Royalty Report: Drugs, Drug Discovery, Gastrointestinal – Collection: 314635

License Grant

South Korean Licensor shall, and hereby does, grant to Licensee an exclusive (even as to Licensor and its Affiliates), royalty-bearing right and license, including the right to sublicense in accordance with this Agreement, under the Licensor Intellectual Property and Licensor’s interest in the Joint Intellectual Property, to Develop, Manufacture, use and Commercialize, including filing for, obtaining and maintaining Regulatory Approval for, Products in the Field in the Territory.

License Property

Product means any pharmaceutical preparation containing one or more Compounds either as its only active ingredient(s) or as part of a Combination Product. For the avoidance of doubt, nothing in this Agreement grants to Licensee or Licensor any right or license under any Patent Rights or Know-How Controlled by Licensor or Licensee, respectively, with respect to any Other API.

Compound means YH12852, which has the chemical structure set forth in this agreement, together with all analogs, derivatives, metabolites, stereoisomers, polymorphs, formulations, mixtures or compositions thereof, and any existing or future improved or modified versions of the foregoing developed by or on behalf of Licensee, its Affiliates or Sublicensees.

Compound (S)-N-(1-(2-((4-amino-3-nitrophenyl)amino)-6-propylpyrimidin-4-yl)pyrrolidin-3-yl)acetamide

Licensor Patent Rights means all Patent Rights in the Territory that are Controlled by Licensor or any of its Affiliates as of the Effective Date or thereafter during the Term (other than Joint Patent Rights) that Cover any Compound or Product. The Licensor Patent Rights existing as of the Effective Date are set forth on Schedule 1.57; provided, however, that, if Licensor is acquired by a Third Party, “Licensor Patent Rights” shall exclude any Patent Rights that (a) are Controlled by such Third Party or the Affiliates of such Third Party (other than Licensor and Licensor Pre-Existing Affiliates) and (b) were not Controlled by Licensor or any of the Licensor Pre-Existing Affiliates immediately prior to the closing of such acquisition transaction; provided further that, if, after the closing of such acquisition, any such Licensor Excluded Affiliate has or acquires Control of any Patent Right that Covers the Development, Manufacture or Commercialization of any Compound or Product and that is used to Develop, Manufacture or Commercialize any such Compound or Product, such additional Patent Right that is Controlled by such Licensor Excluded Affiliate shall be included in Licensor Patent Rights.

9,890,138 – Diaminopyrimidine derivatives and processes for the preparation thereof
10,227,330 – Diaminopyrimidine derivatives and processes for the preparation thereof
9,850,227 – Diaminopyrimidine derivatives and processes for the preparation thereof

Licensee is a global pharmaceutical company offering one-stop custom synthesis services of active pharmaceutical products (APIs) and intermediates.

YH12852 is a novel, potent and highly selective 5-hydroxytryptamine 4 (5-HT4) receptor agonist. Other 5-HT receptor agonists with less 5-HT4 selectivity have been shown to successfully treat GI mobility disorders such as chronic constipation, constipation-predominant irritable bowel syndrome, functional dyspepsia and gastroparesis.

Field of Use

YH12852 is a small molecule drug in development for the treatment of functional gastrointestinal (GI) disorders (FGID).

License Grant

Licensor and its Affiliates hereby grant Netherland Licensee (i) an exclusive (even as to Licensor and its Affiliates, royalty-bearing license (with the right to grant sublicenses at one or more tier(s) under the Licensor Technology, (a) to research, have researched, Develop, have Developed, use and have used TZP-101 and Product in the Field in the Licensed Territory and (b) to sell, offer for sale, have sold, import and otherwise Commercialize or have Commercialized Product in the Field in the Licensed Territory; (ii) a nonexclusive, worldwide, royalty-free license (with the right to grant sublicenses at one or more tier(s), under the Licensor Technology, to manufacture and have manufactured TZP-101 and Product worldwide solely for research, Development, use or Commercialization of such Products in the Field in the Licensed Territory under the license granted to Licensee; (iii) an exclusive (even as to Licensor and its Affiliates, royalty free license (with the right to grant sub-licenses at one or more tier(s) under Licensor’s interest in the Joint Inventions to (a) research, have researched, Develop, have Developed and use and have used TZP-101 and Product in the Field in the Licensed Territory and (b) sell, offer for sale, have sold, import and otherwise Commercialize or have Commercialized the Products in the Field in the Licensed Territory; and (iv) a nonexclusive, worldwide, royalty-free license (with the right to grant sublicenses at one or more tier(s), under the Joint Inventions, to manufacture and have manufactured TZP-101 and Product worldwide solely for Development, use or Commercialization of such Product in the Field in the Licensed Territory under the license granted to Licensee. Licensee shall not have the right to conduct or have conducted research and/or Development activities in the Retained Territory for the generation of data in support of Regulatory Filings to the Regulatory Authorities in the Licensed Territory except as expressly permitted under this Agreement or with the prior written consent of Licensor.  For clarity, the licenses granted to Licensee by Licensor and its Affiliates shall not include any rights for Licensee to research, Develop, make, have made, use, sell, offer for sale, distribute, import, export and otherwise commercialize any other proprietary compound of Licensor (including any proprietary compound which Licensor licenses to a Third Party) that is not TZP-101.

License Property

The compound under development, called ghrelin agonist ulimorelin (TZP-101), is entering Phase III clinical trials.
TZP-101 means Licensor’s proprietary ghrelin agonist known as TZP-101 (ulimorelin), having the chemical structure set forth in Agreement, including any salt, ester, solvate, polymorphic form, stereoisomer, metabolite, and pro-drug thereof.

Product means any pharmaceutical product comprising TZP-101 as an active ingredient irrespective of its formulation.

US 7,476,653 – Macrocyclic modulators of the ghrelin receptor

Licensor Product-Specific Patent means (a) the Patents set forth and (b) any other Patent that becomes Controlled by Licensor or its Affiliates at any time after the Effective Date (including Licensor Sole Patents but excluding Licensor’s interest in any Joint Patents) that (i) is necessary for Licensee and/or its Affiliates to have rights under in order to Develop, manufacture, use and/or Commercialize TZP-101 and/or Products in the Field; and (ii) is not a Licensor Other-Product Patent.

US 7,452,862 – Conformationally-controlled biologically active macrocyclic small molecules as motilin antagonists or ghrelin agonists

Licensor Other-Product Patent means (a) the Patents set forth and (b) any other Patent that becomes Controlled by Licensor or its Affiliates after the Effective Date (including Licensor Sole Patents but excluding Licensor’s interest in any Joint Patents) that (i) is necessary for Licensee and/or its Affiliates to have rights under in order to Develop, manufacture, use and/or Commercialize TZP-101 and/or Products in the Field; and (ii) covers any of Licensor’s proprietary technology (A) that is generally applicable or can be applied to Licensor’s discovery or development program in addition to the development program relating to TZP-101 and Product, or (B) that is applicable or can be applied to one or more compounds or products in addition to TZP-101 or Product, or (C) that covers the composition of matter of, or the method of discovering, making or using, any compounds or products (or any design, component, formulation or part thereof) in addition to TZP-101 or Product.

US 7,491,695 – Methods of using macrocyclic modulators of the ghrelin receptor

Field of Use

TZP-101 is for the acceleration of gastrointestinal (GI) recovery in patients undergoing abdominal surgery.

The deal is for development of a treatment targeting diseases of the muscles of the gastrointestinal track – called gastrointestinal dysmotility –

License Grant

For the Research License, The Canadian Licensor grants to the Licensee of Japan a co-exclusive, solely with respect to Licensor, right and license, under the Licensor Intellectual Property, to conduct Licensees responsibilities under the Research Program in the Field in the Territory during the Selection Period.

For the Development and Commercialization License, Licensor grants an exclusive, even as to Licensor, right and license, under the Licensor Intellectual Property, to Develop Selected Compounds into Licensed Products intended for use in the Field in the Territory, and make and have made, use, offer for sale, sell, have sold and import Selected Compounds and Licensed Products in the Field in the Territory.

For the Grant of Certain Jointly Developed Methyl Gene Collaboration Intellectual Property for use Outside the Field, Licensor grants a perpetual, irrevocable, non-exclusive right and license to use, solely outside the Field, Licensor Collaboration Intellectual Property that is Formulation Technology or Know-How that directly relates to the physicochemical property pharmacokinetics/pharmacodynamics relationship in ocular tissue, and is jointly developed, conceived or created by or on behalf of Licensor and/or its Affiliates, on the one hand, and by or on behalf of Licensee and/or its Affiliates, on the other hand.

License Property

The patents are titled
Inhibitors of VEOF Receptor and HOF Receptor;
Inhibitors of Protein Tyrosine Kinase Activity;
Kinase Inhibitors and Uses Thereof;
Processes and Intermediates for Preparing Fused;
Heterocyclic Kinase Inhibitors;
Inhibitors of Protein Tyrosine Kinase Activity;
Inhibitors of Kinase Activity.

A Compound is a molecule that is a small molecule that is a small molecule tyrosine kinase inhibitor as its main mechanism of action, and any salts, hydrates, solvates, polymorphs, free base, isomers, prodrugs, metabolites and/or liposomal or other formulations thereof or other compositions consisting of such molecule non-covalently bonded with other moieties, but excluding any derivative of such molecule in which the chemical structure of such molecule is altered.

Field of Use

Field means the prevention, treatment, control, mitigation or palliation in humans of diseases, disorders and other medical conditions caused by choroidal angiogenesis, including, without limitation, age-related macular degeneration, and diabetic retinopathy and retinal edema; in each case using local delivery of the active pharmaceutical agents to the eye.  For the avoidance of doubt, “local delivery” shall include, without limitation, topical, intravitreal, periorbital, intraocular and other local administration to the eye, the ocular and/or periocular tissues and spaces, including, without limitation, via delivery devices, but in any event, subject to Section 3.6, shall not include systemic delivery, including, without limitation, parenteral or sublingual delivery or delivery through a patch.  The Field shall expressly exclude the prevention, treatment, control, mitigation or palliation of any Indications other than above (e.g., treatment of cancer, including, without limitation, neoplasia and other pre-cancerous conditions and ocular cancer, is excluded).

License Grant

Licensor shall, and hereby does, grant to Licensee an exclusive (even as to Licensor and its Affiliates), royalty-bearing right and license, including the right to sublicense in accordance with this Agreement(b), under the Licensor Intellectual Property and Licensor’s interest in the Joint Intellectual Property, to Develop, Manufacture, use and Commercialize, including filing for, obtaining and maintaining Regulatory Approval for, Products in the Field in the Territory.

License Property

Product means any pharmaceutical preparation containing one or more Compounds either as an active ingredient(s) or any Combination Product. For the avoidance of doubt, nothing in this Agreement grants to Licensee any right or license under any Patent Rights or Know-How Controlled by Licensor with respect to any Other API.

Compound means RX-3117 (fluorocyclopentenylcytosine or also known as roducitabine) [which is a cytidine analog, similar to gemcitabine,][with a sequence of 4-amino-1-[(1S,4R,5S)-2-fluoro-4,5-dihydroxy-3-(hydroxymethyl)cyclopent-2-en-1-yl] pyrimidin-2-one] together with all analogs, derivatives, metabolites, stereoisomers, polymorphs, formulations, mixtures or compositions thereof covered by Licensor Intellectual Property, and any existing or future improved or modified versions of the foregoing developed by or on behalf of Licensee, its Affiliates or Sublicensees.

Patent
7,405,214 – Nucleoside derivatives and therapeutic use thereof
9,782,410 – Fluorocyclopentenylcytosine methods of use

Field of Use

RX-3117 is an oral, anticancer agent with an improved pharmacological profile relative to gemcitabine and other nucleoside analogs. Rx-3117 has a family of patents extending into 2036 as well as U.S. Food and Drug Administration (FDA) Orphan Designation for the treatment of Pancreatic Cancer. Licensee will evaluate the potential benefit of RX-3117 for patients with such cancers as pancreatic or non-small cell lung cancer.

License Grant

For the Exclusive License in the Territory. Licensor grants to the Licensee of Japan, an exclusive license, under the Licensor Patents that cover the Territory and the Licensor Know-How and Licensors rights under the Joint Inventions and the Joint Patents, to research, develop, make, have made, use, import, market, offer for sale and sell the Licensed Molecules and Products in the Field in the Territory.

For Research and Manufacturing License Outside the Territory, Licensor grants a non-exclusive license, with the right to sublicense, under the Licensor Patents that cover outside of the Territory and the Licensor Know-How and Licensors rights under the Joint Inventions and Joint Patents, to research, develop and manufacture the Licensed Molecules and Products outside the Territory solely for the purpose of advancing the research, development and commercialization of the Licensed Molecules and Products in the Field in the Territory.

License Property

Licensor is developing the Licensed Molecules and Products for use in the Field;  Licensor is a biopharmaceutical company using technology to fuel drug discovery and clinical development of novel treatments for central nervous system disorders.

Licensed Molecules shall mean any and all compounds that arc claimed or covered by an Licensor Patent, including, but not limited to PCAP-872, PCAP-831, PCAP-924 and PCAP-130, and the salts, metabolites and pro-drugs of such compounds.

Product shall mean a pharmaceutical product containing at least one Licensed Molecule, including all dosage forms, formulations, line extensions and modes of administration thereof.

The patents include
–  Amino substituted diary [a,d.] Cycloheptene analogs as muscarinic agonists and methods of treatment of Neuropsychiatric disorders,
–  Use of N-Desmethylclozapine and related compounds as dopamine stabilizing agents, and,
–  Prodrugs of muscarinic agonists and methods of treatment of Neuropsychiatric disorders.

Field of Use

This collaboration agreement is to develop and commercialize a novel class of pro-cognitive drugs to treat patients with schizophrenia and related disorders in Japan and several other Asian countries.