Abstract: The invention provides quinazoline compounds that are inhibitors of PDK1. Also provided are pharmaceutical compositions including the compounds, and methods of treating proliferative diseases, such as cancers, with the compounds or compositions.

Abstract: Disclosed are a pharmaceutical composition having excellent antitumor activity, and a method for treating a cancer. Specifically, excellent antitumor activity is achieved when 4-(3-chloro-4-(cyclopropylaminocarbonyl)aminophenoxy)-7-methoxy-6-quinolinecarboxamide or an analogous compound thereof, a pharmacologically acceptable salt thereof or a solvate thereof is used in combination with gemcitabine or erlotinib, a pharmacologically acceptable salt thereof or a solvate of any of them.

Abstract: A combination therapy for treating patients suffering from proliferative diseases or diseases associated with persistent angiogenesis is disclosed. The patient is treated with a camptothecin derivative and one or more chemotherapeutic agents selected from a microtubule active agent; an alkylating agent; an anti-neoplastic anti-metabolite; a platin compound; a topoisomerase II inhibitor; a VEGF inhibitor; a tyrosine kinase inhibitor; an EGFR kinase inhibitor; an mTOR kinase inhibitor; an insulin-like growth factor I inhibitor; a Raf kinase inhibitor; a monoclonal antibody; a proteasome inhibitor; a HDAC inhibitor; and ionizing radiation.

Abstract: The present invention relates to bicyclic heterocycles of general formula wherein Ra, Rb and Rc are defined as in claim 1, their tautomers, their stereoisomers, their mixtures and their salts, in particular their physiologically acceptable salts with inorganic or organic acids and bases, which have valuable pharmacological properties, in particular an inhibitory action on the signal transduction mediated by tyrosine kinases, their use for the treatment of illnesses, in particular of tumoral diseases and of benign prostatic hyperplasia (BPH), of diseases of the lung and of the airways, and the preparation thereof.

Abstract: The present invention relates to novel quinazoline derivatives with less skin irritation and an excellent action of strongly suppressing scratching behavior, and pharmaceutical compositions containing a quinazoline derivative as an active ingredient. The present invention is directed to the quinazoline derivatives represented by the general formula [1] or pharmaceutically acceptable salts thereof. In the general formula [1], R1 represents hydrogen or the like; R2 represents hydrogen or the like; R3 and R4 are the same or different and represent hydrogen, alkyl, alkoxy or halogen; R5 is combined with R6 to represent alkylene or represents hydrogen, hydroxy, alkyl, phenyl or alkoxy; R6 represents alkyl, cycloalkyl, phenyl, a 5- to 10-membered aromatic heterocyclic group containing one to three heteroatoms selected from the group consisting of a nitrogen atom, an oxygen atom and a sulfur atom, or —N(R6-1)(R6-2).

Abstract: Quinazoline derivatives of the following formula: wherein R1, R2, R3, R4, R5, X, Y, and Z are defined herein. It also discloses a method of treating cancer with one of these compounds.

Abstract: A compound of general formula I wherein: Ra is a benzyl, 1-phenylethyl, or 3-chloro-4-fluorophenyl group; Rb is a dimethylamino, N-methyl-N-ethylamino, diethylamino, N-methyl-N-isopropylamino, N-methyl-N-cyclopropylamino, N-methyl-N-(2-methoxyethyl)amino, N-ethyl-N-(2-methoxyethyl)amino, bis(2-methoxyethyl)amino, morpholino, N-methyl-N-(tetra-hydrofuran-3-yl)amino, N-methyl-N-(tetrahydrofuran-2-ylmethyl)amino, N-methyl-N-(tetra-hydrofuran-3-ylmethyl)amino, N-methyl-N-(tetrahydropyran-4-yl)amino, or N-methyl-N-(tetrahydropyran-4-ylmethyl)amino group; and Rc is a cyclopropylmethoxy, cyclobutyloxy, cyclopentyloxy, tetrahydrofuran-3-yloxy, tetrahydrofuran-2-ylmethoxy, tetrahydrofuran-3-ylmethoxy, tetrahydropyran-4-yloxy, or tetrahydropyran-4-ylmethoxy group, or a tautomer, stereoisomer, or salt thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases which have valuable pharmacological properties, in particular an inhibitory effect on signal transduction

Abstract: The present invention provides methods of treating baldness in a subject and generating new hair follicles, comprising epidermal disruption and administration of a compound that promotes a differentiation of an uncor?mitted epidermal cell into a hair follicle cell. The present invention also provides methods for hair removal and inducing hair pigmentation.

Abstract: The present invention relates to the use of quinazolines of formula (I), wherein the groups Ra to Rd have the meanings given in the claims and specification, in cancer therapy.

Abstract: The invention relates to a therapy of cancer comprising co-administration to a person in need of such treatment and/or co-treatment of a person in need of such treatment with effective amounts of: (1) a compound 1 of formula (I), wherein the groups Ra to Rd have the meanings given in the claims and specification; and (2) at least a further chemotherapeutic agent 2; optionally in combination with radiotherapy, radio-immunotherapy and/or tumour resection by surgery, furthermore, the invention relates to corresponding medicaments and the preparation thereof.

Abstract: The present invention relates to novel amorphous form of [6,7-Bis(2-methoxy-ethoxy)-quinazolin-4-yl]-(3-ethynyl-phenyl) (erlotinib hydrochloride), to solid amorphous dispersion of erlotinib hydrochloride and a carrier such as PVP or solid PEG, to processes for their preparations, to pharmaceutical compositions containing them and to method of treatment using the same. The amorphous form or solid amorphous dispersion of erlotinib hydrochloride obtained in this invention is useful in preparing pharmaceutical dosage forms.

Abstract: The present invention relates to compounds and methods which may be useful as inhibitors of phosphodiesterase 4 (PD E4) for the treatment or prevention of inflammatory diseases and other diseases involving elevated levels of cytokines and proinflammatory mediators.

Abstract: This invention provides quinazoline derivatives represented by the structural formula: (I); wherein: R2 is hydrogen, NR?R?, C1-7 alkyl, arylC1-7 alkyl or C3-10 cycloalkyl; R4 is amino, C1-7 alkyl, C2-7 alkenyl, C3-10 cycloalkyl, C3-10 cycloalkenyl, aryl, heterocyclic, arylalkyl, heterocyclic-substituted C1-7 alkyl or C3-10 cycloalkyl-C1-7 alkyl; R5 is hydrogen or C1-7 alkyl, or R5 and R4 together with the nitrogen atom to which they are attached form a heterocyclic ring; Y is a single bond, C1-7alkylene, C2-7 alkenylene or C2-7 alkynylene; R6 is halogen, heteroaryl or aryl; R? and R? are each independently hydrogen, C1-7 alkyl-carbonyl or C1-7 alkyl; provided that R4 is not phenyl substituted with morpholino when R2 is H and R5 is H, and provided that when NR4R5 is piperazinyl, said NR4R5 is either non-substituted or substituted with methyl or acetyl; a pharmaceutically acceptable addition salt, a stereoisomer, a mono- or a di-N-oxide, a solvate or a pro-drug thereof, for the treatment of viral infections.

Abstract: The present invention provides methods of identifying an agents that inhibit tumor cells from undergoing an epithelial to mesenchymal transition, impair tumor cell mobility, and thus inhibit tumorigenicity. The present invention also provides compositions comprising said agents, and methods for their preparation and use. The present invention also provides methods for inhibiting tumor cells in a patient from undergoing an epithelial to mesenchymal transition by administration of inhibitors of PAK2 kinase, that optionally also inhibit PAK1 kinase. Such methods may be employed in combination with other anti-cancer agents such as EGFR or IGF-1R kinase inhibitors.

Abstract: Disclosed are 4-arylamino-quinazolines and analogs thereof effective as activators of caspases and inducers of apoptosis. The compounds of this invention are useful in the treatment of a variety of clinical conditions in which uncontrolled growth and spread of abnormal cells occurs.

Abstract: The invention relates to the inhibition of the Cyclin-Dependent Kinase Inhibitor (CDKI) pathway. More particularly, the invention relates to methods for inhibiting the CDKI pathway for studies of and intervention in senescence-related and other CDKI-related diseases.

Abstract: The invention provides methods for modulating tumor cell proliferation by contacting cells (e.g. tumor cells) with a TACE inhibitor and a compound that inhibits EGFR tyrosine kinase, whereby the TACE inhibitor enhances the sensitivity of the cell to the EGFR tyrosine kinase inhibitor. Additionally, methods for treating cancer and methods for identifying TACE inhibitors is also provided.

Abstract: A method of potentiating the efficacy of an antineoplastic agent such as temozolomide, comprises the administration of an antifolate agent as defined herein. Also disclosed are compositions, including pharmaceutical compositions, comprising the antineoplastic agent and an antifolate agent, and the use of such compounds and compositions thereof to treat a variety of cancers, such as melanoma. Unit dosage forms and kits are also contemplated and disclosed.

Abstract: This invention relates to novel quinazoline derivatives, and their pharmaceutically acceptable salts. The invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions beneficially treated by inhibiting cell surface tyrosine receptor kinases.

Abstract: The present disclosure provides compounds that inhibit protein kinases, such as JAK, Axl, or Syk kinases, compositions comprising the compounds and methods of using the compounds to inhibit protein kinase and treat and/or prevent diseases associated with inappropriate kinase activity.

Abstract: The present invention provides methods of preparing antifolate compounds. The inventive methods can particularly be use for preparing compounds exhibiting improved bioavailability, making the compound particularly useful in pharmaceutical compositions. The compounds prepared according to the inventive methods are useful in the treatment of multiple conditions, including abnormal cell proliferation, inflammatory diseases, asthma, and arthritis.

Abstract: The present invention provides a method for treating tumors or tumor metastases in a patient, comprising administering to the patient a therapeutically effective amount of an EGFR kinase inhibitor, combined with treating the patient simultaneously or sequentially with radiation therapy, with or without additional agents or treatments, such as other anti-cancer drugs. A preferred example of an EGFR kinase inhibitor that can be used in practicing this invention is the compound erlitinib HCl (also known as Tarceva™).

Abstract: The present invention provides pharmaceutical compositions comprising an antifolate compound. The composition exhibit improved bioavailability, and they particularly incorporate beneficial excipients that increase solubility and bioavailability, such as cyclodextrins or compounds formed of fatty acid esters of glycerol and polyethylene glycol esters. The pharmaceutical compositions are useful in the treatment of multiple conditions, including abnormal cell proliferation, inflammatory diseases, asthma, and arthritis.

Abstract: The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain amino-ethyl-amino-aryl (AEAA) compounds which, inter alia, inhibit protein kinase D (PKD) (e.g., PKD1, PKD2, PKD3). The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit PKD, and in the treatment of diseases and conditions that are mediated by PKD, that are ameliorated by the inhibition of PKD, etc., including proliferative conditions such as cancer, etc.

Abstract: A method of treating an individual comprising: evaluating the disease state of said individual through quantitative and/or qualitative assays; administering in amounts sufficient to treat said disease at least three agents wherein at least one agent is an inhibitor of the human epidermal receptor pathway, at least one agent is signal transduction inhibitor and at least one agent is an angiogenesis inhibitor and; reevaluating the disease state of said individual presenting through quantitative and/or qualitative assays. A composition comprising a first agent that is an inhibitor of the human epidermal receptor pathway, a second agent that is an angiogenesis inhibitor and a third agent that is an inhibitor of Akt wherein said first agent, second agent, third agent and combinations thereof are present in amounts that when administered to an individual in a diseased state are sufficient to treat said disease.

Abstract: The invention relates to the compounds of formula (I) having antithrombotic activity which especially inhibit blood clotting factor IXa, to methods for producing the same and to the use thereof as drugs.

Abstract: The present invention relates to a quinoline or quinazoline derivative having the general formula (A): in which R3, R4, W, Y and Q are indicated in the description and the claims, the use of the compounds of the general formula (A) for the treatment of various disorders, and the preparation of compounds of the general formula (A).

Abstract: The present invention relates generally to the fields of molecular biology and growth factor regulation. More specifically, the invention relates to combination therapies for the treatment of pathological conditions, such as cancer.

Abstract: This invention relates to methods for treating, preventing and/or managing cancer in a subject including enhancing the efficacy of a Receptor Tyrosine Kinase inhibitor (e.g., a small molecule RTK inhibitor, e.g., Sorafenib or Erlotinib) by administering to the subject a Vascular Disrupting Agent (e.g., a Combretastatin or derivative thereof) sequentially or simultaneously in combination with said RTK inhibitor. Pharmaceutical compositions comprising a combination of a RTK inhibitor and a VDA are also provided.

Abstract: The present invention provides compounds for modulating receptor kinase activity, particularly ephrin and EGFR, and methods of treating diseases mediated by receptor kinase activity utilizing the compounds and pharmaceutical compositions thereof. Diseases mediated by receptor kinase activity include, but are not limited to, diseases characterized in part by abnormal levels of cell proliferation (i.e. tumor growth), programmed cell death (apoptosis), cell migration and invasion and angiogenesis associated with tumor growth. Compounds of the invention include “spectrum selective” kinase modulators, compounds that inhibit, regulate and/or modulate signal transduction across subfamilies of receptor-type tyrosine kinases, including ephrin and EGFR.

Abstract: The present invention relates to a method of treating cancer in a mammal and to pharmaceutical combinations useful in such treatment. In particular, the method relates to a cancer treatment method that includes administering an erb family inhibitor and an IGF-1R inhibitor to a mammal suffering from a cancer.

Abstract: The present invention provided methods for treating lung cancers using therapeutic agents for lung cancers comprising erbB receptor inhibitors as active ingredients. Methods for examining the responsiveness of lung cancer patients to erbB receptor inhibitors by using blood amphiregulin (AREG) as an indicator were provided. Furthermore, methods for treating lung cancers in which responsiveness to an erbB receptor inhibitor is determined based on blood AREG concentration, and in which therapeutic agents are selectively administered to patients expected to be responsive, were also provided. Advanced therapeutic effects can be expected by administering an erbB receptor inhibitor to patients predicted to be responsive. The present invention contributes to the improvement of therapeutic effects of gefitinib (Product name: Iressa®) and such on lung cancers.

Abstract: The present invention relates to sulphoximine-substituted quinazoline derivatives of the formula (I), processes for their preparation and their use as a medicament for the treatment of various diseases.

Abstract: This invention relates to pulsatile dose administration of gossypol, a gossypol-related compound or pharmaceutical compositions thereof for treating diseases, disorders and conditions responsive to gossypol or gossypol-related compound, inhibiting the activity of anti-apoptotic Bcl-2 family proteins, inducing apoptosis in cells and increasing the sensitivity of cells to inducers of apoptosis.

Abstract: The present invention describes a method or uses of prevention and/or treatment of a cancer or a tumor, and in particular to a combination therapy, methods, compositions and pharmaceutical packages comprising an inhibitor of receptors of the EGFR family or a chemotherapeutically active pyrimidine analogue and certain platinum-based chemotherapeutic agents.

Abstract: Provided are Breast Cancer Resistance Protein (BCRP) inhibitors, P-glycoprotein (P-gp) inhibitors and chemotherapeutic agents for use in the treatment of cancer by combination therapy of the BCRP inhibitor and/or P-gp inhibitor with the chemotherapeutic agent. The chemotherapeutic agent is an imidazotetrazine, e.g. temozolomide.

Abstract: Methods for using death receptor ligands, such as Apo-2 ligand/TRAIL polypeptides or death receptor antibodies, and EGFR inhibitors to treat pathological conditions such as cancer are provided. Embodiments of the invention include methods of using Apo2L/TRAIL or death receptor antibodies such as DR5 antibodies and DR4 antibodies in combination with EGFR inhibitors, such as Tarceva™.

Abstract: Quinazolines of the formula (I) in which R, R1, R2, R3, R4 and Y have the meaning indicated in Patent claim 1, and their salts or solvates as glycoprotein 1bIX antagonists.

Abstract: Compositions and methods for promoting neural regeneration in a patient determined to have a lesion in a mature CNS neuron are disclosed. The method comprises the step of contacting the neuron with an EGFR inhibitor sufficient to promote regeneration of the neuron.

Abstract: The invention relates to the guanine derivatives of general formula (I), and to hydrates or solvents thereof, for use as neuropeptide FF receptor antagonists in the treatment of pains and hyperalgesia, of withdrawal symptoms of addiction to alcohol, psychotropic drugs or nicotine and in the prevention of or recovery from these addictions, for the regulation of insulin release, food intake, memory functions, blood pressure, electrolyte and energy metabolism, and in the treatment of urinary incontinence

Abstract: The present invention provides a composition and a method for treating tumors or tumor metastases in a patient, comprising administering to the patient simultaneously or sequentially a therapeutically effective amount of a combination of an EGFR kinase inhibitor and a KIT kinase inhibitors, with or without additional agents or treatments, such as other anti-cancer drugs or radiation therapy. A preferred example of an EGFR kinase inhibitor that can be used in practicing this invention is the compound erlotinib HCl (also known as TARCEVA®). A preferred example of a KIT kinase inhibitor that can be used in practicing this invention is OSI-930 and OSI-817.

Abstract: Methods of treating blood disorders are described.

Abstract: The present invention provides 2-aminoquinazoline derivatives represented by formula (I): wherein R1 and R2 may be the same or different and each represents a hydrogen atom, substituted or unsubstituted lower alkyl, and the like; X represents a bond or CR7aR7b wherein R7a and R7b may be the same or different and each represents a hydrogen atom, and the like; when X is a bond, R3 represents substituted or unsubstituted aryl or a substituted or unsubstituted aromatic heterocyclic group; when X is CR7aR7b wherein R7a and R7b have the same meanings as defined above, respectively, R3 represents substituted or unsubstituted lower alkoxy, substituted or unsubstituted aryl, and the like; R4 represents a hydrogen atom, hydroxy, substituted or unsubstituted lower alkoxy, and the like; and R5 represents a hydrogen atom, substituted or unsubstituted aryl, and the like, or a pharmaceutically acceptable salt thereof.

Abstract: The invention provides a novel crystalline form of Erlotinib HCl, processes for its preparation, and formulations thereof.

Abstract: Compounds of formula (I) or (II) are dihydrofolate reductase inhibitors, useful for the treatment of, for example, cell proliferative diseases: wherein A and D are independently —CHR7— or —NR7—; E and G are independently ?CR7— or ?N—; each R6 independently represents hydrogen or —OR7; R7 is hydrogen or C1-C6 alkyl; R1 is a carboxylic acid group (—COOH), or an ester group which is hydrolysable by one or more intracellular carboxylesterase enzymes to a carboxylic acid group; R2 is the side chain of a natural or non-natural alpha amino acid which does not contain a carboxyl, or carboxyl ester group; Y is a bond, —C(?O)—, —S(?O)2—, —C(?O)NR3—, —C(?S)—NR3, —C(?NH)NR3 or —S(?O)2NR3— wherein R3 is hydrogen or optionally substituted C1-C6 alkyl; L1 is a divalent radical of formula -(Alk1)m(Q)n(Alk2)p- wherein m, n and p are independently 0 or 1, and Q, Alk1 and Alk2 are as defined in the claims; X1 represents a bond; —C(?O); or —S(?O)2—; —NR4C(?O)—, —C(?O)NR4—, —NR4C(?O)NR5—, —NR4S(?O)2—, or —S(?O)2NR4— wherein R

Abstract: The present invention provides novel tricyclic spiro-oxathiine naphthoquinone derivatives, a synthetic method for making the derivatives, and the use of the derivatives to induce cell death and/or to inhibit proliferation of cancer or precancerous cells. The naphthoquinone derivatives of the present invention are related to the compound known as ?-lapachone (3,4-dihydro-2,2-dimethyl-2H-naphtho(1,2-b)pyran-5,6-dione).

Abstract: The present invention is directed to a compound of Formula I or a single isomer thereof; where the compound is optionally as a pharmaceutically acceptable salt, hydrate, solvate or combination thereof, in addition to methods of preparing a Compound of Formula I, and methods of using a Compound of Formula I to treat cancer.

Abstract: The present invention relates to the anhydrous and hydrate forms of N-(3-ethynylphenyl)-6,7-bis(2-methoxyethoxy)-4-quinazolinamine mesylate. The invention also relates to pharmaceutical compositions containing N-(3-ethynylphenyl)-6,7-bis(2-methoxyethoxy)-4-quinazolinamine mesylate and to methods of treating hyperproliferative disorders, such as cancer, by administering N-(3-ethynylphenyl)-6,7-bis(2-methoxyethoxy)-4-quinazolinamine mesylate.

Abstract: Novel wortmannin analogs and their use in inhibiting PI-3-kinase activity in mammals and the treatment or prevention of cancer and tumor formation in a subject are described herein. Preferably, the wortmannin analogs may be administered with other chemotherapeutic agents in the treatment of cancer.

Abstract: A method using quinazoline derivatives, celastrol, cape, BAY 11-7082, rocaglamide, and 7-Methoxy-5,11,12-trihydroxy-coumestan is administered to a mammal for the treatment and prevention of viral diseases and cancers. The chemical compounds are targeted to inhibit NF-?B transcriptional activity. These treatments for viral diseases, especially for infection caused by HIV, and cancers may be accomplished utilizing quinazoline derivatives, celastrol, cape, BAY 11-7082, rocaglamide, 7-Methoxy-5,11,12-trihydroxy-coumestan, and compounds similar to them alone or in combination with prior art other therapy.