Merck + Co., Inc.

The Medical College of Pennsylvania

Hahnemann Univ.

Azriel Schmidt

Gideon A Rodan

Su Jane Rutledge

Robert L Vogel

M Katharine Holloway

Shun-ichi Harada

Eitan Friedman

John Howard Hutchinson

Mark E Duggan

Wasyl Halczenko

Soumya P Sahoo

Michael J Breslin

Dwight A Towler

Carlo J Gambone

The(rhesus monkey) Nur77 (rhNur77) nuclear receptor and the nucleic acid encoding the rhNur77 nuclear receptor are described. Further described are methods for identifying analytes that modulate expression or activity of the rhNur77 nuclear receptor. Analytes that affect Nur77 expression or activity may be used to treat or inhibit inflammatory diseases, for example, osteoarthritis and various bone, neurological, and prostrate disorders. The rhNur77 may also be used to treat various cancers, for example, prostate, ovarian, colon, lung, and gastric cancer.

Rhesus monkey Nur77

Compounds of structural formula (I) as herein defined are disclosed as useful in a method for modulating the androgen receptor in a tissue selective manner in a patient in need of such modulation, as well as in a method of agonizing the androgen receptor in a patient, and in particular the method wherein the androgen receptor is antagonized in the prostate of a male patient or in the uterus of a female patient and agonized in bone and/or muscle tissue. These compounds are useful in the treatment of conditions caused by androgen deficiency or which can be ameliorated by androgen administration, including: osteoporosis, periodontal disease, bone fracture, bone damage following bone reconstructive surgery, sarcopenia, frailty, aging skin, male hypogonadism, post-menopausal symptoms in women, atherosclerosis, hypercholesterolemia, hyperlipidemia, aplastic anemia and other hematopoietic disorders, pancreatic cancer, renal cancer, arthritis and joint repair, alone or in combination with other active agents. In addition, these compounds are useful as pharmaceutical composition ingredients alone and in combination with other active agents.

Androgen receptor modulators and methods for use thereof

The inhibition of natural bone formation experienced in the prophylaxis and/or treatment of bone resorption disease with a bisphosphonic acid or a pharmaceutically acceptable salt thereof is overcome by the concommitant administration of an agent that binds to the androgen receptor.

Combination of an agent that binds to the androgen receptor and a bisphosphonic acid in the prevention and/or treatment of diseases involving calcium or phosphate metabolism

A human protein tyrosine phosphatase (PTP) has been identified and its cDNA has been isolated. This PTP, denoted PTP-OB, has a receptor-like three dimensional structure and is present in osteoblasts. PTP-OB is involved in osteoblast differentiation, and modulators of PTP-OB activity in turn modulate osteoblast differentiation, osteoclast differentiation and osteoclast activity.

Method of identifying modulators of protein tyrosine phosphatase activity

Human steroid receptor

A novel human protein tyrosine phosphatase (PTP) has been identified and its cDNA has been isolated. This novel PTP, denoted PTP-OB, has a receptor-like three dimensional structure and is present in osteoblasts. PTP-OB is involved in osteoblast differentiation, and modulators of PTP-OB activity in turn modulate osteoblast differentiation, osteoclast differentiation and osteoclast activity.

Human protein tyrosine phosphatase OB protein

Wnt-x growth factor polypeptide, DNA encoding same, and Wnt-x antibody

The NER receptor is a novel member of the steroid hormone receptor superfamily and has been prepared by cDNA cloning from a human osteosarcoma SAOS-2/B10 cell library. The complete sequence of human NER complementary DNA (Seq. ID No. 1), expression systems including a COS stable expression system, the expressed protein (SEQ. ID No. 2) and an assay using the COS expression system are disclosed. The assay may be used to identify agents which activate transcription mediated by the NER receptor, and which are useful for potentiating the activity of a modulator of a G-protein coupled receptor wherein the G-protein coupled receptor is a member of the steroid hormone receptor superfamily.

Method for finding transcription activators of the NER steroid hormone

CDNA encoding a novel human protein tyrosine phosphatase

Use of the novel receptor NER TOFA (5-(tetradecyloxy)-2-furan-carboxylic acid) to treat Alzheimer's disease.

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Bryn Mawr, PA, United States of America

Azriel Schmidt