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1. 发明授权

US4874747A Polycyclic heterocyclic compounds, a process for their preparation and their use in human and veterinary medicine 失效
标题翻译：多环杂环化合物，其制备方法及其在人兽药中的应用
公开(公告)号：US4874747A
公开(公告)日：1989-10-17
申请号：US188547
申请日：1988-04-29
申请人： Braham Shroot , Jacques Eustache , Jean-Michel Bernardon , Philippe Nedoncelle
发明人： Braham Shroot , Jacques Eustache , Jean-Michel Bernardon , Philippe Nedoncelle
IPC分类号： A61K8/00 , A61K8/49 , A61K31/335 , A61K31/34 , A61K31/343 , A61K31/38 , A61K31/381 , A61K31/40 , A61K31/403 , A61K31/415 , A61K31/4184 , A61K31/42 , A61K31/423 , A61K31/70 , A61K31/7024 , A61P11/00 , A61P17/00 , A61P29/00 , A61P35/00 , A61Q5/00 , A61Q19/00 , C07C205/06 , C07C205/25 , C07D209/60 , C07D235/02 , C07D263/52 , C07D263/60 , C07D277/60 , C07D307/92 , C07D333/74 , C07H13/08
CPC分类号： A61K8/49 , A61K8/4946 , A61K8/4973 , A61K8/4986 , A61Q19/00 , A61Q5/008 , C07C205/06 , C07C205/25 , C07D209/60 , C07D235/02 , C07D263/60 , C07D307/92 , C07D333/74 , A61Q19/007 , A61Q19/008 , A61Q7/00 , Y10S514/863 , Y10S514/88 , Y10S514/912
摘要： A polycyclic heterocyclic compound has the formula ##STR1## wherein n is 1 or 2,R.sub.1 l represents (i) lower alkyl, (ii) --CH.sub.2 OH or (iii) ##STR2## R.sub.2 represents (a) hydrogen, (b) ##STR3## or (c)--OR.sub.3, R.sub.3 represents hydrogen, C.sub.1 -C.sub.20 alkyl mono or polyhydroxyalkyl, aryl or aralkyl optionally substituted, the residue of a sugar or ##STR4## wherein p is 1, 2, or 3, and r' and r" represent hydrogen, lower alkyl, mono or polyhydroxyalkyl, aryl optionally substituted, amino acid residue, aminated sugar residue, or together form a heterocycle,X represents oxygen, sulfur, SO, SO.sub.2 or --NR.sub.4,Y represents CR.sub.4 or a nitrogen atom andR.sub.4 represents hydrogen or lower alkyl.This polycyclic heterocyclic compound can be used in human and veterinary medicine and especially in the topical or systemic treatment of determatologic diseases.
摘要翻译：多环杂环化合物具有下式（I）其中n为1或2，R 1表示（ⅰ）低级烷基，（ⅱ）-CH 2 OH或（ⅲ）R 2表示（a）氢，（b 或者（c）-OR 3，R 3表示氢，任选取代的C 1 -C 20烷基单或多羟基烷基，芳基或芳烷基，糖或其中p是1,2或3的残基，并且r '和r“表示氢，低级烷基，单或多羟基烷基，任选取代的芳基，氨基酸残基，胺化糖残基，或一起形成杂环，X表示氧，硫，SO，SO 2或-NR 4，Y表示CR 4或氮原子，R 4表示氢或低级烷基。这种多环杂环化合物可以用于人和兽医学，特别是局部或全身治疗病原性疾病。

2. 发明授权

US4440935A Bicycloimidazoles 失效
标题翻译：双环咪唑
公开(公告)号：US4440935A
公开(公告)日：1984-04-03
申请号：US420076
申请日：1982-09-20
申请人： Fu-chih Huang
发明人： Fu-chih Huang
IPC分类号： C07C37/055 , C07C39/23 , C07C43/215 , C07C205/25 , C07D263/52 , C07D263/60 , C07D265/34 , C07D413/04 , A61K31/425 , C07D235/24
CPC分类号： C07D263/52 , C07C205/25 , C07C37/055 , C07C41/16 , C07D263/60 , C07D265/34 , C07D413/04 , C07C2102/10
摘要： Bicycloimidazoles having the structure: ##STR1## wherein n is 3, 4, or 5R.sub.1 is hydrogen or alkyl,R.sub.2 is hydrogen, alkyl, hydroxyl, alkoxy, cyano, phenyl, carboxyl, tetrazole, or halogen,R.sub.3 is tetrazole, carboxamide or ##STR2## wherein Z is oxygen, sulfur, or NH andR.sub.4 is H, alkali metal, ammonium, alkyl, alkoxyalkyl, aryl, or aralkyl,are novel and useful as antiallergic agents. The compounds are formulated with a pharmaceutical carrier for oral, parental, inhalational, or rectal means of administration.
摘要翻译：具有以下结构的双环咪唑：其中n为3,4或5个R 1为氢或烷基，R 2为氢，烷基，羟基，烷氧基，氰基，苯基，羧基，四唑或卤素，R 3为四唑，甲酰胺或其中Z是氧，硫或NH，R4是H，碱金属，铵，烷基，烷氧基烷基，芳基或芳烷基，是新颖的，可用作抗过敏剂。化合物与用于口服，亲本，吸入或直肠给药方式的药物载体一起配制。

3. 发明授权

US3960957A 2-(6'-methoxynaphth-2'yl) propionaldoxime and 5'-halo derivatives thereof 失效
标题翻译： 2-（6（4-甲氧基萘-2-基）（40）基丙氧基肟及其5（40-卤代衍生物）
公开(公告)号：US3960957A
公开(公告)日：1976-06-01
申请号：US540011
申请日：1975-01-10
申请人： Francisco Sanchez Alvarez
发明人： Francisco Sanchez Alvarez
IPC分类号： C07B57/00 , C07C39/38 , C07C45/46 , C07C51/08 , C07C51/16 , C07C51/36 , C07C51/377 , C07C51/487 , C07C59/64 , C07C205/37 , C07C131/00
CPC分类号： C07C205/25 , C07B57/00 , C07C205/37 , C07C39/38 , C07C45/46 , C07C45/58 , C07C51/08 , C07C51/16 , C07C51/36 , C07C51/377 , C07C51/487 , C07C59/64
摘要： New compounds, 2-(6'-methoxynaphth-2'-yl)propylene oxide, 2-(6'-methoxynaphth-2'-yl)propionaldoxime, 2-hydroxy-2-(6'-methoxynaphth-2'-yl)-propionitrile, 2-(6'methoxynaphth-2'-yl)acrylonitrile, 2-(6'-methoxynaphth-2'-yl)acrylic acid, the corresponding 5'-halo compounds and 2-(5'-halo-6'-methoxynaphth-2'-yl)propionaldehyde are useful intermediates in producing 2-(6'-methoxynaphth-2'-yl)propionic acid and the corresponding 5'-halo acids from 6-methoxy-2-acetylnaphthalene and the corresponding 5-halo compounds. The 2-propionic acids are anti-inflammatory, analgesic, anti-pyretic and anti-pruritic agents. The 2-propionaldehydes, obtained from the 2-acetyl compounds by way of the 2-propylene oxide, can be converted directly to the 2-propionic acids by way of the 2-propionaldoximes and the 2-propionitriles or more directly by Jones oxidation. Alternatively the 2-acrylonitriles, obtained from the 2-acetyl compounds by way of the 2-hydroxy-2-propionitrile, can be converted to the 2-propionic acid by way of the 2-acrylic acid or 2-propionitrile.
摘要翻译：新化合物2-（6'-甲氧基硫化-2'-基）环氧丙烷，2-（6'-甲氧基硫杂-2'-基）丙氧基肟，2-羟基-2-（6'-甲氧基硫杂-2'-基）） - 丙腈，2-（6'-甲氧基硫杂-2'-基）丙烯腈，2-（6'-甲氧基硫杂-2'-基）丙烯酸，相应的5'-卤素化合物和2-（5'- 6'-甲氧基硫杂-2'-基）丙醛是制备2-（6'-甲氧基硫杂-2'-基）丙酸和相应的5-甲氧基-2-乙酰基萘的5'-卤代酸的有用的中间体和相应的 5-卤代化合物。 2-丙酸是抗炎，止痛，抗热解和抗瘙痒剂。通过2-环氧丙烷从2-乙酰基化合物获得的2-丙醛可以通过2-丙炔肟和2-丙腈直接转化为2-丙酸，或者通过琼斯氧化直接转化成2-丙酸。或者，通过2-羟基-2-丙腈从2-乙酰基化合物获得的2-丙烯腈可以通过2-丙烯酸或2-丙腈转化成2-丙酸。

4. 发明授权

US3873594A 2-(6-Methoxynaphth-2-yl) propionitrile 失效
标题翻译： 2-（6-甲氧基萘-2-基）丙腈
公开(公告)号：US3873594A
公开(公告)日：1975-03-25
申请号：US35453773
申请日：1973-04-26
申请人： SYNTEX CORP
发明人： ALVAREZ FRANCISCO SANCHEZ
IPC分类号： C07C43/225 , C07C205/25 , C07C205/37 , C07C121/66
CPC分类号： C07C45/46 , C07C43/225 , C07C45/58 , C07C205/25 , C07C205/37 , C07C49/84 , C07C47/277
摘要： New compounds, 2-(6''-methoxynaphth-2''-yl)propylene oxide, 2-(6''methoxynaphth-2''-yl)propionaldoximo, 2-hydroxy-2-(6''methoxynaphth-2''-yl)propionitrile, 2-(6''-methoxynaphth-2''yl)acrylonitrile, 2-(6''-methoxynaphth-2''-yl)acrylic acid, the corresponding 5''-halo compounds and 2-(5''-halo-6''-methoxynaphth2''-yl)propionaldehyde are useful intermediates in producing 2(6''-methoxynaphth-2''-yl)propionic acid and the corresponding 5''halo acids from 6-methoxy-2-acetylnaphthalene and the corresponding 5-halo compounds. The 2-propionic acids are antiinflammatory, analgesic, anti-pyretic and anti-pruritic agents. The 2-propionaldehydes, obtained from the 2-acetyl compounds by way of the 2-propylene oxide, can be converted directly to the 2propionic acids by way of the 2-propionaldoximes and the 2propionitriles or more directly by Jones oxidation. Alternatively the 2-acrylonitriles, obtained from the 2-acetyl compounds by way of the 2-hydroxy-2-propionitrile, can be converted to the 2propionic acid by way of the 2-acrylic acid or 2-propionitrile.
摘要翻译：新化合物2-（6'-甲氧基硫杂-2'-基）环氧丙烷，2-（6'-甲氧基硫杂-2'-基）丙基肟基，2-羟基-2-（6'-甲氧基硫杂-2'-基））丙腈，2-（6'-甲氧基硫杂-2'-基）丙烯腈，2-（6'-甲氧基硫杂-2'-基）丙烯酸，相应的5'-卤代化合物和2-（5'- 6'-甲氧基硫杂-2'-基）丙醛是制备2-（6'-甲氧基硫杂-2'-基）丙酸和相应的5-甲氧基-2-乙酰基萘的5'-卤代酸的有用的中间体， 5-卤代化合物。 2-丙酸是抗炎，止痛，抗热解和抗瘙痒剂。通过2-环氧丙烷从2-乙酰基化合物获得的2-丙醛可以通过2-丙炔肟和2-丙腈直接转化为2-丙酸，或者通过琼斯氧化直接转化成2-丙酸。或者，通过2-羟基-2-丙腈从2-乙酰基化合物获得的2-丙烯腈可以通过2-丙烯酸或2-丙腈转化成2-丙酸。

5. 发明授权

US3830854A Substituted 5,8-dimethyl-5,6,7,8-tetrahydro-1-naphthols 失效
标题翻译：取代的5,8-二甲基-5,6,7,8-四氢-1-萘酚
公开(公告)号：US3830854A
公开(公告)日：1974-08-20
申请号：US156870
申请日：1970-01-08
申请人： ALLIED CHEM
发明人： DEGGINGER E , BALQUIST J
IPC分类号： A01N31/16 , C07C37/62 , C07C39/42 , C07C79/24
CPC分类号： A01N31/16 , C07C37/62 , C07C39/42 , C07C205/25 , C07C2602/10
摘要： MATERIALS CAN BE PROTECTED FROM ATTACK BY INSECTS, MITES AND NEMATODES BY APPLYING TO THE MATERIAL A 5,8 DIMETHYL5,6,7,8-TERAHYDRO-1-NAPHTHOL HAVING THE FORMULA

5,8-DI(H3C-),X,Y,Z-5,6,7,8-TETRAHYDRO-1-NAPHTHOL

WHEREIN X, Y AND Z ARE SUBSTITUENTS INDEPENDENTLY OC CUPYING THE 2,3 AND 4 POSTIONS: X IS HYDROGEN, FLUORINE, CHLORINE, OR BROMINE, Y IS FLUORINE, CHLORINE, BROMINE, NITRO OR LOWER ALKOXY , AND Z IS HYDROGEN OR NITRO. THE TETRAHYDRONAPHTHOLS WHEREIN Z IS HYDROGEN CAN BE PREPARED BY CYCLIALKYLATING A PHENOL HAVING CORRESPONDING X AND Y SUBSTITUENTS (Y NOT BEING NITRO) WITH 1,5 HEXADIENE IN THE PRESENCE OF A CATALYST SUCH AS ALIMINUM PLICATE, ALTERNATIVELY, TETRAHYDRONAPHTHOLS WHEREIN X AND/OR Y ATE CHLORINE OR BROMINE CAN BE PREPARED BY 5DIRECT HALOGENATION OF THE CYCLIALKYLATION PRODUCT LETRAHYDRONAHTHOLS WHEREIN Z AND OR Y ARE NITRO CAN BE PREPARED BY NITATING THE CYCLIALKYLATION PRODUCT.

6. 发明授权

US3390161A Process for separating trace quantites of an impurity isotope from a mixture of elements 失效
标题翻译：从元素混合物中分离杂质同位素的微量元素的方法
公开(公告)号：US3390161A
公开(公告)日：1968-06-25
申请号：US31234163
申请日：1963-09-30
申请人： BENDIX CORP
发明人： FRAIOLI ANTHONY V
IPC分类号： C07C201/00 , C07C201/16 , C22B3/26
CPC分类号： C22B3/0009 , C07C201/00 , C07C201/16 , Y02P10/234 , C07C207/04 , C07C205/25

7. 发明授权

US09402850B2 BAX agonist, compositions, and methods related thereto 有权
公开(公告)号：US09402850B2
公开(公告)日：2016-08-02
申请号：US14709580
申请日：2015-05-12
申请人： EMORY UNIVERSITY , BOARD OF REGENTS OF THE UNIVERSITY OF TEXAS SYSTEM
发明人： Xingming Deng , Jia Zhou , Chunyong Ding
IPC分类号： A61K31/05 , A61K31/5375 , C07D213/73 , C07D213/74 , C07C271/16 , C07C205/11 , C07C205/25 , C07C205/35 , C07C309/65 , C07C311/21 , C07C211/52 , C07C215/88 , C07C217/20 , C07C217/26 , C07C217/94 , C07C233/18 , C07C233/25 , C07C233/80 , C07D209/10 , C07D295/088 , C07D211/46 , C07D295/185 , C07D295/26 , C07D213/61 , C07D213/64 , A61K31/085 , A61K31/138 , A61K31/404 , A61K31/44 , A61K31/4412 , A61K31/4465 , A61K31/495 , A61K45/06 , C07C217/60 , C07D209/12 , C07D213/643
CPC分类号： A61K31/5375 , A61K31/05 , A61K31/085 , A61K31/138 , A61K31/404 , A61K31/44 , A61K31/4412 , A61K31/4465 , A61K31/495 , A61K45/06 , C07C205/11 , C07C205/25 , C07C205/35 , C07C211/52 , C07C215/88 , C07C217/20 , C07C217/26 , C07C217/60 , C07C217/94 , C07C233/18 , C07C233/25 , C07C233/80 , C07C271/16 , C07C309/65 , C07C311/21 , C07C2601/02 , C07C2603/18 , C07D209/10 , C07D209/12 , C07D211/46 , C07D213/61 , C07D213/64 , C07D213/643 , C07D213/73 , C07D213/74 , C07D295/088 , C07D295/185 , C07D295/26
摘要： The disclosure relates to BAX activators and therapeutic uses relates thereto. In certain embodiments, the disclosure relates to methods of treating or preventing cancer, such as lung cancer, comprising administering a therapeutically effective amount of a pharmaceutical composition comprising a compound disclosed herein or pharmaceutically acceptable salt to a subject in need thereof.

8. 发明授权

US09040567B2 BAX agonist, compositions, and methods related thereto 有权
标题翻译： BAX激动剂，组合物和与之有关的方法
公开(公告)号：US09040567B2
公开(公告)日：2015-05-26
申请号：US14239177
申请日：2012-08-17
申请人： Xingming Deng , Jia Zhou , Chunyong Ding
发明人： Xingming Deng , Jia Zhou , Chunyong Ding
IPC分类号： A61K31/05 , C07D213/73 , C07D213/74 , C07C271/16 , C07C205/11 , C07C205/25 , C07C205/35 , C07C309/65 , C07C311/21 , C07C211/52 , C07C215/88 , C07C217/20 , C07C217/26 , C07C217/94 , C07C233/18 , C07C233/25 , C07C233/80 , C07D209/10 , C07D295/088 , C07D211/46 , C07D295/185 , C07D295/26 , C07D213/61 , C07D213/64 , A61K31/085 , A61K31/138 , A61K31/404 , A61K31/44 , A61K31/4412 , A61K31/4465 , A61K31/495 , A61K31/5375 , A61K45/06 , C07C217/60 , C07D209/12 , C07D213/643
CPC分类号： A61K31/5375 , A61K31/05 , A61K31/085 , A61K31/138 , A61K31/404 , A61K31/44 , A61K31/4412 , A61K31/4465 , A61K31/495 , A61K45/06 , C07C205/11 , C07C205/25 , C07C205/35 , C07C211/52 , C07C215/88 , C07C217/20 , C07C217/26 , C07C217/60 , C07C217/94 , C07C233/18 , C07C233/25 , C07C233/80 , C07C271/16 , C07C309/65 , C07C311/21 , C07C2601/02 , C07C2603/18 , C07D209/10 , C07D209/12 , C07D211/46 , C07D213/61 , C07D213/64 , C07D213/643 , C07D213/73 , C07D213/74 , C07D295/088 , C07D295/185 , C07D295/26
摘要： The disclosure relates to BAX activators and therapeutic uses relates thereto. In certain embodiments, the disclosure relates to methods of treating or preventing cancer, such as lung cancer, comprising administering a therapeutically effective amount of a pharmaceutical composition comprising a compound disclosed herein or pharmaceutically acceptable salt to a subject in need thereof.
摘要翻译：本公开涉及BAX活化剂和治疗用途。在某些实施方案中，本公开涉及治疗或预防癌症（例如肺癌）的方法，包括向有需要的受试者施用治疗有效量的包含本文公开的化合物或药学上可接受的盐的药物组合物。

9. 发明申请

US20100298567A1 NITRATION OF ACTIVATED AROMATICS IN MICROREACTORS 审中-公开
标题翻译：微生物中激活的芳族化合物的硝化
公开(公告)号：US20100298567A1
公开(公告)日：2010-11-25
申请号：US12160804
申请日：2006-01-12
申请人： Dominique Roberge , Laurent Ducry
发明人： Dominique Roberge , Laurent Ducry
IPC分类号： C07D239/02 , C07C205/00 , C07C63/04 , C07D211/72
CPC分类号： C07C201/08 , B01J19/0093 , B01J2219/0086 , B01J2219/00984 , C07C205/23 , C07C205/22 , C07C205/25 , C07C205/37 , C07C205/59 , C07C205/60
摘要： The invention relates to the nitration of aromatic or heteroaromatic compounds, wherein an activated aromatic or heteroaromatic compound and a nitration agent, optionally in the presence of a solvent, are mixed intensely in a microreactor, and wherein the proportion of the nitration agent to the activated aromatic or heteroaromatic compound, the concentration of nitration agent in the reaction mixture, and the temperature are selected at levels such high that the nitration begins autocatalytically, and wherein the nitration product is obtained after leaving the microreactor and, optionally after an after-reaction time outside the microreactor.
摘要翻译：本发明涉及芳族或杂芳族化合物的硝化，其中任选在溶剂存在下的活化芳族或杂芳族化合物和硝化剂在微反应器中强烈混合，并且其中硝化剂与活化的芳族或杂芳族化合物，硝化剂在反应混合物中的浓度和温度选择为使得硝化开始自动催化的水平，并且其中硝化产物在离开微反应器之后获得，并且任选地在反应后时间在微反应器外面。

10. 发明授权

US06903114B2 Derivatives of naphthalene with COMT inhibiting activity 有权
标题翻译：具有COMT抑制活性的萘衍生物
公开(公告)号：US06903114B2
公开(公告)日：2005-06-07
申请号：US10380286
申请日：2001-09-14
申请人： Reijo Bäckström , Jarmo Pystynen , Timo Lotta , Martti Ovaska , Jyrki Taskinen
发明人： Reijo Bäckström , Jarmo Pystynen , Timo Lotta , Martti Ovaska , Jyrki Taskinen
IPC分类号： A61P25/16 , C07C45/00 , C07C45/30 , C07C45/46 , C07C45/56 , C07C45/67 , C07C47/57 , C07C47/575 , C07C49/83 , C07C49/84 , C07C65/11 , C07C205/25 , C07C205/37 , C07C205/43 , C07C205/45 , C07C205/59 , C07C245/10 , C07C255/53 , C07C311/29 , C07D207/44 , C07D207/452 , C07D215/20 , C07D217/10 , C07D295/192 , A61K31/47
CPC分类号： C07D207/452 , C07C45/00 , C07C45/30 , C07C45/46 , C07C45/565 , C07C45/673 , C07C47/57 , C07C47/575 , C07C49/83 , C07C49/84 , C07C65/11 , C07C205/25 , C07C205/37 , C07C205/43 , C07C205/45 , C07C205/59 , C07C245/10 , C07C255/53 , C07C311/29 , C07D215/20 , C07D217/10 , C07D295/192
摘要： Compounds of formula (I′), wherein A, R1 to R3 and t are as defined in the disclosure, exhibit COMT enzyme inhibiting activity so that they are useful as COMT inhibitors.
摘要翻译：式（I'）的化合物，其中A，R 1至R 3和t如本公开所定义，表现出COMT酶抑制活性，因此它们可用作 COMT抑制剂。

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