WATER SOLUBLE LUMINESCENCE OXYGEN SENSOR AND METHOD
    3.
    发明申请
    WATER SOLUBLE LUMINESCENCE OXYGEN SENSOR AND METHOD 审中-公开
    水溶性发光氧传感器及方法

    公开(公告)号:WO99040424A1

    公开(公告)日:1999-08-12

    申请号:PCT/US1999/002418

    申请日:1999-02-04

    Abstract: The oxygen concentration of a sample is determined utilizing a water-soluble metal ligand complex which is brought into interactive proximity with the sample to form a mixture. The mixture is irradiated with electromagnetic light energy so as to cause emission of light indicative of oxygen. The emitted light is measured, and the measurement utilized so as to determine oxygen concentration of the sample.

    Abstract translation: 使用与样品相互接近以形成混合物的水溶性金属配体络合物来测定样品的氧浓度。 用电磁光能照射混合物,以便发出指示氧的光。 测量发射光,并利用测量来确定样品的氧浓度。

    IMMUNO-MODULATOR EXHIBITING ANTI-MICROBIAL AND ANTI-MYCOBACTERIAL ACTIVITIES, METHOD FOR PRODUCING THE SAME AND PHARMACEUTICAL PREPARATION FOR TREATING MYCOBACTERIOSES AS WELL AS LUNG CHRONIC AND NON SPECIFIC CONDITIONS, SEXUALLY TRANSMITTED DISEASES AND THE RESULTING IMMUNO-DEFICIENCY
    4.
    发明申请
    IMMUNO-MODULATOR EXHIBITING ANTI-MICROBIAL AND ANTI-MYCOBACTERIAL ACTIVITIES, METHOD FOR PRODUCING THE SAME AND PHARMACEUTICAL PREPARATION FOR TREATING MYCOBACTERIOSES AS WELL AS LUNG CHRONIC AND NON SPECIFIC CONDITIONS, SEXUALLY TRANSMITTED DISEASES AND THE RESULTING IMMUNO-DEFICIENCY 审中-公开
    免疫调节剂展示抗微生物和抗真菌活性,其生产方法和用于治疗MYCOBACTERIOSES的药物制剂以及肺特异性疾病和非特异性疾病,多发性传染病和结果性免疫缺陷

    公开(公告)号:WO99007699A1

    公开(公告)日:1999-02-18

    申请号:PCT/RU1998/000264

    申请日:1998-08-11

    CPC classification number: C07D401/12

    Abstract: The present invention pertains to the field of medicine and more precisely relates to a novel immuno-modulator of formula (I) which exhibits anti-microbial and anti-mycobacterial activities. This modulator is produced by reacting equimolecular amounts of 6-methyluracyl-5-sulphochloride and isoniazide in acetonitrile at a high temperature. The preparation is practically not toxic (LD50 in severe conditions exceeding 7000 mg/kg) and can be used according to given clinical tests for expressing the immuno-modulating and anti-mycobacterial activity. This preparation can be used for correcting various immuno-deficiencies including in HIV-infected patients as well as for treating mycobacterioses such as leprosy, tuberculosis, etc. This preparation can be administered internally or parenterally. The compound described in the present invention represents the active substance of this pharmaceutical preparation, wherein said preparation can be used against secondary immuno-deficiencies or mycobacterioses.

    Abstract translation: 本发明涉及医学领域,更具体地说涉及一种具有抗微生物和抗分枝杆菌活性的式(I)的新型免疫调节剂。 该调节剂是通过使等分子量的6-甲基尿酰基-5-磺酰氯和异烟肼在乙腈中在高温下反应制备的。 该制剂实际上没有毒性(LD50在严重条件下超过7000mg / kg),并且可以根据给出的临床试验用于表达免疫调节和抗分枝杆菌活性。 该制剂可用于校正包括HIV感染患者在内的各种免疫缺陷以及用于治疗诸如麻风病,结核病等分枝杆菌的这种制剂。该制剂可以内部或肠胃外给药。 本发明中描述的化合物代表该药物制剂的活性物质,其中所述制剂可用于二次免疫缺陷或分枝杆菌。

    SUBSTITUTED HETEROCYCLIC DERIVATIVES
    6.
    发明申请
    SUBSTITUTED HETEROCYCLIC DERIVATIVES 审中-公开
    取代的杂环衍生物

    公开(公告)号:WO2014079850A1

    公开(公告)日:2014-05-30

    申请号:PCT/EP2013/074211

    申请日:2013-11-20

    Abstract: The present invention relates to compounds of general formula (I-1) or (I-2) wherein R 1 is hydrogen, lower alkyl, lower alkoxy, halogen, O(CH 2 ) 2 -lower akoxy, O(CH 2 ) 2 N(CH 3 ) 2 , or O(CH 2 )-morpholinyl; R 1' is hydrogen, lower alkyl, lower alkoxy, halogen, O(CH 2 ) 2 -lower akoxy, O(CH 2 ) 2 N(CH 3 ) 2 , or O(CH 2 )-morpholinyl; with the proviso that both R 1 and R 1' may be simultaneously hydrogen, but only one of R 1 and R 1' is lower alkyl, lower alkoxy, halogen, O(CH 2 ) 2 -lower akoxy, O(CH 2 ) 2 N(CH 3 ) 2 , or O(CH 2 )-morpholinyl; Het is a 5-or 6 membered heteroaryl group, wherein the heteroatom is selected from N, O or S; X is -CRR'-, -CRR'-NR'-, -C(O)-, -CH 2 -S-, -CH 2 -S(O) 2 -, CH 2 -O- or -CH 2 -CRR'-; R/R' are independently from each other hydrogen, lower alkyl, hydroxy or phenyl, or R and R' may form together with the carbon atom to which they are attached a cyclopropyl ring; R 2 is lower alkyl, -C(O)O-lower alkyl, C 3-6 -cycloalkyl optionally substituted by lower alkyl or =O, bridged cyclohexyl or C 3-6 -cycloalkenyl, or is a 5-membered heteroaryl group, wherein the heteroatom is selected from N, O or S and which is optionally substituted by one or more lower alkyl, or is pyridinyl, optionally substituted by halogen or lower alkoxy; or is phenyl, optionally substituted by one or more R 2' , selected from halogen, cyano, S(O) 2 -lower alkyl, lower alkyl, lower alkyl substituted by halogen, lower alkoxy, lower alkoxy substituted by halogen or amino, or is benzo[1,3]dioxolyl, naphthyl, indolyl, benzo-isoxazolyl, 2,3-dihydro-1H-indenyl, optionally substituted by lower alkoxy or by an oxo group, or is 3,4-dihydro-2H- [1,4]oxazinyl, optionally substituted by an oxo group, or is a five or six membered heterocycloalkyl group; or to a pharmaceutically acceptable acid addition salt, to a racemic mixture or to its corresponding enantiomer and/or optical isomers thereof. The compounds may be used for the treatment or prophylaxis of schizophrenia, obsessive-compulsive personality disorder, major depression, bipolar disorders, anxiety disorders, normal aging, epilepsy, retinal degeneration, traumatic brain injury, spinal cord injury, post-traumatic stress disorder, panic disorder, Parkinson's disease, dementia, Alzheimer's disease, mild cognitive impairment, chemotherapy-induced cognitive dysfunction, Down syndrome, autism spectrum disorders, hearing loss, tinnitus, spinocerebellar ataxia, amyotrophic lateral sclerosis, multiple sclerosis, Huntington's disease, stroke, radiation therapy, chronic stress, abuse of neuro-active drugs, such as alcohol, opiates, methamphetamine, phencyclidine and cocaine.

    Abstract translation: 本发明涉及通式(I-1)或(I-2)的化合物,其中R 1是氢,低级烷基,低级烷氧基,卤素,O(CH 2)2 - 低级烷氧基,O(CH 2)2 N(CH 3) 2或O(CH 2) - 吗啉基; R 1'是氢,低级烷基,低级烷氧基,卤素,O(CH 2)2 - 低级烷氧基,O(CH 2)2 N(CH 3)2或O(CH 2) 条件是R1和R1'可以同时为氢,但R1和R1'中只有一个为低级烷基,低级烷氧基,卤素,O(CH2)2-低级烷氧基,O(CH2)2N(CH3)2, 或O(CH 2) - 吗啉基; Het是5或6元杂芳基,其中杂原子选自N,O或S; X是-CRR'-,-CRR'-NR'-,-C(O) - , - CH 2 -S-, -​​ CH 2 -S(O)2 - ,CH 2 -O-或-CH 2 -CRR' R / R'彼此独立地是氢,低级烷基,羟基或苯基,或者R和R'可以与它们所连接的碳原子一起形成环丙基环; R 2是低级烷基,-C(O)O-低级烷基,任选地被低级烷基或= O,桥连的环己基或C 3-6 - 环烯基取代的C 3-6 - 环烷基,或是5元杂芳基,其中杂原子 选自N,O或S,并且其任选被一个或多个低级烷基取代,或任选被卤素或低级烷氧基取代的吡啶基; 或任选被一个或多个选自卤素,氰基,S(O)2 - 低级烷基,低级烷基,被卤素取代的低级烷基,低级烷氧基,被卤素或氨基取代的低级烷氧基)的一个或多个R 2' 苯并[1,3]二氧杂环戊烯基,萘基,吲哚基,苯并恶唑基,2,3-二氢-1H-茚基,任选被低级烷氧基或氧代基取代,或是3,4-二氢-2H- [ 4]恶嗪基,任选被氧代基取代,或是五或六元杂环烷基; 或其药学上可接受的酸加成盐与外消旋混合物或其相应的对映体和/或光学异构体反应。 这些化合物可用于治疗或预防精神分裂症,强迫症人格障碍,重度抑郁症,双相情感障碍,焦虑症,正常老化,癫痫,视网膜变性,创伤性脑损伤,脊髓损伤,创伤后应激障碍, 恐慌症,帕金森病,痴呆,阿尔茨海默病,轻度认知障碍,化疗诱发的认知功能障碍,唐氏综合征,自闭症谱系障碍,听力损失,耳鸣,脊髓小脑性共济失调,肌萎缩性侧索硬化,多发性硬化,亨廷顿病,中风,放射治疗 ,慢性应激,滥用神经活性药物,如酒精,阿片剂,甲基苯丙胺,苯环利定和可卡因。

    OXIME O-ETHER COMPOUNDS AND FUNGICIDES FOR AGRICULTURAL AND HORTICULTURAL USE
    8.
    发明申请
    OXIME O-ETHER COMPOUNDS AND FUNGICIDES FOR AGRICULTURAL AND HORTICULTURAL USE 审中-公开
    OXIME O-ETHER化合物和农业和农业用途的杀真菌剂

    公开(公告)号:WO01034568A1

    公开(公告)日:2001-05-17

    申请号:PCT/JP2000/007744

    申请日:2000-11-02

    CPC classification number: C07D213/53 A01N43/40 C07D213/61

    Abstract: Novel oxime O-ether compounds represented by general formula [I]; and fungicides for agricultural and horticultural use, containing the compounds as the active ingredient [I] wherein R is C1-6 alkyl, C3-6 cycloalkyl, C1-6 alkoxy, or the like; m is an integer of 1 to 4; R is hydrogen, C1-6 alkyl, or the like; R and R are each hydrogen or C1-6 alkyl; R is hydrogen, C1-6 alkyl, or the like; R is C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 alkoxy, halogeno, or the like; and n is an integer of 1 to 4.

    Abstract translation: 由通式[I]表示的新型肟O-醚化合物; 和用于农业和园艺用途的杀真菌剂,其含有化合物作为活性成分[I],其中R 1为C 1-6烷基,C 3-6环烷基,C 1-6烷氧基等; m为1〜4的整数。 R 2是氢,C 1-6烷基等; R 3和R 4各自为氢或C 1-6烷基; R 5是氢,C 1-6烷基等; R 6是C 1-6烷基,C 2-6烯基,C 2-6炔基,C 1-6烷氧基,卤代等; n为1〜4的整数。

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