Board of Patent Appeals and Interferences
Patent and Trademark Office (P.T.O.)
*1 EX PARTE WERNER SKUBALLA, HELMUT DAHL, BERND RADUCHEL, HELMUT VORBRUGGEN
AND OLAF LOGE
Appeal No. 86-1591
June 2, 1989
Heard: January 12, 1989
Application for Patent filed June 25, 1984, Serial No. 623,869. Novel Prostacyclin Derivatives, Process For The Preparation Thereof, And Use Thereof As Medicinal Agents.
Anthony J. Zelano et al. for Appellants
Primary Examiner--Ethel G. Love
Before Seidleck, Sofocleous and Metz
This appeal involves claims 18, 19, 20 and 21. Claims 1 through 17, the only other claims in the case, have been allowed by the examiner.
A copy of the appealed claims, together with the only independent claim in the case, namely claim 1, is attached to this opinion as an appendix.
The following reference has been relied upon by the examiner only for the purpose of showing the state of the art.
World Patent 83/04021 Nov. 24, 198??
Claims 18 through 21 stand rejected under 35 USC 112, first and second paragraphs, since the invention as claimed therein is not described in such full, clear, concise and exact terms as to enable any person skilled in the art to make and use the same, and/or for failing to particularly point out and distinctly claim the subject matter which appellants regard as their invention.
We have carefully considered all of the arguments advanced by appellants and the examiner and find that we agree with appellants. Accordingly, we will not sustain the aforementioned rejection.
The present invention is directed to novel prostacyclin derivatives (allowed claims 1 through 17), to pharamaceutical compositions comprising a pharmacologically acceptable carrier and an effective amount of one of said prostacyclin derivatives (claims 18 and 19), to a method of inhibiting gastric acid secretion in a patient by administering an effective amount of said prostacyclin derivative to the patient (claim 20) and to a method for achieving certain biological responses in a patient by administering an effective amount of the prostacyclin derivative (claim 21).
The examiner initially contends that composition claims 18 and 19 are not in compliance with the requirements of 35 USC 112, since there is no use defined for the compositions being claimed. We are unable to subscribe to the examiner's contention. The claim language does, in fact, point out and identify the compositions which appellants regard as their invention, namely, pharmaceutical compositions comprising a compound of allowed claim 1 plus a pharmacologically acceptable carrier. Moreover, the recitation of an intended use is not required in the present composition claims, particularly when they are read in light of the instant specification. We agree with appellants that the instant specification is fully adequate in teaching a skilled worker how to utilize the compounds of the allowed claims as well as compositions containing these compounds.
*2 The examiner is also of the opinion that claims 18, 20 and 21 are indefinite in the recitation "an effective amount" since they fail to state the function which is to be achieved by the amount of active ingredient present. We are unable to subscribe to the examiner's contention, particularly as to the method of use claims, namely claims 20 and 21 which set forth the function or functions to be achieved by administering the claimed 5-cyanoprostacyclin compounds to the patient. As to claim 18, we note that it is directed to pharmaceutical compositions and not simply to compositions. The included compositions therefore are to be utilized for pharmaceutical purposes. As such, this claim requires that the amount of the active agent be effective for a pharmacological utility. Moreover, the recitation "an effective amount," is definite, particularly when read in light of the instant disclosure. In our opinion, pages 9 through 12 of the instant specification provide fully adequate guidelines as to intended utilities and how the uses can be effected. For example, we note that the specification teaches that the novel prostacyclins of the present invention, although more selective with regard to potency, exhibit the properties typical for the prostacyclins of the prior art and may be utilized to achieve similar biological responses. The conventional dosages, etc., for prostacyclins are set forth at pages 10 and 11. While some experimentation may be required to determine optimum dosages for these more potent prostacyclins in order to achieve a particular biological response, such experimentation is not considered to be undue.
We also agree with appellants that claim 21 is not rendered indefinite because it recites diverse utilities. We are satisfied that the skilled worker in this art could readily optimize effective dosages and administration regimens for each of the recited utilities. As is well known, the specific dosage for a given patient under specific conditions and for a specific disease will routinely vary, but determination of the optimum amount in each case can readily be accomplished by simple routine procedures. Thus, both the dosage and the mode of administration for all recited uses of claim 21 are sufficiently supported by the instant disclosure.
The decision of the examiner is reversed.
BOARD OF PATENT APPEALS AND INTERFERENCES
James A. Seidleck
Andrew H. Metz
1. A 5-cyanoprostacyclin of the formula
TABULAR OR GRAPHIC MATERIAL SET FORTH AT THIS POINT IS NOT DISPLAYABLE
A is a -CH 2-CH 2-, trans-C????CH-, or -C??C-; W is hydroxymethylene, RO-methylene, or
CH 3 CH 3
-C- or -C- wherein thee OH- or OR-group can be in the
A- or B-position;
R is tetrahydropyranyl, tetrahydrofuranyl, a??ethoxyethyl, trimethylsilyl, dimethyl-tert-butylsilyl, tribenzylsilyl or an acyl group of a C 1-15-hydrocarbon carboxylic or sulfonic acid;
*3 D and E together are a direct bond, or
D is (CH@2)n, a straight-chain-C1-5-alkylene group or a branched-or straight-chain, -alkylene, -alkenylene or group of 2-5 carbon atoms, or one of these groups substituted by fluorine and
n is 1, 2, or 3;
R 2 is (a) C @1-10 alkyl or alkenyl; (b) C1-10 alkyl or alkenyl, each substituted by C6-10 aryl or by C@6-10 aryl substituted by 1-3 halogen atoms, a phenyl group, 1-3 C1-4 alkyl groups or a chloromethyl, fluoromethyl, trifluoromethyl, carboxy, hydroxy or C1-4 alkoxy group; (c) C3-10 cycloalkyl, (d) C3-10 cycloalkyl substituted by C1-4 alkyl, (e) C6-10 aryl, (f) C6-10 aryl substituted by 1-3 halogen atoms, a phenyl group, 1-3 C1-4 alkyl groups or a chloromethyl, fluoromethyl, trifluoromethyl, carboxy, hydroxy or C1-4 alkoxy group; or (h) an aromatic heterocycle of 5 or 6 ring atoms one of which is O, N or S, the remainder being ??
R 1 is OH or OR; and
TABULAR OR GRAPHIC MATERIAL SET FORTH AT THIS POINT IS NOT DISPLAYABLE
wherein R 6, R 7, R 8, R 9, R 10, and R 11 can be identical or different and each is hydrogen, C1-5-alkyl, C6-10 aryl, or C6-10 aryl substituted by 1-3333 halogen atoms, a phenyl group, 1-3 C1-4 alkyl groups or a chloromethyl, fluoromethyl, trifluoromethyl, carboxy, hydroxy or C1-4 alkoxy group.
19. A composition of claim 18, wherein the amount of said compound is 0.01- 100 mg.
20. A method of inhibiting gastric acid secretion or for cytoprotection in a patient comprising administering an effective amount of a compound of claim 1 to the patient.
21. A method for achieving an effect in a patient comprising administering an effective amount of a compound of claim 1 to the patient wherein the effect is lowering of peripheral arterial or coronary vascular resistance, inhibition of thrombocyte aggregation or dissolution of platelet thrombi, myocardial cytoprotection and thus lowering of systemic blood pressure without simultaneously lowering stroke volume and coronary blood flow; treatment for stroke, prophylaxis or therapy of coronary heart disease, coronary thromboses, cardiac infarction, peripheral arterial diseases, arteriosclerosis or thrombosis, prophylaxis and therapy of ischemic attacks of the CNS system, therapy for shock, inhibition of bronchoconstriction, inhibition of gastric acid secretion, cytoprotection for gastric or intestinal mucosa, cytoprotection in the liver or pancreas, antiallergic treatment, lowering of pulmonary vascular resistance or pulmonary blood pressure, promotion of kidney blood flow, utilization in place of heparin or as an adjuvant in dialysis of hemofiltration, preservation of blood plasma stores, inhibition of labor, treatment of gestational toxicosis, enhancement of cerebral blood flow, or treatment for antiproliferative or antidiarrheogenic purposes