43results about How to "Ease of detectability" patented technology

A compound of the formula:or a pharmaceutically acceptable salt thereof, wherein R is unsubstituted, mono-, di- or tri-substituted (C3-C11)cycloalkyl or (C3-C11)cycloalkenyl or the like, A is unsubstituted (C1-C7)alkyl or (C2-C5 )alkenyl, or unsubstituted, mono-, di- or tri-substituted aryl, or aromatic-heterocyclic or the like, Y is hydrogen, halo, amino or mercapto, or unsubstituted, mono-, di- or tri- substituted (C1-C10)alkyl-M-, (C3-C7)cycloalkyl-M-, (C2-C6)alkenyl-M-, (C1-C4)alkyl-NH-((C1-C4)alkyl)-M-, di(C1-C4)alkyl-N-((C1-C4)alkyl)-M-, aryl-M-, aromatic or non-aromatic heterocyclic-M-, aryl-(C1-C5)alkyl-M- or aromatic non-aromatic heterocyclic-(C1-C5)alkyl-M-, wherein M is a covalent bond O, S, NH or the like, or the like; Z1, Z2, Z3 and Z4 are hydrogen or the like, has ORL1-receptor agonist activity, and are useful as analgesics or the like in mammalian subjects.

A compound of the formula: or a pharmaceutically acceptable salt, ester or ether thereof, wherein R1 through R12 are independently hydrogen or the like; X1 and X2 are independently CH2 or the like; R13 is hydrogen or the like; or R12 and R13 taken together with three ring atoms of the quinoline ring separating said substituents form a heterocyclic ring; R14 and R15 are hydrogen or the like or these groups taken together form oxo; and the dotted line represents a single or double bond. These compounds are ligands for ORL-1 receptor and especially are antagonists for said receptor.

A compound of the formula:or a pharmaceutically acceptable salt thereof, whereinR1 and R2 are independently selected from hydrogen, halo, hydroxy, (C1-C4)alkyl, halo (C1-C4)alkyl and the like; R3 and R4 are independently selected from hydrogen, halo(C1-C10)alkyl, optionally substituted (C1-C6)alkyl and the like, or R3 and R4, together with the nitrogen atom to which they are attached, form an optionally substituted fully saturated, partially saturated or fully unsaturated heterocyclic ring; and R5 is (C4-C11)cycloalkyl and the like, has ORL1-receptor agonist activity, and are useful as analgesics or the like in mammalian subjects.

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.

The present invention relates to a compound of the formula (I) or a pharmaceutically acceptable salt thereof, wherein R^1, R², R³, R⁴, R⁵, A, X, n, and are as defined herein. Such novel benzamidazole derivatives are useful in trv treatment of abnormal cell growth, such as cancer, in mammals. This invention ate relates to a method of using such compounds in the treatment of abnormal cell growth in mammals, especially humans, and to pharmaceutical compositions containing sue compounds.

The invention relates to compounds of the Formula 1

and to pharmaceutically acceptable salts and solvates thereof, wherein A, X², X⁴, X⁵ and X¹ are as defined herein. The invention also relates to methods of treating abnormal cell growth in mammals by administering the compounds of Formula 1 and to pharmaceutical compositions for treating such disorders which contain the compounds of Formula 1.

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.

A compound of the formula: or a pharmaceutically acceptable salt thereof, wherein R1 is unsubstituted, mono-, di- or tri-substituted (C3-C11)cycloalkyl or (C3-C11)cycloalkenyl or the like, A is unsubstituted (C1-C7)alkyl or (C2-C5)alkenyl, hydroxy-(C1-C4)alkyl, (C1-C4)alkoxy-(C=O), or unsubstituted, mono-, di- or tri- substituted aryl, or aromatic-heterocyclic or the like, M is a covalent bond O, S, NH or the like, Y is 4- to 12-membered bicyclic-carbocyclic rings or 4- to 12-membered bicyclic-heterocyclic rings, or 5- to 17 membered spirocarbocyclic rings or 5- to 17-membered spiroheterocyclic rings or the like, Z1, Z2, Z3 and Z4 are hydrogen or the like, is disclosed. These compounds have ORL1-receptor agonist activity, and are thus useful as analgesics or the like in mammalian subjects.

The present invention provides substituted 2-aminopyridines useful in treating cell proliferative disorders. The novel compounds of the present invention are potent inhibitors of cyclin-dependent kinases 4 (cdk4).

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.

There is provided compounds of formula (I), wherein A₁, A₄, A_4a, A₅, B¹, B^1a, B², B^2a, B³, B^3a, B⁴, B^4a and R³ have meanings given in the description, and pharmaceutically-acceptable esters, amides, solvates or salts thereof, which compounds are useful in the treatment of diseases in which inhibition of a protein or lipid kinase (e.g. a PI3-K and/or mTOR) is desired and/or required, and particularly in the treatment of cancer or a proliferative disease.

There is provided compounds of formula (I): wherein R¹, R² and R³ have meanings given in the description, and pharmaceutically-acceptable esters, amides, solvates or salts thereof, which compounds are useful in the treatment of diseases in which inhibition of a protein or lipid kinase (e.g. PI3-K, particularly class I PI3K) is desired and/or required, and particularly in the treatment of cancer.

The present invention relates to a series of substituted bicyclic[3.1.0]amines of the Formula I:

wherein A, B, D, Q, V, W, X, Y, Z, R², R³, R⁴, R⁵, R¹⁴, R¹⁵, R³⁰. o, p, s,t and q are as defined in the specification, their pharmaceutically acceptable salts, pharmaceutical compositions thereof, and their use for the enhancement of cognition and the treatment of the positive and negative symptoms of schizophrenia and other psychoses in mammals, including humans.

The present invention provides novel 3,4-disubstituted-1H-pyrrolo[2,3-b]pyridine derivatives and 4,5-disubstituted-7H-pyrrolo[2,3-c]pyridazine derivatives of Formula I, and the pharmaceutically acceptable salts thereof

wherein R¹, R², R³, R⁴ and X are as defined in the specification. The invention is also directed to pharmaceutical compositions comprising the compounds of formula I and to use of the compounds in the treatment of diseases associated with LRRK2, such as neurodegenerative diseases including Parkinson's disease or Alzheimer's disease, cancer, Crohn's disease or leprosy.

A compound of the formula: or a salt, prodrug or solvate thereof, wherein R1 and R2 groups are all hydrogen; A is a benzofuzed azahetero ring; W1-W2 is CH2-CH2; X1-X2 is CH2-CH2; and Z is methylene or carbonyl; or the like, is a ligand for ORL1-receptor and are useful for treating or preventing pain, a CNS disorder or the like in mammalian subjects.

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.

There is provided compounds of formula (I), wherein A¹, A², A³, A⁴, n, the dotted lines, B¹, B^1a, B², B^2a, B³, B^3a, B⁴, B^4a, R² and R³ have meanings given in the description, and pharmaceutically-acceptable esters, amides, solvates or salts thereof, which compounds are useful in the treatment of diseases in which inhibition of a protein kinase (e.g. a PI3-K and/or mTOR) is desired and/or required, and particularly in the treatment of cancer or a proliferative disease.

The present invention relates to the following compounds

wherein the integers are as defined in the description, and where the compounds may be useful as medicaments, for instance for use in the treatment of tuberculosis.