Karo Bio Ab

Bristol-Myers Squibb Compnay

Karo Pharma Ab

Neeraj Garg

Denis E Ryono

Johan Malm

Konrad Koehler

Chris Litten

Ana Maria Garcia Collazo

Minsheng Zhang

Jon J Hangeland

Yolanda V Caringal

Yi-Lin Li

William N Washburn

Wei Meng

Bruce A Ellsworth

Joakim Löfstedt

Ramakrishnan Chidambaram

Ye Liu

Aiping Cheng

Lars Krüger

Lars Hagberg

Thomas Ericsson

Thomas Anders Wilson Ericsson

Lars Johan Malm

Venkatramana M Rao

Mahmoud Rahimi Ghadim

Li Yi-Lin

Mahmoud Rahimi-Ghadim

Daniel Nöteberg

Eva Koch

Lars KRÜGER

Joakim LÖFSTEDT

Daniel NÖTEBERG

Sandra Gracin

Ake Rasmuson

Compounds of formula (I) or a pharmaceutically acceptable ester, amide, carbamate or salt thereof, including a salt of such an ester, amide or carbamate in which Rto Rhave meanings as defined in the Specification, are useful as estrogen receptor ligands. 

Estrogen receptor ligands

Novel thyroid receptor ligands are provided having the general formula I wherein In addition, a method is provided for preventing, inhibiting or treating diseases or disorders associated with metabolic dysfunction or which are dependent upon the expression of a Tregulated gene, wherein a compound as described above is administered in a therapeutically effective amount.

Substituted anilide ligands for the thyroid receptor

New thyroid receptor ligands are provided which have general formula (I) in which: n is an integer from 0 to 4; Ris halogen, trifluoromethyl, or alkyl of 1 to 6 carbons or cycloalkyl of 3 to 7 carbons; Rand Rare the same or different and are hydrogen, halogen, alkyl of 1 to 4 carbons or cycloalkyl of 3 to 5 carbons, at least one of Rand Rbeing other than hydrogen; Ris a carboxylic acid amide (CONR'R&#x2033;) or an acylsulphonamide (CONHSOR&#x2032;) derivative, or a pharmaceutically acceptable salt thereof, and all stereolsom thereof; or when n is equal to or greater than one, Rmay be heteroaromatic moiety which may be substituted or unsubstituted, or an amine (NR&#x2032;R&#x2033;). Ris hydrogen or an acyl (such as acetyl or benzoyl) or other group capable of bioconversion to generate the free phenol structure (wherein R&#x2014;H). In addition, a method is provided for preventing, inhibiting or treating a disease associated with metabolism dysfunction or which is dependant upon the expression of a Tregulated gene, wherein a compound as described above is administered in a therapeutically effective amount. Examples of such diseases associated with metabolism dysfunction or are dependent upon the expression of a Tregulated gene include obesity, hypercholesterolemia, atherosclerosis, cardiac arrhythmias, depression, osteoporosis, hypothyroidism, goiter, thyroid cancer as well as glaucoma, congestive heart failure and skin disorders. 

Thyroid receptor ligands and method II

This invention relates to compounds of the formula (I) which are thyroid receptor ligands, and are preferably selective for the thyroid hormone receptor &#x3b2;, to methods of preparing such compounds and to methods for using such compounds such as in the regulation of metabolism. 

Thyroid receptor ligands, pharmaceutical compositions comprising them and their use in the treatment of disorders influenced by thyroid hormones

This invention relates to novel compounds, which are thyroid receptor ligands, and to methods of preparing such compounds. In addition, a method is provided for preventing, inhibiting or treating diseases or disorders associated with metabolism dysfunction or which are dependent upon the expression of a T3 regulated gene, wherein a compound as described herein is administered in a therapeutically effective amount.

Benzamide derivatives as thyroid receptor ligands

New thyroid receptor ligands are provided which have general formula (I) in which: n is an integer from 0 to 4; Ris halogen, trifluoromethyl, or alkyl of 1 to 6 carbons or cycloalkyl of 3 to 7 carbons; Rand Rare the same or different and are hydrogen, halogen, alkyl of 1 to 4 carbons or cycloalkyl of 3 to 5 carbons, at least one of Rand Rbeing other than hydrogen; Ris a carboxylic acid amide (CONR'R&#x2033;) or an acylsulphonamide (CONHSO2R&#x2032;) derivative, or a pharmaceutically acceptable salt thereof, and all stereoisomers thereof; or when n is equal to or greater than one, Rmay be a heteroaromatic moiety which may be substituted or unsubstituted, or an amine (NR&#x2032;R&#x2033;). Ris hydrogen or an acyl (such as acetyl or benzoyl) or other group capable of bioconversion to generate the free phenol structure (wherein R=H). In addition, a method is provided for preventing, inhibiting or treating a disease associated with metabolism dysfunction or which is dependent upon the expression of a Tregulated gene, wherein a compound as described above is administered in a therapeutically effective amount. Examples of such diseases associated with metabolism dysfunction or are dependent upon the expression of a Tregulated gene include obesity, hypercholesterolemia, atherosclerosis, cardiac arrhythmias, depression, osteoporosis, hypothyroidism, goiter, thyroid cancer as well as glaucoma, congestive heart failure and skin disorders.

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Tumba, Sweden

Neeraj Garg