML     94K 
61: R41         Fair Value Measurements (Tables)                    HTML     90K 
62: R42         Description of Business (Details)                   HTML    186K 
63: R43         Summary of Significant Accounting Policies          HTML     66K 
                (Details)                                                        
64: R44         INVESTMENT IN EQUITY SECURITIES, AT FAIR VALUE AND  HTML     37K 
                LONG-TERM INVESTMENTS - Summary of Investments                   
                (Details)                                                        
65: R45         INVESTMENT IN EQUITY SECURITIES, AT FAIR VALUE AND  HTML     47K 
                LONG-TERM INVESTMENTS - Summary of Long-term                     
                investments (Details)                                            
66: R46         Investment in Equity Securities, at Fair Value and  HTML    116K 
                Long-Term Investments (Details)                                  
67: R47         Inventories (Details)                               HTML     36K 
68: R48         Leases - (Details)                                  HTML     60K 
69: R49         Leases - Right of Use Assets and Liabilities        HTML     40K 
                (Details)                                                        
70: R50         LEASES - Supplemental Cash Flow (Details)           HTML     32K 
71: R51         LEASES - Future Undiscounted Cash Flows (Details)   HTML     46K 
72: R52         Property, Plant and Equipment (Details)             HTML     44K 
73: R53         Property, Plant and Equipment - Additional          HTML     45K 
                Information (Details)                                            
74: R54         INTANGIBLE ASSETS - Net Definite-lived Intangible   HTML     39K 
                Assets (Details)                                                 
75: R55         INTANGIBLE ASSETS - Changes in intangible assets    HTML     35K 
                (Details)                                                        
76: R56         INTANGIBLE ASSETS - Expected Future Amortization    HTML     41K 
                Expense (Details)                                                
77: R57         INTANGIBLE ASSETS - Additional Information          HTML     46K 
                (Details)                                                        
78: R58         ASSETS HELD FOR SALE - Additional Information       HTML     43K 
                (Details)                                                        
79: R59         ASSETS HELD FOR SALE - Components of assets         HTML     37K 
                held-for-sale (Details)                                          
80: R60         Grants (Details)                                    HTML     40K 
81: R61         Bank Borrowings (Details)                           HTML     43K 
82: R62         Note Payable (Details)                              HTML     39K 
83: R63         Redeemable Noncontrolling Interest (Details)        HTML     51K 
84: R64         Redeemable Noncontrolling Interest - Changes in     HTML     40K 
                Redeemable Noncontrolling Interest (Details)                     
85: R65         Stockholders' Equity (Details)                      HTML     84K 
86: R66         Stockholders' Equity - Warrants Activity (Details)  HTML     54K 
87: R67         Net Loss Per Share (Details)                        HTML     31K 
88: R68         Net Loss Per Share - Basic and diluted net loss     HTML     45K 
                per share computation (Details)                                  
89: R69         Employee Benefit Plan (Details)                     HTML     33K 
90: R70         STOCK-BASED COMPENSATION - Compensation Expense     HTML     37K 
                (Details)                                                        
91: R71         STOCK-BASED COMPENSATION - Weighted-Average         HTML     44K 
                Assumptions (Details)                                            
92: R72         STOCK-BASED COMPENSATION - Options Outstanding      HTML     93K 
                (Details)                                                        
93: R73         STOCK-BASED COMPENSATION - Stock Option             HTML     63K 
                Outstanding (Details)                                            
94: R74         Stock-Based Compensation (Details)                  HTML     73K 
95: R75         INCOME TAXES - Loss Before Income Taxes (Details)   HTML     36K 
96: R76         INCOME TAXES - Deferred Income Tax Assets And       HTML     43K 
                Liabilities (Details)                                            
97: R77         INCOME TAXES - Reconciliation Of The Provision For  HTML     49K 
                Income Taxes (Details)                                           
98: R78         INCOME TAXES - Gross Unrecognized Tax Benefits      HTML     34K 
                (Details)                                                        
99: R79         Income Taxes (Details)                              HTML     40K 
100: R80         FAIR VALUE MEASUREMENTS - Financial and             HTML     47K  
                Non-Financial Assets and Liabilities (Details)                   
101: R81         FAIR VALUE MEASUREMENTS - Quantitative Information  HTML     39K  
                about Level 3 Fair Value Measurements (Details)                  
102: R82         Fair Value Measurements (Details)                   HTML     48K  
103: R83         Related Party Transactions (Details)                HTML     72K  
104: R84         Commitments and Contingencies (Details)             HTML     42K  
105: R85         Subsequent Events (Details)                         HTML     79K  
107: XML         IDEA XML File -- Filing Summary                      XML    189K  
20: XML         XBRL Instance -- casi-20201231x10k_htm               XML   2.24M 
106: EXCEL       IDEA Workbook of Financial Reports                  XLSX    136K  
16: EX-101.CAL  XBRL Calculations -- casi-20201231_cal               XML    198K 
17: EX-101.DEF  XBRL Definitions -- casi-20201231_def                XML    811K 
18: EX-101.LAB  XBRL Labels -- casi-20201231_lab                     XML   1.47M 
19: EX-101.PRE  XBRL Presentations -- casi-20201231_pre              XML   1.31M 
15: EX-101.SCH  XBRL Schema -- casi-20201231                         XSD    233K 
108: JSON        XBRL Instance as JSON Data -- MetaLinks              465±   702K  
109: ZIP         XBRL Zipped Folder -- 0001558370-21-003735-xbrl      Zip    660K  


‘EX-101.DEF’   —   XBRL Definitions — casi-20201231_def


This Exhibit is an XBRL XML File.


                                                                                                                                                                                
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10 Subsequent Filings that Reference this Filing

  As Of               Filer                 Filing    For·On·As Docs:Size             Issuer                      Filing Agent

 3/28/24  CASI Pharmaceuticals, Inc.        20-F       12/31/23  142:21M                                    Toppan Merrill Bridge/FA
 4/26/23  CASI Pharmaceuticals, Inc.        20-F       12/31/22  129:16M                                    Toppan Merrill Bridge/FA
 4/26/23  CASI Pharmaceuticals, Inc. (DE)   20-F       12/31/22  129:16M                                    Toppan Merrill Bridge/FA
 3/28/22  CASI Pharmaceuticals, Inc. (DE)   10-K       12/31/21  104:11M                                    Toppan Merrill Bridge/FA
10/29/21  CASI Pharmaceuticals, Inc. (DE)   424B5                  1:316K                                   Toppan Merrill/FA
 8/13/21  CASI Pharmaceuticals, Inc. (DE)   S-8         8/13/21    3:78K                                    Toppan Merrill/FA
 8/13/21  CASI Pharmaceuticals, Inc. (DE)   S-8 POS     8/13/21    3:77K                                    Toppan Merrill/FA
 8/13/21  CASI Pharmaceuticals, Inc. (DE)   S-8 POS     8/13/21    3:77K                                    Toppan Merrill/FA
 8/13/21  CASI Pharmaceuticals, Inc. (DE)   S-8 POS     8/13/21    3:77K                                    Toppan Merrill/FA
 4/29/21  CASI Pharmaceuticals, Inc. (DE)   10-K/A     12/31/20   12:513K                                   Toppan Merrill/FA


16 Previous Filings that this Filing References

  As Of               Filer                 Filing    For·On·As Docs:Size             Issuer                      Filing Agent

 2/10/21  CASI Pharmaceuticals, Inc. (DE)   10-Q/A      9/30/20   13:304K                                   Toppan Merrill/FA
11/09/20  CASI Pharmaceuticals, Inc. (DE)   10-Q        9/30/20   91:7.2M                                   Toppan Merrill/FA
 7/24/20  CASI Pharmaceuticals, Inc. (DE)   8-K:1,8,9   7/21/20    5:274K                                   Toppan Merrill/FA
 3/16/20  CASI Pharmaceuticals, Inc. (DE)   10-K       12/31/19   98:6.9M                                   Toppan Merrill/FA
 8/09/19  CASI Pharmaceuticals, Inc. (DE)   10-Q        6/30/19   75:16M                                    Toppan Merrill/FA
 7/19/19  CASI Pharmaceuticals, Inc. (DE)   8-K:1,9     7/19/19    4:312K                                   Toppan Merrill/FA
 5/15/19  CASI Pharmaceuticals, Inc. (DE)   10-Q        3/31/19   78:5.6M                                   Toppan Merrill/FA
 4/30/19  CASI Pharmaceuticals, Inc. (DE)   DEF 14A     6/20/19    1:699K                                   Toppan Merrill/FA
 3/29/19  CASI Pharmaceuticals, Inc. (DE)   10-K       12/31/18   91:7.7M                                   Toppan Merrill/FA
 9/14/18  CASI Pharmaceuticals, Inc. (DE)   8-K:1,3,9   9/11/18    4:373K                                   Toppan Merrill/FA
 3/23/18  CASI Pharmaceuticals, Inc. (DE)   8-K:1,3,9   3/19/18    4:214K                                   Toppan Merrill/FA
 2/23/18  CASI Pharmaceuticals, Inc. (DE)   8-K:1,9     2/23/18    3:251K                                   Toppan Merrill/FA
10/19/17  CASI Pharmaceuticals, Inc. (DE)   8-K:1,9    10/13/17    7:427K                                   Toppan Merrill/FA
 8/14/17  CASI Pharmaceuticals, Inc. (DE)   10-Q        6/30/17   40:1.7M                                   Toppan Merrill/FA
 4/17/07  CASI Pharmaceuticals, Inc.        8-K:5,8,9   4/16/07    9:152K                                   Bowne - DC/FA
 6/06/06  CASI Pharmaceuticals, Inc.        8-K:1,9     6/01/06    3:66K                                    Bowne - DC/FA
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