76 results about "Integrelin" patented technology

The invention relates to conjugates of anti-integrin specific antibodies with cytotoxic compounds, the synthesis, selection, and use of such conjugates for use in cancer therapy or other diseases mediated by cell proliferation, cell migration, or inflammation and which pathology involves angiogenesis or neovascularization of new tissue. In addition the invention relates to combination therapy of such diseases wherein the treatment comprises use of said conjugates in combination with one or more other treatment modalities including but not limited to: chemotherapy, surgery or radiation therapy. The preferred conjugates contain maytansinoid compounds linked to the antibody by a disulfide linkage, and preferred chemotherapeutic agents are doxorubicin, a taxane, a camptothecin, a podophyllotoxin, a nucleoside analog, or a pyrimidine analog.

The present invention relates to fluorinated compounds of formula I and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing the fluorinated compounds of the invention, and methods of treating macular degeneration, diabetic retinopathy (DR), macular edema, diabetic macular edema (DME), and macular edema following retinal vein occlusion (RVO), by administering these compounds and pharmaceutical compositions to subjects in need thereof.

The invention relates to anti-α2 integrin antibodies and their uses. Humanized antibodies are disclosed that bind to the I domain of α2 integrin and inhibit the interaction of α2β1 integrin with collagen. Also disclosed are therapeutic uses of anti-α2 integrin antibodies in treating α2β1-mediated disorders, including anti-α2 integrin antibodies that bind to α2 integrin without activating platelets.

Phenylalanine derivatives of the following formula, analogues thereof and pharmaceutically acceptable salts thereof have an antagonistic activity to α4 integrin. They are used as therapeutic agents or preventive agents for various diseases concerning α4 integrin in which α4 integrin-depending adhesion process participates in the pathology, such as inflammatory diseases, rheumatoid arthritis, inflammatory bowel diseases, systemic lupus erythematosus, multiple sclerosis, Sjögren's syndrome, asthma, psoriasis, allergy, diabetes, cardiovascular diseases, arterial sclerosis, restenosis, tumor proliferation, tumor metastasis and transplantation rejection.wherein R1 is a methyl group and R2 is a methoxy group.

The invention discloses application of HM-3 and platinum, paclitaxel or capecitabine medicine for preparing a solid tumor medicine, belonging to the field of medicines for treating tumor. Platinum, paclitaxel or capecitabine antimetabolites serve as active components and accompanied by a pharmaceutically acceptable carrier to be prepared into various pharmaceutically acceptable preparations. A plurality of experiments show that an integrin blocker HM-3 is clear in target; the integrin blocker HM-3 is reasonably used together with the platinum, paclitaxel or capecitabine for effectively suppressing growth of tumors in lung cancer, liver cancer, stomach cancer, breast cancer, cervical cancer, ovarian cancer, intestinal cancer, and the like. The combined medicine serves as a medicine and is capable of effectively treating tumors; the combined medicine is scientific, reasonable, feasible and effective, so that the treatment spectrum for treating the tumors is greatly expanded; the toxic and side effects are reduced; the HM-3 and platinum, paclitaxel or capecitabine medicine is prominent in social value and market value.

The present invention relates to methods and compositions designed for the treatment, management or prevention of cancer. The methods of the invention comprise the administration of an effective amount of one or more antagonists of Integrin αVβ3 alone or in combination with the administration of an effective amount of one or more other agents useful for cancer therapy. The invention also provides pharmaceutical compositions comprising one or more antagonists of Integrin αVβ3 and / or one or more other agents useful for cancer therapy. In particular, the invention is directed to methods of treatment and prevention of cancer by the administration of a therapeutically or prophylactically effective amount of one or more antagonists of Integrin αVβ3 alone or in combination with standard and experimental therapies for treatment or prevention of cancer. Also included are methods for screening for epitope-specific Integrin αVβ3 antagonists which can be used according to the methods of the invention. In addition, methods for facilitating the use of Integrin αVβ3 antagonists in the analysis of Integrin αVβ3 expression in biopsies of animal model and clinical study samples are also contemplated.

The invention relates to conjugates of anti-integrin specific antibodies with cytotoxic compounds, the synthesis, selection, and use of such conjugates for use in cancer therapy or other diseases mediated by cell proliferation, cell migration, or inflammation and which pathology involves angiogenesis or neovascularization of new tissue. In addition the invention relates to combination therapy of such diseases wherein the treatment comprises use of said conjugates in combination with one or more other treatment modalities including but not limited to: chemotherapy, surgery or radiation therapy. The preferred conjugates contain maytansinoid compounds linked to the antibody by a disulfide linkage, and preferred chemotherapeutic agents are doxorubicin, a taxane, a camptothecin, a podophyllotoxin, a nucleoside analog, or a pyrimidine analog.

The invention discloses 1,3-dihydro-1-oxo-2H-isobenzazole compounds (I) and pharmaceutically acceptable salts thereof, and also discloses preparation methods for the compounds, and uses of the compounds in preparing medicines for preventing and / or treating various diseases caused by the mediation of integrin alpha v beta 3, such as tumor metastasis, tumor growth, solid tumor growth, angiogenesis, retinopathy, macular degeneration, osteoporosis, arthritis, smooth muscle cell migration and atherosclerosis symptoms or diseases.

The present invention provides methods for predicting whether an individual having inflammatory bowel disease (IBD) is likely to respond to vedolizumab treatment. Also provided are methods for predicting whether an individual with IBD such as Crohn's disease or ulcerative colitis will develop autoantibodies against vedolizumab. The present invention also provides a treatment regimen for an IBD patient which includes measuring the level of one or more predictive markers of response to vedolizumab prior to administering the anti-α4β7 integrin drug.

The invention discloses a traditional Chinese medicine composition for treating luteal phase defect type infertility and menstrual disorder. The traditional Chinese medicine composition disclosed by the invention is prepared from the following components in parts by weight: 1-6 parts of fried radix paeoniae alba, 1-9 parts of common yam rhizome, 1-6 parts of dogwood, 0.5-3 parts of vinegar baked bupleurum root, 1-9 parts of the seed of Chinese dodder, 1.5-9 parts of sliced cornu cervi, 1.5-9 parts of amethyst and 1-6 parts of radix salviae miltiorrhizae. According to the compound composition provided by the invention, by means of syndrome differentiation and treatment, the formula is obtained through a lot of experimental screening under the guidance of theories of traditional Chinese medicines; experimental results show that the traditional Chinese medicine composition is capable of improving the structure and form of ovary mitochondria endoplasmic reticulum, improving structures of endometrial glands and mesenchyme, adjusting ovary secreted active substances E2 and P, reducing endometrium estrogen receptors and progestrone receptors and increasing expression of integrins alpha v and beta 3; therefore, the endometrium receptivity can be increased; the embryo implantation action is promoted; the traditional Chinese medicine composition has the good effect for treating infertility; and furthermore, the traditional Chinese medicine composition is free from toxic and side effect, and safe and reliable to use.

A method of treating glaucoma is described herein. The method includes the steps of providing an ultrasonic device that emits ultrasonic energy, holding the ultrasonic device at a location external to the trabecular meshwork, transmitting the ultrasonic energy at a frequency to a desired location for a predetermined time, causing biochemical changes to be initiated within the eye that may include triggering a presumed integrin response that initiates biochemical changes typified by but not limited to cytokines, enzymes, macrophage activity and heat shock proteins, and dislodging material built up in the trabecular meshwork.

The invention relates to the prophylaxis and / or treatment of fibrosis and / or fibrotic diseases by means of antibodies. Above all, the invention relates to the administration of an anti-alpha-v integrin (receptor) antibody to patients suffering from fibrosis and / or fibrotic diseases, including but not limited to systemic sclerosis (SSc). More specifically, the instant invention relates to the treatment of fibrotic diseases of the skin, lung, heart, liver and / or kidney by means of said antibody. Even more specifically, the instant invention relates to the administration of a recombinant, de-immunized monoclonal antibody targeting αv-integrins patients suffering from systemic sclerosis, including, but not limited to systemic sclerosis of the skin, lung, heart and / or kidney by means of the anti-alpha-v integrin antibody DI17E6 and structural mutants or modifications thereof.

The invention discloses 18F-E[c(RGDyk)2], a medicine box used for automatic production thereof, and a preparation method and use of the medicine box, relates to a polyethylene terephthalate (PET) developer and a preparation method and use thereof and relates to the technical field of radiative medicines and nuclear medicines. The medicine box contains a raw material reagent A and a raw material reagent B. A bottle A contains E[c(RGDyk)2]-NO2; and A bottle B contains acetonitrile solution of crown ether K222 / K2CO3. The 18F-E[c(RGDyk)2] prepared by the medicine box has high absorbing performance and excellent retaining performance in model mouse tumor, and has a very high target / non target ratio, excellent pharmacokinetic characteristic and high biological performance, and can completely meet the requirements of PET developer of tumour integrin alphavbeta3 receptor.

Methods of treatment of colorectal cancer can include the administration of the anti-alpha-v integrin (receptor) antibody Abituzumab. Preferably, the methods of treating colorectal cancer can include treating Stage II-IV colorectal cancer, metastatic colorectal cancer, left-sided colorectal cancer and / or left-sided metastatic colorectal cancer, involving the administration of said Abituzumab to patients in need thereof. Abituzumab is also useful for the manufacture of a medicament for treating colorectal cancer, preferably colorectal cancer as defined herein. Abituzumab is further useful for the manufacture of a medicament for treating colorectal cancer in combination with suitable targeted therapy concepts, such as growth factor or growth factor receptor targeting monoclonal antibodies, and / or chemotherapy.

A method is used for treating bone metastasis diseases in subjects. The method preferably depends on whether the subject shows certain specific proteins levels in one or more body fluids prior to or during treatment. The treatment includes the administration of at least one pan αv integrin inhibitor to a subject, a medicament for use in said new methods, and a method of predicting the outcome of a treatment with at least one pan αv integrin inhibitor based on the specific protein levels in one or more body fluids of the subject.

The invention discloses fusion protein with anti-tumor, anti-inflammation and oculopathy-treatment functions and a preparation method and application thereof, which belong to the technical field of biological pharmacy. Specifically, the invention relates to the fusion protein of an integrin blocking agent, which has the function of inhibiting tumor angiogenesis and has the integrin affinity and the combining capacity. A rigid (R) or flexible (F) linker is adopted to fuse two polypeptides, so as to respectively obtain protein A and protein G, the medicine effect can be increased, the half-life period can be extended, the stability can be enhanced, and the fusion protein has the characteristics of strong action effect, low toxicity and the like and can be used for preventing and treating solid tumors, all kinds of inflammation and angiogenesis oculopathy. The fusion protein structurally comprises two angiogenesis inhibiting polypeptides and the amino acid linker between the two angiogenesis inhibiting polypeptides, and the fusion protein is expressed in colibacillus or eukaryocyte by using a genetic engineering method and is obtained through separation and purification of a GST (Glutathione S Transferase) affinity column.

The present invention provides N-methylated cyclic hexapeptides comprising RGD and at least one alanine residue. The present invention further provides prodrugs comprising the cyclic hexapeptides. Pharmaceutical compositions comprising said cyclic hexapeptides are also disclosed as well as methods of their production and use in treating integrin related conditions and diseases.

Provided herein are integrin inhibitors, compositions thereof, and methods of their uses. Crystalline forms of salts of the inhibitors are also described, along with methods of preparing the crystalline forms. X-ray powder diffraction data, thermogravimetric analysis, and differential scanning calorimetry data are provided for the crystalline forms. The integrin inhibitors are useful for treatment of, inter alia, fibrotic diseases.

Tetrahydronaphthyridines of formulaare disclosed. These compounds selectively inhibit αVβ3 without activating the αVβ3 receptor. They are useful for treating osteoporosis, acute myelogenous leukemia, sickle cell disease, focal segmental glomerulosclerosis, fibrosis, supravalvular aortic stenosis associated with Williams syndrome, tumors expressing αVβ3, tumor metastasis, bone resorption, T-cell lymphoma, retinal disease, age-related macular degeneration, diabetic retinitis, and herpes simplex virus infection. They may also be used for inhibiting tumor angiogenesis.

An object of the present invention is to provide a method for efficiently separating megakaryocytes and platelets produced from the megakaryocytes, and an instrument for efficiently separating megakaryocytes and platelets produced from the megakaryocytes. According to the present invention, a method for separating megakaryocytes and platelets, including a contact step of bringing a culture solution that contains at least megakaryocytes into contact with a substrate coated with a biocompatible polymer that adheres to the megakaryocytes via at least one of a VLA-4 integrin or a VLA-5 integrin; a culture step of culturing the megakaryocytes to produce platelets before and / or after the contact step; and a recovery step of recovering the culture solution after the contact step and the culture step is provided.