Royalty Report: Drugs, Disease, Therapeutic – Collection: 372405

License Grant

Licensor hereby grants to Licensee, and Licensee hereby accepts from Licensor, a non-transferable, non-sublicensable, royalty-bearing license under the Patent License and the Know-How License (the Product License), solely within the Field of Use within the Territory to
(i) Research, develop or Commercialize, or have researched, developed or commercialized the Licensed Products;
(ii) Make and use the applicable Licensed Products;
(iii) Have made the applicable Licensed Products in accordance with this agreement;
(iv) Sell, offer for sale, promote and market the applicable Licensed Products (by itself, an Affiliate or through one or more Third Parties); and
(v) Import or have imported each Licensed Product.

License Property

Licensed Product(s) means collectively, (i) a product containing Iferanserin as an active ingredient, and (ii) any additional licensed products as agreed to by the Parties from time to time.

Iferanserin means the serotonin (5-HT2) receptor antagonist S-MPEC (iferanserin (INN) = (E)-2’-{2- [(2S)-l-methyl-2-piperidyl]ethyl}cinnamanilide serotonin receptor antagonist C23H28N2O, CAS 58754-46- 4). The definition includes all its various chemical forms, including derivatives acids, bases, esters, salts, isomers, enantiomers, pro-drug forms, metabolites, hydrates, solvates, polymorphs and degradants thereof in crystal, powder or other form and improvements, including new formulations and combinations and in addition, any back-up compounds to be provided by Licensor.

Licensor Patents means the (i) Patents listed
5,780,487 – S-2-[2-(1-methyl-2-piperidyl) ethyl] cinnamanilide
5,266,571 – Treatment of hemorrhoids with 5-HT.sub.2 antagonists
5,605,902 – 5-HT.sub.2 receptor antagonist compositions useful in treating venous conditions

Iferanserin is a drug which acts as a selective 5-HT2A receptor antagonist. It is under development as an intra-rectal formulation for the treatment of hemorrhoid disease, and as of February 2012, is in phase IIb clinical trials.

Field of Use

Field of Use means the field consisting of the topical treatment of any anorectal disorders in humans relating to utilize Iferanserin to deliver a rectal ointment compound for the treatment of hemorrhoids in human.

Anorectal conditions affect the anus and rectum. Fissures, fistulas, condyloma and hemorrhoids are among the most common anorectal conditions. In some cases, symptoms like pain, itching, burning, bleeding and/or swelling can significantly affect a patient's lifestyle.

License Grant

For the Exclusive License. Licensor grants a non-transferable, sole and exclusive, even as to Licensor and its Affiliates, worldwide license, with the right to sublicense, under the Licensor Patent Rights and Know-How, to make, have made, use, sell, offer to sell, import, research, develop, commercialize and otherwise exploit the Licensed Compound and Licensed Product in the Field in the Territory.

License Property

The Licensed Compound means Bicifadine and any prodrugs, optical isomers, hydrates, solvates, salt forms and polymorphs of Bicifadine.

Bicifadine (DOV-220075) is a nonopioid analgesic. It is an inhibitor of both the norepinephrine and serotonin transporters and an NMDA antagonist with a non-narcotic profile. Bicifadine was shown to have potent analgesic activity in vivo and was chosen for further development for the treatment of pain.

Field of Use

Field means the treatment of any diseases, disorders and conditions in humans, other than the treatment or amelioration of vasomotor symptoms caused by or occurring in relation to or connection with menopause or other female hormonal fluctuations in a patient undergoing treatment.

License Grant

Licensor grants to Licensee of Germany, an exclusive right and license under the Licensor Patent Rights, the Licensor Know-How and Licensors interest in the Joint Patent Rights and Joint Know-How to research, have researched, develop, have developed, register, have registered, use, have used, make, have made, import, have imported, export, have exported, market, have marketed, distribute, have distributed, sell and have sold PET Ligand and Products in the Field in the Territory.

Licensee has the right to develop and commercialize the PET Ligand as set forth.

License Property

Licensor has discovered proprietary compounds of the NMDA class and possesses proprietary intellectual property rights relating thereto, including the Licensor Patent Rights.

Licensor patents and technology relate to Imidazole Derivatives.  The invention relates to novel Imidazole Derivatives which are NMDA receptor subtype specific blockers, useful in the treatment of acute forms of neurodegeneration (stroke, brain trauma) and  of chronic forms of neurodegeneration ( Alzheimers disease, Parkinson, Huntingtons disease, ALS).

The products covered by the License Agreement are xO0678867; xO0693960; xO4378536; xO4394127; xO0631908; and, xO0717626.

The term Compound shall mean any of xO-0631908, xO-0678867, xO-0693960, xO4378536, x0-4394127, xO-0717626 and other compound structures Covered by the patent applications and patents for NMDA-2B receptor antagonists listed to the Agreement, including their salts, polymorphs, crystal forms, esters, hydrates, solvates, chelates, clathrates, metabolites that are NMDA-2B receptor antagonists, pro-drugs, isomers and enantiomers.

The term EVT 101 shall mean xO-4394127.

The term EVT 103 shall mean xO-0717626.

The term PET Ligand shall mean a Compound, with the exception of EVT 101 and EVT 103,
appropriately labelled for use in positron emission tomography for the specific labelling of NMDA NR2B subunit containing receptors in vivo.

Field of Use

The patent portfolio covers NMDA receptor NR2B subtype selective antagonists (the
EVT 100 family) for the treatment of a variety of CNS disorders such as Alzheimer’s disease, neuropathic pain and Parkinson’s Disease.