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1. 发明申请

US20140296336A1 SOLID RETARD FORMULATIONS BASED ON SOLID DISPERSIONS 审中-公开
标题翻译：基于固体分散体的固体残留配方
公开(公告)号：US20140296336A1
公开(公告)日：2014-10-02
申请号：US13993066
申请日：2011-12-22
申请人： Gunther Berndl , Juergen Weis , Dietrich Granzow , Bernd Liepold , Ute Lander , Ulrich Westedt
发明人： Gunther Berndl , Juergen Weis , Dietrich Granzow , Bernd Liepold , Ute Lander , Ulrich Westedt
IPC分类号： A61K47/34 , A61K9/00 , A61K31/167 , A61K47/32 , A61K31/192 , A61K31/216
CPC分类号： A61K47/34 , A61K9/00 , A61K9/146 , A61K9/2027 , A61K9/2031 , A61K9/2095 , A61K31/167 , A61K31/192 , A61K31/216 , A61K47/32
摘要： A formulation comprising a melt-processed solid dispersion product comprising an active agent, a pharmaceutically acceptable thermoplastic polymer of N-vinyl lactams, and a pharmaceutically acceptable polyvinyl alcohol-polyalkylene glycol graft copolymer. A method for producing said formulation.
摘要翻译：包含熔融加工的固体分散体产品的制剂，其包含活性剂，N-乙烯基内酰胺的药学上可接受的热塑性聚合物和药学上可接受的聚乙烯醇 - 聚亚烷基二醇接枝共聚物。一种制备所述制剂的方法。

2. 发明授权

US08765918B2 Human antibodies that bind human interleukin-12 有权
标题翻译：结合人白介素12的人抗体
公开(公告)号：US08765918B2
公开(公告)日：2014-07-01
申请号：US13429104
申请日：2012-03-23
申请人： Jochen G. Salfeld , Michael Roguska , Michael Paskind , Subhashis Banerjee , Daniel Edward Tracey , Michael White , Zehra Kaymakcalan , Boris Labkovsky , Paul Sakorafas , Geertruida M. Veldman , Amy Venturini , Angela Widom , Stuart Friedrich , Nicholas W. Warne , Angela Myles , John Gawain Elvin , Alexander Robert Duncan , Elaine Joy Derbyshire , Sara Carmen , Stephen Smith , Thor Las Holtet , Sarah Leila Du Fou
发明人： Jochen G. Salfeld , Michael Roguska , Michael Paskind , Subhashis Banerjee , Daniel Edward Tracey , Michael White , Zehra Kaymakcalan , Boris Labkovsky , Paul Sakorafas , Geertruida M. Veldman , Amy Venturini , Angela Widom , Stuart Friedrich , Nicholas W. Warne , Angela Myles , John Gawain Elvin , Alexander Robert Duncan , Elaine Joy Derbyshire , Sara Carmen , Stephen Smith , Thor Las Holtet , Sarah Leila Du Fou
IPC分类号： C07K16/24 , A61K39/395 , A61K38/00
CPC分类号： C07K16/244 , A61K9/0019 , A61K38/208 , A61K39/00 , A61K39/3955 , A61K39/39591 , A61K45/06 , A61K47/20 , A61K47/22 , A61K47/26 , A61K2039/505 , C07K14/5434 , C07K16/00 , C07K16/18 , C07K2317/21 , C07K2317/565 , C07K2317/73 , C07K2317/76 , C07K2317/94 , Y10S514/863 , Y10S514/885 , Y10S514/886
摘要： Human antibodies, preferably recombinant human antibodies, that specifically bind to human interleukin-12 (hIL-12) are disclosed. Preferred antibodies have high affinity for hIL-12 and neutralize hIL-12 activity in vitro and in vivo. An antibody of the invention can be a full-length antibody or an antigen-binding portion thereof. The antibodies, or antibody portions, of the invention are useful for detecting hIL-12 and for inhibiting hIL-12 activity, e.g., in a human subject suffering from a disorder in which hIL-12 activity is detrimental. Nucleic acids, vectors and host cells for expressing the recombinant human antibodies of the invention, and methods of synthesizing the recombinant human antibodies, are also encompassed by the invention.
摘要翻译：公开了特异性结合人白细胞介素-12（hIL-12）的人抗体，优选重组人抗体。优选的抗体对hIL-12具有高亲和力，并在体外和体内中和hIL-12活性。本发明的抗体可以是全长抗体或其抗原结合部分。本发明的抗体或抗体部分可用于检测hIL-12和抑制hIL-12活性，例如在患有hIL-12活性有害的病症的人类受试者中。用于表达本发明的重组人抗体的核酸，载体和宿主细胞以及合成重组人抗体的方法也包括在本发明中。

3. 发明申请

US20130245003A1 CARBOXAMIDE COMPOUNDS AND THEIR USE AS CALPAIN INHIBITORS 有权
标题翻译：羧酰胺化合物及其作为钙蛋白酶抑制剂的用途
公开(公告)号：US20130245003A1
公开(公告)日：2013-09-19
申请号：US13849826
申请日：2013-03-25
申请人： Abbott GmbH & Co. KG
发明人： Andreas Kling , Wilfried Hornberger , Helmut Mack , Achim Moeller , Volker Nimmrich , Dietmar Seemann , Wilfried Lubisch
IPC分类号： C07D401/04 , C07D491/048 , C07D401/14
CPC分类号： C07D401/04 , C07D401/14 , C07D405/14 , C07D409/14 , C07D491/048 , C07D493/04 , C07D513/04
摘要： The present invention relates to novel carboxamide compounds and their use for the manufacture of a medicament. The carboxamide compounds are inhibitors of calpain (calcium dependant cysteine proteases). The invention therefore also relates to the use of these carboxamide compounds for treating a disorder associated with an elevated calpain activity.The carboxamide compounds are compounds of the general formula I in which R1, R2, R3a, R3b, W, Y and X have the meanings mentioned in the claims and the description, the tautomers thereof and the pharmaceutically suitable salts thereof. In particular, the compounds have the general formula I-A.a′ and I-A.a″ in which m, E, R1, R3a, R3b, R2, Ry, Rw and Rw6* have the meanings mentioned in the claims, n is 0, 1 or 2, the tautomers thereof and the pharmaceutically suitable salts thereof.
摘要翻译：本发明涉及新的羧酰胺化合物及其用于制备药物的用途。羧酰胺化合物是钙蛋白酶（钙依赖性半胱氨酸蛋白酶）的抑制剂。因此，本发明还涉及这些羧酰胺化合物用于治疗与升高的钙蛋白酶活性相关的病症的用途。羧酰胺化合物是通式I的化合物，其中R1，R2，R3a，R3b，W，Y和X具有权利要求书和说明书中所述的含义，其互变异构体及其药学上合适的盐。特别地，化合物具有通式IA.a'和IA.a“，其中m，E，R1，R3a，R3b，R2，Ry，Rw和Rw6 *具有权利要求中提及的含义，n为0 ，1或2，其互变异构体及其药学上合适的盐。

4. 发明授权

US08486984B2 Aminomethyl substituted bicyclic aromatic compounds suitable for treating disorders that respond to modulation of the dopamine D3 receptor 失效
标题翻译：适用于治疗对多巴胺D3受体调节作出反应的疾病的氨基甲基取代的二环芳族化合物
公开(公告)号：US08486984B2
公开(公告)日：2013-07-16
申请号：US11665287
申请日：2005-10-14
申请人： Karla Drescher , Andreas Haupt , Liliane Unger , Sean C. Turner , Wilfried Braje , Roland Grandel
发明人： Karla Drescher , Andreas Haupt , Liliane Unger , Sean C. Turner , Wilfried Braje , Roland Grandel
IPC分类号： A61K31/404 , A61K31/4184 , C07D209/14 , C07D235/14
CPC分类号： C07D471/04 , C07D209/14 , C07D209/62 , C07D235/14
摘要： The present invention relates to an aminomethyl substituted bicyclic aromatic compound of the formula I The invention also relates to the use of a compound of the formula I or a pharmaceutically acceptable salt thereof for preparing a pharmaceutical composition for the treatment of a medical disorder susceptible to treatment with a dopamine D3 receptor ligand.
摘要翻译：本发明涉及式I的氨基甲基取代的双环芳族化合物。本发明还涉及式I化合物或其药学上可接受的盐在制备用于治疗易受治疗的医学疾病的药物组合物中的用途与多巴胺D3受体配体。

5. 发明授权

US08486931B2 Substituted oxindole compounds 有权
标题翻译：取代的羟吲哚化合物
公开(公告)号：US08486931B2
公开(公告)日：2013-07-16
申请号：US12529542
申请日：2008-02-29
申请人： Herve Genesle , Thorsten Oost , Charles W. Hutchins , Liliane Unger , Wilfried Hornberger , Wilfried Lubisch , Astrid Netz , Alfred Hahn
发明人： Herve Genesle , Thorsten Oost , Charles W. Hutchins , Liliane Unger , Wilfried Hornberger , Wilfried Lubisch , Astrid Netz , Wolfgang Wernet
IPC分类号： A61K31/4439 , A61K31/454 , A61K31/4709 , A61K31/496 , A61K31/551
CPC分类号： C07D401/14 , C07D401/04 , C07D401/12 , C07D471/08
摘要： The present invention relates to compounds of the general formula (I) in which A, B, R1, R2 and Het have the meaning given in claim 1; Y is a bivalent group of the formula in which D is C1-C3-alkylene, where D may have a substituent R5; R3 is hydrogen, C1-C8-alkyl or together with R4 is C1-C3-alkylene which may have a radical R5a, or together with R5 is C1-C3-alkylene, and R4 is hydrogen, C1-C8-alkyl or together with R3 is C1-C3-alkylene which may have a radical R5a, or together with R5 is C1-C3-alkylene, where R5 together with R5a, where present, are a bond or C1-C3-alkylene; and where one of the following conditions is satisfied: R3 together with R4 is C1-C3-alkylene which may have a radical R5a; or R3 together with R5 is C1-C3-alkylene; or R4 together with R5 is C1-C3-alkylene where the radical A is different from phenyl when the radical B is phenyl or naphthyl; and medicaments which comprise such compounds and the use thereof for the prophylaxis and/or treatment of vasopressin-dependent and/or oxytocin-dependent diseases.
摘要翻译：本发明涉及通式（I）的化合物，其中A，B，R1，R2和Het具有权利要求1中给出的含义; Y是下式的二价基团，其中D是C 1 -C 3 - 亚烷基，其中D可以具有取代基R 5; R 3是氢，C 1 -C 8烷基或与R 4一起是可以具有基团R 5a的C 1 -C 3亚烷基，或与R 5一起为C 1 -C 3 - 亚烷基，并且R 4是氢，C 1 -C 8 - 烷基或与 R 3是可以具有基团R 5a的C 1 -C 3亚烷基，或与R 5一起为C 1 -C 3 - 亚烷基，其中R 5与存在的R a a为键或C 1 -C 3 - 亚烷基; 并且其中满足以下条件之一：R 3与R 4一起可以具有基团R 5a的C 1 -C 3 - 亚烷基; 或R 3与R 5一起为C 1 -C 3 - 亚烷基; 或R 4与R 5一起为C 1 -C 3 - 亚烷基，其中基团B为苯基或萘基时，基团A不同于苯基; 以及包含这些化合物的药物及其用于预防和/或治疗加压素依赖性和/或催产素依赖性疾病的用途。

6. 发明申请

US20130150367A1 CARBOXAMIDE COMPOUNDS AND THEIR USE AS CALPAIN INHIBITORS 审中-公开
标题翻译：羧酰胺化合物及其作为钙蛋白酶抑制剂的用途
公开(公告)号：US20130150367A1
公开(公告)日：2013-06-13
申请号：US13610975
申请日：2012-09-12
申请人： Helmut Mack , Andreas Kling , Katja Jantos , Achim Moeller , Wilfried Hornberger , Charles W. Hutchins
发明人： Helmut Mack , Andreas Kling , Katja Jantos , Achim Moeller , Wilfried Hornberger , Charles W. Hutchins
IPC分类号： C07D207/22 , C07D275/03 , C07D409/12 , C07D401/06 , C07D417/12 , C07D405/12 , C07D211/78 , C07D233/32
CPC分类号： C07D207/22 , C07D207/26 , C07D207/28 , C07D211/76 , C07D211/78 , C07D213/81 , C07D233/32 , C07D233/34 , C07D239/10 , C07D275/03 , C07D401/06 , C07D401/12 , C07D405/12 , C07D409/12 , C07D417/12
摘要： The present invention relates to novel carboxamide compounds and their use for the manufacture of a medicament. The carboxamide compounds are inhibitors of calpain (calcium dependant cysteine proteases). The invention therefore also relates to the use of these carboxamide compounds for treating a disorder associated with an elevated calpain activity.The carboxamide compounds are compounds of the general formula I in which R1, R2, R3a, R3b, R4, Q, Y, A and X have the meanings mentioned in the claims and the description, the tautomers thereof and the pharmaceutically suitable salts thereof. In particular, the compounds have the general formula Ia and Ib in which R1, r, R2b, R3a, R3b, R4, Y and X have the meanings mentioned in the claims, including the tautomers thereof and the pharmaceutically suitable salts thereof. Of these compounds those are preferred wherein Y is a moiety CH2—CH2, CH2—CH2—CH2, N(Ry#)—CH2, N(Ry#)—CH2—CH2 or CH═CH—CH═, each optionally having 1 or 2 H-atoms replaced with identical or different radicals Ry, wherein Ry and Ry# have the meanings mentioned in the claims.
摘要翻译：本发明涉及新的羧酰胺化合物及其用于制备药物的用途。羧酰胺化合物是钙蛋白酶（钙依赖性半胱氨酸蛋白酶）的抑制剂。因此，本发明还涉及这些羧酰胺化合物用于治疗与升高的钙蛋白酶活性相关的病症的用途。羧酰胺化合物是通式I的化合物，其中R 1，R 2，R 3a，R 3b，R 4，Q，Y，A和X具有权利要求和说明书中所述的含义及其互变异构体及其药学上合适的盐。特别地，化合物具有通式Ia和Ib，其中R1，r，R2b，R3a，R3b，R4，Y和X具有权利要求中提及的含义，包括其互变异构体及其药学上合适的盐。在这些化合物中，优选其中Y为CH2-CH2，CH2-CH2-CH2，N（Ry＃）-CH2，N（Ry＃）-CH2-CH2或CH = CH-CH =，各自任选具有1 或2个H原子被相同或不同的基团Ry取代，其中Ry和Ry＃具有权利要求中提及的含义。

7. 发明申请

US20130122519A1 Method for Detection of Ischemic Strokes 审中-公开
标题翻译：缺血性脑卒中检测方法
公开(公告)号：US20130122519A1
公开(公告)日：2013-05-16
申请号：US13812163
申请日：2011-07-28
申请人： Ingo Curdt , Stuart Blincko , Jens Dhein , Viswanath Devanarayan , Joan Montaner Villalonga
发明人： Ingo Curdt , Stuart Blincko , Jens Dhein , Viswanath Devanarayan , Joan Montaner Villalonga
IPC分类号： G01N33/53
CPC分类号： G01N33/6893 , G01N33/5308 , G01N2800/2871
摘要： The present invention relates to the identification and use of diagnostic markers for ischemic stroke of the lacunar subtype. The invention relates to devices and kits for performing these methods.
摘要翻译：本发明涉及腔隙亚型缺血性卒中诊断标记物的鉴定与应用。本发明涉及用于执行这些方法的装置和套件。

8. 发明申请

US20130116241A1 NOVEL INHIBITOR COMPOUNDS OF PHOSPHODIESTERASE TYPE 10A 审中-公开
标题翻译：磷酸二酯酶类型10A的新型抑制剂化合物
公开(公告)号：US20130116241A1
公开(公告)日：2013-05-09
申请号：US13660524
申请日：2012-10-25
申请人： Abbott GmbH & Co. KG , AbbVie Inc.
发明人： Hervé Geneste , Michael Ochse , Karla Drescher , Sean Turner , Berthold Behl , Loic Laplanche , Jürgen Dinges , Clarissa Jakob , Lawrence Black
IPC分类号： C07D495/04 , C07D471/04 , C07D417/14
CPC分类号： C07D519/00 , C07D401/06 , C07D401/14 , C07D405/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D491/048 , C07D495/04
摘要： The present invention relates to novel compounds of the formula I which are inhibitors of phosphodiesterase type 10A and to their use for the manufacture of a medicament and which thus are suitable for treating or controlling of medical disorders selected from neurological disorders and psychiatric disorders, for ameliorating the symptoms associated with such disorders and for reducing the risk of such disorders. wherein Q is O or S, X1 is N or CH, X2 is N or C—R7; X3 is O, S—X4═C(R8)—, where C(R8) is bound to the carbon atom which carries R2, or —X5═C(R9)—, where X5 is bound to the carbon atom which carries R2; X4 is N or C—R9; X5 is N; Het is selected from optionally substituted phenyl, monocyclic hetaryl and fused bicyclic hetaryl; R1 is selected inter alia from hydrogen, halogen, OH, C1-C4-alkyl, trimethylsilyl, C1-C4-alkylsulfanyl, C1-C4-alkoxy-C1-C4-alkyl, C1-C4-alkoxy, C1-C4-alkoxy-C1-C4-alkoxy, the moiety Y1-Cyc1; R2 is selected inter alia from hydrogen, halogen, OH, C1-C4-alkyl, trimethylsilyl, C1-C4-alkoxy-C1-C4-alkyl, C1-C4-alkoxy, C1-C4-alkoxy-C1-C4-alkoxy, C2-C4-alkenyloxy, etc; A represents one of the following groups A1, A2, A3, A4 or A5: where * indicates the points of attachment to Het and to the nitrogen atom, respectively; and where R3 to R9, R3e, R3f, A′, Y1 and Cyc1 are defined in the claims.
摘要翻译：本发明涉及式I的新型化合物，其是10A型磷酸二酯酶的抑制剂及其用于制备药物的用途，因此其适用于治疗或控制选自神经障碍和精神疾病的医学病症，用于改善与这些疾病相关的症状并降低这种疾病的风险。其中Q为O或S，X1为N或CH，X2为N或C-R7; X3为O，S-X4 = C（R8） - ，其中C（R8）与携带R2的碳原子结合，或-X5 = C（R9） - ，其中X5与携带R2的碳原子结合 ; X4是N或C-R9; X5是N; Het选自任选取代的苯基，单环杂芳基和稠合双环杂芳基; R1特别选自氢，卤素，OH，C 1 -C 4 - 烷基，三甲基甲硅烷基，C 1 -C 4烷基硫烷基，C 1 -C 4 - 烷氧基-C 1 -C 4烷基，C 1 -C 4 - 烷氧基，C 1 -C 4烷氧基 - C1-C4-烷氧基，Y1-Cyc1部分; R2选自氢，卤素，OH，C 1 -C 4 - 烷基，三甲基甲硅烷基，C 1 -C 4 - 烷氧基-C 1 -C 4 - 烷基，C 1 -C 4 - 烷氧基，C 1 -C 4 - 烷氧基-C 1 -C 4烷氧基， C2-C4-烯氧基等; A代表以下组A1，A2，A3，A4或A5：其中*表示分别与Het和氮原子相连的点; 并且在权利要求中定义R3至R9，R3e，R3f，A'，Y1和Cyc1。

9. 发明授权

US08350055B2 Heteroaryl-substituted 1,3-dihydroindol-2-one derivatives and medicaments containing them 有权
公开(公告)号：US08350055B2
公开(公告)日：2013-01-08
申请号：US12839612
申请日：2010-07-20
申请人： Thorsten Oost , Wilfried Hornberger , Herve Geneste , Daryl Richard Sauer , Wolfgang Wernet , Andrea Hager-Wernet, legal representative , Liliane Unger , Wilfried Lubisch
发明人： Thorsten Oost , Wilfried Hornberger , Herve Geneste , Daryl Richard Sauer , Wolfgang Wernet , Liliane Unger , Wilfried Lubisch
IPC分类号： C07D411/00
CPC分类号： C07D401/14 , C07D401/12 , C07D403/14 , C07D405/14 , C07D409/04 , C07D409/14 , C07D413/14 , C07D417/14 , C07D513/04
摘要： The present invention relates to novel 1,3-dihydroindol-2-one (oxindole) derivatives of the formula (I) in which A, R3, R4, R5, R6, and R7 are defined according to claim 1, and to medicaments containing them for the treatment of diseases. In particular, the novel oxindole derivatives can be used for the control and/or prophylaxis of various vasopressin-dependent or oxytocin-dependent diseases.

10. 发明授权

US08337733B2 Preparation of compositions with essentially noncrystalline embedded macrolide antibiotics 有权
标题翻译：具有基本上非晶体嵌入的大环内酯类抗生素的组合物的制备
公开(公告)号：US08337733B2
公开(公告)日：2012-12-25
申请号：US12673230
申请日：2008-08-14
申请人： Ulrich Westedt , Jörg Rosenberg , Martin Knobloch , Norbert Steiger , Harald Hach
发明人： Ulrich Westedt , Jörg Rosenberg , Martin Knobloch , Norbert Steiger , Harald Hach
IPC分类号： B29C47/00
CPC分类号： A61K9/146 , B29C47/40 , B29C47/6056 , B29C47/64
摘要： A description is given of a process for the preparation of a pharmaceutical composition of a macrolide antibiotic in essentially noncrystalline form, in which the macrolide antibiotic, a water-swellable polymer and a proton donor are blended in an extruder in the presence of water and forced through a die, the ratio by weight of the sum of macrolide antibiotic, water-swellable polymer and proton donor to water being at least 1:1. The macrolide antibiotic is preferably clarithromycin and the water-swellable polymer is preferably chosen from crosslinked polyvinylpyrrolidone, crosslinked sodium carboxymethylcellulose and crosslinked polyacrylic acid.
摘要翻译：描述了制备基本上非结晶形式的大环内酯类抗生素药物组合物的方法，其中大环内酯类抗生素，水溶胀性聚合物和质子供体在水和挤出机的存在下在挤出机中共混通过模具，大环内酯类抗生素，水溶胀性聚合物和质子供体与水的总量的重量比至少为1:1。大环内酯类抗生素优选为克拉霉素，水溶胀性聚合物优选选自交联聚乙烯吡咯烷酮，交联羧甲基纤维素钠和交联聚丙烯酸。

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