111results about How to "Ease of preparation and detectability" patented technology

The invention relates to new therapeutically active and selective inhibitors of the enzyme dipeptidyl peptidase-IV, pharmaceutical compositions comprising the compounds and the use of such compounds for treating diseases that are associated with proteins that are subject to processing by DPP-IV, such as Type 2 diabetes mellitus, hyperglycemia, impaired glucose tolerance, metabolic syndrome (Syndrome X or insulin resistance syndrome), glucosuria, metabolic acidosis, cataracts, diabetic neuropathy, diabetic nephropathy, diabetic retinopathy, diabetic cardiomyopathy, Type 1 diabetes, obesity, conditions exacerbated by obesity, hypertension, hyperlipidemia, atherosclerosis, osteoporosis, osteopenia, frailty, bone loss, bone fracture, acute coronary syndrome, infertility due to polycystic ovary syndrome, short bowel syndrome, anxiety, depression, insomnia, chronic fatigue, epilepsy, eating disorders, chronic pain, alcohol addiction, diseases associated with intestinal motility, ulcers, irritable bowel syndrome, inflammatory bowel syndrome and to prevent disease progression in Type 2 diabetes. The invention also relates to a method of identifying an insulin secretagogue agent for diabetes.

The present invention relates to methods for treating cancer comprising utilizing a combination of signal transduction inhibitors. More specifically, the present invention relates to combinations of so called cell cycle inhibitors with mitogen stimulated kinase signal transduction inhibitors, more specifically combinations of CDK inhibitors with mitogen stimulated kinase signal transduction inhibitors, more preferably MEK inhibitors. Other embodiments of the invention relate to additional combinations of the aforesaid combinations with standard anti-cancer agents such as cytotoxic agents, palliatives and antiangiogenics. Most specifically this invention relates to combinations of 6-acetyl-8-cyclopentyl-5-methyl-2-(5-piperazin-1-yl-pyridin-2-ylamino)-8H-pyrido[2,3-d]pyrimidin-7-one including salt forms, which is a selective cyclin-dependent kinase 4 (CDK4) inhibitor, in combination with one or more MEK inhibitors, most preferably N-[(R)-2,3-dihydroxy-propoxy]-3,4-difluoro-2-(2-fluoro-4-iodo-phenylamino)-benzamide. The aforementioned combinations are useful for treating inflammation and cell proliferative diseases such as cancer and restenosis.

Alpha substituted carboxylic acids of formula (I):

wherein R¹ and R² are as defined in the specification and R³ is

wherein Y, Ar¹, Ar², Ar³, R⁴, R⁵, R⁶, R⁷, R⁸, R⁹, R^9a, R¹⁰, R¹¹, R¹², R¹⁷, ring A, and p are as defined in the specification; pharmaceutical compositions containing effective amounts of said compounds or their salts are useful for treating PPAR, specifically PPAR α/γ related disorders, such as diabetes, dyslipidemia, obesity and inflammatory disorders.

Alpha substituted carboxylic acids of formula (I):

wherein R¹ and R² are as defined in the specification and R³ is

wherein Y, Ar¹, Ar², Ar³, R⁴, R⁵, R⁶, R⁷, R⁸, R⁹, R^9a, R¹⁰, R¹¹, R¹², R¹⁷, ring A, and p are as defined in the specification; pharmaceutical compositions containing effective amounts of said compounds or their salts are useful for treating PPAR, specifically PPAR α/γ related disorders, such as diabetes, dyslipidemia, obesity and inflammatory disorders.

The present invention provides substituted 2-aminopyridines of formula I, wherein R1, A1, W, X, and Y are as defined in the specification, useful in treating cell proliferative disorders. The novel compounds of the present invention are potent inhibitors of cyclin-dependent kinases 4 (Cdk4).

The present invention relates to a compound of formula (I):

or a pharmaceutically acceptable salt or solvate thereof, wherein:

• • Ring A is (4-12)-membered heterocyclyl;
  • Ring B is a fused benzene ring selected from the group consisting of:

The present invention relates to the use of a compound of formula I wherein R2 is R-NH wherein R is a branched or unbranched alkyl radical, a piperidinyl group or pyrrolidinyl group, each of which may be optionally substituted by one or more -OH, halogen, amino or hydroxyalkyl groups; R6 is phenylamino, benzylamino or pyridyl-methylamino, indan-5-amino, where in each case the aryl group may be unsubstituted or substituted by one or more -OR'', halogen, NO2, amino or COOR' groups, wherein R' and R'' are each independently H or a branched or unbranched alkyl group; and R9 is a branched or unbranched alkyl group or a cycloalkyl group; in the treatment of an autoimmune disorder. The invention further relates to a method of treating an autoimmune disorder comprising administering to a subject in need thereof a therapeutically effective amount of a compound of formula I.

The present invention relates to a method of treating disorders of the central nervous system (CNS) and other disorders in a mammal, including a human, by administering to the mammal a CNS-penetrant α7 nicotinic receptor agonist. It also relates to pharmaceutical compositions containing a pharmaceutically acceptable carrier and a CNS-penetrant α7 nicotinic receptor agonist.

The invention relates to compounds of the formula 1

• [0001]
  • or a pharmaceutically acceptable salt, prodrug or hydrates thereof, wherein X, L, R¹, R², R³ and R⁴ are as defined herein. The invention also relates to pharmaceutical compositions containing the compounds of formula 1 and to methods of treating hyperproliferative disorders in a mammal by administering the compounds of formula 1.

A compound of formula I, or a pharmaceutically acceptable salt or ester thereof,

Further aspects relate to pharmaceutical compositions, therapeutic uses and process for preparing compounds of formula I.

Compounds, tautomers and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula I,

as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.

The present invention relates to 1,3-disubstituted-1H-pyrazolo[3,4-d]pyrimidin-4-amine derivatives, 5,7-disubstituted-pyrrolo[2,1-f][1,2,4]triazin-4-amine derivatives or 5,7-disubstituted-imidazo[5,1-f][1,2,4]triazine-4-amine derivatives, and pharmaceutically acceptable salts thereof. The compounds are potentiators of Cystic Fibrosis Transmembrane conductance Regulator (CFTR). The invention also discloses pharmaceutical compositions comprising the compounds, optionally in combination with additional therapeutic agents, and methods of potentiating, in mammals, including humans, CFTR by administration of the compounds. These compounds are useful for the treatment of cystic fibrosis (CF), asthma, bronchiectasis, chronic obstructive pulmonary disease (COPD), constipation, Diabetes mellitus, dry eye disease, pancreatitis, rhinosinusitis, Sjôgren's Syndrome, and other CFTR associated disorders.

Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula (I) as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.

Novel compounds according to the formula

• • and pharmaceutically acceptable salts, solvates, or hydrates thereof; wherein
  • each occurrence of A is independently selected from CH or N;
  • X is selected from the group consisting of —CH₂—, —O—, —NH—, (C₁-C₆)alkylamino-, (C₁-C₆)alkylaminocarbonylamino-, (C₁-C₆)alkylcarbonylamino-, (C₁-C₆)alkylsulfonylamino-, phenylsulfonylamino-, carbonyl, —NH—C(O)—, —N(C₁-C₆)alkyl-C(O)—, —S(O)_y— where y is 0, 1 or 2, and;
  • n in —(CH₂)_n— is 1, 2 or 3; and
  • R¹, R², and R³ are as described herein; pharmaceutical compositions that including these compounds, and methods for the treatment of autoimmune disease, inflammation, allergy, transplant rejection, and other circumstances where administration of an immunosuppressive agent is of therapeutic benefit.