Abstract: Compounds of formula I wherein: R1 is and R2, R4, and R6-9 are defined herein, and pharmaceutically acceptable salts and esters thereof. These compounds inhibit PI3 kinase and mTOR, and may be used to treat diseases mediated by PI3 kinase and mTOR, such as a variety of cancers. Methods for making and using the compounds of this invention are disclosed. Various compositions containing the compounds of this invention are also disclosed.
Type:
Application
Filed:
April 23, 2014
Publication date:
September 4, 2014
Applicant:
WYETH LLC
Inventors:
Aranapakam Mudumbai VENKATESAN, Zecheng CHEN, Christoph Martin DEHNHARDT, Osvaldo DOS SANTOS, Efren Guillermo DELOS SANTOS, Arie ZASK, Jeroen Cunera VERHEIJEN, Joshua Aaron KAPLAN, David James RICHARD, Semiramis AYRAL-KALOUSTIAN, Tarek Suhayl MANSOUR, Ariamala GOPALSAMY, Kevin Joseph CURRAN, Mengxiao SHI
Abstract: The present invention provides compositions comprising methylnaltrexone or a salt thereof, and compositions and formulations thereof, for oral administration.
Type:
Application
Filed:
July 31, 2013
Publication date:
September 4, 2014
Applicant:
Wyeth, LLC
Inventors:
Syed M. Shah, Christopher Richard Diorio, Eric C. Ehrnsperger, Xu Meng, Kadum A. Al Shareffi, Jonathan Marc Cohen
Abstract: The present invention provides a compound of formula I: wherein X?, R1, and R2 are as defined herein, and compositions thereof.
Type:
Grant
Filed:
May 2, 2013
Date of Patent:
September 2, 2014
Assignee:
Wyeth LLC
Inventors:
Nataliya Bazhina, George Joseph Donato, III, Steven R. Fabian, John Lokhnauth, Sreenivasulu Megati, Charles Melucci, Christian Ofslager, Niketa Patel, Galen Radebaugh, Syed M. Shah, Jan Szeliga, Huyi Zhang, Tianmin Zhu
Abstract: The present invention relates to new formulations containing one or more estrogens and 2-Phenyl-1-[4-(2-Aminoethoxy)-Benzyl]-Indole compounds which are useful as estrogenic agents, as well as pharmaceutical compositions and methods of treatment utilizing these compounds, which have the general structures below:
Abstract: Methods for preparing monomeric cytotoxic drug/carrier conjugates with a drug loading significantly higher than in previously reported procedures and with decreased aggregation and low conjugate fraction (LCF) are described. Cytotoxic drug derivative/antibody conjugates, compositions comprising the conjugates and uses of the conjugates are also described. Monomeric calicheamicin derivative/anti-CD22 antibody conjugates, compositions comprising the conjugates and uses of the conjugates are also described.
Type:
Application
Filed:
March 7, 2014
Publication date:
August 21, 2014
Applicant:
WYETH HOLDINGS LLC
Inventors:
ARTHUR KUNZ, Justin Keith Moran, Joseph Thomas Rubino, Neera Jain, Eugene Joseph Vidunas, John McLean Simpson, Nishith Merchant, John Francis Dijoseph, Mark Edward Ruppen, Nitin Krishnaji Damle, Paul David Robbins, Andrew George Popplewell
Abstract: Methods of immunizing older adult subjects against Streptococcus pneumoniae infection are provided. Provided methods comprise immunization of naïve adult subjects with a conjugated pneumococcal polysaccharide vaccine. Optionally, initial immunization may be followed by additional immunization doses comprising conjugated pneumococcal polysaccharide vaccine or unconjugated pneumococcal polysaccharide vaccine composition.
Type:
Grant
Filed:
April 26, 2007
Date of Patent:
August 19, 2014
Assignee:
Wyeth LLC
Inventors:
George Rainer Siber, Peter R. Paradiso, Jill G. Hackell, Stephen Paul Lockhart, William P. Hausdorff
Abstract: An apparatus and method for analyzing the morphometry of a human hip joint is provided. The apparatus includes image receiving means for receiving a digital image of a hip joint and image analysis means, including an Active Shape Model configured to identify a set of landmark points on the image, wherein the set of points includes points which correspond to features of the proximal femur and the region of the pelvis forming the acetabulum. The ASM is further configured to generate an image data-set from the co-ordinates of the landmark points; and data comparison means for comparing the image data-set with one or more comparative data-sets to obtain value(s) for one or more output modes which characterize the variation of the image data-set from the comparative data-set(s), to provide an indication of the presence and/or severity of osteoarthritis in the hip and/or the risk of the hip joint developing osteoarthritis.
Type:
Grant
Filed:
August 12, 2009
Date of Patent:
August 19, 2014
Assignees:
Wyeth Pharmaceuticals, Inc., TMRI, Ltd
Inventors:
Jennifer Susan Gregory, Richard Malcom Aspden, Rebecca Jane Barr, Kanako Yoshidashire, David Macaulay Reid
Abstract: An immunogenic composition having 13 distinct polysaccharide-protein conjugates and optionally, an aluminum-based adjuvant, is described. Each conjugate contains a capsular polysaccharide prepared from a different serotype of Streptococcus pneumoniae (1, 3, 4, 5, 6A, 6B, 7F, 9V, 14, 18C, 19A, 19F and 23F) conjugated to a carrier protein. The immunogenic composition, formulated as a vaccine, increases coverage against pneumococcal disease in infants and young children globally, and provides coverage for serotypes 6A and 19A that is not dependent on the limitations of serogroup cross-protection.
Type:
Grant
Filed:
April 4, 2012
Date of Patent:
August 19, 2014
Assignee:
Wyeth LLC
Inventors:
William P. Hausdorff, George Rainer Siber, Peter R. Paradiso
Abstract: The present invention provides lyophilized formulations comprising methylnaltrexone, and processes for preparation of provided formulations. Additionally provided are compositions and products containing the methylnaltrexone formulation, as well as methods for producing formulations, compositions and products. Provided formulations as well as compositions and products containing methylnaltrexone formulations are useful for preventing, treating delaying, diminishing or reducing the severity and/or incidence of side effects resulting from administration of analgesic opioids.
Abstract: Modified and stabilized propeptides of Growth Differentiation Factor proteins, such as GDF-8 and Bone Morphogenetic Protein-11, are disclosed. Also disclosed are methods for making and using the modified propeptides to prevent or treat human or animal disorders in which an increase in muscle tissue would be therapeutically beneficial. Such disorders include muscle or neuromuscular disorders (such as amyotrophic lateral sclerosis, muscular dystrophy, muscle atrophy, congestive obstructive pulmonary disease, muscle wasting syndrome, sarcopenia, or cachexia), metabolic diseases or disorders (such as such as type 2 diabetes, noninsulin-dependent diabetes mellitus, hyperglycemia, or obesity), adipose tissue disorders (such as obesity), and bone degenerative diseases (such as osteoporosis).
Type:
Application
Filed:
September 19, 2013
Publication date:
August 14, 2014
Applicant:
WYETH LLC
Inventors:
Neil M. Wolfman, Soo Peang Khor, Kathleen N. Tomkinson
Abstract: The present invention provides improved methods for producing a solution containing high molecular weight isolated Streptococcus pneumoniae 19A capsular polysaccharides. In certain methods, a fermentation culture of Streptococcus pneumoniae bacterial cells that produce serotype 19A capsular polysaccharides is fermented for less than 6 hours before the bacterial cells are lysed the capsular polysaccharides are harvested. In other methods, CO2 is supplied to the fermentation culture. Supplying CO2 to the fermentation culture includes adding bicarbonate ions to the fermentation culture, adding carbonate ions to the fermentation culture, adding mixtures of bicarbonate and carbonate ions to the fermentation culture, and overlaying the fermentation culture with CO2.
Abstract: Methods of using compounds which are progesterone receptor agonists for contraception and the treatment of progesterone-related maladies alone or in combination with an estrogen receptor agonist or progesterone receptor antagonist are provided. These compounds have the structure: wherein R1, R2, R3, R4, R5, and Q1 are defined herein.
Type:
Grant
Filed:
May 30, 2013
Date of Patent:
August 5, 2014
Assignee:
Wyeth LLC
Inventors:
Puwen Zhang, Andrew Fensome, Eugene A. Terefenko, Lin Zhi, Todd K. Jones, James P. Edwards, Christopher M. Tegley, Jay E. Wrobel, Mark A. Collins
Abstract: Compositions, preferably pharmaceutical compositions, containing micronized tanaproget, or pharmaceutically acceptable salt thereof, microcrystalline cellulose, croscarmellose sodium, sodium lauryl sulfate, butylated hydroxyanisole, povidone, and magnesium stearate, are provided. The compositions are useful in contraception and hormone replacement therapy and in the treatment and/or prevention of uterine myometrial fibroids, benign prostatic hypertrophy, benign and malignant neoplastic to disease, dysfunctional bleeding, uterine leiomyomata, endometriosis, polycystic ovary syndrome, and carcinomas and adenocarcinomas of the pituitary, endometrium, kidney, ovary, breast, colon, and prostate and other hormone-dependent tumors, and in the preparation of medicaments useful therefor. Additional uses include stimulation of food intake.
Type:
Grant
Filed:
November 29, 2012
Date of Patent:
July 29, 2014
Assignee:
Wyeth LLC
Inventors:
Arwinder S. Nagi, Ramarao S. Chatlapalli, Shamim Hasan, Rolland W. Carson, Mohamed Ghorab
Abstract: The invention provides preferred dosage ranges, maximum concentrations, average concentrations and monitoring regimes for use in treatment of Alzheimer's disease using antibodies to A?. The invention also provides monitoring regimes that as can assess changes in symptoms or signs of the patient following treatment.
Abstract: Child-resistant bulk dose dispensing packaging unit, and a method for opening the packaging unit, including a container and a lid engaged with the container. The container includes a reservoir, an aperture at a top end of the reservoir, and a protrusion extending from a surface of the container. The lid engages with the container and slides between a closed position and an open position. The lid includes a top wall, a side wall extending down from an outer edge of the top wall, and a post configured to engage the protrusion at a first position when the lid is closed so as to keep the lid closed. At least a portion of the post extends substantially parallel to the side wall at a distance from the side wall. Pressing the side wall inward places the post at a second position, wherein at the second position the post is disengaged from the protrusion.
Abstract: Compositions containing micronized tanaproget, or a pharmaceutically acceptable salt thereof, and ethinyl estradiol and methods of preparing the same are provided. Also provided are kits containing the compositions, methods of contraception and hormone replacement therapy including administering a composition containing micronized tanaproget and ethinyl estradiol.
Abstract: The present invention provides a compound of formula I: wherein X?, R1, and R2 are as defined herein, and compositions thereof; useful as a peripheral mu opioid receptor antagonist.
Abstract: The present invention provides compositions, desirably pharmaceutical compositions, containing micronized tanaproget. The compositions can also contain microcrystalline cellulose, croscarmellose sodium, anhydrous lactose, magnesium stearate, micronized edetate calcium disodium hydrous, and micronized sodium thiosulfate pentahydrate. The compositions are useful in contraception and hormone replacement therapy and in the treatment and/or prevention of uterine myometrial fibroids, benign prostatic hypertrophy, benign and malignant neoplastic disease, dysfunctional bleeding, uterine leiomyomata, endometriosis, polycystic ovary syndrome, and carcinomas and adenocarcinomas of the pituitary, endometrium, kidney, ovary, breast, colon, and prostate and other hormone-dependent tumors, and in the preparation of medicaments useful therefor. Additional uses include stimulation of food intake.