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41. 发明申请

US20140044775A1 SYNTHETIC LUNG SURFACTANT AND USE THEREOF 有权
标题翻译：合成肺表面活性剂及其用途
公开(公告)号：US20140044775A1
公开(公告)日：2014-02-13
申请号：US14030719
申请日：2013-09-18
申请人： University of Rochester , The Los Angles Biomedical Research Institute at Harbor-UCLA Medical Center , University of Guelph
发明人： Robert H. Notter , Zhengdong Wang , Adrian L. Schwan , Zhongyi Wang , Jason A. Davy , Alan J Waring , Frans Walther , Larry M. Gordon
IPC分类号： C07K14/785 , C07F9/09
CPC分类号： C07F9/091 , A61K9/0082 , C07F9/4006 , C07F9/4075 , C07K14/001 , C07K14/785
摘要： The present invention relates to synthetic lung surfactant compositions that contain one or more of phospholipase-resistant phospho-glycerol derivatives, phospholipase-resistant phospho-choline derivatives, and surface active proteins or peptides, more preferably a combination of at least two or all three of these materials. Novel phospholipase-resistant phospho-glycerol derivatives, phospholipase-resistant phospho-choline derivatives, and surface active peptides are also disclosed herein. Uses of the surfactant compositions of the present invention to treat endogenous surfactant dysfunctional or deficient lung tissue, to prepare synthetic peptides for use in the surfactant compositions, and to deliver therapeutic agents are also disclosed.
摘要翻译：本发明涉及含有一种或多种磷脂酶抗性磷酸甘油衍生物，磷脂酶抗性磷酸胆碱衍生物和表面活性蛋白质或肽的合成肺表面活性剂组合物，更优选至少两种或全部三种这些材料。本文还公开了新型磷脂酶抗性磷酸甘油衍生物，磷脂酶抗性磷酸胆碱衍生物和表面活性肽。还公开了本发明的表面活性剂组合物用于治疗内源性表面活性物质功能障碍或缺乏肺组织，制备用于表面活性剂组合物的合成肽和递送治疗剂的用途。

42. 发明申请

US20140024734A1 HALOGEN-FREE POLY(ALKYLENE PHOSPHATES) 有权
标题翻译：无卤素（亚磷酸氢盐）
公开(公告)号：US20140024734A1
公开(公告)日：2014-01-23
申请号：US13942128
申请日：2013-07-15
申请人： LANXESS Deutschland GmbH
发明人： Jan-Gerd HANSEL , Heiko TEBBE
IPC分类号： C08K5/521 , C08L75/08 , C08L75/06 , C07F9/141
CPC分类号： C07F9/141 , C07F9/091 , C08G18/42 , C08G18/4825 , C08G2101/0008 , C08G2101/0083 , C08K5/0066 , C08K5/521 , C08K2201/014 , C08L75/06 , C08L75/08 , C08L75/04
摘要： The present invention relates to halogen-free oligomer mixtures of poly(alkylene phosphates), production of these and use as flame retardants, and also to flame-retardant polyurethanes comprising halogen-free oligomer mixtures as flame retardants.
摘要翻译：本发明涉及聚（亚烷基磷酸酯）的无卤低聚物混合物，它们的制备和用作阻燃剂，还涉及包含无卤素低聚物混合物作为阻燃剂的阻燃聚氨酯。

43. 发明申请

US20140012011A1 COMPOUNDS FOR PREPARING IMMUNOLOGICAL ADJUVANT 有权
标题翻译：制备免疫调节剂的化合物
公开(公告)号：US20140012011A1
公开(公告)日：2014-01-09
申请号：US13947593
申请日：2013-07-22
申请人： Eisai R&D Management Co., Ltd.
发明人： Francis G. Fang , James E. Foy , Lynn Hawkins , Charles Lemelin , Andre LesCarbeau , Xiang Niu , Kuo-Ming Wu
IPC分类号： C07D263/14
CPC分类号： C07D263/14 , C07C217/28 , C07C271/16 , C07F9/091 , C07F9/1411 , C07F9/2408
摘要： The present invention provides methods for preparing TLR-4 receptor agonist E6020: and stereoisomers thereof, which compounds are useful as an immunological adjuvants when co-administered with antigens such as vaccines for bacterial and viral diseases. Also provided are synthetic intermediates.
摘要翻译：本发明提供了制备TLR-4受体激动剂E6020及其立体异构体的方法，当与抗原如用于细菌和病毒疾病的疫苗共同施用时，该化合物可用作免疫佐剂。还提供了合成中间体。

44. 发明授权

US08618080B2 Immunomodulatory compounds and treatment of diseases related to an overproduction of inflammatory cytokines 失效
标题翻译：免疫调节化合物和与炎症细胞因子过度生成有关的疾病的治疗
公开(公告)号：US08618080B2
公开(公告)日：2013-12-31
申请号：US13073737
申请日：2011-03-28
申请人： Jacques Bauer , Carlo Chiavaroli , Stephane Moutel
发明人： Jacques Bauer , Carlo Chiavaroli , Stephane Moutel
IPC分类号： A01N57/00 , A61K31/66
CPC分类号： A61K31/661 , A61K31/16 , A61K31/221 , A61K31/6615 , C07F9/091
摘要： Method of using immunomodulatory compounds for treating diseases related to an overproduction of inflammatory cytokines, including diseases selected from asthma, atopic dermatitis, allergic rhinitis, prostatitis, inflammatory bowel disease, diabetes, and rheumatoid arthritis, the compounds being of general formula (I): wherein: m and n, independently from each other, are an integer ranging from 1 to 4, X and Y represent —COON, —O—P(O)(OH)2, —O—S02(OH), —NH2, —OH, —CONH(CH2)n1—NH2, —CO—NH—CH(COOH)—(CH2)n1—COOH, —CO—NH—CH(COOH)—(CH2)n1—NH2, —O—CO—(CH2)n1—NH2, —O—CO—(CH2)n1—CHOH—CH2OH, —O—CO—(CH2)n1—OH, —O—CO—(CH2)n1—COOH, —O—CO—(CH2)n1—CHO, —O—CO—(CH2)n1—NH—CO—(CH2)n2—COOH, R1 and R2 each designate an acyl group derived from a saturated or unsaturated, straight-or branched-chain carboxylic acid having from 2 to 18 carbon atoms, which is unsubstituted or bears one to three substituents selected among hydroxyl, dihydroxyphosphoryloxy, alkyl of 2 to 18 carbon atoms, alkoxy of 2 to 18 carbon atoms, acyloxy of 2 to 18 carbon atoms in the acyl moiety, amino, acylamino.
摘要翻译：使用免疫调节化合物治疗与炎性细胞因子过度生成有关的疾病的方法，所述疾病包括选自哮喘，特应性皮炎，过敏性鼻炎，前列腺炎，炎性肠病，糖尿病和类风湿性关节炎的疾病，所述通式（I）的化合物：其中：m和n彼此独立地为1至4的整数，X和Y表示-COON，-OP（O）（OH）2，-O-SO 2（OH），-NH 2，-OH ，-CONH（CH2）n1-NH2，-CO-NH-CH（COOH） - （CH2）n1-COOH，-CO-NH-CH（COOH） - （CH2）n1-NH2，-O-CO- （CH2）n1-NH2，-O-CO-（CH2）n1-CHOH-CH2OH，-O-CO-（CH2）n1-OH，-O-CO-（CH2）n1-COOH，-O-CO- CH2）n1-CHO，-O-CO-（CH2）n1-NH-CO-（CH2）n2-COOH，R1和R2各自表示衍生自饱和或不饱和的直链或支链羧酸的酰基具有2至18个碳原子，其是未取代的或带有1-3个选自羟基，二羟基磷酰氧基，2至18个碳原子的烷基，2至18个碳原子的烷氧基原子，酰基部分中2至18个碳原子的酰氧基，氨基，酰氨基。

45. 发明授权

US08569270B2 Diphenyl sulfide derivatives and medicines containing same as active ingredient 有权
标题翻译：二苯硫醚衍生物和含有活性成分的药物
公开(公告)号：US08569270B2
公开(公告)日：2013-10-29
申请号：US13382011
申请日：2010-07-08
申请人： Yasushi Kohno , Kiyoshi Fujii , Momoko Taru , Keita Miyoshi
发明人： Yasushi Kohno , Kiyoshi Fujii , Momoko Taru , Keita Miyoshi
IPC分类号： A61K31/663 , C07F9/09
CPC分类号： A61K31/662 , C07F9/091 , C07F9/3808 , C07F9/4006 , C07F9/4015
摘要： Provided are diphenyl sulfide derivatives which have excellent S1P3 antagonistic activity and are useful as drugs. Intensive studies have been made for the purpose of creating a compound having S1P3 antagonistic activity. As a result of the intensive studies, it has been found that diphenyl sulfide derivatives represented by general formula (1) have excellent S1P3 antagonistic activity. In general formula (1), R1 is a hydrogen atom or the like; R2 is an optionally substituted alkyl group having 1 to 6 carbon atoms, or the like; X is a methylene group which may be substituted with one or two fluorine atoms, or the like; Y is a hydrogen atom or the like; and Z is a halogen atom.
摘要翻译：提供具有优异的S1P3拮抗活性并可用作药物的二苯硫醚衍生物。为了制备具有S1P3拮抗活性的化合物，已进行了深入研究。作为深入研究的结果，已经发现由通式（1）表示的二苯硫醚衍生物具有优异的S1P3拮抗活性。通式（1）中，R 1为氢原子等; R2是任选取代的碳原子数为1〜6的烷基等; X是可被一个或两个氟原子取代的亚甲基等; Y是氢原子等; Z为卤素原子。

46. 发明申请

US20130266591A1 USE OF TRI-SUBSTITUTED GLYCEROL COMPOUNDS FOR THE TREATMENT OF HEMATOLOGICAL MALIGNANCIES 审中-公开
标题翻译：三取代甘氨酸化合物用于治疗血液恶性疾病的用途
公开(公告)号：US20130266591A1
公开(公告)日：2013-10-10
申请号：US13910717
申请日：2013-06-05
申请人： Alphaptose GmbH , Universitatsklinikum Hamburg-Eppendorf
发明人： Axel Rolf Zander , Francis Ayuk Ayuketang , Wolfgang Richter , Lutz Weber
IPC分类号： A61K31/661 , A61K45/06 , A61K39/395 , C07F9/09
CPC分类号： A61K31/661 , A61K31/4965 , A61K31/513 , A61K31/52 , A61K31/685 , A61K31/7048 , A61K39/39533 , A61K45/06 , C07F9/091 , A61K2300/00
摘要： The present invention relates to the use of a tri-substituted glycerol compound for the manufacture of a medicament for the treatment of hematological malignancies. The invention also refers to a kit-of-parts comprising such a medicament. Finally, the invention also relates to a corresponding method for the treatment of such conditions as well as to an in vitro method for determining the susceptibility of such malignant cells to a medicament as defined in the invention.
摘要翻译：本发明涉及三取代甘油化合物在制备用于治疗血液恶性肿瘤的药物中的用途。本发明还涉及包含这种药物的成套工具。最后，本发明还涉及用于治疗这些病症的相应方法以及用于确定这样的恶性细胞对本发明所定义的药物敏感性的体外方法。

47. 发明授权

US08536363B2 Compounds and methods for delivery of prostacyclin analogs 有权
公开(公告)号：US08536363B2
公开(公告)日：2013-09-17
申请号：US13558757
申请日：2012-07-26
申请人： Ken Phares , David Mottola
发明人： Ken Phares , David Mottola
IPC分类号： C07C327/00 , C07C69/716 , A61K31/192 , A61K31/216
CPC分类号： C07C59/13 , A61K9/0019 , A61K9/0053 , A61K31/192 , A61K31/216 , A61K31/223 , A61K31/235 , C07C51/412 , C07C59/70 , C07C69/712 , C07C229/08 , C07C235/06 , C07C235/08 , C07C259/06 , C07C2103/10 , C07C2603/10 , C07F9/091 , C07F9/117
摘要： This invention pertains generally to prostacyclin analogs and methods for their use in promoting vasodilation, inhibiting platelet aggregation and thrombus formation, stimulating thrombolysis, inhibiting cell proliferation (including vascular remodeling), providing cytoprotection, preventing atherogenesis and inducing angiogenesis. Generally, the compounds and methods of the present invention increase the oral bioavailability and circulating concentrations of treprostinil when administered orally. Compounds of the present invention have the following formula:

48. 发明授权

US08519170B2 Compounds for preparing immunological adjuvant 有权
公开(公告)号：US08519170B2
公开(公告)日：2013-08-27
申请号：US13468634
申请日：2012-05-10
申请人： Francis G. Fang , James E. Foy , Lynn Hawkins , Charles Lemelin , Andre Lescarbeau , Xiang Niu , Kuo-Ming Wu
发明人： Francis G. Fang , James E. Foy , Lynn Hawkins , Charles Lemelin , Andre Lescarbeau , Xiang Niu , Kuo-Ming Wu
IPC分类号： C07C229/00
CPC分类号： C07D263/14 , C07C217/28 , C07C271/16 , C07F9/091 , C07F9/1411 , C07F9/2408
摘要： The present invention provides methods for preparing TLR-4 receptor agonist E6020: and stereoisomers thereof, which compounds are useful as an immunological adjuvants when co-administered with antigens such as vaccines for bacterial and viral diseases. Also provided are synthetic intermediates.

49. 发明申请

US20130216607A1 ZWITTERIONIC LIPIDS 有权
标题翻译： ZWITTERICIC LIPIDS
公开(公告)号：US20130216607A1
公开(公告)日：2013-08-22
申请号：US13816882
申请日：2011-08-15
申请人： Francis C. Szoka, JR. , Colin Walsh , Vincent Venditto , Juliane Nguyen , Emily Perttu
发明人： Francis C. Szoka, JR. , Colin Walsh , Vincent Venditto , Juliane Nguyen , Emily Perttu
IPC分类号： C07C229/12 , A61K9/127 , A61K47/18 , C07J9/00 , A61K47/28
CPC分类号： C07C229/12 , A61K9/1272 , A61K47/186 , A61K47/28 , C07C279/14 , C07C309/14 , C07F9/091 , C07F9/54 , C07F9/650952 , C07J9/00 , C07J41/0055 , C40B40/04
摘要： In various embodiments, the present invention provides zwitterionic lipids, encapsulants incorporating these zwitterionic lipids and such encapsulants encapsulating one or more bioactive agent. An exemplary bioactive agent is a nucleic acid. Also provided are pharmaceutical formulations of the encapsulants and methods of using such formulations to deliver a bioactive agent to a subject in treating or diagnosing disease in that subject.
摘要翻译：在各种实施方案中，本发明提供两性离子脂质，包含这些两性离子性脂质的密封剂和封装一种或多种生物活性剂的这种密封剂。示例性的生物活性剂是核酸。还提供了密封剂的药物制剂和使用这些制剂将生物活性剂递送到受试者以治疗或诊断该受试者的疾病的方法。

50. 发明授权

US08513418B2 Substituted bicyclic methyl amine derivatives as sphingosine-1 phosphate receptors modulators 失效
标题翻译：取代的双环甲基胺衍生物作为鞘氨醇-1-磷酸受体调节剂
公开(公告)号：US08513418B2
公开(公告)日：2013-08-20
申请号：US13445991
申请日：2012-04-13
申请人： Janet A. Takeuchi , Ling Li , Wha Bin Im
发明人： Janet A. Takeuchi , Ling Li , Wha Bin Im
IPC分类号： C07D215/12 , C07F9/09 , C07F9/38 , C07F9/60
CPC分类号： C07C215/08 , C07C217/54 , C07D215/12 , C07F9/091 , C07F9/3808 , C07F9/3834 , C07F9/60
摘要： The present invention relates to novel substituted bicyclic methyl amine derivatives which are useful as sphingosine-1-phosphate receptors modulators and useful for treating a wide variety of disorders associated with modulation of sphingosine-1-phosphate receptors.
摘要翻译：本发明涉及可用作鞘氨醇-1-磷酸受体调节剂并可用于治疗与调节鞘氨醇-1-磷酸受体相关的多种疾病的新型取代的二环甲基胺衍生物。

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