公开(公告)号：US09518040B2

公开(公告)日：2016-12-13

申请号：US14833689

申请日：2015-08-24

Applicant: Rigel Pharmaceuticals, Inc.

Inventor： Somasekhar Bhamidipati ,  Marina Gelman ,  Pingyu Ding ,  Rajinder Singh ,  Jeffrey Clough ,  Todd Kinsella ,  Donald Payan

IPC: C07D405/04 ,  C07D487/04 ,  C07D453/02 ,  C07D417/14 ,  C07D401/04 ,  C07F9/6503 ,  C07D417/04 ,  C07D471/04 ,  C07D405/14 ,  C07D401/14 ,  C07D213/26 ,  C07D498/04 ,  C07D413/04 ,  C07D513/04

CPC classification number: C07D401/04 ,  C07D213/26 ,  C07D401/14 ,  C07D405/04 ,  C07D405/14 ,  C07D413/04 ,  C07D417/04 ,  C07D417/14 ,  C07D453/02 ,  C07D471/04 ,  C07D487/04 ,  C07D498/04 ,  C07D513/04 ,  C07F9/65038

Abstract: Described are GCF-8 inhibitors of the formula (I), and pharmaceutically acceptable salts thereof, wherein n, R1, R2, R5, R6, X and Z are defined herein. Also provided are pharmaceutical compositions comprising the same. Such compounds and compositions are useful in methods for inhibiting GDF-8 in a cell and methods for treating a patient suffering from a disease or disorder, wherein the patient would therapeutically benefit from an increase in mass or strength of muscle tissue.

公开(公告)号：US09108993B2

公开(公告)日：2015-08-18

申请号：US14187586

申请日：2014-02-24

Applicant: Allergan, Inc.

Inventor： Janet A. Takeuchi ,  Ling Li ,  Wha Bin Im ,  Ken Chow

IPC: A61K31/415 ,  C07F9/06 ,  C07F9/6503 ,  C07D231/54

CPC classification number: C07F9/65038 ,  C07D231/54

Abstract: The present invention relates to pyrazole derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.

Abstract translation: 本发明涉及吡唑衍生物，其制备方法，含有它们的药物组合物及其作为药物作为鞘氨醇-1-磷酸受体调节剂的用途。

公开(公告)号：US20120277190A1

公开(公告)日：2012-11-01

申请号：US13544130

申请日：2012-07-09

Applicant: Arthur R. Gomtsyan ,  Erol K. Bayburt ,  John R. Koenig ,  Kennan C. Marsh ,  Robert G. Schmidt, JR. ,  Chih-Hung Lee ,  Weili Wang ,  Jerome F. Daanen ,  Brian S. Brown

Inventor： Arthur R. Gomtsyan ,  Erol K. Bayburt ,  John R. Koenig ,  Kennan C. Marsh ,  Robert G. Schmidt, JR. ,  Chih-Hung Lee ,  Weili Wang ,  Jerome F. Daanen ,  Brian S. Brown

IPC: A61K31/5377 ,  C07D231/56 ,  A61K31/416 ,  A61P13/10 ,  A61K31/454 ,  C07F9/09 ,  A61K31/675 ,  A61P25/00 ,  C07D413/06 ,  C07D401/12

CPC classification number: C07D405/12 ,  C07D231/56 ,  C07D403/12 ,  C07F9/65038

Abstract: Compounds of formula (I) wherein A, R1, R2, and R3 are defined in the specification, and which are useful as therapeutic compounds particularly for treating disorders or conditions associated with inflammation, pain, bladder overactivity, urinary incontinence, and other disorders caused by or exacerbated by TRPV1.

Abstract translation: 其中A，R 1，R 2和R 3在本说明书中定义并且可用作特别用于治疗与炎症，疼痛，膀胱过度活动，尿失禁和其他疾病相关的疾病或病症的治疗化合物的式（I）化合物 由TRPV1引起或加剧。

公开(公告)号：US07547720B2

公开(公告)日：2009-06-16

申请号：US11641212

申请日：2006-12-19

Applicant: James B. Doherty ,  Meng-Hsin Chen ,  Luping Liu ,  Swaminathan R. Natarajan ,  Robert M. Tynebor

Inventor： James B. Doherty ,  Meng-Hsin Chen ,  Luping Liu ,  Swaminathan R. Natarajan ,  Robert M. Tynebor

IPC: A61K31/416 ,  C07D231/56

CPC classification number: C07F9/65038 ,  C07D231/56

Abstract: This invention relates to potent potassium channel blocker compounds of Formula I or a formulation thereof for the treatment of glaucoma and other conditions which leads to elevated intraocular pressure in the eye of a patient. This invention also relates to the use of such compounds to provide a neuroprotective effect to the eye of mammalian species, particularly humans.

公开(公告)号：US20070010491A1

公开(公告)日：2007-01-11

申请号：US10569921

申请日：2004-08-31

Applicant: Meng Hsin Chen ,  James Doherty ,  Luping Liu ,  Swaminathan Natarajan ,  Robert Tynebor

Inventor： Meng Hsin Chen ,  James Doherty ,  Luping Liu ,  Swaminathan Natarajan ,  Robert Tynebor

IPC: A61K31/4439 ,  A61K31/675

CPC classification number: C07D401/06 ,  C07F9/65038 ,  C07F9/65583

Abstract: This invention relates to potent potassium channel blocker compounds of Formula (I) or a formulation thereof for the treatment of glaucoma and other conditions which leads to elevated intraoccular pressure in the eye of a patient. This invention also relates to the use of such compounds to provide a neuroprotective effect to the eye of mammalian species, particularly humans, or a pharmaceutically acceptable salt, in vivo hydrolysable ester, enantiomer, diastereomer or mixture thereof: formula (II) represents C6-10 aryl or C3-10 heterocyclyl, said aryl or heterocyclyl optionally substituted with 1-3 groups selected from Ra; Z represents (CH2)nPO(OR)(OR*).

Abstract translation: 本发明涉及式（I）的有效钾通道阻断剂化合物或其制剂用于治疗青光眼和导致患者眼睛中眼内压升高的其它病症。 本发明还涉及这些化合物对哺乳动物物种，特别是人类或其药学上可接受的盐，体内可水解的酯，对映异构体，非对映体或其混合物的眼睛的神经保护作用的用途：式（II） 所述芳基或杂环基任选被1-3个选自R a，R b，R 3，R 3，R 3， Z表示（CH 2）n PO（OR）（OR *）。

公开(公告)号：US06828427B1

公开(公告)日：2004-12-07

申请号：US08973381

申请日：1998-03-25

Applicant: Normand Hebert

Inventor： Normand Hebert

IPC: C07H2100

CPC classification number: C07D207/337 ,  B01J2219/00592 ,  B01J2219/00695 ,  C07D207/12 ,  C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D401/06 ,  C07D401/14 ,  C07D403/06 ,  C07D413/06 ,  C07D417/12 ,  C07D473/34 ,  C07F9/143 ,  C07F9/2408 ,  C07F9/2429 ,  C07F9/572 ,  C07F9/5728 ,  C07F9/59 ,  C07F9/65031 ,  C07F9/65038 ,  C07F9/6506 ,  C07F9/6512 ,  C07F9/6521 ,  C07F9/6533 ,  C07F9/65335 ,  C07F9/6547 ,  C07F9/6561 ,  C07F9/65616 ,  C07H21/00 ,  C12Q1/6811 ,  C40B40/04 ,  C40B50/14

Abstract: Oligomeric compounds comprising a plurality of aminodiol monomer subunits joined by linking groups are provided, as well as libraries of such compounds and processes for preparing the oligomeric compounds and libraries.

Abstract translation: 提供了包含通过连接基团连接的多个氨基二醇单体亚基的低聚化合物，以及这些化合物的文库和制备低聚化合物和文库的方法。

公开(公告)号：US20030065146A1

公开(公告)日：2003-04-03

申请号：US10162365

申请日：2002-06-03

Inventor： Phillip D. Cook ,  Oscar L. Acevedo ,  Peter W. Davis ,  David J. Ecker ,  Normand Hebert

IPC: C07K014/00 ,  C07F009/6512

CPC classification number: C07H21/00 ,  B01J2219/00592 ,  B01J2219/00695 ,  C07B2200/11 ,  C07F9/143 ,  C07F9/2408 ,  C07F9/2429 ,  C07F9/572 ,  C07F9/5728 ,  C07F9/59 ,  C07F9/65031 ,  C07F9/65038 ,  C07F9/6506 ,  C07F9/6512 ,  C07F9/6521 ,  C07F9/6533 ,  C07F9/65335 ,  C07F9/6547 ,  C07F9/6561 ,  C07F9/65616

Abstract: Novel ethylene glycol compounds bearing various functional groups are used to prepare oligomeric structures. The ethylene glycol monomers can be joined via standard phosphate linkages including phosphodiester and phosphorothioate linkages. Useful functional groups include nucleobases as well as polar groups, hydrophobic groups, ionic groups, aromatic groups and/or groups that participate in hydrogen-bonding.

Abstract translation: 使用具有各种官能团的新型乙二醇化合物来制备低聚结构。 乙二醇单体可以通过包括磷酸二酯和硫代磷酸酯键的标准磷酸键连接。 有用的官能团包括核碱基以及参与氢键的极性基团，疏水基团，离子基团，芳族基团和/或基团。

公开(公告)号：US06175007B1

公开(公告)日：2001-01-16

申请号：US09117665

申请日：1998-08-04

Applicant: Cyrill Zagar ,  Elisabeth Heistracher ,  Olaf Menke ,  Gerhard Hamprecht ,  Markus Menges ,  Peter Sch{umlaut over (a)}fer ,  Karl-Otto Westphalen ,  Ulf Misslitz ,  Helmut Walter

Inventor： Cyrill Zagar ,  Elisabeth Heistracher ,  Olaf Menke ,  Gerhard Hamprecht ,  Markus Menges ,  Peter Sch{umlaut over (a)}fer ,  Karl-Otto Westphalen ,  Ulf Misslitz ,  Helmut Walter

IPC: C07D27300

CPC classification number: C07F9/6561 ,  A01N57/24 ,  A01N57/32 ,  C07F9/4015 ,  C07F9/4056 ,  C07F9/5537 ,  C07F9/65031 ,  C07F9/65038 ,  C07F9/6506 ,  C07F9/650905 ,  C07F9/6512 ,  C07F9/6539 ,  C07F9/65583 ,  C07F9/65586

Abstract: Phosphonic acid compounds I wherein Eth is optionally substituted 1,2-ethynediyl, ethanediyl or ethene-1,2-diyl; Y1 is oxygen or sulfur; Y2 is oxygen, sulfur or —N(R6)—; Y3 is oxygen, sulfur or —N(R7)—; R1, R2, R6 and R7 are hydrogen or optionally substituted alkyl, alkenyl, alkynyl, cycloalkyl, phenyl or heterocyclyl, or R1 and R2, R1 and R6, R2 and R7 together are optionally substituted 1,2-ethanediyl, 1,3-propylene, tetramethylene, pentamethylene or ethyleneoxyethylene, or R1 and R2 together are optionally substituted 1,2-phenylene; R3 is cyano, halogen, alkyl, haloalkyl, alkoxy or haloalkoxy; R4 is hydrogen or halogen, and R5 is a heterocycle &PHgr;1 to &PHgr;22 as defined in the specification, their manufacture and intermediates therefore. The phosphonic acid compounds are effective against unwanted plants and act as desiccants and defoliants.

Abstract translation: 膦酸化合物Ⅰ其中任选被取代的1,2-亚乙炔基，乙二基或乙烯-1,2-二基; Y1是氧或硫; Y2是氧，硫或-N（R6） - ; Y3是氧，硫或-N （R 7） - ; R 1，R 2，R 6和R 7是氢或取代的烷基，烯基，炔基，环烷基，苯基或杂环基，或R 1和R 2，R 1和R 6，R 2和R 7一起是任选取代的1,2-乙二基， ，3-亚丙基，四亚甲基，五亚甲基或亚乙基氧乙烯，或者R 1和R 2一起是任选取代的1,2-亚苯基; R 3是氰基，卤素，烷基，卤代烷基，烷氧基或卤代烷氧基; R 4是氢或卤素，R 5是杂环＆ 1至＆lt; PHgr 22，因此其制造和中间体。 膦酸化合物对有害植物有效，作为干燥剂和脱叶剂。

公开(公告)号：US3729481A

公开(公告)日：1973-04-24

申请号：US3729481D

申请日：1971-05-24

Applicant: TENNECO CHEM

Inventor： MINIERI P

IPC: C07D231/56 ,  C07F9/24 ,  C07F9/6503 ,  C09D5/14 ,  C07D49/18

CPC classification number: C09D5/14 ,  C07D231/56 ,  C07F9/24 ,  C07F9/65032 ,  C07F9/65038

Abstract: COMPOUNDS THAT HAVE THE STRUCTURAL FORMULA

1-(X-CH2-COO-CH2-),3-Z,YN-1H-INDAZOLE

WHEREIN X REPRESENTS HALOGEN OR THIOCYANATO, Y REPRESENTS HALOGEN OR NITRO, Z REPRESENTS HALOGEN OR HYDROGEN, AND N IS AN INTEGER IN THE RANGE OF ZERO TO 2 CAN BE USED TO CONTROL THE GROWTH OF VARIOUS PLANT AND ANIMAL PESTS. AMONG THE MOST ACTIVE OF THESE COMPOUNDS IS N1-THIOCYANATOACETOXYMETHYL-6-NITROINDAZOLE.

公开(公告)号：US3729480A

公开(公告)日：1973-04-24

申请号：US3729480D

申请日：1971-05-24

Applicant: TENNECO CHEM

Inventor： MINIERI P

IPC: C07D231/56 ,  C07F9/24 ,  C07F9/6503 ,  C09D5/14 ,  C07D49/18

CPC classification number: C09D5/14 ,  C07D231/56 ,  C07F9/24 ,  C07F9/65032 ,  C07F9/65038

Abstract: COMPOUNDS THAT HAVE THE STRUCTURAL FORMULA

1-(X-CH2-CO-),3-Z,YN-1H-INDAZOLE

WHEREIN X REPRESENTS HALOGEN, PHENOXY, OR THIOCYANATO, Y REPRESENTS HALOGEN OR NITRO, Z REPRESENTS HALOGEN OR HYDROGEN, AND N IS AN INTEGER IN THE RANGE OF ZERO TO 2 CAN BE USED TO CONTROL THE GROWTH OF VARIOUS PLANT AND ANIMAL PESTS. AMONG THE MOST ACTIVE OF THESE COMPOUNDS IS N1-CHLOROACETYL6-NITROINDAZOLE.