Royalty Report: Drugs, Diagnostic, Drug Discovery – Collection: 290550

Licensor grant to Licensee an exclusive worldwide license, with a right to grant sublicenses, under their rights in and to the Licensor X-Patents and under their interests in Licensee X-Patents to make, have made, use, sell, offer for sale, have sold and import certain X-Compounds, which X-Compounds contain a para-C1-C4-alkoxy substituted phenyl or pyridyl group in the place of 'Ar' as in formula (I) of WO 98/03510 and formula (I) or WO 97/29109 where such phenyl or pyridyl group is otherwise freely substituted and which X-Compounds otherwise specifically do not include a total of ten (10) compounds which may be named by Licensor in writing to Licensee within six (6) months of the Effective Date and provided that said specifically named ten (10) compounds were not previously made by an employee of Licensee in a written record before said naming by Licensor or which  may be named by Licensor in writing to Licensee after six (6) months and before twelve (12) months of the Effective Date and provided that said specifically named ten (10) compounds were not previously named by an employee of Licensee in a written record before said naming by Licensor.

X-Product means a Product comprised of an X-Compound.

X-Compounds means compounds which, as compounds or chemical entities, are specifically or generically within  the published claims of WO 98/03510 or which are specifically or generically within the published claims of WO 97 /29109 and which is a pyrazolopyrimidine having a base structure.  For clarity and in accordance with the foregoing, an X-Compound is not and does not include those compounds described in WO 98/03510 as pyrazolotriazines wherein A in formula (I) therein is a nitrogen (N) atom.

Licensee X-Patents means the rights granted by any governmental authority under a Patent derived from from WO 98/03510 and any counterparts  thereof, and  additionally, the rights  granted by any governmental authority  under a Patent which claims an X-Compound as a novel compound or chemical entity, which Patent is owned or Controlled by Licensee at any time.

Licensee X-Patents licensed to Licensor under this Article will be considered by Licensor a Program Patent under the agreement between Licensor effective January 1, 1995 for the purpose of determining the rights therein and the obligations therefor as between Licensor only.

Patent means (i) valid and enforceable letters patent including any extensions, registration, confirmation, reissue,  continuation, divisional, continuation-in-part, re-examination, or renewal thereof, and (ii) pending applications for letters patent.

Product means any form or dosage of a compound for pharmaceutical use in humans or other animals or for use as a diagnostic tool that consists of an X-Product or N-Product, as the case may be.

N-Product means a Product comprised of an N-Compound.

N-Compounds means those compounds which, as compounds or chemical entities, are specifically or generically within the scope of the published claim number 4 of WO 98/35967 and includes those compounds as described in the disclosure of WO 98/35967 and shown as substructures (II) and as (Ila), (Ilb) and (lie).

CORTICOTROPIN RELEASING FACTOR ('CRF'). Corticotropin releasing factor, the central regulator of the body's overall response to stress, affects multiple systems by functioning both as an endocrine factor and a neurotransmitter. CRF acts as a hormone at the pituitary gland causing the secretion of the steroid cortisol from the adrenal glands resulting in a number of metabolic effects, including suppression of the immune system. CRF also functions as a neurotransmitter in the brain and plays a critical role in coordinating psychological and behavioral responses to stress such as increased heart rate, anxiety, arousal and reduced appetite. In addition to neuroendocrine and neurotransmitter roles, accumulating evidence suggests that CRF may also integrate actions between the immune and central nervous systems in response to physiological and psychological stressors. The body has several mechanisms to regulate the effects of CRF. The Company's cloning of human CRF receptors and binding proteins suggests that the diverse functions of CRF are mediated through distinct receptor subtypes which are differentially distributed in specific brain areas and in tissues outside of the central nervous system. These targets may offer a mechanism to modulate specific actions of CRF without affecting the broad range of its activities. There are several diseases and disorders such as anxiety, depression and substance abuse in which CRF levels are increased. The deleterious effects of high levels of CRF may be countered by the administration of selective CRF receptor antagonists.

Field means the discovery, synthesis, and selection of X-Compounds and N-Compounds and the manufacture,  development and use of Products.

Licensor grant to Licensee an exclusive worldwide license, with a right to grant sublicenses, under their rights in and to the Licensor X-Patents and under their interests in Licensee X-Patents to make, have made, use, sell, offer for sale, have sold and import certain X-Compounds, which X-Compounds contain a para-C1-C4-alkoxy substituted phenyl or pyridyl group in the place of 'Ar' as in formula (I) of WO 98/03510 and formula (I) or WO 97/29109 where such phenyl or pyridyl group is otherwise freely substituted and which X-Compounds otherwise specifically do not include a total of ten (10) compounds which may be named by Licensor in writing to Licensee within six (6) months of the Effective Date and provided that said specifically named ten (10) compounds were not previously made by an employee of Licensee in a written record before said naming by Licensor or which  may be named by Licensor in writing to Licensee after six (6) months and before twelve (12) months of the Effective Date and provided that said specifically named ten (10) compounds were not previously named by an employee of Licensee in a written record before said naming by Licensor.

X-Compounds means compounds which, as compounds or chemical entities, are specifically or generically within  the published claims of WO 98/03510 or which are specifically or generically within the published claims of WO 97 /29109 and which is a pyrazolopyrimidine having a base structure.  For clarity and in accordance with the foregoing, an X-Compound is not and does not include those compounds described in WO 98/03510 as pyrazolotriazines wherein A in formula (I) therein is a nitrogen (N) atom.

Licensee X-Patents means the rights granted by any governmental authority under a Patent derived from from WO 98/03510 and any counterparts  thereof, and  additionally, the rights  granted by any governmental authority  under a Patent which claims an X-Compound as a novel compound or chemical entity, which Patent is owned or Controlled by Licensee at any time.

Licensee X-Patents licensed to Licensor under this Article will be considered by Licensor a Program Patent under the agreement between Licensor effective January 1, 1995 for the purpose of determining the rights therein and the obligations therefor as between Licensor only.

Product means any form or dosage of a compound for pharmaceutical use in humans or other animals or for use as a diagnostic tool that consists of an X-Product or N-Product, as the case may be.

N-Product means a Product comprised of an N-Compound.

N-Compounds means those compounds which, as compounds or chemical entities, are specifically or generically within the scope of the published claim number 4 of WO 98/35967 and includes those compounds as described in the disclosure of WO 98/35967 and shown as substructures (II) and as (Ila), (Ilb) and (lie).

Licensor grants to Licensee a co-exclusive worldwide license, with the right to grant sublicenses, under Licensor X-Patents and under Licensors interest in Licensee X-Patents to make, have made, use, sell, offer to sell, have sold and import X-Compounds, which X-Compounds do not contain  a para-C1-C4-alkoxy substituted phenyl or pyridyl group in the place of 'Ar as in formula a (I) of WO 98/03510 and formula (I) or WO 98/29109 where such phenyl or pyridyl group is otherwise freely substituted and which X-Compounds otherwise specifically include a total of ten (10) compounds which may be named by Licensee in writing to Licensor within six (6) months of the Effective Date and provided that said specifically ten (10) compounds  were not previously made by an employee of Licensor in a written record before said naming by Licensee. For clarity  and in accordance with the foregoing, Licensor does not grant to Licensee a license (exclusive or non-exclusive) to any subject  matter disclosed or claimed in  WO 98/03510 that is a pyrazolotriazine or otherwise as shown in formula {I) therein wherein A is a nitrogen (N) atom.

X-Compounds means compounds which, as compounds or chemical entities, are specifically or generically within  the published claims of WO 98/03510 or which are specifically or generically within the published claims of WO 97 /29109 and which is a pyrazolopyrimidine having a base structure.  For clarity and in accordance with the foregoing, an X-Compound is not and does not include those compounds described in WO 98/03510 as pyrazolotriazines wherein A in formula (I) therein is a nitrogen (N) atom.

Licensor X-Patents means the rights granted by any governmental authority under a Patent derived from from WO 98/03510 and any counterparts  thereof, and  additionally, the rights  granted  by any governmental authority  under a Patent which claims an X-Compound as a novel compound or chemical entity, which Patent is owned or Controlled by Licensor at any time.

Licensor X-Patents licensed to Licensee under this Article will be considered by Licensee a Program Patent under the agreement between Licensee effective January 1, 1995 for the purpose of determining the rights therein and the obligations therefor as between Licensee only.

Product means any form or dosage of a compound for pharmaceutical use in humans or other animals or for use as a diagnostic tool that consists of an X-Product or N-Product, as the case may be.

N-Product means a Product comprised of an N-Compound.

N-Compounds means those compounds which, as compounds or chemical entities, are specifically or generically within the scope of the published claim number 4 of WO 98/35967 and includes those compounds as described in the disclosure of WO 98/35967 and shown as substructures (II) and as (Ila), (Ilb) and (lie).

Licensor Compound means any 5-HT6 receptor antagonist for which Licensor as of the Effective Date has rights, whether by reason of its own conception of such antagonist, or under agreement with a Third Party, and are Covered by Licensor Patent Rights. Licensor Compounds shall include any 5-HT6 receptor antagonist for which Licensee during the term of this Agreement has rights by reason of its own conception of such antagonist and which also is Covered by the Licensor Patent Rights. A list of the Licensor Compounds shall be updated from time-to-time.

Licensee Product means any pharmaceutical product that includes, in whole or as a component, any Licensee Compound as an active ingredient thereof.

Licensee Compound means any 5-HT6 receptor antagonist for which Licensee as of the Effective Date or during the term of this Agreement has rights, by reason of its own conception of such antagonist, and are Covered by Licensee Patent Rights, but are not covered by the Licensor Patent Rights. A list of the Licensee Compounds shall be updated from time-to-time.

Licensor Patent Rights means all Patent Rights that Licensor owns, or otherwise has the right to grant the licenses herein relating to 5-HT6 receptor antagonists as updated from time-to-time, including (a) any patents issuing from any such patent applications listed hereto and (b) any divisional applications, continuation applications, continuation-in-part applications, substitutions, extensions, supplementary protection certificates, reissues, reexaminations, renewals or the like related to the patents and patent applications listed hereto. Licensor Patent Rights do not include Licensors non-exclusive license from NIH to the 5-HT6 receptor patents.

6,100,291 – Pyrrolidine-indole compounds having 5-HT.sub.6 affinity
6,133,287 – Piperidine-indole compounds having 5-HT.sub.6 affinity
6,251,893 – Bicyclic piperidine and piperazine compounds having 5-HT6 receptor affinity

Licensee Patent Rights means all Patent Rights that Licensee owns relating to 5-HT6 receptor antagonists as updated from time-to-time, including (a) any patents issuing from any such patent applications listed hereto and (b) any divisional applications, continuation applications, continuation-in-part applications, substitutions, extensions, supplementary protection certificates, reissues, reexaminations, renewals or the like related to the patents and patent applications listed.

U.S. Patent Application No. 11/676,203 – Compounds having 5-HT6 receptor affinity
U.S. Provisional Patent Application No. 60/890,324 – 6 substituted compounds having 5-HT6 receptor affinity