Nobex Corporation

Biocon Limited

Other

Nnochiri Ekwuribe

Christopher H Price

Balasingam Radhakrishnan

Amy L Odenbaugh

Aslam M Ansari

Jennifer A Riggs-Sauthier

Richard Soltero

Kenneth D James

Navdeep Balkrishna Malkar

Monica Puskas

Diti Aggarwal

Michelle Ferro

Anthony James Hickey

Jennifer Riggs

Li Li Bovet

Bruce Rehlaender

Tatyana Dyakonov

James Gordon Still

Muthukumar Ramaswamy

Jennifer Ann Filbey

Balasingam Rhadakrishnan

Jayanthi Sethuraman Rajagopalan

Leo Pavliv

Kenneth Duke James, Jr

Gary S Bartley

Karen Polowy

Foyeke Opawale

Balasingam Radhakrishan

Wes Anderson Jr

Wes Anderson, Jr

Diti Sangal

Adam M Ansari

Elizabeth Malson

Balasingham Radhakrishnan

Rodger Liddle

Prodrug compounds which metabolize into 5-ASA or analogs thereof, and taurine or analogs thereof, in the colon site are disclosed. Pharmaceutical compositions including the compounds, and methods of treatment using the compounds, are also disclosed. Such compounds have utility for treating or preventing gastrointestinal disorders, including colon cancer, ulcerative colitis and Crohn's disease.

Aromatic carboxylic acid derivatives for treatment and prophylaxis of gastrointestinal diseases including colon cancers

An insulin compound coupled to a modifying moiety having a formula:&#x2014;X&#x2014;R&#x2014;Y-PAG-Z&#x2014;R&#x2003;&#x2003;(Formula VI)

Cation complexes of insulin compound conjugates, formulations and uses thereof

An insulin conjugate is disclosed in which insulin is coupled to a modifying moiety of the formula X&#x2014;R&#x2014;Y-PAG-Z&#x2014;Rwherein X, Y, and Z are linking groups, Ris a capping group, and PAG is a carbon chain that incorporates one or more alkylene glycol moieties.

Insulin-oligomer conjugates, formulations and uses thereof

Methods are disclosed for preparing compounds of Formula I: where R, R, and Rare independently hydrogen or Cto Calkyl, and Ris: where Ris selected from the group consisting of hydrogen and Cto Calkyl, or where R, Rand Rare independently hydrogen or Cto Calkyl; or the esters or pharmacologically acceptable salts thereof. The compounds and or their metabolites can be used to treat or prevent various diseases, particularly inflammatory conditions of the GI tract.

Synthesis of azo bonded immunoregulatory compounds

Fatty acid compositions for administration of of pharmaceutical agents, such as proteins and peptides, protein and peptide conjugates, and/or cation-polypeptide conjugate complexes. In particular, the invention provides a solid pharmaceutical composition formulated for oral administration by ingestion, having from about 0.1 to about 75% w/w fatty acid component, where the fatty acid component comprises saturated or unsaturated C4, C5, C6, C7, C8, C9, C10, C11, or C12 fatty acids and/or salts of such fatty acids; and a therapeutic agent. Further, the invention provides a liquid pharmaceutical composition formulated for oral administration by ingestion, comprising: from about 0.1 to about 10% w/v fatty acid component, where the fatty acid component comprises saturated or unsaturated C4, C5, C6, C7, C8, C9, C10, C11, or C12 fatty acids and/or salts of such fatty acids; and a therapeutic agent.

Fatty acid formulations and oral delivery of proteins and peptides, and uses thereof

A simple chain-extending approach was established for the scale-up of the monoprotected monodisperse PEG diol materials. Reactions of THP-(OCHCH)&#x2014;OMs (n=4, 8, 12) with a large excess of commercially available H&#x2014;(OCHCH)&#x2014;OH (n=1-4) under basic conditions led to THP-(OCHCH)&#x2014;OH (n=5-15). Similarly, Me-(OCHCH)&#x2014;OH (n=4-11, 13) were prepared from Me-(OCHCH)&#x2014;OMs (n=3, 7, 11). For the chain elongation steps, 40-80% yields were achieved through extraction purification. PEG oligomer libraries I and II were generated in 50-95% overall yields by alkylation or acylation of THP-(OCHCH)&#x2014;OH (n=1-15) followed by deprotection. Alkylation of Me-(OCHCH)&#x2014;OH (n=1-11, 13) with X&#x2014;(CH)&#x2014;COR (X=Br or OMs) and subsequent hydrolysis led to PEG oligomer library III in 30-60% overall yields. Combinatorial purification techniques were adapted to the larger-scale library synthesis. A total of 498 compounds, each with a weight of 2-5 g and a minimum purity of 90%, were synthesized.

Combinatorial synthesis of PEG oligomer libraries

Methods are disclosed for preparing compounds of Formula I: where R, R, and Rare independently hydrogen or Cto Calkyl, and Ris: where Ris selected from the group consisting of hydrogen and Cto Calkyl, or where R, Rand Rare independently hydrogen or Cto Calkyl; or the esters or pharmacologically acceptable salts thereof. The methods can involve converting a suitably functionalized aniline compound to a diazonium salt (which aniline compound can be first formed by reduction of a nitrobenzene) and coupling the diazonium salt with a suitably functionalized benzene compound. The suitably functionalized aniline compound either includes a primary alcohol or aldehyde group, which is then oxidized to a carboxylic acid group, or includes a nitrile or amide group, which is hydrolyzed to a carboxylic acid group. The methods can also involve the direct coupling (via reduction of nitro groups to form an azo linkage) of suitably functionalized nitrobenzenes. The compounds and or their metabolites can be used to treat or prevent various diseases, particularly inflammatory conditions of the GI tract.

The present invention provides a compound having a formula: where Ris selected from the group consisting of alkyl, CH(OCH)OCH, and &#x2014;(OCH)OCH; n is 0-4; Olig is an oligomer having a formula:-L-O-PAGR.R]where L is a optional linker moiety selected from the group consisting of &#x2014;CHO&#x2014;, &#x2014;CHOX&#x2014;, &#x2014;OX&#x2014;, &#x2014;C(O)&#x2014;, &#x2014;C(O)X, &#x2014;NH&#x2014;, &#x2014;NHC(O)&#x2014;, &#x2014;XNHC(O)&#x2014;, &#x2014;NHC(O)X&#x2014;, &#x2014;C(O)NH&#x2014;, &#x2014;C(O)NHX&#x2014;, and where X is alkylor is not present, Y is N or O or is not present, and Ris alkyl; PAG is a linear or branched polyalkylene glycol moiety; Ris an alkylcapping moiety if X is present or alkylif X is not present; and q is a number from 1 to the maximum number of branches on PAG; and m is 1-5.

Aryl carbamate oligomers for hydrolyzable prodrugs and prodrugs comprising same

The invention provides compositions comprising 4-APAA compounds and methods for treating disorders involving inflammation of the intestinal system, such as inflammatory bowel disease. The methods and compositions of the invention also include combinations of 4-APAA compounds and 5-ASA compounds for treatment of such disorders.

Methods and compositions employing 4-aminophenylacetic acid compounds

Calcitonin drug-oligomer conjugates that include a calcitonin drug coupled to an oligomer including a single polyalkylene glycol moiety consisting of between 4 and 10 polyalkylene glycol subunits are disclosed. Pharmaceutical compositions including such conjugates and methods of treating bone disorders by administering such conjugates are also disclosed.

Calcitonin drug-oligomer conjugates, and uses thereof

The invention provides a complex including a cation and an insulin compound conjugate. The insulin compound conjugate includes insulin compound, such as human insulin or an analog thereof, conjugated to a modifying moiety, such as a polyethylene glycol moiety. The invention also includes solids and pharmaceutical compositions including such complexes, methods of making such complexes, and methods of using such complexes in the treatment of insulin compound deficiencies and other ailments. Further, the invention includes novel insulin compound conjugates and modifying moieties for use in making novel insulin compound conjugates. The invention also includes fatty acid compositions for administration of pharmaceutical agents, such as the novel insulin compound conjugates, and/or the cation-insulin compound conjugate complexes of the invention.

Cation complexes of insulin compound conjugates, formulation and uses thereof

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Cary, NC, United States of America

Nnochiri Ekwuribe