cas 120157-97-3, N-BOC-2-(4-BROMO-PHENYL)-ETHYLAMINE

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Studies toward the development of new silicon-containing building blocks for the direct 18F-labeling of peptides
Silicon-containing prosthetic groups have been conjugated to peptides to allow for a single-step labeling with 18F radioisotope. The fairly lipophilic di-tert-butylphenylsilane building block contributes unfavorably to the pharmacokinetic profile of bombesin conjugates. In this article, theoretical and experimental studies toward the development of more hydrophilic silicon-based building blocks are presented. Density functional theory calculations were used to predict the hydrolytic stability of di-tert-butylfluorosilanes 2-23 with the aim to improve the in vivo properties of 18F-labeled silicon-containing biomolecules. As a further step toward improving the pharmacokinetic profile, hydrophilic linkers were introduced between the lipophilic di-tert-butylphenylsilane building block and the bombesin congeners. Increased tumor uptake was shown with two of these peptides in xenograft-bearing mice using positron emission tomography and biodistribution studies. The introduction of a hydrophilic linker is thus a viable approach to improve the tumor uptake of 18F-labeled silicon-bombesin conjugates.
Dialer, Lukas O.,Selivanova, Svetlana V.,Müller, Carmen J.,Müller, Adrienne,Stellfeld, Timo,Graham, Keith,Dinkelborg, Ludger M.,Kr?mer, Stefanie D.,Schibli, Roger,Reiher, Markus,Ametamey, Simon M.
p. 7552 - 7563
(2013)
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H2O2/Peroxynitrite-Activated Hydroxamic Acid HDAC Inhibitor Prodrugs Show Antileukemic Activities against AML Cells
Occurrence of acute myeloid leukemia (AML) results in abundant endogenous reactive oxygen species (ROS)/reactive nitrogen species (RNS) in AML cells and in disease-relevant microenvironments. Histone deacetylase inhibitor (HDACi) prodrug approach was designed accordingly by masking the hydroxamic acid zinc binding group with hydrogen peroxide (H2O2)/peroxynitrite (PNT)-sensitive, self-immolative aryl boronic acid moiety. Model prodrugs 5-82 and 5-23 were activated in AML cells to release cytotoxic HDACis, evidenced by inducing acetylation markers and reducing viability of AML cells. Intracellular activation and antileukemic activities of prodrug were increased or decreased by ROS/PNT inducers and scavengers, respectively. Prodrugs 5-82 and 5-23 also enhanced the potency of chemotherapy drug cytarabine, supporting the potentials of this prodrug class in combinatorial treatment.
Liao, Yi,Xu, Liping,Ou, Siyu,Edwards, Holly,Luedtke, Daniel,Ge, Yubin,Qin, Zhihui
p. 635 - 640
(2018)
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Optimization and Evaluation of Novel Antifungal Agents for the Treatment of Fungal Infection
Due to the increased morbidity and mortality by fungal infections and the emergence of severe antifungal resistance, there is an urgent need for new antifungal agents. Here, we screened for antifungal activity in our in-house library through the minimum inhibitory concentration test and derived two hit compounds with moderate antifungal activities. The hit compounds' antifungal activities and drug-like properties were optimized by substituting various aryl ring, alkyl chain, and methyl groups. Among the optimized compounds, 22h was the most promising candidate with good drug-like properties and exhibited potent fast-acting fungicidal antifungal effects against various fungal pathogens and synergistic antifungal activities with some known antifungal drugs. Additionally, 22h was further confirmed to disturb fungal cell wall integrity by activating multiple cell wall integrity pathways. Furthermore, 22h exerted significant antifungal efficacy in both the subcutaneous infection mouse model and ex vivo human nail infection model.
Bahn, Yong-Sun,Cheong, Eunji,Choi, Ji Won,Jang, Bo Ko,Kim, Dahee,Kim, Hyeon Jeong,Kim, Hyeon Ji,Kim, Siwon,Lee, Dong-Gi,Lee, Jong-Seung,Lee, Kyung-Tae,Lee, Myung Ha,Lee, Ye Rim,Park, Jong-Hyun,Park, Ki Duk,Park, Sun Jun,Seo, Kyung Jin,Yeon, Seul Ki
supporting information
p. 15912 - 15935
(2021/11/10)

COMPOUNDS
Compounds of general formula (I) wherein R1, R2, R3, R4 and X are as defined herein are inhibitors of the epithelial sodium channel (ENaC) and are useful for the treatment or prevention respiratory diseases and
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Paragraph 0951-0954

(2021/06/26)

SELECTIVE NEURONAL NITRIC OXIDE SYNTHASE INHIBITORS
Disclosed are 7-phenyl-2-aminoquinoline compounds that are shown to inhibit the biological activity of neuronal nitric oxide synthases (nNOSs). Also disclosed are pharmaceutical compositions comprising the compounds, and methods of using the compounds and
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Paragraph 0092; 0109

(2021/04/30)

Direct Access to Primary Amines from Alkenes by Selective Metal-Free Hydroamination
Direct and selective synthesis of primary amines from easily available precursors is attractive yet challenging. Herein, we report the rapid synthesis of primary amines from alkenes via metal-free regioselective hydroamination at room temperature. Ammonium carbonate was used as ammonia surrogate for the first time, allowing for efficient conversion of terminal and internal alkenes into linear, α-branched, and α-tertiary primary amines under mild conditions. This method provides a straightforward and powerful approach to a wide spectrum of advanced, highly functionalized primary amines which are of particular interest in pharmaceutical chemistry and other areas.
Du, Yi-Dan,Chen, Bi-Hong,Shu, Wei
supporting information
p. 9875 - 9880
(2021/03/29)

Amphiphilic Polymeric Nanoparticles for Photoredox Catalysis in Water
Photoredox catalysis has recently emerged as a powerful synthesis tool in organic and polymer chemistry. In contrast to the great achievements realized in organic solvents, performing photocatalytic processes efficiently in aqueous media encounters several challenges. Here, it is presented how amphiphilic single-chain polymeric nanoparticles (SCPNs) can be utilized as small reactors to conduct light-driven chemical reactions in water. By incorporating a phenothiazine (PTH) catalyst into the polymeric scaffold, metal-free reduction and C?C cross-coupling reactions can be carried out upon exposure to UV light under ambient conditions. The versatility of this approach is underlined by a large substrate scope, tolerance towards oxygen, and excellent recyclability. This approach thereby contributes to a sustainable and green way of implementing photoredox catalysis.
Eisenreich, Fabian,Meijer,Palmans, Anja R. A.
supporting information
p. 10355 - 10361
(2020/07/27)

IRAK DEGRADERS AND USES THEREOF
The present invention provides compounds, compositions thereof, and methods of using the same.
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Paragraph 00962; 004581-004583

(2020/06/19)

First Contact: 7-Phenyl-2-Aminoquinolines, Potent and Selective Neuronal Nitric Oxide Synthase Inhibitors That Target an Isoform-Specific Aspartate
Inhibition of neuronal nitric oxide synthase (nNOS), an enzyme implicated in neurodegenerative disorders, is an attractive strategy for treating or preventing these diseases. We previously developed several classes of 2-aminoquinoline-based nNOS inhibitor
Cinelli, Maris A.,Reidl, Cory T.,Li, Huiying,Chreifi, Georges,Poulos, Thomas L.,Silverman, Richard B.
p. 4528 - 4554
(2020/05/05)

CHEMICAL COMPOUNDS
The present disclosure describes novel compounds, or their pharmaceutically acceptable salts, pharmaceutical compositions containing them, and their medical uses. The compounds of the disclosure have activity as prostaglandin EP4 receptor antagonists, and are useful in the treatment or alleviation of pain and inflammation and other inflammation-associated disorders, such as arthritis, treating or preventing disorders or medical conditions selected from pain, inflammatory diseases and the like. Also described herein are methods of treating pain by administering the compounds of the disclosure, which are EP4 receptor antagonists.
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Paragraph 0110-0112

(2020/08/22)

P300/CBP HAT INHIBITORS
Provided are compounds of Formula (I): and pharmaceutically acceptable salts and compositions thereof, which are useful for treating a variety of conditions associated with histone acetyltransferase (HAT).
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Paragraph 00102; 00176-00177

(2019/09/04)

BIS(PENTAHYDROXYHEXYL)AMINO SUBSTITUTED 2-{[(3-AMINO-PYRAZIN-2-YL)FORMAMIDO]METHYL}-1H-1,3-BENZODIAZOL-3-IUM DERIVATIVES AS ENAC INHIBITORS FOR TREATING RESPIRATORY DISEASES
The present invention discloses bis(pentahydroxyhexyl)amino substituted 2-{[(3-amino-pyrazin-2-yl)formamido]methyl}-1H-1,3- benzodiazol-3-ium derivatives of formula (I) as inhibitors of ENaC and are of use in the treatment of respiratory diseases and conditions, skin conditions or ocular conditions, wherein the respiratory disease or condition is e.g. cystic fibrosis, chronic obstructive pulmonary disease (COPD), chronic bronchitis, emphysema, bronchiectasis, including non-cystic fibrosis bronchiectasis, and asthma; the skin condition is e.g. psoriasis, atopic dermatitis and ichthyosis; and the ocular condition is e.g. dry eye disease.
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Page/Page column 60; 61

(2019/05/10)

Compound 1-[2-[4-(2-ethyl-6,8-dimethylimidazo[1,2-α]pyrazin-3-yl)phenyl]ethyl]-3-(p-tolylsulfonyl)urea as a prostaglandin EP4 receptor antagonist
The present invention describes novel compounds, or veterinary or pharmaceutically acceptable salts thereof, veterinary or pharmaceutical compositions thereof, and medical uses thereof. The compounds of the invention have activity as prostaglandin EP4 rec
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Page/Page column 17

(2019/04/15)

Diketopyrrolopyrrole derivative and application thereof
The invention provides a diketopyrrolopyrrole derivative and application thereof as well as relates to a diketopyrrolopyrrole derivative. The structural formula of the diketopyrrolopyrrole derivativeis as shown in a formula (I): the formula (I) is as shown in the description; in the formula (I), R1 is selected from a group as shown in a formula (I-a), a formula (I-b), a formula (I-c), a formula (I-d) or a formula (I-e) (the formulas are as shown in the description); and in the formula (I-a), the formula (I-b), the formula (I-c), the formula (I-d) and the formula (I-e), * shows connection position. The diketopyrrolopyrrole derivative has excellent photoelectric property and can be applied in the field of organic photoelectric functional devices.
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Paragraph 0067; 0068; 0069

(2018/12/05)

Synthesis and evaluation of biaryl derivatives for structural characterization of selective monoamine oxidase B inhibitors toward Parkinson's disease therapy
Benzyloxyphenyl moiety is a common structure of highly potent, selective and reversible inhibitors of monoamine oxidase B (MAO-B), safinamide and sembragiline. We synthesized 4-(benzyloxy)phenyl and biphenyl-4-yl derivatives including halogen substituents on the terminal aryl unit. In addition, we modified the carbon linker between amine group and the biaryl linked unit. Among synthesized compounds, 12c exhibited the most potent and selective MAO-B inhibitory effect (hMAO-B IC50: 8.9 nM; >10,000-fold selectivity over MAO-A) as a competitive inhibitor. In addition, 12c showed greater MAO-B inhibitory activity and selectivity compared to well-known MAO-B inhibitors such as selegiline, safinamide and sembragiline. In the MPTP-induced mouse model of Parkinson's disease (PD), 12c significantly protected the tyrosine hydroxylase (TH)-immunopositive DAergic neurons and attenuated the PD-associated behavioral deficits. This study suggests characteristic structures as a MAO-B inhibitor that may provide a good insight for the development of therapeutic agents for PD.
Yeon, Seul Ki,Choi, Ji Won,Park, Jong-Hyun,Lee, Ye Rim,Kim, Hyeon Jeong,Shin, Su Jeong,Jang, Bo Ko,Kim, Siwon,Bahn, Yong-Sun,Han, Gyoonhee,Lee, Yong Sup,Pae, Ae Nim,Park, Ki Duk
supporting information
p. 232 - 244
(2017/12/08)

BENZODIAZOLIUM COMPOUNDS AS ENAC INHIBITORS
Compounds of general formula (I) wherein R1, R2, R3, R4, R5 and X are as defined herein are inhibitors of the epithelial sodium channel (ENaC) and are useful for the treatment or prevention respirator
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Page/Page column 153-154

(2018/06/12)

Phthalazone hydroxamic acid derivative as well as preparation method and application thereof
The invention discloses a phthalazone hydroxamic acid compound with poly(ADP-ribose) polymerase (PARP) and/or histone deacetylase (HDAC) inhibitory activity as well as a preparation method and application thereof. A structural formula of the phthalazone hydroxamic acid compound is shown in a formula I described in the specification, wherein R1 is a hydrogen atom or halogen, R2 is a hydrogen atom or halogen, Y is an oxygen atom, methylene or difluorine-substituted methylene, Z is described in the specification, and G is a chemical bond, methylene, fluoromethylene or a double bond. In vitro cell proliferation experiments show that the compound shown in the formula I can well inhibit proliferation of multiple tumor cells. A PARP and HDAC inhibitory experiment shows that the compound shown in the formula I is a compound with good inhibitory activity on PARP and/or HDAC.
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Paragraph 0051; 0054-0057

(2017/09/01)

THIENOPYRAZINE CARBOXAMIDES AS UBIQUITIN-SPECIFIC PROTEASE INHIBITORS
The disclosure relates to inhibitors of USP28 and/or USP25 useful in the treatment of cancers, inflammation, autoimmune diseases, and infectious diseases, having the Formula: (I), where R1, R2, R3, R4, R4', R5, R6, X, and n are described herein.
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Paragraph 00257

(2017/09/05)

THIENOPYRIDINE CARBOXAMIDES AS UBIQUITIN-SPECIFIC PROTEASE INHIBITORS
The disclosure relates to inhibitors of USP28 and/or USP25 useful in the treatment of cancers, inflammation, autoimmune diseases, and infectious diseases, having the Formula (I), where R1, R2, R3, R4, R5, R5', R6, R7, X, m, and n are described herein.
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Paragraph 00330

(2017/09/05)

Discovery of new antimalarial agents: Second-generation dual inhibitors against FP-2 and PfDHFR via fragments assembely
Malaria parasites are a leading cause of worldwide mortality from infectious disease. Cysteine protease falcipain-2 (FP-2) and Plasmodium falciparum dihydrofolate reductase (PfDHFR) play vital roles, which are absolutely essential, in the parasite life cycle. In this study, based on the structures of uniform fragments of reported PfDHFR inhibitors and the first-generation dual inhibitors against FP-2 and PfDHFR, we identified a novel series of dual inhibitors through fragments assembly. Lead optimization led to the discovery of 24, which showed high potency against FP-2 (IC50 = 10.0 μM), PfDHFR (IC50 = 84.1 nM), P. falciparum 3D7 (IC50 = 53.1 nM), clinical isolated strains Fab9 (IC50 = 14.2 nM) and GB4 (IC50 = 23.4 nM). The in vivo inhibition assays against P. berghei in 10 days indicated 24 had a more beneficial effect on the growth inhibition of P. berghei than artemisinin and an identical effect with pyrimethamine. Additionally, 24 moderately inhibited the proliferation of chloroquine-resistant P. falciparum Dd2 strain. Collectively, these data revealed that 24 could be an excellent lead compound as FP-2 and PfDHFR dual inhibitor for the treatment of malaria.
Chen, Wenhua,Huang, Zhenghui,Wang, Wanyan,Mao, Fei,Guan, Longfei,Tang, Yun,Jiang, Hualiang,Li, Jian,Huang, Jin,Jiang, Lubin,Zhu, Jin
p. 6467 - 6478
(2017/10/31)

Synthesis and biological evaluation of indole-2-carboxamides bearing photoactivatable functionalities as novel allosteric modulators for the cannabinoid CB1 receptor
5-Chloro-3-ethyl-N-(4-(piperidin-1-yl)phenethyl)-1H-indole-2-carboxamide (ORG27569, 1) is a prototypical allosteric modulator for the cannabinoid CB1 receptor. Based on this indole-2-carboxamide scaffold, we designed and synthesized novel CB1 allosteric m
Qiao, Chang-Jiang,Ali, Hamed I.,Ahn, Kwang H.,Kolluru, Srikanth,Kendall, Debra A.,Lu, Dai
p. 517 - 529
(2016/07/06)

INHIBITORS OF FATTY ACID AMIDE HYDROLASE
The present invention provides compounds, and pharmaceutically acceptable compositions thereof, encompassed by any of formulae (I), (II), (III), (IV), (V), or (VI), or subgenera thereof. The present invention also provides methods for treating an FAAH mediated disease, disorder or condition by administering a therapeutically effective amount of a compound or composition comprising a compound of any of formulae (I), (II), (III), (IV), (V), or (VI), or subgenera thereof, to a patient in need thereof. Additionally, the present invention provides methods for inhibiting FAAH by administering a therapeutically effective amount of a compound or composition comprising a compound of any of formulae (I), (II), (III), (IV), (V), or (VI), or subgenera thereof, to a patient in need thereof.
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Paragraph 1105

(2016/01/15)

HEPATITIS B CORE PROTEIN ALLOSTERIC MODULATORS
ABSTRACT The present disclosure provides, in part, compounds having allosteric effector properties against Hepatitis B virus Cp. Also provided herein are methods of treating viral infections, such as hepatitis B, comprising administering to a patient in need thereof a disclosed compound.
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Paragraph 000449

(2015/10/05)

MOLECULES HAVING CERTAIN PESTICIDAL UTILITIES, AND INTERMEDIATES, COMPOSITIONS, AND PROCESSES RELATED THERETO
This disclosure relates to the field of molecules having pesticidal utility against pests in Phyla Nematoda, Arthropoda, and/or Mollusca, processes to produce such molecules and intermediates used in such processes, compositions containing such molecules,
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Paragraph 0372; 0373

(2014/09/29)

Synthesis of photoreactive 2-phenethylamine derivatives-synthesis of adenosine derivatives enabling functional analysis of adenosine receptors by photoaffinity labeling
2-Phenylethylamine is well known as a substructure of many biologically active compounds, and the synthesis of its photoreactive derivatives to allow the analysis of biological functions is reported. This allowed us to synthesise ligands for adenosine rec
Murai, Yuta,Masuda, Katsuyoshi,Ogasawara, Yui,Wang, Lei,Hashidoko, Yasuyuki,Hatanaka, Yasumaru,Iwata, So,Kobayashi, Takuya,Hashimoto, Makoto
p. 2428 - 2433
(2013/05/22)

Preparation of phenylethylbenzamide derivatives as modulators of DNMT3 activity
DNA-methyltransferases (DNMTs) are a class of epigenetic enzymes that catalyze the transfer of a methyl moiety from the methyl donor S-adenosyl-l-methionine onto the C5 position of cytosine in DNA. This process is dysregulated in cancers and leads to the hypermethylation and silencing of tumor suppressor genes. The development of potent and selective inhibitors of DNMTs is of utmost importance for the discovery of new therapies for the treatment of cancer. We report herein the synthesis and DNMT inhibitory activity of 29 analogues derived from NSC 319745. The effect of selected compounds on the methylation level in the MDA-MB-231 human breast cancer cell line was evaluated using a luminometric methylation assay. Molecular docking studies have been conducted to propose a binding mode for this series.
Kabro, Anzhelika,Lachance, Hugo,Marcoux-Archambault, Iris,Perrier, Valerie,Dore, Vicky,Gros, Christina,Masson, Veronique,Gregoire, Jean-Marc,Ausseil, Frederic,Cheishvili, David,Laulan, Nathalie Bibens,St-Pierre, Yves,Szyf, Moshe,Arimondo, Paola B.,Gagnon, Alexandre
p. 1562 - 1570
(2013/12/04)

Peripherally Acting Opioid Compounds
The invention relates to a compound of Formula I, II, III, IV or a pharmaceutically acceptable ester or prodrug thereof:
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Page/Page column 16-17

(2013/02/28)

Tetrahydroquinoline Derivatives And Their Pharmaceutical Use
Tetrahydroquinoline compounds of formula (I) and salts thereof, pharmaceutical compositions containing such compounds and their use in therapy.
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Page/Page column 42

(2012/08/28)

INHIBITION OF BACTERIAL BIOFILMS WITH ARYL CARBAMATES
Disclosure is provided for carbamate compounds that prevent, remove and/or inhibit the formation of biofilms, compositions including these compounds, devices including these compounds, and methods of using the same.
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Page/Page column 33

(2012/02/01)

TETRAHYDROQUINOLINE DERIVATIVES AND THEIR PHARMACEUTICAL USE
Tetrahydroquinoline compounds of Formula (I) and salts thereof, pharmaceutical compositions containing such compounds and their use in therapy.
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Page/Page column 94-95

(2011/06/11)

Novel specific inhibitors of ubiquitin specific protease 7, the pharmaceutical compositions thereof and their therapeutic applications
The present invention concerns new compounds of formula (I), their process of preparation and their therapeutic use.
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Page/Page column 13

(2010/08/07)

SULFONYLATED TETRAHYDROAZOLOPYRAZINES AND THEIR USE AS MEDICINAL PRODUCTS
The present invention relates to sulfonylated tetrahydroazolopyrazines, methods for the preparation thereof, medicinal products containing these compounds and the use of substituted indole compounds for the preparation of medicinal products (Formula I).
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Page/Page column 118

(2010/09/18)

NOVEL INDOLE DERIVATIVE HAVING INHIBITORY ACTIVITY ON I B KINASE
Disclosed is a compound represented by the general formula (1) or a salt thereof. The compound or a salt thereof has an inhibitory activity on IKKβ and is therefore useful as preventive and/or therapeutic agent for a disease associated with IKKβ. In the formula, R1 represents a hydrogen atom, a lower alkyl group, an aryl group, a hydroxy group, or the like; R2 represents a halogen atom, a lower alkyl group, a lower alkenyl group, a lower alkynyl group, or the like; and m represents 0, 1, 2, or the like.
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Page/Page column 38

(2009/12/05)

HYDANTOIN DERIVATIVES USEFUL AS ANTIBACTERIAL AGENTS
This invention relates to compounds of the Formula (I): or a pharmaceutically acceptable salt, solvate, ester or isomer thereof, which is useful for the treatment of diseases or conditions mediated by LpxC.
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Page/Page column 47

(2008/06/13)

Methods and compositions for treating pain
The present application relates to compounds and methods for treating pain, incontinence and other conditions.
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Page/Page column 47

(2010/11/28)

NON-ANILINIC DERIVATIVES OF ISOTHIAZOL-3(2H)-ONE 1,1-DIOXIDES AS LIVER X RECEPTOR MODULATORS
The present invention relates to certain novel compounds of the formula (I) to processes for preparing such compounds, to their the utility in modulation of nuclear hormone receptors Liver X Receptor (LXR) α (NR1H3) and/or β (NR1H2) and in treating and/or preventing clinical conditions including cardiovascular diseases such as atherosclerosis; inflammatory diseases, Alzheimer's disease, lipid disorders (dyslipidemias) whether or not associated with insulin resistance, type 2 diabetes and other manifestations of the metabolic syndrome, to methods for their therapeutic use and to pharmaceutical compositions containing them.
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Page/Page column 183-184

(2008/06/13)

AMINOALCOHOL DERIVATIVES
The present invention relates to a compound formula [I]: wherein Y is bond,--O--(CH2)n--(in which n is 1, 2, 3 or 4), etc., Z is cyano, tetrazolyl, etc., R1 is hydrogen, lower alkyl, etc., R2 is hydrogen or an amino protective group, R3 is hydrogen or lower alkyl, R4 is hydrogen or lower alkyl, R5 and R8 are each independently hydrogen, halogen, hydroxy, lower alkyl, etc., R6 is hydrogen, lower alkyl, etc., R9 is hydrogen or lower alkyl, and i is 1 or 2, or a salt thereof. The compound [I] of the present invention and pharmaceutically acceptable salts thereof are useful for the prophylactic and/or the therapeutic treatment of pollakiurea or urinary incontinence.
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(2008/06/13)

DERIVATIVES OF SUCCINIC AND GLUTARIC ACIDS AND ANALOGS THEREOF USEFUL AS INHIBITORS OF PHEX
The present invention relates to derivatives of succinic and glutaric acids and analogues thereof, having the following general formula (I), useful as inhibitors of PHEX. These derivatives are useful for promoting generation of bone mass and treating or preventing diseases or conditions associated with a phosphate metabolism defect. Methods for preparation and intermediates are also disclosed.
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Page 49-51

(2010/02/07)

Aryl aniline beta2 adrenergic receptor agonists
The invention provides novel β2 adrenergic receptor agonist compounds of formula (I): wherein R1-R13 and w have any of the values described in the specification. The invention also provides combinations of such compounds and other therapeutic agents, pharmaceutical compositions comprising such compounds and combinations, methods of using such compounds to treat diseases associated with β2 adrenergic receptor activity, and processes and intermediates useful for preparing such compounds.
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Page 37

(2008/06/13)

SULFONYLQUINOXALONE ACETAMIDE DERIVATIVES AND RELATED COMPOUNDS AS BRADYKININ ANTAGONISTS
Disclosed are sulfonylquinoxalone acetamide derivatives useful as bradykinin antagonists to relieve symptons, associated with bradykinin including pain, inflammation, bronchoconstriction, cerebral edema, etc.
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Page/Page column 161

(2010/02/07)

A generic approach for the catalytic reduction of nitriles
The scope of nickel boride mediated reduction of nitriles has been extended further to allow the preparation of Boc protected amines via a mild catalytic process. It is noteworthy that the toxicity of this procedure is greatly reduced due to its catalytic
Caddick, Stephen,Judd, Duncan B.,Lewis, Alexandra K. De K.,Reich, Melanie T.,Williams, Meredith R. V.
p. 5417 - 5423
(2007/10/03)

Sulfonamide derivatives
The present invention provides certain sulfonamide derivatives useful for potentiating glutamate receptor function in a mammal and therefore, useful for treating a wide variety of conditions, such as psychiatric and neurological disorders.
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(2008/06/13)

Cyclic amine derivatives-CCR-3 receptor antagonists
This invention relates to certain cyclic amine derivatives of Formula (I) that are CCR-3 receptor antagonist, pharmaceutical compositions containing them, methods for their use and methods for preparing these compounds.
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Page column 65

(2010/01/31)

Sulphonamide derivatives
Glutamate receptor function in a mammal may be potentiated using an effective amount of a compound of formulaR1—L—NHSO2R2??Iin whichR1 represents an unsubstituted or substituted aromatic or heteroaromatic group;R2 represents (1-6C)alkyl, (3-6C)cycloalkyl, (1-6C)fluoroalkyl, (1-6C)chloroalkyl, (2-6C)alkenyl, (1-4C)alkoxy(1-4C)alkyl, phenyl which is unsubstituted or substituted by halogen, (1-4C)alkyl or (1-4C)alkoxy, or a group, of formula R3R4N in which R3 and R4 each independently represents (1-4C)alkyl or, together with the nitrogen atom to which they are attached form an azetidinyl, pyrrolidinyl, piperidinyl, morpholino, piperazinyl, hexahydroazepinyl or octahydroazocinyl group; andL represents a (2-4C)alkylene chain which is unsubstituted or substituted by one or two substituents selected independently from (1-6C)alkyl, aryl(1-6C)alkyl, (2-6C)alkenyl, aryl(2-6C)alkenyl and aryl, or by two substituents which, together with the carbon atom or carbon atoms to which they are attached form a (3-8C)carbocyclic ring;and pharmaceutically acceptable salts thereof.Also disclosed are compounds of formula I, processes for preparing them and pharmaceutical compositions containing them.
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(2008/06/13)

Cyclic amine derivatives- CCR-3 receptor antagonists
This invention relates to certain cyclic amine derivatives of Formula (I) that are CCR-3 receptor antagonists, pharmaceutical compositions containing them, methods for their use and methods for preparing these compounds.
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(2008/06/13)

Urokinase inhibitors
Compounds having the formula are inhibitors of urokinase and are useful in the treatment of diseases in which urokinase plays a role. Also disclosed are urokinase-inhibiting compositions and a method of inhibiting urokinase in a mammal.
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(2008/06/13)

Ukokinase inhibitors
Compounds having the formula are inhibitors of urokinase and are useful in the treatment of diseases in which urokinase plays a role. Also disclosed are urokinase-inhibiting compositions and a method of inhibiting urokinase in a mammal.
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(2008/06/13)

Biarylpropylsulfonamides as novel, potent potentiators of 2-amino-3-(5-methyl-3-hydroxyisoxazol-4-yl)-propanoic acid (AMPA) receptors [1]
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Ornstein,Zimmerman,Arnold,Bleisch,Cantrell,Simon,Zarrinmayeh,Baker,Gates,Tizzano,Bleakman,Mandelzys,Jarvie,Ho,Deverill,Kamboj
p. 4354 - 4358
(2007/10/03)

Convenient synthesis of protected primary amines form nitriles
Investigations into the use of nickel chloride and sodium borohydride for the reduction of nitriles showed the secondary amine dimers to be the major products under normal conditions. The addition of a suitable trapping agent, such as di-tert-butyl dicarbonate, allowed the isolation of the protected primary amines. (C) 2000 Elsevier Science Ltd.
Caddick, Stephen,De K. Haynes, Alexandra K.,Judd, Duncan B.,Williams, Meredith R.V.
p. 3513 - 3516
(2007/10/03)

A New Method for the Synthesis of Amides from Amines: Ruthenium Tetroxide Oxidation of N-Protected Alkylamines
A simple synthetic method for the preparation of amides from the corresponding primary alkylamines was elaborated using ruthenium tetroxide (RuO4) oxidation as a key step.
Tanaka, Ken-Ichi,Yoshifuji, Shigeyuki,Nitta, Yoshihiro
p. 3125 - 3129
(2007/10/02)