Merck + Co., Inc.

Joung L Goulet

Peter J Sinclair

William H Parsons

Frederick Wong

Xingfang Hong

Sander G Mills

Matthew J Wyvratt

Mark T Goulet

Dennis M Zaller

Julianne A Hunt

Mark A Holmes

William K Hagmann

Philippe L Durette

Kathleen M Rupprecht

Jianming Bao

James B Doherty

Charles G Caldwell

Soumya P Sahoo

Hyun O Ok

Shouwu Miao

John E Stelmach

Meng-Hsin Chen

Swaminathan R Natarajan

Rose M Cubbon

Luping Liu

Helen M Armstrong

Richard Beresis

Florida Kallashi

David D Wisnoski

Richard T Cummings

James E Thompson

Mark G Steiner

Rowena D Ruzck

Benzimidazo[4,5-f]isoquinolinone derivatives are inhibitors of Janus protein tyrosine kinases (Jak), and as such are useful as immunosuppressants, and in the treatment of diseases including asthma, allergies, autoimmune diseases.

Benzimisazo[4,5-f]isoquinolinone derivatives

(Halo-benzo carbonyl)heterocyclo fused phenyl p38 kinase inhibiting agents

Pyrimidine compounds (Formula I), or their pharmaceutically acceptable salts, hydrates, solvates, crystal forms and individual diastereomers, and pharmaceutical compositions including the same, which are inhibitors of tyrosine kinase enzymes, and as such are useful in the prophylaxis and treatment of protein tyrosine kinase-associated disorders, such as immune diseases, hyperproliferative disorders and other diseases in which inappropriate protein kinase action is believed to play a role, such as cancer, angiogensis, atheroscelerosis, graft rejection, rheumatoid arthritis and psoriasis.

Src kinase inhibitor compounds

Pyrimidine compounds (Formula I), or their pharmaceutically acceptable salts, hydrates, solvates, crystal forms and individual diastereomers, and pharmaceutical compositions including the same, which are inhibitors of tyrosine kinase enzymes, and as such are useful in the prophylaxis and treatment of proteins tyrosine kinase-associated disorders, such as immune diseases, hyperproliferative disorders and other diseases in which inappropriate protein kinase action is believed to play a role, such as cancer, angiogensis, atheroscelerosis, graft rejection, rheumatoid arthritis and psoriasis.

SRC kinase inhibitor compounds

Novel phosphinic acid-containing peptidyl compounds of formula I are found to be useful inhibitors of matrix metalloendoproteinase-mediated diseases including osteoarthritis, rheumatoid arthritis, septic arthritis, tumor invasion in certain cancers, periodontal disease, corneal ulceration, proteinuria, dystrophobic epidermolysis bullosa, and coronary thrombosis associated with atherosclerotic plaque rupture. These inhibitors may also be useful in preventing the pathological sequelae following a traumatic injury that could lead to permanent disability. These compounds may also have utility as a means for birth control by preventing ovulation or implantation. ##STR1##

Substituted phosphinic acid-containing peptidyl derivatives as

O-Heteroaryl, O-alkylheteroaryl, O-alkenylheteroaryl and O-alkynylheteroaryl-macrolides of the general structural Formula I: ##STR1## have been prepared from suitable precursors by alkylation and/or arylation at C-3' and/or C-4' of the cyclohexyl ring. These macrolide immunosuppressants are useful in a mammalian host for the treatment of autoimmune diseases, infectious diseases, the prevention of rejection of foreign organ transplants and/or related afflictions, diseases and illnesses.

O-heteroaryl, O-alkylheteroaryl, O-alkenylheteroaryl and

O-Heteroaryl, O-alkylheteroaryl, O-alkenylheteroaryl and O-alkynylheteroarylmacrolides of the general structural Formula I: ##STR1## have been prepared from suitable precursors by alkylation and/or arylation at C-3' and/or C-4' of the cyclohexyl ring. These macrolide immunosuppressants are useful in a mammalian host for the treatment of autoimmune diseases, infectious diseases, the prevention of rejection of foreign organ transplants and/or related afflictions, diseases and illnesses.

D-heteroaryl, O-alkylheteroaryl, O-alkenylheteroaryl and

N-Heteroaryl, N-alkylheteroaryl, N-alkenylheteroaryl and N-alkynylheteroaryl macrolides of the general structural Formula I: ##STR1## have been prepared from suitable precursors by amination, alkylation and/or arylation at C-3' and/or C-4' of the cyclohexyl ring. These macrolide immunosuppressants are useful in a mammalian host for the treatment of autoimmune diseases, infectious diseases and/or the prevention of rejection of foreign organ transplants. In addition, these macrolide immunosuppressants are useful in the topical treatment of inflammatory and hyperproliferative skin diseases and cutaneous manifestations of immunologically-mediated illnesses. Also, these macrolides are useful in the treatment of reversible obstructive airways disease, particularly asthma. Furthermore, these macrolides are useful as hair revitalizing agents, especially in the treatment of male pattern alopecia or alopecia senilis.

N-heteroaryl, N-alkylheteroaryl, N-alkenylheteroaryl and

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Westfield, NJ, United States of America

Joung L Goulet