Sphaera Pharma Pte. Ltd.

Singapore, Singapore

Sphaera Pharma Pte. Ltd.

Singapore, Singapore

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Dugar S.,Sphaera Pharma Pte. Ltd. | Dhandia A.,Sphaera Pharma Pvt. Ltd.
ACS Symposium Series | Year: 2016

Entrepreneurship is a mix of attitude, talent and perseverance. Successful new ventures are planned, created, and managed. Every venture demands three types of resources time, people and capital. Conventional RandD model with the big pharma has relied on a blockbuster strategy - the need for a major breakthrough in drug discovery and development capable of delivering billion dollar revenues. The new age RandD model needs to be scalable with most of the costs being variable and only a small fixed cost and capacity structure. A successful entrepreneur on the international front needs creative out-of-the-box thinking, attention to compliance, with the understanding that the concepts of innovation and entrepreneurship need to be disruptive.


Dugar S.,Sphaera Pharma Pte. Ltd. | Sharma A.,Sphaera Pharma Pvt. Ltd. | Kuila B.,Sphaera Pharma Pvt. Ltd. | Mahajan D.,Sphaera Pharma Pvt. Ltd. | And 2 more authors.
Synthesis (Germany) | Year: 2014

A simple and efficient method has been developed for the synthesis of substituted morpholines by a sequence of coupling, cyclization, and reduction reactions of easily available amino alcohols and α-halo acid chlorides. Various mono-, di-, and trisubstituted morpholines, spiro morpholines, and ring-fused morpholines, as well as morpholine homologues, were synthesized in good to excellent yields by a single methodology under similar reaction conditions. The method was also used in a multigram synthesis of (3S)-3-methylmorpholine.


Dugar S.,Sphaera Pharma Pte. Ltd. | Hollinger F.P.,Sphaera Pharma Pte. Ltd. | Mahajan D.,Sphaera Pharma Pvt. Ltd. | Sen S.,Sphaera Pharma Pvt. Ltd. | And 9 more authors.
ACS Medicinal Chemistry Letters | Year: 2015

A new class of potent PI3Kα inhibitors is identified based on aryl substituted morpholino-triazine scaffold. The identified compounds showed not only a high level of enzymatic and cellular potency in nanomolar range but also high oral bioavailability. The three lead molecules (based on their in vitro potency) when evaluated further for in vitro metabolic stability as well as pharmacokinetic profile led to the identification of 26, as a candidate for further development. The IC50 and EC50 value of 26 is 60 and 500 nM, respectively, for PI3Kα enzyme inhibitory activity and ovarian cancer (A2780) cell line. The identified lead also showed a high level of microsomal stability and minimal inhibition activity for CYP3A4, CYP2C19, and CYP2D6 at 10 μM concentrations. The lead compound 26, demonstrated excellent oral bioavailability with an AUC of 5.2 μM at a dose of 3 mpk in mice and found to be well tolerated in mice when dosed at 30 mpk BID for 5 days. © 2015 American Chemical Society.


Dugar S.,Sphaera Pharma Pte. Ltd | Hollinger F.P.,Sphaera Pharma Pte. Ltd | Kuila B.,Sphaera Pharma Pvt. Ltd | Arora R.,Sphaera Pharma Pvt. Ltd | And 2 more authors.
Bioorganic and Medicinal Chemistry Letters | Year: 2015

Over activation of the PI3K/Akt/mTOR pathway is found in most cancer tumor types. Controlled regulation of this pathway using PI3K inhibitors can provide therapeutic significance in cancer treatment. Herein, we report the synthesis and evaluation of pyrrolotriazine based novel small molecules as pan-PI3K inhibitors. The SAR studies based on in vitro potency along with microsomal metabolic stability screening, identified 18 as a preclinical lead found to be suitable for in vivo evaluation. The identified lead was also found to be a selective inhibitor of PI3K isoforms and mTOR when screened across a panel of 23 homologous kinases. © 2015 Elsevier Ltd.


Patent
Inhibikase Therapeutics, Sphaera Pharma Pvt. Ltd. and Sphaera Pharma Pte. Ltd. | Date: 2013-10-04

Novel compounds and their synthesis are described. Methods for using these compounds in the prevention or treatment of cancer, a bacterial infection or a viral infection in a subject are also described.


Patent
Sphaera Pharma Pte Ltd. | Date: 2013-10-07

The present invention discloses novel chemical compounds obtained by causing a covalent attachment of a modifying agent of the structure provided for formula 1, to a functional group or a heteroatom of a heterocyclic ring system in chemical compound with improved chemical and biological properties. Wherein: Y is DRUG-CO; DRUG-OCO; DRUG-NRCO, and X is selected from.


Patent
Sphaera Pharma Pte. Ltd. | Date: 2012-01-24

The present invention provides synthetic processes for preparing racemic and/or optically pure epicatechin, epigallocatechin and related polyphenols as such or as their variously functionalized derivatives. A principle objective of the disclosure is to provide a new and useful method of synthesis to obtain polyphenols in isomerically pure and/or racemic forms.


Patent
Sphaera Pharma Pte. Ltd. | Date: 2013-07-23

The present invention relates to novel triazine compounds of formula (1). The present invention also discloses compounds of formula I along with other pharmaceutical acceptable excipients and use of the compounds to modulate the PI3K/mTOR pathway.


PubMed | Sphaera Pharma Pvt. Ltd and Sphaera Pharma Pte. Ltd
Type: Journal Article | Journal: Bioorganic & medicinal chemistry letters | Year: 2015

Over activation of the PI3K/Akt/mTOR pathway is found in most cancer tumor types. Controlled regulation of this pathway using PI3K inhibitors can provide therapeutic significance in cancer treatment. Herein, we report the synthesis and evaluation of pyrrolotriazine based novel small molecules as pan-PI3K inhibitors. The SAR studies based on in vitro potency along with microsomal metabolic stability screening, identified 18 as a preclinical lead found to be suitable for in vivo evaluation. The identified lead was also found to be a selective inhibitor of PI3K isoforms and mTOR when screened across a panel of 23 homologous kinases.


PubMed | Sphaera Pharma Pte. Ltd. and Sphaera Pharma Pvt. Ltd.
Type: Journal Article | Journal: ACS medicinal chemistry letters | Year: 2015

A new class of potent PI3K inhibitors is identified based on aryl substituted morpholino-triazine scaffold. The identified compounds showed not only a high level of enzymatic and cellular potency in nanomolar range but also high oral bioavailability. The three lead molecules (based on their in vitro potency) when evaluated further for in vitro metabolic stability as well as pharmacokinetic profile led to the identification of 26, as a candidate for further development. The IC50 and EC50 value of 26 is 60 and 500 nM, respectively, for PI3K enzyme inhibitory activity and ovarian cancer (A2780) cell line. The identified lead also showed a high level of microsomal stability and minimal inhibition activity for CYP3A4, CYP2C19, and CYP2D6 at 10 M concentrations. The lead compound 26, demonstrated excellent oral bioavailability with an AUC of 5.2 M at a dose of 3 mpk in mice and found to be well tolerated in mice when dosed at 30 mpk BID for 5 days.

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