78 results about "Vitamin D Analog" patented technology

Methods for treating and preventing obesity, inhibiting adipocyte differentiation, inhibiting increased SCD-1 gene transcription, and / or reducing body fat in a subject include administering at least one analog of 1α,25-dihydroxyvitamin D3 or 1α,25-dihydroxyvitamin D2 or a pharmaceutical composition that includes such an analog to a subject in need thereof. The analog may be a 19-nor vitamin D analog such as a compound of formula IA, a compound of formula IB, or a mixture thereof where the variables R1, R2, and R3 have the values described herein.

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.

Compounds of formula IA or IB are provided where X1, X2 and X3 are independently selected from H or hydroxy protecting groups and R1 is 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; 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.

Compounds of formula IA or IB are provided where X1, X2 and X3 are independently selected from H or hydroxy protecting groups and R1 is 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; 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.

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.

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.

Compounds of formula IA or IB are provided where X1, X2 and X3 are independently selected from H or hydroxy protecting groups and R1 is 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; 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 application relates to methods of treating, preventing, and ameliorating fibrosis, such as fibrosis of the liver. In particular, the application relates to methods of using a vitamin D receptor agonist (such as vitamin D, vitamin D analogs, vitamin D precursors, and vitamin D receptor agonists precursors) for the treatment of liver fibrosis. Also disclosed are methods for screening for agents that treat, prevent, and ameliorate fibrosis.

Embodiments of the present invention are directed to methods and kits for determining the presence or absence, and the amount if present, of vitamin D analogs in samples. One embodiment of the present method for detecting the presence or absence of vitamin D analogs in a sample comprises the steps of adding an effective amount of a multiple charge cationic agent to the sample to form a cationic treated sample. The effective amount of a multiple charge cationic agent enhances the signal from vitamin D analogs upon analysis by mass spectroscopy.

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.

Oral and topical pharmaceutical compositions, kits and methods of treatment thereof for treating various skin disorder including acne, psoriasis, ichthyosis, photoaging, photodamaged skin, and, skin cancer. Exemplary vitamin D analogs as active pharmaceutical ingredients include 2-methylene-19-nor-20(S)-1α-hydroxy-bishomopregnacalciferol, 19-nor-26,27-dimethylene-20(S)-2-methylene-1α,25-dihydroxyvitamin D3, 2-methylene-1α,25-dihydroxy-(17E)-17(20)-dehydro-19-nor-vitamin D3, 2-methylene-19-nor-(24R)-1α,25-dihydroxyvitamin D2, 2-methylene-(20R,25S)-19,26-dinor-1α,25-dihydroxyvitamin D3, 2-methylene-19-nor-1α-hydroxy-pregnacalciferol, 1α-hydroxy-2-methylene-19-nor-homopregnacalciferol, (20R)-1α-hydroxy-2-methylene-19-nor-bishomopregnacalciferol, 2-methylene-19-nor-(20S)-1α-hydroxy-trishomopregnacalciferol, 2-methylene-23,23-difluoro-1α-hydroxy-19-nor-bishomopregnacalciferol, 2-methylene-(20S)-23,23-difluoro-1α-hydroxy-19-nor-bishomopregnancalciferol, (2-(3′hydroxypropyl-1′,2′-idene)-19,23,24-trinor-(20S)-1α-hydroxyvitamin D3, 2-methylene-18,19-dinor-(20S)-1α,25-dihydroxyvitamin D3, a stereoisomer thereof, a prodrug thereof in oral compositions, a salt thereof, and / or a solute thereof. Compounds that activate retinoic acid receptors, such as retinoyls and retinoyl esters, include 13-cis-retinoic acid, all-trans-retinoic acid, (2E,4E,6Z,8E)-3,7-dimethyl-9-(2,6,6-trimethyl-1-cyclohexeneyl)nona-2,4,6,8-tetraenoic acid, 9-(4-methoxy-2,3,6-trimethyl-phenyl)-3,7-dimethyl-nona-2,4,6,8-tetraenoic acid, 6-[3-(1-adamantyl)-4-methoxyphenyl]-2-napthoic acid, 4-[1-(3,5,5,8,8-pentamethyl-tetralin-2-yl)ethenyl]benzoic acid, retinobenzoic acid, ethyl 6-[2-(4,4-dimethylthiochroman-6-yl)ethynyl]pyridine-3-carboxylate, retinoyl t-butyrate, retinoyl pinacol, retinoyl cholesterol, an isomer thereof, a prodrug thereof for oral compositions, an ester thereof, a salt thereof, and / or, a solute thereof. Combinations of such active ingredients demonstrate synergistic efficacy.

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 method for prevention and / or treatment of an autoimmune disease, comprising administering a composition, said composition comprising at least one beta cell autoantigen, to a subject The subject may have a serum vitamin-D level above 50 nanomole / liter or the composition may be administered by intralymphatic injection or injection directly into a lymph node, or over a period of weeks, months, or years. The invention also relates to a composition comprising a plurality of particles, each having immobilised on its surface at least one first and at least one second antigen, wherein the first antigen is a beta cell autoantigen, and the second antigen is either a tolerogen or a beta cell autoantigen, and to composition comprising i) at least one beta cell autoantigen, and at least one of iia) an IL-10 inducing compound selected from the group consisting of vitamin-D, vitamin-D analogs, tyrosine kinase inhibitors, gamma-amino butyric acid, and gamma-amino butyric acid analogs; and iib) a compound that reduces the dendritic cells' ability to activate naïve CD4+ Tcells, such as a cyclooxygenase inhibitor, a CTLA-4 compound or a TNF alpha inhibitor. The invention also relates to pharmaceutical kits and to medical use of beta cell autoantigens.

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.

19-nor-vitamin D analogs having an additional dihydrofuran ring connecting the 3β-oxygen and carbon-2 of the A-ring of the analog, and pharmaceutical uses therefore, are described. These compounds exhibit selective in vitro and in vivo activities, making them therapeutic agents for the treatment or prophylaxis of autoimmune diseases, some types of cancers, metabolic bone diseases, osteomalacia, osteopenia, secondary hyperparathyroidism, psoriasis, or other skin diseases.

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.

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.