- Novel O-acylated amidoximes and substituted 1,2,4-oxadiazoles synthesised from (+)-ketopinic acid possessing potent virus-inhibiting activity against phylogenetically distinct influenza A viruses
-
This article describes the synthesis and antiviral activity evaluation of new substituted 1,2,4-oxadiazoles containing a bicyclic substituent at position 5 of the heterocycle and O-acylated amidoximes as precursors for their synthesis. New compounds were
- Borisevich, Sophia S.,Chernyshov, Vladimir V.,Esaulkova, Iana L.,Popadyuk, Irina I.,Salakhutdinov, Nariman F.,Sinegubova, Ekaterina,Yarovaya, Olga I.,Zarubaev, Vladimir V.
-
-
- Development of a Raltegravir-based Photoaffinity-Labeled Probe for Human Immunodeficiency Virus-1 Integrase Capture
-
Photoaffinity labeling (PAL) is one of the upcoming and powerful tools in the field of molecular recognition. It includes the determination of dynamic parameters, such as the identification and localization of the target protein and the site of drug binding. In this study, a photoaffinity-labeled probe for full-length human immunodeficiency virus-1 integrase (HIV-1 IN) capture was designed and synthesized, following the structure of the FDA-approved drug Raltegravir. This photoprobe was found to retain the HIV IN inhibitory potential in comparison with its parent molecule and demonstrates the ability to label the HIV-1 IN protein. Putative photoprobe/inhibitor binding sites near the catalytic site were then identified after protein digestion coupled to mass and molecular modeling analyses.
- Pala, Nicolino,Esposito, Francesca,Tramontano, Enzo,Singh, Pankaj Kumar,Sanna, Vanna,Carcelli, Mauro,Haigh, Lisa D.,Satta, Sandro,Sechi, Mario
-
supporting information
p. 1986 - 1992
(2020/11/09)
-
- BENZODIAZEPINE DERIVATIVES, COMPOSITIONS, AND METHODS FOR TREATING COGNITIVE IMPAIRMENT
-
This invention relates to benzodiazepine derivatives, compositions comprising therapeutically effective amounts of those derivatives and methods of using those derivatives or compositions in treating cognitive impairment associated with CNS disorders. It also relates to the use of an α5-containing GABAA receptor agonist (e.g., an α5-containing GABAA receptor positive allosteric modulator) in treating cognitive impairment associated with CNS disorders in a subject in need or at risk thereof, including age-related cognitive impairment, Mild Cognitive Impairment (MCI), amnestic MCI, Age-Associated Memory Impairment, Age Related Cognitive Decline, dementia, Alzheimer's Disease(AD), prodromal AD, PTSD, schizophrenia, bipolar disorder, ALS, cancer-therapy-related cognitive impairment, mental retardation, Parkinson's disease, autism spectrum disorders, fragile X disorder, Rett syndrome, compulsive behavior, and substance addiction. It also relates to the use of an α5-containing GABAA receptor agonist (e.g., an α5-containing GABAA receptor positive allosteric modulator) in treating brain cancers (including brain tumors, e.g., medulloblastomas), and cognitive impairment associated therewith.
- -
-
Paragraph 0524
(2020/01/11)
-
- Discovery of BR102375, a new class of non-TZD PPARγ full agonist for the treatment of type 2 diabetes
-
As a potential treatment of type 2 diabetes, a novel PPARγ non-TZD full agonist, compound 18 (BR102375) was identified from the original lead BR101549 by the SAR efforts of the labile metabolite control through bioisosteres approach. In vitro assessments
- Choung, Wonken,Yang, Deokmo,Kim,Choi, Hyukjoon,Lee, Bo Ram,Park, Min,Jang, Su Min,Lim, Jae Soo,Kim, Woo Sik,Kim, Kyung-Hee,Chin, Jungwook,Jung, Kyungjin,Lee, Geumwoo,Hong,Jang, Tae-ho,Joo, Jeongmin,Hwang, Hayoung,Myung, Jayhyuk,Kim, Seong Heon
-
p. 2275 - 2282
(2019/06/27)
-
- BENZODIAZEPINE DERIVATIVES, COMPOSITIONS, AND METHODS FOR TREATING COGNITIVE IMPAIRMENT
-
This invention relates to benzodiazepine derivatives, compositions comprising therapeutically effective amounts of those benzodiazepine derivatives and methods of using those derivatives or compositions in treating cognitive impairment associated with central nervous system (CNS) disorders. In particular, it relates to the use of a α5-containing GABAA receptor agonist (e.g., a α5-containing GABAA receptor positive allosteric modulator) as described herein in treating cognitive impairment associated with central nervous system (CNS) disorders in a subject in need or at risk thereof, including, without limitation, subjects having or at risk for age-related cognitive impairment, Mild Cognitive Impairment (MCI), amnestic MCI (aMCI), Age-Associated Memory Impairment (AAMI), Age Related Cognitive Decline (ARCD), dementia, Alzheimer's Disease(AD), prodromal AD, post traumatic stress disorder (PTSD), schizophrenia, bipolar disorder, amyotrophic lateral sclerosis (ALS), cancer-therapy-related cognitive impairment, mental retardation, Parkinson's disease (PD), autism spectrum disorders, fragile X disorder, Rett syndrome, compulsive behavior, and substance addiction. It also relates to the use of a α5-containing GABAA receptor agonist (e.g., a α5-containing GABAA receptor positive allosteric modulator) as described herein in treating brain cancers (including brain tumors, e.g., medulloblastomas), and cognitive impairment associated therewith.
- -
-
Paragraph 1316
(2018/07/05)
-
- Substituted aminopyrimidine compounds and their method and use thereof
-
The invention relates to a new aminopyrimidine compound and an application thereof as a drug for treating disorder or diseases related to PI3-kinase abnormity in a free form or a pharmaceutically acceptable salt and preparation form. The invention also relates to a pharmaceutical composition which contains the new aminopyrimidine compound and an application of the pharmaceutical composition in treating mammal disorder or diseases and especially treating human disorder or diseases related to the PI3-kinase abnormity, such as treatment of immunity and inflammatory diseases of PI3-kinase regulation which plays a leading role in a leucocyte function and treatment of proliferative diseases which are related to PI3-kinase activity and include but not limited to leukaemia and solid tumor.
- -
-
Paragraph 1326; 1327; 1328
(2017/12/28)
-
- COMPOUNDS AS HEPATITIS C INHIBITORS AND USES THEREOF IN MEDICINE
-
Provided herein are compounds as hepatitis C inhibitors and uses thereof in medicine. Specifically, provided herein is a compound of Formula (I) or a stereoisomer, a tautomer, an enantiomer, an N-oxide, a hydrate, a solvate, a metabolite, a pharmaceutically acceptable salt or a prodrug thereof, which can be used for treating HCV infection or hepatitis C diseases. Also provided herein are a pharmaceutically acceptable composition containing such compound and a method of treating HCV infection or hepatitis C diseases comprising administering the compound or pharmaceutical composition thereof disclosed herein.
- -
-
Paragraph 00214
(2016/09/22)
-
- BENZODIAZEPINE DERIVATIVES, COMPOSITIONS, AND METHODS FOR TREATING COGNITIVE IMPAIRMENT
-
This invention relates to benzodiazepine derivatives, compositions comprising therapeutically effective amounts of those benzodiazepine derivatives and methods of using those derivatives or compositions in treating cognitive impairment associated with central nervous system (CNS) disorders. In particular, it relates to the use of a α5- containing GABAA receptor agonist (e.g., a α5-containing GABAA receptor positive allosteric modulator) as described herein in treating cognitive impairment associated with central nervous system (CNS) disorders in a subject in need or at risk thereof, including, without limitation, subjects having or at risk for age-related cognitive impairment, Mild Cognitive Impairment (MCI), amnestic MCI (aMCI), Age- Associated Memory Impairment (AAMI), Age Related Cognitive Decline (ARCD), dementia, Alzheimer' s Disease(AD), prodromal AD, post traumatic stress disorder (PTSD), schizophrenia, bipolar disorder, amyotrophic lateral sclerosis (ALS), cancer-therapy-related cognitive impairment, mental retardation, Parkinson' s disease (PD), autism spectrum disorders, fragile X disorder, Rett syndrome, compulsive behavior, and substance addiction.
- -
-
Paragraph 0469
(2017/01/02)
-
- COMPOUND HAVING GPR119 AGONISTIC ACTIVITY, METHOD FOR PREPARING THE SAME, AND PHARMACEUTICAL COMPOSITION INCLUDING THE SAME AS EFFECTIVE COMPONENT
-
The present invention relates to a novel compound having a GPR1 19 agonistic activity, a method for preparing the same, and a pharmaceutical composition including the same as an effective component. The present invention has an effective hypoglycemic acti
- -
-
Page/Page column 21
(2016/05/19)
-
- BENZODIAZEPINE DERIVATIVES, COMPOSITIONS, AND METHODS FOR TREATING COGNITIVE IMPAIRMENT
-
This invention relates to benzodiazepine derivatives, compositions comprising therapeutically effective amounts of those benzodiazepine derivatives and methods of using those derivatives or compositions in treating cognitive impairment associated with central nervous system (CNS) disorders. In particular, it relates to the use of a a5- containing GABAA receptor agonist (e.g., a α5 -containing GABAA receptor positive allosteric modulator) as described herein in treating cognitive impairment associated with central nervous system (CNS) disorders in a subject in need or at risk thereof, including, without limitation, subjects having or at risk for age-related cognitive impairment, Mild Cognitive Impairment (MCI), amnestic MCI (aMCI), Age-Associated Memory Impairment (AAMI), Age Related Cognitive Decline (ARCD), dementia, Alzheimer's Disease(AD), prodromal AD, post traumatic stress disorder (PTSD), schizophrenia, bipolar disorder, amyotrophic lateral sclerosis (ALS), cancer-therapy-related cognitive impairment, mental retardation, Parkinson's disease (PD), autism spectrum disorders, fragile X disorder, Rett syndrome, compulsive behavior, and substance addiction.
- -
-
Paragraph 0349
(2015/07/07)
-
- Practical synthesis of N -substituted cyanamides via tiemann rearrangement of amidoximes
-
A facile and general synthesis of various N-substituted cyanamides was accomplished by the Tiemann rearrangement of amidoximes with benzenesulfonyl chlorides (TsCl or o-NsCl) and DIPEA.
- Lin, Chia-Chi,Hsieh, Tsung-Han,Liao, Pen-Yuan,Liao, Zhen-Yuan,Chang, Chih-Wei,Shih, Yu-Chiao,Yeh, Wen-Hsiung,Chien, Tun-Cheng
-
supporting information
p. 892 - 895
(2014/03/21)
-
- Synthesis and methemoglobinemia-inducing properties of benzocaine isosteres designed as humane rodenticides
-
A number of isosteres (oxadiazoles, thiadiazoles, tetrazoles and diazines) of benzocaine were prepared and evaluated for their capacity to induce methemoglobinemia - with a view to their possible application as humane pest control agents. It was found that an optimal lipophilicity for the formation of methemoglobin (metHb) in vitro existed within each series, with 1,2,4-oxadiazole 3 (metHb% = 61.0 ± 3.6) and 1,3,4-oxadiazole 10 (metHb% = 52.4 ± 0.9) demonstrating the greatest activity. Of the 5 candidates (compounds 3, 10, 11, 13 and 23) evaluated in vivo, failure to induce a lethal end-point at doses of 120 mg/kg was observed in all cases. Inadequate metabolic stability, particularly towards hepatic enzymes such as the CYPs, was postulated as one reason for their failure.
- Conole, Daniel,Beck, Thorsten M.,Jay-Smith, Morgan,Tingle, Malcolm D.,Eason, Charles T.,Brimble, Margaret A.,Rennison, David
-
supporting information
p. 2220 - 2235
(2014/04/17)
-
- New compounds, pharmaceutical compositions and uses thereof
-
The present invention relates to compounds of general formula I, wherein the groups R1, LP, LQ, Ar, m and n are as defined in the application, which have valuable pharmacological properties, and in particular bind to the GPR119 receptor and modulate its activity.
- -
-
Paragraph 0373; 0374
(2013/03/28)
-
- NEW COMPOUNDS, PHARMACEUTICAL COMPOSITIONS AND USES THEREOF
-
The present invention relates to compounds of general formula I, wherein R1, LP, HetAr, Ar, and n are as defined in the application, which have valuable pharmacological properties, and in particular bind to the GPR119 receptor and modulate its activity.
- -
-
Paragraph 0404; 0405
(2013/06/26)
-
- N- CYCLOPROPYL - N- PIPERIDINYLBENZAMIDES AS GPR119 MODULATORS
-
The present invention relates to compounds of general formula I, wherein the groups R1, LP, LQ, Ar, mand n are as defined in the application, which have valuable pharmacological properties, and in particular bind to the GPR119 receptor and modulate its activity.
- -
-
Page/Page column 89
(2012/10/07)
-
- Synthesis of benzoxazines, quinazolines and 4H-benzo[e][1,3]thiazine by ANRORC rearrangements of 1,2,4-oxadiazoles
-
1,2,4-Oxadiazoles undergo ANRORC (addition of nucleophile, ring-opening and ring-closure) rearrangements upon reaction with excess of n-butyllithium to give benzoxazines, benzothiazines, and quinazolines in good yields under mild conditions. Georg Thieme Verlag Stuttgart · New York.
- Draghici, Bogdan,El-Gendy, Bahaa El-Dien M.,Katritzky, Alan R.
-
supporting information; experimental part
p. 547 - 550
(2012/04/04)
-
- SUBSTITUTED PIPERIDINES AS GPR119 MODULATORS FOR THE TREATMENT OF METABOLIC DISORDERS
-
The present invention relates to compounds of general formula (I), wherein R1, Lp, HetAr, Ar, and n are as defined in the application, which have valuable pharmacological properties, and in particular bind to the GPR119 receptor and modulate its activity.
- -
-
Page/Page column 106-107
(2013/02/27)
-
- Investigating the role of metal chelation in HIV-1 integrase strand transfer inhibitors
-
HIV-1 integrase (IN) has been validated as an attractive target for the treatment of HIV/AIDS. Several studies have confirmed that the metal binding function is a crucial feature in many of the reported IN inhibitors. To provide new insights on the metal
- Bacchi, Alessia,Carcelli, Mauro,Compari, Carlotta,Fisicaro, Emilia,Pala, Nicolino,Rispoli, Gabriele,Rogolino, Dominga,Sanchez, Tino W.,Sechi, Mario,Sinisi, Valentina,Neamati, Nouri
-
experimental part
p. 8407 - 8420
(2012/02/14)
-
- PROCESS FOR THE PREPARATION OF OXADIAZOLES
-
Process for the preparation of oxadiazoles, useful as intermediates in the preparation of biologically active molecules.
- -
-
Page/Page column 11
(2011/12/14)
-
- BICYCLIC COMPOUNDS AND USE AS ANTIDIABETICS
-
The present invention relates to novel compounds that are useful in the treatment of metabolic disorders, particularly type II diabetes mellitus and related disorders, and also to the methods for the making and use of such compounds.
- -
-
Page/Page column 23
(2010/03/02)
-
- COMPOUNDS AND COMPOSITIONS AS MODULATORS OF GPR119 ACTIVITY
-
The invention provides compounds of Formula (I): pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with the activity of GPR119.
- -
-
Page/Page column 38-39
(2009/10/18)
-
- GPR119 Receptor Agonists
-
Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of metabolic diseases and disorders such as, for example, type II diabetes mellitus.
- -
-
Page/Page column 21
(2009/12/05)
-
- Discovery of the first potent and orally efficacious agonist of the orphan G-protein coupled receptor 119
-
GPR119 is a rhodopsin-like GPCR expressed in pancreatic β-cells and incretin releasing cells in the GI tract. As with incretins, GPR119 increases cAMP levels in these cell types, thus making it a highly attractive potential target for the treatment of dia
- Semple, Graeme,Fioravanti, Beatriz,Pereira, Guillherme,Calderon, Imelda,Uy, Jane,Choi, Karoline,Xiong, Yifeng,Ren, Albert,Morgan, Michael,Dave, Vibha,Thomsen, William,Unett, David J.,Xing, Charles,Bossie, Stuart,Carroll, Chris,Chu, Zhi-Liang,Grottick, Andrew J.,Hauser, Erin K.,Leonard, James,Jones, Robert M.
-
scheme or table
p. 5172 - 5175
(2009/07/01)
-
- PIPERAZINE COMPOUNDS FOR THE INHIBITION OF HAEMATOPOIETIC PROSTAGLANDIN D SYNTHASE
-
The present invention relates to compounds of general formula (I): wherein A, Y, X, n and B are as defined herein; and their use in the treatment and prevention of metabolic disorders, inflammatory conditions, allergic conditions, fever, pain including allodynia and nociception, eating disorders, cachexia, brain injuries, cancer of the genitals, sleep apnoea, cardiovascular disease, flush effect associated with nicotinic acid and related compounds or for the promotion of wound healing. Certain compounds of general formula (I) are new and the invention also relates to these compounds and to their use in medicine.
- -
-
Page/Page column 109
(2008/12/04)
-
- COMPOUNDS AND COMPOSITIONS AS MODULATORS OF GPR119 ACTIVITY
-
The invention provides compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with the activity of GPR119.
- -
-
Page/Page column 98
(2008/12/08)
-
- GPR119 AGONISTS FOR THE TREATMENT OF DIABETES AND RELATED DISORDERS
-
The present invention relates to novel compounds that are useful in the treatment of metabolic disorders, particularly Type II diabetes mellitus and related disorders, and also to the methods for the making and use of such compounds.
- -
-
Page/Page column 116
(2010/11/29)
-
- THIAZOLYL-DIHYDRO-CYCLOPENTAPYRAZOLE
-
Disclosed are compounds of general formula (I), wherein the groups R1, R2, Ra and Rb have the meanings given in the claims and specification, the tautomers, racemates, enantiomers, diastereomers and the mixtures
- -
-
Page/Page column 23
(2008/06/13)
-
- THIAZOLYL-DIHYDRO-CHINAZOLINE
-
Disclosed are compounds of general formula (I), wherein the groups A, R1, R2, Ra and Rb have the meanings given in the claims and specification, the tautomers, racemates, enantiomers, diastereomers and the mixtures thereof, and optionally the pharmacologically acceptable acid addition salts, solvates and hydrates thereof, and processes for preparing these thiazolyl-dihydro-quinazolines and the use thereof as pharmaceutical compositions.
- -
-
Page/Page column 26
(2008/06/13)
-
- THIAZOLYL-DIHYDRO-INDAZOLE
-
Disclosed are compounds of general formula (I), wherein the groups R1, R2, Ra and Rb have the meanings given in the claims and specification, the tautomers, racemates, enantiomers, diastereomers and the mixtures thereof, and optionally the pharmacologically acceptable acid addition salts, solvates and hydrates thereof, and processes for preparing these thiazolyl-dihydro-indazoles and the use thereof as pharmaceutical compositions.
- -
-
Page/Page column 24-25
(2008/06/13)
-
- Dihydroxypyrimidine-4-carboxamides as novel potent and selective HIV integrase inhibitors
-
Human immunodeficiency virus type-1 (HIV-1) integrase, one of the three constitutive viral enzymes required for replication, is a rational target for chemotherapeutic intervention in the treatment of AIDS that has also recently been confirmed in the clinical setting. We report here on the design and synthesis of N-benzyl-5,6-dihydroxypyrimidine-4-carboxamides as a class of agents which exhibits potent inhibition of the HIV-integrase-catalyzed strand transfer process. In the current study, structural modifications on these molecules were made in order to examine effects on HIV-integrase inhibitory potencies. One of the most interesting compounds for this series is 2-[1-(dimethylamino)-1-methylethyl]-N-(4-fluorobenzyl)-5,6-dihydroxypyrimidine- 4-carboxamide 38, with a CIC95 of 78 nM in the cell-based assay in the presence of serum proteins. The compound has favorable pharmacokinetic properties in preclinical species (rats, dogs, and monkeys) and shows no liabilities in several counterscreening assays, highlighting its potential as a clinically useful antiviral agent.
- Pace, Paola,Di Francesco, M. Emilia,Gardelli, Cristina,Harper, Steven,Muraglia, Ester,Nizi, Emanuela,Orvieto, Federica,Petrocchi, Alessia,Poma, Marco,Rowley, Michael,Scarpelli, Rita,Laufer, Ralph,Paz, Odalys Gonzalez,Monteagudo, Edith,Bonelli, Fabio,Hazuda, Daria,Stillmock, Kara A.,Summa, Vincenzo
-
p. 2225 - 2239
(2007/10/03)
-
- TRIAZOLE DERIVATIVES AS VASOPRESSIN ANTAGONISTS
-
Compounds of formula (I), or pharmaceutically acceptable derivatives thereof, wherein: R1 represents a group selected from H, CF3, and C1-6 alkyl (optionally substituted by C1-6 alkyloxy or triazolyl); R2/
- -
-
Page/Page column 34
(2010/11/24)
-
- SUBSTITUTED ARYL AND HETEROARYL DERIVATIVES AS MODULATORS OF METABOLISM AND THE PROPHYLAXIS AND TREATMENT OF DISORDERS RELATED THERETO
-
The present invention relates to certain substituted aryl and heteroaryl derivative of Formula (I) that are modulators of metabolism. Accordingly, compounds of the present invention are useful in the treatment of metabolic-related disorders and complicati
- -
-
Page/Page column 165-166
(2008/06/13)
-
- TRISUBSTITUTED ARYL AND HETEROARYL DERIVATIVES AS MODULATORS OF METABOLISM AND THE PROPHYLAXIS AND TREATMENT OF DISORDERS RELATED THERETO
-
The present invention relates to certain trisubstituted aryl and heteroaryl derivatives of Formula (I) that are modulators of metabolism. Accordingly, compounds of the present invention are useful in the prophylaxis or treatment of metabolic disorders and complications thereof, such as, diabetes and obesity.
- -
-
Page/Page column 191
(2008/06/13)
-
- FUSED-ARYL AND HETEROARYL DERIVATIVES AS MODULATORS OF METABOLISM AND THE PROPHYLAXIS AND TREATMENT OF DISORDERS RELATED THERETO
-
The present invention relates to certain fused aryl and heteroaryl derivatives of Formula (I) that are modulators of metabolism. Accordingly, compounds of the present invention are useful in the prophylaxis or treatment of metabolic disorders and complica
- -
-
-
- NOVEL ALKYNYL DERIVATIVES AS MODULATORS OF METABOTROPIC GLUTAMATE RECEPTORS
-
The present invention relates to novel compounds of formula (I) wherein W, n, X and W’ are defined in the description; invention compounds are modulators of metabotropic glutamate receptors - subtype 5 (“mGluR5”) which are useful for the treatment of central nervous system disorders as well as other disorders modulated by mGluR5 receptors.
- -
-
Page/Page column 98
(2008/06/13)
-
- Synthesis of various 3-substituted 1,2,4-oxadiazole-containing chiral β3- and α-amino acids from Fmoc-protected aspartic acid
-
Various 3-substituted chiral 1,2,4-oxadiazole-containing Fmoc-β 3- and α-amino acids were synthesized from FmoC-(L or D)-Asp(OtBu)-OH and Fmoc-L-Asp-OtBu, respectively, in three steps (i.e., condensation of an aspartyl derivative with different
- Hamze?, Abdallah,Hernandez, Jean-Franc?ois,Fulcrand, Pierre,Martinez, Jean
-
p. 7316 - 7321
(2007/10/03)
-
- Modification of the Tiemann rearrangement: One-pot synthesis of N,N-disubstituted cyanamides from amidoximes
-
A three-stage one-pot synthetic procedure for transformation of amidoximes to N,N-disubstituted cyanamides in 70-92% yield is described.
- Bakunov, Stanislav A.,Rukavishnikov, Alexey V.,Tkachev, Alexey V.
-
p. 1148 - 1159
(2007/10/03)
-
- Herbicidal quinolinyloxadiazoles
-
The present invention relates to novel quinolinyloxadiazole derivatives of the following formula (I) having processes for their preparation and their use as herbicides and plant growth regulants, especially their use in the selective kill and control of barnyardgrass in the presence of rice. STR1 wherein, A and B are selected from the group consisting of hydrogen, halogen and C1 -C3 lower alkyl; R is a C3 -C4 alkyl or cycloalkyl, phenyl, pyridyl, benzyl, phenoxyalkyl or phenylthioalkyl, and aromatic groups in these radicals are optionally substituted with 1?3 substituents selected from the group consisting of halogen, C1 -C4 alkyl, C1 -C4 alkoxy, C1 -C4 alkylthio C2 -C6 alkoxyalkyl and an anolog thereof.
- -
-
-
- Imidazothienopyrimidines useful in psychopharmaceutical preparations
-
New heterocyclic compounds having the general formula STR1 wherein STR2 wherein R'' is C 1-6 -alkyl, C 3-7 -cycloalkyl or C 1-6 -alkoxymethyl;R 4 is C 1-6 -alkyl;--S-- is STR3 and wherein R 5 and R 6 independently are hydrogen, C 1-6 -alkyl, or aryl.The c
- -
-
-
- New Acetonylsubstituted Azoles, I. 5-Acetonyl-1,2,4-oxadiazoles
-
Aliphatic amidoximes R-C(NH2)=NOH react with diketene to yield 5-acetonyl-3-alkyl-1,2,4-oxadiazoles, which are susceptible to a wide variety of reactions at the keto-group as well as at the methylene-group.Their transformations into 1-methyl-2-oxadiazolyl
- Kuebel, Boerries
-
p. 781 - 792
(2007/10/02)
-