公开(公告)号：US20230112865A1

公开(公告)日：2023-04-13

申请号：US17843194

申请日：2022-06-17

申请人： Rigel Pharmaceuticals, Inc.

发明人： Yan CHEN ,  Jiaxin YU ,  Simon SHAW ,  Ihab DARWISH ,  Vanessa TAYLOR ,  Somasekhar BHAMIDIPATI ,  Zhushou LUO ,  Rao KOLLURI

IPC分类号： C07D401/14 ,  C07D401/12 ,  C07D403/12 ,  C07D403/14 ,  C07D405/14 ,  C07D471/08 ,  C07D487/04 ,  C07D491/107 ,  A61K31/553 ,  C07D267/02 ,  C07D413/12 ,  C07D413/14 ,  C07D493/04

摘要： Disclosed herein are kinase inhibitory compounds, such as a receptor-interacting protein-1 (RIP1) kinase inhibitor compounds, as well as pharmaceutical compositions and combinations comprising such inhibitory compounds. The disclosed compounds, pharmaceutical compositions, and/or combinations may be used to treat or prevent a kinase-associated disease or condition, particularly a RIP1-associated disease or condition.

公开(公告)号：US20230082516A1

公开(公告)日：2023-03-16

申请号：US17417201

申请日：2020-01-07

申请人： KYORIN PHARMACEUTICAL CO., LTD.

发明人： Shigeki SETO ,  Hitomi YAMADA ,  Yoshifumi SAITO ,  Haruaki KURASAKI

IPC分类号： C07D265/36 ,  C07D267/02 ,  C07D267/22 ,  C07D498/04 ,  C07D281/02 ,  C07D519/00 ,  C07D279/16 ,  C07D471/04

摘要： [Problem]
To provide a compound having a 15-PGDH inhibitory effect.
[Solution]
A compound represented by general formula (1) or a pharmacologically acceptable salt thereof.

公开(公告)号：US11407736B2

公开(公告)日：2022-08-09

申请号：US17012779

申请日：2020-09-04

申请人： Rigel Pharmaceuticals, Inc.

发明人： Yan Chen ,  Jiaxin Yu ,  Simon Shaw ,  Ihab Darwish ,  Vanessa Taylor ,  Somasekhar Bhamidipati ,  Zhushou Luo ,  Rao Kolluri

IPC分类号： C07D471/04 ,  C07D491/048 ,  C07D495/04 ,  C07D513/04 ,  A61K31/55 ,  A61K31/5517 ,  A61K31/54 ,  C07D401/14 ,  C07D401/12 ,  C07D403/12 ,  C07D403/14 ,  C07D405/14 ,  C07D471/08 ,  C07D487/04 ,  C07D491/107 ,  A61K31/553 ,  C07D267/02 ,  C07D413/12 ,  C07D413/14 ,  C07D493/04

摘要： Disclosed herein are kinase inhibitory compounds, such as a receptor-interacting protein-1 (RIP1) kinase inhibitor compounds, as well as pharmaceutical compositions and combinations comprising such inhibitory compounds. The disclosed compounds, pharmaceutical compositions, and/or combinations may be used to treat or prevent a kinase-associated disease or condition, particularly a RIP1-associated disease or condition.

公开(公告)号：US09783507B2

公开(公告)日：2017-10-10

申请号：US15419217

申请日：2017-01-30

申请人： THERAVANCE BIOPHARMA R&D IP, LLC

发明人： Melissa Fleury ,  Anne-Marie Beausoliel ,  Adam D. Hughes ,  Daniel D. Long ,  Donna A. A. Wilton

IPC分类号： C07D295/24 ,  C07D205/04 ,  C07D267/02 ,  C07D317/10 ,  C07D249/04 ,  C07D249/10 ,  C07D231/14 ,  C07D261/18 ,  C07D263/34 ,  C07D263/38 ,  C07D271/07 ,  C07D213/81 ,  C07D239/28 ,  C07D231/20 ,  C07D275/03 ,  C07D471/04 ,  C07D403/12

CPC分类号： C07D249/04 ,  A61K31/415 ,  A61K31/4192 ,  A61K31/4196 ,  A61K31/42 ,  A61K31/421 ,  A61K31/4245 ,  A61K31/425 ,  A61K31/437 ,  A61K31/44 ,  A61K31/4985 ,  A61K31/505 ,  A61K45/06 ,  A61P9/04 ,  A61P9/12 ,  A61P13/12 ,  C07C229/34 ,  C07C271/22 ,  C07D213/81 ,  C07D231/14 ,  C07D231/18 ,  C07D231/20 ,  C07D233/70 ,  C07D233/90 ,  C07D235/08 ,  C07D237/14 ,  C07D239/28 ,  C07D239/34 ,  C07D249/10 ,  C07D249/12 ,  C07D249/18 ,  C07D261/12 ,  C07D261/18 ,  C07D263/18 ,  C07D263/34 ,  C07D263/38 ,  C07D271/07 ,  C07D275/03 ,  C07D295/10 ,  C07D309/40 ,  C07D319/06 ,  C07D401/04 ,  C07D403/04 ,  C07D403/06 ,  C07D403/12 ,  C07D405/12 ,  C07D405/14 ,  C07D471/04

摘要： In one aspect, the invention relates to compounds having the formula I: where R1-R6 are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising these compounds; methods of using these compounds; and processes and intermediates for preparing these compounds.

公开(公告)号：US08309540B2

公开(公告)日：2012-11-13

申请号：US12446763

申请日：2007-10-22

申请人： Nigel J. Liverton ,  Joseph P. Vacca ,  John A. McCauley ,  Joseph J. Romano ,  Michael T. Rudd

发明人： Nigel J. Liverton ,  Joseph P. Vacca ,  John A. McCauley ,  Joseph J. Romano ,  Michael T. Rudd

IPC分类号： A61K31/33 ,  A61K31/47 ,  C07D201/16 ,  C07D223/00 ,  C07D267/02 ,  C07D273/00

CPC分类号： C07D498/18

摘要： The present invention relates to macrocyclic compounds of formula (I) that are useful as inhibitors of the hepatitis C virus (HCV) NS3 protease, their synthesis, and their use for treating or preventing HCV infections. (I)

摘要翻译： 本发明涉及可用作丙型肝炎病毒（HCV）NS3蛋白酶抑制剂及其合成及其用于治疗或预防HCV感染的用途的式（I）的大环化合物。 （一世）

公开(公告)号：US20100160627A1

公开(公告)日：2010-06-24

申请号：US12359465

申请日：2009-01-26

申请人： Bruce Thomas Dembofsky ,  Robert Jacobs ,  Cyrus Ohnmacht

发明人： Bruce Thomas Dembofsky ,  Robert Jacobs ,  Cyrus Ohnmacht

IPC分类号： C07D267/02

CPC分类号： C07K5/06034 ,  A61K38/00 ,  C07D223/16 ,  C07D267/10 ,  C07D267/14 ,  C07D281/06 ,  C07D281/10 ,  C07D405/04 ,  C07D417/12 ,  C07D417/14 ,  C07K5/06026 ,  C07K5/06191

摘要： Compounds having the formula (I) pharmaceutical compositions containing them and their methods of use for the treatment of neurological disorders related to amyloid β protein production and neurological disorders such as Alzheimer's disease. These compounds inhibit γ secretase and thereby inhibit the production of amyloid β protein, thereby acting to prevent the formation of neurological deposits of amyloid protein.

摘要翻译： 具有式（I）的药物组合物含有它们的化合物及其用于治疗与淀粉样蛋白相关的神经障碍的方法; 蛋白质生产和神经系统疾病如阿尔茨海默病。 这些化合物抑制γ分泌酶，从而抑制淀粉样蛋白的生成; 蛋白质，从而起到防止淀粉样蛋白质神经沉积的形成的作用。

公开(公告)号：US07507816B2

公开(公告)日：2009-03-24

申请号：US10866099

申请日：2004-06-14

申请人： Heinz Uragg ,  Corinna Maul ,  Helmut Buschmann ,  Bernd Sundermann ,  Hagen-Heinrich Hennies

发明人： Heinz Uragg ,  Corinna Maul ,  Helmut Buschmann ,  Bernd Sundermann ,  Hagen-Heinrich Hennies

IPC分类号： C07D267/02 ,  C07D267/04 ,  C07D267/06 ,  C07D267/08 ,  C07D267/10 ,  C07D281/02 ,  C07D281/04 ,  C07D281/06

CPC分类号： C07D295/096 ,  A61K31/40 ,  A61K31/445 ,  A61K31/535 ,  A61K31/55

摘要： Pharmaceutical compositions containing substituted aminoalcohols, the use of preparations containing substituted aminoalcohols for treatment of conditions such as pain, emesis, neurotropic conditions, cardiovascular diseases, urinary incontinence, diarrhea, pruritus, alcohol or drug dependency, inflammation, depression, decreased vigilance, or depressed libido, as well as 2-(aminomethyl)cycloalkane-1-ol compounds and a process for their preparation.

摘要翻译： 含有取代氨基醇的药物组合物，含有取代氨基醇的制剂用于治疗诸如疼痛，呕吐，神经营养状况，心血管疾病，尿失禁，腹泻，瘙痒，酒精或药物依赖性，炎症，抑郁，降低的警惕性或抑郁症 性状，以及2-（氨基甲基）环烷烃-1-醇化合物及其制备方法。

公开(公告)号：US20080287419A1

公开(公告)日：2008-11-20

申请号：US12120914

申请日：2008-05-15

申请人： Milan Bruncko ,  Hong Ding ,  Steven W. Elmore ,  Aaron R. Kunzer ,  Christopher L. Lynch ,  William J. McClellan ,  Cheol Min Park ,  Xiahong Song ,  Xilu Wang

发明人： Milan Bruncko ,  Hong Ding ,  Steven W. Elmore ,  Aaron R. Kunzer ,  Christopher L. Lynch ,  William J. McClellan ,  Cheol Min Park ,  Xiahong Song ,  Xilu Wang

IPC分类号： A61K31/553 ,  C07D413/02 ,  A61K31/5377 ,  C07D223/02 ,  A61K31/496 ,  A61P35/00 ,  C07D295/00 ,  A61K31/55 ,  C07D267/02

CPC分类号： C07D295/155 ,  C07D487/08 ,  C07D491/08

摘要： Compounds which inhibit the activity of anti-apoptotic family protein members, compositions containing the compounds and methods of treating diseases during which occur expression one or more than one of an anti-apoptotic family protein member are disclosed.

摘要翻译： 公开了抑制抗凋亡家族蛋白成员的活性的化合物，含有该化合物的组合物和治疗疾病的方法，其中表达一种或多种抗凋亡家族蛋白质成员。

公开(公告)号：US20080280881A1

公开(公告)日：2008-11-13

申请号：US12140686

申请日：2008-06-17

申请人： Jean-Francois Bonfanti ,  Koenraad Josef Lodewijk Andries ,  Jerome Michel Claude Fortin ,  Philippe Muller ,  Frederic Marc Maurice Doublet ,  Christophe Meyer ,  Rudy Edmond Willebrords ,  Tom Valerius Josepha Gevers ,  Philip Maria Martha Born Timmerman

发明人： Jean-Francois Bonfanti ,  Koenraad Josef Lodewijk Andries ,  Jerome Michel Claude Fortin ,  Philippe Muller ,  Frederic Marc Maurice Doublet ,  Christophe Meyer ,  Rudy Edmond Willebrords ,  Tom Valerius Josepha Gevers ,  Philip Maria Martha Born Timmerman

IPC分类号： A61K31/553 ,  C07D413/14 ,  A61K31/5377 ,  A61P31/12 ,  C07D267/02

CPC分类号： C07D413/12 ,  C07D401/06 ,  C07D401/14 ,  C07D413/14

摘要： The present invention concerns morpholinyl containing benzimidazoles having inhibitory activity on the replication of the respiratory syncytial virus and having the formula a prodrug, N-oxide, addition salt, quaternary amine, metal complex or stereochemically isomeric form thereof wherein G is a direct bond or optionally substituted C1-10alkanediyl; R1 is Ar1 or a monocyclic or bicyclic heterocycle Q is R7, pyrrolidinyl substituted with R7, piperidinyl substituted with R7 or homopiperidinyl substituted with R7; one of R2a and R3a is selected from halo, optionally mono- or polysubstituted C1-6alkyl, optionally mono- or polysubstituted C2-6alkenyl, nitro, hydroxy, Ar2, N(R4aR4b), N(R4aR4b)sulfonyl, N(R4aR4b)carbonyl, C1-6alkyloxy, Ar2oxy, Ar2C1-6alkyloxy, carboxyl, C1-6alkyloxycarbonyl, or —C(=Z)Ar2; and the other one of R2a and R3a is hydrogen; in case R2a is different from hydrogen then R2b is hydrogen, C1-6alkyl or halogen and R3b is hydrogen; in case R3a is different from hydrogen then R3b is hydrogen, C1-6alkyl or halogen and R2b is hydrogen. It further concerns the preparation thereof and compositions comprising these compounds, as well as the use thereof as a medicine.

公开(公告)号：US20080227770A1

公开(公告)日：2008-09-18

申请号：US10566883

申请日：2004-07-30

申请人： Shogo Marui ,  Takashi Miki ,  Shoutarou Miura ,  Tomoyuki Nishimoto ,  Yoshihisa Nakada

发明人： Shogo Marui ,  Takashi Miki ,  Shoutarou Miura ,  Tomoyuki Nishimoto ,  Yoshihisa Nakada

IPC分类号： A61K31/553 ,  C07D267/02 ,  A61P3/00

CPC分类号： C07D413/06 ,  C07D267/14 ,  C07D417/06

摘要： A compound represented by the formula [1]: wherein ring A and ring B each represent an optionally substituted benzene ring; ring C represents an optionally further substituted aromatic ring; R1 represents a lower alkyl group optionally substituted with an optionally substituted hydroxyl group; X1a represents a bond or optionally substituted lower alkylene; X1b represents a bond or optionally substituted lower alkylene; x2 represents a bond, —O— or —S—; X3 represents a bond or an optionally substituted divalent hydrocarbon group; Y represents an optionally esterified or amidated carboxyl group, or a salt thereof. The compound of the formula [I] is safer and has more potent lipid lowering activity such as squalene synthase inhibitory activity (cholesterol lowering activity) and triglyceride lowering activity, and thus it is a compound useful as an agent for preventing or treating hyperlipemia.

摘要翻译： 由式[1]表示的化合物：其中环A和环B各自表示任选取代的苯环; 环C表示任选进一步取代的芳环; R 1表示任选被任选取代的羟基取代的低级烷基; X 1a表示键或任选取代的低级亚烷基; X 1b表示键或任选取代的低级亚烷基; x 2表示键，-O-或-S-; X 3表示键或任选取代的二价烃基; Y表示任选酯化或酰胺化的羧基，或其盐。 式[I]的化合物更安全并且具有更强的降脂活性，例如角鲨烯合酶抑制活性（降胆固醇活性）和甘油三酯降低活性，因此它是可用作预防或治疗高脂血症的药剂的化合物。