T 0357/98 (Lactam-quinolones/PROCTER & GAMBLE) of 13.1.2000

Summary of Facts and Submissions

I. The appeal lodged on 22 December 1997 lies from the decision of the Examining Division posted on 21 October 1997 refusing European patent application No. 89 202 635.2 (European publication No. 366 189).

II. The decision of the Examining Division was based on claims 1 to 15 filed with letter dated 3 June 1997 according to the then pending request. The Examining Division held that the claims, in particular independent claim 1 as amended, contained subject-matter which extended beyond the content of the application as filed, thus contravening Article 123(2) EPC.

The Examining Division held in particular that the limitation of the group B to a penicillinyl-moiety in the general formula of claim 1 represented a selection lacking disclosure in the application as filed, that the specific heteroatoms in the heterocycles as defined in claim 1 had no counterpart in the application as filed and that in claim 1 the optional substitution of the carbocycles and heterocycles as disclosed in the original application was missing.

III. The Appellant (Applicant) submitted amended claims 1 to 17. on 27 February 1998 together with the Statement of Grounds of Appeal and additionally on 27 July 1999. He argued that the amendments made to the claims overcame the objections raised in the decision under appeal.

IV. In a communication from the Board pursuant to Article 11(2) of the rules of procedure of the Boards of Appeal, the Appellant's attention was drawn to additional aspects and objections in the assessment of whether or not the amendments made satisfy the requirements of Article 123(2) EPC. Furthermore, the Appellant was informed that any fresh set of claims extending the scope of the claims compared with that of the claims in the decision under appeal restoring deficiencies previously raised in examination proceedings and met by the restrictions previously made to the claims may not be admitted in the appeal proceedings pursuant to Rule 86 (3) EPC.

In reply, the Appellant submitted on 20 December 1999 new claims 1 to 16 requiring a written opinion on the allowability of these claims. He argued essentially that the amendments now made found support in the application as filed and he referred to particular sections of the original application. With respect to the penicillinyl-moiety for group B in claim 1 as amended he pointed to the penem structure disclosed on page 19, line 15 and following of the application as filed. Fresh claim 1 as amended read as follows:

"1. A compound having the structure:

FORMULA

wherein in the group (Q)

(1) A1 is N or C(R7); where

(i) R7 is hydrogen, hydroxy, alkoxy, nitro, cyano, halogen, C1-C8 alkyl, or N(R8)(R9), and

(ii) R8 and R9 are, independently, R8a where R8a is hydrogen; C1-C8 alkyl; C2-C8 alkenyl; a 3-9 atom monocyclic or 7-17 atom polycyclic carbocycle; or a 3-9 atom monocyclic or 7-17 atom polycyclic heterocycle; or R8 and R9 together form a 3-9 atom monocyclic or 7-17 atom polycyclic heterocycle including the nitrogen to which they are bonded; and wherein said heterocycles have one or more heteroatoms selected from O, N or S;

(2) A2 is N or C(R2); where R2 is hydrogen or halogen;

(3) A3 is N or C(R5); where R5 is hydrogen;

(4) R1 is hydrogen or R15;

(5) R3 is hydrogen, halogen, or R16;

(6) R15 is C1-C8 alkyl; a 3-9 atom monocyclic or 7-17 atom polycyclic carbocycle; a 3-9 atom monocyclic or 7-17 atom polycyclic heterocycle; alkoxy; hydroxy; C2-C8 alkenyl; arylalkyl; or N(R8)(R9); and wherein said arylalkyl is a C1-C8 alkyl substituted with an aryl group; wherein said heterocycles have one or more heteroatoms selected from O, N or S;

(7) R16 is C1-C8 alkyl; a 3-9 atom monocyclic or 7-17 atom polycyclic carbocycle; or a 3-9 atom monocyclic or 7-17 atom polycyclic heterocycle; wherein said heterocycles have one or more heteroatoms selected from O, N or S;

(8) R4 is hydroxy; and

(9) R6 is hydrogen, halogen, nitro, or N(R8)(R9); and wherein:

(1) when A1 is C(R7), R1 and R7 may together form a 3-9 atom monocyclic or 7-17 atom polycyclic heterocycle including N' and A1; wherein said heterocycles have one or more heteroatoms selected from O, N or S;

(2) when A2 is C(R2), R2 and R3 may together form -O-(CH2)n-O-, where n is an integer from 1 to 4;

(3) when A3 is C(R5), R4 and R5 may together form a 3-9 atom monocyclic or 7-17 atom polycyclic heterocycle including the carbon atoms to which R4 and R5 are bonded and the carbon atom to which said carbon atoms are bonded; and wherein said heterocycles have one or more heteroatoms selected from O, N or S; and

(4) when A3 is C(R5), R1 and R5 may together form a 3-9 atom monocyclic or 7-17 atom polycyclic heterocycle including N' and the adjacent carbon to which R5 is bonded; and wherein said heterocycles have one or more heteroatoms selected from O, N or S;

wherein, in the group (B)

R10 is hydrogen; halogen; C1-C8 alkyl; C2-C8 alkenyl; a 3-8 atom heteroalkyl having 1 or 2 heteroatoms selected from O, N or S; a 3-9 atom monocyclic or 7-17 atom polycyclic carbocycle; a 3-9 atom monocyclic or 7-17 atom polycyclic heterocycle; R8a-O-; R8aCH=N-; (R8)(R9)N-; R17-C(=CHR20)-C(=O)NH-; R17-C(=NO-R19)-C(=O)NH-; or R18-(CH2)m-C(=O)NH-; and wherein said heterocycles have one or more heteroatoms selected from O, N or S; and where

(1) m is an integer from 0 to 9;

(2) R17 is hydrogen; C1-C8 alkyl; C2-C8 alkenyl; a 3-8 atom heteroalkyl having 1 or 2 heteroatoms selected from O, N or S; a heteroalkenyl having 2 to 8 carbon atoms and heteroatoms selected from O, N or S; a 3-9 atom monocyclic or 7-17 atom polycyclic carbocycle; or a 3-9 atom monocyclic or 7-17 atom polycyclic heterocycle; wherein said heterocycles have one or more heteroatoms selected from O, N or S;

(3) R18 is R17, -Y1, or -CH(Y2)(R17);

(4) R19 is R17; arylalkyl; heteroarylalkyl; -C(R22)(R23)COOH; -C(=O)O-R17; or -C(=O)NH-R17; wherein said arylalkyl is a C1-C8 alkyl substituted with an aryl group and wherein said heteroarylalkyl is a C1-C8 alkyl substituted with a heteroaryl group having one or more heteroatoms selected from O, N or S; and where R22 and R23 are, independently, R17 or together form a 3-9 atom monocyclic or 7-17 atom polycyclic carbocycle or a 3-9 atom monocyclic or 7-17 atom polycyclic heterocycle, including the carbon atom to which R22 and R23 are bonded; and wherein said heterocycles have one or more heteroatoms selected from O, N or S;

(5) R20 is R19, halogen -Y1, or -CH(Y2)(R17);

(6) Y1 is -C(=O)OR21, -C(=O)R21, -N(R24)R21, -S(O)pR29, or -OR29; and Y2 is Y1 or -OH, -SH, or -SO3H;

(a) p is an integer from 0 to 2;

(b) R24 is hydrogen; C1-C8 alkyl; C2-C8 alkenyl; a 3-8 atom heteroalkyl having 1 or 2 heteroatoms selected from O, N or S; a heteroalkenyl having 2 to 8 carbon atoms and heteroatoms selected from O, N or S; a 3-9 atom monocyclic or 7-17 atom polycyclic carbocycle; a 3-9 atom monocyclic or 7-17 atom polycyclic heterocycle; -SO3H; -C(=O)R25; or, when R18 is -CH(N(R24)R21)R17), R24 and R21 may together form a 3-9 atom monocyclic or 7-17 atom polycyclic heterocycle; wherein said heterocycle consists of one or more heteroatoms selected from O, N or S; and

(c) R25 is R17; NH(R17); N(R17)(R26); O(R26); or S(R26); where R26 is C1-C8 alkyl; C2-C8 alkenyl; a 3-9 atom monocyclic or 7-17 atom polycyclic carbocycle; a 3-9 atom monocyclic or 7-17 atom polycyclic heterocycle; or when R25 is N(R17)(R26), R26 and R17 may together form a 3-9 atom monocyclic or 7-17 atom polycyclic heterocycle; wherein said heterocycles have one or more heteroatoms selected from O, N or S; and

(7) R21 is R29 or hydrogen; where R29 is C1-C8 alkyl; C2-C8 alkenyl; arylalkyl consisting of a C1-C8 alkyl substituted with an aryl group; a 3-8 atom heteroalkyl having 1 or 2 heteroatoms selected from O, N or S; a heteroalkenyl having 2 to 8 carbon atoms and heteroatoms selected from O, N or S; heteroarylalkyl, consisting of a C1-C8 alkyl substituted with a heteroaryl group substituted with one or more heteroatoms selected from O, N or S; a 3-9 atom monocyclic or 7-17 atom polycyclic carbocycle; a 3-9 atom monocyclic or 7-17 atom polycyclic heterocycle; or, when Y1 is N(R24)R21 and R21 is R29, R21 and R24 may together form a 3-9 atom monocyclic or 7-17 atom polycyclic heterocycle including the nitrogen atom to which R24 is bonded; wherein said heterocycles have one or more heteroatoms selected from O, N or S;

R11 is hydrogen, halogen, alkoxy, or R27C(=O)NH-, where

R27 is hydrogen or C1-C8 alkyl; and

L links Q to B; and L is L', -X2t-R39-L', or -X3t-R39-L', where L' is Q', -X2-Q', -X3-Q'', -X4t- C(=Y3u)-Z-Q'', -X5t-PO(Y4u R8a)-Z'-Q'', or X5tSO2-Z'-Q'';

(1) t and u are, independently, 0 or 1;

(2) R39 is C1-C8 alkyl, C2-C8 alkenyl, a 3-8 atom heteroalkyl having one or two heteroatoms selected from O, N or S, a heteroalkenyl having 2 to 8 carbon atoms and heteroatoms selected from O, N or S, a 3-9 atom monocyclic or 7-17 atom polycyclic heterocycle; and wherein said heterocycles have one or more heteroatoms selected from O, N or S;

(3) X2 is oxygen, or S(O)v, where v is an integer from 0. to 2;

(4) X3 is nitrogen; N(R40); N+(R41)(R42); or R43-N(R41); where

(a) R40 is R8a; -O R8a; or -C(=O)R8a;

(b) R41 and R42 are, independently, hydrogen; C1-C8 alkyl; C2-C8 alkenyl; a 3-9 atom monocyclic or 7-17 atom polycyclic or a 3-9 atom monocyclic or 7-17 atom polycyclic heterocycle, or, together with Q'', comprise a 3-9 atom monocyclic or 7-17 atom polycyclic heterocycle as R15 or R16; and wherein said heterocycles have one or more heteroatoms selected from O, N or S;

(c) R43 is N(R41), oxygen or sulfur;

(5) X4 is oxygen, sulfur, NR40, or R43-NR41;

(6) X5 is oxygen or NR41;

(7) Y3 is oxygen, sulfur, N(R40) or N+(R41)(R42);

(8) Y4 is oxygen or NR41;

(9) Z is nil, oxygen, sulfur, nitrogen, NR40, or N(R41)-R43;

(10) Z' is nil, oxygen, nitrogen, or NR41;

(11) Q' is R15 or R16; and

(12) Q'' is Q'; or together with X2, X3, Z or Z', is an R15 or R16 group;

wherein references herein to carbocycle(s) and heterocycle(s) mean substituted or unsubstituted ring radicals; and pharmaceutically-acceptable salts and biohydrolyzable esters thereof, and hydrates thereof."

VI. The Appellant requested in writing that the decision under appeal be set aside and that a patent be granted on the basis of claims 1 to 16 filed with the letter dated 20 December 1999.

VII. Oral proceedings were held on 13 January 2000 in the absence of the Appellant who, after having been duly summoned, informed the Board with the letter dated 5. January 2000 that he withdrew his auxiliary request for oral proceedings. At the end of the oral proceedings the decision of the Board was given orally.

Reasons for the Decision

1. The appeal is admissible.

2. The issue arising from this appeal is whether or not the claims, in particular independent claim 1 as amended, satisfy the requirements of Article 123(2) EPC, which is stated in the decision under appeal as being the sole ground for refusal of the application.

3. Amendments (Article 123(2) EPC)

3.1. The subject-matter of claim 1 is based on claim 1 of the application as originally filed. The formula of the penicillinyl-moiety for the group B in both general formulae of claim 1 is supported by page 19, lines 15 to 30 of the application as filed wherein the ring member W is S. The linkage of the group (Q) to the groups (L) and (B) via the group R15 in the one general formula or via the group R16 in the other general formula of claim 1 represents the graphical reproduction of the typewritten alternative embodiments (I) (C) (1) and (I) (C) (2) of claim 1 as filed, respectively. The definitions of the chain length of the alkyl and alkenyl groups as having 1 to 8 or 2 to 8 carbon atoms, respectively, find support on page 15, lines 5 and 13 of the application as filed. The carbocyclic and heterocyclic rings are defined on page 15, lines 15, 18 to 20, 24 and 28 to 30 of the original application to be substituted or unsubtituted and to be a 3-9 atom monocyclic or 7-17 atom polycyclic carbocycle or heterocycle, thus, providing a proper basis for the respective amendments throughout claim 1. Page 15, lines 1 and 26 of the application as filed backs up the features of claim 1 that the heterocycles have one or more heteroatoms and that the latter are selected from O, N or S. The definition of the arylalkyl and heteroarylalkyl groups in claim 1 to consist of a C1-C8 alkyl substituted with an aryl or heteroaryl group having one or more heteroatoms selected from O, N or S, respectively, is found on page 16, line 9 in combination with page 15, lines 1, 5, 24 to 26 and 34 of the application as filed. The number of 3-8 atoms and of 1 or 2 heteroatoms comprised in the heteroalkyl groups of claim 1 is based on page 15, lines 9 to 11 of the original application. The definition of the heteroalkenyl groups in claim 1 as having 2 to 8 carbon atoms finds support on page 15, lines 12 and 13 of the application as filed. The reformulated wording "and wherein" comprised in between the first and the second section of the list of definitions for the group (Q) clarifies merely the original fact that the second section recite definitions in addition to those of the first section, without adding subject-matter extending beyond the content of the application as filed.

3.2. The further claims 2 to 16 find a basis in claims 5 to 13, 15 and 17 to 20 as originally filed.

3.3. For these reasons, the Board concludes that the claims 1 to 16 as amended meet the requirements of Article 123(2) EPC.

4. Remittal

4.1. It follows from the above, that by substantially amending the refused independent claim 1, the Appellant has overcome the objections pursuant to Article 123(2) EPC raised in the decision under appeal. The examination not yet having been concluded, the Board exercises its power under Article 111(1) EPC to remit the case to the Examining Division for further prosecution.

4.2. The Board has noted some misprints within claim 1 giving rise to unclarity, namely:

- in the second general formula the chemical bond between the ring member N' and the substituent R1 is missing and the ring member N'' does not clearly form the bridge atom;

- in both general formulae the zigzag line linking the penicilinyl moiety (B) and the group (L) shows two edges which appears ambiguous since it symbolizes one methylene group;

- the wordings "consists of" and "substituted with" comprised in the definitions (6)(b) or (7) of the group (B), respectively, appear to be inappropriate in the given context of a heterocycle or a heteroaryl group, respectively;

- the opening bracket for R17 is missing in the definition (6)(b) of the group (B); and

- the term "carbocycle" is missing in the definition (4) (b) of the group (L) in claim 1.

Any corrective action which may become necessary to bring the dependent claims into line with the amendments made to independent claim 1 is left to the Appellant and the Examining Division.

ORDER

For these reasons it is decided that:

1. The decision under appeal is set aside.

2. The case is remitted to the first instance for further prosecution.