77 results about "Vitamin D Analog" patented technology

Disclosed are compositions containing a VDRA/Vitamin D analog to treat or prevent kidney disease, including chronic kidney disease. The present invention also relates to methods of treating kidney disease by administering to a patient a pharmaceutical composition containing a therapeutically effective amount of a VDRA/Vitamin D analog. Compositions according to the invention include a VDRA/Vitamin D analog and at least one of the following agents: an ACE inhibitor, an angiotensin (II) receptor blocker (ARB) and aldosterone blocker in therapeutically effective amounts to inhibit renin production or inhibit activation of the renin-angiotensin-aldosterone system. Preferred compositions contain paricalcitol with at least one of these other agents. Such combinations can avoid ACE inhibition escape and aldosterone escape with subsequent increase in angiotensin (II) and aldosterone generation.

A composition is described comprising a vitamin D analog and a retinoid wherein: (a) the vitamin D analog is capable of binding a vitamin D receptor or being converted in vivo into a compound capable of binding a vitamin D receptor; and (b) the retinoid is selected from the group consisting of retinol in a concentration of at least about 1.0% and a retinoid characterized by having a substitution at the 4-position. Further, methods of treating disorders characterized by abnormal cell-proliferation and/or cell-differentiation are also described.

A composition is described comprising a vitamin D analog and a retinoid, wherein: (a) the vitamin D analog is capable of binding a vitamin D receptor or being converted in vivo into a compound capable of binding a vitamin D receptor; and (b) the retinoid is selected from the group consisting of a compound capable of binding a retinoic acid receptor, retinol in a concentration of at least about 0.1% and a compound in a concentration of at least about 0.% capable of being converted in vivo into retinol. Further, methods of treating disorders characterized by abnormal cell-proliferation and/or cell-differentiation are also described.

Disclosed are compositions containing a VDRA/Vitamin D analog to treat or prevent kidney disease, including chronic kidney disease. The present invention also relates to methods of treating kidney disease by administering to a patient a pharmaceutical composition containing a therapeutically effective amount of a VDRA/Vitamin D analog. Compositions according to the invention include a VDRA/Vitamin D analog and at least one of the following agents: an ACE inhibitor, an angiotensin (II) receptor blocker (ARB) and aldosterone blocker in therapeutically effective amounts to inhibit renin production or inhibit activation of the renin-angiotensin-aldosterone system. Preferred compositions contain paricalcitol with at least one of these other agents. Such combinations can avoid ACE inhibition escape and aldosterone escape with subsequent increase in angiotensin (II) and aldosterone generation.

A treatment for obesity and overweight comprises administering a vitamin D analog. The analog effectively inhibits an increase in body fat to animals at risk and decreases the basal fat content of animals. The treatment has a positive effect on the lean body component such that while there is an overall decrease in body weight, there is also a decrease in percent body fat. This decrease can be proportionally greater than the overall decrease in body weight. In addition, the treatment has a positive effect on bone turnover and osteogenesis making the vitamin D analog a beneficial treatment for the symptoms of menopause. Various exemplary embodiments of the treatment use the 2-alkylidene derivatives of vitamin D₃, such as the 2-alkylidene-19-nor derivatives in both the R and S configurations at carbon-20.

Disclosed are pharmaceutical compositions containing Vitamin D receptor activators or Vitamin D analogs to treat, prevent or inhibit vascular disease among other conditions. The pharmaceutical compositions may also include ACE inhibitors or other agents. Also disclosed are methods of reducing PAI-1 expression by administering effective amounts of Vitamin D receptor activators or Vitamin D analogs to a mammal in need thereof. Additionally disclosed are methods of preventing, inhibiting or treating thrombosis in a mammal in need of such prevention, inhibition or treatment comprising administering effective amounts of Vitamin D receptor activators or Vitamin D analogs to the mammal.

The invention discloses a vitamin D analog preparation and a preparation method thereof. The invention aims to solve the problems that a conventional preparation method of vitamin D analog has difficulty in meeting the uniformity requirement and during the granulation process, drugs are converted and degraded easily. For the first time, a double screw extrusion technology is used to prepare a solid preparation of vitamin D analog. Various vitamin D analogs are taken as model drugs, on the basis that a preparation technology of solid preparations is deeply researched, alfacalcidol, eldecalcitol, or calcitriol is chosen to prepare the solid preparation by using a double screw extruding machine; the uniformity meets the pharmacopeia requirements; the drug stability is obviously enhanced, andthe drug quality is greatly improved.

Provided is a method of general applicability of epimerizing a vitamin-D analog having an asymmetric allylic carbon atom at the C-24 position. The method is of particular utility in making calcipotriene.

Provided is a method of selectively enzymatically esterifying or selectively enzymatically solvolyzing epimers of analogs of vitamin D having a stereogenic center at C-24 that has a free or esterified OH group. The metod can be used, for example, for separating mixed epimers of the vitamin D analog.

The invention relates to a spray containing Vitamin D analog, wherein the medicinal solution comprises, (1) one or more vitamin D analog, (2) fatty medicinal solution carrier, the vitamin D analog is represented by formula (I). The spray has good pharmaceutical property and high stability.

Disclosed are pharmaceutical compositions containing Vitamin D receptor activators or Vitamin D analogs to treat, prevent or inhibit vascular disease. The pharmaceutical compositions may also include ACE inhibitors or other agents. Also disclosed are methods of reducing PAI-1 expression by administering effective amounts of Vitamin D receptor activators or Vitamin D analogs to a mammal in need thereof. Additionally disclosed are methods of preventing, inhibiting or treating thrombosis in a mammal in need of such prevention, inhibition or treatment comprising administering effective amounts of Vitamin D receptor activators or Vitamin D analogs to the mammal.

The present invention relates to a process for purifying Doxercalciferol, a synthetic vitamin D analog, also known as 1α-hydroxy vitamin D₂, to the purity greater than 99.5% by crystallization from a mixed solvent of methanol and acetonitrile. Each of the individual impurities can be controlled no more than 0.1% which meets the individual unknown impurities specification requirement of International Conference on Harmonisation (ICH) guideline. The crystallization yield is more than 75% which is suitable for employed as a commercial process.

A composition that includes a corticosteroid (e.g., betamethasone dipropionate), a vitamin D analog (e.g., calcipotriene) and an acyl ester of 1,2,3-trihydroxypropane or an ether thereof; and a method of treating a dermatologic condition (e.g., psoriasis vulgaris) in a mammal (e.g., human); are provided. The method includes topically administering to a mammal in need of such treatment an effective amount of the composition, to the affected topical area, for a period of time effective to treat the dermatologic condition.

Compounds of formula I, II or III are provided where X₁, X₂ and X₃ are independently selected from H and hydroxy protecting groups and R₁ and R₂ are independently selected from H or straight or branched chain alkyl groups having from 1 to 8 carbon atoms, straight or branched chain alkenyl groups having from 2 to 8 carbon atoms, straight or branched chain hydroxy-substituted alkyl groups having from 1 to 8 carbon atoms, or straight and branched chain hydroxy-substituted alkenyl groups having from 2 to 8 carbon atoms; and R₃ is independently selected from straight or branched chain alkyl groups having from 1 to 8 carbon atoms, straight or branched chain alkenyl groups having from 2 to 8 carbon atoms, straight or branched chain hydroxy-substituted alkyl groups having from 1 to 8 carbon atoms, or straight and branched chain hydroxy-substituted alkenyl groups having from 2 to 8 carbon atoms. Such compounds are used in preparing pharmaceutical compositions and are useful in treating a variety of biological conditions.

This invention discloses 2-methylene-vitamin D analogs, and specifically (20S)-1α,25 -dihydroxy-2-methylene-vitamin D₃ as well as (5E)-(20S)-1α,25-dihydroxy-2 -methylene-vitamin D₃ and (20R)-1α,25-dihydroxy-2-methylene-vitamin D₃, as well as pharmaceutical uses therefor. These compounds exhibit relatively high binding activity and pronounced activity in arresting the proliferation of undifferentiated cells and inducing their differentiation to the monocyte thus evidencing use as an anti-cancer agent especially for the treatment or prevention of osteosarcoma, leukemia, colon cancer, breast cancer, skin cancer or prostate cancer. These compounds also have relatively high calcemic activities evidencing use in the treatment of bone diseases.