Merck + Co., Inc.

Other

Thomas R Beattie

Matthew J Wyvratt

Burton G Christensen

Frank P DiNinno

Michael H Fisher

Tsung-Ying Shen

Byron H Arison

Hyun O Ok

Francis J Dumont

Tesfaye Biftu

Mark T Goulet

David B Johnston

John Hannah

Shu S Yang

San-Bao Hwang

Thomas W Doebber

Philippe L Durette

Timothy Francis Gallagher

Shieh-Shung T Chen

Lovji D Cama

Raymond F White

Georgette Dezeny

Robert Stevenson

Amy M Hale

The invention is directed to an animal carrier for use inside and outside of vehicles which comprises a cage-like enclosure having a top, a front, a rear, and a pair of sides intersecting with at least the front and a carriage for supporting the enclosure having a bottom, a front, a rear, and a pair of sides intersecting with at least the rear. Attachment members removably connect the cage with the carriage. At least one wedge is secured with the carriage rear and is adapted to be engaged with a seat belt of the vehicle for removably securing the carrier within the vehicle.

Pet car seat and carry-all

Hydroxymacrolides and derivatives of the general structural Formula I: ##STR1## have been prepared from suitable precursors by oxidation at C-20. These macrolides are useful as antagonists of FK-506-type immunosuppressants. The compounds of the present invention are useful for modifying dosages of FK-506-type immunosuppressants in the treatment of autoimmune diseases, infectious diseases and/or the prevention of rejection of foreign organ transplants. In addition, the compounds of the present invention have utility as antidotes for overdoses of FK-506-type immunosuppressants.

Antagonists of immunosuppressive macrolides

Described is a process for producing a new immunosuppressant, a C-31 desmethyl, C-19/C-22 cyclic hemiketal biotransformation analog (Compound I) of FR-900520, under novel fermentation conditions utilizing the novel microorganism, Streptomyces, lavendulae ATCC No. 55209. Also disclosed is the C-31 methylated derivative (Compound II) of Compound I produced by enzymatic methylation using 31-O-desmethylimmunomycin O-methyl transferase, (DIMT), a methyl transferase enzyme. The macrolide immunosuppressants are useful in preventing human host rejection of foreign organ transplants, e.g. bone marrow, liver, lung, kidney and heart transplants.

C-31 desmethyl FR-900520 cyclic hemiketal immunosuppressant agent

Aminomacrolides of the general structural Formula I: ##STR1## have been prepared from suitable precursors by incorporation of a nitrogen substituent 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.

Aminomacrolides and derivatives having immunosuppressive activity

A method for the modification of treatment of an immuno regulatory disorder or disease with an FK-506-type immunosuppressive macrolide comprising the administration to a mammalian species in need of such modification of an effective amount of a compound of the formula I. ##STR1##

Fluoromacrolides and derivatives of the general structural Formula I: ##STR1## have been prepared from suitable precursors by oxidation and fluorination at C-20. 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.

Fluoromacrolides having immunosuppressive activity

Ring-expanded macrolides related to FK-506 have immunosuppressive activity.

Thermally re-arranged FK-506 derivatives having immunosuppressant

Ring-expanded, immunosuppressive macrolides, are produced by heating and rearranging FK-506 and related compounds.

Immunoregulants, immunosuppressants, process to make ring expanded

Analogs of 2,5-Diaryl tetrahydrofurans which were substituted or unsubstituted at 3,4-positions were prepared. These compounds are found to have potent and specific PAF (Platelet Activating Factor) antagonistic activities and thereby useful in the treatment of various diseases or disorders mediated by the PAF, for example, inflammation, cardiovascular disorder, asthma, lung edema, adult respiratory distress syndrome, pain, and aggregation of platelets.

Method of use of 2,5-diaryl tetrahydrofurans and analogs thereof as

2,5-Diaryl tetrahydrofurans and analogs thereof as PAF-antagonists

Phosphatidyl inositol analogs are found to be effective phospholipase C inhibitors and thereby potent anti-inflammatory and analgesic agents. These phosphatidyl inositol analogs are prepared by condensation of a protected inositol with a substituted phosphonic or phosphorous acid followed by removal of protecting groups.

Phosphatidyl inositol analogs useful as anti-inflammatory/analgesic

Sulfonyl or carbonyl derivatives of inositols are found to be effective phospholipase C inhibitors and thereby potent anti-inflammatory and analgesic agents. These inositol derivatives are prepared by condensation of a protected inositol with a substituted sulfonic or carboxylic acid derivative followed by removal of protecting groups.

Sulfonyl or carbonyl inositol derivatives useful as

Novel cephalosporin compounds having a substituted or unsubstituted vinyl group at the 3-position are prepared by the reaction of a phosphoranylidene compound with a compound containing a carbonyl group. The novel cephalosporin compounds are active against a range of gram-negative and gram-positive microorganisms and are of value in human and veterinary medicine.

Cephalosporin compounds

Disclosed are antibiotic 7-(substituted methyl) cephalosporins, derivatives and nuclear analogues thereof; wherein the methyl substituent is, inter alia, hydroxyl, ketonic oxygen, imino nitrogen, amino or thio. Also disclosed are processes for the preparation of such compounds and their pharmaceutically acceptable salt, ester and amide derivatives; pharmaceutical compositions comprising such compounds; and methods of treatment comprising administering such compounds and compositions when an antibiotic effect is indicated.

Growing community of inventors

Scotch Plains, NJ, United States of America

Thomas R Beattie