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7592350 |
Polycyclic compounds as potent alpha2-adrenoceptor antagonists
A compound of formula I,
wherein X, Z, R 1 to R 10 , R 15 , R 16 , m, n, r and t are as defined in claim 1, or a pharmaceutically acceptable salt or ester thereof, useful as an alpha-2...
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7541463 |
Sulfur-containing naphthalimide derivatives
The invention discloses novel sulfur-containing naphthalimide derivatives, and the preparation and uses thereof. The conjugated plane of naphthalimide derivatives of the invention is enlarged by...
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7541346 |
Pancratistatin cyclic phosphate prodrugs and phenpanstatin cyclic phosphate prodrugs
Selective phosphorylation of phenpanstatin (3a) with tetrabutylammonium dihydrogen phosphate and dicyclohexylcarbodiimide in pyridine followed by cation exchange chromatographic procedures was...
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7531550 |
Pseudobase benzo[c]phenanthridines with improved efficacy, stability, and safety
Pseudobase benzo[c]phenanthridines and the pharmaceutically acceptable salts thereof of Formula I
are provided herein. The variables R, R 1 , R 2 , R 3 , and R 4 are defined herein. Certain...
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7517883 |
Solubilized topoisomerase poisons
The invention provides compounds of formula I:
wherein
A, B, W, Y, Z, and R 1 have any of the meanings defined in the specification and their pharmaceutically acceptable salts. The invention...
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7470703 |
Yohimbine derivatives and use thereof
Yohimbine derivatives are disclosed having modification of the C-16 carboxyl group to include a sidechain and where the resulting derivative does not possess a second yohimbine pharmacophore (i.e.,...
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7387790 |
Pharmaceutical and diagnostic compositions containing nanoparticles useful for treating targeted tissues and cells
Nanoparticles made from a select group of lipids and optionally containing a therapeutically active agent are employed in pharmaceutical compositions for delivery to targeted tissues and/or cells...
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7323449 |
Thionucleoside derivatives as inhibitors of RNA-dependent RNA viral polymerase
The present invention provides thionucleoside compounds and certain derivatives thereof which are inhibitors of RNA-dependent RNA viral polymerase. These compounds are inhibitors of RNA-dependent...
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7319105 |
Cytotoxic agents
The invention provides compounds of the invention pharmaceutical compositions comprising a compound of the invention, processes for preparing compounds of the invention, intermediates useful for...
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7312228 |
Cytotoxic indeno and isoindoloisoquinolones
The synthesis and biological activity of benzoisoindoloisoquinolone compounds are described. The synthesis and biological activity of C-11-substituted indenoisoquinolones are also described....
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7276512 |
Benzo[a]pyrano[3,2-h]acridin-7-one compounds
A compound selected from those of formula (I):
wherein:
X and Y represent a group selected from hydrogen, halogen, hydroxy, alkoxy, nitro, cyano, alkyl, trihaloalkyl and NR a R b ,...
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7232830 |
Method for treatment of neurodegenerative diseases and effects of aging
A method for treatment of neurodegenerative disease conditions stemming from multiple sclerosis, aging, autoimmune diseases and fibromyalgia. A compound effective to increase neuronal metabolism of...
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7201913 |
Oral formulations for anti-tumor compounds
The present invention relates to a semi-solid filling medium which comprises a camptothecin derivative; a pharmaceutically acceptable carrier matrix which is a polyglycolized glyceride; and an...
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7199130 |
Substituted 5,6,6a, 11b-tetrahydro-7-oxa-5-aza-benzo[c]fluorene-6-carboxylic acid compounds as NMDA-antagonists
Substituted 5,6,6a,11b-tetrahydro-7-oxa-5-aza-benzo[c]fluorene-6-carboxy
lic acid compounds, and processes for the production thereof, pharmaceutical compositions containing these compounds and the...
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7173041 |
Polyglutamic acid-camptothecin conjugates and methods of preparation
The invention provides polyglutamic acid-therapeutic agent conjugates and methods for their preparation and use.
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7153864 |
Polyglutamic acid-camptothecin conjugates and methods of preparation
The invention provides polyglutamic acid-therapeutic agent conjugates and methods for their preparation and use.
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7151108 |
[3,4-a:3,4-c]carbazole compounds
A compound selected from those of formula (I):
wherein:
W 1 represents, together with carbon to which it is bonded, phenyl, pyridyl, Z represents a group of formula U—V as defined in...
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7144891 |
Benzo[b ]pyrano[3,2- h ]acridin-7-one cinnamate compounds
A compound selected from those of formula (I):
wherein:
X and Y represent a group selected from hydrogen, halogen, alkoxy, nitro, cyano, alkyl, alkenyl, polyhaloalkyl and —NR a R b ...
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7125873 |
Beta-amino tetrahydroimidazo (1, 2-a) pyrazines and tetrahydrotrioazolo (4, 3-a) pyrazines as dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes
The present invention is directed to compounds which are inhibitors of the dipeptidyl peptidase-IV enzyme (“DP-IV inhibitors”) and which are useful in the treatment or prevention of diseases in...
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7115619 |
N8, N13 -disubstituted quino[4,3,2-kl]acridinium salts as therapeutic agents
The present invention pertains to certain N 8 ,N 13 -disubstituted quino[4,3,2-kl]acridinium salts of formula (Q − ) which inhibit telomerase wherein: p is an integer from 0 to 4; q is an integer...
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7105492 |
Camptothecin derivatives having antitumor activity
Camptothecin derivatives of camptothecin of formula (I)
exhibit antitumor activity and show a good therapeutic index and are used in the treatment of tumors, viral infections and antiplasmodium...
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6992089 |
Nitro and amino substituted topoisomerase agents
The invention provides compounds of formula I:
wherein R 1 -R 9 , W, and X have any of the meanings defined in the specification and their pharmaceutically acceptable salts. The invention also...
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6992088 |
Nitro and amino substituted heterocycles as topoisomerase I targeting agents
The invention provides compounds of formula I:
wherein: R 1 -R 5 , “a” and X have any of the meanings defined in the specification and their pharmaceutically acceptable salts. The...
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6987109 |
Solubilized topoisomerase poison agents
The invention provides compounds of formula I:
wherein
A, B, W, Y, Z, and R 1 have any of the meanings defined in the specification and their pharmaceutically acceptable salts. The...
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6967215 |
Tetrahydrocarbazoles, a process for the preparation of those compounds, and the use thereof
Tetrahydrocarbazoles of formula
where Q is —SO 2 —; —O—; or —(CO)—; X is —(CH)—; or —N—; m is from 1 to 3; t is 0 or 1 and the remaining substituents are as defined herein,...
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6964964 |
Topoisomerase poison agents
The invention provides compounds of formula I:
wherein
A, B, W, Y, Z, R 1 , R 3 and R 4 have any of the meanings defined in the specification and their pharmaceutically acceptable...
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6946472 |
Polycyclic compounds exhibiting anti-tumor activities
This invention is concerned with novel polycyclic compounds of formula [I],
wherein ring A, ring B, R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , X, Y, R 1′ , R 2′ , R 3′ , R 4′ , R 5′ , R 6...
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6893668 |
Process for isolation of anticancer agent camptothecin from Nothapodytes foetida
The present invention relates to an improved and economical process for the isolation of anticancer agent Camptothecin from the twigs and stem of Nothapodytes foetida using hot extraction 20(S)...
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6878737 |
Reversal of multidrug resistance in human colon carcinoma cells
The present invention describes the use of fumitremorgin A, B and C and a series of diketopiperazines of Formula (I) to resensitize multidrug resistant (MDR) cancer cells to the cytotoxic effects...
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6875439 |
Formulation containing amphipathic weak base and/or amphipathic cation and multiple drug resistance inhibitor
Methods are provided relating to the enhanced cytoplasmic accumulation of amphipathic weakly basic or amphipathic cationic molecules in prokaryotes and eukaryotes under conditions of high...
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6844353 |
Fungicidal properties of sampangine and its analogs to agriculturally important fungal plant pathogens
It has been found that sampangine and related analogs such as benzo[4,5]sampangine, 4-bromosampangine and 4-methoxysampangine may be used as effective fungicidal agents for plants. Fungicidal plant...
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6740659 |
Treatment of dyskinesia
The invention relates to the use of compounds which inhibit selectively mu opioid receptor activity, or activation, for the treatment of dyskinesia (which, for example, may arise as a side effect...
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6706704 |
Method of inducing opioid analgesia and anesthesia without respiratory suppression
The invention is directed to a pharmaceutical composition and a corresponding method for inhibiting respiratory depression in a mammalian subject during treatment with opiates. The composition...
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6699676 |
Uses of ouabain and ouabain-like molecules in apoptosis related pathologies
Longterm elevation of the intracellular Na + /K + ratio inhibits macromolecule synthesis and proliferation in the majority of cell types studied so far, including vascular smooth muscle cells...
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6686388 |
Regulators of the hedgehog pathway, compositions and uses related thereto
The present invention makes available methods and reagents for inhibiting aberrant growth states resulting from hedgehog gain-of-function, ptc loss-of-function or smoothened gain-of-function...
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6680326 |
Polycyclic compounds
Novel polycyclic compounds of the formula [I], wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , ring A, ring B, X, Y and Z are as defined herein and the pharmaceutically acceptable salts...
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6656948 |
Cytotoxic compounds: derivatives of the pyrido&lsqb 2,3,4-kl&rsqb acridine ring system
Compounds of the following formula: wherein all variables are as defined in the specification. The compounds have cytotoxic properties and can therefore be used in the treatment of malignant...
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6645975 |
Process for the preparation of dinaposoline
The present invention relates to a novel process for the preparation of compounds of the formula wherein R 1 , R 2 , R 4 , R 5 , R 6 and A are as defined herein, and to certain derivations of...
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6642248 |
Benzo&lsqb b&rsqb pyrano&lsqb 3,2-h&rsqb acridin-7-one compounds
A compound selected from those of formula (I): wherein: X and Y represent group selected from hydrogen, halogen, mercapto, cyano, nitro, alkyl, trihaloalkyl, trihaloalkylcarbonylamino, —ORa,...
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6638943 |
Yohimbine dimers exhibiting binding selectivities for α2 adrenergic receptors
The present invention relates to yohimbine dimer compounds, pharmaceutical compositions containing such dimer compounds, methods of making such dimer compounds, and uses thereof. The yohimbine...
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6632822 |
Compounds and therapeutic methods
The present invention relates to indolo[3,2-j]phenanthridine compounds and their use in the treatment of cancer and other diseases of humans and animals including parasitic diseases such as those...
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6608073 |
Intranasal codeine for the rapid suppression of cough and rapid relief of pain
This invention provides a method of rapidly and reliably delivering codeine, alone or in combination with other compounds, to the systemic circulation by administration via the nasal route to...
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6589939 |
Camptothecin derivatives having antitumor activity
Camptothecin derivatives of camptothecin of formula (I): wherein the groups R 1 , R 2 and R 3 are as defined in the description are disclosed. The compounds of formula (I) are endowed with...
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6583150 |
Pharmaceutical composition based on polyaromatic compounds
A pharmaceutical composition comprising an efficient amount of a compound selected among the compounds of formulae (I) and (II). The compounds have useful cytotoxic properties providing therapeutic...
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6548515 |
Dihydrofuro&lsqb 3,4-b&rsqb quinolin-1-one compounds
The invention relates to compound of formula (I): wherein: represents a single or double bond, R 0 represents hydrogen or hydroxy or alkoxy, R 1 and R 2 , which are identical or different,...
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6538008 |
Combination of a selective NMDA NR2B antagonist and an opioid analgesic
A combination of a selective NMDA NR2B antagonist and an opioid analgesic is useful in the treatment of pain or nociception.
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6528519 |
Use of tetrandrine and its derivatives to treat malaria
The specification discloses the treatment of malaria through the use of tetrandrine and its derivatives.
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6514934 |
Imidazoline α-adrenergic receptor antagonist compounds in combination with nitric oxide donors, compositions and methods of use
The present invention is directed to nitrosated or nitrosylated α-adrenergic receptor antagonists, compositions comprising α-adrenergic receptor antagonists that are optionally substituted with...
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6511986 |
Method of treating estrogen receptor positive carcinoma
This invention provides a method of treating or inhibiting an estrogen receptor positive carcinoma in a mammal in need thereof, which comprises providing said mammal with an effective amount of a...
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6509344 |
Indenoisoquinolines as antineoplastic agents
A number of indenoisoquinolines were prepared and evaluated for cytotoxicity in human cancer cell cultures and for activity versus topoisomerase I. The two most cytotoxic indenoisoquinolines proved...
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