公开(公告)号：US08415347B2

公开(公告)日：2013-04-09

申请号：US12850958

申请日：2010-08-05

Applicant: José Maria Cid-Núñez ,  Antonius Adrianus Hendrikus Petrus Megens ,  Andrés Avelino Trabanco-Suárez ,  Mohamed Koukni ,  Georges Joseph Cornelius Hoornaert ,  Frans Josef Cornelius Compernolle ,  Tomasz Kozlecki ,  Hua Mao ,  Sushil Chandra Jha ,  Francisco Javier Fernández-Gadea

Inventor： José Maria Cid-Núñez ,  Antonius Adrianus Hendrikus Petrus Megens ,  Andrés Avelino Trabanco-Suárez ,  Mohamed Koukni ,  Georges Joseph Cornelius Hoornaert ,  Frans Josef Cornelius Compernolle ,  Tomasz Kozlecki ,  Hua Mao ,  Sushil Chandra Jha ,  Francisco Javier Fernández-Gadea

IPC: A61K31/5377 ,  A61K31/403 ,  A61K31/496 ,  A61K31/381 ,  A61K31/4985 ,  A61K31/352 ,  A61K31/435 ,  C07D491/044 ,  C07D209/58 ,  C07D413/04 ,  C07D333/80 ,  C07D487/04

CPC classification number: C07D333/80 ,  C07D209/70 ,  C07D221/18 ,  C07D307/93 ,  C07D311/94 ,  C07D487/04 ,  C07D491/04

Abstract: This invention concerns novel substituted tetracyclic tetrahydrofuran, pyrrolidine and tetrahydrothiophene derivatives with binding affinities towards serotonin receptors, in particular 5-HT2A and 5-HT2C receptors, and towards dopamine receptors, in particular dopamine D2 receptors and with norepinephrine reuptake inhibition properties, pharmaceutical compositions comprising the compounds according to the invention, the use thereof as a medicine, in particular for the prevention and/or treatment of a range of psychiatric and neurological disorders, in particular certain psychotic, cardiovascular and gastrokinetic disorders and processes for their production.The compounds according to the invention can be represented by general Formula (I) and comprises also the pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric forms thereof, the N-oxide form thereof and prodrugs thereof, wherein all substituents are defined as in Claim 1.

Abstract translation: 本发明涉及对5-羟色胺受体，特别是5-HT2A和5-HT2C受体以及对多巴胺受体，特别是多巴胺D2受体和去甲肾上腺素再摄取抑制性质具有结合亲和力的新型取代四环四氢呋喃，吡咯烷和四氢噻吩衍生物，包含 根据本发明的化合物，其用作药物，特别是用于预防和/或治疗一系列精神和神经障碍，特别是某些精神病性，心血管和胃肠功能障碍及其生产方法。 根据本发明的化合物可以由通式（I）表示，并且还包括其药学上可接受的酸或碱加成盐，其立体化学异构形式，其N-氧化物形式及其前药，其中所有取代基定义为 在权利要求1中。

公开(公告)号：US20120295318A1

公开(公告)日：2012-11-22

申请号：US13567509

申请日：2012-08-06

Applicant: VLADIMIR V. POPIK ,  Andrei A. Poloukhtine ,  Geert-Jan Boons ,  Margaretha Wolfert

Inventor： VLADIMIR V. POPIK ,  Andrei A. Poloukhtine ,  Geert-Jan Boons ,  Margaretha Wolfert

IPC: C07C49/665 ,  C12P7/26 ,  B01J19/12 ,  C07D495/04 ,  C07D313/20 ,  C07D491/044 ,  C12N11/02 ,  C07D249/16

CPC classification number: C07D249/16 ,  C07C41/18 ,  C07C43/215 ,  C07C43/23 ,  C07C49/753 ,  C07C2603/36 ,  C07D495/04

Abstract: Cyclic alkynes (e.g., cyclooctynes such as dibenzocyclooctynes) can be photochemically generated from cyclopropenones as disclosed herein. The cyclic alkynes can be reacted (e.g., in situ) with materials having alkyne-reactive groups (e.g., azide groups in a “click” reaction). In preferred embodiments, the generation and reaction of the cyclic alkyne can proceed in the absence of a catalyst (e.g., Cu(I)). These reactions can be useful, for example, for the selective labeling of living cells that are metabolically modified with azido-containing surface monosaccharides, or for light-directed surface patterning.

Abstract translation: 环烷烃（例如环辛烯如二苯并环辛烯）可由本文公开的环丙烯酮光化学产生。 环状炔可以与具有炔反应性基团的物质（例如原位）反应（例如，在咔哒反应中为叠氮基）。 在优选的实施方案中，环状炔的生成和反应可以在不存在催化剂（例如Cu（I））的情况下进行。 这些反应可用于例如用含叠氮基表面单糖代谢修饰的活细胞的选择性标记，或用于光定向表面图案化。

公开(公告)号：US20120251491A1

公开(公告)日：2012-10-04

申请号：US13320427

申请日：2010-05-12

Applicant: Stuart B. Rosenblum ,  Kevin X. Chen ,  Joseph A. Kozlowski ,  F. George Njoroge ,  Craig A. Coburn

Inventor： Stuart B. Rosenblum ,  Kevin X. Chen ,  Joseph A. Kozlowski ,  F. George Njoroge ,  Craig A. Coburn

IPC: A61K31/4178 ,  C07D487/04 ,  C07D493/04 ,  A61K31/4184 ,  A61K31/4188 ,  C07D471/04 ,  A61K31/4745 ,  C07D491/044 ,  A61K31/55 ,  C07D401/14 ,  A61K31/473 ,  A61K31/498 ,  A61K38/21 ,  A61K31/7088 ,  A61K39/12 ,  A61K39/395 ,  A61K31/7056 ,  A61P31/14 ,  A61P37/04 ,  A61P31/12 ,  C07D403/14

CPC classification number: C07D403/14 ,  C07C403/04 ,  C07D403/04 ,  C07D471/04 ,  C07D487/04 ,  C07D491/044 ,  C07D493/04

Abstract: The present invention relates to novel Fused Tricyclic Aryl Compounds, compositions comprising at least one Fused Tricyclic Aryl Compound, and methods of using the Fused Tricyclic Aryl Compounds for treating or preventing HCV infection in a patient.

Abstract translation: 本发明涉及新的熔融三环芳基化合物，包含至少一种稠合三环芳基化合物的组合物，以及使用稠合三环芳基化合物治疗或预防患者HCV感染的方法。

公开(公告)号：US20120178941A1

公开(公告)日：2012-07-12

申请号：US13401238

申请日：2012-02-21

Applicant: Luca Parlanti ,  Jurong Yu

Inventor： Luca Parlanti ,  Jurong Yu

IPC: C07D491/044

CPC classification number: C07D417/06 ,  A61K47/551 ,  A61K47/65 ,  C07D491/044 ,  C07D493/04 ,  C07K5/1021

Abstract: A process for making aziridinyl epothilone compounds according to formula G, starting from a compound according formula C where R1, R2, R3, R4, R5, R6, R12, R13, Z1 and Z2 in formulae (G) and (C) are as defined herein. The aziridinyl epothilone compounds of formula (G) are useful for the treatment of cancer.

Abstract translation: 式（G）和（C）中R 1，R 2，R 3，R 4，R 5，R 6，R 12，R 13，Z 1和Z 2的化合物为式 本文定义。 式（G）的氮丙啶基埃坡霉素化合物可用于治疗癌症。

公开(公告)号：US20120035227A1

公开(公告)日：2012-02-09

申请号：US13020245

申请日：2011-02-03

Applicant: Anthony W. Czarnik

Inventor： Anthony W. Czarnik

IPC: C07D491/044 ,  A61P35/04 ,  A61K31/427

CPC classification number: C07D491/044

Abstract: The present application describes deuterium-enriched ixabepilone, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.

Abstract translation: 本申请描述了氘富集的伊沙匹隆，其药学上可接受的盐形式，以及使用其的治疗方法。

公开(公告)号：US20100273791A1

公开(公告)日：2010-10-28

申请号：US12769861

申请日：2010-04-29

Applicant: Braj Bhushan LOHRAY ,  Vidya Bhushan Lohray ,  Brijesh Srivastava

Inventor： Braj Bhushan LOHRAY ,  Vidya Bhushan Lohray ,  Brijesh Srivastava

IPC: A61K31/416 ,  C07D231/54 ,  C07D491/044 ,  C07D495/04 ,  A61K31/454 ,  A61K31/4162 ,  A61K31/5377 ,  A61K31/496 ,  C07C69/738 ,  C07D313/08 ,  C07D337/08

CPC classification number: C07D495/14 ,  C07D495/04

Abstract: The present invention relates to novel compounds of general formula (I), their regioisomers, tautomeric forms, novel intermediates involved in their synthesis. The present invention also relates to a process of preparing compounds of general formula (I), their regioisomers, their tautomeric forms, their pharmaceutically acceptable salts, pharmaceutical compositions containing them, and novel intermediates involved in their synthesis.

Abstract translation: 本发明涉及通式（I）的新型化合物，其区域异构体，互变异构体，涉及其合成的新型中间体。 本发明还涉及制备通式（I）的化合物，其区域异构体，其互变异构形式，其药学上可接受的盐，含有它们的药物组合物以及参与其合成的新中间体的方法。

公开(公告)号：US07732459B2

公开(公告)日：2010-06-08

申请号：US11900744

申请日：2007-09-13

Applicant: Kenneth G. Carson ,  Geraldine C. B. Harriman ,  Shomir Ghosh

Inventor： Kenneth G. Carson ,  Geraldine C. B. Harriman ,  Shomir Ghosh

IPC: A61K31/4353 ,  A61P29/00 ,  C07D491/044 ,  A61P19/02 ,  A61P9/10

CPC classification number: C07D491/044 ,  C07D491/04

Abstract: The invention provides compounds having the formula: wherein R1 is halogen. The invention also provides compositions comprising the compounds, and methods of treating diseases or disorders that comprise administering one or more of the compounds to a subject in need thereof. The disclosed compounds have CCR1 antagonist activity.

Abstract translation: 本发明提供具有下式的化合物：其中R1是卤素。 本发明还提供包含该化合物的组合物，以及治疗疾病或病症的方法，其包括向有需要的受试者施用一种或多种化合物。 所公开的化合物具有CCR1拮抗剂活性。

公开(公告)号：US20090318529A1

公开(公告)日：2009-12-24

申请号：US10561711

申请日：2004-06-18

Applicant: William H. Fenical ,  Paul R. Jensen ,  Tracy J. Mincer ,  Robert H.R. Feling

Inventor： William H. Fenical ,  Paul R. Jensen ,  Tracy J. Mincer ,  Robert H.R. Feling

IPC: A61K31/407 ,  C07D491/044

CPC classification number: C07D491/044 ,  A61K31/407 ,  C07D491/04 ,  C12P17/188

Abstract: The present invention is based on the discovery that certain fermentation products of the marine actinomycete strains CNB392 and CNB476 are effective inhibitors of hyperproliferative mammalian cells. The CNB392 and CNB476 strains lie within the family Micromonosporaceae, and the generic epithet Salinospora has been proposed for this obligate marine group. The reaction products produced by this strain are classified as salinosporamides, and are particularly advantageous in treating neoplastic disorders due to their low molecular weight, low IC50 values, high pharmaceutical potency, and selectivity for cancer cells over fungi.

Abstract translation: 本发明基于以下发现：海洋放线菌株CNB392和CNB476的某些发酵产物是过度增殖哺乳动物细胞的有效抑制剂。 CNB392和CNB476菌株位于Micromonosporaceae中，并且为该专业海洋群体提出了通用表型Salinospora。 由该菌株产生的反应产物分类为salinosporamide，并且由于其低分子量，低​​IC 50值，高药物效力和对真菌的癌细胞的选择性而特别有利于治疗肿瘤性疾病。

公开(公告)号：US07635712B2

公开(公告)日：2009-12-22

申请号：US11705694

申请日：2007-02-12

Applicant: William Fenical ,  Paul Jensen ,  Tracy Mincer ,  Robert H. R. Feling

Inventor： William Fenical ,  Paul Jensen ,  Tracy Mincer ,  Robert H. R. Feling

IPC: A61K31/407 ,  A61P35/00 ,  C07D491/044

CPC classification number: A61K31/407 ,  A61K31/397 ,  A61K31/424 ,  A61K31/43 ,  A61K45/06 ,  C07D491/04 ,  C07D491/044 ,  C12P17/18 ,  C12P17/188

Abstract: The present invention is based on the discovery that certain fermentation products of the marine actinomycete strains CNB392 and CNB476 are effective inhibitors of hyperproliferative mammalian cells. The CNB392 and CNB476 strains lie within the family Micromonosporaceae, and the generic epithet Salinospora has been proposed for this obligate marine group. The reaction products produced by this strain are classified as salinosporamides, and are particularly advantageous in treating neoplastic disorders due to their low molecular weight, low IC50 values, high pharmaceutical potency, and selectivity for cancer cells over fungi.

Abstract translation: 本发明基于以下发现：海洋放线菌株CNB392和CNB476的某些发酵产物是过度增殖哺乳动物细胞的有效抑制剂。 CNB392和CNB476菌株位于Micromonosporaceae中，并且为该专业海洋群体提出了通用表型Salinospora。 由该菌株产生的反应产物分类为salinosporamide，并且由于其低分子量，低​​IC 50值，高药物效力和对真菌的癌细胞的选择性而特别有利于治疗肿瘤性疾病。

公开(公告)号：US20090298906A1

公开(公告)日：2009-12-03

申请号：US12464686

申请日：2009-05-12

Applicant: Venkat Rami Reddy Macherla ,  Barbara Christine Potts ,  Rama Rao Manam ,  Katherine A. McArthur ,  Ta-Hsiang Chao ,  Saskia Theodora Cornelia Neuteboom

Inventor： Venkat Rami Reddy Macherla ,  Barbara Christine Potts ,  Rama Rao Manam ,  Katherine A. McArthur ,  Ta-Hsiang Chao ,  Saskia Theodora Cornelia Neuteboom

IPC: A61K31/407 ,  C07D491/044 ,  A61P35/00

CPC classification number: C07D491/04

Abstract: Disclosed herein are compounds of Formula (I) that include a sulfonate ester, ester or ether group. Compounds of Formula (I) can be included in pharmaceutical compositions, and can be used to treating and/or ameliorating a disease or condition, such as cancer, a microbial disease and/or inflammation.

Abstract translation: 本文公开了包含磺酸酯，酯或醚基团的式（I）化合物。 式（I）的化合物可以包括在药物组合物中，并且可以用于治疗和/或改善疾病或病症，例如癌症，微生物疾病和/或炎症。