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2-substituted-1-piperidyl benzimidazole compounds as ORL1-receptor agonists

InactiveUS6172067B1Ease of presentationEase of detectabilityBiocideNervous disorderArylMedicinal chemistry

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.

2-substituted-1-piperidyl benzimidazole compounds as ORL1-receptor agonists

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Owner:PFIZER PHAMACEUTICALS INC

N-substituted spiropiperidine compounds as ligands for ORL-1 receptor

InactiveUS20030158219A1Easy to prepareEase of detectabilityBiocideNervous disorderHydrogenQuinoline

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.

N-substituted spiropiperidine compounds as ligands for ORL-1 receptor

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Owner:PFIZER INC

Pyrrolopyrimidine derivatives

InactiveUS20050037999A1Avoid problemsEase of detectabilityBiocideOrganic active ingredientsPyrroleProdrug

The invention relates to compounds of the formula 1 or a pharmaceutically acceptable salt, prodrug or hydrates thereof, wherein Q, A, L, R1, R2 and R3 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.

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Owner:PFIZER INC

Somatostatin antagonists and agonists that act at the sst subtype 2 receptor

InactiveUS20020128206A1Ease of detectabilityEasy to prepareDipeptide ingredientsMetabolism disorderArylMammal

Compounds according to the formula: 1 and pharmaceutically acceptable salts, solvates or hydrates thereof, wherein group Ar is optionally substituted (C.sub.6-C.sub.10)aryl or (C.sub.1-C.sub.9)heteroaryl; X is a direct link, --CH.sub.2 --, --SO.sub.2 --, --CO--, --CHR.sup.1-- where R.sup.1 is(C.sub.1-C.sub.6) alkyl, or --CR.sup.1'R.sup.1"-where both R.sup.1' and R.sup.1" are, independently, (C.sub.1-C.sub.6)alkyl; Y is N or CH; and Z and W are as herein defined, and pharmaceutical compositions thereof, and methods useful to facilitate secretion of growth hormone(GH) in mammals.

Somatostatin antagonists and agonists that act at the sst subtype 2 receptor

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Owner:HAY BRUCE A +2

2-benzimidazolylamine compounds as ORL-1-receptor agonists

InactiveUS6340681B1Ease of presentationEase of detectabilityAntibacterial agentsBiocideAgonistMedicinal chemistry

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.

2-benzimidazolylamine compounds as ORL-1-receptor agonists

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Owner:PFIZER PHAMACEUTICALS INC

Pyrrolopyre compounds useful in treatment of cancer

InactiveUS20050130994A1Ease of detectabilityEasy to prepareBiocideOrganic active ingredientsDiseaseChemical compound

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.

Pyrrolopyre compounds useful in treatment of cancer

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Owner:PFIZER INC

Benzimidazole derivatives

InactiveUS20100029615A1Ease of detectabilityEasy to prepareBiocideOrganic chemistryBenzimidazole derivativeAbnormal cell

The present invention relates to a compound of the formula (I) or a pharmaceutically acceptable salt thereof, wherein R1, 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.

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Owner:PFIZER INC

Integrin antagonists useful as anticancer agents

InactiveUS20060116383A1Ease of detectabilityEasy to prepareBiocideOrganic chemistryDiseaseIntegrin antagonist

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.

Integrin antagonists useful as anticancer agents

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Owner:ALCATEL LUCENT SAS

Alkyl-Substituted Hexahydropyrano[3,4-d][1,3]Thiazin-2-Amine Compounds

InactiveUS20150239908A1Ease of detectabilityEasy to prepareNervous disorderOrganic chemistryTautomerAlkyl

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.

Alkyl-Substituted Hexahydropyrano[3,4-d][1,3]Thiazin-2-Amine Compounds

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Owner:PFIZER INC

2-Substituted-1-piperidyl benzimidazole compounds as ORL1-receptor agonists

InactiveUS20030109549A1Ease of detectabilityEase of presentationBiocideAnimal repellantsArylMedicinal chemistry

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.

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Owner:ITO FUMITAKA +2

Benzimidazole compounds as ORL1-receptor agonists

InactiveUS20020049212A1Ease of detectabilityEase of presentationBiocideSenses disorderArylPharmaceutical medicine

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.

Benzimidazole compounds as ORL1-receptor agonists

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Owner:PFIZER INC +1

2-(Pyridin-2-ylamino)-pyrido [2,3-D]pyrimidin-7-ones

InactiveUS20050137214A1Ease of detectabilityEasy to prepareBiocideOrganic active ingredientsBiochemistryCyclin

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).

2-(Pyridin-2-ylamino)-pyrido [2,3-D]pyrimidin-7-ones

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Owner:WARNER-LAMBERT CO

Novel Lactams as Beta Secretase Inhibitors

InactiveUS20110224231A1Ease of detectabilityEasy to prepareBiocideSenses disorderΒ secretaseLactam

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 Lactams as Beta Secretase Inhibitors

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Owner:PFIZER INC

Imidazopyrazines as protein kinase inhibitors

InactiveUS7511040B2Ease of detectabilityEasy to prepareBiocideOrganic chemistryDiseasePTK Inhibitors

In its many embodiments, the present invention provides a novel class of imidazopyrazine compounds as inhibitors of protein and / or Aurora kinases, methods of preparing such compounds, pharmaceutical compositions including one or more such compounds, methods of preparing pharmaceutical formulations including one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the protein or Aurora kinases using such compounds or pharmaceutical compositions. An illustrative compound of the invention is shown below:

Imidazopyrazines as protein kinase inhibitors

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Owner:SCHERING CORP

Inhibitors of pi3 kinase

ActiveUS20130053371A1Ease of detectabilityEasy to prepareBiocideNervous disorderLipid kinasesPI3-Kinase Inhibitors

There is provided compounds of formula (I), wherein A1, A4, A4a, A5, B1, B1a, B2, B2a, B3, B3a, B4, B4a 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.

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Owner:FUNDACION CENT NACIONAL DE INVESTIGACIONES ONCOLOGICAS CARLOS III

Quinolone compound and pharmaceutical composition

ActiveUS20110269705A1Effective in treatment and preventionImprove mitochondrial functionBiocideSenses disorderNeurological dysfunctionQuinolone

The present invention provides a quinolone compound that inhibits the chronic progression of Parkinson's disease or protects dopamine neurons from disease etiology, thereby suppressing the progression of neurological dysfunction, so as to prolong the period of time until L-dopa is administered while also improving neuronal function; the quinolone compound of the invention is represented by Formula (1):wherein:R1 represents hydrogen or the like;R2 represents hydrogen or the like;R3 represents substituted or unsubstituted phenyl or the like;R4 represents halogen or the like;R5 represents hydrogen or the like;R6 represents hydrogen or the like; andR7 represents hydrogen or the like.

Quinolone compound and pharmaceutical composition

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Owner:OTSUKA PHARM CO LTD

Methods, compounds, and compositions for inhibition of ROS

ActiveUS9963452B2Promotes stability and dispersibilityEase of detectabilityOrganic chemistryAntineoplastic agentsTyrosineCell growth

The present invention relates to a method using some novel compounds and compositions for the inhibition of ROS tyrosine kinase. In particular, the present invention covers a method to treat abnormal cell growth, such as cancer, with ROS 10 inhibitors and compositions having ROS inhibitors. An illustrative compound of the invention is shown below Formula (I).

Owner:GRUENEBERG DORRE A

Imidazo [2, 1-B] [1, 3, 4] Thiadiazole Derivatives

ActiveUS20120094996A1Ease of detectabilityEasy to prepareBiocideNervous disorderDiseaseLipid kinases

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.

Imidazo [2, 1-B] [1, 3, 4] Thiadiazole Derivatives

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Owner:FUNDACION CENT NACIONAL DE INVESTIGACIONES ONCOLOGICAS CARLOS III

Bicyclic [3.1.0] derivatives as glycine transporter inhibitors

ActiveUS20050096375A1Easy to prepareGood metabolic stabilityBiocideNervous disorderMedicinal chemistryGlycine transporter

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.

Bicyclic [3.1.0] derivatives as glycine transporter inhibitors

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Owner:PFIZER INC +1

NOVEL 3,4-DISUBSTITUTED-1H-PYRROLO[2,3-b]PYRIDINES AND 4,5-DISUBSTITUTED-7H-PYRROLO[2,3-c]PYRIDAZINES AS LRRK2 INHIBITORS

ActiveUS20170002000A1Ease of detectabilityEasy to prepareNervous disorderOrganic chemistryLeprosyCrohn's disease

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 thereofwherein 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.

NOVEL 3,4-DISUBSTITUTED-1H-PYRROLO[2,3-b]PYRIDINES AND 4,5-DISUBSTITUTED-7H-PYRROLO[2,3-c]PYRIDAZINES AS LRRK2 INHIBITORS

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Owner:PFIZER INC

Pyridylamino compounds and methods of use thereof

InactiveUS20050080100A1Ease of detectabilityEasy to prepareBiocideGroup 5/15 element organic compoundsNegative symptomPyridine

This invention relates to a series of pyridylamino compounds of the formula I wherein Z1, Z2, W, X, Y and R1 are defined as in the specification, that exhibit activity as glycine transport inhibitors, their pharmaceutically acceptable salts, pharmaceutical compositions containing them, 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.

Pyridylamino compounds and methods of use thereof

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Owner:PFIZER INC

Spiropiperidine compounds as ligands for ORL-1receptor

InactiveUS20030078279A1Ease of detectabilityEase of presentationBiocideNervous disorderPreventing painBenzofuran

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.

Spiropiperidine compounds as ligands for ORL-1receptor

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Owner:PFIZER INC

Novel Heteroaryl Imidazoles And Heteroaryl Triazoles As Gamma-Secretase Modulators

InactiveUS20120202787A1Ease of detectabilityEasy to prepareBiocideSenses disorderGamma secretaseStereochemistry

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 Heteroaryl Imidazoles And Heteroaryl Triazoles As Gamma-Secretase Modulators

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Owner:PFIZER INC

Cycloalkylene amide compounds as NR2B receptor antagonists

InactiveUS20040152715A1Potent binding activityReduced inhibitory activityBiocideSenses disorderDiseaseAryl

This invention provides a compound of the formula (I): wherein R<1 >represents wherein R<5 >represents a hydroxy group or the like; R<6 >and R<7 >independently represents a hydrogen atom or the like: V represents an alkylene or the like: W represents a carbon atom or the like: Z represents a carbon or the like: R<2 >represents a hydrogen atom or the like: R<3 >represents a hydrogen or the like: A represents a cycloalkylene or the like: X represents a covalent bond or the like: R<4 >represents an aryl or the like. These compounds are useful for the treatment of disease conditions caused by overactivation of NMDA NR2B receptor such of pain, or the like in mammalian. This invention also provides a pharmaceutical composition comprising the above compound.