Patents by Inventor Vladimir Evgenievich Nebolsin

Vladimir Evgenievich Nebolsin has filed for patents to protect the following inventions. This listing includes patent applications that are pending as well as patents that have already been granted by the United States Patent and Trademark Office (USPTO).

  • Publication number: 20240116898
    Abstract: The invention relates to chemistry of organic substances, pharmacology and medicine, and concerns treating diseases associated and with aberrant activity of cells of the immune system, more particularly for treating lung, respiratory tract and abdominal diseases, radiation sickness and pain syndrome, and also other diseases by using compounds of formula (A) wherein R1 is —C(O)—R2—C(O)— or —R2—C(O)n— group, where R2 is —(CH2)n— group optionally substituted with one or two C1-C6 alkyls, or phenyl, n is an integer from 0 to 4; wherein compounds are selected from the group consisting of the group of compounds as set out in the description. These compounds, as well as pharmaceutically acceptable salts thereof, are highly effective in inhibiting glutaminyl cyclase, which is involved, in particular, in processes of post-translational modification of chemokines and chemotaxis of monocytes, macrophages and other cells of the immune system.
    Type: Application
    Filed: November 3, 2023
    Publication date: April 11, 2024
    Inventors: Vladimir Evgenievich NEBOLSIN, Anastasia Vladimirovna RYDLOVSKAYA, Tatyana Alexandrovna KROMOVA
  • Patent number: 11845740
    Abstract: The invention relates to chemistry of organic substances, pharmacology and medicine, and concerns treating diseases associated and with aberrant activity of cells of the immune system, more particularly for treating lung, respiratory tract and abdominal diseases, radiation sickness and pain syndrome, and also other diseases by using compounds of formula (A) wherein R1 is —C(O)—R2—(O)— or —R2—C(O)— group, where R2 is —(CH2)n-group optionally substituted with one or two C1-C6 alkyls, or phenyl, n is an integer from 0 to 4; wherein compounds are selected from the group consisting of the group of compounds as set out in the description. These compounds, as well as pharmaceutically acceptable salts thereof, are highly effective in inhibiting glutaminyl cyclase, which is involved, in particular, in processes of post-translational modification of chemokines and chemotaxis of monocytes, macrophages and other cells of the immune system.
    Type: Grant
    Filed: May 24, 2018
    Date of Patent: December 19, 2023
    Assignees: LTD “VALENTA-INTELLEKT”
    Inventors: Vladimir Evgenievich Nebolsin, Anastasia Vladimirovna Rydlovskaya, Tatyana Alexandrovna Kromova
  • Publication number: 20230203016
    Abstract: The present invention relates to novel biologically active compounds, in particular dicarboxylic acid bisamide derivatives of general formula I: or pharmaceutically acceptable salts thereof, which are able to form complexes with or chelate metal ions. The invention also relates to the use of said compounds as an agent for the prevention and/or treatment of cardiovascular, viral, cancer, neurodegenerative and inflammatory diseases, diabetes, age-related diseases, diseases caused by microbial toxins, alcoholism and alcoholic cirrhosis, anaemia, porphyria cutanea tarda, and transition metal salt poisoning. The present invention also relates to novel methods for preparing dicarboxylic acid bisamide derivatives of general formula I.
    Type: Application
    Filed: December 21, 2022
    Publication date: June 29, 2023
    Inventors: Vladimir Evgenievich NEBOLSIN, Tatyana Alexandrovna KROMOVA, Galina Alexandrovna ZHELTUKHINA
  • Patent number: 11584709
    Abstract: The invention relates to the chemistry of organic compounds, pharmacology and medicine and concerns therapy for obesity, psoriasis, Crohn's disease, colitis, irritable bowel syndrome, diarrhea, nausea and vomiting, as well as a number of other diseases associated with the activity of cathepsin S, cannabinoid receptors type 1, tachykinin receptors type 1 and 2, prokineticin receptors type 1 and 2, bradykinin receptors type 1, melanocortin receptors MC4R, serotonin receptors 5-HT2B and NB-kB signaling pathway, by using benzyl (2S)-2-[2-(4-hydroxyphenyl)acetamido]-3-phenylpropanoate compound. The compound and pharmaceutically acceptable adducts, hydrates and solvates thereof are a cathepsin S inhibitor, cannabinoid receptor type 1 agonist, tachykinin receptor type 1 and 2 antagonist, prokineticin receptor type 1 and 2 antagonist, bradykinin receptor type 1 antagonist, melanocortin receptor MC4R antagonist, serotonin receptor 5-HT2B antagonist, and NB-kB signaling pathway inhibitor.
    Type: Grant
    Filed: May 24, 2018
    Date of Patent: February 21, 2023
    Assignee: “PHARMENTERPRISES EURASIA” LIMITED LIABILITY COMPANY
    Inventors: Vladimir Evgenievich Nebolsin, Tatyana Alexandrovna Kromova, Anastasia Vladimirovna Rydlovskaya
  • Patent number: 11571411
    Abstract: The invention relates to the therapy of diseases associated with the activity of histamine receptors, in particular for the treatment of allergic diseases, preferably the therapy of perennial and persistent allergic rhinitis, itch, as well as a number of other diseases associated with the activity of histamine receptor type 3 and/or 4, using compound N,N?-bis(2-(1H-imidazol-5-yl)ethyl)malonamide. This compound, as well as pharmaceutically acceptable salts, hydrates, or solvates thereof, is an antagonist of histamine receptor type 3 and/or 4. The invention also relates to pharmaceutical compositions containing a therapeutically effective amount of Compound I.
    Type: Grant
    Filed: May 22, 2019
    Date of Patent: February 7, 2023
    Assignee: PHARMENTERPRISES ALLERGY LLC
    Inventor: Vladimir Evgenievich Nebolsin
  • Publication number: 20220362230
    Abstract: The present invention relates to the medicine, in particular, to a new drug effective for the treatment of diseases associated with aberrant interferon gamma signaling, such as Sjögren's syndrome, dermatomyositis, systemic lupus erythematosus, or systemic sclerosis; for the treatment of patients suffering from cough; and for the treatment of disorders in steroid-resistant patients, such as asthma, rheumatoid arthritis, systemic lupus erythematosus, and gastrointestinal diseases, by administering a compound 1-(2-(1H-imidazol-4-yl)ethyl) piperidin-2,6-dione The invention provides the creation of a new effective drug for overcoming steroid resistance.
    Type: Application
    Filed: November 22, 2019
    Publication date: November 17, 2022
    Applicant: "CHEMIMMUNE THERAPEUTICS" LIMITED LIABILITY COMPANY
    Inventor: Vladimir Evgenievich NEBOLSIN
  • Publication number: 20220324843
    Abstract: The present invention relates to novel biologically active compounds, in particular dicarboxylic acid bisamide derivatives of general formula I: or pharmaceutically acceptable salts thereof, which are able to form complexes with or chelate metal ions. The invention also relates to the use of said compounds as an agent for the prevention and/or treatment of cardiovascular, viral, cancer, neurodegenerative and inflammatory diseases, diabetes, age-related diseases, diseases caused by microbial toxins, alcoholism and alcoholic cirrhosis, anaemia, porphyria cutanea tarda, and transition metal salt poisoning. The present invention also relates to novel methods for preparing dicarboxylic acid bisamide derivatives of general formula I.
    Type: Application
    Filed: November 18, 2021
    Publication date: October 13, 2022
    Inventors: Vladimir Evgenievich NEBOLSIN, Tatyana Alexandrovna KROMOVA, Galina Alexandrovna ZHELTUKHINA
  • Patent number: 11439631
    Abstract: The invention relates to medicine and concerns the treatment of diseases related to the aberrant activity of fractalkine and monocyte chemoattractant proteins 1-4 (CCL2, CCL7, CCL8, CCL13), preferably the treatment of pain, fever, pneumonia, bronchitis, bronchiolitis, alveolitis, rheumatoid arthritis, psoriasis and other diseases, using the compound 1-(2-(1H-imidazol-4-yl)ethyl)piperidine-2,6-dione or a pharmaceutically acceptable salt or solvate thereof The present invention also relates to pharmaceutical compositions that contain a therapeutically effective amount of the claimed compound according to the invention. The present compound and pharmaceutically acceptable salts thereof are highly effective in inhibiting the activity of the glutaminyl cyclase enzyme, which is involved in particular in processes of post-translational modification of the above-mentioned cytokines.
    Type: Grant
    Filed: March 6, 2018
    Date of Patent: September 13, 2022
    Assignee: “CHEMIMMUNE THERAPEUTICS” LIMITED LIABILITY COMPANY
    Inventors: Vladimir Evgenievich Nebolsin, Anastasia Vladimirovna Rydlovskaya
  • Patent number: 11414377
    Abstract: The invention relates to organic chemistry, pharmacology and medicine and is concerned with the treatment of inflammatory and autoimmune diseases, such as psoriasis, atopic dermatitis, prurigo, Crohn's disease, colitis, gastrointestinal diseases such as diarrhoea and irritable bowel syndrome, respiratory diseases such as asthma, COPD, bronchitis, rhinitis, and also cough and a series of other diseases associated with the activity of opioid and tachykinin receptors and of TRPV1 and TRPM8 ion channels using a 2-phenylethylamine N-(p-hydroxyphenylacetyl)phenylalanine compound The invention, and also pharmaceutically acceptable adducts, hydrates, solvates are agonists of opioid receptors, antagonists of tachykinin receptors and of TRPV1 and TRPM8 ion channels. The invention also relates to pharmaceutical compositions comprising a therapeutically effective amount of the compound according to the invention.
    Type: Grant
    Filed: May 7, 2019
    Date of Patent: August 16, 2022
    Assignee: IBD THERAPEUTICS LLC
    Inventor: Vladimir Evgenievich Nebolsin
  • Publication number: 20210361624
    Abstract: The invention relates to the therapy of diseases associated with the activity of histamine receptors, in particular for the treatment of allergic diseases, preferably the therapy of perennial and persistent allergic rhinitis, itch, as well as a number of other diseases associated with the activity of histamine receptor type 3 and/or 4, using compound N,N?-bis(2-(1H-imidazol-5-yl)ethyl)malonamide. This compound, as well as pharmaceutically acceptable salts, hydrates, or solvates thereof, is an antagonist of histamine receptor type 3 and/or 4. The invention also relates to pharmaceutical compositions containing a therapeutically effective amount of Compound I.
    Type: Application
    Filed: May 22, 2019
    Publication date: November 25, 2021
    Applicant: PHARMENTERPRISES ALLERGY LLC
    Inventor: Vladimir Evgenievich NEBOLSIN
  • Publication number: 20210284600
    Abstract: The invention relates to the chemistry of organic compounds, pharmacology and medicine and concerns therapy for obesity, psoriasis, Crohn's disease, colitis, irritable bowel syndrome, diarrhea, nausea and vomiting, as well as a number of other diseases associated with the activity of cathepsin S, cannabinoid receptors type 1, tachykinin receptors type 1 and 2, prokineticin receptors type 1 and 2, bradykinin receptors type 1, melanocortin receptors MC4R, serotonin receptors 5-HT2B and NB-kB signaling pathway, by using benzyl (2S)-2-[2-(4-hydroxyphenyl)acetamido]-3-phenylpropanoate compound. The compound and pharmaceutically acceptable adducts, hydrates and solvates thereof are a cathepsin S inhibitor, cannabinoid receptor type 1 agonist, tachykinin receptor type 1 and 2 antagonist, prokineticin receptor type 1 and 2 antagonist, bradykinin receptor type 1 antagonist, melanocortin receptor MC4R antagonist, serotonin receptor 5-HT2B antagonist, and NB-kB signaling pathway inhibitor.
    Type: Application
    Filed: May 24, 2018
    Publication date: September 16, 2021
    Applicant: "PHARMENTERPRISES EURASIA" LIMETED LIABILITY COMPANY
    Inventors: Vladimir Evgenievich NEBOLSIN, Tatyana Alexandrovna KROMOVA, Anastasia Vladimirovna RYDLOVSKAYA
  • Publication number: 20210246149
    Abstract: The invention relates to a new zinc complex with gamma-L-glutamylhistamine with a metal/ligand ratio of 1/1. In particular, the invention relates to a compound of the formula The complex according to the invention helps to restore the barrier functions of the epithelial tissue and suppresses the aberrant activity of the immune cells. The invention also relates to the method of complex preparation and use of said zinc complex for the treatment of atopic dermatitis and other diseases associated with impaired barrier functions of epithelial tissue and the development of an aberrant inflammatory response. The invention also relates to the use of the prepared complex for inhibiting glutaminyl cyclase. This invention also concerns pharmaceutical compositions comprising a therapeutically effective amount of a compound of the invention.
    Type: Application
    Filed: August 22, 2019
    Publication date: August 12, 2021
    Applicant: OBSCHESTVO S OGRANICHENNOI OTVETSTVENNOSTIYU "Z THERAPEUTICS"
    Inventor: Vladimir Evgenievich NEBOLSIN
  • Publication number: 20210070692
    Abstract: The invention relates to organic chemistry, pharmacology and medicine and is concerned with the treatment of inflammatory and autoimmune diseases, such as psoriasis, atopic dermatitis, prurigo, Crohn's disease, colitis, gastrointestinal diseases such as diarrhoea and irritable bowel syndrome, respiratory diseases such as asthma, COPD, bronchitis, rhinitis, and also cough and a series of other diseases associated with the activity of opioid and tachykinin receptors and of TRPV1 and TRPM8 ion channels using a 2-phenylethylamine N-(p-hydroxyphenylacetyl)phenylalanine compound The invention, and also pharmaceutically acceptable adducts, hydrates, solvates are agonists of opioid receptors, antagonists of tachykinin receptors and of TRPV1 and TRPM8 ion channels. The invention also relates to pharmaceutical compositions comprising a therapeutically effective amount of the compound according to the invention.
    Type: Application
    Filed: May 7, 2019
    Publication date: March 11, 2021
    Applicant: IBD THERAPEUTICS LLC
    Inventor: Vladimir Evgenievich NEBOLSIN
  • Patent number: 10772870
    Abstract: The invention relates to the field of medicine and concerns an agent that stimulates tissue regeneration and the recovery of diminished tissue and organ function. A medicinal agent for the treatment and/or prophylaxis of a pathological condition selected from the group including metabolic syndrome, impaired glucose tolerance, hepatitis, particularly chronic hepatitis and toxic hepatitis, idiopathic pulmonary fibrosis (IPF), emphysema of the lungs, chronic obstructive pulmonary disease (COPD) and cachexia, particularly as a result of impaired glucose tolerance, pulmonary fibrosis, chronic obstructive pulmonary disease, cancer and other diseases, is proposed in the form of an agent based on Treamide. The latter is a bisamide derivative of dicarboxylic acid of formula (I) or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: August 14, 2018
    Date of Patent: September 15, 2020
    Assignee: Treamid Therapeutics GmbH
    Inventors: Vladimir Evgenievich Nebolsin, Anastasia Vladimirovna Rydlovskaya, Alexandr Mikhailovich Dygai, Tatiana Gennadievna Borovskaya, Evgenii Germanovich Skurikhin
  • Patent number: 10745414
    Abstract: The invention is relevant to chemistry of organic compounds, pharmacology and medicine, and is related to prevention and treatment of musculoskeletal diseases in human and animals associated with the disorder of bone and/or cartilage metabolism, particularly with such musculoskeletal diseases as osteoporosis, osteoarthritis and osteochondrosis, using a new salt form of 2,2-dimethyl-6-((4-((3,4,5-trimethoxyphenyl)amino)-1,3,5-triazine-2-yl)amino)-2H-pyrido[3,2-b][1,4]oxazine-3(4H)-one. A salt of this compound with 4-methylbenzenesulfonic acid including its hydrates, solvates and polymorphic modifications of the salt, hydrates and solvates is featured with acceptable pharmacokinetic parameters and increased efficiency in the inhibition of Src-family kinases and Syk kinase, as well as other therapeutically significant kinases. This invention also covers pharmaceutical compositions containing therapeutically effective amount of the salt according to the invention.
    Type: Grant
    Filed: May 10, 2017
    Date of Patent: August 18, 2020
    Assignee: LIMITED “MOLECULAR TECHNOLOGIES”
    Inventors: Vladimir Evgenievich Nebolsin, Fedor Nikolaevich Novikov, Germes Grigorievich Chilov, Oleg Valentinovich Stroganov, Viktor Sergeevich Stroilov, Ilya Yurievich Titov
  • Publication number: 20200188379
    Abstract: The invention relates to medicine and concerns the treatment of diseases related to the aberrant activity of fractalkine and monocyte chemoattractant proteins 1-4 (CCL2, CCL7, CCL8, CCL13), preferably the treatment of pain, fever, pneumonia, bronchitis, bronchiolitis, alveolitis, rheumatoid arthritis, psoriasis and other diseases, using the compound 1-(2-(1H-imidazol-4-yl)ethyl)piperidine-2,6-dione or a pharmaceutically acceptable salt or solvate thereof The present invention also relates to pharmaceutical compositions that contain a therapeutically effective amount of the claimed compound according to the invention. The present compound and pharmaceutically acceptable salts thereof are highly effective in inhibiting the activity of the glutaminyl cyclase enzyme, which is involved in particular in processes of post-translational modification of the above-mentioned cytokines.
    Type: Application
    Filed: March 6, 2018
    Publication date: June 18, 2020
    Applicant: "CHEMIMMUNE THERAPEUTICS" LIMITED LIABILITY COMPANY
    Inventors: Vladimir Evgenievich NEBOLSIN, Anastasia Vladimirovna RYDLOVSKAYA
  • Publication number: 20200087285
    Abstract: The invention relates to chemistry of organic substances, pharmacology and medicine, and concerns treating diseases associated and with aberrant activity of cells of the immune system, more particularly for treating lung, respiratory tract and abdominal diseases, radiation sickness and pain syndrome, and also other diseases by using compounds of formula (A) wherein R1 is —C(O)—R2—(O)— or —R2—C(O)— group, where R2 is —(CH2)n-group optionally substituted with one or two C1-C6 alkyls, or phenyl, n is an integer from 0 to 4; wherein compounds are selected from the group consisting of the group of compounds as set out in the description. These compounds, as well as pharmaceutically acceptable salts thereof, are highly effective in inhibiting glutaminyl cyclase, which is involved, in particular, in processes of post-translational modification of chemokines and chemotaxis of monocytes, macrophages and other cells of the immune system.
    Type: Application
    Filed: May 24, 2018
    Publication date: March 19, 2020
    Applicant: OBSCHESTVO S OGRANICHENNOI OTVETSTVENNOSTIYU "PHARMENTERPRISES"
    Inventors: Vladimir Evgenievich NEBOLSIN, Anastasia Vladimirovna RYDLOVSKAYA, Tatyana Alexandrovna KROMOVA
  • Publication number: 20190292198
    Abstract: The invention is relevant to chemistry of organic compounds, pharmacology and medicine, and is related to prevention and treatment of musculoskeletal diseases in human and animals associated with the disorder of bone and/or cartilage metabolism, particularly with such musculoskeletal diseases as osteoporosis, osteoarthritis and osteochondrosis, using a new salt form of 2,2-dimethyl-6-((4-((3,4,5-trimethoxyphenyl)amino)-1,3,5-triazine-2-yl)amino)-2H-pyrido[3,2-b][1,4]oxazine-3(4H)-one. A salt of this compound with 4-methylbenzenesulfonic acid including its hydrates, solvates and polymorphic modifications of the salt, hydrates and solvates is featured with acceptable pharmacokinetic parameters and increased efficiency in the inhibition of Src-family kinases and Syk kinase, as well as other therapeutically significant kinases. This invention also covers pharmaceutical compositions containing therapeutically effective amount of the salt according to the invention.
    Type: Application
    Filed: May 10, 2017
    Publication date: September 26, 2019
    Inventors: Vladimir Evgenievich NEBOLSIN, Fedor Nikolaevich NOVIKOV, Germes Grigorievich CHILOV, Oleg Valentinovich STROGANOV, Viktor Sergeevich STROILOV, Ilya Yurievich TITOV
  • Patent number: 10377739
    Abstract: A compound having the following formula: or a pharmaceutically acceptable salt thereof. A medicament or pharmaceutical composition contains the compound. A method of treating a respiratory tract disease includes administering to a patient an effective amount of a compound or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: November 15, 2018
    Date of Patent: August 13, 2019
    Assignee: OBSCHESTVO S OGRANICHENNOI OTVETSTVENNOSTIYU “PHARMENTERPRISES”
    Inventors: Vladimir Evgenievich Nebolsin, Tatyana Alexandrovna Kromova
  • Publication number: 20190084961
    Abstract: A compound having the following formula: or a pharmaceutically acceptable salt thereof. A medicament or pharmaceutical composition contains the compound. A method of treating a respiratory tract disease includes administering to a patient an effective amount of a compound or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: November 15, 2018
    Publication date: March 21, 2019
    Inventors: Vladimir Evgenievich Nebolsin, Tatyana Alexandrovna Kromova