T 0469/97 (Heteroarylpiperidines, pyrrolidines and piperazines) of 28.6.2000

European Case Law Identifier: ECLI:EP:BA:2000:T046997.20000628
Date of decision: 28 June 2000
Case number: T 0469/97
Application number: 92924151.1
IPC class: C07D 261/20
Language of proceedings: EN
Download and more information:
Decision text in EN (PDF, 52.632K)
Documentation of the appeal procedure can be found in the Register
Bibliographic information is available in: EN
Versions: Unpublished
Title of application: Heteroarylpiperidines, Pyrrolidines and Piperazines and their use as Antipsychotics and Analgetics
Applicant name: Aventis Pharmaceuticals Inc.
Opponent name: -
Board: 3.3.01

Headnote

-
Relevant legal provisions:
European Patent Convention 1973 Art 123(2)
European Patent Convention 1973 Art 54(2)
European Patent Convention 1973 Art 111(1)
European Patent Convention 1973 R 88
Keywords: Main request - support in the application as filed (no)
First auxiliary request - correction of obvious mistake (no) - support in the application as filed (no)
Second auxiliary request - support in the application as filed (yes) - novelty (yes)
Remittal to first instance for further prosecution
Catchwords:

-

Cited decisions:
G 0003/89
G 0011/91
T 0493/90
T 0532/95
Citing decisions:
-

Summary of Facts and Submissions

I. The Appellant (Applicant) lodged an appeal on 7 January 1997 against the decision of the Examining Division posted on 19 November 1996 refusing European patent application 92 924 151.1 (European publication No. 0 612 318).

II. The decision of the Examining Division was based on claims 1 to 221 filed with letter dated 21 May 1996 in response to the first official communication. The Examining Division held that:

- the subject-matter of claims 1, 152, 169, 174, 183, 185 to 187, 191 to 200, 205 and 216 to 221 failed to satisfy the requirements of Article 123(2) EPC. The Examining Division noted, in particular, that the second disclaimer of claim 152 had been amended in such a way that different compounds were now excluded,

- the subject-matter of claims 1, 169 and 191 failed to satisfy the requirements of Article 84 EPC and

- the subject-matter of claims 1, 2, 10 to 64, 68, 106, 107, 152 to 154, 156, 157, 159, 162, 169 to 178 and 179 to 182 failed to satisfy the requirements of Article 54 EPC in view of the following documents:

(1) EP-A-0 402 644

(2) EP-A-0 398 425

(3) GB-A-2 163 432

(4) EP-A-0 196 096.

III. With the Statement of Grounds of Appeal, the Appellant submitted in essence that the Examining Division had not invited the Applicant as often as necessary to file his observations as provided by Article 96(2) EPC and that the refusal of the application was based on grounds or evidence on which Applicant had not had a full opportunity to present its comments contrary to the provisions of Article 113(1) EPC and requested:

- As the main request, that the contested decision be set aside for "substantial procedural violation" (Article 96(2) and Article 113(1) EPC) and the case be remitted to the Examining Division,

- As the first auxiliary request, that the European patent application be remitted to the first instance with the order to grant a patent on the basis of the refused claims 1 to 221,

- As the second auxiliary request that the European patent application be remitted to the first instance with the order to grant a patent on the basis of the claims 1 to 149 filed with the statement of grounds of appeal,

- As the third auxiliary request, that the European application be remitted to the first instance with the order to grant a patent on the basis of the claims 1 to 26 filed with the statement of the grounds of appeal.

IV. With a letter of 30 July 1999, the Appellant requested as the fourth auxiliary request that the European application be granted on the basis of another set of claims 1 to 28. With letter of 30 December 1999, the Appellant abandoned all the previous requests except the fourth auxiliary request, the latter becoming therefore the main request.

V. In response to a communication of the Board dated 2. February 2000, the Appellant submitted on 30 May 2000 as sole request a new set of claims 1 to 25 and requested that the case be remitted to the first instance for further prosecution.

VI. At the oral proceedings which took place on 28 June 2000, the Appellant submitted, in addition to the main request (see point V above), two sets of claims as auxiliary requests I (claims 1 to 28), II (claims 1 to 48), respectively. Independent claims of each request are quoted below as far as necessary in the context of this decision.

(a) Main request

1. A compound of the formula:

FORMULA (I)

wherein

X is -O-, -S-, -NH-, or -N-R2

R2 is selected from the group consisting of C1-C6 alkyl, aryl C1-C6 alkyl, aryl, cycloalkyl, aroyl, alkanoyl, and phenylsulfonyl groups;

p is 1 or 2;

Y is hydrogen, C1-C6 alkyl, hydroxy, chlorine, fluorine, bromine, iodine, C1-C6 alkoxy, trifluoromethyl, nitro, or amino, when p is 1;

Y is C1-C6 alkoxy, hydroxy or halogen when p is 2 and X is -O-;

Q1 is selected from the group consisting of:

FORMULA (a)

and

FORMULA (b)

where Z is -CH- or -N-; and Y2 is

FORMULA

in which (R1) is R20, R21 or R22, wherein:

R20 is -(CH2)n- where n is 2, 3, 4 or 5;

R21 is

-CH2-CH=CH-CH2-,

-CH2-C C-CH2-,

-CH2-CH=CH-CH2-CH2-,

-CH2-C C-CH2-CH2-, or

-CH2 -CH2-C C-CH2-,

the -CH=CH- bond being cis or trans;

R22 is R20 or R21 in which one or more carbon atoms of R20 or R21 are substituted by at least one C1-C6 linear alkyl group, phenyl group or

FORMULA

where Z1 is C1-C6 alkyl, -OH, C1-C6 alkoxy, -CF3, -NO2, NH2 or halogen; R4 is hydrogen, C1-C6 alkyl, C1-C6 alkoxy, hydroxy, amino, mono- or dialkylamino, C1-C3 acyl amino, C1-C6 alkanoyl, trifluoromethyl, chlorine, fluorine, bromine, -O-C(=O)-(C1-C12 straight or branched chain) alkyl or -C(=O)-aryl; in which aryl is phenyl or

FORMULA

where R5 is hydrogen, C1-C6 alkyl, C1-C6 alkoxy, hydroxy, chlorine, fluorine, bromine, iodine, C1-C6 monoalkylamino, C1-C6 dialkylamino, nitro, cyano, trifluoromethyl, trifluoromethoxy; with the proviso that in formula (I), Z is not

-N-, when X is -S-, Y is hydrogen, C1-C6 alkyl, hydroxy, halogen, C1-C6 alkoxy, CF3, R1 is -R20-, and R4 is hydrogen;

all geometric, optical and stereoisomers thereof, or a pharmaceutically acceptable acid addition salt thereof.

23. 6-aceto-2-[4-(6-fluoro-1,2-benzisoxazol-3-yl)-1- piperidinyl]-methyl-1,4-benzodioxan; or 2-[4-(6-fluoro-1,2- benzisoxazol-3-yl)-1-piperidinyl]-methyl- 1,4-benzodioxan, or a pharmaceutical acceptable acid addition salt thereof.

24. A pharmaceutical composition comprising a compound according to any one of claims 1 to 23 and a pharmaceutically acceptable carrier.

25. Use of a compound having one of the formula I or I' for the preparation of a medicament for treating psychoses, where I is as defined in claim 1 and I' represents

FORMULA (I)

wherein

X, R2, p, Y, are as defined in claim 1,

Q1 is selected from the group consisting of:

FORMULA (a)

and

FORMULA (b)

where Z is -CH- or -N-; and

Y2 is

in which:

n is 1 or 2;

R4 is hydrogen or -C(=O)-CH3

all geometric, optical and stereoisomers thereof,

or a pharmaceutically acceptable acid addition salt thereof.

(b) First auxiliary request

The first auxiliary request differs essentially from the main one in that the proviso of claim 1 was amended to read:

"with the proviso that in formula (4) R4 is not H when R1

is R20, Z is -N- (emphasized by the Board), X is -S-, Y is hydrogen, halogen, lower alkyl, lower alkoxy, hydroxy or trifluoromethyl, and p is 1 or 2;"

A new product claim 19 was added related essentially to the compound of formula I' as defined in the claim 25 of the main request.

(c) Second auxiliary request

The second auxiliary request differs essentially from the main one in that:

- in claim 1, the substituent Z is -N- was cancelled (the compounds of formula (I) being restricted to piperidine derivatives) and the proviso was amended to read

"with the proviso that R4 is not H when R1 is

R20, Z is not -N-, X is -S-, Y is hydrogen, halogen, C1-C6 alkyl, C1-C6 alkoxy, hydroxy or trifluoromethyl, and p is 1 or 2;"

- in use claim 23 (which corresponds essentially to the claim 25 of the main request), the proviso was deleted and the formula (b) of the substituent Q1 in formula I' was cancelled.

- dependent use claims 24 to 48 are based on the dependent product claims 2 to 22.

VII. The Appellant's submissions both in the written proceedings and at the oral proceedings can be summarised as follows:

VII.1 Although the proviso present in claim 1 of the main request excluded piperazine compounds, while the proviso as filed excluded the corresponding piperidine compounds, this change was supported by document (3) which disclosed the excluded piperazine compounds.

VII.2 In the wording of the proviso of claim 1 of the first auxiliary request, the deletion of the word "not" was to be considered as the correction of an obvious mistake which should be allowed according to Rule 88 EPC. In particular, it was clear, in view of the description as filed that among the seventeen provisos present, only the proviso at stake contained a double negation and, therefore, the man skilled in the art would have noted that an error was present. Moreover, most of the examples related to piperidine compounds and the proviso of the application as filed was not in line with the said disclosure taken as a whole. The correction was furthermore obvious in view of the disclosure of document (3).

VII.3 The subject-matter of the claims of the three requests (main request, first and second auxiliary requests) directed to the compounds or to pharmaceutical compositions was novel over document (3). Concerning the subject-matter of the claims directed to the use of compounds for treating psychoses, the disclosure of document (3) showed no evidence of any tests effectively carried out to determine the antipsychotic effect of the disclosed compounds. It was, in particular pointed out that the tests described page 6, lines 5 to 37 related to the measure of the drugs's analgesic activity.

VIII. The Appellant requested that the decision be set aside and that the matter be remitted to the first instance for further prosecution on the basis of the claims of the main request of 26 May 2000, or of the claims of the first or second auxiliary request submitted at the oral proceedings on 28 June 2000.

IX. At the end of the oral proceedings the decision of the board was given orally.

Reasons for the Decision

1. The appeal is admissible.

Main request

2. Article 123(2) EPC - Fair basis

2.1. The Appellant admitted in the course of the oral proceedings that claim 1 of the main request contained a proviso excluding piperazine compounds, while a proviso excluding piperidine compounds was present in the description and claims as filed. This amounts to the incorporation of a material (piperidine compounds) originally excluded. The present claim 1 extends, therefore, beyond the content of the application as filed and does not meet the requirement of Article 123(2) EPC.

2.2. For this reason the present main request is not allowable.

First auxiliary request

3. Article 123(2) - Rule 88 EPC Corrections of errors

3.1. The Appellant submitted that an error had occurred in the description of the application as filed so that its text did not conform to what was intended and he sought to correct that error in order to bring the text and the claim 1 of the present request into conformity with the intended wording.

3.2. In order for a correction under Rule 88, second sentence, EPC to be allowable, it must be established

(a) that an error is in fact present in the document filed at the EPO, and

(b) that the correction of the error is obvious in the sense that it is immediately evident that nothing else would have been intended than what is offered as the correction.

(see T 493/90 of 10 December 1991, point 2 and T 532/95 of 4 March 1999, point 3.2.1 of the reasons for the decision).

3.3. With respect to the above requirement (a), the application in suit as filed must contain such an obvious error that a skilled person has no doubt that this information is not correct and - considered objectively - cannot be to read as such (see opinion G 3/89 and decision G 11/91, OJ EPO 1993, 117 and 125, point 5 of the reasons for the decision). In the present case the proviso present in the description as filed excludes some piperidine compounds as admitted by the Appellant. The Board notes, first, that this proviso is clear in the sense there is no ambiguity as to the excluded compounds. The argument of the Applicant regarding the non compliance of the said proviso with the examples is not convincing given that the Appellant has not shown that any example fell within the definition of the proviso. There is no discrepancy between the examples and the said proviso. Furthermore, the double negation present in the said proviso is certainly not in line with the wordings of the other provisos. However, as already mentioned, this singular wording does not lead to any ambiguity and given that it is the sole expression used in the application as filed (page 15, bottom paragraph; page 28, third paragraph; claim 1, page 210, third paragraph; claim 191, page 268, third paragraph; claim 192, page 277, third paragraph and claim 194, page 295, third paragraph), it cannot be deduced therefrom that an error is present. The other argument regarding the fact that this proviso was intended to exclude the compounds of document (3) is also not acceptable because document (3) is not cited in the application as filed, so this is not an intention the reader could deduce from the original application text.

3.4. It is the Board's conclusion that the new wording of the proviso present in claim 1 of the present request is not allowable as a correction under Rule 88 EPC and, therefore, that the subject-matter of claim 1 of the first auxiliary request extends beyond the content of the application as filed contrary to the requirement of Article 123(2) EPC.

4. Second auxiliary request

4.1. Articles 123(2) and 84 EPC

4.2. The subject-matter of claim 1 is based on the claim 1 of the application as originally filed with the further restriction to compounds of formula (I) wherein Y2 is a benzodioxan-2-yl hydrocarbylene group of formula (4) and that expressions such as "lower" alkyl or alkyleneyl mean "C1-C6" (see page 18, lines 14 ff. of the application as filed) , the substituent (a) being itself limited to the piperidine moiety (Z is -CH-).

4.3. The Board sees no objection under Article 123(2) EPC against the present claim 1. In particular, the restrictions set out in point 4.2 above do not amount to a selection of a specific sub-class of compounds not disclosed in the application as filed but, on the contrary, consist of a limitation to possibilities each of which was already disclosed in the application as filed. The claim is also clear.

4.4. However, the Board has noted that the term ", Z is I not -N-" present in the wording of the proviso was redundant as this meaning had been cancelled (see point 4.2 above). Such a correction is left to the Appellant and the Examining Division in the subsequent prosecution.

4.5. The subject-matter of dependent claims 2 to 22 is supported by the application as filed:

- claims 2 to 9 are respectively supported by the application as filed, namely claim 95; claim 153; claim 154; claim 157; claim 158; claim 159; claim 160; claim 161.

- claims 10 to 16 are supported by the application as filed page 31, first and second paragraph and page 18, lines 14 ff.

- claim 17 is supported by the application as filed, page 34, line 9.

- claims 18 to 20 are supported by the application as filed, page 64, first paragraph.

- claim 21 is supported by the application as filed, namely claims 93 and 94.

- claim 22 is supported by the application as filed, namely claim 191 (see last two lines).

Those claims are also clear within the meaning of Article 84 EPC.

4.6. The subject-matter of independent claim 23 is based:

- for the compounds of formula (I) on the claim 193 of the application as originally filed with the further restriction to the compounds of formula (I) wherein Y2 is a benzodioxan-2-yl hydrocarbylene group of formula (4) and

- for the compounds of formula (I') on the description, pages 30 to 32; page 20, seventh paragraph; pages 17 to 18, bridging paragraph and page 18, lines 14 ff. The Board sees no objection under Articles 123(2) and 84 EPC for the same reasons as set out at point 4.3 above.

4.7. The subject-matter of dependent claims 24 to 48 is supported by the application as filed.

- claim 24 is supported by originally filed claim 193 and page 18, lines 14 ff.,

- claims 25 to 34 are respectively supported by the application as filed, namely claim 95; claim 153; claim 154; claim 155; claim 156; claim 157; claim 158; claim 159; claim 160; claim 161,

- claims 35 to 41 are supported by the application as filed page 31, first and second paragraph and page 18, lines 14 ff.,

- claim 42 is supported by the application as filed, page 34, line 9,

- claims 43 to 45 are supported by the application as filed, page 64, first paragraph,

- claim 46 is supported by the application as filed, page 32. The restriction of the compounds of formula (I') to those where n is 2 does not amount to a selection among several lists but to an admissible limitation among a single list (n is 1 or 2),

- claim 47 related to compounds of formula (I') according to claim 23 is supported by the description of the application as filed for the same reasons as set out in point 4.6. However, the Board has noticed subsequently that the group (b) had been kept on while it is obvious that this group is no longer in line with the claim 23 and furthermore it was the intention of the Appellant to limit the scope of claim 23 and, as a result, of the therefrom depending claim 47. Such a correction is left to the Appellant and the Examining Division,

- claim 48 is supported by the claims 93 and 94 as originally filed.

Those claims are also clear within the meaning of Article 84 EPC.

5. Novelty - Article 54(2) EPC

5.1. After examination of the disclosures of documents (1), (2) and (4), the Board has reached the conclusion that the subject-matter as defined in the claims of the second auxiliary request is novel. Since, in the decision under appeal or in the course of the examination proceedings, the Examining Division acknowledged the novelty of the now claimed subject-matter with respect to those documents, it is not necessary to give detailed reasons for this finding.

5.2. Document (3) relates to 1,2-benzisothiazol-3-yl-piperazine derivatives having analgesic properties of formula:

FORMULA

wherein R1 is, in particular, a benzodioxan-2-yl-lower alkylene group (see page 2, lines 33 to 51).

5.3. In the Board's judgment, claims 1 to 22 directed to heteroaryl piperidine derivatives are novel in view of the disclosure of document (3). The claims 23 to 48, directed to the use of compounds for the preparation of a medicament for treating psychoses, are also novel since document (3) describes only compounds having analgesic activity.

6. Remittal

6.1. The amendments made overcome the objections pursuant to Articles 84, 123(2), 54(2) EPC which led to refusal of the application 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.

6.2. As mentioned in points 4.4 and 4.7, the Board has noted a redundancy in claim 1 and a discrepancy in claim 47, namely:

- in the proviso of claim 1, the term ", Z is

not -N-" is redundant,

- in dependent claim 47 the group Q1 formula (b) should be deleted to put this claim in compliance with independent claim 23.

Moreover, in dependent claim 2 the word "salt" should be added between the last two words of that claim in order to correct an obvious omission and in claim 23 the second signification "lower" alkyl for Y in formula (I) need to be amended into "C1-C6" for reasons of consistency.

ORDER

For these reasons it is decided that:

1. The decision under appeal is set aside.

2. The matter is remitted to the first instance for further prosecution on the basis of the claims of the second auxiliary request submitted at oral proceedings on 28 June 2000.

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