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91. 发明公开

KR1020120006051A ＣＣＲ2의 4-아제티디닐-1-헤테로원자 연결된 사이클로헥산 길항제 无效
标题翻译： CCR2的4-AZETIDINYL-1-HETEROATOM连接环孢菌素拮抗剂
公开(公告)号：KR1020120006051A
公开(公告)日：2012-01-17
申请号：KR1020117026820
申请日：2010-04-15
申请人： 얀센 파마슈티카 엔.브이.
发明人： 장쑤큉 , 후프나젤헤더래이 , 수이지후아
IPC分类号： C07D401/08 , A61K31/4427 , A61P3/00
CPC分类号： C07D417/08 , C07D401/08 , C07D403/08 , C07D405/08 , C07D413/08
摘要： 본 발명은 화학식 I의 화합물을 포함한다.
[화학식 I]
.
상기 식에서, X, R
1 , R
2 , R
3 및 R
4 는 본 명세서에 정의된 바와 같다. 본 발명은 또한, II형 당뇨병, 비만 및 천식인 증후군, 장애 또는 질환을 예방, 치료 또는 개선시키는 방법을 포함한다. 본 발명은 또한, 치료적 유효량의, 적어도 하나의 화학식 I의 화합물의 투여에 의해 포유동물에서 CCR2 활성을 억제시키는 방법을 포함한다.

92. 发明授权

KR100163185B1 치환된 아졸일메틸시클로알칸올 및 이들을 함유하는 살균제 失效
标题翻译：取代的AZOLYLMETHYLCYCLO烷醇和含有它们的杀真菌剂
公开(公告)号：KR100163185B1
公开(公告)日：1998-12-01
申请号：KR1019900021104
申请日：1990-12-17
申请人： 바스프 에스이
发明人： 라이너젤레 , 베른하르트찌페러 , 미하엘카일 , 노르베르트괴츠 , 에버하르트암머만 , 기젤라로렌츠 , 라이너코베르 , 토마스퀴켄횐너 , 알블흐트하레우스 , 빌헬름라데마허
IPC分类号： C07D249/08 , A01N43/50 , C07D233/60 , C07D401/12 , C07D403/08
CPC分类号： C07D303/22 , A01N43/50 , A01N43/653 , C07D231/12 , C07D233/56 , C07D249/08 , C07D303/04 , C07D303/08 , C07D303/34 , C07D405/06 , C07D405/08 , C07D407/04 , C07D407/06 , C07D493/10
摘要： 본 발명은 하기 일반식(I)의 아졸일메틸시클로알칸, 식물에 허용되는 이들의 산부가염과 금속 착물, 및 상기 화합물을 함유하는 성장 조절제 및 살균제에 관한 것이다;
상기 식에서, R
1 및 R
5 는 같거나 다르며, 각각 수소 알킬이고; R
1 및 R
5 는 탄소원자와 함께 CH=CH-R
7 또는 CH-ZR
7 을 형성하는 것으로, 여기서 Z는 CH
2 , O, S, SO, SO
2 또는 NR
8 이고, R
7 은 알킬, 페닐, 비페닐, 나프틸, 헤테로아릴, 벤질 또는 시클로알킬(여기서, 상기 기들중 각각은 치환될 수 있음), 또는 테트라히드로피란일이고; R
2 및 R
3 는 각각 수소 또는 알킬이거나, R
1 및 R
5 가 CH=CH-R
7 를 형성하는 경우 R
2 및 R
3 는 서로 함께 추가로 =CH-R
7 을 형성할 수 있고; R
4 , R
8 은 각각 수소 또는 알킬이거나, 또는 R
3 및 R
4 는 탄소 원자와 함께 포화 또는 불포화된 5-원자 또는 6-원자 탄소고리를 형성하거나, 또는 R
2 , R
3 , R
4 및 R
9 는 탄소원자와 함께 비치환되거나 할로겐-치환된 페닐고리를 형성하거나, 또는 R
1 및 R
5 가 C=CH-R
7 를 형성하는경우, R
2 및 R
3 는 탄소원자와 함께 추가로 =CH-R
7 를 형성할 수 있고; R
2 및 R
9 내지 R
12 는 각각
수소, 알킬, 페닐, 비페닐, 나프틸, 헤테로아릴, 벤질, 디옥소란일 또는 시클로알킬(여기서, 상기 기들은 치환될 수 있음)이고; T는 (CH
2 )
n , =CR
11 R
12 , O 또는 S를 말하는 것으로, 여기서, n은 1 내지 5의 정수인데, 단, R
1 내지 R
12 는 동시에 수소가 아니며, R
2 내지 R
4 및 R
6 내지 R
12 가 수소인 경우 R
1 및 R
5 는 서로함께 또는

93. 发明申请

WO2013057251A3 HETEROARYL HYDROXAMIC ACID DERIVATIVES AND THEIR USE IN THE TREATMENT, AMELIORATION OR PREVENTION OF A VIRAL DISEASE 审中-公开
标题翻译：异氟烷酸衍生物及其在治疗，改善或预防病毒性疾病中的应用
公开(公告)号：WO2013057251A3
公开(公告)日：2013-06-06
申请号：PCT/EP2012070757
申请日：2012-10-19
申请人： HOFFMANN LA ROCHE , SAVIRA PHARMACEUTICALS GMBH , EUROPEAN MOLECULAR BIOLOGY LAB EMBL
发明人： CLASSEN-HOUBEN DIRK , WOLKERSTORFER ANDREA , SZOLAR OLIVER , SMITH MARK , SO SUNG-SAU , CUSACK STEPHEN , LANGER THIERRY , GIETHLEN BRUNO , MORICE CHRISTOPHE , MICHAUT-SIMON CELINE , ZUBIETA CHLOE
IPC分类号： C07D213/81 , A61K31/44 , A61P31/16 , C07D217/26 , C07D401/04 , C07D401/12 , C07D401/14 , C07D405/08 , C07D413/04 , C07D471/04 , C07D495/04
CPC分类号： C07D213/81 , A61K31/44 , A61K31/4439 , A61K31/444 , A61K31/4545 , A61K31/47 , A61K31/472 , A61K31/496 , A61K31/519 , A61K31/5377 , A61K45/06 , C07D215/48 , C07D217/26 , C07D401/04 , C07D401/12 , C07D401/14 , C07D405/04 , C07D405/08 , C07D413/04 , C07D471/04 , C07D493/10 , C07D495/04
摘要： The present invention relates to a compound having the general formula I, optionally in the form of a pharmaceutically acceptable salt, solvate, polymorph, prodrug, tautomer, racemate, enantiomer, or dsasiereomer or mixture thereof, which is useful in treating, ameloriating or preventing a viral disease. Furthermore, specific combination therapies are disclosed.
摘要翻译：本发明涉及一种具有通式I的化合物，其任选呈药学上可接受的盐，溶剂合物，多晶型物，前体药物，互变异构体，外消旋物，对映体或dsasiereomer或其混合物的形式，其可用于治疗，预防或预防病毒性疾病此外，公开了具体的组合疗法。

94. 发明申请

WO2013057251A2 HETEROARYL HYDROXAMIC ACID DERIVATIVES AND THEIR USE IN THE TREATMENT, AMELIORATION OR PREVENTION OF A VIRAL DISEASE 审中-公开
标题翻译：杂芳基氢醌酸衍生物及其在治疗，改善或预防病毒性疾病中的用途
公开(公告)号：WO2013057251A2
公开(公告)日：2013-04-25
申请号：PCT/EP2012/070757
申请日：2012-10-19
申请人： F. HOFFMANN-LA ROCHE AG , SAVIRA PHARMACEUTICALS GMBH , EUROPEAN MOLECULAR BIOLOGY LABORATORY
发明人： CLASSEN-HOUBEN, Dirk , WOLKERSTORFER, Andrea , SZOLAR, Oliver , SMITH, Mark , SO, Sung-Sau , CUSACK, Stephen , LANGER, Thierry , GIETHLEN, Bruno , MORICE, Christophe , MICHAUT-SIMON, Céline , ZUBIETA, Chloe
IPC分类号： C07D213/81 , C07D217/26 , C07D401/04 , C07D401/12 , C07D401/14 , C07D405/08 , C07D413/04 , C07D471/04 , C07D495/04 , A61K31/44 , A61P31/16
CPC分类号： C07D213/81 , A61K31/44 , A61K31/4439 , A61K31/444 , A61K31/4545 , A61K31/47 , A61K31/472 , A61K31/496 , A61K31/519 , A61K31/5377 , A61K45/06 , C07D215/48 , C07D217/26 , C07D401/04 , C07D401/12 , C07D401/14 , C07D405/04 , C07D405/08 , C07D413/04 , C07D471/04 , C07D493/10 , C07D495/04
摘要： The present invention relates to a compound having the general formula I, optionally in the form of a pharmaceutically acceptable salt, solvate, polymorph, prodrug, tautomer, racemate, enantiomer, or dsasiereomer or mixture thereof, which is useful in treating, ameloriating or preventing a viral disease. Furthermore, specific combination therapies are disclosed.
摘要翻译：本发明涉及具有通式I的化合物，任选呈其药学上可接受的盐，溶剂化物，多晶型物，前药，互变异构体，外消旋物，对映异构体或dsasomalomer或其混合物的形式，其可用于治疗，改善或预防病毒性疾病。此外，披露了特定的联合疗法。

95. 发明申请

WO2011012862A1 HERBICIDALLY ACTIVE HETEROARYL-SΥBSTITΥTED CYCLIC DIONES OR DERIVATIVES THEREOF 审中-公开
标题翻译：除草剂活性异丁基-S？BSTIT？环状二环或其衍生物
公开(公告)号：WO2011012862A1
公开(公告)日：2011-02-03
申请号：PCT/GB2010/001449
申请日：2010-07-29
申请人： SYNGENTA LIMITED , JEANMART, Stephane André Marie , LONGSTAFF, Adrian , MATHEWS, Christopher John , RUSSELL, Claire Janet , VINER, Russell Colin , WOOD, Frances Kathryn
发明人： JEANMART, Stephane André Marie , LONGSTAFF, Adrian , MATHEWS, Christopher John , RUSSELL, Claire Janet , VINER, Russell Colin , WOOD, Frances Kathryn
IPC分类号： C07D401/08 , C07D405/08 , C07D409/08 , C07D417/08 , C07D417/14 , A01N43/78
CPC分类号： C07D405/08 , A01N43/10 , A01N43/54 , A01N43/56 , A01N43/78 , C07D401/08 , C07D409/08 , C07D417/08 , C07D417/14
摘要： The invention relates to a compound of formula (I), which is suitable for use as a herbicide wherein G is hydrogen or an agriculturally acceptable metal, sulfonium, ammonium or latentiating group; Q is a unsubstituted or substituted C 3 -C 8 saturated or mono-unsaturated heterocyclyl containing at least one heteroatom selected from O, N and S, or Q is heteroaryl or substituted heteroaryl; m is 1, 2 or 3; and Het is an optionally substituted monocyclic or bicyclic heteroaromatic ring; and wherein the compound is optionally an agronomically acceptable salt thereof.
摘要翻译：本发明涉及式（I）化合物，其适用作除草剂，其中G为氢或农业上可接受的金属，锍，铵或潜伏基; Q是含有至少一个选自O，N和S的杂原子的未取代或取代的C3-C8饱和或单不饱和杂环基，或Q是杂芳基或取代的杂芳基; m为1,2或3; Het是任选取代的单环或双环杂芳环; 并且其中所述化合物任选为其农学上可接受的盐。

96. 发明申请

WO2009137412A1 THERAPEUTIC COMPOUNDS 审中-公开
标题翻译：治疗化合物
公开(公告)号：WO2009137412A1
公开(公告)日：2009-11-12
申请号：PCT/US2009/042724
申请日：2009-05-04
申请人： ALLERGAN, INC. , OLD, David, W. , NGO, Vinh, X.
发明人： OLD, David, W. , NGO, Vinh, X.
IPC分类号： C07C205/59 , C07C255/46 , C07C255/57 , C07C235/02 , C07C69/24 , C07C69/732 , C07C69/738 , C07C69/76 , C07D213/00 , C07D215/00 , C07D265/30 , C07D277/00 , C07D307/00 , C07D333/00 , C07D413/00 , C07D409/00
CPC分类号： C07C325/02 , C07C205/59 , C07C255/46 , C07C255/57 , C07C405/00 , C07C2601/08 , C07C2601/10 , C07C2602/08 , C07C2602/10 , C07D213/50 , C07D213/74 , C07D215/14 , C07D215/26 , C07D277/56 , C07D295/088 , C07D307/68 , C07D333/16 , C07D333/38 , C07D405/08 , C07D409/06 , C07D417/08 , C07D417/12
摘要： Compounds comprising formula (I) or a pharmaceutically acceptable salt thereof, a dashed line represent the presence or absence of a double bond, are disclosed, wherein J 1 , J 2 , U 1 , B, Y, and A are as described in claims 1-12. Methods, compositions, and medicaments related thereto are also disclosed, for treating glaucoma, inflammatory bowel disease and baldness.
摘要翻译：公开了包含式（I）化合物或其药学上可接受的盐的化合物，虚线代表双键的存在或不存在，其中J1，J2，U1，B，Y和A如权利要求1-12所述。还公开了用于治疗青光眼，炎症性肠病和秃发的方法，组合物和与之相关的药物。

97. 发明申请

WO2008039418A2 ACYLATED PIPERIDINE DERIVATIVES AS MELANOCORTIN-4 RECEPTOR MODULATORS 审中-公开
标题翻译：酰化哌啶衍生物作为黑色素-4受体调节剂
公开(公告)号：WO2008039418A2
公开(公告)日：2008-04-03
申请号：PCT/US2007020606
申请日：2007-09-24
申请人： MERCK & CO INC , BAKSHI RAMAN K , DELLUREFICIO JAMES P , HONG QINGMEI , JIAN TIANYING , LIU JIAN , NARGUND RAVI P , YE ZHIXIONG
发明人： BAKSHI RAMAN K , DELLUREFICIO JAMES P , HONG QINGMEI , JIAN TIANYING , LIU JIAN , NARGUND RAVI P , YE ZHIXIONG
IPC分类号： A61K31/454
CPC分类号： C07D405/14 , C07D211/26 , C07D401/08 , C07D405/08 , C07D413/08 , C07D471/04 , C07D487/08 , C07D491/08 , C07D498/04
摘要： Certain novel N-acylated spiropiperidine derivatives are ligands of the human melanocortin receptor(s) and, in particular, are selective ligands of the human melanocortin-4 receptor (MC-4R). They are therefore useful for the treatment, control, or prevention of diseases and disorders responsive to the modulation of MC-4R, such as obesity, diabetes, nicotine addiction, alcoholism, sexual dysfunction, including erectile dysfunction and female sexual dysfunction.
摘要翻译：某些新的N-酰化的螺哌啶衍生物是人黑皮质素受体的配体，特别是人黑皮质素-4受体（MC-4R）的选择性配体。因此它们可用于治疗，控制或预防对调节MC-4R有响应的疾病和病症，例如肥胖症，糖尿病，尼古丁成瘾，酒精中毒，性功能障碍，包括勃起功能障碍和女性性功能障碍。

98. 发明申请

WO2006094602A1 INDANE 审中-公开
标题翻译：二氢化茚
公开(公告)号：WO2006094602A1
公开(公告)日：2006-09-14
申请号：PCT/EP2006/001283
申请日：2006-02-13
申请人： MERCK PATENT GMBH , FINSINGER, Dirk , BRUGE, David , BUCHSTALLER, Hans-Peter , EMDE, Ulrich , SCHIEMANN, Kai , STAEHLE, Wolfgang , AMENDT, Christiane , HEISS, Nina , ZENKE, Frank
发明人： FINSINGER, Dirk , BRUGE, David , BUCHSTALLER, Hans-Peter , EMDE, Ulrich , SCHIEMANN, Kai , STAEHLE, Wolfgang , AMENDT, Christiane , HEISS, Nina , ZENKE, Frank
IPC分类号： C07C211/42 , C07C211/30 , C07C49/67 , C07D211/70 , C07D263/04 , C07D239/04 , C07D239/06 , C07D211/96
CPC分类号： C07D405/08 , C07C45/46 , C07C49/67 , C07C49/747 , C07C49/755 , C07C225/22 , C07C255/56 , C07D211/14 , C07D211/70 , C07D221/16 , C07D295/03
摘要： Verbindungen der Formel (I) worin R 1 , R 2 , R 3 , R 4 , und q die in Anspruch 1 angegebenen Bedeutungen haben, können u.a. zur Behandlung von Tumoren eingesetzt werden.
摘要翻译：式（I）化合物，其中R ^{1 ，R ^{2 ，R ^{3 ，R ^{4 和q 具有权利要求1中给出的含义，可以特别用于肿瘤的治疗。}}}}

99. 发明申请

WO02051831A1 OXYBENZAMIDES DERIVATIVES AS FACTOR XA INHIBITORS 审中-公开
标题翻译： OXYBENZAMIDES衍生物作为因子XA抑制剂
公开(公告)号：WO02051831A1
公开(公告)日：2002-07-04
申请号：PCT/EP2001/014842
申请日：2001-12-15
IPC分类号： C07D243/08 , A61K31/166 , A61K31/167 , A61K31/18 , A61K31/277 , A61K31/38 , A61K31/4184 , A61K31/422 , A61K31/435 , A61K31/4355 , A61K31/437 , A61K31/44 , A61K31/4418 , A61K31/4439 , A61K31/445 , A61K31/4453 , A61K31/4465 , A61K31/4468 , A61K31/451 , A61K31/4525 , A61K31/453 , A61K31/4535 , A61K31/454 , A61K31/4545 , A61K31/4709 , A61K31/495 , A61K31/496 , A61K31/4965 , A61K31/497 , A61K31/505 , A61K31/506 , A61K31/551 , A61K31/635 , A61P7/00 , A61P7/02 , A61P7/04 , A61P9/00 , A61P9/08 , A61P9/10 , A61P11/00 , A61P29/00 , A61P43/00 , C07C235/50 , C07C237/42 , C07C255/60 , C07C311/46 , C07C311/51 , C07D211/26 , C07D211/58 , C07D211/96 , C07D213/30 , C07D213/38 , C07D213/40 , C07D213/64 , C07D213/74 , C07D213/89 , C07D235/06 , C07D235/08 , C07D239/42 , C07D239/69 , C07D241/12 , C07D295/12 , C07D295/13 , C07D295/18 , C07D295/192 , C07D317/58 , C07D333/16 , C07D333/58 , C07D401/00 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D405/04 , C07D405/08 , C07D405/12 , C07D405/14 , C07D409/12 , C07D409/14 , C07D413/04 , C07D413/14 , C07D417/14 , C07D471/04 , C07D491/04 , C07D491/048
CPC分类号： C07D213/40 , C07C235/50 , C07C311/46 , C07C2601/14 , C07D211/26 , C07D211/58 , C07D211/96 , C07D213/38 , C07D213/74 , C07D213/89 , C07D235/06 , C07D239/42 , C07D295/13 , C07D295/192 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D405/04 , C07D405/08 , C07D409/12 , C07D409/14 , C07D413/04 , C07D413/14 , C07D471/04 , C07D491/04
摘要： The present invention relates to compounds of the formula I, R -Q-X-Q'-W-U-V-G-M (I) in which R0; Q; X; Q'; W; U, V, G and M have the meanings indicated in the claims. The compounds of the formula I are valuable pharmacologically active compounds. They exhibit a strong antithrombotic effect and are suitable, for example, for the therapy and prophylaxis of cardiovascular disorders like thromboembolic diseases or restenoses. They are reversible inhibitors of the blood clotting enzymes factor Xa (Fxa) and/or factor VIIa (FVIIa), and can in general be applied in conditions in which an undesired activity of factor Xa and/or factor VIIa is present or for the cure or prevention of which an inhibition of factor Xa and/or factor VIIa is intended. The invention furthermore relates to processes for the preparation of compounds of the formula I, their use, in particular as active ingredients in pharmaceuticals, and pharmaceutical preparations comprising them.
摘要翻译：本发明涉及式I化合物，R 0 -Q-X-Q'-W-U-V-G-M（I），其中R 0; Q; X; Q'; 瓦; U，V，G和M具有权利要求中所示的含义。式I的化合物是有价值的药理活性化合物。它们具有强烈的抗血栓形成作用，并且适用于例如治疗和预防心血管疾病如血栓栓塞性疾病或再狭窄。它们是血液凝固酶因子Xa（Fxa）和/或因子VIIa（FVIIa）的可逆抑制剂，并且通常可用于存在因子Xa和/或因子VIIa的不期望活性或用于治愈或预防因子Xa和/或因子VIIa的抑制。本发明还涉及制备式I化合物的方法，其用途，特别是作为药物中的活性成分，以及包含它们的药物制剂。

100. 发明申请

WO1995000489A1 ISOQUINOLINE DERIVATIVES AS THERAPEUTIC AGENTS 审中-公开
标题翻译：作为治疗剂的异喹啉衍生物
公开(公告)号：WO1995000489A1
公开(公告)日：1995-01-05
申请号：PCT/EP1994001926
申请日：1994-06-10
申请人： THE BOOTS COMPANY PLC , SARGENT, Bruce, Jeremy , JOHNSTON, David, Norman , CREW, Andrew, Philip, Austin
发明人： THE BOOTS COMPANY PLC
IPC分类号： C07D217/04
CPC分类号： C07D401/08 , C07D217/04 , C07D405/08 , C07D409/08
摘要： Tetrahydroisoquinoline compounds of formula (I) and pharmaceutically acceptable salts thereof, in which: R1 represents one or more substituents selected from H, halo, hydroxy, alkyl (optionally substituted by hydroxy), alkoxy, alkylthio, alkylsulphinyl, alkyl-sulphonyl, nitro, cyano, polyhaloalkyl, polyhaloalkoxy, phenyl (optionally substituted by one or more of halo, alkyl or alkoxy), or R1 is optionally alkylated carbamoyl; R2 represents a saturated or unsaturated aliphatic group optionally substituted by hydroxy or alkoxy; E represents an alkylene chain optionally substituted by one or more alkyl groups; and G represents (a) optionally substituted saturated or unsaturated alicyclic group containing 3 to 8 carbon atoms, or (b) optionally substituted saturated or unsaturated aliphatic chain containing 1 to 12 carbon atoms, or (c) optionally substituted 5 or 6 membered heterocyclic ring containing one or more N or O atoms or SOn groups in which n is 0, 1 or 2; and O &cir& _-acylated derivatives thereof which provide lipophilic esters have utility in analgesia or in the treatment of psychoses (e.g. schizophrenia), Parkinson's desease, Lesch-Nyan syndrome, attention deficit disorder or cognitive impairment or in the relief of drug dependence or tardive dyskynesia.
摘要翻译：式（I）的四氢异喹啉化合物及其药学上可接受的盐，其中：R1表示一个或多个选自H，卤素，羟基，烷基（任选被羟基取代），烷氧基，烷硫基，烷基亚磺酰基，烷基磺酰基，硝基，氰基，多卤代烷基，多卤代烷氧基，苯基（任选被卤素，烷基或烷氧基中的一个或多个取代），或R 1任选被烷基化的氨基甲酰基; R2表示任选被羟基或烷氧基取代的饱和或不饱和脂族基; E表示任选被一个或多个烷基取代的亚烷基链; G表示（a）含有3〜8个碳原子的任选取代的饱和或不饱和脂环基，或（b）任选取代的含有1至12个碳原子的饱和或不饱和脂族链，或（c）任选取代的5或6元杂环含有一个或多个N或O原子或其中n为0,1或2的SO n基团; 和其提供亲脂性酯的O＆Cir＆_酰化衍生物可用于镇痛或治疗精神病（例如精神分裂症），帕金森氏症，莱斯奈恩综合征，注意力缺陷障碍或认知障碍或缓解药物依赖或迟缓 dyskynesia。

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