Jina Pharmaceuticals Inc.

Libertyville, IL, United States

Jina Pharmaceuticals Inc.

Libertyville, IL, United States
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Patent
Jina Pharmaceuticals Inc. | Date: 2017-04-10

The present invention relates to the methods for preparing synthetic guggulphospholipids, their fatty acid analogues and other bioactive molecules. The present invention relates to E-guggulsterone and Z-guggulsterone or mixture of E- and Z-guggulsterones, and E-guggulsterol and Z-guggulsterol or mixture of E- and Z-guggulsterols synthetically modified to guggulphospholipids and analogues and salts thereof, fatty acid analogues of guggulsterols, guggulsulfate and salts thereof, guggulphosphate and salts thereof; and guggulsterols conjugated with drugs for use as prodrugs. Also the present invention provides a novel method for the preparation of E-guggulsterol and Z-guggulsterol or mixture of E- and Z-guggulsterols from a mixture of E- and Z-guggulsterones. The present invention further relates to guggulphospholipids and other bioactive molecules incorporated into complexes such as liposomes, complexes, emulsions, vesicles, micelles, and mixed micelles, which can include other active agents, such as hydrophobic or hydrophilic drugs for use, e.g., in treatment of human and animal diseases.


Ahmad A.,Jina Pharmaceuticals Inc. | Shahabuddin S.,Jina Pharmaceuticals Inc. | Sheikh S.,Jina Pharmaceuticals Inc. | Kale P.,Lambda Therapeutic | And 3 more authors.
Clinical Pharmacology and Therapeutics | Year: 2010

Endoxifen is an active metabolite of tamoxifen, a drug used in the treatment of breast cancer. In order to be clinically effective, tamoxifen must be converted to endoxifen by cytochrome P450 2D6 (CYP2D6). A study involving single escalating oral doses was conducted in humans to evaluate the safety, tolerability, and pharmacokinetics (PK) of endoxifen. This is the first study demonstrating that single oral doses of endoxifen are safe and well tolerated and have sufficient bioavailability to reach systemically effective levels in human subjects. Furthermore, it was found that endoxifen is rapidly absorbed and systemically available and that it displays dose proportionality in peak drug concentrations in plasma (Cmax) and area under the concentration-time curve extrapolated from 0 to ∞(AUC 0-∞) over the dose range 0.5-4.0mg. © 2010 American Society for clinical Pharmacology and Therapeutics.


PubMed | Jina Pharmaceuticals Inc. and Nia Life science
Type: | Journal: Data in brief | Year: 2015

A new synthetic methodology for cationic glycolipids using p-aminophenyl--d-mannopyranoside (PAPM), p-aminophenyl--d-galactopyranoside (PAPG) was developed. PAPM-lipids and PAPG-lipids conjugates were also synthesized for targeting drugs to receptors. A binding inhibition study of synthesized p-(dimethylamino butylamido) phenyl--d-mannopyranoside (1a) with Concanavalin A was performed using invertase enzyme. In addition, transfection of pSV--gal reporter gene with was investigated in A549 cells.


Ali S.M.,Jina Pharmaceuticals Inc. | Ahmad A.,Jina Pharmaceuticals Inc. | Shahabuddin S.,Jina Pharmaceuticals Inc. | Ahmad M.U.,Jina Pharmaceuticals Inc. | And 2 more authors.
Bioorganic and Medicinal Chemistry Letters | Year: 2010

Protein kinase C (PKC) plays a major role in regulation of both pre and postsynaptic neurotransmission. Excessive activation of PKC results in symptoms related to bipolar disorder. Tamoxifen, a widely used breast cancer drug is known to inhibit PKC and demonstrate antimanic properties in human. We describe herein the synthesis of endoxifen, a tamoxifen active metabolite and compared its PKC inhibitory activity with that of tamoxifen. Endoxifen exhibited fourfold higher potency compared to tamoxifen. © 2010 Elsevier Ltd. All rights reserved.


Ahmad A.,Jina Pharmaceuticals Inc. | Ali S.M.,Jina Pharmaceuticals Inc. | Ahmad M.U.,Jina Pharmaceuticals Inc. | Sheikh S.,Jina Pharmaceuticals Inc. | Ahmad I.,Jina Pharmaceuticals Inc.
Breast Cancer Research and Treatment | Year: 2010

Endoxifen is the key active metabolite of Tamoxifen, a widely used breast cancer drug. Orally administered Tamoxifen, is extensively metabolized by cytochrome P450 (CYP) enzymes, namely CYP3A4 and CYP2D6, into active metabolites, especially Endoxifen. Due to genetic polymorphism of CYP2D6, significant numbers of women metabolize Tamoxifen to varying degree and may not receive the optimal benefit from Tamoxifen treatment. We show that oral administration of Endoxifen achieved the optimally effective systemic levels reliably, which may eliminate variability associated with Tamoxifen metabolism that leads to unpredictability in efficacy. Furthermore, use of Endoxifen may avoid a potential serious drug interaction found between Tamoxifen and commonly used selective serotonin reuptake inhibitors, antidepressants. Endoxifen was active in inhibiting the growth of various breast tumor cell lines in NCI 60-Cell Line Screen. Orally administered Endoxifen is rapidly absorbed and systemically available when tested in female rats. The Endoxifen-treated rats showed 787% higher exposure (AUC0-∞) and 1,500% higher concentration (Cmax) levels of Endoxifen when compared with Tamoxifen. Oral Endoxifen administration once a day for 28 consecutive days at dosages 2, 4, and 8 mg/kg proved safe and resulted in progressive inhibition of the growth of the human mammary tumor xenografts in female mice. This is the first ever in vivo report on Endoxifen as a potentially new therapeutic agent for breast cancer. © Springer Science+Business Media, LLC. 2010.


Ahmad M.U.,Jina Pharmaceuticals Inc. | Ali S.M.,Jina Pharmaceuticals Inc. | Ahmad A.,Jina Pharmaceuticals Inc. | Sheikh S.,Jina Pharmaceuticals Inc. | Ahmad I.,Jina Pharmaceuticals Inc.
Chemistry and Physics of Lipids | Year: 2010

Two guggullipid derivatives, Z-guggulsulfate [4,17(20)-pregnadiene-3-one-16β-sulfate] sodium salt and Z-guggullaurate [4,17(20)-pregnadiene-3-one-16β-laurate], have been synthesized and evaluated for liposomal drug delivery system. Its precursor, Z-guggulsterol [4,17(20)-pregnadiene-3-one-16β-ol], is also synthesized in gram scale starting from guggulsterone using the novel combination of known reactions in fewer steps and with higher yield than previously reported synthesis. These new synthetic guggullipid derivatives were also used in the preparation of liposomes. This new class of lipid molecules will be a useful tool in the development of nanosomal or liposomal drug delivery system. © 2010 Elsevier Ireland Ltd. All rights reserved.


Patent
Jina Pharmaceuticals Inc. | Date: 2010-05-21

The present invention provides compositions containing endoxifen, formulations and liposomes of endoxifen, methods of preparation of such agents and formulations, and use of such agents and formulations for the treatment of a subject having or at risk for psychiatric and neurodegenerative diseases, infectious diseases, fertility disorders, osteoporosis, osteoarthritis, and/or cardiovascular diseases. Specifically, the present invention relates to compositions comprising endoxifen for use in the treatment of such disorders or predisposition to such disorders, for use in manufacture of medicaments for treating such disorders, and methods comprising use of such compositions in such treatments.


The present invention relates to a methods of preparing active compounds complexed with lipids using aqueous systems that are free of organic solvents, and methods of using the complexes, e.g., in treating a disease in a subject. In some embodiments, the present invention comprises a composition comprising a complex comprising at least one active compound, e.g., a polyene antibiotic, an immunosuppressant agent such as tacrolimus or a taxane or taxane derivative, and one or more lipids. In some embodiments, the present invention provides a method comprising preparing a composition comprising a lipid complex comprising at least one active compound and at least one lipid and administering the composition to a subject. In certain embodiments the subject is a mammal. In certain preferred embodiments, the subject is human.


Patent
Jina Pharmaceuticals Inc. | Date: 2016-04-27

The present invention provides compositions containing endoxifen, formulations and liposomes of endoxifen, methods of preparation of such agents and formulations, and use of such agents and formulations for the treatment of breast cancer and other breast diseases and diseases susceptible to endoxifen. In particular, the compositions of the present invention include liposomes, complexes, vesicles, emulsions, micelles and mixed micelles of endoxifen in which the compositions further contain any of a variety of neutral or charged lipids and desirably, cholesterol and cholesterol derivatives, sterols, Z- and E-guggulsterones, phospholipids, fatty acids, vitamin D, and vitamin E. The present invention also provides methods of preparing endoxifen. The present invention provides methods for treating and preventing breast cancer and other breast related diseases by administrating novel formulations or compositions comprising a therapeutically effective amount of endoxifen.


Trademark
Jina Pharmaceuticals Inc. | Date: 2010-06-30

Drug delivery agents consisting of compounds that facilitate delivery of a wide range of pharmaceuticals.

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