Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Nitrogen containing other than solely as a nitrogen in an...
Reexamination Certificate
2000-09-15
2003-05-06
Weddington, Kevin E. (Department: 1614)
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Nitrogen containing other than solely as a nitrogen in an...
C514S023000, C514S057000, C514S866000
Reexamination Certificate
active
06559188
ABSTRACT:
The invention relates to a combination, such as a combined preparation or pharmaceutical composition, respectively, which comprises nateglinide or repaglinide and at least one other antidiabetic compound selected from the group consisting of thiazolidinedione derivatives (glitazones), sulfonyl urea derivatives and metformin for simultaneous, separate or sequential use in the prevention, delay of progression or treatment of diseases, especially metabolic disorders and in particular type 2 diabetes and diseases and conditions associated with diabetes; the use of such combination for the preparation of a medicament for the prevention, delay of progression or treatment of metabolic disorders; the use of such combination for the cosmetic treatment of a mammal in order to effect a cosmetically beneficial loss of body weight; a method of prevention, delay of progression or treatment of diseases in warm-blooded animals; a method of improving the bodily appearance of a warm-blooded animal; to a pharmaceutical composition which comprises nateglinide as the sole active agent in the composition and a pharmaceutically acceptable carrier and to a process of making such pharmaceutical composition.
The generally accepted aims in the treatment of diabetes are to provide relief from symptoms, improvement of the quality of life and prevention of both acute (hyperosmolar coma and ketoacidosis) and chronic complications (e.g. diabetic neuropathy, diabetic nephropathy and premature atherosclerosis). Type 2 diabetes is characterized by both increased peripheral insulin resistance and abnormal insulin secretion. At least two abnormalities of insulin secretion are recognized: in the first phase insulin is both delayed and inadequate in the face of elevated circulating glucose levels and in the second phase insulin secretion is lost. Several metabolic, hormonal, and pharmacological entities are known to stimulate insulin secretion including glucose, amino-acids and gastrointestinal peptides. The Diabetes Control and Complications Trial (DCCT) performed in Type I IDDM subjects has established that lowering of blood glucose is associated with decreases in the onset and progression of diabetic microvascular complications (Diabetes Control and Complications Trial Research Group; N. Engl. J. Med. 1993, 329, 977-986). Therefore, one therapeutic focus is on optimizing and potentially normalizing glycemic control in subjects with type 2 diabetes. Presently available oral agents fail to meet this therapeutic challenge in some patient subgroups, result sometimes in side-effects or are fraught with other problems.
The present invention relates to a combination, such as a combined preparation or pharmaceutical composition, respectively, which comprises nateglinide of formula (I)
or repaglinide and at least one other antidiabetic compound selected from the group consisting of thiazolidinedione derivatives (glitazones), sulfonyl urea derivatives and metformin, in which the active ingredients are present in each case in free form or in the form of a pharmaceutically acceptable salt and optionally at least one pharmaceutically acceptable carrier; for simultaneous, separate or sequential use, particularly in the prevention, delay of progression or treatment of diseases, especially metabolic disorders and in particular type 2 diabetes mellitus and diseases and conditions associated with diabetes mellitus. Such a combination is preferably a combined preparation or a pharmaceutical composition.
By the term “a combined preparation or pharmaceutical composition, respectively, which comprises nateglinide or repaglinide and at least one other antidiabetic compound selected from the group consisting of glitazones, sulfonyl urea derivatives and metformin, in which the active ingredients are present in each case in free form or in the form of a pharmaceutically acceptable salt and optionally at least one pharmaceutically acceptable carrier, for simultaneous, separate or sequential use”, there is meant especially a “kit of parts” in the sense that the components nateglinide or repaglinide and at least one other antidiabetic compound selected from the group consisting of glitazones, sulfonyl urea derivatives and metformin can be dosed independently or by use of different fixed combinations with distinguished amounts of the components, i.e. simultaneously or at different time points. The parts of the kit of parts can then e.g. be administered simultaneously or chronologically staggered, that is at different time points and with equal or different time intervals for any part of the kit of parts. Preferably, the time intervals are chosen such that the effect on the treated disease or condition in the combined use of the parts is larger than the effect which would be obtained by use of only any one of the components. Preferably, there is at least one beneficial effect, e.g. a mutual enhancing of the effect of nateglinide or repaglinide and at least one other antidiabetic compound selected from the group consisting of glitazones, sulfonyl ureas and metformin, in particular a synergism, e.g. a more than additive effect, additional advantageous effects, less side effects, a combined therapeutical effect in a non-effective dosage of one or each of the components nateglinide or repaglinide and at least one other antidiabetic compound selected from the group consisting of glitazones, sulfonyl urea derivatives and metformin, and especially a strong synergism between nateglinide or repaglinide and at least one other antidiabetic compound selected from the group consisting of glitazones, sulfonyl urea derivatives and metformin.
In particular, the present invention relates to a method of treating metabolic disorders, more especially diabetes and in particular type 2 diabetes mellitus, or a disease or condition associated with diabetes comprising administering to a warm-blooded animal in need thereof a jointly therapeutically effective amount of a combined preparation comprising nateglinide and an antidiabetic thiazolidinedione derivative, wherein each of the active ingredients are present in free form or in the form of a pharmaceutically acceptable salt.
By the term “a combined preparation or pharmaceutical composition, respectively, which comprises nateglinide and an antidiabetic thiazolidinedione derivative, wherein each of the active ingredients are present in free form or in the form of a pharmaceutically acceptable salt and optionally at least one pharmaceutically acceptable carrier, as a combined preparation for simultaneous, separate or sequential use”, there is meant especially a “kit of parts” in the sense that the components nateglinide and the antidiabetic thiazolidinedione derivative can be dosed independently or by use of different fixed combinations with distinguished amounts of the components at different time points. Preferably, there is at least one beneficial effect, e.g. a mutual enhancing of the effect of nateglinide and the antidiabetic thiazolidinedione derivative, in particular a synergism, e.g. a more than additive effect, additional advantageous effects, less side effects, a combined therapeutical effect in a non-effective dosage of one or each of the components nateglinide and the antidiabetic thiazolidinedione derivative, especially a strong synergism between nateglinide and the anti-diabetic thiazolidinedione derivative.
“Diseases and conditions associated with diabetes mellitus” as defined in this application comprise, but are not restricted to hyperglycemia, hyperinsulinaemia, hyperlipidaemia, insulin resistance, impaired glucose metabolism, obesity, diabetic retinopathy, macular degeneration, cataracts, diabetic nephropathy, glomerulosclerosis, diabetic neuropathy, erectile dysfunction, premenstrual syndrome, vascular restenosis and ulcerative colitis. Furthermore, “diseases and conditions associated with diabetes mellitus” comprise, but are not restricted to: coronary heart disease, hypertension, angina pectoris, myocardial infarction, stroke, skin and connective tissue disorders, foot ulcerations, metabolic ac
Allison Malcolm
Ball Michele Ann
Gatlin Marjorie Regan
Guitard Christiane
Karnachi Anees Abdulquadar
Novartis AG
Thallemer John D.
Weddington Kevin E.
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