- A straightforward enantioselective synthesis of F17807
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An efficient approach for the enantioselective synthesis of the 1,4-benzodioxane F17807 drug is reported. The developed route relied on two key steps, namely SNAr and Mitsunobu reactions, which permitted a straightforward access to the title co
- Alliot, Julien,Gravel, Edmond,Buisson, David-Alexandre,Larquetoux, Laurent,Nicolas, Marc,Doris, Eric
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Read Online
- Complexity of Blocking Bivalent Protein-Protein Interactions: Development of a Highly Potent Inhibitor of the Menin-Mixed-Lineage Leukemia Interaction
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The protein-protein interaction between menin and mixed-lineage leukemia 1 (MLL1) plays an important role in development of acute leukemia with translocations of the MLL1 gene and in solid tumors. Here, we report the development of a new generation of menin-MLL1 inhibitors identified by structure-based optimization of the thienopyrimidine class of compounds. This work resulted in compound 28 (MI-1481), which showed very potent inhibition of the menin-MLL1 interaction (IC50 = 3.6 nM), representing the most potent reversible menin-MLL1 inhibitor reported to date. The crystal structure of the menin-28 complex revealed a hydrogen bond with Glu366 and hydrophobic interactions, which contributed to strong inhibitory activity of 28. Compound 28 also demonstrates pronounced activity in MLL leukemia cells and in vivo in MLL leukemia models. Thus, 28 is a valuable menin-MLL1 inhibitor that can be used for potential therapeutic applications and in further studies regarding the role of menin in cancer.
- Borkin, Dmitry,Klossowski, Szymon,Pollock, Jonathan,Miao, Hongzhi,Linhares, Brian M.,Kempinska, Katarzyna,Jin, Zhuang,Purohit, Trupta,Wen, Bo,He, Miao,Sun, Duxin,Cierpicki, Tomasz,Grembecka, Jolanta
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Read Online
- Investigating alkyl nitrates as nitric oxide releasing precursors of multitarget acetylcholinesterase-monoamine oxidase B inhibitors
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Herein we envisaged the possibility of exploiting alkyl nitrates as precursors of alcohol-bearing dual inhibitors targeting acetylcholinesterase (AChE) and monoamine oxidase B (MAO B), key enzymes in neurodegenerative syndromes such as Alzheimer's disease (AD), through biotransformation unmasking an alcoholic function upon nitric oxide (NO) release. The cooperation to neuroprotection of low fluxes of NO and target enzymes’ inhibition by the alcohol metabolites might return a multitargeting effect. The in vitro screening towards ChEs and MAOs of a collection of 21 primary alcohols disclosed a subset of dual inhibitors, among which three diverse chemotypes were selected to study the corresponding nitrates. Nitrate 14 proved to be a brain permeant, potent AChE-MAO B inhibitor by itself. Moreover, it protected human SH-SY5Y lines against rotenone and hydrogen peroxide with a poor inherent cytotoxicity and showed a slow conversion profile to its alcohol metabolite 9d that still behaved as bimodal and neuroprotective molecule.
- Pisani, Leonardo,Iacobazzi, Rosa Maria,Catto, Marco,Rullo, Mariagrazia,Farina, Roberta,Denora, Nunzio,Cellamare, Saverio,Altomare, Cosimo Damiano
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p. 292 - 309
(2018/10/25)
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- N-(3-(7H-PYRROLO[2,3-D]PYRIMIDIN-4-YL)PHENYL)BENZAMIDE DERIVATIVES
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The invention relates to compounds of the formula (I) (I) or a pharmaceutically acceptable salt thereof, wherein the substituents are as defined in the specification; to intermediates in the preparation of the compounds, to pharmaceutical compositions comprising the compounds and to use of the compounds in the treatment of disease.
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Page/Page column 99
(2019/10/23)
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- Piperidine amino derivative and application thereof in fighting schizophrenia
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The invention discloses a piperidine amino compound and an application thereof in fighting schizophrenia. Pharmacological experiment results show that the piperidine amino compound related to by the invention has good water solubility, has high affinity with dopamine D, D, 5-HT, and 5-HT receptors, and has good selectivity on D/D receptors. In-vivo test results show that a preferable compound has a good anti-schizophrenia effect, is relatively low in acute toxicity, high in safety and good in pharmacokinetic characteristic, and has a development value as a high-efficiency low-toxicity novel anti-schizophrenia new drug. The piperidine amino compounds are compounds represented as a structural general formula (I), or salts of the compounds, or hydrates of the salts.
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- NEW ANTI-MALARIAL AGENTS
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The present invention is related to new trioxolane derivatives of formula (I) in the manufacture of a medicament for preventing or treating malaria. Specifically, the present invention is related to trioxolane derivatives useful for the preparation of a pharmaceutical formulation for the inhibition of malaria parasite proliferation.
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Paragraph 0154; 0155
(2018/04/26)
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- Design, synthesis and biological evaluation of 7H-pyrrolo[2,3-d]pyrimidin-4-amine derivatives as selective Btk inhibitors with improved pharmacokinetic properties for the treatment of rheumatoid arthritis
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Bruton's tyrosine kinase (Btk) is a Tec family kinase with a well-defined role in the B cell receptor (BCR) and Fcγ receptor (FcR) signaling pathways, which makes it a uniquely attractive target for the treatment of autoimmune diseases, such as rheumatoid arthritis (RA). We reported a series of compounds bearing 7H-pyrrolo [2,3-d]pyrimidin-4-amine scaffold that potently inhibited Btk in vitro. Analysis of the structure-activity relationships (SAR) and drug-like profiles led to the discovery of the optimal compound B16. B16 preferentially inhibited Btk (IC50 = 21.70 ± 0.82 nM) over closely related kinases with moderate selectivity. Cell-based tests also confirmed that B16 significantly inhibited Btk Y223 auto-phosphorylation and PLCγ2 Y1217 phosphorylation. MTT revealed that B16 displayed weak suppression against normal LO2, HEK293 and THP-1 cell lines with IC50 values over 30 μM. Moreover, B16 showed very weak potential to block the hERG channel (IC50 = 11.10 μM) in comparison to ibrutinib (IC50 = 0.97 μM). Owing to its favorable physicochemical properties (ClogP = 2.53, aqueous solubility ≈ 0.1 mg/mL), pharmacokinetic profiles (F = 49.15%, t1/2 = 7.02 h) and reasonable CYP450 profile, B16 exhibited potent anti-arthritis activity and similar efficacy to ibrutinib in reducing paw thickness in CIA mice. In conclusion, B16 is a potent, selective and durable inhibitor of Btk and has the potential to a safe and efficacious treatment for arthritis.
- He, Linhong,Pei, Heying,Zhang, Chufeng,Shao, Mingfeng,Li, Dan,Tang, Mingli,Wang, Taijing,Chen, Xiaoxin,Xiang, Mingli,Chen, Lijuan
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- 2-(BICYCLO-HETEROARYL)-ISONICOTINIC DERIVATIVES AS HISTONE DEMETHYLASE INHIBITORS
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The invention relates to compounds of Formula (I) as described herein, useful as histone demethylase inhibitors. The invention also relates to pharmaceutical compositions comprising these compounds and to their use in therapy, including e.g., in the treatment of cancer.
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Page/Page column 89
(2018/09/12)
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- With anti-platelet aggregation activity of the piperidinyl substituted 5- hydroxy color acid derivatives
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The invention relates to the field of pharmaceutical chemistry, particularly piperidyl substituted 5-hydroxytryptophane derivatives (I) with anti-platelet aggregation activity, and a preparation method and pharmaceutical application thereof, wherein R1, R2 and n are defined in the specification. The pharmacodynamical test proves that the piperidyl substituted 5-hydroxytryptophane derivatives have favorable anti-platelet aggregation activity.
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- Synthesis and pharmacological characterization of novel N-(trans-4-(2-(4-(benzo[d]isothiazol-3-yl)piperazin-1-yl)ethyl)cyclohexyl)amides as potential multireceptor atypical antipsychotics
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A series of novel benzisothiazolylpiperazine derivatives combining potent dopamine D2and D3, and serotonin 5-HT1Aand 5-HT2Areceptor properties were synthesized and evaluated for their potential antipsychotic properties. The most-promising derivative was 9j. The unique pharmacological features of 9j were a high affinity for D2, D3, 5-HT1A, and 5-HT2Areceptors, together with a 20-fold selectivity for the D3versus D2subtype, and a low affinity for muscarinic M1(reducing the risk of anticholinergic side effects), and for hERG channels (reducing incidence of QT interval prolongation). In animal behavioral models, 9j inhibited the locomotor-stimulating effects of phencyclidine, blocked conditioned avoidance response, and improved the cognitive deficit in the novel object recognition tests in rats. 9j exhibited a low potential for catalepsy, consistent with results with risperidone. In addition, favorable brain penetration of 9j in rats was detected. These studies have demonstrated that 9j is a potential atypical antipsychotic candidate.
- Chen, Xiao-Wen,Sun, Yuan-Yuan,Fu, Lei,Li, Jian-Qi
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p. 332 - 353
(2016/08/04)
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- TARGETED THERAPEUTICS
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The present invention provides pharmacological compounds including an effector moiety conjugated to a binding moiety that directs the effector moiety to a biological target of interest. Likewise, the present invention provides compositions, kits, and methods (e.g., therapeutic, diagnostic, and imaging) including the compounds. The compounds can be described as a protein interacting binding moiety-drug conjugate (SDC-TRAP) compounds, which include a protein interacting binding moiety and an effector moiety. For example, in certain embodiments directed to treating cancer, the SDC-TRAP can include an Hsp90 inhibitor conjugated to a cytotoxic agent as the effector moiety.
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- TARGETED THERAPEUTICS
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The present invention provides pharmacological compounds including an effector moiety conjugated to a binding moiety that directs the effector moiety to a biological target of interest. Likewise, the present invention provides compositions, kits, and methods (e.g., therapeutic, diagnostic, and imaging) including the compounds. The compounds can be described as a protein interacting binding moiety-drug conjugate (SDC-TRAP) compounds, which include a protein interacting binding moiety and an effector moiety. For example, in certain embodiments directed to treating cancer, the SDC-TRAP can include an Hsp90 inhibitor conjugated to a cytotoxic agent as the effector moiety.
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- TARGETED THERAPEUTICS
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The present invention provides pharmacological compounds including an effector moiety conjugated to a binding moiety that directs the effector moiety to a biological target of interest. Likewise, the present invention provides compositions, kits, and methods (e.g., therapeutic, diagnostic, and imaging) including the compounds. The compounds can be described as a protein interacting binding moiety-drug conjugate (SDC-TRAP) compounds, which include a protein interacting binding moiety and an effector moiety. For example, in certain embodiments directed to treating cancer, the SDC-TRAP can include an Hsp90 inhibitor conjugated to a cytotoxic agent as the effector moiety.
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- GHRELIN O-ACYL TRANSFERASE INHIBITOR
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The present invention provides novel GOAT inhibitors and their salts and pharmaceutical compositions thereof.
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Paragraph 0033-0034
(2015/05/26)
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- SUBSTITUTED PIPERIDYL-ETHYL-PYRIMIDINE AS GHRELIN O-ACYL TRANSFERASE INHIBITOR
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The present invention provides novel GOAT inhibitors and their salts and pharmaceutical compositions thereof.
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Page/Page column 9
(2015/06/03)
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- NOVEL INDOLE DERIVATIVE COMPOUND AND PHARMACEUTICAL COMPOSITION COMPRISING THE SAME
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The present invention provides a novel indole derivative compound, an isomer thereof, a pharmaceutically acceptable salt thereof, or a hydrate or solvate thereof. The compound according to the present invention can selectively inhibit histone deacetylase (HDAC), and thus can be used to effectively treat a disease associated with histone deacetylase (HDAC) activity.
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Paragraph 468-470
(2015/07/16)
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- AUTOTAXIN INHIBITORS COMPRISING A HETEROAROMATIC RING-BENZYL-AMIDE-CYCLE CORE
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The present invention relates to novel compounds that are autotaxin inhibitors, processes for their preparation, pharmaceutical compositions and medicaments containing them and to their use in diseases and disorders mediated by autotaxin.
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Page/Page column 336
(2015/02/02)
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- TARGETED THERAPEUTICS
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The present invention provides pharmacological compounds including an effector moiety conjugated to a binding moiety that directs the effector moiety to a biological target of interest. Likewise, the present invention provides compositions, kits, and methods (e.g., therapeutic, diagnostic, and imaging) including the compounds. The compounds can be described as a protein interacting binding moiety-drug conjugate (SDC-TRAP) compounds, which include a protein interacting binding moiety and an effector moiety. For example, in certain embodiments directed to treating cancer, the SDC-TRAP can include an Hsp90 inhibitor conjugated to a cytotoxic agent as the effector moiety.
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- SUBSTITUTED TETRAHYDROISOQUINOLINE COMPOUNDS AS FACTOR XIA INHIBITORS
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The present invention provides compounds of Formula (I) or stereoisomers, pharmaceutically acceptable salts thereof, wherein all of the variables are as defined herein. These compounds are inhibitors of factor XIa and/or plasma kallikrein which may be used as medicaments.
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Paragraph 00339
(2013/04/25)
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- Discovery of (2 S)-1-[4-(2-{6-amino-8-[(6-bromo-1,3-benzodioxol-5-yl) sulfanyl]-9 H-purin-9-yl}ethyl)piperidin-1-yl]-2-hydroxypropan-1-one (MPC-3100), a purine-based Hsp90 inhibitor
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Modulation of Hsp90 (heat shock protein 90) function has been recognized as an attractive approach for cancer treatment, since many cancer cells depend on Hsp90 to maintain cellular homeostasis. This has spurred the search for small-molecule Hsp90 inhibitors. Here we describe our lead optimization studies centered on the purine-based Hsp90 inhibitor 28a containing a piperidine moiety at the purine N9 position. In this study, key SAR was established for the piperidine N-substituent and for the congeners of the 1,3-benzodioxole at C8. These efforts led to the identification of orally bioavailable 28g that exhibits good in vitro profiles and a characteristic molecular biomarker signature of Hsp90 inhibition both in vitro and in vivo. Favorable pharmacokinetic properties along with significant antitumor effects in multiple human cancer xenograft models led to the selection of 28g (MPC-3100) as a clinical candidate.
- Kim, Se-Ho,Bajji, Ashok,Tangallapally, Rajendra,Markovitz, Benjamin,Trovato, Richard,Shenderovich, Mark,Baichwal, Vijay,Bartel, Paul,Cimbora, Daniel,McKinnon, Rena,Robinson, Rosann,Papac, Damon,Wettstein, Daniel,Carlson, Robert,Yager, Kraig M.
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p. 7480 - 7501
(2012/11/06)
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- Substituted Benzamide Compounds
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Substituted benzamide compounds corresponding to formula (I) in which R5, R6, R7, R8, a, b, c, d, t, D and X have defined meanings, a process for their preparation, pharmaceutical compositions comprising such compounds, and a method of using such compounds to treat pain and other conditions mediated at least in part via the bradykinin 1 receptor.
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- PRODRUGS OF THERAPEUTIC COMPOUNDS
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The present invention provides compounds, pharmaceutical compositions and medicaments comprising such compounds, and the use of these compounds, compositions, and medicaments in methods of treating diseases and disorders such as cancers.
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Page/Page column 41-42
(2012/11/13)
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- Design and synthesis of novel sulfonamide-containing bradykinin hB 2 receptor antagonists. Synthesis and structure-relationships of α,α-tetrahydropyranylglycine
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A series of α,α-cycloalkylglycine sulfonamide compounds of general formula 1 has previously been identified by our group as selective human B2(hB2) receptor antagonists. Here we report the in vitro and in vivo BK antagonist activity
- Fincham, Christopher I.,Bressan, Alessandro,D'Andrea, Piero,Ettorre, Alessandro,Giuliani, Sandro,Mauro, Sandro,Meini, Stefania,Paris, Marielle,Quartara, Laura,Rossi, Cristina,Squarcia, Antonella,Valenti, Claudio,Daniela, Fattori,Maggi, Carlo Alberto
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supporting information; experimental part
p. 2091 - 2100
(2012/05/05)
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- 2,5-Disubstituted pyridines as potent GPR119 agonists
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A series of 2-piperazinyl-5-alkoxypyridines were synthesized and screened against human GPR119 receptor. Through SAR analysis, compounds containing 2-alkylsulfonylpiperazinyl-5-alkoxypyridines were discovered and found to be potent agonists of the human GPR119 receptor.
- Wu, Yulin,Kuntz, Judith D.,Carpenter, Andrew J.,Fang, Jing,Sauls, Howard R.,Gomez, Daniel J.,Ammala, Carina,Xu, Yun,Hart, Shane,Tadepalli, Sarva
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scheme or table
p. 2577 - 2581
(2010/06/19)
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- Indol-3-ylcycloalkyl ketones: Effects of N1 substituted indole side chain variations on CB2 cannabinoid receptor activity
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Several 3-acylindoles with high affinity for the CB2 cannabinoid receptor and selectivity over the CB1 receptor have been prepared. A variety of 3-acyl substituents were investigated, and the tetramethylcyclopropyl group was found to lead to high affinity CB2 agonists (5, 16). Substitution at the N1-indole position was then examined. A series of aminoalkylindoles was prepared and several substituted aminoethyl derivatives were active (23-27, 5) at the CB2 receptor.Astudy of N1 nonaromatic side chain variants provided potent agonists at the CB2 receptor (16, 35-41, 44-47, 49-54, and 57-58). Several polar side chains (alcohols, oxazolidinone) were well-tolerated for CB2 receptor activity (41, 50), while others (amide, acid) led to weaker or inactive compounds (55 and 56). N1 aromatic side chains also afforded several high affinity CB2 receptor agonists (61, 63, 65, and 69) but were generally less potent in an in vitro CB2 functional assay than were nonaromatic side chain analogues.
- Frost, Jennifer M.,Dart, Michael J.,Tietje, Karin R.,Garrison, Tiffany R.,Grayson, George K.,Daza, Anthony V.,El-Kouhen, Odile F.,Yao, Betty B.,Hsieh, Gin C.,Pai, Madhavi,Zhu, Chang Z.,Chandran, Prasant,Meyer, Michael D.
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experimental part
p. 295 - 315
(2010/06/11)
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- Therapeutic Compounds and Their Use in Treating Diseases and Disorders
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The invention provides novel therapeutic compounds, pharmaceutical compositions comprising these compounds, and methods for using these compounds and compositions to treat diseases and disorders, such as cancer.
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Page/Page column 141-142
(2009/06/27)
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- GPCR AGONISTS
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Compounds of formula (I): or pharmaceutically acceptable salts thereof, are GPCR agonists and are useful as for the treatment of obesity and diabetes.
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Page/Page column 21
(2010/11/25)
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- NEW CARBONYLATED (AZA)CYCLOHEXANES AS DOPAMINE D3 RECEPTOR LIGANDS
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The invention relates to compounds of the general formula (I): to the process for preparing them, and to the use thereof as a therapeutic agent.
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Page/Page column 99
(2008/06/13)
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- PYRIDYL NON-AROMATIC NITROGENATED HETEROCYCLIC-1-CARBOXYLATE ESTER DERIVATIVE
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[Problem] To provide a compound usable for treatment of diseases associated with fatty acid amide hydrolase (FAAH), especially for treatment of urinary frequency and urinary incontinence, overactive bladder and/or pain. [Means for Solution] We have found that a novel pyridyl non-aromatic nitrogen-containing heterocyclic-1-carboxylate derivative and its pharmaceutically acceptable salt has a potent FAAH-inhibitory activity. Further, the pyridyl non-aromatic nitrogen-containing heterocyclic-1-carboxylate derivative of the present invention has an excellent effect for increasing an effective bladder capacity, an excellent effect for relieving urinary frequency and an excellent anti-allodynia effect, and is therefore usable for treatment of urinary frequency and urinary incontinence, overactive bladder and/or pain.
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Page/Page column 29
(2008/06/13)
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- 3-CYCLOALKYLCARBONYL INDOLES AS CANNABINOID RECEPTOR LIGANDS
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The present invention provides novel compounds of Formula (I), which are CB2 selective ligands useful for the treatment of pain.
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Page/Page column 37
(2008/06/13)
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- SUBSTITUTED PIPERAZINES AS CB1 ANTAGONISTS
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Compounds of Formula (I): Chemical formula should be inserted here as it appears on the abstract in paper form. or pharmaceutically acceptable salts, solvates, or esters thereof, are useful in treating diseases or conditions mediated by CB1 receptors, such as metabolic syndrome and obesity, neuroinflammatory disorders, cognitive disorders and psychosis, addiction (e.g., smoking cessation), gastrointestinal disorders, and cardiovascular conditions.
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Page/Page column 181
(2010/11/08)
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- Substituted homopiperidine, piperidine or pyrrolidine derivatives
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A novel class of substituted homopiperidine, piperidine and pyrrolidine derivatives, methods for their preparation, pharmaceutical compositions comprising them and use thereof in the treatment of disorders related to the histamine H3 receptor. More particularly, the compounds possess histamine H3 receptor antagonistic activity and are thus useful in the treatment of disorders in which a histamine H3 receptor blockade is beneficial.
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Page/Page column 13-14
(2010/02/11)
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- PYRAZOLOPYRIDINE DERIVATES
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New compounds of formula (I) and the salts, solvates and prodrugs thereof, wherein the meanings for the various substituents are as disclosed in the description. These compounds are useful as p38 kinase inhibitors.
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- SUBSTITUTED HOMOPIPERIDINE, PIPERIDINE OR PYRROLIDINE DERIVATIVES
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A novel class of substituted homopiperidin, piperidine and pyrrolidine derivatives, methods for their preparation, pharmaceutical compositions comprising them and use thereof in the treatment of disorders related to the histamine H3 receptor. More particularly, the compounds possess histamine H3 receptor antagonistic activity and are useful in the treatment of disorders in which a histamine H3 receptor blockade is beneficial.
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- BENZIMIDAZOLONE DERIVATIVES
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This invention relates to benzimidazolone derivatives, represented by compounds of a general formula [I] ???[in which R1 and R2 stand for, e.g., hydrogen atoms; R3a, R3b, R4, R5 stand for, e.g., hydrogen atoms and alkyl groups; R6 stands for e.g., aryl or heteroaryl groups; A ring stands for 5- to 8-membered aliphatic heterocyclic ring containing one nitrogen atom; and Z stands for carbonyl group or sulfonyl group]. The benzimidazolone derivatives of the invention exhibit antagonism to muscarinic acetylcholine receptors, and are useful as treating agent and/or prophylactic of Parkinson's disease; drug-induced parkinsonism, dystonia, akinesia, pancreatitis, bilestone/cholecystitis, biliary dyskinesia, achalasia, pain, itch, cholinergic urticaria, irritable bowel syndrome, vomiting, nausea, dizziness, Meniere's disease, motion sickness and urinary disturbance.
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- Muscarinic M3 receptor antagonists with (2R)-2-[(1R)-3,3-Difluorocyclopentyl]-2-hydroxyphenylacetamide Structures. Part 2
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Optimization of the amine part of our original muscarinic M3 receptor antagonist 1 was performed to identify M3 receptor antagonists that are superior to 1. Compounds carrying a variety of diamine moieties without hydrophobic substituent on the nitrogen atom were screened against the binding affinity for the M3 receptor and the selectivity for M3 over the M1 and M2 receptors. This process led to a 4-aminopiperidinamide (2l) with a Ki value of 5.1 nM and with a selectivity of the M3 receptor that was 46-fold greater than that of the M2 receptor. Further derivatization of 2l by inserting a spacer group or by incorporating alkyl group(s) into the amine part resulted in the identification of an 4-(aminoethyl)piperidinamide 2l-b with a Ki value of 3.7 nM for the M3 receptor and a selectivity for the M3 receptor that was 170-fold greater than that of the M2 receptor.
- Ogino, Yoshio,Ohtake, Norikazu,Kobayashi, Kensuke,Kimura, Toshifumi,Fujikawa, Toru,Hasegawa, Takuro,Noguchi, Kazuhito,Mase, Toshiaki
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p. 2167 - 2172
(2007/10/03)
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- Carboxylic acid derivatives, medicaments comprising these compounds, their use and processes for their production
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The present invention relates to carboxylic acid derivatives of the general formula STR1 in which Ra to Rc, A, B, D, E and X1 to X3 are as defined in claim 1, their tautomers, their stereoisomers including their mixtures, and their salts, in particular their physiologically tolerated salts with inorganic or organic acids or bases, which have useful pharmacological properties, preferably aggregation-inhibiting inhibiting actions, medicaments containing these compounds, their use and processes for their preparation.
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- Cyclic urea derivatives, pharmaceutical compositions containing these compounds and processes for preparing them
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The invention relates to cyclic urea derivatives of general formula I STR1 wherein Ra, Rb, X and Y are defined as in claim 1, the tautomers, stereoisomers and salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, which have valuable pharmacological properties, preferably aggregation inhibiting effects, and to drugs containing the compounds and processes for preparing them.
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