摘要:
The present invention relates to novel compounds of the following formula, where the dotted line designates an optional bond: ##STR1## wherein "het" designates a five membered heterocyclic ring which may include 1 or 2 double bonds and 1-4 heteroatoms selected from nitrogen, oxygen or sulphur, provided that "het" may not designate a 1,2,4- or 1,3,4-oxadiazole; R.sup.1 -R.sup.5 are as defined in the specification;as well as individual stereo isomers and pharmaceutically acceptable acid addition salts thereof.The invention moreover relates to methods for the preparation of the compounds of formula I, to novel intermediates, to pharmaceutical compositions containing same and to methods for the treatment of disorders, caused by malfunction of the acetylcholine (AcCh) or muscarinic system, by administering a non-toxic effective amount of a compound of formula I.
摘要:
The present invention relates to novel compounds of the following formula, where the dotted line designates an optional bond: ##STR1## wherein "het" designates a five membered heterocyclic ring which may include 1 or 2 double bonds and 1-4 heteroatoms selected from nitrogen, oxygen or sulphur, provided that "het" may not designate a 1,2,4- or 1,3,4-oxadiazole;R.sup.1 is selected from hydrogen, lower alkyl, optionally substituted with phenyl which may be substituted with halogen, lower alkyl, or lower alkoxy, or a group R.sup.6 --CO--NH--CH.sub.2 -- or R.sup.6 --O--CO--, wherein R.sup.6 is lower alkyl, branched or unbranched, or phenyl optionally substituted with halogen, trifluoromethyl, lower alkyl, hydroxy, lower alkoxy, or lower acyloxy;R.sup.2 and R.sup.3 are the same or different, each representing hydrogen, lower alkyl, cycloalkyl (3-6 C-atoms), lower alkenyl, lower alkadienyl, lower alkynyl, optionally substituted with hydroxy, halogen or phenyl, in which the phenyl group may be substituted with halogen, trifluoromethyl, lower alkyl, hydroxy or lower alkoxy; R.sup.2 and R.sup.3 may further, respectively, be selected from trifluoromethyl or phenyl optionally substituted with halogen, trifluoromethyl, lower alkyl, hydroxy, lower alkoxy or lower acyloxy, or R.sup.2 and R.sup.3 may, respectively, be a group OR.sup.7 or SR.sup.7 wherein R.sup.7 is defined as R.sup.2 or R.sup.3, andif "het" includes 2 or more carbon atoms, R.sup.4 and R.sup.5 are the same or different, and each is defined as R.sup.2 or R.sup.3, and if "het" includes only one carbon atom, there is only one substituent, R.sup.4, on the heterocyclic ring, and R.sup.4 is defined as R.sup.2 or R.sup.3,as well as individual stereo isomers and pharmaceutically acceptable acid addition salts thereof.The invention moreover relates to methods for the preparation of the compounds of formula I, to novel intermediates, to pharmaceutical compositions containing same and to methods for the treatment of disorders, caused by malfunction of the acetylcholine (AcCh) or muscarinic system, by administering a non-toxic effective amount of a compound of formula I.
摘要:
##STR1## Fused benzo compounds of formula (I), wherein A is a 2 to 6 membered hydrocarbon spacer group, B is a polar divalent group selected from SO, SO 2 , and a group (a); U is C, N or CH; X is a divalent 3-4 membered chain optionally comprising one or more heteroatoms; R 1 is an aliphatic hydrocarbon group, arylalkyl or diphenylalkyl; R 2 and R 3 are hydrogen or alkyl or together form an ethylene or propylene bridge; R 4 , R 5 and R 6 are hydrogen or substituents; R 7 and R 8 are hydrogen or substituents including, a group --COOR 9 and a group --CONR 10 R 11 ; are 5-HT 1A receptor ligands useful in the treatment of CNS disorders. Pharmaceutical compositions comprising the compounds and their use for the manufacture of a pharmaceutical preparation are also disclosed.
摘要:
Fused benzo compounds of formula I are provided, wherein A is a 2 to 6 membered hydrocarbon spacer group, B is a polar divalent group selected from a group (a); U is C, N or CH; X is a divalent 3-4 membered chain optionally comprising one or more heteroatoms; R.sup.1 is an aliphatic hydrocarbon group, arylalkyl or diphenylalkyl; R.sup.2 and R.sup.3 are hydrogen or alkyl or together form an ethylene or propylene bridge; R.sup.4, R.sup.5 and R.sup.6 are hydrogen or substituents; R.sup.7 and R.sup.8 are hydrogen or substituents including --COOR.sup.9 and --CONR.sup.10 R.sup.11 ; are 5-HT.sub.1A receptor ligands useful in the treatment of CNS disorders. Pharmaceutical compositions comprising the compounds and their use for the manufacture of a pharmaceutical preparation are also provided.
摘要:
A type of composite material where the matrix material and additive are held together by covalently or non-covalently bound ligands is described. A particularly useful composite material covered by the present invention is a carbon nanotube-reinforced composite material where the matrix consists of a polymer, covalently attached to a linker, where said linker is non-covalently attached to the carbon nanotube. Methods for the preparation of such composite materials are provided.
摘要:
Novel compounds carrying ligands capable of binding to counter receptors on relevant target cells are disclosed. The compounds possess a number of advantageous features, rendering them very suitable for a wide range of applications, including use as detection systems, detection of relevant target cells as well as a number of other methods. In particular, novel MHC complexes comprising one or more MHC molecules are disclosed. The affinity and specificity of the MHC-peptide complexes are surprisingly high. The possibility of presenting to the target cells a plurality of MHC-peptide complexes makes the MHC complexes according to the present invention an extremely powerful tool e.g. in the field of therapy and diagnosis. The invention generally relates to the field of therapy, including therapeutic methods and therapeutic compositions. Also comprised by the present invention is the sample-mounted use of MHC complexes and MHC multimers.
摘要:
Composite material, where the matrix material and the additive are held together by covalently or non-covalently bound ligands. The linker unit between matrix and additive has the structure Ligand1-LinkerL-Ligand 2, wherein Ligand1 and Ligand2 are a bond or a chemical entity that is capable of binding covalently or non-covalently to a structural entity, such as a polymer matrix or the additive (ex. CNT, graphene, carbon nanofiber, etc), and LinkerL is a chemical bond or entity that links Ligand1 and Ligand2.
摘要:
The invention relates to a variant of a parent fungal glucoamylase, which exhibits improved thermal stability and/or increased specific activity using saccharide substrates.
摘要:
Novel compounds carrying ligands capable of binding to counter receptors on relevant target cells are disclosed. The compounds possess a number of advantageous features, rendering them very suitable for a wide range of applications, including use as detection systems, detection of relevant target cells as well as a number of other methods. In particular, novel MHC complexes comprising one or more MHC molecules are disclosed. The affinity and specificity of the MHC-peptide complexes are surprisingly high. The possibility of presenting to the target cells a plurality of MHC-peptide complexes makes the MHC complexes according to the present invention an extremely powerful tool e.g. in the field of therapy and diagnosis. The invention generally relates to the field of therapy, including therapeutic methods and therapeutic compositions. Also comprised by the present invention is the sample-mounted use of MHC complexes and MHC multimers.
摘要:
A fungal wild-type lipolytic enzyme having a higher ratio of activity on polar lipids compared with triglycerides, wherein the enzyme preferably has a phospholipid:triglyceride activity ratio of at least 4. Preferably, the lipolytic enzyme according to the present invention has a glycolipid:triglyceride hydrolyzing activity ratio of at least 1.5. In one embodiment, the fungal lipolytic enzyme according to the present invention comprises an amino acid sequence as shown in SEQ ID NO: 1 or SEQ ID No. 2 or SEQ ID No. 4 or SEQ ID No. 6 or an amino acid sequence which has at least 90% identity thereto. The present invention further encompasses a nucleic acid encoding a fungal lipolytic enzyme, which nucleic acid is selected from the group consisting of: (a) a nucleic acid comprising a nucleotide shown in SEQ ID No. 3, SEQ ID No. 5 or SEQ ID No. 7; (b) a nucleic acid which is related to the nucleotide sequence of SEQ ID No. 3, SEQ ID No. 5 or SEQ ID No. 7 by the degeneration of the genetic code; and (c) nucleic acid comprising a nucleotide sequence which has at least 90% identity with the nucleotide sequence shown in SEQ ID No. 3, SEQ ID No. 5 or SEQ ID No. 7.
摘要翻译:与甘油三酯相比,极性脂质活性比例更高的真菌野生型脂肪分解酶,其中所述酶优选具有至少为4的磷脂:甘油三酯活性比。优选地,根据本发明的脂肪分解酶具有糖脂: 甘油三酯水解活性比至少为1.5。 在一个实施方案中,根据本发明的真菌脂肪分解酶包含如SEQ ID NO:1或SEQ ID No.2或SEQ ID No.4或SEQ ID No.6所示的氨基酸序列或氨基酸序列, 与其具有至少90%的同一性。 本发明还包括编码真菌脂肪分解酶的核酸,该核酸选自:(a)包含SEQ ID No.3,SEQ ID No.5或SEQ ID No.5所示核苷酸的核酸 第7号 (b)通过遗传密码的退化与SEQ ID No.3,SEQ ID No.5或SEQ ID No.7的核苷酸序列有关的核酸; 和(c)核酸,其包含与SEQ ID No.3,SEQ ID No.5或SEQ ID No.7所示的核苷酸序列具有至少90%同一性的核苷酸序列。