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1. 发明申请

US20180325874A1 [1,2,4]TRIAZOLO[1,5-A]PYRIDINYL SUBSTITUTED INDOLE COMPOUNDS 审中-公开
公开(公告)号：US20180325874A1
公开(公告)日：2018-11-15
申请号：US16042116
申请日：2018-07-23
申请人： Bristol-Myers Squibb Company
发明人： Alaric J. Dyckman , Dharmpal S. Dodd , Christopher P. Mussari , Laxman Pasunoori , Sreekantha Ratna Kumar
IPC分类号： A61K31/4196 , C07D249/00 , C07D471/04 , A61K31/4427 , A61K31/437 , A61K45/06
摘要： Disclosed are compounds of Formula (I) or a salt thereof, wherein R1, R2, R3, R4, R5, m, n, and p are defined herein. Also disclosed are methods of using such compounds as inhibitors of signaling through Toll-like receptor 7, or 8, or 9, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating inflammatory and autoimmune diseases.

2. 发明授权

US08530506B2 Process for production of biphenyl derivative 失效
标题翻译：联苯衍生物生产工艺
公开(公告)号：US08530506B2
公开(公告)日：2013-09-10
申请号：US13509817
申请日：2010-09-24
申请人： Masahiko Seki
发明人： Masahiko Seki
IPC分类号： A61K31/41 , C07D249/00
CPC分类号： C07D257/04 , C07D403/10 , Y02P20/55
摘要： The invention provides a production method of a biaryltetrazole derivative useful as an intermediate for an angiotensin II receptor antagonist.The method comprises reacting an aryltetrazole derivative with a benzene derivative, deprotecting or reducing the resulting compound and halogenating the deprotected or reduced compound.
摘要翻译：本发明提供了可用作血管紧张素II受体拮抗剂中间体的联芳基四唑衍生物的制备方法。该方法包括使芳基四唑衍生物与苯衍生物反应，使得到的化合物脱保护或还原，并将脱保护或还原的化合物卤化。

3. 发明授权

US08455657B2 Process for the preparation of 3-alkylsulfinylbenzoyl derivatives 有权
标题翻译： 3-烷基亚磺酰基苯甲酰基衍生物的制备方法
公开(公告)号：US08455657B2
公开(公告)日：2013-06-04
申请号：US13335662
申请日：2011-12-22
申请人： Mark James Ford , Jan Peter Schmidt , Helmut Kohlhepp
发明人： Mark James Ford , Jan Peter Schmidt , Helmut Kohlhepp
IPC分类号： C07D271/08 , C07D271/10 , C07D271/00 , C07D257/04 , C07D249/00 , C07D231/10 , C07C319/00
CPC分类号： C07C315/04 , C07C2601/16 , C07D231/20 , C07C317/46
摘要： A process is described for the preparation of 3-alkylsulfinylbenzoyl derivatives of the formula (IIIa) by reaction of 3-alkylsulfinylbenzoic acids of the formula (Ib) with compounds of the formula (II) in the presence of a chlorinating agent and a base. In the formulae specified above, Y is a radical such as pyrazolyl and cyclohexanedionyl. R1, R2 and R3 are radicals such as halogen, nitro, cyano and alkyl.
摘要翻译：描述了通过在氯化剂和碱的存在下使式（Ib）的3-烷基亚磺酰基苯甲酸与式（II）的化合物反应来制备式（IIIa）的3-烷基亚磺酰基苯甲酰基衍生物的方法。在上述式中，Y是吡唑基和环己二酰基等基团。 R1，R2和R3是卤素，硝基，氰基和烷基等基团。

4. 发明授权

US08450350B2 Triazoles as inhibitors of fatty acid synthase 有权
标题翻译：三唑作为脂肪酸合酶的抑制剂
公开(公告)号：US08450350B2
公开(公告)日：2013-05-28
申请号：US13101970
申请日：2011-05-05
申请人： Adilah Bahadoor , Alfredo C. Castro , Lawrence K. Chan , Gregg F. Keaney , Marta Nevalainen , Vesa Nevalainen , Stephane Peluso , Thomas T. Tibbitts
发明人： Adilah Bahadoor , Alfredo C. Castro , Lawrence K. Chan , Gregg F. Keaney , Marta Nevalainen , Vesa Nevalainen , Stephane Peluso , Thomas T. Tibbitts
IPC分类号： A61K31/41 , A61K31/4192 , C07D249/00 , C07D249/06
CPC分类号： A61K31/4192 , A61K31/454 , A61K31/4709 , A61K45/06 , C07D249/04 , C07D249/06 , C07D249/18 , C07D401/06 , C07D401/12 , C07D471/04
摘要： Provided herein are triazole FASN inhibitors of the formula (I): or a pharmaceutically acceptable form thereof; wherein the variables RA, X, RB, and RC are defined herein. Also provided herein are pharmaceutical compositions of the compounds provided herein as well as methods of their use for the treatment of various disorders such as hyperproliferative disorders, inflammatory disorders, obesity-related disorders and microbial infections.
摘要翻译：本文提供式（I）的三唑FASN抑制剂：或其药学上可接受的形式; 其中变量RA，X，RB和RC在本文中定义。本文还提供本文提供的化合物的药物组合物及其用于治疗各种疾病如过度增殖性疾病，炎症性疾病，肥胖相关病症和微生物感染的方法。

5. 发明授权

US08436027B2 Azole compounds used as tuberculostatic and leishmanicide agents 有权
标题翻译：用作结核菌和利什曼替尼剂的唑类化合物
公开(公告)号：US08436027B2
公开(公告)日：2013-05-07
申请号：US12981315
申请日：2010-12-29
申请人： Nubia Boechat , Marilia dos Santos Costa , Maria Cristina da Silva Lourenço , Ivan Neves, Jr. , Marcelo da Silva Genestra , Vitor Francisco Ferreira
发明人： Nubia Boechat , Marilia dos Santos Costa , Maria Cristina da Silva Lourenço , Ivan Neves, Jr. , Marcelo da Silva Genestra , Vitor Francisco Ferreira
IPC分类号： A61K31/41 , C07D249/00
CPC分类号： A61K31/4192 , C07D233/90 , C07D249/06
摘要： This invention refers to new 1,2,3-triazole and imidazole compounds included in the families of compounds represented by general formula VIII. This invention also refers to a pharmaceutical composition comprising at least one of the azole compounds represented by the general formula VIII, to the use of such compositions and to methods of treatment or inhibition of tuberculosis and leishmaniasis.
摘要翻译：本发明涉及由通式VIII表示的化合物族中包括的新的1,2,3-三唑和咪唑化合物。本发明还涉及药物组合物，其包含至少一种由通式VIII表示的唑类化合物，该组合物的用途以及治疗或抑制结核病和利什曼病的方法。

6. 发明授权

US08389739B1 Modulators of retinoid-related orphan receptor gamma 有权
标题翻译：类视黄醇相关孤儿受体γ的调节剂
公开(公告)号：US08389739B1
公开(公告)日：2013-03-05
申请号：US13114616
申请日：2011-05-24
申请人： Scott Thacher , Xiaolin Li , Robert Babine , Bruno Tse
发明人： Scott Thacher , Xiaolin Li , Robert Babine , Bruno Tse
IPC分类号： C07D249/08 , C07D249/00 , C07D251/00 , C07D251/40 , A01N41/06 , A01N37/00 , A61K31/58
CPC分类号： C07J9/005 , A61K31/58 , C07C311/21 , C07D249/12 , C07D401/14 , C07D493/10 , C07J9/00 , C07J21/00
摘要： Methods for modulating (inhibiting or stimulating) retinoid-related orphan receptor γ (RORγ) activity. This modulation has numerous effects, including inhibition of TH-17 cell function and/or TH-17 cell activity, and inhibition of re-stimulation of TH-17 cells, which are beneficial to treatment of inflammation and autoimmune disorders. Stimulation of RORγ results in stimulation of TH-17 cell function and/or activity which is beneficial for immune-enhancing compositions (e.g., vaccines).
摘要翻译：调节（抑制或刺激）类视黄醇相关孤儿受体γ（RORγ）活性的方法。这种调节具有许多作用，包括TH-17细胞功能和/或TH-17细胞活性的抑制，以及TH-17细胞再刺激的抑制，这有利于治疗炎症和自身免疫性疾病。刺激RORγ导致TH-17细胞功能和/或活性的刺激，这有利于免疫增强组合物（例如疫苗）。

7. 发明授权

US08389557B2 Triazole derivatives useful as Axl inhibitors 有权
标题翻译：用作Axl抑制剂的三唑衍生物
公开(公告)号：US08389557B2
公开(公告)日：2013-03-05
申请号：US12965545
申请日：2010-12-10
申请人： Rajinder Singh , Catherine Sylvain , Sacha Holland , Jing Zhang , John J. Partridge , Jeffrey Clough , Ankush Argade
发明人： Rajinder Singh , Catherine Sylvain , Sacha Holland , Jing Zhang , John J. Partridge , Jeffrey Clough , Ankush Argade
IPC分类号： A61K31/41 , C07D249/00
CPC分类号： C07D403/12 , C07D249/14 , C07D405/12 , C07D413/12 , C07D417/12
摘要： Methods of using triazole derivatives in treating diseases or conditions associated with Axl catalytic activity are disclosed.
摘要翻译：公开了使用三唑衍生物治疗与Axl催化活性有关的疾病或病症的方法。

8. 发明授权

US08293777B2 Angiotensin II receptor antagonists 失效
标题翻译：血管紧张素II受体拮抗剂
公开(公告)号：US08293777B2
公开(公告)日：2012-10-23
申请号：US12629419
申请日：2009-12-02
申请人： Michael Man-Chu Lo , Amjad Ali , Ravi P. Nargund
发明人： Michael Man-Chu Lo , Amjad Ali , Ravi P. Nargund
IPC分类号： A61K31/34 , A61K31/41 , C07D249/00 , C07D409/02
CPC分类号： C07D403/10 , C07D235/08 , C07D257/04 , C07D409/06
摘要： A compound having the structure wherein R is an angiotensin receptor antagonist active group, and Y is Y is selected from the group consisting of R1 is selected from the group consisting of —O—C1-6 alkyl, —O-aryl, —O-heteroaryl, —O—C3-8 cycloalkyl, —C1-6 alkyl, -aryl, -heteroaryl, and —C3-8 cycloalkyl; R2 and R3 are independently selected from the group consisting of hydrogen and C1-4 alkyl, or a pharmaceutically acceptable salt or hydrate thereof, which is useful for treating hypertension.
摘要翻译：具有其中R为血管紧张素受体拮抗剂活性基团且Y为Y的结构的化合物选自R 1选自-O-C 1-6烷基，-O-芳基，-O- 杂芳基，-O-C 3-8环烷基，-C 1-6烷基， - 芳基， - 杂芳基和-C 3-8环烷基; R2和R3独立地选自氢和C 1-4烷基，或其药学上可接受的盐或水合物，其可用于治疗高血压。

9. 发明授权

US08288399B2 Medicine containing pyrimidine derivative 失效
标题翻译：含有嘧啶衍生物的药物
公开(公告)号：US08288399B2
公开(公告)日：2012-10-16
申请号：US12222599
申请日：2008-08-12
申请人： Tomiichiro Oda , Shigeko Uryu , Shinya Tokuhiro
发明人： Tomiichiro Oda , Shigeko Uryu , Shinya Tokuhiro
IPC分类号： A61K31/519 , A61K31/4196 , A61K31/407 , C07D487/14 , C07D249/00 , C07D487/12
CPC分类号： C07D487/14 , A61K31/519
摘要： Method for treating Alzheimer's disease, Parkinson's disease, Huntington's chorea or Pick's disease by administering to a patient a compound of formula (I) wherein R1 represents hydrogen; R2 represents hydrogen, a C1-C6 alkyl group or C3-C6 cycloalkyl group; A represents nitrogen; D represents a methylene group, a methyl methylene group, a halogen atom substituted methylene group or a halogen substituted methyl methylene group; E represents CH2, CHR3 wherein R3 represents a C1-C6 alkyl group, CH or a carbon atom substituted by a C1-C6 alkyl group; Arom represents aryl, aryl having from 1 to 3 identical or different substituent groups selected from halogen, C1-C6 alkyl, and C1-C6 alkyloxy, heteroaryl or heteroaryl having from 1 to 3 substituent groups, selected from halogen, C1-C6 alkyl and C1-C6 alkyloxy. The part represented by is a single bond or double bond.
摘要翻译：通过向患者施用其中R 1表示氢的式（I）化合物治疗阿尔茨海默氏病，帕金森氏症，亨廷顿氏舞蹈病或皮克病的方法， R2表示氢，C1-C6烷基或C3-C6环烷基; A表示氮; D表示亚甲基，甲基亚甲基，卤素原子取代的亚甲基或卤素取代的甲基亚甲基; E表示CH 2，CHR 3，其中R 3表示C 1 -C 6烷基，CH或被C 1 -C 6烷基取代的碳原子; Arom表示芳基，具有1至3个选自卤素，C 1 -C 6烷基和C 1 -C 6烷氧基，具有1至3个取代基的杂芳基或杂芳基的1至3个相同或不同的取代基的芳基，其选自卤素，C 1 -C 6烷基和 C1-C6烷氧基。所代表的部分是单键或双键。

10. 发明授权

US08269018B2 Pyrazolotriazole compound and electrophotographic toner 有权
标题翻译：吡唑并三唑化合物和电子照相调色剂
公开(公告)号：US08269018B2
公开(公告)日：2012-09-18
申请号：US13192110
申请日：2011-07-27
申请人： Kimihiko Ookubo , Ryohei Iwamoto , Koji Daifuku , Keiko Ishidai , Kaori Ono , Issei Nakahara
发明人： Kimihiko Ookubo , Ryohei Iwamoto , Koji Daifuku , Keiko Ishidai , Kaori Ono , Issei Nakahara
IPC分类号： C07D249/00 , G03G9/09
CPC分类号： C09B23/04 , G03G9/0906 , G03G9/0924
摘要： A compound represented by Formula (X-1) is disclosed. in the formula, Rx1 and Rx2 each independently represents an alkyl group, Lx is a hydrogen atom or an alkyl group, Gx1 is an alkyl group having 2 or more carbon atoms, Gx2 is an alkyl group or an aromatic hydrocarbon group, Gx3 is a hydrogen atom, a halogen atom, a Gx4-CO—NH— group or a Gx5-N(Gx6)-CO—group, Gx5 and Gx6 each independently represents a hydrogen atom or a substituent, and Qx1, Qx2, Qx3, Qx4 and Qx5 each independently represents a hydrogen atom or a substituent. An electrophotographic toner containing the compound is also disclosed.
摘要翻译：公开了由式（X-1）表示的化合物。在式中，Rx1和Rx2各自独立地表示烷基，Lx是氢原子或烷基，Gx1是具有2个以上碳原子的烷基，Gx2是烷基或芳香族烃基，Gx3是氢原子，卤原子，Gx4-CO-NH基或Gx5-N（Gx6）-CO-基，Gx5和Gx6各自独立地表示氢原子或取代基，Qx1，Qx2，Qx3，Qx4和 Qx5各自独立地表示氢原子或取代基。还公开了含有该化合物的电子照相调色剂。

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