Akzo Nobel N.v.

Pharmacopeia Drug Discovery, Inc.

Akzo Nebel

Anton Egbert Peter Adang

Roland Ellwood Dolle

Koc-Kan Ho

Tao Guo

Edward McDonald

Kurt William Saionz

Guizhen Dong

Steven G Kultgen

Ruiyan Liu

Peng Geng

Nicole Corine Renee Van Straten

Gerritdina Geziena Gerritsma

Nicole Corine Renée Van Straten

Jacobus Albertus Maria Peters

The invention relates to bisaryl derivatives of the formula I,wherein (R,R) is selected from (H,H), O, (H,CH), (H,OH) and (H,CN); Ar is substituted phenyland A is a group of formula II, III, IV or V: An example is (3S,6S)-1-N-(7-phenylheptyl)-3-(4-(3,4,5-trimethoxyphenyl)benzyl)-4-N-methyl-6-methyl-2,5-dioxo-1,4-piperazine: The compounds of the invention have FSH receptor modulatory activity and can be used for the control of fertility, for contraception or for treatment of hormone-dependent disorders.

Bisaryl derivatives having FSH modulatory activity

The invention relates to a bicyclic heteroaromatic derivative compound according to general formula (II),or a pharmaceutically acceptable salt thereof. The compounds of the invention have LH receptor activating activity and can be used in fertility regulating therapies.

Bicyclic heteroaromatic compounds useful as LH agonists

Serine protease inhibitors

Serine protease inhibitors, prodrugs thereof and pharmaceutically acceptable salts thereof are disclosed. The serine protease inhibitors exhibit anticoagulant activity and are useful for treating or preventing thrombin related diseases.

The invention relates to a cornound having formula (I), wherein A, B, X, Y and r are as defined in the description, or a prodrug thereof or a pharnnaceutically acceptable salt thereof. The compounds of the invention have anticoagulant activity and can be used in treating or preventing thrombin-related diseases.

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Eindhoven, Netherlands

Anton Egbert Peter Adang