摘要:
The invention aims at providing novel compounds useful as primer in producing mucin-type glycopeptides which are useful in a wide field including materials for biochemical research, drugs, and food and the production of which was difficult in the prior art; and a process for the production of glycopeptides by using the primers. The aim is attained by providing novel glycopeptide derivatives (represented by the general formula (I)) which each bear an aldehyde or ketone group at the end and each contain an amino acid residue cleavable with a protease; and an easy and simple process for the production of glycopeptides by using the derivative as the primer.
摘要:
It is considered that MMP-13 inhibitors contribute to the treatment or prevention against the diseases caused by or related to activity of MMP-13, especially osteoarthritis (OA). Therefore, the development of MMP-13 inhibitors has been desired. A compound represented by the general formula (I):
wherein Z is 1,4-phenylene and the like; R 1 is hydroxy and the like; R 2 is hydrogen atom, optionally substituted lower alkyl, and the like; R 12 is hydrogen atom; or R 2 and R 12 taken together with the adjacent carbon atom may form a ring; R 3 is hydrogen atom, optionally substituted lower alkyl, and the like; R 4 is halogen, lower alkyl, and the like; m is 0, 1, or 2; X is a bond, -C≡C-, and the like; Y is optionally substituted phenyl, optionally substituted naphthyl, and the like, its optically active substance, their pharmaceutically acceptable salt, or a solvate thereof.
摘要翻译:认为MMP-13抑制剂有助于治疗或预防由MMP-13,特别是骨关节炎(OA)引起的或与MMP-13的活性有关的疾病。 因此,期望MMP-13抑制剂的发展。 由通式(I)表示的化合物:其中Z是1,4-亚苯基等; R 1是羟基等; R 2是氢原子,任选取代的低级烷基等; R 12是氢原子; 或R 2和R 12与相邻碳原子一起可以形成环; R 3是氢原子,任选取代的低级烷基等; R 4是卤素,低级烷基等; m为0,1或2; X是一个债券,-C¡C等等; Y是任选取代的苯基,任选取代的萘基等,其光学活性物质,其药学上可接受的盐或其溶剂化物。
摘要:
The present invention provides a new use of an agent that inhibits bile acid reabsorption. An agent that inhibits bile acid reabsorption is useful for the prevention of fatty liver.
摘要:
Disclosed herein are a novel crystal of a novel triterpene derivative, a method for producing the crystals, and a pharmaceutical preparation obtained by using the crystals. The novel crystal is a crystal of a compound (I) of the formula (I):
(wherein A is optionally substituted lower alkylene (substituent: mono- or di- lower alkyl, lower alkylidene, or lower alkylene having two or more carbons); Z + is either of the groups shown below:
(wherein R 1 and R 2 are each independently hydrogen, optionally substituted amino lower alkyl or optionally substituted cyclic amino; R 3 is hydrogen or amino; X is N or CR 4 (R 4 is hydrogen or optionally substituted lower alkyl)), a pharmaceutically acceptable salt or a solvate thereof.
摘要翻译:式1的化合物:其中A为任选取代的低级亚烷基(取代基:具有两个或更多个碳的单或二低级烷基,低级亚烷基或低级亚烷基); Z +为以下所示的基团之一:(其中R1 和R2各自独立地为氢,任选取代的氨基低级烷基或任选取代的环状氨基; R3为氢或氨基; X为N或CR4(R4为氢或任选取代的低级烷基)),其药学上可接受的盐或溶剂化物。
摘要:
[Problems to be Solved] To provide a novel compound having antiviral activity, especially inhibitory activity against HIV integrase, a pharmaceutical composition, especially anti-HIV drug, containing the same. [Means to Solve the Problem] A compound of the formula:
(wherein: R 1 is optionally substituted aralkyl; R 2 and R 3 are each independently hydrogen, optionally substituted alkyl, optionally substituted amino, optionally substituted alkenyl or optionally substituted alkoxy (provided that each substituent for "optionally substituted" is a noncyclic group); R 4 is hydrogen, optionally substituted carboxy, optionally substituted formylamino, optionally substituted carbamoyl, optionally substituted amino (provided that a substituent on amino in "optionally substituted formylamino", "optionally substituted carbamoyl" and "optionally substituted amino" may form an optionally-substituted N-atom containing heterocyclic ring together with an adjacent N atom), optionally substituted alkyl, optionally substituted alkenyl, optionally substituted aryl, or optionally substituted heteroaryl) or a salt thereof.
摘要翻译:[待解决的问题]提供具有抗病毒活性,特别是抗HIV整合酶抑制活性的新型化合物,含有该化合物的药物组合物,特别是抗HIV药物。 [解决问题的方法]下式化合物:其中:R 1为任选取代的芳烷基; R 2和R 3各自独立地为氢,任选取代的烷基,任选取代的氨基,任选取代的烯基或任选取代的烷氧基(提供 “任选取代的”的每个取代基是非环基团; R 4是氢,任选取代的羧基,任选取代的甲酰氨基,任选取代的氨基甲酰基,任选取代的氨基(条件是“任选取代的甲酰氨基”上的氨基上的取代基, 取代的氨基甲酰基“和”任选取代的氨基“可以与相邻的N原子一起形成任选取代的含有N原子的杂环),任选取代的烷基,任选取代的烯基,任选取代的芳基或任选取代的杂芳基)或其盐 。
摘要:
Cephem compounds having groups of general formula (II) at the 3-position of the cephem ring, or salts or hydrates thereof, wherein Het is a mono- or poly-cyclic hetero-ring having one or more atoms selected from among N, O and S which may be the same or different from each other; R1 is hydrogen, optionally substituted lower alkyl or lower alkenyl; A is optionally substituted lower alkylene, lower alkenylene or a single bond while B is optionally substituted imino or a single bond, or alternatively A and B may be united to form a single bond; and D is a single bond or group (a).
摘要:
An immunoassay method specific for mammalian gamma -BNP derivatives which comprises using a first antibody reacting with mammalian alpha -BNP and a second antibody reacting with preproBNP or gamma -BNP derivatives but not with alpha -BNP and wherein at least one of these antibodies has been detectably labeled or supported on a solid phase.
摘要:
A cephem compound, wherein the cephem ring has a substituent at the 3-position, which substituent is shown by the formula II, wherein Het is a mono- or polycyclic heterocyclic group comprising one or more hetero atoms selected from the group consisting of N, O and S which may be the same or different from each other; R 1 is hydrogen, an optionally substituted lower alkyl or an optionally substituted lower alkenyl; A is an optionally substituted lower alkylene, an optionally substituted lower alkenylene or a single bond; B is an optionally substituted imino or a single bond; or A and B taken together may form a single bond; and D is a single bond or a group of the formula (a):
摘要翻译:头孢烯化合物,其中头孢烯环在3位上具有取代基,该取代基由式II表示,其中Het是包含一个或多个选自N, O和S可以相同或不同; R 1是氢,任选取代的低级烷基或任选取代的低级烯基; A是任选取代的低级亚烷基,任选取代的低级亚烯基或单键; B是任选取代的亚氨基或单键; 或A和B组合在一起可形成单一债券; 和D是单键或式(a)的基团:
摘要:
A method for inhibiting the decomposition of mammalian natriuretic peptides, in particular, BNP by using containers wherein the face coming into contact with specimens is made of a material capable of inhibiting the activation of a substance decomposing peptides. This method makes it possible to stably and conveniently collect specimens for assaying natriuretic peptides. Also provided is a method for assaying natriuretic peptides by using these containers.