[유기화학기술]Pfizer, Inc/ Pfizer Pharmaceuticals, LLC/ Wyeth, LLC/ PF Prism CV/ Pfizer Manufacturing Holdings, LLC 대 Mylan, Inc./ Mylan Pharmaceuticals, Inc./ AGILA SPECIALTIES PRIVATE LTD. 간의 유기화학기술 관련 특허 분쟁

발생일자 2015.01.08

사건번호 1:15-cv-00026

법원국가 UNITED STATES OF AMERICA

관할법원명 D.C.Delaware(지방법원)

침해권리 특허

원고명

Pfizer, Inc/ Pfizer Pharmaceuticals, LLC/ Wyeth, LLC/ PF Prism CV/ Pfizer Manufacturing Holdings, LLC ( 미국 / 외국기업 )

피고명 Mylan, Inc./ Mylan Pharmaceuticals, Inc./ AGILA SPECIALTIES PRIVATE LTD. ( 미국 / 외국기업 )

소송유형 침해금지

분쟁내용

[Pfizer, Inc et al v. Mylan, Inc. et al] 사건번호 1:15-cv-00026에 따르면 원고 Pfizer, Inc/ Pfizer Pharmaceuticals, LLC/ Wyeth, LLC/ PF Prism CV/ Pfizer Manufacturing Holdings, LLC는 피고 Mylan, Inc./ Mylan Pharmaceuticals, Inc./ AGILA SPECIALTIES PRIVATE LTD.을 상대로 특허 US7879828|US8372995을 침해하였다는 이유로 미국 델라웨어 지방법원에 소를 제기하였다.

분쟁결과 분쟁중

산업분류 화학∙바이오 > 유기화학기술

계쟁제품 Tigecycline lyophilized product for IV infusion containing 50 mg tigecycline, generic version of TYGACIL

지재권번호/명칭

US7879828 Tigecycline compositions and methods of preparation

US8372995 Crystalline solid forms of tigecycline and methods of preparing same

Tigecycline compositions and methods of preparation

Abstract

The present invention relates to novel tigecycline compositions with improved stability in both solid and solution states and processes for making these compositions. These compositions comprise tigecycline, a suitable carbohydrate, and an acid or buffer.

Claims

What is claimed is:

1. A composition comprising tigecycline, lactose, and an acid selected from hydrochloric acid and gentisic acid, wherein the molar ratio of tigecycline to lactose is between about 1:0.2 and about 1:5 and the pH of the composition in a solution is between about 3.0 and about 7.0.

2. The composition of claim 1 wherein the composition is lyophilized.

3. The composition of claim 1 wherein the composition is in solid form.

4. The composition of claim 1 wherein the pH of the composition in a solution is between about 4.0 and about 5.0.

5. The composition of claim 4 wherein the pH of the composition in a solution is between about 4.2 and about 4.8.

6. The composition of claim 1 wherein the acid is hydrochloric acid.

7. The composition of claim 2 wherein the acid is hydrochloric acid.

8. The composition of claim 3 wherein the acid is hydrochloric acid.

9. The composition of claim 1 wherein the molar ratio of tigecycline to lactose is between about 1:1.6 and about 1:3.3.

10. The composition of claim 1 wherein the pH of the composition in a solution is between about 4.5 and about 6.0.

11. The composition of claim 1 wherein the pH of the composition in a solution is between about 4.5 and about 5.5.

12. A composition comprising tigecycline, lactose, and hydrochloric acid, wherein the molar ratio of tigecycline to lactose is between about 1:0.2 and about 1:5 and the pH of the composition in a solution is between about 3.0 and about 7.0.

13. The composition of claim 12 wherein the molar ratio of tigecycline to lactose is between about 1:1.6 and about 1:3.3.

14. The composition of claim 12 wherein the pH of the composition in a solution is between about 4.0 and about 5.0.

15. The composition of claim 14 wherein the pH of the composition in a solution is between about 4.2 and about 4.8.

16. The composition of claim 12 wherein the pH of the composition in a solution is between about 4.5 and about 6.0.

17. The composition of claim 16 wherein the pH of the composition in a solution is between about 4.5 and about 5.5.

18. The composition of claim 12 wherein the composition is in solid form.

19. The composition of claim 13 wherein the composition is in solid form.

20. The composition of claim 14 wherein the composition is in solid form.

21. The composition of claim 15 wherein the composition is in solid form.

22. The composition of claim 16 wherein the composition is in solid form.

23. The composition of claim 17 wherein the composition is in solid form.

Crystalline solid forms of tigecycline and methods of preparing same

Abstract

Crystalline solid forms of tigecycline, Form I, Form II, Form III, Form IV, and Form V, compositions comprising these crystalline solid forms, and processes for preparing these crystalline solid forms are described herein.

Claims

We claim:

1. A Form I tigecycline having X-ray powder diffraction peaks at about 5.2.degree. 2.theta., about 8.3.degree. 2.theta., about 11.1.degree. 2.theta., and about 24.8.degree. 2.theta. and having a hot stage melting point onset temperature of about 170.degree. C. to about 172.degree. C.

2. A composition consisting essentially of Form I tigecycline having X-ray powder diffraction peaks at about 5.2.degree. 2.theta., about 8.3.degree. 2.theta., about 11.1.degree. 2.theta., and about 24.8.degree. 2.theta. and having a hot stage melting point onset temperature of about 170.degree. C. to about 172.degree. C.

3. A process for preparing Form I tigecycline comprising crystallizing tigecycline out of a solution to form a slurry, and filtering the slurry to isolate Form I tigecycline having X-ray powder diffraction peaks at about 5.2.degree. 2.theta., about 8.3.degree. 2.theta., about 11.1.degree. 2.theta., and about 24.8.degree. 2.theta. and having a hot stage melting point onset temperature of about 170.degree. C. to about 172.degree. C.

4. The process of claim 3 wherein the solution contains methylene chloride.

5. The process of claim 3 further comprising drying the solution prior to the crystallizing step.

6. The process of claim 3 further comprising stirring the slurry prior to the filtering step.

7. The process of claim 3 further comprising combining said Form I tigecycline with at least one pharmaceutically suitable carrier to form a pharmaceutical composition.

8. A pharmaceutical composition made by the process of claim 7.

9. The process of claim 7 further comprising lyophilizing said pharmaceutical composition.

10. A pharmaceutical composition made by the process of claim 9.

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