UNITED STATES

SECURITIES AND EXCHANGE COMMISSION

Washington, D.C. 20549

SCHEDULE 13G

(Rule 13d-102)

INFORMATION TO BE INCLUDED IN STATEMENTS FILED PURSUANT

TO RULES 13d-1(b), (c), AND (d) AND AMENDMENTS THERETO FILED

PURSUANT TO RULE 13d-2(b)

(Amendment No. 7)1

 

ArQule, Inc.

 (Name of Issuer)

Common Stock, par value $0.01 per share

 (Title of Class of Securities)

04269E107

 (CUSIP Number)

May 30, 2018

 (Date of Event Which Requires Filing of this Statement)

 

Check the appropriate box to designate the rule pursuant to which this Schedule is filed:

     Rule 13d-1(b)

     Rule 13d-1(c)

     Rule 13d-1(d)

 

 

 

1              The remainder of this cover page shall be filled out for a reporting person’s initial filing on this form with respect to the subject class of securities, and for any subsequent amendment containing information which would alter disclosures provided in a prior cover page.

The information required on the remainder of this cover page shall not be deemed to be “filed” for the purpose of Section 18 of the Securities Exchange Act of 1934 (“Act”) or otherwise subject to the liabilities of that section of the Act but shall be subject to all other provisions of the Act (however, see the Notes).

 

CUSIP NO. 04269E107

 

  1   NAME OF REPORTING PERSON  
         
        Biotechnology Value Fund, L.P.  
  2   CHECK THE APPROPRIATE BOX IF A MEMBER OF A GROUP (a) ☒
        (b) ☐
           
  3   SEC USE ONLY    
           
             
  4   CITIZENSHIP OR PLACE OF ORGANIZATION  
         
        Delaware  
NUMBER OF   5   SOLE VOTING POWER  
SHARES          
BENEFICIALLY         0 shares  
OWNED BY   6   SHARED VOTING POWER  
EACH          
REPORTING         5,883,722 (1)  
PERSON WITH   7   SOLE DISPOSITIVE POWER  
         
          0 shares  
    8   SHARED DISPOSITIVE POWER  
           
          5,883,722 (1)  
  9   AGGREGATE AMOUNT BENEFICIALLY OWNED BY EACH REPORTING PERSON  
         
        5,883,722 (1)  
  10   CHECK BOX IF THE AGGREGATE AMOUNT IN ROW (9) EXCLUDES CERTAIN SHARES     ☐
       
           
  11   PERCENT OF CLASS REPRESENTED BY AMOUNT IN ROW (9)  
         
        6.1% (1)  
  12   TYPE OF REPORTING PERSON  
         
        PN  

(1) Includes 1,201,053 shares of Common Stock currently issuable upon the exercise of certain warrants.

 

2

CUSIP NO. 04269E107

  1   NAME OF REPORTING PERSON  
         
        Biotechnology Value Fund II, L.P.  
  2   CHECK THE APPROPRIATE BOX IF A MEMBER OF A GROUP (a) ☒
        (b) ☐
           
  3   SEC USE ONLY    
           
             
  4   CITIZENSHIP OR PLACE OF ORGANIZATION  
         
        Delaware  
NUMBER OF   5   SOLE VOTING POWER  
SHARES          
BENEFICIALLY         0 shares  
OWNED BY   6   SHARED VOTING POWER  
EACH          
REPORTING         4,009,275 (1)  
PERSON WITH   7   SOLE DISPOSITIVE POWER  
         
          0 shares  
    8   SHARED DISPOSITIVE POWER  
           
          4,009,275 (1)  
  9   AGGREGATE AMOUNT BENEFICIALLY OWNED BY EACH REPORTING PERSON  
         
        4,009,275 (1)  
  10   CHECK BOX IF THE AGGREGATE AMOUNT IN ROW (9) EXCLUDES CERTAIN SHARES     ☐
       
           
  11   PERCENT OF CLASS REPRESENTED BY AMOUNT IN ROW (9)  
         
        4.2% (1)  
  12   TYPE OF REPORTING PERSON  
         
        PN  

(1) Includes 823,231 shares of Common Stock currently issuable upon the exercise of certain warrants.

 

3

CUSIP NO. 04269E107

 

  1   NAME OF REPORTING PERSON  
         
        Biotechnology Value Trading Fund OS LP  
  2   CHECK THE APPROPRIATE BOX IF A MEMBER OF A GROUP (a) ☒
        (b) ☐
           
  3   SEC USE ONLY    
           
             
  4   CITIZENSHIP OR PLACE OF ORGANIZATION  
         
        Cayman Islands  
NUMBER OF   5   SOLE VOTING POWER  
SHARES          
BENEFICIALLY         0 shares  
OWNED BY   6   SHARED VOTING POWER  
EACH          
REPORTING         970,992 (1)  
PERSON WITH   7   SOLE DISPOSITIVE POWER  
         
          0 shares  
    8   SHARED DISPOSITIVE POWER  
           
          970,992 (1)  
  9   AGGREGATE AMOUNT BENEFICIALLY OWNED BY EACH REPORTING PERSON  
         
        970,992 (1)  
  10   CHECK BOX IF THE AGGREGATE AMOUNT IN ROW (9) EXCLUDES CERTAIN SHARES     ☐
       
           
  11   PERCENT OF CLASS REPRESENTED BY AMOUNT IN ROW (9)  
         
        1.0% (1)  
  12   TYPE OF REPORTING PERSON  
         
        PN  

(1) Includes 199,687 shares of Common Stock currently issuable upon the exercise of certain warrants.

 

4

CUSIP NO. 04269E107

 

  1   NAME OF REPORTING PERSON  
         
        BVF Partners OS Ltd.  
  2   CHECK THE APPROPRIATE BOX IF A MEMBER OF A GROUP (a) ☒
        (b) ☐
           
  3   SEC USE ONLY    
           
             
  4   CITIZENSHIP OR PLACE OF ORGANIZATION  
         
        Cayman Islands  
NUMBER OF   5   SOLE VOTING POWER  
SHARES          
BENEFICIALLY         0 shares  
OWNED BY   6   SHARED VOTING POWER  
EACH          
REPORTING         970,992 (1)  
PERSON WITH   7   SOLE DISPOSITIVE POWER  
         
          0 shares  
    8   SHARED DISPOSITIVE POWER  
           
          970,992 (1)  
  9   AGGREGATE AMOUNT BENEFICIALLY OWNED BY EACH REPORTING PERSON  
         
        970,992 (1)  
  10   CHECK BOX IF THE AGGREGATE AMOUNT IN ROW (9) EXCLUDES CERTAIN SHARES     ☐
       
           
  11   PERCENT OF CLASS REPRESENTED BY AMOUNT IN ROW (9)  
         
        1.0% (1)  
  12   TYPE OF REPORTING PERSON  
         
        CO  

(1) Includes 199,687 shares of Common Stock currently issuable upon the exercise of certain warrants.

  

5

CUSIP NO. 04269E107

 

  1   NAME OF REPORTING PERSON  
         
        BVF Partners L.P.  
  2   CHECK THE APPROPRIATE BOX IF A MEMBER OF A GROUP (a) ☒
        (b) ☐
           
  3   SEC USE ONLY    
           
             
  4   CITIZENSHIP OR PLACE OF ORGANIZATION  
         
        Delaware  
NUMBER OF   5   SOLE VOTING POWER  
SHARES          
BENEFICIALLY         0 shares  
OWNED BY   6   SHARED VOTING POWER  
EACH          
REPORTING         12,076,844 (1)  
PERSON WITH   7   SOLE DISPOSITIVE POWER  
         
          0 shares  
    8   SHARED DISPOSITIVE POWER  
           
          12,076,844 (1)  
  9   AGGREGATE AMOUNT BENEFICIALLY OWNED BY EACH REPORTING PERSON  
         
        12,076,844 (1)  
  10   CHECK BOX IF THE AGGREGATE AMOUNT IN ROW (9) EXCLUDES CERTAIN SHARES     ☐
       
           
  11   PERCENT OF CLASS REPRESENTED BY AMOUNT IN ROW (9)  
         
        12.3% (1)  
  12   TYPE OF REPORTING PERSON  
         
        PN, IA  

(1) Includes 2,439,932 shares of Common Stock currently issuable upon the exercise of certain warrants.

 

6

CUSIP NO. 04269E107

 

  1   NAME OF REPORTING PERSON  
         
        BVF Inc.  
  2   CHECK THE APPROPRIATE BOX IF A MEMBER OF A GROUP (a) ☒
        (b) ☐
           
  3   SEC USE ONLY    
           
             
  4   CITIZENSHIP OR PLACE OF ORGANIZATION  
         
        Delaware  
NUMBER OF   5   SOLE VOTING POWER  
SHARES          
BENEFICIALLY         0 shares  
OWNED BY   6   SHARED VOTING POWER  
EACH          
REPORTING         12,076,844 (1)  
PERSON WITH   7   SOLE DISPOSITIVE POWER  
         
          0 shares  
    8   SHARED DISPOSITIVE POWER  
           
          12,076,844 (1)  
  9   AGGREGATE AMOUNT BENEFICIALLY OWNED BY EACH REPORTING PERSON  
         
        12,076,844 (1)  
  10   CHECK BOX IF THE AGGREGATE AMOUNT IN ROW (9) EXCLUDES CERTAIN SHARES     ☐
       
           
  11   PERCENT OF CLASS REPRESENTED BY AMOUNT IN ROW (9)  
         
        12.3% (1)  
  12   TYPE OF REPORTING PERSON  
         
        CO  

(1) Includes 2,439,932 shares of Common Stock currently issuable upon the exercise of certain warrants.

 

7

CUSIP NO. 04269E107

 

  1   NAME OF REPORTING PERSON  
         
        Mark N. Lampert  
  2   CHECK THE APPROPRIATE BOX IF A MEMBER OF A GROUP (a) ☒
        (b) ☐
           
  3   SEC USE ONLY    
           
             
  4   CITIZENSHIP OR PLACE OF ORGANIZATION  
         
        United States  
NUMBER OF   5   SOLE VOTING POWER  
SHARES          
BENEFICIALLY         0 shares  
OWNED BY   6   SHARED VOTING POWER  
EACH          
REPORTING         12,076,844 (1)  
PERSON WITH   7   SOLE DISPOSITIVE POWER  
         
          0 shares  
    8   SHARED DISPOSITIVE POWER  
           
          12,076,844 (1)  
  9   AGGREGATE AMOUNT BENEFICIALLY OWNED BY EACH REPORTING PERSON  
         
        12,076,844 (1)  
  10   CHECK BOX IF THE AGGREGATE AMOUNT IN ROW (9) EXCLUDES CERTAIN SHARES     ☐
       
           
  11   PERCENT OF CLASS REPRESENTED BY AMOUNT IN ROW (9)  
         
        12.3% (1)  
  12   TYPE OF REPORTING PERSON  
         
        IN  

(1) Includes 2,439,932 shares of Common Stock currently issuable upon the exercise of certain warrants.

 

8

CUSIP NO. 04269E107

 

Item 1(a).Name of Issuer:

 

ArQule, Inc., a Delaware corporation (the “Issuer”).

 

Item 1(b).Address of Issuer's Principal Executive Offices:

 

One Wall Street

Burlington, Massachusetts 01803

 

Item 2(a).Name of Person Filing
Item 2(b).Address of Principal Business Office or, if None, Residence
Item 2(c).Citizenship

 

Biotechnology Value Fund, L.P. (“BVF”)

1 Sansome Street, 30th Floor

San Francisco, California 94104

Citizenship: Delaware

 

Biotechnology Value Fund II, L.P. (“BVF2”)

1 Sansome Street, 30th Floor

San Francisco, California 94104

Citizenship: Delaware

 

Biotechnology Value Trading Fund OS LP (“Trading Fund OS”)

PO Box 309 Ugland House

Grand Cayman, KY1-1104

Cayman Islands

Citizenship: Cayman Islands

 

BVF Partners OS Ltd. (“Partners OS”)

PO Box 309 Ugland House

Grand Cayman, KY1-1104

Cayman Islands

Citizenship: Cayman Islands

 

BVF Partners L.P. (“Partners”)

1 Sansome Street, 30th Floor

San Francisco, California 94104

Citizenship: Delaware

 

BVF Inc.

1 Sansome Street, 30th Floor

San Francisco, California 94104

Citizenship: Delaware

 

Mark N. Lampert (“Mr. Lampert”)

1 Sansome Street, 30th Floor

San Francisco, California 94104

Citizenship: United States

 

Each of the foregoing is referred to as a “Reporting Person” and collectively as the “Reporting Persons.”

 

9

CUSIP NO. 04269E107

 

Item 2(d).Title of Class of Securities:

 

Common Stock, par value $0.01 per share (the “Common Stock”)

 

Item 2(e).CUSIP Number:

 

04269E107

 

Item 3.If This Statement is Filed Pursuant to Rule 13d-1(b), or 13d-2(b) or (c), Check Whether the Person Filing is a:

 

  /x/

Not applicable.

       
  (a) / / Broker or dealer registered under Section 15 of the Exchange Act.
       
(b) / / Bank as defined in Section 3(a)(6) of the Exchange Act.
       
  (c) / / Insurance company as defined in Section 3(a)(19) of the Exchange Act.
       
  (d) / / Investment company registered under Section 8 of the Investment Company Act.
       
  (e) / / An investment adviser in accordance with Rule 13d-1(b)(1)(ii)(E).
       
  (f) / / An employee benefit plan or endowment fund in accordance with Rule 13d-1(b)(1)(ii)(F).
       
  (g) / / A parent holding company or control person in accordance with Rule 13d-1(b)(1)(ii)(G).
       
  (h) / / A savings association as defined in Section 3(b) of the Federal Deposit Insurance Act.
       
  (i) / / A church plan that is excluded from the definition of an investment company under Section 3(c)(14) of the Investment Company Act.
       
  (j) / / Group, in accordance with Rule 13d-1(b)(1)(ii)(J).  
       
  (k) / / Group, in accordance with Rule 240.13d-1(b)(1)(ii)(K). If filing as a non-U.S. institution in accordance with Rule 240.13d-1(b)(1)(ii)(J), please specify the type of institution: ____

 

Item 4.Ownership

 

(a)Amount beneficially owned:

 

On October 11, 2017, the Reporting Persons participated in a private placement (the “Private Placement”) with the Issuer. Pursuant to the Private Placement, the Reporting Persons acquired in the aggregate 9,037,054 shares of Common Stock and warrants (the “Warrants”) exercisable for an aggregate of 2,439,932 shares of Common Stock. Pursuant to the Private Placement, the Warrants are subject to an exercise limitation, and may not be exercised if, after such exercise, the Reporting Persons would beneficially own in the aggregate, as determined in accordance with Section 13(d) of the Securities Exchange Act of 1934, more than 19.9% of the number of shares of Common Stock then issued and outstanding. Such Warrants have an initial exercise price of $1.75 per share, subject to adjustment pursuant to the terms of the Warrants, and expire on October 11, 2021. As of June 1, 2018, the Warrant exercise limitation described above does not limit the exercise of the Warrants by the Reporting Persons.

10

CUSIP NO. 04269E107

 

As of June 1, 2018 (i) BVF beneficially owned 5,883,722 shares of Common Stock, including 1,201,053 shares of Common Stock issuable upon the exercise of Warrants, (ii) BVF2 beneficially owned 4,009,275 shares of Common Stock, including 823,231 shares of Common Stock issuable upon the exercise of Warrants and (iii) Trading Fund OS beneficially owned 970,992 shares of Common Stock, including 199,687 shares of Common Stock issuable upon the exercise of Warrants.

 

Partners OS, as the general partner of Trading Fund OS, may be deemed to beneficially own the 970,992 shares of Common Stock beneficially owned by Trading Fund OS.

 

Partners, as the general partner of BVF, BVF2, the investment manager of Trading Fund OS, and the sole member of Partners OS, may be deemed to beneficially own the 12,076,844 shares of Common Stock beneficially owned in the aggregate by BVF, BVF2, Trading Fund OS, and certain Partners managed accounts (the “Partners Managed Accounts”), including 1,212,855 shares of Common Stock, which includes 215,961 shares of Common Stock issuable upon the exercise of Warrants, held in the Partners Managed Accounts.

 

BVF Inc., as the general partner of Partners, may be deemed to beneficially own the 12,076,844 shares of Common Stock beneficially owned by Partners.

 

Mr. Lampert, as a director and officer of BVF Inc., may be deemed to beneficially own the 12,076,844 shares of Common Stock beneficially owned by BVF Inc.

 

The foregoing should not be construed in and of itself as an admission by any Reporting Person as to beneficial ownership of any shares of Common Stock owned by another Reporting Person. Partners OS disclaims beneficial ownership of the shares of Common Stock beneficially owned by Trading Fund OS. Each of Partners, BVF Inc. and Mr. Lampert disclaims beneficial ownership of the shares of Common Stock beneficially owned by BVF, BVF2, Trading Fund OS, and the Partners Managed Accounts, and the filing of this statement shall not be construed as an admission that any such person or entity is the beneficial owner of any such securities.

 

(b)Percent of class:

 

The following percentages are based on a denominator which is the sum of: (i) 95,495,327 shares of Common Stock outstanding as of May 16, 2018, as disclosed in the Issuer’s Registration Statement on Form S-3 filed with the Securities and Exchange Commission on May 17, 2018, and (ii) certain or all of the 2,439,932 shares of Common Stock underlying Warrants, as applicable.

 

As of June 1, 2018 (i) BVF beneficially owned approximately 6.1% of the outstanding shares of Common Stock, (ii) BVF2 beneficially owned approximately 4.2% of the outstanding shares of Common Stock, (iii) Trading Fund OS beneficially owned approximately 1.0% of the outstanding shares of Common Stock, (iv) Partners OS may be deemed to beneficially own approximately 1.0% of the outstanding shares of Common Stock, and (v) each of Partners, BVF Inc. and Mr. Lampert may be deemed to beneficially own approximately 12.3% of the outstanding shares of Common Stock (approximately 1.3% of the outstanding shares of Common Stock are held in the Partners Managed Accounts).

 

11

CUSIP NO. 04269E107

 

(c)Number of shares as to which such person has:

 

(i)Sole power to vote or to direct the vote

 

See Cover Pages Items 5-9.

 

(ii)Shared power to vote or to direct the vote

 

See Cover Pages Items 5-9.

 

(iii)Sole power to dispose or to direct the disposition of

 

See Cover Pages Items 5-9.

 

(iv)Shared power to dispose or to direct the disposition of

 

See Cover Pages Items 5-9.

 

Item 5.Ownership of Five Percent or Less of a Class.

 

Not Applicable.

 

Item 6.Ownership of More than Five Percent on Behalf of Another Person.

 

Partners, BVF Inc. and Mr. Lampert share voting and dispositive power over the shares of Common Stock beneficially owned by BVF, BVF2, Trading Fund OS, and the Partners Managed Accounts.

 

Item 7.Identification and Classification of the Subsidiary That Acquired the Security Being Reported on by the Parent Holding Company or Control Person.

 

Not Applicable.

 

Item 8.Identification and Classification of Members of the Group.

 

See Exhibit 99.1 to Amendment No. 3 to the Schedule 13G filed with the Securities and Exchange Commission on February 16, 2016.

 

Item 9.Notice of Dissolution of Group.

 

Not Applicable.

 

Item 10.Certifications.

 

By signing below each of the undersigned certifies that, to the best of its knowledge and belief, the securities referred to above were not acquired and are not held for the purpose of or with the effect of changing or influencing the control of the issuer of the securities and were not acquired and are not held in connection with or as a participant in any transaction having that purpose or effect.

 

12

CUSIP NO. 04269E107

 

SIGNATURE

 

After reasonable inquiry and to the best of his knowledge and belief, each of the undersigned certifies that the information set forth in this statement is true, complete and correct.

 

Dated: June 1, 2018

 

BIOTECHNOLOGY VALUE FUND, L.P.   BVF INC.
       
By: BVF Partners L.P., its general partner   By:

/s/ Mark N. Lampert

By: BVF Inc., its general partner     Mark N. Lampert
        President
By:

/s/ Mark N. Lampert

   
  Mark N. Lampert    
  President  

/s/ Mark N. Lampert

      MARK N. LAMPERT
       
BIOTECHNOLOGY VALUE FUND II, L.P.    
       
By: BVF Partners L.P., its general partner    
By: BVF Inc., its general partner    
       
By:

/s/ Mark N. Lampert

   
  Mark N. Lampert    
  President    
       
       
BVF PARTNERS L.P.    
       
By: BVF Inc., its general partner    
       
By:

/s/ Mark N. Lampert

   
  Mark N. Lampert    
  President    
       
       
BVF PARTNERS OS LTD.    
       
By: BVF Partners L.P., its sole member    
By: BVF Inc., its general partner    
       
By:

/s/ Mark N. Lampert

   
  Mark N. Lampert    
  President    

       
       
Biotechnology Value Trading Fund OS LP    
       
By: BVF Partners L.P., its investment manager    
By: BVF Inc., its general partner    
       
By:

/s/ Mark N. Lampert

   
  Mark N. Lampert    
  President    

 

13