ТИОЭФИРЗАМЕЩЕННЫЕ ИМИДАЗОХИНОЛИНЫ

Описываются имидазохинолиновые производные формулы (I) где Х представляет собой алкил, -CHR3-; Z представляет собой -S-, -SO- или -SO2- группу; R1 выбран из группы, включающей алкил и незамещенный фенил; R2 выбран из группы, включающей атом водорода; алкил; алкил-Y-алкил; каждый R3 представляет собой атом водорода; Y представляет собой -О-; n равен 0. Описывается также тетраимидазохинолиновое производное, фармацевтические композиции на их основе, способ стимулирования биосинтеза цитокина в организме животного. Предлагаемые в изобретении соединения и композиции могут вызывать биосинтез различных цитокинов и в связи с этим использоваться для лечения различных болезней, включая вирусные и опухолевые заболевания. 9 н. и 11 з.п. ф-лы, 1 табл.

СРЕДСТВО ПРОТИВ КИСЛОТОУСТОЙЧИВЫХ БАКТЕРИЙ, СОДЕРЖАЩЕЕ ПИРИДОНКАРБОНОВЫЕ КИСЛОТЫ В КАЧЕСТВЕ АКТИВНОГО КОМПОНЕНТА

Изобретение относится к средству против кислотоустойчивых бактерий, содержащему в качестве активного компонента производное пиридонкарбоновой кислоты, его фармацевтически приемлемую соль или его гидрат, которое проявляет высокую антибактериальную активность в отношении Mycobacterium tuberculosis и атипичных кислотоустойчивых бактерий. Описывается средство против кислотоустойчивых бактерий, содержащее в качестве активного компонента соединение, представленное следующей общей формулой (1), его соль или его гидрат где R1 представляет циклическую алкильную группу, имеющую 3-6 углеродных атомов, которая может иметь заместитель(и), выбранные из атомов галогена; R2представляет атом водорода; R3 представляет атом водорода; А1 представляет неполную структуру, представленную формулой (2) где X2 представляет атом галогена, алкильную группу, имеющую 1-6 углеродных атомов или алкоксигруппу, имеющую 1-6 углеродных атомов; А1, А2 и А3 образуют неполную структуру вместе с углеродными атомами, объединенными ...

N,N'-(СУЛЬФОНИЛДИ-1,4-ФЕНИЛЕН)БИС(N'',N''- ДИМЕТИЛФОРМАМИДИН)1,2,3,4-ТЕТРАГИДРО-6-МЕТИЛ-2,4- ДИОКСО-5-ПИРИМИДИНСУЛЬФОНАТ, СТИМУЛИРУЮЩИЙ КЛЕТОЧНЫЙ МЕТАБОЛИЗМ И ОБЛАДАЮЩИЙ ИММУНОТРОПНОЙ И АНТИМИКОБАКТЕРИАЛЬНОЙ АКТИВНОСТЬЮ

FIELD: organic chemistry. SUBSTANCE: invention relates to new biologically active chemical compounds - derivatives of diaminodiphenyl-sulfone of the general formula (I) 8999$ гс пы Го (19) 13) ВИ “” 2 436 668 Сл РОССИЙСКОЕ АГЕНТСТВО ПО ПАТЕНТАМ И ТОВАРНЫМ ЗНАКАМ 5 МК С 070 239/60, А 61 К 31/505 12) ОПИСАНИЕ ИЗОБРЕТЕНИЯ К ПАТЕНТУ РОССИЙСКОЙ ФЕДЕРАЦИИ (21), (22) Заявка: 97117514/04, 07.10.1997 (71) Заявитель: Голощапов Николай Михайлович, (24) Дата начала действия патента: 07.10.1997 Мичурина Елена Андреевна, Филипских Тамара Петровна, (46) Дата публикации: 10.09.1999 Голощапова Елена Николаевна, (56) Ссылки: КИ 2086543 С1, 10.08.97. КЦ 2044728 Костюк Любовь Елизаровна СЛ, 27.09.95. ЗЦ 459228 А, 25.02.75. ЗИ (72) Изобретатель: Голощапов Н.М., 687074 А, 1979. СВ 1511517 А, 17.05.78. Мичурина Е.А., Филипских Т.П., Голощапова (98) Адрес для переписки: Е.Н., Костюк Л.Е., Сударева Т.Т., Хаитов 141321, Московская обл., Сергиево-Посадский Р.М. ‚ Цывкина Г.И., Решетов А.Л. район, п/о Краснозаводск, пос.Зеленая (73) Патентообладатель: Дубрава, Филиал Российского гос.центра Голощапов Николай Михайлович, экспертизы лекарств, Голощапову Н.М. Мичурина Елена Андреевна Филипских Тамара Петровна, Голощапова Елена Николаевна, Костюк Любовь Елизаровна (71) Заявитель (прод.): Сударева Татьяна Тимофеевна, Хаитов Рахим Мусаевич, Цывкина Галина Ивановна, Решетов Александр Леонидович (73) Патентообладатель (прод.): Сударева Татьяна Тимофеевна, Хаитов Рахим Мусаевич, Цывкина Галина Ивановна, Решетов Александр Леонидович (54) М,М!'-(СУЛЬФОНИЛДИ-1,4-ФЕНИЛЕН)БИС(М",М"- ДИМЕТИЛФОРМАМИДИН)1,2,3,4-ТЕТРАГИДРО-6-МЕТИЛ-2,4- ДИОКСО-5-ПИРИМИДИНСУЛЬФОНАТ, СТИМУЛИРУЮЩИЙ КЛЕТОЧНЫЙ МЕТАБОЛИЗМ И ОБЛАДАЮЩИЙ ИММУНОТРОПНОЙ И АНТИМИКОБАКТЕРИАЛЬНОЙ АКТИВНОСТЬЮ (57) Реферат: средства для лечения лепры, туберкулеза и Изобретение откосится к новым других иммунодефицитных заболеваний. 12 биологически активным химическим табл. соединениям, производным с Э диаминодифенилсульфона общей формулы 1, сн сн 30. которые ...

СПОСОБ ПОЛУЧЕНИЯ ЭКСТРАКТА, ОБЛАДАЮЩЕГО ПРОТИВОЛЕПРОЗНОЙ АКТИВНОСТЬЮ

Изобретение относится к области медицины, а именно к фитотерапии, и может быть, в частности, использовано для получения экстракта, обладающего противолепрозной активностью. После 6-дневной экстракции корня солодки голой 40% этиловым спиртом в неотфильтрованную смесь (20 г растительного сырья в 100 мл спиртового раствора) добавляют в соотношении 1:1 (100 мл смеси, 100 мл буфера) буфер, содержащий, мас.%: хлористый кальций не более 0,014, хлористый калий не более 0,04, калий фосфорнокислый однозамещенный не более 0,006, магний сернокислый не более 0,02, хлористый магний не более 0,02, хлористый натрий не более 0,08, натрий кислый углекислый не более 0,035, натрий фосфорнокислый двухзамещенный не более 0,024; глюкоза не более 0,1, растворенных в 100 мл дистиллированной воды, при этом полученный раствор последующие 4 дня хранят при температуре 3°С, в темном месте при ежедневном его встряхивании. После чего экстракт отфильтровывают и 3-кратно автоклавируют при 0,5 атм в течение 10 мин. Изобретение ...

ПРОИЗВОДНЫЕ ПИПЕРИДИНА ПОЛЕЗНЫЕ В КАЧЕСТВЕ МОДУЛЯТОРОВ АКТИВНОСТИ РЕЦЕПТОРОВ ХЕМОКИНОВ

... 1. Соединение формулы (I) где Т представляет собой С(O) или S(O)2; W представляет собой С(O) или S(O)2; Х представляет собой СН2, О или NH; Y представляет собой CR5 или N; R1 представляет собой возможно замещенный арил или возможно замещенный гетероциклил; R2 представляет собой водород или C1-6алкил; R3 представляет собой водород или возможно замещенный C1-6алкил; R4 представляет собой алкил, возможно замещенный арил, возможно замещенный аралкил или возможно замещенный гетероциклил; R5 представляет собой водород или C1-6алкил; где вышеупомянутые арильные и гетероциклильные группировки возможно замещены галогеном, циано, нитро, гидрокси, оксо, S(O)pR25, OC(O)NR6R7, NR8R9, NR10 C(O)R11, NR12C(O)NR13R14, S(O)2NR15R16, NR17S(O)2R18, C(O)NR19R20, C(O)R21, CO2R22, NR23CO2R24, C1-6алкилом, CF3, группировкой C1-6алкокси(C1-6)алкил, C1-6алкокси, OCF3, C1-6алкокси(C1-6)алкокси, C2-6алкилтио, C2-6алкенилом, C2-6алкинилом, C3-10циклоалкилом (который сам возможно замещен C1-4алкилом или оксо), метилендиокси ...

СРЕДСТВО ПРОТИВ КИСЛОТОУСТОЙЧИВЫХ БАКТЕРИЙ, СОДЕРЖАЩЕЕ ГЕТЕРОЦИКЛИЧЕСКИЕ ПРОИЗВОДНЫЕ БЕНЗОКСАЗИНА ВКАЧЕСТВЕ АКТИВНОГО КОМПОНЕНТА

... 1. Средство против кислотоустойчивых бактерий, содержащее в качестве активного компонента соединение, представленное следующей общей формулой (1), его соль или его гидрат где R2 представляет атом водорода; R3 представляет атом водорода, аминогруппу, тиольную группу, галогенметильную группу, алкильную группу, имеющую 1-6 углеродных атомов, алкенильную группу, имеющую 2-6 углеродных атомов, алкинильную группу, имеющую 2-6 углеродных атомов, или алкоксигруппу, имеющую 1-6 углеродных атомов, из них аминогруппа может иметь в качестве заместителя(ей) одну или несколько групп, выбранных из формильной группы, алкильной группы, имеющей 1-6 углеродных атомов, и ацильной группы, имеющей 2-5 углеродных атомов; А1 представляет неполную структуру, представленную формулой (2) где Х2 и описанный выше R1 могут быть объединены с образованием циклической структуры, включающей часть исходного ядра, причем образованное при этом кольцо может содержать атом кислорода, атом азота или атом серы в качестве кольцеобразующего ...

ВЕЩЕСТВА, ПРОЯВЛЯЮЩИЕ АНТИМИКРОБНУЮ, АНТИГРИБКОВУЮ, АНТИПРОТОЗОЙНУЮ АКТИВНОСТИ

Предложен новый класс соединений для борьбы с возбудителями бактериальной, протозойной и грибковой природы. Соединения являются производными гетеронитроалкенов (диоксолы, оксазолы, имидазолы) с указанными ниже структурными формулами и эффективны в отношении грамположительных бактерий и грамотрицательных аэробов, грибков рода Candida, Trichophyton и др., трихомонад. Они могут использоваться при лечении раневых инфекций, грибковых поражений, септических состояний, пневмонии, трахомы, орнитоза, сальмонеллеза, в том числе в ветеринарии. 5 н.п. ф-лы, 5 табл. 1. 1,3-бензодиоксол-5-β-нитроэтилен 2. 1,3-бензодиоксол-5-β-нитропропилен 3. бензимидазол-5-β-нитропропилен 4. 2-метилбензимидазол-5-β -нитроэтилен 5. бензоксазол-5-β-нитроэтилен 6. 2-метилбензоксазол-5-β-нитропропилен ...

Антилепрозное средство "димоцифон"

Способ лечения больных лепрой

ANTIMIKROBIELL WIRKSAMES ODER ENDOTOXIN NEUTRALISIERENDES POLYPEPTID

SULFONAMIDETHER - SUBSTITUIERTE IMIDAZOCHINOLINE

[1,4']-BIPIPERIDIN VERBINDUNGEN

Oral verabreichte Peptide zur Linderung von Atherosklerose

Bridged piperazine derivatives

Bridged piperazine derivatives.

Novel dihydroxyhexanoic acid derivatives.

Bicyclic piperidine derivatives as antagonists of the CCR1 chemokine receptor.

Novel dihydroxyhexanoic acid derivatives.

Dihydroxyhexanoic acid derivatives of the greneral formula are useful to treat inflammation and other immune disorders.

Novel method of treatment

Novel method of treatment.

A method for the treatment of a disease or condition associated with increased numbers of neutrophils and/or neutrophil over-activation in a mammal such as a human, which method comprises administering an effective, non-toxic and pharmaceutically acceptable amount of a ppary agonist, such as compound (1), to a mammal in need thereof.

Novel dihydroxyexanoic acid derivatives

Bridged piperazine derivatives.

A compound of the formula or the pharmaceutically acceptable salt thereof; wherein a, c, d, k, l, m, w, x, yz, r1, and r4 are as defined, and useful to treat inflammation and other immune disorders.

Bicyclic piperidine derivatives as antagonists of the CCR1 chemokine receptor.

Heterocyclic amide derivatives.

A compound of the formula (1) or the pharmaceutically acceptable salt thereof; wherein R1,R2,R3 and R4 are as defined above useful to treat inflammation and other immune disorders.

Bridged piperazine derivatives

Tartrate salts of thiazolidinedione derivative

New antimicrobial compounds, their synthesis and their use for treatment of mammalian infections

Bicyclic piperidine derivatives as antagonists of the CCR1 chemokine receptor.

Heterocyclic amide derivatives.

New antimicrobial compounds, their synthesis and their use for treatment of mammalian infections

Heterocyclic amide derivatives

Novel dihydroxyexanoic acid derivatives

Novel method of treatment

New antimicrobial compounds, their synthesis and their use for treatment of mammalian infections

Bicyclic piperidine derivatives as antagonists of the CCR1 chemokine receptor.

Heterocyclic amide derivatives

TETRAHYDROPYRIDYL ALKYL HETEROZYKLE ONE, PROCEDURE FOR YOUR PRODUCTION AND PHARMACEUTICAL COMPOSITIONS IT CONTAINING

ANTIBIOTIC OR ANTI-PARASITIC COMPOSITIONS FROM ANIONI OR KATIONI DENDRIMEREN

ANTIMICROBIALLY EFFECTIVE OR ENDOTOXIN NEUTRALIZING POLYPEPTID

USE OF A REPLIKATIONDEFIZIENTEN SMALLPOX VIRUS VECTOR FOR THE INCREASE OF THE CD4+ T-ZELLIMMUNANTWORT AGAINST ANTIGEN

COMBINATIONS FOR THE TREATMENT OF MULTIPLE MYELOM

APHERESE OF LEUKOCYTES FROM BLOOD FOR THE TREATMENT OF HIV

ARALKYLTETRAHYDROPYRIDINE, THEIR PRODUCTION AND PHARMACEUTICAL COMPOSITIONS, THIS CONTAINING

EVALUATION OF PATIENTS WITH MORE PROGRESSIVE IMMUNOSUPPRESSION

NEW THIENO (2,3-D) PYRIMIDINDIONE, PROCEDURE FOR YOUR PRODUCTION AND YOUR USE IN the THERAPY

REKOMBINANTE MYKOBAKTERIELLE EXPRESS ION CARRIER AS WELL AS THEIR USE

Substituted acylanilides and methods of use thereof

This invention provides SARM compounds and uses thereof in treating a variety of diseases or conditions in a subject, including, , a muscle wasting disease and/or disorder or a bone-related disease and/or disorder.

NOVEL SUBSTITUTED INDOLES

Methods and compositions using immunomodulatory compounds for treatment and management of cancers and other diseases

Heterocyclic ether substituted imidazoquinolines

Human monoclonal antibodies to FC alpha receptor (CD89)

Receptor-binding compounds and methods for identifying them

Evaluation and treatment of patients with progressive immunosuppression

Novel compounds

Pyrimidine compounds and their use as modulators of chemokine receptor activity

Use of bisphosphonates for the prevention and treatment of infectious processes

Vaccine compositions comprising cd-1 antigens and t-cell stimulating compound and methods of use thereof

Use of anti-muscarinic agents and calcium channel blockers in combination

NOVEL COMPOUNDS

The invention provides compounds of general formula (I) wherein Q, R, R2, R4, R5, R6, R7 and R8 are as defined in the specification, processes for their preparation, pharmaceutical compositions containing them and their use in therapy.

METHOD OF INHIBITING PATHOGENICITY OF INFECTIOUS AGENTS

The present invention relates to methods of detecting or identifying inhibitors of a Z-DNA binding ligand to Z-DNA, methods of inhibiting the pathogenicity of an infectious agent, antiviral therapies, and compounds that inhibit complex formation between a Z-DNA binding ligand and Z-DNA.

THIOETHER SUBSTITUTED IMIDAZOQUINOLINES

Imidazoquinoline and tetrahydroimidazoquinoline compounds that contain thioether functionality at the 1-position are useful as immune response modifiers. The compounds and compositions of the invention can induce the biosynthesis of various cytokines and are useful in the treatment of a variety of conditions including viral diseases and neoplastic diseases.

PYRAZOLIDINOL COMPOUNDS

The invention provides the use of an optionally hydroxy-protected 4-hydroxy or hydroperoxy-3,5-dioxopyrazolidine or an equivalent wherein a pyrazolidine ri ng attached oxygen is replaced by a sulphur, or a physiologically acceptable sa lt thereof, for the manufacture of a medicament for use in therapy or prophylaxis. Additionally, the invention provides a method of combatting HIV infection which comprises administering to an HIV-infected patient a T- lymphocyte growth suppressing agent, preferably a pyrazolidinol, in an amoun t sufficient to suppress T-lymphocyte growth in said patient for a period sufficient to reduce the T-lymphocyte concentration in lymph nodes in said patient by at least 25 % said administration being repeated at intervals of at least 3 months.

ARYL ETHER SUBSTITUTED IMIDAZOQUINOLINES

Imidazoquinoline and tetrahydroimidazoquinoline compounds that contain ether and aryl or alkenyl functionality at the 1-position are useful as immune response modifiers. The compounds and compositions of the invention can induce the biosynthesis of various cytokines and are useful in the treatment of a variety of conditions including viral diseases and neoplastic diseases.

HETEROCYCLIC AMIDES USEFUL AS PROTEIN MODULATORS

Disclosed are compounds having the formula (I-N), wherein q, r, s, A, B, C, RA1, RA2, RB1, RB2, RC1, RC2, R3, R4, R5, R6, R14, R15, R16, and R17, are as defined herein, or a tautomer thereof, or a salt, particularly a pharmaceutically acceptable salt, thereof.

LONG-ACTING FORMULATIONS

This invention concerns pharmaceutical compositions for administration via intramuscular or subcutaneous injection, comprising micro- or nanoparticles of the anti- TB compound bedaquiline, suspended in an aqueous pharmaceutically acceptable carrier, and the use of such pharmaceutical compositions in the treatment and prophylaxis of a pathogenic mycobacterial infection.

INTERFERON-ALPHA INDUCED GENE

The present invention relates to identification of a gene upregulated by interferon-.alpha. administration corresponding to the cDNA sequences set forth in SEQ. ID. No. 1 or in SEQ. ID. No. 3. Determination of expression products of this gene is proposed as having utility in predicting responsiveness to treatment with interferon-.alpha. and other interferons which act at the Type 1 interferon receptor. Therapeutic use of the protein encoded by the same gene is also envisaged.

SUBSTITUTED ACYLANILIDES AND METHODS OF USE THEREOF

This invention provides SARM compounds and uses thereof in treating a var iety of diseases or conditions in a subject, including, inter alia, a muscle wasting disease and/or disorder or a bone-related disease and/or disorder.< /SDOAB> ...

ORALLY ADMINISTERED PEPTIDES TO AMELIORATE ATHEROSCLEROSIS

This invention provides novel peptides that ameliorate one or more symptoms of atherosclerosis (see Figure 23). The peptides comprises at least one class A amphipathic helix and at least one D-amino acid. The peptides are highly stable and readily administered via an oral route.

ORALLY ADMINISTERED PEPTIDES TO AMELIORATE ATHEROSCLEROSIS

This invention provides novel peptides that ameliorate one or more symptoms of atherosclerosis (see Figure 23). The peptides comprises at least one class A amphipathic helix and at least one D-amino acid. The peptides are highly stable and readily administered via an oral route.

TETRAHYDRONAPHTHALEN-2-OL DERIVATIVES

The present invention relates to novel tetrahydronaphthalen-2-ol derivatives, to pharmaceutical compositions comprising these compounds and to their use in therapy, in particular to their use for the manufacture of a medicament for the prevention or treatment of lower urinary tract symptoms,benign prostate hyperplasia,prostate cancer,hot flushes, anxiety, depression, breast cancer, medullary thyroid carcinoma, ovarian cancer, inflammatory bowel disease, arthritis, endometriosis, and colon cancer.

METHODS AND COMPOSITIONS USING 3-(4-AMINO-1-OXO-1,3-DIHYDROISOINDOL-2-YL)-PIPERIDINE-2,6-DIONE FOR TREATMENT AND MANAGEMENT OF HEPATOCELLULAR CARCINOMA

Uses for treating, preventing and/or managing hepatocellular carcinoma. Specific embodiments encompass the use of an immunomodulatory compound alone or in combination with an additional active ingredient. The invention further relates to reducing or avoiding adverse side effects associated with chemotherapy, radiation therapy, hormonal therapy, biological therapy or immunotherapy which comprise the use of an immunomodulatory compound. Pharmaceutical compositions, single unit dosage forms, and commercial packages suitable for use of the invention are also disclosed. In one embodiment, there is provided use of a compound of the formula (see above formula) for treating, preventing and/or managing hepatocellular carcinoma.

METHODS AND COMPOSITIONS USING 3-(4-AMINO-1-OXO-1,3-DIHYDRO-ISOINDOL-2-YL)-PIPERIDINE-2,6-DIONE FOR TREAMENT AND MANAGEMENT OF SOLID TUMORS

Uses for treating, preventing and/or managing solid tumors. Specific embodiments encompass the use of an immunomodulatory compound alone or in combination with an additional active ingredient. The invention further relates to reducing or avoiding adverse side effects associated with chemotherapy, radiation therapy, hormonal therapy, biological therapy or immunotherapy which comprise the use of an immunomodulatory compound. Pharmaceutical compositions, single unit dosage forms, and commercial packages suitable for use of the invention are also disclosed. In one embodiment, the immunomodulatory compound is a compound of the formula (see above formula) ...

METHODS AND COMPOSITIONS USING 3-(4-AMINO-1-OXO-1,3-DIHYDRO-ISOINDOL-2-YL)-PIPERIDINE-2,6-DIONE OR 4-(AMINO)-2-(2,6-DIOXO(3-PIPERIDYL))-ISOINDOLINE-1,3-DIONE FOR TREATMENT AND MANAGEMENT OF AMYLOIDOSIS

... ²² Uses for treating, preventing and/or managing amyloidosis. Specific ²embodiments encompass the use of an immunomodulatory compound alone or in ²combination with an additional active ingredient. The invention further ²relates to ²reducing or avoiding adverse side effects associated with chemotherapy, ²radiation ²therapy, hormonal therapy, biological therapy or immunotherapy which comprise ²the ²use of an immunomodulatory compound. Pharmaceutical compositions, single unit ²dosage forms, and commercial packages suitable for use of the invention are ²also ²disclosed. In one embodiment, immunomodulatory compound is a compound of the ²formula (see formula I). ²In another embodiment, the immunomodulatory compound is a compound of ²the formula (see formula II).² ...

COMPOUNDS HAVING MUSCARINIC RECEPTOR ANTAGONIST AND BETA2 ADRENERGIC RECEPTOR AGONIST ACTIVITY

The present invention relates to compounds acting both as muscarinic receptor antagonists and beta2 adrenergic receptor agonists of general formula I, to processes for their preparation, to compositions comprising them, to therapeutic uses for the prevention or treatment of broncho-obstructive or inflammatory diseases, and combinations with other pharmaceutical active ingredients. Various different groups can be represented by Q, Z, Y, G, Ri, R2 M and R4- ...

SUBSTITUTED 2-(2,6-DIOXO-3-FLUOROPIPERIDIN-3-YL)-ISOINDOLINES AND THEIR USE TO REDUCE TNF.ALPHA. LEVELS

A chiral compound is described, in racemic, (R)- or (S)- form, which is a 2-(2,6-dioxo-3-fluoropiperidin-3-yl)- isoindoline of the formula: (see formula I) in which Y is oxygen or H2 and each of R1, R2, R3, and R4, independently of the others, is hydrogen, halo, alkyl of 1 to 4 carbon atoms, alkoxy of 1 to 4 carbon atoms, or amino, or the acid addition salts of said 2-(2,6-dioxo-3- fluoropiperidin-3-yl)-isoindolines which contain a nitrogen atom capable of being protonated. 1-Oxo-2-(2,6-dioxo-3- fluoropiperidin-3-yl)-isoindolines and 1,3-dioxo-2-(2,6- dioxo-3-fluoropiperidin-3-yl)-isoindolines reduce the levels of inflammatory cytokines such as TNF.alpha. in a mammal. A typical embodiment is 1,3-dioxo-2-(2,6-dioxo-3--fluoropiperidin-3-yl)- isoindoline.

Method for preparing thiotétrazoles non-nucleoside reverse transcriptase inhibitors (ITINN) for the treatment of HIV.

L’invention concerne un procédé de préparation de thiotétrazoles comprenant une étape de transformation de la N-(naphtalén-1-yl)-1,2,3,4-thiatriazol-5-amine en un anion thiolate dans du benzène en présente de triéthylamine, et une étape de réaction de cet anion thiolate avec un électrophile bromure. Ces thiotétrazoles sont utilisables en tout qu’inhibiteurs de transcriptase inverse non nucléosidiques/ITINN) pour le traitement du VIH. En particulier, le 2-((1-naphtalén-1-yl)-1H-tétrazol-5-yl) thio)-N-(2-nitrophényl) acétamide est un ITINN puissant avec une activité nanomolaire. L’invention porte aussi sur un procédé de préparation d’un thiotétrazole à partir d’un thiatriazole à substitution N-alkyle en C1.

PEPTIDE, COMPOSITION FOR ORAL ADMINISTRATION, SET (VERSIONS), METHOD OF REDUCING SYMPTOM INTENSITY ATHEROSCLEROSIS (VERSIONS) AND METHOD FOR FACILITATING OR PREVENTION OF CORONARY COMPLICATIONS IN MAMMAL (VERSIONS)

COMBINED METHOD OF TREATMENT BASED ON INHIBITORS OF SIGNAL OF PD-AND-1

BICYCLIC PIPERIDINE DERIVATIVES AS ANTAGONISTS OF CHEMOKINE RECEPTOR CCR1

DERIVATIVES OF HETEROCYCLIC AMIDE

NEW METHOD OF TREATMENT OF

HETEROCYCLIC AMIDES, USEFUL AS MODULATORS OF PROTEINS

METHODS FOR TREATMENT OF MICROBIAL INFECTIONS IN HUMANS AND ANIMALS

ЛЕКАРСТВЕННОЕ СРЕДСТВО

Представленное изобретение относится к лекарственному средству, включающему активное вещество и целевые добавки, причем в качестве активного вещества оно содержит (2,4-дигидрокси-6-метил-5-пиримидил)-(4-пиридинкарбонилгидразинил)сульфон формулы (III) или его фармацевтически приемлемые соли и изомеры в эффективном количестве. Кроме того предложенное лекарственное средство дополнительно может содержать по меньшей мере одно противотуберкулезное средство, такое как изониозид, рефампицин, пиразинамид. Предложенное лекарственное средство может быть изготовлено в виде таблеток, комбинированных таблеток, капсул, сиропа и инъекций.

HETEROCYCLIC AMIDES, USEFUL AS MODULATORS OF PROTEINS

NEW DERIVATIVES OF DIHYDRO KSIGEKSANOVOI ACID

Настоящее изобретение раскрывает производные дигидроксигексановой кислоты общей формулы (I)которые полезны для лечения воспаления и других иммунных нарушений.Отчет о международном поиске был опубликован 1999.10.21. The present invention discloses dihydroxyhexanoic acid derivatives of general formula (I) which are useful for the treatment of inflammation and other immune disorders. The international search report was published 1999.10.21.

ARYL ETHER SUBSTITUTED IMIDAZOQUINOLINES, PHARMACEUTICAL COMPOSITION BASED THEREON

HETEROCYCLIC AMIDE DERIVATIVES

ГЕТЕРОЦИКЛИЧЕСКИЕ АМИДЫ, ПРИГОДНЫЕ В КАЧЕСТВЕ МОДУЛЯТОРОВ БЕЛКОВ

В изобретении раскрыты соединения, имеющие формулу где q, r, s, A, B, C, RA1, RA2, RB1, RB2, RC1, RC2, R3, R4, R5, R6, R14, R15, R16 и R17 имеют значения, определенные в описании, или их таутомер, или соль, в частности их фармацевтически приемлемая соль.

ARALKILTETRAGIDRO PYRIDINES, THEIR PRODUCTION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM

ИММУНОМОДУЛЯТОР С АНТИМИКРОБНОЙ И АНТИМИКОБАКТЕРИАЛЬНОЙ АКТИВНОСТЬЮ, СПОСОБ ЕГО ПОЛУЧЕНИЯ И ЛЕКАРСТВЕННЫЙ ПРЕПАРАТ ДЛЯ ЛЕЧЕНИЯ МИКОБАКТЕРИОЗОВ, ХРОНИЧЕСКИХ НЕСПЕЦИФИЧЕСКИХ ЗАБОЛЕВАНИЙ ЛЕГКИХ, ЗАБОЛЕВАНИЙ, ПЕРЕДАЮЩИХСЯ ПОЛОВЫМ ПУТЕМ, И ИММУНОДЕФИЦИТА НА ИХ ОСНОВЕ

Изобретение относится к области медицины, точнее к новому иммуномодулятору с антимикробной и антимикобактериальной активностью следующей формулы: Его получают взаимодействием эквимолекулярных количеств 6-метилурацил-5-сульфохлорида и изониазида в ацетонитриле при повышенной температуре. Препарат практически не токсичен (ЛД50 в остром опыте более 7000 мг/кг), проявляет, по данным клинических испытаний, выраженную иммуномодулирующую и антимикобактериальную активность. Может быть использован для коррекции различных иммунодефицитов, включая ВИЧ-носительство, и в терапии микобактериозов (лепра, туберкулез и другие). Назначается для применения внутрь и парентерально. Заявляемое соединение является действующим веществом лекарственного препарата, применяемого при вторичных иммунодефицитах и микобактериозах.

Heterocyclic Amide Derivatives, Pharmaceutical Compositions Containing the Same and Use Thereof for Treatment of Inflammation and Other Immune Disorders

NEW DERIVATIVES ANTI-INFECTIEUX, THEIR METHOD OF PREPARATION, PHARMACEUTICAL COMPOSITIONS THE CONTAINER AND THEIR USES INTO THERAPEUTIC.

treatment for mycobacterial infections with ciclipostina

NOVEL COMPLEXES OF FATTY ACID ESTERS OF POLYHYDROXYALKANES AND NIACINAMIDE

NOVEL COMPOUNDS AS ANTI-MYCOBACTERIALS

The present disclosure relates to antibacterial compounds. In particular, the compounds are for inhibiting the growth of bacteria, particularly Mycobacterium tuberculosis (Mtb), and/or targeting bacteria having phospho-MurNAc-pentapeptidetranslocase. The present disclosure also relates to compositions containing these compounds and methods of the use of these compounds and compositions.

USES OF PPAR-GAMMA AGONISTS IN NEUTROPHIL-INDUCED DISEASES

A method for treatment of a disease or condition associated with increased numbers of neutrophils and/or neutrophil over-activation in a mammal such as a human, which method comprises administering an effective, non-toxic and pharmaceutically acceptable amount of a PPARγ agonist, such as fosiglitazone (BRL49653) or its maleate salts, or pioglitazone, to a mammal in need thereof.

USE OF OPRI LIPOPROTEIN FROM PSEUDOMONAS AS A TH1 INDUCING NATURAL ADJUVANT FOR HETEROLOGOUS ANTIGENS

The present invention relates to the use of the major OprI lipoprotein of Pseudomonas aeruginosa to elicit a Type-1 immune response towards a heterologous antigen. The invention relates specifically to the use of Oprl - antigen fusion proteins to elicit said Typ-1 response. More particurarly, the present invention is directed to pharmaceutical formulations comprising Oprl and/or Oprl fusion proteins, optionnaly together with a suitable excipient, to stimulate the Th1 dependent, cellular immune response.

Stabilized biodegradable neurotoxin implants

Biodegradable neurotoxin implants and methods of making and using such implants are provided. Biodegradable neurotoxin implants include a neurotoxin, a biodegradable polymer component, and an acidity regulating component. The biodegradable polymer component is effective in controlling the release of the neurotoxin from the implant when the implant is located in a patient's body. The acidity regulating component is effective in maintaining a pH of the implant in a desired range that may be effective in stabilizing the neurotoxin as the implant biodegrades when the implant is located in a patient's body. In one embodiment, an implant includes a botulinum toxin, a biodegradable polymer, and either monomers from which a biodegradable polymer is derived or oligomers including monomeric units substantially identical to a monomer from which a biodegradable polymer is derived, or a combination of such monomers and oligomers. The oligomers and biodegradable polymer may be derived from a single type of monomer. The implants disclosed herein may be administered to a human or animal patient in which a therapeutic effect is desired for prolonged periods of time.

Methods for reducing granulomatous inflammation

This document provides methods and materials for reducing bacterial induced granulomatous inflammation in a mammal using agents that reduce B7-H1 expression or activity.

4-substituted benzoxaborole compounds and uses thereof

Substituted benzoxaboroles whose structure comprises Formula (III), wherein R 3 is selected from —CH 3 , —CH 2 CH 3 , —CH 2 ═CH 2 , —CH 2 CH 2 CH 3 , —CH(CH 3 ) 2 , —CH 2 CH 2 ═CH 2 , and cyclopropyl, R 1 and R 2 are each independently selected from H, —CH 3 , —CH 2 CH 3 , —CH 2 CH 2 CH 3 , and —CH(CH 3 ) 2 ; compositions containing such compounds, their use in therapy, including their use as anti-mycobacterial agents, for example in the treatment of a mycobacterial infection in a mammal, and methods for the preparation of such compounds, are provided.

New Polyimino Ketoaldehydes

where n1 is the number of carbon atoms connected to nitrogen atom by a double bond and can take on values of 25 to 41, and where n2 is the number of —CH2— groups and can take on values of 15 to 23, as well as their biologically acceptable salts and solvates.

Methods of using a vaccine composition containing synthetic adjuvant

Compositions and methods, including vaccines and pharmaceutical compositions for inducing or enhancing an immune response are disclosed based on the discovery of useful immunological adjuvant properties in a synthetic, glycopyranosyl lipid adjuvant (GLA) that is provided in substantially homogeneous form. Chemically defined, synthetic GLA offers a consistent vaccine component from lot to lot without the fluctuations in contaminants or activity that compromise natural-product adjuvants. Also provided are vaccines and pharmaceutical compositions that include GLA and one or more of an antigen, a Toll-like receptor (TLR) agonist, a co-adjuvant and a carrier such as a pharmaceutical carrier.

Treatment and prevention of diseases mediated by microorganisms via drug-mediated manipulation of the eicosanoid balance

The invention provides a method of enhancing the efficacy of antibiotic treatment of tuberculosis, trypanosomiasis, leprosy, and leishmaniasis involving co-administering to a mammal undergoing antibiotic treatment therapeutically effective amounts of a first compound that is an inhibitor of 5-lipoxygenase and optionally a second compound that is a product of the cyclooxygenase pathways. The invention also provides a pharmaceutical composition comprising an antibiotic, an inhibitor of 5-lipoxygenase, and a product of the cyclooxygenase pathways.

TRIPLE COMBINATION

The invention provides a combination comprising 4-methyl-8-phenoxy-1-(2-phenylethyl)-2,3-dihydro-1H-pyrrolo[3,2-c]quinoline or a pharmaceutically acceptable derivative thereof, mupirocin or a pharmaceutically acceptable derivative thereof and neomycin or a pharmaceutically acceptable derivative thereof. This triple combination is particularly useful for the treatment and/or prevention of microbial infections. 1. A combination comprising 4-methyl-8-phenoxy-1-(2-phenylethyl)-2 ,3-dihydro-1H-pyrrolo[3 ,2-c]quinoline or a pharmaceutically acceptable derivative thereof , mupirocin or a pharmaceutically acceptable derivative thereof and neomycin or a pharmaceutically acceptable derivative thereof.2. The combination according to claim 1 , wherein the concentration of 4-methyl-8-phenoxy-1-(2-phenylethyl)-2 claim 1 ,3-dihydro-1H-pyrrolo[3 claim 1 ,2-c]quinoline or a pharmaceutically acceptable derivative thereof is from about 0.01 to 2% by weight of the total combination.3. The combination according to claim 1 , wherein the concentration of mupirocin or a pharmaceutically acceptable derivative thereof is from 0.2 to 2% by weight of the total combination.4. The combination according to claim 1 , wherein the concentration of neomycin or a pharmaceutically acceptable derivative thereof is from 0.05 to 1% by weight of the total combination.5. A method of preventing and/or treating a microbial infection in a mammal claim 1 , wherein the method comprises administering a combination comprising 4-methyl-8-phenoxy-1-(2-phenylethyl)-2 claim 1 ,3-dihydro-1H-pyrrolo[3 claim 1 ,2-c]quinoline or a pharmaceutically acceptable derivative thereof claim 1 , mupirocin or a pharmaceutically acceptable derivative thereof and neomycin or a pharmaceutically acceptable derivative thereof.6. The method according to for use in killing multiplying claim 5 , non-multiplying or clinically latent microorganisms associated with a microbial infection.7. A method of using 4-methyl-8-phenoxy-1-(2-phenylethyl ...

Methods of using gpr119 receptor to identify compounds useful for increasing bone mass in an individual

The present invention relates to methods of using GPR119 receptor to identify compounds useful for increasing bone mass in an individual. Agonists of GPR119 receptor are useful as therapeutic agents for treating or preventing a condition characterized by low bone mass, such as osteoporosis, and for increasing bone mass in an individual. Agonists of GPR119 receptor promote bone formation in an individual.

具有cxcr3拮抗剂活性的取代的杂环化合物

本发明申请公开了一种化合物或所述化合物的对映体、立体异构体、旋转异构体、互变异构体、外消旋体或前药，或所述化合物的药学上可接受的盐、溶剂合物或酯，或所述前药的药学上可接受的盐、溶剂合物或酯，所述化合物或其药学上可接受的盐、溶剂合物或酯具有式(1)所示通用结构，其中各部分定义同本文。还公开了用式(1)化合物治疗趋化因子介导的疾病的方法，例如对某些疾病和病症的姑息疗法、治疗疗法、预防疗法，这些疾病有例如炎性疾病(一个或多个非限定性实例包括银屑病)、自身免疫性疾病(一个或多个非限定性实例包括类风湿性关节炎、多发性硬化)、移植排斥(一个或多个非限定性实例包括同种异体移植排斥、异种移植排斥)、感染性疾病(例如结核样型麻风)、固定性药疹、皮肤迟发型过敏反应、I型糖尿病、病毒性脑膜炎和肿瘤。

分枝杆菌比较基因组学作为鉴定分枝杆菌病的诊断、预防或治疗靶的工具

本发明涉及编码蛋白质或部分蛋白质的纯化核苷酸序列或者多核苷酸的选择方法，所述的蛋白质或部分蛋白质具有至少一种决定分枝杆菌菌种的生存或毒力的必需功能，所述的选择方法是将结核分枝杆菌的基因组序列与麻风分枝杆菌的基因组序列对齐排列进行比较基因组分析。并且本发明公开了结核分枝杆菌及麻风分枝杆菌标志性多肽，编码这些多肽的核苷酸，以及使用这些核苷酸及其编码的多肽的方法。

Methods of using GPR119 receptor to identify compounds useful for increasing bone mass in an individual

본 발명은 특정 개체에게서 골 질량을 증가시키는 데에 유용한 화합물을 확인하기 위해 GPR119 수용체를 사용하는 방법에 관한 것이다. GPR119 수용체의 작동제는 낮은 골 질량을 특징으로 하는 질환, 예를 들어 골다공증을 치료 또는 예방하고, 특정 개체에게서 골 질량을 증가시키기 위한 치료제로서 유용하다. GPR119 수용체의 작동제는 특정 개체에게서 골 형성을 증진시켜 준다. The present invention is directed to methods of using the GPR119 receptor to identify compounds useful for increasing bone mass in certain individuals. Agonists of the GPR119 receptor are useful as therapeutic agents for treating or preventing diseases characterized by low bone mass, such as osteoporosis, and for increasing bone mass in certain individuals. Agonists of the GPR119 receptor enhance bone formation in certain individuals. GPR119 수용체의 작동제, 골다공증 치료, 골 질량 증가 GPR119 receptor agonists, osteoporosis treatment, bone mass increase

METHODS AND COMPOSITIONS FOR DISEASE TREATMENT

Metalloenzyminhibitorforbindelser

Methods for reducing granulomatous inflammation

This document provides methods and materials for reducing bacterial induced granulomatous inflammation in a mammal using agents that reduce B7-H1 expression or activity.

USE OF 2.2-CYCLOLIGNANES AS PROMOTERS FOR THE PIGMENTATION OF SKIN OR HAIR

La présente invention concerne l'utilisation de 2,2'-cyclolignanes pour la préparation d'une composition destinée à induire et/ou restaurer et/ou stimuler une pigmentation de la peau, des poils ou des cheveux ou encore destinée à préserver l'intégrité du cheveu, à limiter la chute des cheveux et à stimuler la repousse capillaire.Enfin, la présente invention a pour objet un procédé de traitement cosmétique d'une peau ou de cheveux nécessitant une pigmentation, comprenant l'application topique sur ladite peau ou lesdits cheveux d'au moins un 2,2'-cyclolignane, ou d'un sel pharmaceutiquement ou cosmétiquement acceptable dudit 2,2'-cyclolignane, représenté par la formule (II), dans un milieu physiologiquement acceptable.

Vaccine composition containing synthetic adjuvant

Compositions and methods, including vaccines and pharmaceutical compositions for inducing or enhancing an immune response are disclosed based on the discovery of useful immunological adjuvant properties in a synthetic, glucopyranosyl lipid adjuvant (GLA) that is provided in substantially homogenous form. Chemically defined, synthetic GLA offers a consistent vaccine component from lot to lot without the fluctuations in contaminants or activity that compromise natural-product adjuvants. Also provided are vaccines and pharmaceutical compositions that include GLA and one or more of an antigen, a Toll-like receptor (TLR) agonist, a co-adjuvant and a carrier such as a pharmaceutical carrier.

Vaccine composition containing synthetic adjuvant

Compositions and methods, including vaccines and pharmaceutical compositions for inducing or enhancing an immune response are disclosed based on the discovery of useful immunological adjuvant properties in a synthetic, glucopyranosyl lipid adjuvant (GLA) that is provided in substantially homogenous form. Chemically defined, synthetic GLA offers a consistent vaccine component from lot to lot without the fluctuations in contaminants or activity that compromise natural-product adjuvants. Also provided are vaccines and pharmaceutical compositions that include GLA and one or more of an antigen, a Toll-like receptor (TLR) agonist, a co-adjuvant and a carrier such as a pharmaceutical carrier.

Methods of using gpr119 receptor to identify compounds useful for increasing bone mass in an individual

Substituted 2-(2,6-dioxo-3-fluoropiperidin-3-yl)-isoindolines and method of reducing inflammatory cytokine levels

1-Oxo-2-(2,6-dioxo-3-fluoropiperidin-3-yl)isoindolines and 1,3-dioxo-2-(2,6-dioxo-3-fluoropiperidin-3-yl)isoindolines reduce the levels of inflammatory cytokines such as TNFα in a mammal. A typical embodiment is 1,3-dioxo-2-(2,6-dioxo-3-fluoropiperidin-3 -yl)-isoindoline.

Spiroisoxazoline compounds having an activity potentiating the activity of an antibiotic

本发明涉及通式(I)的螺异噁唑啉化合物：

Stent

FIELD: medicine. SUBSTANCE: invention refers to medicine, more specifically to stents and bag catheters with improved rapamycin release coating, and also to methods for producing such coatings. EFFECT: production of stents and bag catheters with improved rapamycin release coating. 10 dwg, 24 ex 2432183 С9 Ко РОССИЙСКАЯ ФЕДЕРАЦИЯ ‚ (19) (1) < дэ < (3) ааа ЮО Ко ом К о ке. С9 (510) МПК АбЛЬ 31/10 (2006.01) АбЛЬ 3116 (2006.01) Аб1Е 2/06 (2006.01) А61К 31/436 (2006.01) Аб/Р 3706 (2006.01) “ ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ (12) СКОРРЕКТИРОВАННОЕ ОПИСАНИЕ ИЗОБРЕТЕНИЯ К ПАТЕНТУ Примечание: библиография отражает состояние при переиздании (21)(22) Заявка: 2009104348/15, 03.07.2007 (24) Дата начала отсчета срока действия патента: 03.07.2007 Приоритет(ы): (30) Конвенционный приоритет: 03.07.2006 РЕ 102006030586.8 (43) Дата публикации заявки: 20.08.2010 Бюл. № 23 (45) Опубликовано: 27.10.2011 (15) Информация о коррекции: Версия коррекции №1 ( С2) (48) Коррекция опубликована: 10.03.2012 Бюл. №7 (56) Список документов, цитированных в отчете о поиске: ОЕ 102004020856 АТ, 14.04.2005. ЕР 0568310 А, 03.11.19993. У быте ТУ, Сотратзоп оЁ те Берайп соа{ед уз Пе ипсожед Домеп-по шЯчепсе оп ге${епо$1$ ог сшиса| осоше. Еогореап Неац 7., 2001 Ос; 22(19): 1808-16 (реферат). КП 2005133199 А, 10.02.2006. (85) Дата начала рассмотрения заявки РСТ на национальной фазе: 10.02.2009 (86) Заявка РСТ: РЕ 2007/001173 (03.07.2007) (87) Публикация заявки РСТ: УГО 2008/003298 (10.01.2008) Адрес для переписки: 127055, Москва, а/я 11, Н.К. Попеленскому (72) Автор(ы): КЮШТЕРС Сабина (ОЕ), ХОРРЕС Роланд (ОЕ), ХОФМАН Михель (ОЕ), ХОФМАН Эрика (ОЕ) (73) Патентообладатель(и): Хемотек АГ (ОЕ) (54) СТЕНТ (57) Реферат: Изобретение относится к медицине, конкретно к стентам и катетерным баллонам с Стр.: 1 улучшенным покрытием для высвобождения рапамицина, а также к способам получения таких покрытий. 14 з.п. ф-лы, 5 табл., 10 ил. ЗСУ сС ПЧ 6Э 2432183 С9 Ко КОЗАМ ЕЕРЕКАТПОМ ЕЕРЕКАГ, ЗЕВУ1СЕ РОК ...

Treatment of secondary immune deficiency

Treatment and prevention of diseases mediated by microorganisms via drug-mediated manipulation of the eicosanoid balance

The invention provides a method of enhancing the efficacy of antibiotic treatment of tuberculosis, trypanosomiasis, leprosy, and leishmaniasis involving co-administering to a mammal undergoing antibiotic treatment therapeutically effective amounts of a first compound that is an inhibitor of 5-lipoxygenase and optionally a second compound that is a product of the cyclooxygenase pathways. The invention also provides a pharmaceutical composition comprising an antibiotic, an inhibitor of 5-lipoxygenase, and a product of the cyclooxygenase pathways.

Vaccine composition containing synthetic adjuvant

Compositions and methods, including vaccines and pharmaceutical compositions for inducing or enhancing an immune response are disclosed based on the discovery of useful immunological adjuvant properties in a synthetic, glucopyranosyl lipid adjuvant (GLA) that is provided in substantially homogeneous form. Chemically defined, synthetic GLA offers a consistent vaccine component from lot to lot without the fluctuations in contaminants or activity that compromise natural-product adjuvants. Also provided are vaccines and pharmaceutical compositions that include GLA and one or more of an antigen, a Toll-like receptor (TLR) agonist, a co-adjuvant and a carrier such as a pharmaceutical carrier.

Vaccine composition comprising a synthetic adjuvant

Methods of using a vaccine composition containing synthetic adjuvant

Compositions and methods, including vaccines and pharmaceutical compositions for inducing or enhancing an immune response are disclosed based on the discovery of useful immunological adjuvant properties in a synthetic, glycopyranosyl lipid adjuvant (GLA) that is provided in substantially homogeneous form. Chemically defined, synthetic GLA offers a consistent vaccine component from lot to lot without the fluctuations in contaminants or activity that compromise natural-product adjuvants. Also provided are vaccines and pharmaceutical compositions that include GLA and one or more of an antigen, a Toll-like receptor (TLR) agonist, a co-adjuvant and a carrier such as a pharmaceutical carrier.

Methods of using a vaccine composition containing synthetic adjuvant

Compositions and methods, including vaccines and pharmaceutical compositions for inducing or enhancing an immune response are disclosed based on the discovery of useful immunological adjuvant properties in a synthetic, glucopyranosyl lipid adjuvant (GLA) that is provided in substantially homogeneous form. Chemically defined, synthetic GLA offers a consistent vaccine component from lot to lot without the fluctuations in contaminants or activity that compromise natural-product adjuvants. Also provided are vaccines and pharmaceutical compositions that include GLA and one or more of an antigen, a Toll-like receptor (TLR) agonist, a co-adjuvant and a carrier such as a pharmaceutical carrier.

Vaccine composition containing synthetic adjuvant

Compositions and methods, including vaccines and pharmaceutical compositions for inducing or enhancing an immune response are disclosed based on the discovery of useful immunological adjuvant properties in a synthetic, glucopyranosyl lipid adjuvant (GLA) that is provided in substantially homogeneous form. Chemically defined, synthetic GLA offers a consistent vaccine component from lot to lot without the fluctuations in contaminants or activity that compromise natural-product adjuvants. Also provided are vaccines and pharmaceutical compositions that include GLA and one or more of an antigen, a Toll-like receptor (TLR) agonist, a co-adjuvant and a carrier such as a pharmaceutical carrier.

Vaccine composition containing synthetic adjuvant

Compositions and methods, including vaccines and pharmaceutical compositions for inducing or enhancing an immune response are disclosed based on the discovery of useful immunological adjuvant properties in a synthetic, glucopyranosyl lipid adjuvant (GLA) that is provided in substantially homogeneous form. Chemically defined, synthetic GLA offers a consistent vaccine component from lot to lot without the fluctuations in contaminants or activity that compromise natural-product adjuvants. Also provided are vaccines and pharmaceutical compositions that include GLA and one or more of an antigen, a Toll-like receptor (TLR) agonist, a co-adjuvant and a carrier such as a pharmaceutical carrier.

Vaccine composition containing synthetic adjuvant

Compositions and methods, including vaccines and pharmaceutical compositions for inducing or enhancing an immune response are disclosed based on the discovery of useful immunological adjuvant properties in a synthetic, glucopyranosyl lipid adjuvant (GLA) that is provided in substantially homogeneous form. Chemically defined, synthetic GLA offers a consistent vaccine component from lot to lot without the fluctuations in contaminants or activity that compromise natural-product adjuvants. Also provided are vaccines and pharmaceutical compositions that include GLA and one or more of an antigen, a Toll-like receptor (TLR) agonist, a co-adjuvant and a carrier such as a pharmaceutical carrier.

Vaccine composition containing synthetic adjuvant

Compositions and methods, including vaccines and pharmaceutical compositions for inducing or enhancing an immune response are disclosed based on the discovery of useful immunological adjuvant properties in a synthetic, glucopyranosyl lipid adjuvant (GLA) that is provided in substantially homogeneous form. Chemically defined, synthetic GLA offers a consistent vaccine component from lot to lot without the fluctuations in contaminants or activity that compromise natural-product adjuvants. Also provided are vaccines and pharmaceutical compositions that include GLA and one or more of an antigen, a Toll-like receptor (TLR) agonist, a co-adjuvant and a carrier such as a pharmaceutical carrier.

Inhibitors of serine protease activity and their use in methods and compositions for treatment of bacterial infections

A novel method of treating and preventing bacterial diseases is provided. In particular, the present invention relates to compositions and methods for inhibition of Gram negative, Gram positive and acid fast bacilli in general and tuberculosis (TB), mycobacterium avium complex (MAC), and anthrax in particular. Thus, the invention relates to modulation of cellular activities, including macrophage activity, and the like. More particularly, the present invention relates to the inhibitory compounds comprising naturally occurring and man-made inhibitors of serine protease.

Inhibitors of serine protease activity and their use in methods and compositions for treatment of bacterial infections

A novel method of treating and preventing bacterial diseases is provided. In particular, the present invention relates to compositions and methods for inhibition of Gram negative, Gram positive and acid fast bacilli in general and tuberculosis (TB), mycobacterium avium complex (MAC), and anthrax in particular. Thus, the invention relates to modulation of cellular activities, including macrophage activity, and the like. More particularly, the present invention relates to the inhibitory compounds comprising naturally occurring and man-made inhibitors of serine protease.

Compositions of, and methods for, alpha-1 anti trypsin Fc fusion molecules

A novel method of treating and preventing bacterial diseases is provided. In particular, the present invention relates to compositions and methods for inhibition of Gram negative, Gram positive and acid fast bacilli in general and tuberculosis (TB), mycobacterium avium complex (MAC), and anthrax in particular. Thus, the invention relates to modulation of cellular activities, including macrophage activity, and the like. More particularly, the present invention relates to the inhibitory compounds comprising naturally occurring and man-made inhibitors of serine protease.

Compositions of, and methods for, alpha-1 anti trypsin Fc fusion molecules

A novel method of treating and preventing bacterial diseases is provided. In particular, the present invention relates to compositions and methods for inhibition of Gram negative, Gram positive and acid fast bacilli in general and tuberculosis (TB), mycobacterium avium complex (MAC), and anthrax in particular. Thus, the invention relates to modulation of cellular activities, including macrophage activity, and the like. More particularly, the present invention relates to the inhibitory compounds comprising naturally occurring and man-made inhibitors of serine.

Compositions of, and methods for, alpha-1 antitrypsin Fc fusion molecules

A novel method of treating and preventing bacterial diseases is provided. In particular, the present invention relates to compositions and methods for inhibition of Gram negative, Gram positive and acid fast bacilli in general and tuberculosis (TB), mycobacterium avium complex (MAC), and anthrax in particular. Thus, the invention relates to modulation of cellular activities, including macrophage activity, and the like. More particularly, the present invention relates to the inhibitory compounds comprising naturally occurring and man-made inhibitors of serine protease.

Compositions of, and methods for, alpha-1 anti trypsin Fc fusion molecules

A novel method of treating and preventing bacterial diseases is provided. In particular, the present invention relates to compositions and methods for inhibition of Gram negative, Gram positive and acid fast bacilli in general and tuberculosis (TB), Mycobacterium avium complex (MAC), and anthrax in particular. Thus, the invention relates to modulation of cellular activities, including macrophage activity, and the like. More particularly, the present invention relates to the inhibitory compounds comprising naturally occurring and man-made inhibitors of serine protease.

Catheter cylinder

FIELD: pharmacology. SUBSTANCE: invention relates to a catheter cylinder, the coating of which consists of paclitaxel and at least one adjuvant selected from the group consisting of tributyl citrate, triethyl citrate and their acetylated derivatives. EFFECT: invention provides immediate release of the antiproliferative agent for a short time interval of 30 to 60 seconds. 3 cl, 10 dwg, 4 tbl, 24 ex РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) (13) 2 633 723 C2 (51) МПК A61L 29/12 (2006.01) A61L 29/16 (2006.01) A61K 47/44 (2006.01) A61F 2/82 (2013.01) A61K 31/337 (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ (12) ОПИСАНИЕ ИЗОБРЕТЕНИЯ К ПАТЕНТУ (21)(22) Заявка: 2011122392, 02.06.2011 (24) Дата начала отсчета срока действия патента: 03.07.2007 Дата регистрации: (73) Патентообладатель(и): Хемотек АГ (DE) Приоритет(ы): (30) Конвенционный приоритет: (56) Список документов, цитированных в отчете о поиске: US 20060083768 A1, 20.04.2006. US 20030064965 A1, 03.04.2003. US 20020042645 A1, 11.04.2002. US 20050288481 A1, 29.12.2005. US 20060067977A1, 30.03.2006. (43) Дата публикации заявки: 10.12.2012 Бюл. № 34 (45) Опубликовано: 17.10.2017 Бюл. № 29 2 6 3 3 7 2 3 R U (54) Катетерный баллон (57) Реферат: Изобретение относится к катетерному баллону, покрытие которого состоит из паклитаксела и по меньшей мере одного адъюванта, выбранного из группы, включающей трибутилцитрат, триэтилцитрат и их ацетилированные производные. Изобретение Стр.: 1 обеспечивает немедленное высвобождение антипролиферативного агента в течение короткого интервала времени, составляющего от 30 до 60 секунд. 2 з.п. ф-лы, 10 ил., 4 табл., 24 пр. C 2 C 2 Адрес для переписки: 127055, Москва, а/я 11, Н.К. Попеленскому 2 6 3 3 7 2 3 03.07.2006 DE 10 2006 030 586.8 Номер и дата приоритета первоначальной заявки, из которой данная заявка выделена: 2009104348 03.07.2006 R U 17.10.2017 (72) Автор(ы): КЮШТЕРС Сабина (DE), ХОРРЕС Роланд (DE), ХОФМАН Михель (DE), ХОФМАН Эрика (DE) RUSSIAN FEDERATION (19) RU (11) (13) ...

Substituted 2-2,6-dioxo-3-fluoropiperidin-3-yl-isoindolines and their use to reduce tnf? levels

1-옥소-2-(2,6-다이옥소-3-플루오로피페리딘-3-일)-아이소인돌린과 1,3-다이옥소-2-(2,6-다이옥소-3-플루오로피페리딘-3-일)-아이소인돌린은 포유동물에서 TNFα와 같은 염증성 사이토카인의 농도를 감소시킨다. 대표적인 화합물은 1,3-다이옥소-2-(2,6-다이옥소-3-플루오로피페리딘-3-일)-아이소인돌린이다. 1-oxo-2- (2,6-dioxo-3-fluoropiperidin-3-yl) -isoindolin and 1,3-dioxo-2- (2,6-dioxo-3- Fluoropiperidin-3-yl) -isoindolin reduces the concentration of inflammatory cytokines such as TNFα in mammals. Representative compounds are 1,3-dioxo-2- (2,6-dioxo-3-fluoropiperidin-3-yl) -isoindolin.

Immunomodulating agent "izofon" showing antimycobacterial activity, method of its preparing and using

FIELD: medicine. SUBSTANCE: invention relates to the novel immunomodulating drug "Izofon" showing an antimycobacterial activity, method of its preparing and using. Method involves the interaction of equimolar amount of 6-methyluracil-5-sulfochloride and isonicotinic acid hydrazide in absolute acetonitrile at 81 C, filtration, precipitate dissolving in hot water, filtration, addition of NH 4 OH to filtrate up to pH 7, precipitate preparing and its crystallization from dimethylformamide (DMFA). Obtained substance is N-(6-methyl-2,4-dioxo-1,2,3,4-tetrahydro- -5-pyrimidinesulfone)-N-isonicotinoylhydrazide hydrate that shows an antimycobacterial activity used orally and by parenteral route. The developed new immunomodulating agent showing an antimycobacterial activity can be used in secondary immunodeficiency and mycobacteriosis also. EFFECT: new agent indicated above, enhanced an antimycobacterial activity. 4 cl, 3 tbl, 5 ex па (19) 13) ВИ” 21414 322 Сл 57 МК А 64 К 31/505, С 070 239/54, 213/44 РОССИЙСКОЕ АГЕНТСТВО ПО ПАТЕНТАМ И ТОВАРНЫМ ЗНАКАМ 12) ОПИСАНИЕ ИЗОБРЕТЕНИЯ К ПАТЕНТУ РОССИЙСКОЙ ФЕДЕРАЦИИ (21), (22) Заявка: 97114347/14, 12.08.1997 (71) Заявитель: Голощапов Николай Михайлович, Голощапова Елена Николаевна, Филипских Тамара Петровна, Мичурина Елена Андреевна, Костюк Любовь Елизаровна (24) Дата начала действия патента: 12.08.1997 (46) Дата публикации: 20.11.1999 (56) Ссылки: ЗИ 1424732 АЗ, 15.09.88. ЗИ 459228 А, 054.02.75. ВЦ 2088231 С1, 27.08.97. В (72) Изобретатель: Голощапов Н.М. 2044728 С1, 27.09.95. КЦ 2074856 С1, 10.08.97. | С1 Голощапова Е.Н., Филипских Т.П., Мичурина Е.А., Костюк Л.Е., Хаитов Р.М., Цывкина (98) Адрес для переписки: Г.И. ‚ Гришин В.К., Стукалов Н.А., Решетов А.Л. 141321, Московская обл., С.Посадский р-н, п/о Краснозаводск, пос."Зеленая дубрава", (73) Патентообладатель: Филиал Российского государственного центра экспертизы лекарств Голощапов Николай Михайлович, Голощапова Елена Николаевна, Филипских Тамара Петровна, Мичурина Елена ...

Manufacture, method, and use of active substance-releasing medical products for permanently keeping blood vessels open

The invention relates to stents and catheter balloons comprising optimized coatings for releasing rapamycin as well as methods for producing said coatings.

Production, method and use of medical products which release agents for opening blood vessels on a permanent basis

Stent (versions) and bag catheter

FIELD: medicine. ^ SUBSTANCE: invention refers to medicine, more specifically to stents and bag catheters with improved rapamycin release coating, and also to methods for producing such coatings. ^ EFFECT: production of stents and bag catheters with improved rapamycin release coating. ^ 10 dwg, 24 ex РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) 2 432 183 (13) C2 (51) МПК A61L A61L A61F A61K A61P 31/10 (2006.01) 31/18 (2006.01) 2/06 (2006.01) 31/436 (2006.01) 37/06 (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ, ПАТЕНТАМ И ТОВАРНЫМ ЗНАКАМ (12) ОПИСАНИЕ ИЗОБРЕТЕНИЯ К ПАТЕНТУ (21)(22) Заявка: 2009104348/15, 03.07.2007 (24) Дата начала отсчета срока действия патента: 03.07.2007 (73) Патентообладатель(и): Хемотек АГ (DE) R U Приоритет(ы): (30) Конвенционный приоритет: 03.07.2006 DE 102006030586.8 (72) Автор(ы): КЮШТЕРС Сабина (DE), ХОРРЕС Роланд (DE), ХОФМАН Михель (DE), ХОФМАН Эрика (DE) (43) Дата публикации заявки: 20.08.2010 Бюл. № 23 2 4 3 2 1 8 3 (45) Опубликовано: 27.10.2011 Бюл. № 30 2 4 3 2 1 8 3 R U (85) Дата начала рассмотрения заявки PCT на национальной фазе: 10.02.2009 C 2 C 2 (56) Список документов, цитированных в отчете о поиске: DE 102004020856 A1, 14.04.2005. EP 0568310 A1, 03.11.19993. Wöhrle J, Comparison of the heparin coated vs the uncoated Jostent-no influence on restenosis or clinical outcome. European Heart J., 2001 Oct; 22(19): 1808-16 (реферат). RU 2005133199 A, 10.02.2006. (86) Заявка PCT: DE 2007/001173 (03.07.2007) (87) Публикация заявки РСТ: WO 2008/003298 (10.01.2008) Адрес для переписки: 127055, Москва, а/я 11, Н.К. Попеленскому (54) СТЕНТ (ВАРИАНТЫ) И КАТЕТЕРНЫЙ БАЛЛОН (57) Реферат: Изобретение относится к медицине, конкретно к стентам и катетерным баллонам с улучшенным покрытием для высвобождения рапамицина, а также к способам получения таких покрытий. 14 з.п. ф-лы, 5 табл., 10 ил. Ñòð.: 1 ru RUSSIAN FEDERATION (19) RU (11) 2 432 183 (13) C2 (51) Int. Cl. A61L A61L A61F A61K A61P 31/10 (2006.01) 31/18 (2006.01) 2/06 (2006.01) 31/436 ...

Substituted 2-(2,6-Dioxo-3-Fluoropiperidine-3-YL)-Isoindolines and their use to reduce TNF-alpha levels

1-Oxo-2-(2,6-dioxo-3-fluoropiperidin-3-yl)-isoindolines and 1,3-dioxo-2-(2,6-dioxo-3-fluoropiperidin-3-yl)-isoindolines reduce the levels of inflammatory cytokines such as TNF alpha in a mammal. A typical embodiment is 1,3-dioxo-2-(2,6-dioxo-3-fluoropiperidin-3-yl)-isoindoline.

Methods for inhibiting tumor cell proliferation

The subject invention concerns methods for inhibition of STAT biological functions using platinum complexes.

Evaluation and treatment of patients with progressive immunosuppression

A soluble immunosuppressive factor present in serum derived from tumor-bearing mammals, is associated with changes in TCR protein subunit levels, T lymphocyte signal transduction pathway proteins. These changes provide a method of determining the level of immunosuppression in a mammal by determining the level of expression of at least one selected TCR subunit protein, a protein in the T lymphocyte signal transduction pathway, or of the NF-KB/rel family and comparing the level and pattern to chat found in non-immunosuppressed individuals: The method is useful to identify patients having T lymphocytes capable of acti-vation for immunotherapy and for identifying agents which cause or reverse immunosuppression. An isolated immunosuppres-sive factor associated with the level of expression of the proteins is useful for suppressing the immune response, for example, in organ transplantation.

Protease inhibitors

The present invention provides HIV protease inhibitors of formulas I, IA, IB, Ib or II, or pharmaceutically acceptable salts thereof, wherein R2 may be, for example, 2-pyridyl-CH2-, 3- pyridyl-CH2-, 4-pyridyl-CH2-, a sulfonyl group as described in the formulas herein including benzenesulfonyl or thiophenesulfonyl groups, R2a-CO)-, R2a being selected from the group consisting of piperonyl, 2-pyranzinyl (unsubstituted or substituted with H, or an alkyl of 1 to 4 carbon atoms) or a picolylamine group as described herein, wherein R3 may be, for example, a phenyl group or diphenylmethyl group as described herein, and wherein Cx may be, for example, COOH, CONR5R6, CH2OH or CH2OR7.

LINEAR PEPTIDE ANTIBIOTICS

А 2016107436 ко РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ (12) ЗАЯВКА НА ИЗОБРЕТЕНИЕ ВЦ "’ 254: 5 <х < (51) МПК СО7К 7/08 (2006.01) # 7 55 У а $02) а 2, р. 777 Ре ре р: А (21)(22) Заявка: 2016107436, 14.08.2014 (71) Заявитель(и): Приоритет(ы): (30) Конвенционный приоритет: 14.08.2013 95 61/865,980; АрКьюЭкс ФАРМАСЬЮТИКЛС, ИНК. (95), ДЖЕНЕНТЕК, ИНК. (05) 14.08.2013 9$ 61/865,982; (72) Автор(ы): 14.08.2013 9$ 61/865,986 (43) Дата публикации заявки: 19.09.2017 Бюл. № 26 (85) Дата начала рассмотрения заявки РСТ на национальной фазе: 14.03.2016 (86) Заявка РСТ: 0$ 2014/051151 (14.08.2014) (87) Публикация заявки РСТ: УГО 2015/023898 (19.02.2015) Адрес для переписки: 119019, Москва, Гоголевский б-р, 11, этаж 3, "Гоулингз Интернэшнл Инк.", Строкова Ольга Владимировна СМИТ Питер Эндрю (05), РОБЕРТС Такер Каррэн (05), ХАЙГУЧИ Роберт И. (0$), ПАРАСЕЛЛИ Прасуна (05), КЁЛЕР Майкл Ф. Т. (05), КРОФОРД Джеймс Джон (05) (54) ЛИНЕЙНЫЕ ПЕПТИДНЫЕ АНТИБИОТИКИ (57) Формула изобретения 1. Соединение, имеющее структуру Формулы (А): Ю2 в“ ВУ * Ад Дому м АИ" &х Оо В о в Формула (А) где В! выбран из: У | ©19 ©11 ©20 213 ма д д А, 218 9 9519 рмз Стр.: 1 па 9$7101910С У А 2016107436 ко В^. В“. в 0. в 1. В “ив. каждый независимо представляют собой -Н, -СН>ОН, -СН (ОН(СНЗ), -СНСЕз, -СНоС(О)ОН, -СН>С(О)ОБВ-, -СН>СН.С(О)ОН, -СНоСН.С(О)ОВ-, -СН.С(О)МН», -СН.СН.С(О)МНЬ, -СНоСН>С(ОУМНС(НХСН.)СО› Н, -СН>СН>С(О)МОНС(Н(СО>ВСН.СОФН, -СНМВ-1В-^, -(СН5)>МВ-1В-^, (СН) МВ-1В-^, -(СН>)МВ-1В-^, (СНМ В уз, -(СН5)4М(Н)С(О)(2,3-дигидроксибензол), необязательно замещенный С\-Сзалкил, необязательно замещенный С!-Согетероалкил, необязательно замещенный Сз-Сзциклоалкил, необязательно замещенный -СН>-С3-Сзциклоалкил, необязательно замещенный гетероциклоалкил, необязательно замещенный арил, необязательно замещенный гетероарил, о "О СХ , ОН, ОН, о и, я ПИ МН М> 5 в? представляет собой метил, этил, изопропил или циклопропил; В> представляет собой Н, метил, этил или -СН>ОН; Во ...

Inhibitors of 11-beta-hydroxy steroid dehydrogenase type 1

本发明涉及通式(I)的化合物且还涉及包括这些化合物的药物组合物并涉及这些化合物在医学和制备对人11－β－羟基类固醇脱氢酶1型酶起作用的药物中的应用。

Vaccine composition containing synthetic adjuvant

Compositions and methods, including vaccines and pharmaceutical compositions for inducing or enhancing an immune response are disclosed based on the discovery of useful immunological adjuvant properties in a synthetic, glycopyranosyl lipid adjuvant (GLA) that is provided in substantially homogeneous form. Chemically defined, synthetic GLA offers a consistent vaccine component from lot to lot without the fluctuations in contaminants or activity that compromise natural-product adjuvants. Also provided are vaccines and pharmaceutical compositions that include GLA and one or more of an antigen, a Toll-like receptor (TLR) agonist, a co-adjuvant and a carrier such as a pharmaceutical carrier.

N, N '- (SULPHONYLDY-1,4-PHENYLENE) BIS (N ", N" -DIMETHYLFORMAMIDINE) -1,2,3,4-TETRAHYDRO-6-METHYL-2,4-DIOXO-5-PYRIMIDIONYSUL STIMULATES CELLULAR METABOLISM AND HAS IMMUNOTROPIC AND ANTIMYCOBACTERIAL ACTIVITY, AND THE METHOD OF OBTAINING IT

The present invention relates to new biologically active chemical compounds of general formula (1) which are derived from a diaminodiphenylsulphone. These compounds are obtained by reacting equimolecular amounts of diaminodiphenylsulphone and 6-methyluracylsulfochloride in a dimethylformamide. These compounds are practically non-toxic (LD50 = 3000 mg/kg) and are active during experiments on the leprosy and tuberculosis mycobacteria. The compounds of the present invention have an influence on cellular exchange and can be used as agents for treating leprosy, tuberculosis as well as other immunodeficiency conditions.

Vaccine composition containing synthetic adjuvant

Compositions and methods, including vaccines and pharmaceutical compositions for inducing or enhancing an immune response are disclosed based on the discovery of useful immunological adjuvant properties in a synthetic, glucopyranosyl lipid adjuvant (GLA) that is provided in substantially homogeneous form. Chemically defined, synthetic GLA offers a consistent vaccine component from lot to lot without the fluctuations in contaminants or activity that compromise natural-product adjuvants. Also provided are vaccines and pharmaceutical compositions that include GLA and one or more of an antigen, a Toll-like receptor (TLR) agonist, a co-adjuvant and a carrier such as a pharmaceutical carrier.

Method for producing the anticholinergic agent tiotropium bromide

Anti-trka antibodies and derivatives thereof

Manufacture, method, and use of active substance-releasing medical products for permanently keeping blood vessels open

본 발명은 라파마이신을 용출하는데 최적화된 코팅을 갖는 스텐트와 카테터 풍선, 및 이들 코팅의 제조방법에 관한 것이다. The present invention relates to stents and catheter balloons with coatings optimized for eluting rapamycin, and methods of making these coatings.

Manufacture, method and use of drug-eluting medical devices for permanently keeping blood vessels open

Manufacture, method, and use of active substance-releasing medical products for permanently keeping blood vessels open.

La invención es concerniente con férulas y globos de catéter que comprenden recubrimientos optimizados para liberar rapamicina, también como métodos para producir tales recubrimientos.

Triple combination

The invention provides a combination comprising 4-methyl-8-phenoxy-1-(2-phenylethyl)-2,3- dihydro-1H-pyrrolo[3,2-c]quinoiine or a pharmaceutically acceptable derivative thereof, mupirocin or a pharmaceuticaliy acceptable derivative thereof and neomycin or a pharmaceutically acceptable derivative thereof. This triple combination is particularly useful for the treatment and/or prevention of microbial infections.

Methods and compositions for treating allergic diseases

Disclosed in the present invention are antibodies that specifically recognize and antagonize human TSLP receptor, and methods of employing these antibodies to treat or ameliorate diseases or disorder mediated by TSLP signaling.

Substituted heterocyclic compounds with cxcr3 antagonist activity

The present application discloses a compound, or enantiomers, stereoisomers, rotamers, tautomers, racemates or prodrug of said compound, or pharmaceutically acceptable salts, solvates or esters of said compound, or of said prodrug, said compound having the general structure shown in Formula (1) , or a pharmaceutically acceptable salt, solvate or ester thereof, wherein the various moieties are defined herein. Also disclosed is a method of treating chemokine mediated diseases, such as, palliative therapy, curative therapy, prophylactic therapy of certain diseases and conditions such as inflammatory diseases (non-limiting example(s) include, psoriasis), autoimmune diseases (non-limiting example(s) include, rheumatoid arthritis, multiple sclerosis), graft rejection (non-limiting example(s) include, allograft rejection, xenograft rejection), infectious diseases (e.g , tuberculoid leprosy), fixed drug eruptions, cutaneous delayed-type hypersensitivity responses, type I diabetes, viral meningitis and tumors using a compound of Formula (1).

Method of manufacture of tiotropiumbromide from anticholinergics

Bulus (1 alfa, 2 , 4 , 5 alfa, 7 )-7-[(hidroksidi-2-tienilasetil)oksi]-9, 9-dimetil-3-oksa-9-azoniatrisiklo[3.3.1.O2,4]nonanbromid imal etmeye yönelik yeni bir yöntem ile ilgilidir. The invention (1 alpha, 2, 4, 5 alpha, 7) -7 - [(hydroxydi-2-thienylacetyl) oxy] -9,9-dimethyl-3-oxa-9-azoniatricyclo [3.3.1.O2,4] The present invention relates to a novel method of manufacturing nonanbromide.

Stent with polymeric coating comprising rapamycin as an active agent

The present invention relates to a method for coating blood vessel supports such as stents by providing an optimized elution of rapamycin. In particular, it relates to a method for coating a stent with a coating solution comprising rapamycin and poly (lactic-co-glycolic acid) (PLGA), wherein the rapamycin and PLGA are dissolved in an anhydrous solvent to prepare the coating solution and wherein the coating of the stent is performed under exclusion of light and by using an inert gas as a carrier gas for the coating solution. The invention also relates to stents that are coated with the coating solution. Stents coated in accordance with the invention are able to rapidly grow into the vessel wall while reducing the risk of resteonosis and/or thrombosis.

Antimicrobial compounds, their synthesis and their use for treatment of mammalian infections

The present invention relates to new antimicrobial compounds, their synthesis and their use for treatment of mammalian infections. The present invention aims at the generation of new compounds with activity against mycobacteria as potential new tuberculosis drugs to overcome problems concerning resistance and drug intolerance. This aim has been solved by providing compounds of the formula 1 wherein R1 and R2 are, independently of each other, NO2, NR7R8, NHOR9, COOR9, CN, CONR10R11, CHO, F, Cl, Br, SO2NR12R13, lower alkoxy, OCF3, mono-, di or trifluoromethyl; R3 and R4 are, independently of each other, H, a saturated or unsaturated, linear or branched aliphatic radical having 1 -3 chain members, F, Cl, Br, lower alkoxy; R5 is H, a saturated or unsaturated, halogenated or unhalogenated, linear or branched aliphatic radical having 1-7 chain members; R is a radical: wherein X is saturated or unsaturated, halogenated or unhalogenated, linear or branched aliphatic radical having 1-5 chain members, or R5 and R6 together represent bivalent radicals wherein n is 1-4: R7 - R13 are, independently of each other H or a saturated or unsaturated, halogenated or unhalogenated, linear or branched aliphatic radical having 1 -5 chain members, phenyl, benzyl or R7 and R8 together R10 and R11 together, R12 and R13 together represent a linear or branched aliphatic bivalent radical having 1 -7 chain members; R14 and R15 are, independently of each other, H, linear or branched aliphatic radical having 1 -5 chain members, F, Cl, Br, NO2, NH1, CF3.

2- (2.6-DIOXO-3-FLUORPIPERIDIN-3-IL) -ISOINDOLINAS SUBSTITUTED AND ITS USE TO REDUCE TNFALFA LEVELS.

Un isómero R ó S de un compuesto seleccionado del grupo formado por (a) una 2(2, 6-dioxo-3-fluorpiperidin-3-il)-isoindolina, de fórmula: (Ver fórmula) en la cual Y es oxígeno ó H2, y cada R1, R2, R3 y R4, independientemente entre sí, es hidrógeno, halo, alquilo de 1 a 4 átomos de carbono, alcoxilo de 1 a 4 átomos de carbono, o amino, y en donde el átomo de carbono al cual el átomo de flúor dibujado está unido, constituye un centro de quiralidad, y (b) las sales de adición ácida de dichas 2-(2, 6-dioxo-3-fluorpiperidin-3-il)-isoindolinas, las cuales contienen un átomo de nitrógeno capaz de ser protonado. An R or S isomer of a compound selected from the group consisting of (a) a 2 (2, 6-dioxo-3-fluorpiperidin-3-yl) -isoindoline, of the formula: (See formula) in which Y is oxygen or H2, and each R1, R2, R3 and R4, independently of one another, is hydrogen, halo, alkyl of 1 to 4 carbon atoms, alkoxy of 1 to 4 carbon atoms, or amino, and wherein the carbon atom at which the drawn fluorine atom is attached, constitutes a chirality center, and (b) the acid addition salts of said 2- (2,6,6-dioxo-3-fluorpiperidin-3-yl) -isoindolines, which contain a nitrogen atom capable of being protonated.

USE OF CANTHIN-6-ONE AND ITS ANALOGUES IN THE TREATMENT OF MICOBACTERIA RELATED DISEASES

Method for producing anticholinergic agent tiotropium bromide

本発明は、（１α，２β，４β，５α，７β）−７−［（ヒドロキシジ−２−チエニルアセチル）オキシ］−９，９−ジメチル−３−オキサ−９−アゾニアトリシクロ［３．３．１．０ ２，４ ］ノナン−臭化物の新規製造方法に関する。

N,n'-(sulphonyldi-1, 4-phenylen) bis (n'',n''- dimethylformamidin)-1, 2,3,4-tetrahydro- 6-methyl-2, 4-dioxo-5-pyrimidinsulphonate for stimulating cellular metabolism and having an immunotropic and anti-bacterial activity and method for producing the same

Antimicrobial compounds, their synthesis and their use for treatment of mammalian infections

The present invention relates to compounds of general formula (I) with activity against mycobacteria as potential new tuberculosis drugs to overcome problems concerning resistance and drug intolerancewherein Rand Rare, independently of each other, NOor trifluoromethyl; Rand Rare H; Ris H, a saturated linear aliphatic radical having 1-3 chain members; Ris a radicalwherein X is saturated linear aliphatic radical having 1-2 chain members; or Rand Rtogether represent bivalent radicals wherein n is 1-4:where Rand Rare, independently of each other, H, linear or branched aliphatic radical having 1-5 chain members, F, Cl, CFor salts thereof. The invention also relates to a pharmaceutical composition comprising compounds of formula (I) and to the use of said compound for preparing a medicament for therapeutic or prevention treatment of microbal infection in mammals and to a method for therapeutic or prevention treatment of microbal infection or tuberculosis infection or leprosy infection in mammals. The invention also relates to a method of the preparation of 2-NRR-4H-1,3-benzothiazin-4- ones of formula (I).

Inhibitors of 11-beta-hydroxy steroid dehydrogenase type 1

The present invention relates to compounds with the formula (I)and also to pharmaceutical compositions comprising the compounds, as well as to the use of the compounds in medicine and for the preparation of a medicament which acts on the human 11-b-hydroxysteroid dehydrogenase type 1 enzyme.

NEW SALTS

1. Гидрохлоридная соль 1-(4-{1-[(E)-4-циклогексил-3-трифторметилбензилоксиимино]этил}-2-этилбензил)азетидин-3-карбоновой кислоты.2. Гидрохлоридная соль 1-(4-{1-[(E)-4-циклогексил-3-трифторметилбензилоксиимино]этил}-2-этилбензил)азетидин-3-карбоновой кислоты по п.1, где указанная соль является, по существу, кристаллической.3. Кристаллическая Форма А гидрохлоридной соли 1-(4-{1-[(E)-4-циклогексил-3-трифторметилбензилоксиимино]этил}-2-этилбензил)азетидин-3-карбоновой кислоты.4. Кристаллическая Форма А гидрохлоридной соли 1-(4-{1-[(E)-4-циклогексил-3-трифторметилбензилоксиимино]этил}-2-этилбензил)азетидин-3-карбоновой кислоты по п.3, характеризующаяся тем, что кристаллическая форма имеет порошковую рентгенограмму, содержащую по меньшей мере один специфический пик при угле 2 Тета = около 8,1º, 12,2º, 15,8º, 18,9º или 19,7º.5. Кристаллическая Форма А гидрохлоридной соли 1-(4-{1-[E)-4-циклогексил-3-трифторметилбензилоксиимино]этил}-2-этилбензил)азетидин-3-карбоновой кислоты по п.3 или 4, характеризующаяся тем, что кристаллическая форма имеет порошковую рентгенограмму, содержащую по меньшей мере четыре специфических пика при угле 2 Тета =8,1º, 12,2º, 12,9º, 13,4º, 15,8º, 16,4º, 16,7º, 17,7º, 18,9º, 19,7º, 20,6º или 23,8º.6. Малатная соль 1-(4-{1-[(E)-4-циклогексил-3-трифторметилбензилоксиимино]этил}-2-этилбензил)азетидин-3-карбоновой кислоты.7. Кристаллическая Форма А малатной соли 1-(4-{1-[(E)-4-циклогексил-3-трифторметилбензилоксиимино]этил}-2-этилбензил)азетидин-3-карбоновой кислоты по п.6, характеризующаяся тем, что кристаллическая форма имеет порошковую рентгенограмму, содержащую по меньшей мере один специфический пик при угле 2 Тета = около 6,8º, 13,7º, 15,8º, 17,2º или 20,5º.8. Кристаллическая Форма А малатной соли РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) (51) МПК C07D 205/04 (13) 2011 129 229 A (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ (12) ЗАЯВКА НА ИЗОБРЕТЕНИЕ (21)(22) Заявка: 2011129229/04, 17.12.2009 (71) Заявитель(и): НОВАРТИС АГ (CH) Приоритет(ы ...

COMPOSITION OF THE VACCINE CONTENTS OF COMPOSITE IMMUNITY

Συνθέσεις και μέθοδοι, που συμπεριλαμβάνουν εμβόλια και φαρμακευτικές συνθέσεις για διέγερση ή ενίσχυση ανοσοαπόκρισης αποκαλύπτονται επί τη βάσει της ανακάλυψης χρήσιμων ιδιοτήτων ανοσολογικού ανοσοενισχυτικού σε ένα συνθετικό, γλυκοπυρανοζύλο λιπιδίου ανοσοενισχυτικά (GLA) που παρέχεται σε ουσιαστικώς ομοιογενή μορφή. Χημικώς ορισμένο, συνθετικό GLA προσφέρει συνεπές συστατικό εμβολίου από παρτίδα σε παρτίδα χωρίς τις διακυμάνσεις σε μολυντές ή δραστικότητα που διακυβεύουν φυσικού-προϊόντος ανοσοενισχυτικά. Παρέχονται επίσης εμβόλια και φαρμακευτικές συνθέσεις που περιλαμβάνουν GLA και ένα ή περισσότερα από αντιγόνο, αγωνιστή Toll-ομοιάζοντα υποδοχέα (TLR), ένα συν-ανοσοενισχυτικό κι ένα φορέα όπως φαρμακευτικό φορέα. Compositions and methods, including vaccines and pharmaceutical compositions for stimulating or enhancing an immune response are disclosed on the basis of the discovery of useful properties of an immunological adjuvant in a synthetic, glycopyranosyl lipid adjuvant (GLA) provided in the substance adjuvant. Chemically defined, synthetic GLA offers a consistent batch-to-batch vaccine component with no fluctuations in contaminants or activity that compromise natural-product adjuvants. Vaccines and pharmaceutical compositions comprising GLA and one or more of an antigen, a Toll-like receptor agonist (TLR), a co-adjuvant and a carrier such as a carrier are also provided.

Methods of treating mycobacterial infections using tetracycline compounds

The present invention provides methods of treating mycobacterial infections or mycobacterial diseases by administering a tetracycline compound, e.g., omadacycline, or a pharmaceutically acceptable salt thereof.

Production, method and use of medical products which release agents for opening blood vessels on a permanent basis

Stent coated with a polysulfone comprises rapamycin and a polymer swellable in methanol, where the weight portion of the polymer related to the total coating is 0.1-50 wt.%. An independent claim is included for a catheter balloon coated with a combination of rapamycin and a vasodilator or of rapamycin and a contrast agent or rapamycin and a vasodilator and a contrast agent. ACTIVITY : Vasotropic. MECHANISM OF ACTION : None give.

Novel dihydroxyhexanoic acid derivatives

Dihydroxyhexanoic acid derivatives of general formula (I) are useful to treat inflammation and other immune disorders.

New compounds

Substituted heterocyclic compounds with cxcr3 antagonist activity

The present application discloses a compound, or enantiomers, stereoisomers, rotamers, tautomers, racemates or prodrug of said compound, or pharmaceutically acceptable salts, solvates or esters of said compound, or of said prodrug, said compound having the general structure shown in Formula (1) , or a pharmaceutically acceptable salt, solvate or ester thereof, wherein the various moieties are defined herein. Also disclosed is a method of treating chemokine mediated diseases, such as, palliative therapy, curative therapy, prophylactic therapy of certain diseases and conditions such as inflammatory diseases (non-limiting example(s) include, psoriasis), autoimmune diseases (non-limiting example(s) include, rheumatoid arthritis, multiple sclerosis), graft rejection (non-limiting example(s) include, allograft rejection, xenograft rejection), infectious diseases (e.g , tuberculoid leprosy), fixed drug eruptions, cutaneous delayed-type hypersensitivity responses, type I diabetes, viral meningitis and tumors using a compound of Formula (1).

Protease inhibitors

Methods of using gpr119 receptor to identify compounds useful for increasing bone mass in an individual

本发明涉及使用GPR119受体鉴定可用于增加个体骨质量的化合物的方法。GPR119受体的促效剂可用作用于治疗或预防特征为低骨质量的病状(诸如骨质疏松症)与用于增加个体骨质量的治疗剂。GPR119受体的促效剂促进个体骨形成。

Piperazine-piperidines with cxcr3 antagonist activity

The present application discloses a compound, or enantiomers, stereoisomers, rotamers, tautomers, racemates or prodrug of said compound, or pharmaceutically acceptable salts, solvates or esters of said compound, or of said prodrug, said compound having the general structure shown in Formula 1 or a pharmaceutically acceptable salt, solvate or ester thereof, wherein the various moieties are defined herein. Also disclosed is a method of treating chemokine mediated diseases, such as, palliative therapy, curative therapy, prophylactic therapy of certain diseases and conditions such as inflammatory diseases (non limiting example(s) include, psoriasis), autoimmune diseases (non limiting example(s) include, rheumatoid arthritis, multiple sclerosis), graft rejection (non limiting example(s) include, allograft rejection, xenograft rejection), infectious diseases (e.g , tuberculoid leprosy), fixed drug eruptions, cutaneous delayed type hypersensitivity responses, ophthalmic inflammation, type I diabetes, viral meningitis and tumors using a compound of Formula 1.

2-piperazin-1-yl-4h-1,3-benzothiazin-4-one derivatives and their use for the treatment of mammalian infections

본 발명은 새로운 2-피페라진-1-일-4 H -1,3-벤조티아진-4-온 유도체 및 세균에 의해 유발된 포유동물의 감염, 특히, 매우 연관된 마이코박테리아의 감염으로 인한 결과인 결핵(TB), 부룰리 궤양 및 나병과 같은 질병을 치료하기 위한 이의 용도에 관한 것이다. The present invention relates to novel 2-piperazin-1-yl- 4H -1,3-benzothiazin-4-one derivatives and the results of infections of mammals caused by bacteria, in particular infections of highly associated mycobacteria Tuberculosis (TB), Buruli ulcer and leprosy.

Compounds having muscarinic receptor antagonist and beta2 adrenergic receptor agonist activity

Vaccine composition containing synthetic adjuvant

本发明基于以基本上均一形态提供的合成吡喃葡萄糖脂佐剂(GLA)的有益免疫学佐剂特性的发现，公开了用于诱导或增强免疫反应的包括疫苗和药物组合物在内的组合物和方法。化学定义的合成GLA提供了包含天然产物佐剂、不同批次之间一致的疫苗组分，没有污染物或活性的波动。也提供了疫苗和药物组合物，其包括GLA以及抗原、钟样受体(TLR)激动剂、辅佐剂和诸如药物载体的载体中的一种或多种。

Vaccine composition containing synthetic adjuvant

SPIROISOXAZOLINE-LIKE COMPOUNDS WITH POTENTIALIZING ACTIVITY OF AN ANTIBIOTIC COMPOSITION AND PHARMACEUTICAL PRODUCT COMPRISING SUCH COMPOUNDS

Composés de type spiroisoxazoline ayant une activité potentialisatrice de l'activité d'un antibiotique-composition et produit pharmaceutiques comprenant de tels composés La présente invention concerne un composé spiroisoxazoline de formule générale (I) : La présente invention concerne également l'utilisation de ce composé en tant que médicament, en particulier dans le traitement des infections bactériennes et mycobactériennes comme la tuberculose en combinaison avec un antibiotique actif contre les bactéries et/ou mycobactéries, ledit composé potentialisant l'activité dudit antibiotique. The present invention relates to a spiroisoxazoline compound of general formula (I): The present invention also relates to the use of this compound. as a medicament, particularly in the treatment of bacterial and mycobacterial infections such as tuberculosis in combination with an antibiotic active against bacteria and / or mycobacteria, said compound potentiating the activity of said antibiotic.

Immunomodulator exhibiting antimicrobial and antimycobacterial activities, method for producing the same and pharmaceutical preparation for treating mycobacterioses as well as pulmonary chronic and non-specific conditions, sexually transmitted diseases and the resulting immuno-deficiency

The present invention pertains to the field of medicine and more precisely relates to a novel immuno-modulator of formula (I) which exhibits antimicrobial and anti-mycobacterial activities. This modulator is produced by reacting equimolecular amounts of 6-methyluracyl-5-sulphochloride and isoniazide in acetonitrile at a high temperature. The preparation is practically not toxic (LD50 in severe conditions exceeding 7000 mg/kg) and can be used according to given clinical tests for expressing the immuno-modulating and anti-mycobacterial activity. This preparation can be used for correcting various immuno-deficiencies including in HIV-infected patients as well as for treating mycobacterioses such as leprosy, tuberculosis, etc. This preparation can be administered internally or parenterally. The compound described in the present invention represents the active substance of this pharmaceutical preparation, wherein said preparation can be used against secondary immunodeficiencies or mycobacterioses.

Vaccine composition containing synthetic adjuvant

실질적으로 균질한 형태로 제공되는 합성 글루코피라노실 지질 애주번트(GLA)의 유용한 면역학적 애주번트 성질의 발견을 기초로 한, 면역반응을 유도 또는 증강시키기 위한 백신 및 약제학적 조성물을 비롯한 조성물과 방법을 개시한다. 화학적으로 특정된 합성 GLA는 제품(lot)마다 천연 산물 애주번트를 손상시키는 오염물이나 활성의 변동 없이 일정한 백신 성분을 제공한다. 또한, GLA; 및 항원, 톨-유사 수용체(TLR) 효능제, 보조애주번트 및 담체, 예컨대 약제학적 담체 중 하나 이상을 포함하는 백신 및 약제학적 조성물도 제공한다. 백신 조성물, 합성 애주번트, 글루코피라노실 지질 애주번트(GLA), 면역반응 유도, 면역반응 증강 Compositions and methods, including vaccines and pharmaceutical compositions for inducing or enhancing an immune response, based on the discovery of useful immunological adjuvant properties of synthetic glucopyranosyl lipid adjuvant (GLA) in substantially homogeneous form. Initiate. Chemically specified synthetic GLA provides a constant vaccine component per lot without contaminant or activity changes that compromise the natural product adjuvant. In addition, GLA; And vaccines and pharmaceutical compositions comprising one or more of an antigen, a toll-like receptor (TLR) agonist, a co-adjuvant and a carrier such as a pharmaceutical carrier. Vaccine composition, synthetic adjuvant, glucopyranosyl lipid adjuvant (GLA), induce immune response, enhance immune response

Benzothiazinone derivatives, their synthesis and their use for treatment of mammalian infections

The disclosure relates to antimicrobial compounds of formula (I), wherein the variables are as defined in the specification, their synthesis and their use as antibacterial agents in infectious diseases of mammals (humans and animals) caused by bacteria, especially diseases like tuberculosis (TB) and leprosy caused by mycobacteria. These compounds have an activity against mycobacteria as potential new tuberculosis drugs to overcome problems concerning resistance and drug intolerance.

Vaccine composition containing synthetic adjuvant

New polyimino ketoaldehydes

The compounds with the general formula (I) are disclosed where n1 is the number of carbon atoms connected to nitrogen atom by a double bond and can take on values between 25 and 41, and where n2 is the number of -CH2- groups and can take on values between 15 and 23, as well as their biologically acceptable salts and solvates.

5-(optionally substituted phenyl) pyridin-2-yl compounds as metalloenzyme inhibitors

The instant invention describes compounds having metalloenzyme modulating activity, and methods of treating diseases, disorders or symptoms thereof mediated by such metalloenzymes. The invention describes a compound of Formula (I), or salt thereof, wherein: (see formula I) MBG is optionally substituted tetrazolyl, optionally substituted triazolyl, or optionally. substituted pyrazolyl; R1 is halo; R2 is halo; each R3 is independently alkyl, cyano, haloalkyl, alkoxy, halo, haloalkoxy, R4 is aryl optionally substituted with 0, 1, 2 or 3 independent R3; R5 is H, or -C(O)alkyl optionally substituted with amino; n is 0, 1, 2 or 3.

Long-term formulations

Esta invención se refiere a composiciones farmacéuticas para la administración por vía intramuscular o inyección subcutánea, que comprende micro o nanopartículas del compuesto bedaquilina anti-TB, suspendido en un vehículo acuoso farmacéuticamente aceptable, y al uso de tales composiciones farmacéuticas en el tratamiento y profilaxis de una infección por micobacterias patógenas. This invention relates to pharmaceutical compositions for administration by intramuscular route or subcutaneous injection, comprising micro or nanoparticles of the anti-TB compound bedaquiline, suspended in a pharmaceutically acceptable aqueous vehicle, and to the use of such pharmaceutical compositions in the treatment and prophylaxis of an infection with pathogenic mycobacteria.

Pharmaceutical preparation containing diaminodiphenylsulphone and brodimoprim

A pharmaceutical preparation contains a diaminodiphenylsulphone and 2,4-diamino-5-(4-bromo-3,5-dimethoxybenzyl)pyrimidine is useful for the treatment of leprosy and/or other mycobacterioses.

Anti-TRKA antibody and derivative thereof

提供了抗TrkA抗体，其包含：a)可变重链，其包含选自如图(1a)所示BXhVH1、BXhVH2、BXhVH3、BXhVH4、BXhVH5或HuVHWOv任意一种，或选自所述序列任一种的变体的序列；和/或b)可变轻链，其包含选自如图(1b)所示BXhVL1、BXhVL2、BXhVL3、BXhVL4、BXhVL5、BXhVL6、BXhVL7或BXhVL8任意一种，或选自所述序列任一种的变体的序列。也提供了结合TrkA的衍生物。本发明的抗体或衍生物可用于包括疼痛治疗的多种治疗中。

Novel a-500359 derivatives

The present invention relates to a compound of formula (I) (see formula I) (wherein R1 and R2 represent an aryl group, a heterocyclic group, an alkyl group, an alkenyl group and the like which are optionally substituted, R3 represents a hydrogen atom or a hydroxyl group, and X1 and X2 represent an oxygen atom or a sulfur atom, or a nitrogen atom which may be substituted), a pharmaceutically acceptable derivative thereof or a salt thereof. The present invention also relates to a pharmaceutical composition comprising a compound described above as an active ingredient for the prevention or treatment of bacterial infections. The present invention includes the use of a compound described above in order to prepare a medicament effective in the prevention or treatment of bacterial infections. The present invention is concerned with a method for the prevention or treatment of bacterial infections in warm-blooded animals comprising administering a pharmacologically effective amount of a compound described above to them.

Platinum complexes for the treatment of tumors

Topical treatment

Salts

This invention relates to a hydrochloride, malate, oxalate and tartrate salt forms of 1-(4-{1-[(E)-4-cyclohexyl-3-trifluoromethyl-benzyloxyimino]-ethyl}-2-ethyl-benzyl)-azetidine-3-carboxylic acid (Compound I), to pharmaceutical compositions comprising this salt, to processes for forming this salt and to its use in medical treatment. In addition, the present invention also relates to new polymorphic forms of each of these salts, as well as to pharmaceutical compositions comprising these polymorphic forms, to processes for obtaining them, and their use in medical treatment.