Abstract: The present invention relates to methods of making quinoline amides of Formula I below, which are microsomal triglyceride transfer protein inhibitors and can be used as medicines.
The present invention also relates to compounds that are used to make quinoline amides of Formula I and methods of making these compounds.
Abstract: The present invention provides novel methods of inhibiting pathological conditions related to organ systems which respond to estrogen agonists comprising administering to a mammal in need of such treatment an effective amount of a compound of formula I
Abstract: This invention relates to compounds of Formula I
or stereoisomers, pharmaceutically acceptable salts or prodrugs thereof or a pharmaceutically acceptable salts of the prodrugs. This invention also relates to pharmaceutical compositions comprising a compound of Formula I, and to methods of treatment of diabetes, insulin resistance, diabetic neuropathy, diabetic nephropathy, diabetic retinopathy, cataracts, hyperglycemia, hypercholesterolemia, hypertension, hyperinsulinemia, hyperlipidemia, atherosclerosis, or tissue ischemia.
Abstract: This invention provides an improved process for cis-1-{2-[4-(6-methoxy-2-phenyl-1,2,3,4-tetrahydronaphthalen-1-yl)phenoxy]ethyl}pyrrolidine which is an intermediate for the preparation of (−)cis-6-phenyl-5-[4-(2-pyrrolidin-1-yl-ethoxy)-phenyl]-5,6,7,8-tetrahydronaphthalene-2-ol which is useful for the treatment of osteoporosis.
Abstract: This invention relates to compounds of Formula I
that inhibit the secretion of apolipoprotein B, to pharmaceutical compositions comprising the compounds, and to methods of treating and/or preventing atherosclerosis, obesity, diabetes, hyperlipidemia, hyperliproproteinemia, hypercholesterolemia, hypertriglyceridemia, hypoalphalipoproteinemia, pancreatitis, myocardial infarction, stroke, restenosis, or Syndrome X. This invention also relates to methods of reducing the secretion of apolipoprotein B and/or inhibiting microsomal triglyceride transfer protein.
Abstract: Compounds of formula I,
wherein
R1 represents C1-4 alkoxy optionally substituted by one or more fluorine atoms;
R2 represents H or C1-6 alkoxy optionally substituted by one or more fluorine atoms;
R3 represents a 5- or 6-membered heterocyclic ring, the ring being optionally substituted;
R4 represents a 4-, 5-, 6-, or 7-membered heterocyclic ring, the ring being optionally fused to a benzene ring or 5- or 6-membered heterocyclic ring, the ring system as a whole being optionally substituted;
L is absent;
and pharmaceutically acceptable salts thereof; are useful in therapy, in particular in the treatment of benign prostatic hyperplasia.
Abstract: The present invention provides novel methods of inhibiting pathological conditions related to organ systems which respond to estrogen agonists comprising administering to a mammal in need of such treatment an effective amount of a compound of formula I
Abstract: The present invention provides compounds that are irreversible inhibitors of tyrosine kinases. Also provided is a method of treating cancer, restenosis, atherosclerosis, endometriosis, and psoriasis and a pharmaceutical composition that comprises a compound that is an irreversible inhibitor of tyrosine kinases.
Type:
Grant
Filed:
June 8, 1999
Date of Patent:
February 5, 2002
Assignee:
Warner-Lambert Company
Inventors:
Alexander James Bridges, William Alexander Denny, Ellen Myra Dobrusin, Annette Marian Doherty, David William Fry, Dennis Joseph McNamara, Howard Daniel Hollis Showalter, Jeffrey B. Smaill, Hairong Zhou
Abstract: This invention provides an improved process for cis-1-{2-[4-(6-methoxy-2-phenyl-1,2,3,4-tetrahydronaphthalen-1-yl)phenoxy]ethyl}pyrrolidine which is an intermediate for the preparation of (−)cis-6-phenyl-5-[4-(2-pyrrolidin-1-yl-ethoxy)-phenyl]-5,6,7,8-tetrahydronaphthalene-2-ol which is useful for the treatment of osteoporosis.
Abstract: The present invention provides compounds of Formula I
The present invention also provides a method of treating cancer and treating or preventing restenosis or atherosclerosis. Also provided by the present invention is a pharmaceutically acceptable composition containing a compound of Formula I.
Type:
Grant
Filed:
April 28, 2000
Date of Patent:
July 24, 2001
Assignee:
Warner-Lambert Company
Inventors:
Jack Bikker, Ellen Myra Dobrusin, Annette Marian Doherty, Matthew Drowns, James Stanley Kaltenbronn, Juergen Kleinschroth, Dennis Joseph McNamara, John Quin, III, Joseph Thomas Repine, Marcin Stasiak
Abstract: A series of 2-(4-hydroxypiperidino)-1-alkanol derivatives are useful as medicaments for the treatment of traumatic injuries to the brain and spinal cord and neuronal degenerative diseases including senile dementias, in mammals, especially humans.
Abstract: The present invention provides compounds that block calcium channels having formula (I). The present invention also provides methods of using the compounds of formula (I) to treat stroke, cerebral ischemia, head trauma, or epilepsy and to pharmaceutical compositions that contain the compounds of formula (I).
Type:
Grant
Filed:
September 29, 1999
Date of Patent:
June 26, 2001
Assignee:
Warner-Lambert Company
Inventors:
Lain-Yen Hu, Michael Francis Rafferty, Todd Robert Ryder
Abstract: The present invention provides compounds that block calcium channels having the Formula I shown below.
The present invention also provides methods of using the compounds of Formula I to treat stroke, cerebral ischemia, head trauma, epilepsy, asthma, amyotrophic lateral sclerosis, or pain and to pharmaceutical compositions that contain the compounds of Formula I.
Type:
Grant
Filed:
June 14, 1999
Date of Patent:
June 26, 2001
Assignee:
Warner-Lambert
Inventors:
Lain-Yen Hu, Michael Francis Rafferty, Todd Robert Ryder
Abstract: This invention is directed to the (L)-tartaric acid salt of 2-amino-N-{1-(2,4-difluoro-benzyloxymethyl)-2-oxo-2-[3-oxo-3a-pyridin-2-ylmethyl-2-(2,2,2-trifluoro-ethyl)-2,3,3a,4,6,7-hexahydro-pyrazolo{4,3-c}pyridin-5-yl]-ethyl]-2-methyl-propionamide which is a growth hormone secretagogue and as such is useful for increasing the level of endogenous growth hormone. In another aspect this invention provides certain intermediates which are useful in the synthesis of the foregoing compound. The (L)-tartaric acid salt of the compound of this invention is useful in the treatment and/or prevention of osteoporosis, insulin resistance and other conditions or diseases associated with growth hormone deficiency. The (L)-tartaric acid salt of the compound of the present invention is also useful in treating osteoporosis when used in combination with: a bisphosphonate compound; estrogen, Premarin, and optionally progesterone; an estrogen agonist or antagonist; or calcitonin.
Type:
Grant
Filed:
September 7, 1999
Date of Patent:
June 19, 2001
Assignee:
Pfizer Inc.
Inventors:
Philip Albert Carpino, Paul Andrew Dasilva-Jardine, Bruce Allen Lefker, Jerry Anthony Murry
Abstract: This invention provides an improved process for cis-1-{2-[4-(6-methoxy-2-phenyl-1,2,3,4-tetrahydronaphthalen-1-yl)phenoxy]ethyl}pyrrolidine which is an intermediate for the preparation of (-)cis-6-phenyl-5-[4-(2-pyrrolidin-1-yl-ethoxy)-phenyl]-5,6,7,8-tetrahydronaphthalene-2-ol which is useful for the treatment of osteoporosis.
Abstract: The present invention relates to a composition for the delivery of a pharmaceutical agent to a patient that comprises polyethylene glycol, an aqueous solution containing polyvinylpyrrolidone, and a pharmaceutical agent. The invention also relates to methods of making a composition for the delivery of a pharmaceutical agent.
Type:
Grant
Filed:
October 21, 1998
Date of Patent:
March 27, 2001
Assignee:
Warner-Lambert Company
Inventors:
Howard Yoshihisa Ando, Steven Edward Rose
Abstract: This invention relates to compounds that are antagonists of dopamine D4 receptors, to methods of treating psychosis and schizophrenia using a compound that is an antagonist of dopamine D4 receptors, and to pharmaceutically acceptable compositions that contain a dopamine D4 receptor antagonist.
Type:
Grant
Filed:
November 4, 1998
Date of Patent:
January 23, 2001
Assignee:
Warner-Lambert Company
Inventors:
Thomas R. Belliotti, Lawrence D. Wise, David J. Wustrow
Abstract: Compounds of formula I,
wherein
R1 represents C1-4 alkoxy optionally substituted by one or more fluorine atoms;
R2 represents H or C1-6 alkoxy optionally substituted by one or more fluorine atoms;
R3 represents a 5- or 6-membered heterocyclic ring, the ring being optionally substituted;
R4 represents a 4-, 5-, 6-, or 7-membered heterocyclic ring, the ring being optionally fused to a benzene ring or a 5- or 6-membered heterocyclic ring, the ring system as a whole being optionally substituted;
X represents CH or N; and
L is absent,
or represents a cyclic group of formula Ia,
or represents a chain of formula Ib,
and pharmaceutically acceptable salts thereof, are useful in therapy, in particular in the treatment of benign prostatic hyperplasia.
Abstract: The invention relates to certain steroidal glycoside derivatives useful as hypocholesterolemic agents and anti-atherosclerosis agents. The present invention is also directed to pharmaceutical compositions comprising such derivatives and use of such derivatives in treating hypercholesterolemia or atherosclerosis.
Abstract: Compounds of formula I, ##STR1## wherein X represents O or S(O).sub.m ;R.sup.1 and R.sup.2 independently represent phenyl, naphthyl or heteroaryl; each of which is optionally fused and optionally substituted;Y represents a bond, O, (CH.sub.2).sub.n, O(CH.sub.2).sub.n, (CH.sub.2).sub.n O, or CH(C.sub.1-6 alkyl)O;R.sup.3 represents H or C.sub.1-6 alkyl;m represents 0, 1, or 2; andn represents 1, or 2;and pharmaceutically acceptable salts thereof, are useful in therapy, in particular in the treatment of restenosis, renal failure and pulmonary hypertension.