Stealth Biotherapeutics Inc.

Arqule, Inc.

Sepracor, Inc.

Other

Martin P Redmon

Scott M Duncan

David P Reed

Jian-Xie Chen

John C Kane

Christopher A Lee

Neil R Barnes

Chris Hugh Senanayake

Stephen Alan Wald

Yun Gao

Roger P Bakale

Manish Tandon

Yaping Hong

Kostas Saranteas

Mark T Kieras

Keith G Baker

Robert Hett

Kevin Q Fang

Erika Volckova

Daniel Pratt

Joseph A West

Judit Bartis

Deirdre Lowe

Disclosed are various crystalline salt forms of D-Arg-Dmt-Lys-Phe-NH.

Crystalline salt forms

Disclosed are crystalline forms of L-Lys(Boc)-Phe-NHand Boc-D-Arg-DMT. The crystalline forms may be used in the synthesis of elamipretide.

Crystalline dipeptides useful in the synthesis of elamipretide

Disclosed are crystalline forms of L-Lys(Boc)-Phe-NHand Boc-D-Arg-DMT.

The present invention relates to a (&#xb1;)-trans-3-(5,6-dihydro-4H-pyrrolo[3,2,1-ij]quinolin-1-yl)-4-(1H-indol-3-yl)pyrrolidine-2,5-dione dichloromethane.

Purified pyrroloquinolinyl-pyrrolidine-2,5-dione compositions and methods for preparing and using same

The present invention relates to a form 1 and form 2 polymorph of (&#x2212;)-trans-3-(5,6-dihydro-4H-pyrrolo[3,2,1-ij]quinolin-1-yl)-4-(1H-indol-3-yl)pyrrolidine-2,5-dione. The present invention also relates to (&#x2212;)-trans-3-(5,6-dihydro-4H-pyrrolo[3,2,1-ij]quinolin-1-yl)-4-(1H-indol-3-yl)pyrrolidine-2,5-dione compounds having a chiral purity greater than 99%, and methods of preparation of these compounds. The present invention also relates to pharmaceutical compositions comprising these (&#x2212;)-trans-3-(5,6-dihydro-4H-pyrrolo[3,2,1-ij]quinolin-1-yl)-4-(1H-indol-3-yl)pyrrolidine-2,5-dione compounds. The present invention provides methods of treating a cell proliferative disorder, such as a cancer, by administering to a subject in need thereof a therapeutically effective amount of a composition comprising (&#x2212;)-trans-3-(5,6-dihydro-4H-pyrrolo[3,2,1-ij]quinolin-1-yl)-4-(1H-indol-3-yl)pyrrolidine-2,5-dione having a chiral purity greater than 99% or a form 1 and form 2 polymorph of (&#x2212;)-trans-3-(5,6-dihydro-4H-pyrrolo[3,2,1-ij]quinolin-1-yl)-4-(1H-indol-3-yl)pyrrolidine-2,5-dione.

The present invention relates to a form 1 and form 2 polymorph of (&#x2212;)-trans-3-(5,6-dihydro-4H-pyrrolo[3,2,1-ij]quinolin-1-yl)-4-(1H-indol-3-yl)pyrrolidine-2,5-dione. The present invention also relates to (&#x2212;)-trans-3-(5,6-dihydro-4H-pyrrolo[3,2,1-ij]quinolin-1-yl)-4-(1H-indol-3-yl) pyrrolidine-2,5-dione compounds having a chiral purity greater than 99%, and methods of preparation of these compounds. The present invention also relates to pharmaceutical compositions comprising these (&#x2212;)-trans-3-(5,6-dihydro-4H-pyrrolo[3,2,1-ij]quinolin-1-yl)-4-(1H-indol-3-yl)pyrrolidine-2,5-dione compounds. The present invention provides methods of treating a cell proliferative disorder, such as a cancer, by administering to a subject in need thereof a therapeutically effective amount of a composition comprising (&#x2212;)-trans-3-(5,6-dihydro-4H-pyrrolo[3,2,1-ij]quinolin-1-yl)-4-(1H-indol-3-yl)pyrrolidine-2,5-dione having a chiral purity greater than 99% or a form 1 and form 2 polymorph of (&#x2212;)-trans-3-(5,6-dihydro-4H-pyrrolo[3,2,1-ij]quinolin-1-yl)-4-(1H-indol-3-yl)pyrrolidine-2,5-dione.

The present invention provides sodium 6-hydroxy-2,2-dimethyl-5-oxo-3,4,5,6-tetrahydro-2H-benzo(h)chromene-6-sulfonate, and its synthesis and uses in the treatment of cancer.

Hydroxy sulfonate of quinone compounds and their uses

Polymorphic crystalline forms of the antihistaminic drug norasternizole are disclosed. Processes for the production of the preferred polymorph are also disclosed.

Norastemizole polymorphs

A method for preparing aerosols of water-sensitive medicaments and a pharmaceutical kit for aerosol administration are disclosed. The kit includes (a) a solid state open matrix network of a medicament in a first container; and (b) an aqueous vehicle in a second container. The first and second containers may be separate or they may be chambers within a single housing. The solid state network may be a unit dose of medicament, and the quantity of aqueous vehicle will then be that quantity needed to deliver one unit dose by aerosol; alternatively, the solid state network may contain a plurality of unit doses of medicament, in which case the quantity of aqueous vehicle will be that quantity needed to deliver the number of unit doses in the network. The kit may also include a metered dose nebulizer. A preferred medicament for use in the method is formoterol.

Dosage form for aerosol administration

A method for universally distributing a therapeutic agent, in an encapsulated form, to the brain of a subject using intrathecal administration, excluding the lumbar region, is described. Methods for treating stroke and/or Traumatic Brain Injury (TBI) are also described. The methods involve intrathecal administration into the cerebrospinal fluid of a subject, of a therapeutic agent in an encapsulated form. Pharmaceutical compositions intended for the amelioration of stroke and/or Traumatic Brain Injury (TBI) are also described. The pharmaceutical compositions comprise a therapeutic agent encapsulated in a pharmaceutically acceptable polymer, suitable for injection into the cerebrospinal fluid of a subject suffering from stroke and/or Traumatic Brain Injury (TBI).

Methods for universally distributing therapeutic agents to the brain

A method is disclosed for the preparation of optically pure isomers of formoterol by the reaction of an optically pure 4-benzyloxy-3-formamidostyrene oxide with an optically pure 4-methoxy-.alpha.-methyl-N-(phenylmethyl)benzeneethanamine followed by debenzylation. Useful intermediates in the process are also disclosed, as are the novel L-tartrate salt of R,R-formoterol and pharmaceutical compositions thereof.

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Oxford, MA, United States of America

Martin P Redmon