BIOTECHNOLOGY VALUE FUND L P
SC 13G/A, 2000-06-30
INVESTMENT ADVICE
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<PAGE>

                       SECURITIES AND EXCHANGE COMMISSION
                              WASHINGTON, DC 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 13d-2(b)
                              (AMENDMENT NO. _2_)(1)

                                   ARQULE INC.
                                   -----------
                                (Name of Issuer)

                                  COMMON STOCK
                                  ------------
                         (Title of Class of Securities)

                                   04269E 10 7
                                   -----------
                                 (CUSIP Number)

                                  JUNE 23, 2000
                                  -------------
             (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)
                  /X/      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 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).

<PAGE>

------------------------------                     ---------------------------
CUSIP NO. 04269E 10 7                  13G                  PAGE 2 OF 8 PAGES
------------------------------                     ---------------------------

<TABLE>
--------- ----------------------------------------------------------------------------------------------------------
  <S>     <C>
   1      NAME OF REPORTING PERSON:
                   BIOTECHNOLOGY VALUE FUND, L.P.
          I.R.S. IDENTIFICATION NO. OF ABOVE PERSON (ENTITIES ONLY):

--------- ----------------------------------------------------------------------------------------------------------
   2      CHECK THE APPROPRIATE BOX IF A MEMBER OF A GROUP*
                                                                                                  (a) /X/  (b) /_/
--------- ----------------------------------------------------------------------------------------------------------
   3      SEC USE ONLY

--------- ----------------------------------------------------------------------------------------------------------
   4      CITIZENSHIP OR PLACE OF ORGANIZATION
                   DELAWARE
----------------------- --------------------------------------------------------------------------------------------
                                 SOLE VOTING POWER
         NUMBER             5           0
           OF                    -----------------------------------------------------------------------------------
         SHARES                  SHARED VOTING POWER
      BENEFICIALLY          6           238,471
        OWNED BY                 -----------------------------------------------------------------------------------
          EACH                   SOLE DISPOSITIVE POWER
        REPORTING           7           0
         PERSON                  -----------------------------------------------------------------------------------
          WITH                   SHARED DISPOSITIVE POWER
                            8           238,471
----------------------- --------------------------------------------------------------------------------------------
   9      AGGREGATE AMOUNT BENEFICIALLY OWNED BY EACH REPORTING PERSON
                   238,471
--------- ----------------------------------------------------------------------------------------------------------
   10     CHECK BOX IF THE AGGREGATE AMOUNT IN ROW (9) EXCLUDES
          CERTAIN SHARES*                                                                                      /_/
--------- ----------------------------------------------------------------------------------------------------------
   11     PERCENT OF CLASS REPRESENTED BY AMOUNT IN ROW 9
                   1.8%
--------- ----------------------------------------------------------------------------------------------------------
   12     TYPE OF REPORTING PERSON*
                   PN
--------- ----------------------------------------------------------------------------------------------------------
</TABLE>

                     * SEE INSTRUCTIONS BEFORE FILLING OUT!


<PAGE>

------------------------------                     ---------------------------
CUSIP NO. 04269E 10 7                  13G                  PAGE 3 OF 8 PAGES
------------------------------                     ---------------------------

<TABLE>
--------- ----------------------------------------------------------------------------------------------------------
  <S>     <C>
   1      NAME OF REPORTING PERSON:
                   BIOTECHNOLOGY VALUE FUND II, L.P.
          I.R.S. IDENTIFICATION NO. OF ABOVE PERSON (ENTITIES ONLY):

--------- ----------------------------------------------------------------------------------------------------------
   2      CHECK THE APPROPRIATE BOX IF A MEMBER OF A GROUP*
                                                                                                  (a) /X/  (b) /_/
--------- ----------------------------------------------------------------------------------------------------------
   3      SEC USE ONLY

--------- ----------------------------------------------------------------------------------------------------------
   4      CITIZENSHIP OR PLACE OF ORGANIZATION
                   DELAWARE
----------------------- --------------------------------------------------------------------------------------------
                                 SOLE VOTING POWER
         NUMBER             5           0
           OF                    -----------------------------------------------------------------------------------
         SHARES                  SHARED VOTING POWER
      BENEFICIALLY          6           392,634
        OWNED BY                 -----------------------------------------------------------------------------------
          EACH                   SOLE DISPOSITIVE POWER
        REPORTING           7           0
         PERSON                  -----------------------------------------------------------------------------------
          WITH                   SHARED DISPOSITIVE POWER
                            8           392,634
----------------------- --------------------------------------------------------------------------------------------
   9      AGGREGATE AMOUNT BENEFICIALLY OWNED BY EACH REPORTING PERSON
                   392,634
--------- ----------------------------------------------------------------------------------------------------------
   10     CHECK BOX IF THE AGGREGATE AMOUNT IN ROW (9) EXCLUDES
          CERTAIN SHARES*                                                                                      /_/
--------- ----------------------------------------------------------------------------------------------------------
   11     PERCENT OF CLASS REPRESENTED BY AMOUNT IN ROW 9
                   2.9%
--------- ----------------------------------------------------------------------------------------------------------
   12     TYPE OF REPORTING PERSON*
                   PN
--------- ----------------------------------------------------------------------------------------------------------
</TABLE>


                     * SEE INSTRUCTIONS BEFORE FILLING OUT!

<PAGE>

------------------------------                     ---------------------------
CUSIP NO. 04269E 10 7                  13G                  PAGE 4 OF 8 PAGES
------------------------------                     ---------------------------


<TABLE>
--------- ----------------------------------------------------------------------------------------------------------
  <S>     <C>
   1      NAME OF REPORTING PERSON:
                   BVF PARTNERS L.P.
          I.R.S. IDENTIFICATION NO. OF ABOVE PERSON (ENTITIES ONLY):

--------- ----------------------------------------------------------------------------------------------------------
   2      CHECK THE APPROPRIATE BOX IF A MEMBER OF A GROUP*
                                                                                                  (a) /X/  (b) /_/
--------- ----------------------------------------------------------------------------------------------------------
   3      SEC USE ONLY

--------- ----------------------------------------------------------------------------------------------------------
   4      CITIZENSHIP OR PLACE OF ORGANIZATION
                   DELAWARE
----------------------- --------------------------------------------------------------------------------------------
                                 SOLE VOTING POWER
         NUMBER             5           0
           OF                    -----------------------------------------------------------------------------------
         SHARES                  SHARED VOTING POWER
      BENEFICIALLY          6           670,505
        OWNED BY                 -----------------------------------------------------------------------------------
          EACH                   SOLE DISPOSITIVE POWER
        REPORTING           7           0
         PERSON                  -----------------------------------------------------------------------------------
          WITH                   SHARED DISPOSITIVE POWER
                            8           670,505
----------------------- --------------------------------------------------------------------------------------------
   9      AGGREGATE AMOUNT BENEFICIALLY OWNED BY EACH REPORTING PERSON
                   670,505
--------- ----------------------------------------------------------------------------------------------------------
   10     CHECK BOX IF THE AGGREGATE AMOUNT IN ROW (9) EXCLUDES
          CERTAIN SHARES*                                                                                      /_/
--------- ----------------------------------------------------------------------------------------------------------
   11     PERCENT OF CLASS REPRESENTED BY AMOUNT IN ROW 9
                   5.0%
--------- ----------------------------------------------------------------------------------------------------------
   12     TYPE OF REPORTING PERSON*
                   PN
--------- ----------------------------------------------------------------------------------------------------------
</TABLE>


                     * SEE INSTRUCTIONS BEFORE FILLING OUT!

<PAGE>

------------------------------                     ---------------------------
CUSIP NO. 04269E 10 7                  13G                  PAGE 5 OF 8 PAGES
------------------------------                     ---------------------------


<TABLE>
--------- ----------------------------------------------------------------------------------------------------------
  <S>     <C>
   1      NAME OF REPORTING PERSON:
                   BVF INC.
          I.R.S. IDENTIFICATION NO. OF ABOVE PERSON (ENTITIES ONLY):

--------- ----------------------------------------------------------------------------------------------------------
   2      CHECK THE APPROPRIATE BOX IF A MEMBER OF A GROUP*
                                                                                                  (a) /X/  (b) /_/
--------- ----------------------------------------------------------------------------------------------------------
   3      SEC USE ONLY

--------- ----------------------------------------------------------------------------------------------------------
   4      CITIZENSHIP OR PLACE OF ORGANIZATION
                   DELAWARE
----------------------- --------------------------------------------------------------------------------------------
                                 SOLE VOTING POWER
         NUMBER             5           0
           OF                    -----------------------------------------------------------------------------------
         SHARES                  SHARED VOTING POWER
      BENEFICIALLY          6           670,505
        OWNED BY                 -----------------------------------------------------------------------------------
          EACH                   SOLE DISPOSITIVE POWER
        REPORTING           7           0
         PERSON                  -----------------------------------------------------------------------------------
          WITH                   SHARED DISPOSITIVE POWER
                            8           670,505
----------------------- --------------------------------------------------------------------------------------------
   9      AGGREGATE AMOUNT BENEFICIALLY OWNED BY EACH REPORTING PERSON
                   670,505
--------- ----------------------------------------------------------------------------------------------------------
   10     CHECK BOX IF THE AGGREGATE AMOUNT IN ROW (9) EXCLUDES
          CERTAIN SHARES*                                                                                      /_/
--------- ----------------------------------------------------------------------------------------------------------
   11     PERCENT OF CLASS REPRESENTED BY AMOUNT IN ROW 9
                   5.0%
--------- ----------------------------------------------------------------------------------------------------------
   12     TYPE OF REPORTING PERSON*
                   IA, CO
--------- ----------------------------------------------------------------------------------------------------------
</TABLE>


* SEE INSTRUCTIONS BEFORE FILLING OUT!

<PAGE>

------------------------------                     ---------------------------
CUSIP NO. 04269E 10 7                  13G                  PAGE 6 OF 8 PAGES
------------------------------                     ---------------------------


ITEM 1(a).        NAME OF ISSUER:
                  Arqule Inc. ("Arqule")

ITEM 1(b).        ADDRESS OF ISSUER'S PRINCIPAL EXECUTIVE OFFICES:

                  200 Boston Avenue
                  Medford, MA  02155

ITEM 2(a).        NAME OF PERSON FILING:

                  This Second Amendment to Schedule 13G is being filed on behalf
                  of the following persons*:

                  (i)      Biotechnology Value Fund, L.P. ("BVF")
                  (ii)     Biotechnology Value Fund II, L.P. ("BVF2")
                  (iii)    BVF Partners L.P.  ("Partners")
                  (iv)     BVF Inc. ("BVF Inc.")

                  *        Attached as Exhibit A is a copy of an agreement among
                           the persons filing (as specified hereinabove) that
                           this Second Amendment to Schedule 13G is being filed
                           on behalf of each of them.

ITEM 2(b).  ADDRESS OF PRINCIPAL BUSINESS OFFICE:

                           The principal business office of the persons
comprising the group filing this Second Amendment to Schedule 13G is located
at 227 West Monroe Street, Suite 4800, Chicago, Illinois, 60606.

ITEM 2(c).        CITIZENSHIP:

                  BVF:                        a Delaware limited partnership
                  BVF2:                       a Delaware limited partnership
                  Partners:                   a Delaware limited partnership
                  BVF Inc.:                   a Delaware corporation

ITEM 2(d).        TITLE OF CLASS OF SECURITIES:

                  Common Stock, par value $.01.

ITEM 2(e).        CUSIP Number:

                  04269E 10 7


<PAGE>

------------------------------                     ---------------------------
CUSIP NO. 04269E 10 7                  13G                  PAGE 7 OF 8 PAGES
------------------------------                     ---------------------------


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: ONE OF
                  THE FOLLOWING

                  Not applicable as this Second Amendment to Schedule 13G is
filed pursuant to Rule 13d 1(c).

ITEM 4.           OWNERSHIP:

                  The information in items 1 and 5 through 11 on the cover
pages (pp. 2 - 5) on this Second Amendment to Schedule 13G is hereby
incorporated by reference.

ITEM 5.           OWNERSHIP OF FIVE PERCENT OR LESS OF A CLASS:

                  If this statement is being filed to report the fact that as
of the date hereof the reporting person has ceased to be the beneficial owner
of more than five percent of the class of securities check the following. /X/

ITEM 6.           OWNERSHIP OF MORE THAN FIVE PERCENT ON BEHALF OF ANOTHER
                  PERSON:

                  BVF shares voting and dispositive power over the shares of
the common stock it beneficially owns with Partners. BVF2 also shares voting
and dispositive power over the shares of the common stock it beneficially
owns with Partners. Partners and BVF Inc. share voting and dispositive power
over the shares of the common stock they beneficially own with, in addition
to BVF and BVF2, certain managed accounts on whose behalf Partners, as
investment manager, purchased such shares. None of the managed accounts
individually owns more than 5% of the common stock of Arqule.

ITEM 7.           IDENTIFICATION AND CLASSIFICATION OF THE SUBSIDIARY WHICH
                  ACQUIRED THE SECURITY BEING REPORTED ON BY THE PARENT HOLDING
                  COMPANY:

                  Not applicable.

ITEM 8.           IDENTIFICATION AND CLASSIFICATION OF MEMBERS OF A GROUP:

                  Not applicable.

ITEM 9.           NOTICE OF DISSOLUTION OF GROUP:

                  Not applicable.

<PAGE>

------------------------------                     ---------------------------
CUSIP NO. 04269E 10 7                  13G                  PAGE 8 OF 8 PAGES
------------------------------                     ---------------------------


ITEM 10.          CERTIFICATION

                  By signing below I certify that, to the best of my
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.

                  After reasonable inquiry and to the best of my knowledge
and belief, I certify that the information set forth in this statement is
true, complete and correct.

Dated:   June 30, 2000

                  BIOTECHNOLOGY VALUE FUND, 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


                  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 INC.


                  By:      /s/ Mark N. Lampert
                           ----------------------------------
                           Mark N. Lampert
                           President



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