公开(公告)号：WO2012047926A2

公开(公告)日：2012-04-12

申请号：PCT/US2011/054812

申请日：2011-10-04

Applicant: THE BRIGHAM AND WOMEN'S HOSPITAL, INC. ,  AUGELLI-SZAFRAN, Corinne E. ,  LU, Dai ,  WEI, HanXun ,  ZHANG, Jing ,  WOLFE, Michael S. ,  SELKOE, Dennis J.

Inventor： AUGELLI-SZAFRAN, Corinne E. ,  LU, Dai ,  WEI, HanXun ,  ZHANG, Jing ,  WOLFE, Michael S. ,  SELKOE, Dennis J.

IPC: C07C311/19 ,  C07C311/41 ,  A61K31/18 ,  A61K31/195 ,  A61P25/28

CPC classification number: C07C311/16 ,  C07C311/17 ,  C07C311/18 ,  C07C311/19 ,  C07C311/29 ,  C07C317/28 ,  C07C317/32 ,  C07C323/42 ,  C07C2601/14 ,  C07D213/42 ,  C07D213/71 ,  C07D263/14 ,  C07D271/06 ,  C07D295/32 ,  C07D333/34

Abstract: This invention relates generally to the discovery of sulfonamide-containing compounds that are inhibitors of ϒ-secretase.

Abstract translation: 本发明一般涉及作为γ-分泌酶抑制剂的含磺酰胺化合物的发现。

公开(公告)号：WO2011126733A3

公开(公告)日：2012-04-05

申请号：PCT/US2011029467

申请日：2011-03-22

Applicant: CHILDRENS MEDICAL CENTER ,  JENSEN FRANCES E

Inventor： JENSEN FRANCES E

IPC: A61K31/197 ,  A61K31/18 ,  A61K31/195 ,  A61K31/341 ,  A61P35/00

CPC classification number: A61K31/197 ,  A61K31/44 ,  A61K31/635 ,  A61K45/06 ,  A61K2300/00

Abstract: Inhibitors of NKCCl, such as bumetanide, when coadministered with inhibitors of GABA transaminase, such as vigabatrin, attenuate both the retinal toxicity and the intramyelinic edema.

Abstract translation: 当联合给予GABA转氨酶抑制剂（例如促血清素）时，NKCCl的抑制剂，例如布美他赛，减弱了视网膜毒性和肉瘤内水肿。

公开(公告)号：WO2012021963A1

公开(公告)日：2012-02-23

申请号：PCT/CA2011/000727

申请日：2011-06-22

Applicant: METASIGNAL THERAPEUTICS INC. ,  SUPURAN, Claudiu ,  DEDHAR, Shoukat ,  MCDONALD, Paul, C. ,  CARTA, Fabrizio

Inventor： SUPURAN, Claudiu ,  DEDHAR, Shoukat ,  MCDONALD, Paul, C. ,  CARTA, Fabrizio

IPC: C07C311/47 ,  A61K31/18 ,  A61K31/63 ,  A61P35/00

CPC classification number: A61K31/63 ,  A61K31/18 ,  A61K31/277 ,  A61K45/06 ,  C07C311/47 ,  C07C2601/08 ,  C07C2602/08 ,  C07C2603/18 ,  A61K2300/00

Abstract: Therapeutic sulfonamide compounds with the formula R-Q-Ar-SO 2 NH 2 are disclosed, wherein R is an aryl, hetaryl, alkyl or cycloalkyl group, Q is the group -L(CH 2 ) n -, wherein n = 0,1 or 2 and L is the group - NHCXNH-, -NHC(S)SNH-, -NHCONHCSNH- or -SO 2 NH-, X is O or S and Ar is a C 6 -C 10 aromatic or a heteroaromatic group that contains at least one heteroatom of oxygen, nitrogen or sulphur, which compounds selectively inhibit CAIX and CAXII, and which are effective in inhibiting hypoxic tumor growth, suppress metastases, and impair and deplete cancer stem cells in mammals.

Abstract translation: 公开了具有式RQ-Ar-SO2NH2的治疗磺酰胺化合物，其中R是芳基，杂芳基，烷基或环烷基，Q是基团-L（CH 2）n - ，其中n = 0,1或2，L是 基团-NHCXNH-，-NHC（S）SNH-，-NHCONHCSNH-或-SO2NH-，X是O或S，Ar是包含至少一个氧，氮或杂原子的C 6 -C 10芳族或杂芳族基团 硫化合物，其选择性地抑制CAIX和CAXII，并且其有效抑制缺氧性肿瘤生长，抑制转移，并损害和消耗哺乳动物中的癌症干细胞。

公开(公告)号：WO2012018868A1

公开(公告)日：2012-02-09

申请号：PCT/US2011/046340

申请日：2011-08-02

Applicant: UNIVERSITY OF CENTRAL FLORIDA RESEARCH FOUNDATION, INC. ,  UNIVERSITY OF TORONTO MISSISSAUGA ,  TURKSON, James ,  GUNNING, Patrick

Inventor： TURKSON, James ,  GUNNING, Patrick

IPC: A61K31/18

CPC classification number: C07D401/04 ,  A61K31/18 ,  C07C311/19 ,  C07C311/29 ,  C07C311/42 ,  C07C311/46 ,  C07C323/49 ,  C07C2601/14 ,  C07D207/48 ,  C07D211/26 ,  C07D211/34 ,  C07D211/60 ,  C07D211/96 ,  C07D213/42 ,  C07D215/36 ,  C07D233/84

Abstract: In one aspect, the invention relates to substituted substituted 2-hydroxy-4-(2- (phenylsulfonamido)acetamido)benzoic acid analogs, derivatives thereof, and related compounds, which are useful as inhibitors of STAT protein activity; synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating disorders of uncontrolled cellular proliferation associated with a STAT protein activity dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.

Abstract translation: 一方面，本发明涉及可用作STAT蛋白活性抑制剂的取代的取代的2-羟基-4-（2-（苯基亚磺酰氨基）乙酰氨基）苯甲酸类似物及其衍生物及相关化合物， 制备化合物的合成方法; 包含该化合物的药物组合物; 以及使用所述化合物和组合物治疗与STAT蛋白活性功能障碍相关的不受控制的细胞增殖紊乱的方法。 该摘要旨在作为用于在特定技术中进行搜索的扫描工具，而不意在限制本发明。

公开(公告)号：WO2012018635A2

公开(公告)日：2012-02-09

申请号：PCT/US2011/045390

申请日：2011-07-26

Applicant: NEUROTHERAPEUTICS PHARMA, INC. ,  WANASKI, Stephen ,  COLLINS, Stephen ,  KINCAID, John

Inventor： WANASKI, Stephen ,  COLLINS, Stephen ,  KINCAID, John

IPC: C07C311/39 ,  A61K31/18 ,  A61P25/28 ,  A61P25/16

CPC classification number: C07C311/40 ,  C07C311/39 ,  C07C311/51 ,  C07C327/48 ,  C07C2601/02 ,  C07D205/04 ,  C07D209/08 ,  C07D213/38 ,  C07D213/75 ,  C07D249/14 ,  C07D261/14 ,  C07D295/088 ,  C07D295/13 ,  C07D295/135 ,  C07D295/155 ,  C07D295/192 ,  C07D295/26 ,  C07D317/64 ,  C07D403/12 ,  C07D413/12

Abstract: The present invention provides acylsulfonamides including bumetanide derivatives and compositions comprising such analogs. The present invention also provides pharmaceutical compositions containing these compounds and methods for their use. All of these analogs are particularly useful for the treatment and/or prophylaxis of conditions that involve the Na+K+Cl- co-transporter or GABAA receptor including but not limited to addictive disorders, Alzheimer's Disease, anxiety disorders, ascites, attention deficit hyperactivity disorder (ADHD), autism spectrum disorders (autism), bipolar disorder, cancer, the improvement of cognitive function, cognitive impairment, cognitive dysfunction, depression, endothelial corneal dystrophy, edema, epilepsy, glaucoma, Huntington's Disease, inflammatory pain, insomnia, ischemia, migraine, migraine with aura, migraine without aura, neuropathic pain, nociceptive neuralgia, nociceptive pain, ocular diseases, pain, Parkinson's disease, periodic limb movement disorder (PLMD), personality disorders, postherpetic neuralgia, psychosis, restless legs syndrome (RLS), schizophrenia, seizure disorders, spasticity, tinnitus, and withdrawal syndromes.

Abstract translation: 本发明提供酰基磺酰胺，包括布美他尼衍生物和包含此类类似物的组合物。 本发明还提供含有这些化合物的药物组合物及其使用方法。 所有这些类似物对于治疗和/或预防涉及Na + K + Cl-共转运蛋白或GABA A受体的病症特别有用，包​​括但不限于成瘾性疾病，阿尔茨海默病，焦虑症，腹水，注意缺陷多动症 障碍（ADHD），自闭症谱系障碍（自闭症），双相情感障碍，癌症，认知功能改善，认知功能障碍，认知功能障碍，抑郁症，内皮角膜营养不良，水肿，癫痫，青光眼，亨廷顿病，炎性疼痛，失眠， ，偏头痛，偏头痛，无光晕偏头痛，神经性疼痛，伤害性感觉神经痛，伤害性疼痛，眼部疾病，疼痛，帕金森病，周期性肢体运动障碍（PLMD），人格障碍，带状疱疹后神经痛，精神病，不宁腿综合征（RLS） ，精神分裂症，癫痫发作障碍，痉挛状态，耳鸣和戒断综合征。

公开(公告)号：WO2011091319A3

公开(公告)日：2011-11-17

申请号：PCT/US2011022147

申请日：2011-01-21

Applicant: BAYLOR RES INST ,  BANCHEREAU JACQUES F ,  MONTES MONICA ,  PALUCKA ANNA KAROLINA ,  SLOAN LOUIS M ,  LEVY YVES ,  AGENCE NATIONALE DE RECH S SUR LE SIDA ET LES HEPATITIS VIRALES

Inventor： BANCHEREAU JACQUES F ,  MONTES MONICA ,  PALUCKA ANNA KAROLINA ,  SLOAN LOUIS M ,  LEVY YVES

IPC: A61K39/12 ,  A61K31/18 ,  A61K38/04 ,  A61K38/16 ,  A61K39/21 ,  A61P31/18 ,  C12N5/0784

CPC classification number: C12N5/0639 ,  A61K39/12 ,  A61K39/21 ,  A61K2039/5154 ,  A61K2039/545 ,  A61K2039/6018 ,  C07K14/005 ,  C12N2501/052 ,  C12N2501/22 ,  C12N2501/24 ,  C12N2740/16222 ,  C12N2740/16234 ,  C12N2740/16322 ,  C12N2740/16334

Abstract: Compositions and methods for the prophylaxis and treatment of human immunodeficiency virus (HIV) infections are disclosed herein. More specifically the present invention discloses describes an autologous dendritic cell (DC) vaccine product derived by culturing a patient's monocytes with granulocyte macrophage colony stimulating factor (GM-CSF) and interferon alpha 2b (IFN-a), loading the DC with a mixture of five lipopeptides of Gag, Nef and Pol HIV antigens, and, optionally activating the DC with lipopolysaccharide (LPS).

Abstract translation: 本文公开了预防和治疗人类免疫缺陷病毒（HIV）感染的组合物和方法。 更具体地，本发明公开了一种通过用粒细胞巨噬细胞集落刺激因子（GM-CSF）和干扰素α2b（IFN-α）培养患者的单核细胞衍生的自体树突状细胞（DC）疫苗产品， 5种Gag，Nef和Pol HIV抗原的脂肽，以及任选地用脂多糖（LPS）活化DC。

公开(公告)号：WO2011043519A3

公开(公告)日：2011-10-20

申请号：PCT/KR2010001633

申请日：2010-03-17

Applicant: KOREA INST SCI & TECH ,  PAE AE NIM ,  CHOO HYUNAH ,  CHO YONG SEO ,  JUN SUN AH ,  CHO HYE JIN ,  PARK WOO KYU ,  KIM JEONG MIN

Inventor： PAE AE NIM ,  CHOO HYUNAH ,  CHO YONG SEO ,  JUN SUN AH ,  CHO HYE JIN ,  PARK WOO KYU ,  KIM JEONG MIN

IPC: C07C311/16 ,  A61K31/18 ,  C07C303/38

CPC classification number: C07C311/18 ,  C07C2601/08 ,  C07D207/09 ,  C07D207/14 ,  C07D211/14 ,  C07D295/13 ,  C07D409/12

Abstract: The present invention relates to sulfonamide derivatives as a serotonin receptor antagonist and serotonin reuptake inhibitor and a pharmaceutically acceptable salt thereof. The sulfonamide derivatives have serotonin 5-HT2A and 5-HT2C receptor antagonizing and serotonin reuptake inhibiting functions, and thus may be efficiently applied to a CNS-related disease such as depression, obesity, psychosis, schizophrenia, suicidal tendency, anxiety, obsessional neurosis, migraine, appetite disorders, sleep disorders, stroke, and withdrawal symptoms caused by drug abuse.

Abstract translation: 本发明涉及作为5-羟色胺受体拮抗剂和5-羟色胺再摄取抑制剂及其可药用盐的磺酰胺衍生物。 磺酰胺衍生物具有5-羟色胺5-HT2A和5-HT2C受体拮抗和5-羟色胺再摄取抑制功能，因此可以有效地应用于CNS相关疾病如抑郁症，肥胖症，精神病，精神分裂症，自杀倾向，焦虑症，强迫症神经症， 偏头痛，食欲障碍，睡眠障碍，中风和药物滥用引起的戒断症状。

公开(公告)号：WO2011112858A1

公开(公告)日：2011-09-15

申请号：PCT/US2011/027974

申请日：2011-03-10

Applicant: NORTH CAROLINA CENTRAL UNIVERSITY ,  THE UNIVERSITY OF NORTH CAROLINA AT CHAPEL HILL ,  WILLIAMS, Alfred L. ,  SCOTT, John ,  YEH, Li-An ,  REDINBO, Matthew

Inventor： WILLIAMS, Alfred L. ,  SCOTT, John ,  YEH, Li-An ,  REDINBO, Matthew

IPC: A01N41/06 ,  A61K31/18

CPC classification number: C07D333/34 ,  A61K31/137 ,  A61K31/42 ,  A61K31/4409 ,  A61K31/4709 ,  A61K31/553 ,  C07D295/135 ,  C07D409/06 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12 ,  C12Q1/34 ,  G01N2333/924 ,  G01N2500/02

Abstract: This invention relates generally to compounds that are glucuronidase inhibitors. Glucuronidase inhibitors described include phenoxy thiophene sulfonamides. Other compounds, for instance pyridine sulfonyls, benzene sulfonyls, thiophene sulfonyls, thiazole sulfonyls, thiophene carbonyls, and thiazole carbonyls, are also contemplated. Also contemplated are compositions including one or more of such compounds for use inhibiting glucuronidase and methods of using one or more of such compounds as a co-drug to be used in combination with the anticancer drug CPT-11.

Abstract translation: 本发明一般涉及葡糖苷酸酶抑制剂的化合物。 所述的葡糖苷酸酶抑制剂包括苯氧基噻吩磺酰胺。 也考虑其它化合物，例如吡啶磺酰基，苯磺酰基，噻吩磺酰基，噻唑磺酰基，噻吩羰基和噻唑羰基。 还考虑了包含一种或多种这样的用于抑制葡糖醛酸糖苷酶的化合物的组合物和使用一种或多种这样的化合物作为与抗癌药物CPT-11组合使用的共同药物的方法。

公开(公告)号：WO2011112623A1

公开(公告)日：2011-09-15

申请号：PCT/US2011/027606

申请日：2011-03-08

Applicant: SPECTRUM PHARMACEUTICALS, INC. ,  NAWROCKI, Steffan, T. ,  CAREW, Jennifer, S, ,  REDDY, Guru

Inventor： NAWROCKI, Steffan, T. ,  CAREW, Jennifer, S, ,  REDDY, Guru

IPC: A61K31/00 ,  A61K31/382 ,  A61K31/7004 ,  A61K33/36 ,  A61K31/138 ,  A61K31/165 ,  A61K31/166 ,  A61K31/167 ,  A61K31/18 ,  A61K31/19 ,  A61K31/222 ,  A61K31/337 ,  A61K31/343 ,  A61K31/39 ,  A61K31/404

CPC classification number: A61K31/27 ,  A61K31/00 ,  A61K31/138 ,  A61K31/165 ,  A61K31/166 ,  A61K31/167 ,  A61K31/18 ,  A61K31/19 ,  A61K31/222 ,  A61K31/337 ,  A61K31/343 ,  A61K31/382 ,  A61K31/39 ,  A61K31/404 ,  A61K31/4045 ,  A61K31/4188 ,  A61K31/427 ,  A61K31/435 ,  A61K31/436 ,  A61K31/4406 ,  A61K31/4545 ,  A61K31/4706 ,  A61K31/495 ,  A61K31/506 ,  A61K31/517 ,  A61K31/69 ,  A61K31/7004 ,  A61K31/7048 ,  A61K33/36 ,  A61K39/3955 ,  A61K45/06 ,  A61K2300/00

Abstract: The present specification provides compositions comprising a thioxanthone-based autophagy inhibitor and/or a cancer therapeutic autophagy inducing compound, pharmaceutical kits comprising these compositions, and methods of treating cancer using such compounds, compositions and kits. Additionally, the present specification provides methods of treating cancer using a thioxanthone- based autophagy inhibitor and a radiotherapy.

Abstract translation: 本说明书提供了包含基于噻吨酮的自噬抑制剂和/或癌症治疗性自噬诱导化合物的组合物，包含这些组合物的药物试剂盒，以及使用这些化合物，组合物和试剂盒治疗癌症的方法。 此外，本说明书提供了使用基于噻吨酮的自噬抑制剂和放射治疗来治疗癌症的方法。

公开(公告)号：WO2011110546A3

公开(公告)日：2011-09-15

申请号：PCT/EP2011/053446

申请日：2011-03-08

Applicant: MAX-PLANCK-GESELLSCHAFT ZUR FÖRDERUNG DER WISSENSCHAFTEN E.V. ,  BAUER, Bianca ,  MEYER, Thomas F.

Inventor： BAUER, Bianca ,  MEYER, Thomas F.

IPC: A61K31/00 ,  A61K31/15 ,  A61K31/155 ,  A61K31/18 ,  A61K31/285 ,  A61K31/351 ,  A61K31/404 ,  A61K31/41 ,  A61K31/4162 ,  A61K31/427 ,  A61K31/429 ,  A61K31/4439 ,  A61K31/47 ,  A61K31/4985 ,  A61K31/517

Abstract: The present invention relates to a pharmaceutical composition comprising at least one inhibitor of SHP-2, optionally together with pharmaceutically acceptable carriers, adjuvants, diluents and/or additives. The present invention also relates to screening methods for identification of a compound suitable as inhibitor of SHP-2.