- Compounds with antiviral and bacteriostatic activity
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The invention discloses a structural design and a synthesis method of compounds with antiviral and bacteriostatic activity. The invention particularly relates to a series of compounds which are obtained by taking piperidine pyrazole boric acid as a main body structure and performing structural modification on the piperidine pyrazole boric acid, so that the compounds become chemical synthetic drugswith the potential of being developed into antibacterial agents or antiviral drugs. The patent content comprises a synthetic route and a synthetic method of the compounds designed for the structure.
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- NEW SUBSTITUTED CYANOINDOLINE DERIVATIVES AS NIK INHIBITORS
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The present invention relates to pharmaceutical agents of formula (I) useful for therapy and/or prophylaxis in a mammal, and in particular to inhibitors of NF- KB-inducing kinase (NIK - also known as MAP3K14) useful for treating diseases such as cancer, inflammatory disorders, metabolic disorders and autoimmune disorders. The invention is also directed to pharmaceutical compositions comprising such compounds, and to the use of such compounds or pharmaceutical compositions for the prevention or treatment of diseases such as cancer, inflammatory disorders, metabolic disorders including obesity and diabetes, and autoimmune disorders.
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Page/Page column 266; 267
(2017/08/20)
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- TETRAHYDRONAPHTHYRIDINES AND AZA DERIVATIVES THEREOF AS HISTAMINE H3 RECEPTOR ANTAGONISTS
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The invention relates to compounds of formula (I), wherein X1a, X1 to X5, Ra, Rb, n and R have the meaning as cited in the description and the claims. Said compounds are useful as Histamine H3 receptor antagonists. The invention also relates to pharmaceutical compositions, the preparation of such compounds as well as the production and use as medicament.
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Page/Page column 66-67
(2009/10/30)
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- 5-Hydroxyindole-2-carboxylic acid amides: Novel histamine-3 receptor inverse agonists for the treatment of obesity
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Obesity is a major risk factor in the development of conditions such as hypertension, hyperglycemia, dyslipidemia, coronary artery disease, and cancer. Several pieces of evidence across different species, including primates, underscore the implication of the histamine 3 receptor (H3R) in the regulation of food intake and body weight and the potential therapeutic effect of H3R inverse agonists. A pharmacophore model, based on public information and validated by previous investigations, was used to design several potential scaffolds. Out of these scaffolds, the 5-hydroxyindole-2-carboxylic acid amide appeared to be of great potential as a novel series of H3R inverse agonist. Extensive structure-activity relationships revealed the interconnectivity of microsomal clearance and hERG (human ether-a-go-go-related gene) affinity with lipophilicity, artificial membrane permeation, and basicity. This effort led to the identification of compounds reversing the (R)-R-methylhistamine-induced water intake increase in Wistar rats and, further, reducing food intake in diet-induced obese Sprague-Dawley rats. Of these, the biochemical, pharmacokinetic, and pharmacodynamic characteristics of (4,4-difluoropiperidin- 1-yl)[1-isopropyl-5-(1-isopropylpiperidin-4-yloxy)-1H-indol-2-yl]-methanone 36 are detailed.
- Pierson, Pascale David,Fettes, Alec,Freichel, Christian,Gatti-McArthur, Silvia,Hertel, Cornelia,Huwyler, J?rg,Mohr, Peter,Nakagawa, Toshito,Nettekoven, Matthias,Plancher, Jean-Marc,Raab, Susanne,Richter, Hans,Roche, Olivier,Sarmiento, Rosa María Rodríguez,Schmitt, Monique,Schuler, Franz,Takahashi, Tadakatsu,Taylor, Sven,Ullmer, Christoph,Wiegand, Ruby
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supporting information; experimental part
p. 3855 - 3868
(2010/02/28)
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- PYRIMIDINE DERIVATIVES CAPABLE OF INHIBITING ONE OR MORE KINASES
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A first aspect of the invention relates to a compound of formula (I), or a pharmaceutically acceptable salt or ester thereof, formula (I): wherein: R1 is C3-8-cycloalkyl; X is O, NR7 or C3-6-heterocycloalkyl; R2 is aryl, heteroaryl, fused or unfused aryl-C3-6-heterocycloalkyl or fused or unfused heteroaryl-C3-6-heterocycIoalkyl, each of which is optionally substituted by one or more substitutents selected from aryl, heteroaryl, C1-6-alkyl, C3-7-cycloalkyl and a group A, wherein said C1-6-alkyl group is optionally substituted by one or more substituents selected from aryl, heteroaryl, R10 and a group A, said heteroaryl group is optionally substituted by one or more R10 groups; and wherein said C3-6-heterocycloalkyl group optionally contains one or more groups selected from oxygen, sulfur, nitrogen and CO; R3 is C1-6-alkyl optionally substituted by one or more substituents selected from aryl, heteroaryl, -NR4R5, -OR6, -NR7(CO)R6, -NR7(CO)NR4R5, -NR7SO2R6, -NR7COOR7, -CONR4R5, C3-6-heterocycloalkyl and formula (a, b, c): wherein R4-7 and A are as defined in the claims. Further aspects relate to the use of said compounds in the treatment of various therapeutic disorders, and more particularly as inhibitors of one or more kinases.
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Page/Page column 106-107
(2009/10/30)
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- PIPERIDINYL-SUBSTITUTED ISOQUINOLONE DERIVATIVES AS RHO-KINASE INHIBITORS
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The invention relates to 6-piperidinyl-substituted isoquinolone derivatives of the formula (I) or isoquinoline derivatives of the formula (I′) useful for the treatment and/or prevention of diseases associated with Rho-kinase and/or Rho-kinase mediated pho
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Page/Page column 46
(2008/06/13)
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- NAPHTHALINE DERIVATIVES USEFUL AS HISTAMINE-3-RECEPTOR LIGANDS
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The present invention relates to compounds of formula (I) wherein A, R1 and R2 are as defined in the description and claims, and pharmaceutically acceptable salts thereof, to the preparation of such compounds and pharmaceutical compositions containing them. The compounds are useful for the treatment and/or prevention of diseases which are associated with the modulation of H3 receptors.
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Page/Page column 78
(2008/06/13)
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- INDOLE DERIVATIVES AS HISTAMINE RECEPTOR ANTAGONISTS
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The present invention relates to compounds of formula (I) wherein X, R1, R2, R3, R4 and R5 are as defined in the description and claims, and pharmaceutically acceptable salts thereof, to the preparati
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Page/Page column 101-102
(2010/02/15)
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- AMIDE DERIVATIVES
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The invention concerns a compound of the Formula (I) wherein m is 0-2 and each R1 is a group such as hydroxy, halogeno, trifluoromethyl heterocyclyl and heterocyclyloxy; R2 is halogeno, trifluoromethyl or (1-6C)alkyl; R3 is hydrogen, halogeno or (1-6C)alkyl; and R4 is (3-6C)cycloalkyl;or pharmaceutically-acceptable salts thereof; processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of diseases or medical condions mediated by cytokines.
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Page/Page column 104
(2010/02/11)
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