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1. 发明授权

US08987262B2 Use of a beta blocker for the manufacture of a medicament for the treatment of hemangiomas 有权
标题翻译： β阻断剂用于制造用于治疗血管瘤的药物的用途
公开(公告)号：US08987262B2
公开(公告)日：2015-03-24
申请号：US13678802
申请日：2012-11-16
申请人： Universite de Bordeaux , Centre Hospitalier Universitaire de Bordeaux
发明人： Christine Leaute-Labreze , Eric Dumas De La Roque , Alain Taieb , Jean-Benoit Thambo
IPC分类号： A61K31/535 , A01N43/42 , A61K31/47 , A01N43/38 , A61K31/40 , A61K31/405 , A01N43/16 , A61K31/35 , A01N43/40 , A61K31/36 , A01N37/12 , A61K31/24 , A01N37/02 , A61K31/22 , A01N47/28 , A61K31/17 , A01N41/06 , A61K31/18 , A01N37/18 , A61K31/165 , A61K31/16 , A01N33/02 , A61K31/135 , A01N35/00 , A61K31/12 , A01N31/00 , A61K31/045 , C07D417/00 , C07D215/00 , C07D209/10 , C07D311/00 , C07D317/44 , C07C69/00 , C07C335/00 , C07C303/00 , C07C307/00 , C07C309/00 , C07C311/00 , C07C273/00 , C07C275/00 , C07C233/00 , C07C235/00 , C07C239/00 , C09B11/02 , C07C211/00 , C07C213/00 , C07C221/00 , C07C225/00 , A61K31/138 , A61K31/167
CPC分类号： A61K31/138 , A61K31/167
摘要： The present technology relates the use of a beta blocker for the manufacture of a medicament for the treatment of hemangiomas, for example of infantile hemangiomas. The beta blocker may be a non-selective beta-blocker, for example propranolol. The present technology provides an alternative to the known compounds, e.g. corticosteroïds, interferon or vincristine, generally used for the treatment of hemangiomas.
摘要翻译：本技术涉及β-阻滞剂在制备用于治疗血管瘤（例如婴儿血管瘤）的药物中的用途。 β受体阻滞剂可以是非选择性β-受体阻滞剂，例如普萘洛尔。本技术提供了已知化合物的替代物，例如皮质激素，干扰素或长春新碱，通常用于治疗血管瘤。

2. 发明授权

US08921391B2 Selective EP4 receptor antagonistic substance for treatment of cancer 有权
标题翻译：用于治疗癌症的选择性EP4受体拮抗物质
公开(公告)号：US08921391B2
公开(公告)日：2014-12-30
申请号：US13265216
申请日：2010-04-22
申请人： Yukinori Take , Shinichi Koizumi , Takako Okumura , Kazuhiko Nonomura
发明人： Yukinori Take , Shinichi Koizumi , Takako Okumura , Kazuhiko Nonomura
IPC分类号： A01N43/42 , A61K31/44 , A01N43/40 , A01N37/12 , A01N37/44 , A61K31/195 , A01N47/28 , A61K31/17 , C07D513/02 , C07D515/02 , C07D211/72 , C07D211/84 , C07D213/56 , C07C273/00 , C07C275/00 , C07C239/00 , A61K31/192 , A61K31/437 , A61K31/4412
CPC分类号： C07D471/04 , A61K31/192 , A61K31/437 , A61K31/44 , A61K31/4412 , A61K45/06 , C07C235/60 , C07D213/82
摘要： This invention provides a medicament for the treatment of cancer, which cause a reduction of cancer. This invention relates to use of a compound which has inhibitory activities against prostaglandin E2 receptor (EP4 receptor) and is represented by the following general formula (I), (II), (III), or (IV), or a pharmaceutically acceptable salt thereof, or a pharmaceutical composition comprising the compound or the salt for the manufacture of a medicament for the treatment of cancer. The invention relates to a method for treatment of cancer comprising administering the compound or a pharmaceutically acceptable salt thereof, or a pharmaceutical composition comprising the compound or the salt to humans or animals. The compound or a pharmaceutically acceptable salt thereof, or the pharmaceutical composition may be used in combination with one or more second active agents.
摘要翻译：本发明提供了用于治疗导致癌症减少的癌症的药物。本发明涉及对前列腺素E2受体（EP4受体）具有抑制活性且由以下通式（I），（II），（III）或（IV）表示的化合物或其药学上可接受的盐或包含该化合物或盐的药物组合物，用于制备用于治疗癌症的药物。本发明涉及一种治疗癌症的方法，其包括将化合物或其药学上可接受的盐或包含该化合物或盐的药物组合物给予人或动物。化合物或其药学上可接受的盐或药物组合物可以与一种或多种第二活性剂组合使用。

3. 发明授权

US08772543B2 Antiproliferative compounds, conjugates thereof, methods therefor, and uses thereof 有权
标题翻译：抗增殖化合物，其缀合物，其方法及其应用
公开(公告)号：US08772543B2
公开(公告)日：2014-07-08
申请号：US13752721
申请日：2013-01-29
申请人： Medarex, Inc.
发明人： Heng Cheng , Sanjeev Gangwar , Qiang Cong , Qian Zhang
IPC分类号： C07C235/00 , C07C237/00 , C07C239/00 , C07C211/00
CPC分类号： C07K7/06 , A61K38/06 , A61K47/6811 , A61K47/6829 , C07C229/14 , C07C229/16 , C07K5/021 , C07K5/06139 , C07K5/10 , C07K16/18
摘要： Antiproliferative compounds having a structure represented by formula (II), where n, R1, R2, R3, R4, and R5 are as defined herein, can be used to treat tumors, optionally when conjugated to a ligand such as an antibody:
摘要翻译：具有由式（II）表示的结构的抗增殖化合物，其中n，R 1，R 2，R 3，R 4和R 5如本文所定义，可任选地当与配体例如抗体缀合时用于治疗肿瘤：

4. 发明授权

US08735625B2 Dual-acting antihypertensive agents 有权
标题翻译：双作用抗高血压药
公开(公告)号：US08735625B2
公开(公告)日：2014-05-27
申请号：US13755404
申请日：2013-01-31
申请人： Seok-ki Choi , Paul R. Fatheree , Ryan Hudson , Keith Jendza , Robert Murray McKinnell , Vivek Sasikumar
发明人： Seok-ki Choi , Paul R. Fatheree , Ryan Hudson , Keith Jendza , Robert Murray McKinnell , Vivek Sasikumar
IPC分类号： C07C239/00 , C07D257/00
CPC分类号： C07C237/20 , C07C243/32 , C07C319/12 , C07C323/22 , C07C323/41 , C07C323/60 , C07C2601/14 , C07D257/04
摘要： The invention is directed to compounds of formula I: wherein Ar, r, R3, X, and R5-7 are as defined in the specification, and pharmaceutically acceptable salts thereof. The compounds of formula I have AT1 receptor antagonist activity and neprilysin inhibition activity. The invention is also directed to pharmaceutical compositions comprising such compounds; methods of using such compounds; and a process and intermediates for preparing such compounds.
摘要翻译：本发明涉及式I化合物：其中Ar，r，R 3，X和R 5-7如说明书中所定义，及其药学上可接受的盐。式I的化合物具有AT1受体拮抗剂活性和去皮质激素抑制活性。本发明还涉及包含这些化合物的药物组合物; 使用这些化合物的方法; 以及制备这些化合物的方法和中间体。

5. 发明授权

US08716337B1 Abuse deterrent and anti-dose dumping pharmaceutical salts useful for the treatment of attention deficit/hyperactivity disorder 有权
公开(公告)号：US08716337B1
公开(公告)日：2014-05-06
申请号：US13445189
申请日：2012-04-12
申请人： Clifford Riley King , Stephen G. D'Ambrosio , David W. Bristol
发明人： Clifford Riley King , Stephen G. D'Ambrosio , David W. Bristol
IPC分类号： A01N37/00 , A61K31/21 , A01N37/10 , A61K31/235 , A01N37/18 , A61K31/165 , C07C69/00 , C07C233/00 , C07C235/00 , C07C237/00 , C07C239/00
CPC分类号： A61K31/4458 , A61K31/137 , A61K31/485 , A61K31/55
摘要： A pharmaceutical composition comprising a drug substance consisting essentially of a pharmaceutically acceptable organic acid addition salt of an amine containing pharmaceutically active compound wherein the amine containing pharmaceutical active compound is selected from the group consisting of racemic or single isomer ritalinic acid or phenethylamine derivatives and the drug substance has a physical form selected from amorphous and polymorphic.

6. 发明授权

US08664440B2 Method for preparing aliskiren and its intermediates thereof 有权
标题翻译：阿利吉仑及其中间体的制备方法
公开(公告)号：US08664440B2
公开(公告)日：2014-03-04
申请号：US13639144
申请日：2010-04-19
申请人： Yongjun Tu , Yi Zhang , Rongde Cheng , Lingchao Peng
发明人： Yongjun Tu , Yi Zhang , Rongde Cheng , Lingchao Peng
IPC分类号： A61K31/16 , C07C239/00
CPC分类号： C07D307/28 , C07C231/02 , C07C231/12 , C07C231/14 , C07C231/18 , C07C269/06 , C07D307/33 , C07C237/22 , C07C271/22
摘要： A method for preparing Aliskiren and intermediate thereof, which comprises the following steps: reacting 4-bromo-1-methoxy-2-(3-methoxypropoxy)benzene with magnesium isopropyl chloride and n-BuLi to obtain the compound of formula XXII; reacting the product of methylsulfonylation of the compound of formula XIX with anhydrous LiBr to obtain the compound of formula XXI; obtaining the intermediate of Aliskiren shown as formula XV by reacting the compound of formula XXII with the compound of formula XXI in an ether as the solvent and in the presence of a catalyst containing iron; then reacting the compound of formula XV with the compound of formula VII to obtain the compound of formula XXIII, following removing R1 from the amino group and obtaining Aliskiren shown as formula I.
摘要翻译：一种制备阿利吉仑及其中间体的方法，包括以下步骤：4-溴-1-甲氧基-2-（3-甲氧基丙氧基）苯与异丙基氯化镁和n-BuLi反应得到式XXII化合物; 使式XIX化合物的甲基磺酰化产物与无水LiBr反应，得到式XXI化合物; 通过使式XXII化合物与式XXI化合物在醚中作为溶剂和在含铁催化剂存在下反应，得到式XV所示的阿利克仑中间体。然后使式XV的化合物与式VII的化合物反应，得到式XXIII的化合物，在从氨基中除去R 1后得到如式I所示的阿利吉仑。

7. 发明授权

US08653129B2 Combination therapy for skin disorders 有权
标题翻译：组合治疗皮肤病
公开(公告)号：US08653129B2
公开(公告)日：2014-02-18
申请号：US13518818
申请日：2011-04-11
申请人： Howard Fein , Mindy B. Berlin
发明人： Howard Fein , Mindy B. Berlin
IPC分类号： A01N43/16 , A61K31/35 , A01N37/18 , A61K31/165 , C07D311/00 , C07C233/00 , C07C235/00 , C07C237/00 , C07C239/00
CPC分类号： A61K31/65 , A61K9/0014 , A61K9/0053 , A61K9/127 , A61K9/48 , A61K9/7023 , A61K31/135 , A61K31/353 , A61K31/496 , A61K31/565 , A61K45/06 , A61K2300/00
摘要： The present invention provides a novel therapeutic combination comprising one or more anti-androgen agents and one or more antibiotic/anti-inflammatory agents or pharmaceutically acceptable salts or hydrates thereof, useful for the treatment of a dermatological disorder.
摘要翻译：本发明提供了一种新颖的治疗组合，其包含一种或多种抗雄激素剂和一种或多种可用于治疗皮肤病的抗生素/抗炎剂或其药学上可接受的盐或水合物。

8. 发明授权

US08633022B2 Dual-terminal amide hydrogelling agent 失效
标题翻译：双末端酰胺水凝胶剂
公开(公告)号：US08633022B2
公开(公告)日：2014-01-21
申请号：US13201111
申请日：2010-02-23
申请人： Hitoshi Tamiaki , Keishiro Ogawa , Kazunori Toma
发明人： Hitoshi Tamiaki , Keishiro Ogawa , Kazunori Toma
IPC分类号： C12N5/00 , C07C239/00
CPC分类号： C07C235/48 , C12N5/0068 , C12N2533/30
摘要： The invention relates to a benzamide derivative represented by formula (1): wherein k1 represents an integer from 0-4, m1 represents an integer from 1-100, and n1 represents an integer from 1-6. In addition, R1 represents a hydrocarbon group with 8-22 carbon atoms bonded to an oxygen atom wherein the oxygen atom is bonded to the adjacent ring of said derivative; R2 represents H or a hydrocarbon group with 1-22 carbon atoms bonded to an oxygen atom wherein the oxygen atom is bonded to the adjacent ring of said derivative; R3 represents H or a hydrocarbon group with 1-22 carbon atoms bonded to an oxygen atom wherein the oxygen atom is bonded to the adjacent ring of said derivative; and R2 and R3 are not H at the same time.
摘要翻译：本发明涉及由式（1）表示的苯甲酰胺衍生物：其中k1表示0-4的整数，m1表示1-100的整数，n1表示1-6的整数。此外，R 1表示与氧原子键合的碳原子数为8〜22的烃基，其中氧原子与所述衍生物的相邻环结合; R2表示H或与氧原子键合的具有1-22个碳原子的烃基，其中氧原子键合到所述衍生物的相邻环上; R3表示H或与氧原子键合的具有1-22个碳原子的烃基，其中氧原子与所述衍生物的相邻环结合; R2和R3不同时为H。

9. 发明授权

US08614251B2 Crystalline form VI of agomelatine, preparation method and application thereof 有权
标题翻译：琼脂糖的结晶形式VI，其制备方法和应用
公开(公告)号：US08614251B2
公开(公告)日：2013-12-24
申请号：US13138615
申请日：2010-03-09
申请人： Hanbin Shan , Peng Zhang , Zhedong Yuan , Xudong Jiang , Yu Huang , Hubo Wang , Xufeng Cao , Xingdong Cheng , Xiong Yu
发明人： Hanbin Shan , Peng Zhang , Zhedong Yuan , Xudong Jiang , Yu Huang , Hubo Wang , Xufeng Cao , Xingdong Cheng , Xiong Yu
IPC分类号： A01N37/18 , A61K31/16 , C07C233/00 , C07C235/00 , C07C237/00 , C07C239/00
CPC分类号： A61K31/165 , C07C233/18
摘要： The invention provides a new crystalline form of agomelatine, preparation and use thereof. The X-ray powder diffraction diagram of the agomelatine crystalline form shows main peaks at the diffraction angles 2θ 11.13°, 11.82°, 17.49°, 18.29°, 19.48°, 19.72°, 20.50°, 21.76°, 22.54°, 22.97°, 24.56°, 25.36°, 27.16° and 31.93°. Said new crystalline form is characterized by high purity, stability and good reproducibility, and thus is advantageous for the pharmaceutical formulation. In addition, the stability and solubility of said crystalline form are also superior over the several existing crystalline forms.
摘要翻译：本发明提供了一种新的结晶形式的agomelatine，其制备和用途。阿魏酸晶体形式的X射线粉末衍射图在衍射角2θ11.13°，11.82°，17.49°，18.29°，19.48°，19.72°，20.50°，21.76°，22.54°，22.97°处显示主峰， 24.56°，25.36°，27.16°和31.93°。所述新的结晶形式的特征在于高纯度，稳定性和良好的再现性，因此对于药物制剂是有利的。此外，所述结晶形式的稳定性和溶解度也优于几种现有的结晶形式。

10. 发明授权

US08507724B2 Compounds for use in the treatment of pain 有权
标题翻译：用于治疗疼痛的化合物
公开(公告)号：US08507724B2
公开(公告)日：2013-08-13
申请号：US13133569
申请日：2009-12-09
申请人： Martin Leuwer , Paul O'Neill , Neil Berry , Gertrud Haeseler
发明人： Martin Leuwer , Paul O'Neill , Neil Berry , Gertrud Haeseler
IPC分类号： C07C233/00 , C07C235/00 , C07C237/00 , C07C239/00 , C07C39/12 , C07C43/20
CPC分类号： C07C39/367 , C07C39/15 , C07C43/23 , C07C235/46
摘要： The present invention concerns compounds derived from the anaethetic propofol. The compounds may be useful in the treatment of pain, particularly, but not exclusively, chronic pain and central pain sensitisation.
摘要翻译：本发明涉及衍生自异步异丙酚的化合物。该化合物可用于治疗疼痛，特别是但不限于，慢性疼痛和中枢性疼痛敏化。

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