You’re using a public version of DrugPatentWatch with 5 free searches available | Register to unlock more free searches. CREATE FREE ACCOUNT

Last Updated: March 28, 2024

Claims for Patent: 8,101,629


✉ Email this page to a colleague

« Back to Dashboard


Summary for Patent: 8,101,629
Title:Salt of 4-[[4-[[4-(2-cyanoethenyl)-2,6-dimethylphenyl]amino]-2-pyrimidinyl- ]amino]benzonitrile
Abstract: The present invention relates to a pharmaceutical composition comprising as active ingredient the hydrochloric acid salt of 4-[[4-[[4-(2-cyanoethenyl)-2,6-dimethyl-phenyl]amino]-2-pyrimidinyl]amino- ]benzonitrile and to processes for their preparation.
Inventor(s): Guillemont; Jerome Emile Georges (Ande, FR), Stevens; Paul Theodoor Agnes (Turnhout, BE), Copmans; Alex Herman (Lille, BE), Peeters; Jozef (Beerse, BE), Stappers; Alfred Elisabeth (Oud-Turnhout, BE), Vandecruys; Roger Petrus Gerebern (Westerlo, BE), Stoffels; Paul (Hoogstraten, BE)
Assignee: Janssen Pharmaceutica N.V. (Beerse, BE)
Application Number:12/845,463
Patent Litigation and PTAB cases: See patent lawsuits and PTAB cases for patent 8,101,629
Patent Claims: 1. A tablet comprising 25 mg base equivalent of a compound of formula (I-a) ##STR00004## in a pharmaceutically acceptable carrier comprising a wetting agent.

2. A tablet according to claim 1 wherein the compound of formula (I-a) is polymorphic Form A characterized by X-ray powder diffraction peaks at two-theta positions 9.7.degree..+-.0.2.degree., 13.5.degree..+-.0.2.degree. and 15.0.degree..+-.0.2.degree..

3. A tablet according to claim 2 wherein the polymorphic Form A is further characterized by X-ray powder diffraction peaks at two-theta positions 9.1.degree..+-.0.2.degree., 11.0.degree..+-.0.2.degree., 14.6.degree..+-.0.2.degree., 22.0.degree..+-.0.2.degree., 25.0.degree..+-.0.2.degree., 25.3.degree..+-.0.2.degree. and 26.7.degree..+-.0.2.degree..

4. A tablet according to claim 2 wherein the polymorphic Form A is characterized by an FTIR spectrum with absorption bands at about 2217, 1652, 1497, 1435, 1338, 1199 and 550 cm.sup.-1.

5. A tablet according to claim 4 wherein polymorphic Form A is further characterized by an FTIR spectrum with absorption bands at 1631, 1596, 1537, 1504, 1249, 1214, 1179, 1152 and 1070 cm.sup.-1.

6. A tablet according to claim 1 wherein the wetting agent is polysorbate 20.

7. A tablet according to claim 1 which is film-coated.

8. A tablet according to claim 1 wherein the tablet comprises a tablet core having the following composition: TABLE-US-00007 Compound of formula (I-a) 27.5 mg Lactose monohydrate 242.0 mg Hypromellose 2910 15 mPa s 5.6 mg Polysorbate 20 1.4 mg Microcrystalline cellulose 52.5 mg Croscarmellose sodium 17.5 mg Colloidal silicon dioxide 1.05 mg Magnesium stearate 2.45 mg

9. A tablet according to claim 1 wherein the tablet comprises a tablet core having the following composition: TABLE-US-00008 Compound of formula (I-a) 27.5 mg Lactose monohydrate 55.145 mg Polyvinylpyrrolidone 3.25 mg Polysorbate 20 0.35 mg Silicified microcrystalline cellulose 16.605 mg Croscarmellose sodium 6.05 mg Magnesium stearate 1.10 mg

10. A tablet comprising 50 mg base equivalent of a compound of formula (I-a) ##STR00005## in a pharmaceutically acceptable carrier comprising a wetting agent.

11. A tablet according to claim 10 wherein the tablet comprises a tablet core having the following composition: Compound of formula (I-a) 55 mg Lactose monohydrate 214.5 mg Hypromellose 2910 15mPas 5.6 mg Polysorbate 20 1.4 mg Microcrystalline cellulose 52.5 mg Croscarmellose sodium 17.5 mg Colloidal silicon dioxide 1.05 mg Magnesium stearate 2.45 mg.

12. A tablet comprising 75 mg base equivalent of a compound of formula (I-a) ##STR00006## in a pharmaceutically acceptable carrier comprising a wetting agent.

13. A tablet according to claim 12 wherein the tablet comprises a tablet core having the following composition: TABLE-US-00009 Compound of formula (I-a) 82.5 mg Lactose monohydrate 165.435 mg Polyvinylpyrrolidone 9.75 mg Polysorbate 20 1.05 mg Silicified microcrystalline cellulose 49.815 mg Croscarmellose sodium 18.15 mg Magnesium stearate 3.30 mg

14. A tablet comprising 100 mg base equivalent of a compound of formula (I-a) ##STR00007## in a pharmaceutically acceptable carrier comprising a wetting agent.

15. A tablet according to claim 14 wherein the tablet comprises a tablet core having the following composition: TABLE-US-00010 Compound of formula (I-a) 110 mg Lactose monohydrate 159.5 mg Hypromellose 2910 15 mPa s 5.6 mg Polysorbate 20 1.4 mg Microcrystalline cellulose 52.5 mg Croscarmellose sodium 17.5 mg Colloidal silicon dioxide 1.05 mg Magnesium stearate 2.45 mg

16. A tablet comprising 150 mg base equivalent of a compound of formula (I-a) ##STR00008## in a pharmaceutically acceptable carrier comprising a wetting agent.

17. A tablet according to claim 16 wherein the tablet comprises a tablet core having the following composition: TABLE-US-00011 Compound of formula (I-a) 165 mg Lactose monohydrate 330.87 mg Polyvinylpyrrolidone 19.5 mg Polysorbate 20 2.1 mg Silicified microcrystalline cellulose 99.63 mg Croscarmellose sodium 36.30 mg Magnesium stearate 6.6 mg

18. A tablet according to claim 1 wherein the compound of formula (I-a) has a particle size of less than 50 .mu.m.

19. A tablet according to claim 1 wherein the compound of formula (I-a) has a particle size of less than 25 .mu.m.

20. A particle of compound of formula (I-a) as defined in claim 1, said particle having a particle size of less than 50 .mu.m.

21. A particle according to claim 20 wherein the particle has a particle size of less than 25 .mu.m.

Make Better Decisions: Try a trial or see plans & pricing

Drugs may be covered by multiple patents or regulatory protections. All trademarks and applicant names are the property of their respective owners or licensors. Although great care is taken in the proper and correct provision of this service, thinkBiotech LLC does not accept any responsibility for possible consequences of errors or omissions in the provided data. The data presented herein is for information purposes only. There is no warranty that the data contained herein is error free. thinkBiotech performs no independent verification of facts as provided by public sources nor are attempts made to provide legal or investing advice. Any reliance on data provided herein is done solely at the discretion of the user. Users of this service are advised to seek professional advice and independent confirmation before considering acting on any of the provided information. thinkBiotech LLC reserves the right to amend, extend or withdraw any part or all of the offered service without notice.