公开(公告)号：EP2451788A1

公开(公告)日：2012-05-16

申请号：EP10737145.2

申请日：2010-07-07

申请人： Chelsea Therapeutics, Inc.

发明人： PIMPLASKAR, Harish K. ,  LEBEDEV, Mikhail ,  HORVATH, Karol

IPC分类号： C07D239/95 ,  A61K31/517 ,  A61P11/06 ,  A61P19/02 ,  A61P29/00 ,  A61P35/00

CPC分类号： C07D239/95

摘要： The present invention provides stable crystalline polymorphic forms of antifolate compounds, particularly (5)-2-{4-[2-(2,4-diamino-quinazolin-6-yl)-ethyl]- benzoylamino}-4-methylene-pentanedioic acid, dipotassium salt, and methods of preparation thereof. The polymorphs may be in the form of hydrates. The invention further provides pharmaceutical compositions comprising the polymorphs and methods of treatment using the polymorphs. The polymorphs are useful in the treatment of multiple conditions, including abnormal cell proliferation, inflammatory diseases, asthma, and arthritis, and the polymorphs may be administered alone in or combination with on or more further active agents.

公开(公告)号：EP2118051B1

公开(公告)日：2011-05-04

申请号：EP08712766.8

申请日：2008-01-31

申请人： Chelsea Therapeutics, Inc.

发明人： TUVESSON ANDERSSON, Helén ,  VELLMAR, Ulf ,  HALLIN, Ingrid ,  SVENSSON, Leif ,  FRITZSON, Ingela

IPC分类号： C07C233/54 ,  C07C233/63 ,  A61K31/196 ,  A61K31/245 ,  A61P29/00

CPC分类号： C07C233/54 ,  C07C233/63 ,  C07C2601/02

摘要： A compound of formula (I) wherein X is CH=CH, CH 2O wherein the oxygen atom is bound to ring B or OCH 2wherein the oxygen atom is bound to ring A; Y is hydrogen, straight or branched C1-C6 alkyl or a pharmaceutically acceptable inorganic cation; R1 is ethyl or cyclopropyl; and R2 and R3 are the same or different and are selected from F, Cl, Br, CF 3and OCF 3. The compound is useful for the treatment of autoimmune diseases, inflammatory diseases, organ transplant rejection and malignant neoplasia. A pharmaceutical composition. A method for preparing the compound.

公开(公告)号：EP2167066A2

公开(公告)日：2010-03-31

申请号：EP08769311.5

申请日：2008-05-07

申请人： Chelsea Therapeutics, Inc.

发明人： ROBERTS, Michael, J. ,  PEDDER, Simon

IPC分类号： A61K31/138 ,  A61K31/195 ,  A61K31/198 ,  A61K31/275 ,  A61K31/345

CPC分类号： A61K31/198 ,  A61K31/135 ,  A61K31/137 ,  A61K31/138 ,  A61K31/195 ,  A61K31/275 ,  A61K31/277 ,  A61K31/345 ,  A61K31/55 ,  A61K45/06 ,  A61K2300/00

摘要： The present invention provides pharmaceutical compositions comprising droxidopa alone, or in combination with one or more further active ingredients, for the treatment of conditions, such as mood disorders, sleep disorders, or attention deficit disorders. In certain embodiments, the compositions useful in the methods of the invention comprise droxidopa and a compound selected from the group consisting of DOPA decarboxylase inhibiting compounds, catechol-0-methyltransferase inhibiting compounds, cholinesterase inhibiting compounds, monoamine oxidase inhibiting compounds, norepinephrine reuptake inhibiting compounds, selective serotonin reuptake inhibiting compounds, tricyclic antidepressant compounds, serotonin norepinephrine reuptake inhibiting compounds, norepinephrine dopamine reuptake inhibiting compound, noradrenergic and specific serotonergic antidepressants, and combinations thereof. The inventive compositions are particularly useful in the treatment of depression, narcolepsy, insomnia, and Attention Deficit/Hyperactivity Disorder (AD/HD).

公开(公告)号：EP2125818A1

公开(公告)日：2009-12-02

申请号：EP08727890.9

申请日：2008-01-18

申请人： Chelsea Therapeutics, Inc.

发明人： ROBERTS, Michael, J. ,  PEDDER, Simon

IPC分类号： C07D487/04 ,  A61K31/519 ,  A61P35/00

CPC分类号： C07D487/04

摘要： The present invention is directed to antifolate compounds having the structure of formula (I). wherein: X is CHR9 or NR9; Y1, Y2, and Y3 independently are O or S; V1 and V2 independently are O, S, or NZ; Z is H, optionally substituted alkyl, optionally substituted alkenyl, optionally substituted alkynyl, or alkaryl; R1 and R2 independently are H, optionally substituted alkyl, optionally substituted alkenyl, optionally substituted alkynyl, or alkaryl; R3 is H, optionally substituted alkyl, optionally substituted alkenyl, optionally substituted alkynyl, optionally substituted alkoxy, hydroxyl, or halo; and R4, R5, R6, R7, Rs, and R9 independently are H, optionally substituted alkyl, optionally substituted alkenyl, optionally substituted alkynyl, acyl, -C(O)-alkyl, - C(O)-alkenyl, or -C(O)-alkynyl; as well as pharmaceutically acceptable esters, amides, salts, solvates, and prodrugs thereof. The compounds are useful in pharmaceutical compositions and in methods of treating multiple conditions, including abnormal cell proliferation, inflammatory diseases, asthma, and arthritis.