摘要:
The present invention relates to a novel pharmaceutical combination, containing an inhibitor of platelet aggregation and a fÊbrate, where the inhibitor of platelet aggregation is preferably either aspirin or clopidogreL Such a pharmaceutical combination of an inhibitor of platelet aggregation and a fÊbrate is expected to be useful in the treatment and/or prevention of myocardial infarction (heart attack), cardiac arrest, peripheral vascular disease (including symptomatic carotid artery disease), congestive heart failure, ischemic heart disease, angina pectoris (including unstable angina), sudden cardiac death, unstable angina, as well as cerebrovascular events such as cerebral infarction, cerebral thrombosis, cerebral ischemia and transient ischemic attack, disorders related to bypass operations (angioplasty), fitting of endovascular prostheses and restenosis, and inflammatory disorders, including arthritic conditions such as rheumatoid arthritis and osteoarthritis, as well as asthma or related airway or respiratory inflammatory disorders.
摘要:
Novel proteins or polypeptides having significant sequence homology to DPPIV, nucleic acids coding therefor, cells which have been modified with such nucleic acid so as to express these proteins, antibodies to these proteins, screening methods for the discovery of new therapeutic agents which are inhibitors of the activity of these proteins or of related proteins, and therapeutic agents discovered by such screening methods, as well as new therapeutic treatments, are all provided.
摘要:
Peptides which exhibit high selectivity for the kappa opioid receptor (KOR) and long duration of peripheral action without significant entry into the brain are created which are sequences of four D-isomer amino acid residues having a C-terminus which is a mono or di-substituted amide. Representative compounds, which have an affinity for the KOR at least 1,000 times their affinity for the mu opioid receptor and an ED.sub.50 of not greater than about 0.5 mg/kg, includeH-D-Phe-D-Phe-D-Nle-D-Arg-NHEt,H-D-Phe-D-Phe-D-Nle-D-Arg-morpholinyl,H-D-Phe-D-Phe-D-Nle-D-Arg-NH-4-picolyl,H-D-Phe-D-Phe-D-Nle-D-Arg-NHPr,H-D-Phe-D-Phe-D-Nle-D-Arg-thiomorpholinyl,H-D-Phe-D-Phe-D-Nle-D-Arg-NEt.sub.2,H-D-Phe-D-Phe-D-Nle-D-Arg-NHMe,H-D-Phe-D-Phe-D-Leu-D-Orn-morpholinyl,H-D-Phe-D-Phe-D-Nle-D-Arg-NHhEt,H-D-Phe-D-Phe-D-Nle-D-Arg-NH-cyclopropyl,H-D-Ala(2Thi)-D-4Cpa-D-Leu-D-Arg-morpholinyl,H-D-Phe-D-Phe-D-Nle-D-Arg-piperidinyl,H-D-Phe-D-Phe-D-Leu-D-Orn-NHEt,H-D-Phe-D-Phe-D-Leu-D-Lys-morpholinyl,andH-D-Phe-D-Phe-D-Nle-D-Arg-piperazinyl.
摘要:
Enantiomers of (S) configuration of formula (I) ##STR1## in which R is H or methyl, with antiallergic and in particular antihistaminic activity, useful as medicinal products.
摘要:
A compound which is a propanamine of general formula (I) ##STR1## in which: R1 is a phenyl radical optionally mono-, di- or trisubstituted,or is a 5- or 6-membered monocyclic heteroaryl radical in which the single heteroatom is nitrogen, oxygen or sulfur,R2 is a lower alkyl radical,R3 and R4 are a hydrogen atom or a lower alkyl, lower alkenyl or lower cycloalkylalkyl radical,or, together with the nitrogen atom to which they are attached, form a saturated 5- to 6-membered heterocycle comprising only one heteroatom,R5 is a 5- to 7-membered cycloalkyl radical, a phenyl radical or a 5- or 6-membered monocyclic heteroaryl radical,and W representsa group .dbd.CH--QH,or a heterocycle .dbd.C[Q--(CH2)n--Q],or a group .dbd.C.dbd.Q, in which groupsQ is an oxygen or sulfur atom,n has the value 2 or 3,W being .dbd.C.dbd.Q only when R3 and R4 are not both hydrogen, and their additions salts with pharmaceutically acceptable acids.A pharmaceutical composition comprising a compound of general formula (I) with the above definitions for the treatment of diarrheal states.
摘要翻译:作为通式(I)的丙胺的化合物,其中:R 1是任选被一个,二或三取代的苯基,或是5或6元单环杂芳基,其中 单个杂原子是氮,氧或硫,R2是低级烷基,R3和R4是氢原子或低级烷基,低级烯基或低级环烷基烷基,或者与它们相连的氮原子一起形成 饱和的5至6元杂环,仅包含一个杂原子,R 5为5-至7-元环烷基,苯基或5-或6-元单环杂芳基,W表示基团= CH-QH, 或杂环= C [Q-(CH 2)nQ]或基团= C = Q,其中基团Q是氧或硫原子,n具有值2或3,W仅当R 3为 和R4不同时为氢,并且它们与药学上可接受的酸相加。 一种药物组合物,其包含具有上述定义用于治疗腹泻状态的通式(I)的化合物。
摘要:
Process for the preparation of a gastric lipase. The stomachs of rabbits or horses undergo extraction by an acid aqueous medium, the lipase extract is salted out by the addition of hydrosoluble salts then, by filtration on a molecular sieve, followed by separation using ion exchange chromatography, an elution fraction containing the lipase is collected.Medicament for fighting against malabsorptions of fatty substances.
摘要:
Aminoalcohols of formula: ##STR1## in which R.sub.1 is alkyl, R.sub.2 H or alkyl, R.sub.3 in particularly H, alkyl, phenylakyl, alkanoyl, phenylalkanoyl, in which N, R.sub.2 and R.sub.3 together form a heterocycle saturated with 5 to 7 chain links.Analgesic medicaments.
摘要:
Benzodiazepines of formula ##STR1## in which R.sub.1 is H of halogen, R.sub.2 is H or halogen, Ar is indolyl, phenyl, naphthyl, indolyl monosubstituted with a halogen or with a methoxy or phenyl mono-, di- or trisubstituted with a halogen or with a methoxy or with a trifluoromethyl group, and n is 2 or 3; and their optical isomers.
摘要:
Aminoethyl imidazole of formula: ##STR1## in which R.sub.1 is a lower alkyl, R.sub.2 is a phenyl or phenoxy radical, optionally substituted by a halogen atom or a lower alkoxy radical, R.sub.3,R.sub.4 and R.sub.5 are a hydrogen atom or a lower alkyl radical and x, y and z have the value 0 or 1, but the values of y and z cannot be the same, together with their acid addition salts with acids.Cytoprotective medicament.
摘要:
The present invention generally relates to a novel therapeutical use of liver X receptor (LXR) agonsits. More specifically, the present invention relates to the use of LXR agonist for the preparation of a medicament useful for the treatment and/or the prevention of a disease associated with beta cells degeneration, such as diabetes, and a method for increasing ex vivo viability of pancreatic islet cells, comprising contacting said islet cells with a LXR agonist.