Royalty Report: Drugs, Delivery, Technical Know How – Collection: 203373

License Grant

The Swiss Licensor grants to Licensee, by third party,  an exclusive, worldwide sub-license under the Licensors Patents and Product Know-how to manufacture, make, have made, import, use, offer for sale, market, distribute, have sold and sell Products in accordance with the Licensees License.

Pursuant to agreements each party has with a third party, this agreement is entered into to allow access to patents for product development between all three parties.

License Property

The product is the dosage forms of a finished product containing ABT-077 as the sole therapeutic or prophylactic active ingredient, in a matrix tablet using the Geomatrix System.

The Geomatrix System means Licensors novel pharmaceutical technology for the controlled release of active substances, and related technology which utilizes a hydrophilic drug-containing matrix tablet to control the release of an active substance through the use of one or more barrier layers, as disclosed in Product Know-how and claimed in the Licensors Patents.

Product  relates to a controlled-release formulation of zileuton.

Field of Use

The Licensee is developing a controlled-released formulation of zileuton for asthma.  The Licensee intend to explore additional indications for zileuton, including chronic obstructive pulmonary disease, or COPD, nasal polyps, mastocytosis and cystic acne.

License Grant

Swiss Licensor hereby grants to English Licensee an exclusive license, with the right to grant sublicenses under the patents, SPCs and Licensor-Know-How to make, have made, use and sell product in the territory, subject to the terms and conditions of this agreement. The rights to make, have made, use and sell shall include all activities concerning the subject matter of patents, SPCs and Licensor-Know-How with respect to the making, use and sale of product only, which activities would, but for the license herein granted, infringe Patents, SPCs and/or Licensor-Know-How. In addition, Licensor hereby grants to Licensee an exclusive license, with the right to grant sublicenses subject to this agreement, to make, have made, use and sell any invention or know-how related to Product which arose under the Letter, whether patented and/or patentable or not, for any purpose directly related to any selective serotonin reuptake inhibitor, provided that Licensor shall be allowed to use any such invention or know-how and the patents covering same, if any, for any other purpose not directly related to any selective serotonin reuptake inhibitor.

License Property

Paroxetine shall mean the chemical compound known as paroxetine, the more specific chemical name of which is [(-)-trans-4-(4- fluorophenyl)-3-[3,4-methylene-dioxyphenoxy) methyl] piperidine] and all pharmaceutically active derivatives thereof such as, but not limited to esters, salts (such as, but not limited to, the hydrochloride salt), hydrates, solvates, polymorphs, prodrugs and isomers thereof.

Geomatrix® Technology shall mean Licensors proprietary oral, modified release (i.e., controlled-release, sustained-release, or delayed release) drug delivery and related technology which utilizes a hydrophilic drug-containing matrix tablet which controls the release of the drug through the use of one or more barrier layers, together with all improvements thereon or thereto.

Product shall mean shall mean an oral delivery system for Paroxetine based on or using the Geomatrix® Technology.

Patents shall mean
4,839,177 – System for the controlled-rate release of active substances
5,422,123 – Tablets with controlled-rate release of active substances
5,476,654 – Process for preparing pharmaceutical compositions having an increased active substance dissolution rate, and the compositions obtained

SPC shall mean a right based upon a patent to exclude others from making, using or selling product, such as a Supplementary Protection Certificate.

Field of Use

Licensee will utilize such technology to develop drugs taken orally in tablet form formulated so as to control the amount, timing and location of the release of the drug in the body for pharmaceutical use in human prescriptions.

License Grant

Licensor hereby grants to Licensee for the Term of this Agreement an exclusive (even as to Licensor) license in the Field under the Licensor Intellectual Property to develop, make, have made, use, sell, offer for sale and import Licensed Product(s) in the Territory.

License Property

Licensed Product(s) means all finished pharmaceutical oral formulations for commercial sale (or, where the context so indicates, a Formulation Candidate) that (i) contain the Compound alone as a therapeutically active ingredient or in combination with any other pharmaceutically active ingredient, and (ii) utilize Licensor Intellectual Property.

Intellectual Property means the Licensed Patents, the Licensor Know-How and the Licensor Technology.

Licensed Patents means Patents owned or controlled by Licensor or which Licensor, through license or otherwise, has or acquires rights, which are necessary or useful for the manufacture, use or sale of Licensed Product, including, but not limited to, compositions, formulations, methods of their manufacture, or methods of their use, or otherwise relate to Licensor Know-How or Licensor Technology, including (i) any of the Patents set forth hereto that contain claims that cover, or which relate to, any aspect of Licensed Product, (ii) the Development Patents and (iii) such other Patents as the Parties may agree in writing from time to time.

5,447,729 – Multilamellar drug delivery systems
5,484,608 – Sustained-release drug delivery system

Licensor Technology means  Licensor’s bioavailability enhancement and/ or controlled-release delivery, formulation, process and manufacturing technologies, including but not limited to the Licensor Lead Technology and the technologies embodied in the Licensed Patents and the Licensor Know-How.

Licensor Lead Technology means Microtrol® multi particulate technology or, as subsequently agreed between the Parties, one of the Other Licensor Technologies as may be applied to the Compound pursuant to the Development Plan.

Compound means trospium chloride, the chemical compound whose specific chemical name is 3-alpha benziloyJoxynortropane-8-spiro-1-pyrrolidinium; chloride, or any other trospium salt.

Field of Use

Trospium chloride (“trospium”) is  indicated for urinary incontinence. Trospium is currently under evaluation in a Phase III clinical study.

License Grant

The Company has previously agreed to pay royalties to CONSULTANT, a member of the Company's Board of Directors, in recognition of the patents developed by CONSULTANT for TIMERx.

License Property

The Company has developed the TIMERx delivery system, a novel drug delivery technology, to address the limitations of currently available oral controlled release delivery systems. The Company believes that the TIMERx system is a major advancement in oral drug delivery that represents the first easily-manufactured oral controlled release drug delivery system that is applicable to a wide variety of drug classes, including soluble drugs, insoluble drugs and drugs with a narrow therapeutic index. The Company is utilizing the TIMERx system to formulate generic versions of branded controlled release drugs, controlled release formulations of currently-marketed.

The TIMERx drug delivery system is a hydrophilic matrix combining primarily a heterodispersed mixture, usually polysaccharides xanthan and locust bean gums, in the presence of dextrose. The physical interaction between these components works to form a strong, binding gel in the presence of water. Drug release is controlled by the rate of water penetration from the gastrointestinal tract into the TIMERx gum matrix, which expands to form a gel and subsequently releases the active drug substance. The TIMERx system can precisely control the release of the active drug substance in a tablet by varying the proportion of the gums, together with the third component, the tablet coating and the tablet manufacturing process. Drugs using TIMERx technology are formulated by combining the active drug substance, the TIMERx drug delivery system and additional excipients and compressing such materials into a tablet.

1)  Directly compressible sustained release excipient.

2)  Sustained release excipient and tablet formulation.

3)  Compressible sustained release solid dosage forms.

4)  EPO Application No. 89309518.2; filed September 19, 1989.

5)  Australian Patent Application No. 43057/89

6)  Japanese Patent Application No. 1-510135

7)  Irish Patent Application No. 2968/89

8)  Canadian Patent Application No. 611,700

9)  Verapamil Tablet Application, Serial No. 736,031 & EPO PCT Applications.

10)  2 U.S. Applications on Bi-modal release.