T 0376/05 (Pyrazolopyrimidines/NEUROGEN) of 6.11.2007

European Case Law Identifier: ECLI:EP:BA:2007:T037605.20071106
Date of decision: 06 November 2007
Case number: T 0376/05
Application number: 00967134.8
IPC class: C07D 487/00
Language of proceedings: EN
Distribution: C
Download and more information:
Decision text in EN (PDF, 33.100K)
Documentation of the appeal procedure can be found in the Register
Bibliographic information is available in: EN
Versions: Unpublished
Title of application: Certain alkylene diamine-substituted pyrazolo[1,5,-a]-1,5-pyrimidines and pyrazolo[1,5-a]-1,3,5-triazines
Applicant name: NEUROGEN CORPORATION, et al
Opponent name: -
Board: 3.3.01
Headnote: -
Relevant legal provisions:
European Patent Convention 1973 Art 123(2)
European Patent Convention 1973 Art 113(2)
European Patent Convention 1973 R 71(2)
Keywords: Non appearance at oral proceedings
No comments on the objections raised in the Board's communication
Amendments (not allowable)
Catchwords:

-

Cited decisions:
-
Citing decisions:
-

Summary of Facts and Submissions

I. The appeal lies from the decision of the examining division refusing the present application.

The examining division considered document (D2) to represent the closest prior art, particularly its examples 26 and 48. The problem to be solved was the provision of selective modulators of NPY1 (i.e. neuropeptide Y1 antagonists). The examining division decided it was obvious from documents (D4) and (D5) to replace a bridging carbon in the bicyclic ring system by a bridging nitrogen atom, and hence to yield the compounds defined in the claims.

II. The following documents were inter alia cited during the examination and/or appeal proceedings:

(D2) WO-A-99 40 091

(D4) A. Gringauz, "Introduction to Medicinal Chemistry", 1997, Wiley-VCH, New York, 141-189

(D5) A. Korolkovas, "Essentials of Medicinal Chemistry", 1988, John Wiley & Sons, New York, 579-869

III. The claims on file are those enclosed with the written statement setting out the ground of appeal dated 9 February 2005, namely claims 1 to 42 of the Main Request and claims 1 to 35 of the Auxiliary Request.

The wording of claim 1 of the Main Request that is relevant to this decision reads as follows:

"1. A compound of the formula

FORMULA/TABLE/GRAPHIC

or a pharmaceutically acceptable salt, hydrate, or acylated prodrug thereof, wherein:

X is N or CR**(14);

R**(1) is selected from H, C1-C6 alkyl, C3-C10 cycloalkyl, (C3-C10 cycloalkyl) C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, cyano, halo, C1-C6 haloalkyl, OR**(7), C1-C6 alkyl-OR**(7); C1-C6 cyanoalkyl, NR**(8)R**(9), C1-C6 alkyl-NR**(8)R**(9);

R**(2) is H, C1-C6 alkyl which optionally forms a C3-C6 aminocarbocycle or a C2-C5 aminoheterocycle with A or B, each of which is optionally substituted with R**(7),

C3-C10 cycloalkyl, or (C3-C10 cycloalkyl) C1-C6 alkyl; or

R**(2) and R**(6) jointly with the 2 nitrogen atoms to which they are bound, form a C2-C5 aminoheterocycle optionally substituted with R**(7), or

R**(2) and A jointly form a C3-C6 aminocarbocycle or a C2-C5 amino heterocycle optionally substituted at with R**(7);

A represents an alkyl chain of 1,2, or 3 carbon atoms which is optionally mono- or di-substituted at each carbon with substituents independently selected from C1-C6 alkyl, C3-C10 cycloalkyl, (C3-C10 cycloalkyl) C1-C6 alkyl, C1-C6 alkenyl, C2-C6 alkynyl, cyano, halo, C1-C6 haloalkyl, OR**(7), C1-C6 alkyl-OR**(7); C1-C6 cyanoalkyl, NR**(8)R**(9), and C1-C6 alkyl-NR**(8)R**(9), or

A and B jointly form a C3-C6 carbocycle, optionally substituted at each atom with R**(7);

B represents an alkyl chain of 1,2 or 3 carbons atoms, which is optionally mono- or di-substituted at each carbon with substituents independently selected from C1-C6 alkyl, C3-C10 cycloalkyl, (C3-C10 cycloalkyl) C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, cyano, halo, C1-C6 haloalkyl, OR**(7), C1-C6 alkyl-OR**(7); C1-C6 cyanoalkyl, NR**(8)R**(9), and C1-C6 alkyl-NR**(8)R**(9), or

B and R**(2) jointly form a C3-C6 aminocarbocycle, which is optionally substituted at each atom with R**(7), or

B and R**(6) jointly form a C3-C6 aminocarbocycle, which is optionally substituted at each atom with R**(7);

R**(3) is selected from H, C1-C6 alkyl, C3-C10 cycloalkyl, (C3-C10 cycloalkyl) C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, cyano, halo, C1-C6 haloalkyl, OR**(7), C1-C6 alkyl-OR**(7), C1-C6 cyanoalkyl, NR**(8)R**(9), C1-C6 alkyl-NR**(8)R**(9);

R**(4) is selected from aryl or heteroaryl, each of which is substituted with 1 to 5 substituents independently selected from C1-C6 alkyl, C3-C10 cycloalkyl, C3-C10 cycloalkenyl, (C3-C10 cycloalkyl) C1-C6 alkyl, C1-C6 alkenyl, C1-C6 alkynyl, halogen, C1-C6 haloalkyl, OR**(7), C1-C6 alkyl-OR**(7), NR**(8)R**(9), C1-C6 alkyl-NR**(8)R**(9), CONR**(8)R**(9), C1-C6 alkyl-CONR**(8)R**(9), COOR**(7), C1-C6 alkyl-COOR**(7), CN, C1-C6 alkyl-CN, SO2NR**(8)R**(9), SO2R**(7), aryl, heteroaryl, heterocycloalkyl, 3-, 4-, or 5-(2-oxo-1,3-oxazolidinyl), wherein at least one of the positions ortho or para to the point of attachment of the aryl or heteroaryl ring to the pyrazole is substituted;

R**(5) is selected from: C1-C6 alkyl, (C3-C10 cycloalkyl) C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, each of which is substituted with 1 to 5 groups independently selected at each occurrence from

R**(14) is H, Cl-C6 alkyl, C3-C10 cycloalkyl, (C3-C10 cycloalkyl) C1-C6 alkyl, C2-C4 alkenyl, C2-

C4 alkynyl, halo, or CN."

The claims of the Auxiliary Request differ from those of the Main Request in that the following parts were deleted

- claims 3 to 6 and 11 to 13 in total;

- in claim 1 some of the meanings given for the radicals R**(1), R**(6) and R**(14);

- in claim 26, the first, eighth and 26th compounds mentioned therein.

IV. As an annex to the summons to oral proceeding dated 31 July 2007, the Board issued a communication summarising its preliminary and non-binding opinion on the case and raised, inter alia, under point 6 the following objections under Article 123 (2) EPC:

"Claim 12 of the Main Request is based on claim 24 as originally filed. The information contained in claim 12 of the Main Request in the four last lines on page 14 of the claims is taken from claim 1 as originally filed. Although this information was present in claim 1 as originally filed, the special combination of meanings of the radicals R**(4) and R**(5) have not been disclosed in the application as filed in combination with the limitations of present claim 12. Therefore, this amendment contravenes the requirements of Article 123 (2) EPC.

6.2 The combination of features of claim 23 of the Main Request is only disclosed in the application as originally filed with the definition of X limited to "N or CH" (see original claim 34). The amendment in claim 23 which now allows X also to mean CR**(14) where R**(14) is not hydrogen thus contravenes the requirements of Article 123 (2) EPC.

6.3 Present claims 27 to 29 of the Main Request and claims 20-22 of the Auxiliary Request refer to compounds, "wherein in an assay of NPY binding the compound exhibits an Ki " of up to certain concentrations. The application as originally filed only discloses such concentrations in connection with the "human NPY1 binding assay" (see page 15, lines 6-9). The claims mentioned above also cover concentration determined by non human assays and the binding to receptors NPY receptors other than NPY1 and thus contravene the requirements of Article 123 (2) EPC.

6.4 Claim 30 of the Main Request and of claim 23 of the Auxiliary Request are directed to the use of the compounds "for production of a medicament for treating ... cardiovascular diseases." This added claim has no basis in the application as originally filed which only discloses the treatment of "certain cardiovascular diseases, for example hypertension." (see the first paragraph on page 4; emphasis added)."

V. The Appellant did not comment on the objections raised in this communication. In his telefax of 5 November 2007 he notified the Board that he did not intend to appear at the oral proceedings.

VI. The Appellant requested that the decision under appeal be set aside and a patent be granted based on the claims of the Main Request or of the Auxiliary Request.

VII. The oral proceedings took place on 6 November 2007 in the absence of the Appellant. At the end of the proceedings, the decision of the Board was announced.

Reasons for the Decision

1. The appeal is admissible.

2. The Appellant has had, in accordance with Article 113 (1) EPC, an opportunity to present his comments on the detailed objections raised in the Board's communication of 31 July 2007, but has not availed himself of this opportunity.

3. On considering the case at the oral proceedings, duly held persuant to Rule 71 (2) EPC despite the absence of the Appellant, the Board sees no reason to depart from the preliminary opinion expressed in the communication and comes to the conclusion that amended claims 12, 23 and 27 to 30 of the Main Request and amended claims 20 to 23 of the Auxiliary Request contain subject-matter which extends beyond the content of the application as filed.

4. Hence the amended claims of both the Main Request and the Auxiliary Request do not comply with the requirements of Articles 123 (2) EPC, so that the appeal must be dismissed.

ORDER

For these reasons it is decided that:

The appeal is dismissed.

Quick Navigation