Patents

PCT/US2010/062310, December 29, 2010

Type II RAF kinase inhibitors

The present invention relates to novel compounds which are able to modulate b-raf kinases, and the use of such compounds in the treatment of various diseases, disorders or conditions.

PCT/US2010/061927, December 22, 2010

Compounds that modulate EGFR activity and methods for treating or preventing conditions therewith

Provided are compounds and methods for treating or preventing kinase-mediated disorders therewith.

PCT/US2010/038518, June 14, 2010

Fused heterocyclic compounds and their uses

The present application relates to therapeutic organic compounds, compositions comprising an effective amount of a therapeutic organic compound; and methods for treating and preventing disease comprising administering and effective amount of a therapeutic organic compound to a subject in need thereof.

PCT/US2010/001341, May 5, 2010

EGFR inhibitors and methods of treating disorders

The present invention relates to novel pyrimidine, pyrrolo-pyrimidine, pyrrolo-pyridine, pyridine, purine and triazine compounds which are able to modulate epidermal growth factor receptor (EGFR), including Her-kinases, and the use of such compounds in the treatment of various diseases, disorders or conditions.

PCT/US2010/000050, January 6, 2010

Pyrimido-Diazepinone kinase scaffold compounds and methods of treating disorders

The present invention relates to novel pyrimido-diazepinone compounds, methods of modulating protein kinases, including MPSl (TTK), ERK5 (BMKl, MAPK7), polo kinase 1,2,3, or 4, Ackl, Ack2, AbI, DCAMKLl, ABLl, AbI mutants, DCAMKL2, ARK5, BRK, MKNK2, FGFR4, TNKl, PLKl, ULK2, PLK4, PRKDl, PRKD2, PRKD3, ROS l, RPS6KA6, TAOKl, TAOK3, TNK2, Bcr-Abl, GAK, cSrc, TPR-Met, Tie2, MET, FGFR3, Aurora, AxI, Bmx, BTK, c-kit, CHK2, Flt3, MST2, p70S6K, PDGFR, PKB, PKC, Raf, ROCK-H, Rskl, SGK, TrkA, TrkB and TrkC, and the use of such compounds in the treatment of various diseases, disorders or conditions.

PCT/US2009/005656, October 16, 2009

Soluble mTOR complexes and modulators thereof

The present invention relates to small molecule modulators of mTORC1 and mTORC2, syntheses thereof, and intermediates thereto. Such small molecule modulators are useful in the treatment of proliferative diseases (e.g., benign neoplasms, cancers, inflammatory diseases, autoimmune diseases, diabetic retinopathy) and metabolic diseases. Novel small molecules are provided that inhibit one or more of mTORC1, mTORC2, and PI3K-related proteins. Novel methods of providing soluble mTORC1 and mTORC2 complexes are discussed, as well as methods of using the soluble complexes in a high-throughput manner to screen for inhibitory compounds.

PCT/US2009/047074, June 11, 2009

Compounds and compositions useful for the treatment of Malaria

The invention provides a class of compounds of formula I, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent malaria.

PCT/US2008/087344, December 18, 2008

Compositions and methods for treating cancers

This invention provides a combination of ATP-competitive BCR-ABL inhibitor and a non-ATP competitive BCR-ABL inhibitor. The combination of the present invention may be used for treating cancers known to be associated with BCR-ABL.

PCT/US2008/013219, November 28, 2008

Small molecule myristate inhibitors of BCR-ABL and methods of use

The present invention provides novel heteroaryl compounds that are linked to an aryl group via an amine linker. Such compounds are useful for the treatment of cancers.

PCT/US2008/074490, August 27, 2008

2-(HET) arylamino-6-aminopyridine derivatives and fused forms thereof as anaolastic lymphoma kinase inhibitors

This invention relates to novel amino substituted pyrimidine compounds of formula (I), pharmaceutical compositions containing such compounds and the use of those compounds or compositions for treating hyper-proliferative and/or angiogenesis disorders, as a sole agent or in combination with other active ingredients.

PCT/US2008/074472, August 27, 2008

Amino substituted pyrimidine pyrollopyridine and pyrazolopyrimidine derivatives useful as kinase inhibitors and in treating proliferative disorders and diseases associated with angiogenesis

This invention relates to novel amino subsituted pyrimidine compounds, pharmaceutical compositions containing such compounds and the use of those compounds or compositions for treating hyper-proliferative and/or angiogenesis disorders, as a sole agent or in combination with other active ingredients.

PCT/US2008/074392, August 27, 2008

2-biphenylamino-4-Aminopyrimidine derivatives as kinase inhibitors

The invention provides novel pyrimidine derivatives of formula (1) and pharmaceutical compositions thereof, and methods for using such compounds. For example, the pyrimidine derivatives of the invention may be used to treat, ameliorate or prevent a condition which responds to inhibition of insulin-like growth factor (IGF- 1 R) or anaplastic lymphoma kinase (ALK).

PCT/US2008/067290, June 18, 2008

Protein kinase inhibitors and methods for using thereof

The invention provides compounds and pharmaceutical compositions thereof, which are useful as protein kinase inhibitors, and methods for using such compounds to treat, ameliorate or prevent a condition associated with abnormal or deregulated kinase activity. In some embodiments, the invention provides methods for using such compounds to treat, ameliorate or prevent diseases or disorders that involve abnormal activation of AIk, AbI, Aurora- A, B-Raf, C- Raf, Bcr-Abl, BRK, BIk, Bmx, BTK, C-Kit, C-Raf, C-Src, EphB1, EphB2, EphB4, FGFR1, FGFR2, FGFR3, FLT1, Fms, Flt3, Fyn, FRK3, JAK2, KDR, Lck, Lyn, PDGFRα, PDGFRβ, PKCα, p38, Src, SIK, Syk, Tie2 and TrkB kinases.

PCT/US2008/063187, May 9, 2008

Protein kinase inhibitors and methods for using thereof

The invention provides compounds of formula (l) and pharmaceutical compositions thereof, which are useful as protein kinase inhibitors, and methods for using such compounds to treat, ameliorate or prevent a condition associated with abnormal or deregulated kinase activity. In some embodiments, the invention provides methods for using such compounds to treat, ameliorate or prevent diseases or disorders that involve abnormal activation of AIk, AbI, Aurora-A, B-Raf, C-Raf, Bcr-Abl, BRK, BIk, Bmx, BTK, c-Kit, c-RAF, CSK, c-SRC, EphBl, EphB2, EphB4, FLTl, Fms, Flt3, Fyn, FRK3, JAK2, KDR, Lck, Lyn, PDGFRalpha, PDGFRbeta, PKCalpha, SAPK2alpha, Src, SIK, Syk, Tie2 and TrkB kinases.

PCT/US2008/050807, January 10, 2008

Purine compounds and compositions as kinase inhibitors for the treatment of plasmodium related disease

The invention provides a class of purine derivates, pharmaceutical compositions comprising such compounds and the use of such compounds to treat or prevent diseases or disorders associated with kinase activity, particularly malaria.

PCT/US2007/008699, April 6, 2007

Compounds and methods for FGF receptor kinase inhibitors

Described are compounds, pharmaceutical compositions comprising such compounds, and methods of using such compounds to treat or prevent disease or disordered associated with abnormal or deregulated kinase activity, particularly diseases or disorders that involve abnormal activity of kinases such as AbI, ALK, AMPK, Aurora, AxI, Bcr-Abl, BIK, Bmx, BRK, BTK, c-Kit, CSK, cSrc, CDKl, CHK2, CKl, CK2, CaMKII, CaMKIV, DYRK2, EGFR, EphBl, FES, FGFRl, FGFR2, FGFR3, Fltl, FlO, FMS, Fyn, GSK3β, IGF lR, IKKα DCKβ, IR, IRAK4, ITK, JAK2, JAK3, JNKlαl, JNK2α, KDR, Lck, LYN, MAPKl, MAPKAP-K2, MEKl, MET, MKK4, MKK6, MST2, NEK2, NLK, p70S6K, PAK2, PDGFR, PDGFRα, PDKl, Pim-2, Plk3, PKA, PKBα, PKCα PKCtheta, PKD2, c-Raf, RET, ROCK-I1 ROCK-II, Ron, Ros, Rskl, SAPK2a, SAPK2b, SAPK3, SAPK4, SGK, SIK, Syk, Tie2, TrkB, WNK3, and ZAP-70.

PCT/US2007/003319, February 6, 2007

Compounds and compositions as protein kinase inhibitors

The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particulary diseases or disorders that involve abnormal activation of the Abl.Bcr-Abl, Bmx, b-RAF, c-RAFI c-SRC,KDR,CSKlFGFR3,JAK2ILck,Met,PKCalpha,SAPK2alpha)Tie2,TrkB and P70S6K kinases.

PCT/US2006/042975, November 3, 2006

Protein kinase inhibitors

The invention provides disubtituted pyrimidine or pyridine compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly diseases or disorders that involve abnormal activation of the Lck, IR, IGF-IR, JNKl , Flt3, Fes, EFGR (Her-1, erbB-1) , cSRC, CDKl/cyclinB, c-RAF, BTK, Bmx, AxI, Aurora-A, AbI, BCR-AbI, TrkB, Tie2, Syk, SGK, SAPK2a, Rskl and Met kinases.

PCT/US2006/041229, October 20, 2006

Compounds and compositions as protein kinase inhibitors

The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly diseases or disorders that involve abnormal activation of the AbI, Bcr-Abl, Aurora- A, AxI, BMX, CHK2, c-RAF, cSRC, Fes, FGFR3, Flt3, IKKα, IR, JNK2α2, Lck, Met, MKK6, MST2, p70S6K, PDGFRα, PKA, PKD2, ROCK-II, Ros, Rskl, SAPK2α, SAPK2β, SAPK3 SAPK4, Syk, Tie2 and TrkB kinases.

PCT/US2006/032877, August 22, 2006

Immunosuppressant compounds and compositions

The present invention relates to immunosuppressants, processes for their production, their uses and pharmaceutical compositions containing them. The invention provides a novel class of compounds useful in the treatment or prevention of diseases or disorders mediated by lymphocyte interactions, particularly diseases associated with EDG receptor mediated signal transduction. This application relates to compounds selected from Formula (Ia), (Ib), (Ic) and (Id).

PCT/US2006/031134, August 9, 2006

Compounds and compositions as protein kinase inhibitors

The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly diseases or disorders that involve abnormal activation of the Abl, Bcr-Abl, BMX, BTK, CHK2, b-RAF, c-RAF, CSK, c-SRC, Fes, FGFR3, Flt3, IKKα , IKKß , JNK2α 2, Lck, Met, MKK4, MKK6, MST2, NEK2, p70S6K, PDGFRß , PKA, PKBα , PKD2, Rsk1, SAPK2α , SAPK2ß , SAPK3, SGK, Tie2 and TrkB kinases.

PCT/US2006/031985, August 15, 2006

Compounds and compositions as protein kinase inhibitors

The invention provides a novel class of compounds of formula I, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly diseases or disorders that involve abnormal activation of the AbI, Bcr- AbI, Aurora-A, SGK, Tie-2, Trk-B, FGFR3, c-kit, b-RAF, c-RAF, DYRK2, Fms, Fyn and PDGFRalpha and PDGFRβ kinases

PCT/US2006/029162, July 25, 2006

5-substituted thiazol-2-yl amino compounds and compositions as protein kinase inhibitors

The invention provides 5-substituted thiazol-2-yl amino compounds of Formula (I): pharmaceutical compositions comprising such compounds and the use of such compounds for the treatment or prevention of diseases or disorders associated with abnormal or deregulated kinase activity, particularly diseases or disorders that involve abnormal activation of Ab 1 , Aurora-A, Ber-Ab1 , Bmx, CDKI/cyclinB, CHK2, Fes, FGFR3, Flt3, GSK3β, JNK1α1 , Lck, MKK4 and TrkB kinases.

PCT/US2006/025706, June 30, 2006

Pyrimidine-substituted benzimidazole derivatives as protein kinase inhibitors

The invention provides, compounds of formula (I), pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly diseases or disorders that involve abnormal activation of Alk, Abl, BRK, Blk, BMX, CSK, c-Src, c-Raf, EGFR, Fes, FGFR3, Fms, Fyn, IGF-IR, IR, IKKα, IKKβ, JAK2, JAK3, KDR, Lck, Met, p70S6k, Ros, Rskl, SAPK2α, SAPK2β, SAPK3, SIK, Tie2, TrkB and/or WNK3 kinases.

PCT/US2006/018096, May 10, 2006

Compounds and compositions as protein kinase inhibitors

The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly diseases or disorders that involve abnormal activation of Abl, Bcr-Abl, Bmx, BTK, b-RAF, c RAF, CSK, cSRC, Fes, FGFR3, Flt3, IKKα, IKKβ, JNK1α1, JNK2α2, Lck, Met, MKK4, MKK6, p70S6K, PAK2, PDGFRα, PKA, PKCα, PKD2, ROCK-II, Ros, Rsk1, SAPK2α, SAPK2β, SAPK3, SAPK4, SGK, Syk, Tie2 and TrkB kinases.

PCT/US2006/018644, May 12, 2006

Compounds and compositions as protein kinase inhibitors

The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly diseases or disorders that involve abnormal activation of the Abl, Bcr-Abl, BMX, BTK, CHK2, b-RAF, c-RAF, CSK, c-SRC, Fes, FGFR3, Flt3, IKK , IKK , JNK2 2, Lck, Met, MKK4, MKK6, MST2, NEK2, p70S6K, PDGFR , PKA, PKB , PKD2, Rsk1, SAPK2 , SAPK2 , SAPK3, SGK, Tie2 and TrkB kinases.

PCT/US2006/018868, May 15, 2006

Pyrrolopyridine derivatives as protein kinase inhibitors

The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly diseases or disorders that involve abnormal activation of the CDKs, Aurora, Jak2, Rock, CAMKII, FLT3, Tie2, TrkB, FGFR3 and KDR kinases.

PCT/US2006/008719, March 10, 2006

Compounds and compositions as protein kinase inhibitors

The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly diseases or disorders that involve abnormal activation of the Abl, Bcr-Abl, BMX, BTK, CHK2, c-RAF, CSK, c-SRC, Fes, FGFR3, Flt3, IKKα , IKKβ, JNK2α 2, Lck, Met, MKK4, MKK6, MST2, NEK2, p70S6K, PDGFRβ , PKA, PKB β, PKD2, Rsk1, SAPK2α , SAPK2β , SAPK3, SGK, Tie2 and TrkB kinases.

PCT/US2006/002266, January 19, 2006

Compounds and compositions as protein kinase inhibitors

The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly diseases or disorders that involve abnormal activation of the Abl, Bcr-Abl, FGFR3, PDGFRβ and b-Raf kinases.

PCT/US2005/040372, November 7, 2005

Compounds and compositions as protein kinase inhibitors

The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly diseases or disorders that involve abnormal activation of the Abl, Bcr-Abl, cSrc, TPR-Met, Tie2, MET, FGFR3, Aurora, Axl, Bmx, BTK, c-kit, CHK2, Flt3, MST2, p70S6K, PDGFR, PKB, PKC , Raf, ROCK-II, Rsk1, SGK, TrkA, TrkB and TrkC kinases.

PCT/EP2005/006815, June 23, 2005

Pyrimidine urea derivatives as kinase inhibitors

The invention relates to compounds of formula (I) wherein the substituents X1, R1, R2, R3 and R4 have the meaning as set forth and explained in the description of the invention, to processes for the preparation of these compounds, pharmaceutical compositions containing same, the use thereof optionally in combination with one or more other pharmaceutically active compounds for the therapy of a disease which responds to an inhibition of protein kinase activity, and a method for the treatment of such a disease.

PCT/US2005/022463, June 23, 2005

Compounds and compositions as protein kinase inhibitors

The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly diseases or disorders that involve abnormal activation of the Abl, Bcr-abl, Bmx, c-RAF, CSK, Fes, FGFR3, Flt3, GSK3β , IR, JNK1α 1, JNK2α 2, Lck, MKK4, MKK6, p70S6K, PDGFRα , Rsk1, SAPK2α, SAPK2β , Syk and Trkβ kinases

PCT/US2005/020371, June 9, 2005

Compounds and compositions as protein kinase inhibitors

The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly diseases or disorders that involve abnormal activation of the Abl, BCR-Abl, PDGF-R, trkB, c-SRC, BMX, FGFR3, b-RAF, SGK, Tie2, Lck, JNK2 2, MKK4, c-RAF, MKK6, SAPK2 and SAPK2 kinases.

PCT/US2005/015118, April 29, 2005

Compounds and compositions as inducers of keratinocyte differentiation

The invention provides compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to induce undifferentiated keratinocytes to differentiate into terminally differentiated keratinocytes. The invention further provides compounds for the treatment of diseases or disorders associated with casein kinase II (CK2), TANK-binding kinase 1 (TBK1) and NIMA-related kinase 9 (NEK9).

PCT/US2005/006311, February 24, 2005

Immunosuppressant compounds and compositions

The present invention relates to immunosuppressant, process for their production, their uses and pharmaceutical compositions containing them. The invention provides a novel class of compounds useful in the treatment or prevention of diseases or disorders mediated by lymphocyte interactions, particularly diseases associated with EDG receptor mediated signal transduction.

PCT/US2005/006123, February 24, 2005

Immunosuppressant compounds and compositions

The present invention relates to immunosuppressants, processes for their production, their uses and pharmaceutical compositions containing them. The invention provides a novel class of compounds useful in the treatment or prevention of diseases or disorders mediated by lymphocyte interactions, particularly diseases associated with EDG receptor mediated signal transduction.

PCT/US2005/004630, February 14, 2005

Compounds and compositions as protein kinase inhibitors

The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly diseases or disorders that involve abnormal activation of the FAK, Abl, BCR-Abl, PDGF-R, c-Kit, NPM-ALK, Flt-3, JAK2 and c-Met kinases.

PCT/US2004/027997, August 27, 2004

Compounds and compositions as protein kinase inhibitors

The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly diseases or disorders that involve abnormal activation of the Abl, BCR-Abl, Bmx, CSK, TrkB, FGFR3, Fes, Lck, B-RAF, C-RAF, MKK6, SAPK2α and SAPK2β kinases.

PCT/US2004/033009, October 8, 2004

Compounds and compositions as protein kinase inhibitors

The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly diseases or disorders that involve abnormal activation of the Abl, BCR-Abl, CSK, JNK1, JNK2, PDGF-R, p38, p70S6K, TGFβ, SRC, EGFR, c-Kit, trkB, FGFR3, Fes, Lck, Syk, RAF, MKK4, MKK6 and SAPK2β kinases

PCT/US2004/032473, September 30, 2004

Compounds and compositions as protein kinase inhibitors

The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly diseases or disorders that involve abnormal activation of the Abl, BCR-Abl, EGF-R, c-erbB2 kinase (HER-2), CHK2, FGFR3, p70S6K, PKC, PDGF-R, p38, TGFβ , KDR, c-Kit, b-RAF, c-RAF, FLT1 and/or FLT4 kinases.

PCT/US2004/032597, October 1, 2004

Compounds and compositions as protein kinase inhibitors

The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly diseases or disorders that involve abnormal activation of the Abl, BCR-Abl, PDGF-R, lck, SAPK2α, p38, TGFβ, KDR, c-Kit, b-RAF, c-RAF, FLT1 and FLT4 kinases.

PCT/US2004/026373, August 13, 2004

6-Substituted aniline purine as RTK inhibitors

The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with cSRC, Lck, FGFR3, Flt3, TrkB, Bmx, and/or PFGFRα kinase activity.

PCT/EP2004/009099, August 13, 2004

2, 4-Pyrimidinediamines useful in the treatment of neoplastic diseases, inflammatory and immune system disorders

Novel pyrimidine derivatives of formula (I) Wherein R is selected from C16-10 aryl, C5-10heteroaryl, C3-12cycloalkyl and C3-10heterocycloalkyl; R0-R6 as described herein; and their use for the manufacture of a medicament for the treatment or prevention of a disease wich responds to inhibition of FAK and/or ALK and/or ZAP-70 and/or IGF-IR.

PCT/US2004/024764, July 29, 2004

Compounds and compositions as protein kinase inhibitors

The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly diseases or disorders that involve abnormal activation of the Abl, BCR-Abl, Bmx, c-Raf, Csk, Fes, FGFR, Flt3, Ikk, IR, JNK, Lck, Mkk, PKC, PKD, Rsk, SAPK, Syk, Trk, BTK, Src, EGFR, IGF, Mek, Ros and Tie2 kinases.

PCT/US2004/015702, May 19, 2004

Immunosuppressant compounds and compositions

The present invention relates to immunosuppressant, process for their production, their uses and pharmaceutical compositions containing them. The invention provides a novel class of compounds useful in the treatment or prevention of diseases or disorders mediated by lymphocyte interactions, particularly diseases associated with EDG receptor mediated signal transduction.

PCT/US2004/015699, May 19, 2004

Immunosuppressant compounds and compositions

The present invention relates to immunosuppressant, process for their production, their uses and pharmaceutical compositions containing them. The invention provides a novel class of compounds useful in the treatment or prevention of diseases or disorders mediated by lymphocyte interactions, particularly diseases associated with EDG receptor mediated signal transduction.

PCT/US2004/015701, May 19, 2004

Immunosuppressant compounds and compositions

The present invention relates to immunosuppressant, process for their production, their uses and pharmaceutical compositions containing them. The invention provides a novel class of compounds useful in the treatment or prevention of diseases or disorders mediated by lymphocyte interactions, particularly diseases associated with EDG receptor mediated signal transduction.

PCT/US2004/015603, May 19, 2004

Immunosuppressant compounds and compositions

The present invention relates to immunosuppressant, process for their production, their uses and pharmaceutical compositions containing them. The invention provides a novel class of compounds useful in the treatment or prevention of diseases or disorders mediated by lymphocyte interactions, particularly diseases associated with EDG receptor mediated signal transduction.

PCT/US2004/013631, April 30, 2004

Compounds and compositions as protein kinase inhibitors

The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases and disorders associated with kinase activity, particularly diseases associated with the activity of CDK1, CDK2, CDK4, CDK5, GSK3β, Bcr-abl, Flt-3, c-Kit, PDGFRβ, Src, Mek1 and CK1.

PCT/US2004/012399, April 22, 2004

Compounds that induce neuronal differentiation in embryonic stem cells

The invention provides a novel class of compounds and compositions that are useful in the treatment or prevention of diseases or disorders associated with kinases, particularly GSK-3ß, c-Abl, HER-1, HER-2, KDR, Flt-3, c-Raf-1, PDGFR- ß, c-Kit, Flt-4, Flt-1, Tek, c-src, CDK1, PDK1, FGFR-1, FGFR-2, Fer, MAP3K13, EPHA7 and c-Met kinases. The invention further relates to the use of the compounds of the invention as potent inducers of neurogenesis in embryonic stem cells.

PCT/US2004/010083, April 2, 2004

Novel compounds and composition as protein kinase inhibitors

The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated tyrosine kinase activity, particularly diseases associated with the activity of PDGF-R, c-Kit and Bcr-abl.

PCT/US2004/006947, March 5, 2004

Cyclic compounds and compositions as protein kinase inhibitors

The invention provides a novel class of cyclic compounds, pharmaceutical compositions comprising such cyclic compounds and methods of using such compounds to treat or prevent diseases and disorders associated with cyclin-dependent kinases (CDKs) activity, particularly diseases associated with the activity of CDK2 and CDK5.

PCT/US2004/004006, February 11, 2004

Novel bicyclic compounds and compositions

The present invention relates to bicyclic derivatives, process for their production, their uses and pharmaceutical compositions containing them. The invention provides a novel class of compounds useful in the treatment or prevention of diseases or disorders mediated by lymphocyte interactions, particularly diseases associated with EDG/S1P receptor mediated signal transduction.

PCT/US2003/032567, October 15, 2003

Compositions and methods for inducing osteogenesis

The present invention provides compositions and methods for differentiating and transdifferentiating mammalian cells into cells of an osteoblast lineage.

PCT/EP2003/005510, May 26, 2003

Bis-aromatic alkanols

The present invention relates to biphenylyl derivatives, processes for their production, their uses and pharmaceutical compositions containing them.

PCT/US2002/032680, Ocotber 12, 2002

Kinase inhibitor scaffolds and methods for their preparation

General methods for the solution phase as well as solid phase synthesis of various substituted heteroaryls has been demonstrated. These substituted heteroaryls can be further elaborated by aromatic substitution with amines at elevated temperature or by anilines, boronic acids and phenols via palladium catalyzed cross-coupling reactions.

PCT/US2002/032679, October 12, 2002

Methods for the synthesis of substituted purines

The invention provides general methods for preparing 2,9-, 2,6,9-, O6-aryl- and O6-alkyl-substituted purines in a combinatorial and traceless fashion. The methods involve, in some embodiments, Mitsunobu alkylation of 2-fluoro-6-phenylsulfenylpurine at N9 with alcohols in solution, followed by C2-capture of the purine core with a resin-bound amine and subsequent oxidation and displacement of the C6 sulfonyl group with amines and anilines.

PCT/US2002/028619, September 6, 2002

Sensory neuron receptors

This invention provides G protein-coupled receptors that are expressed in mammalian sensory neurons of dorsal root ganglia. Both nucleic acids that encode the receptors, and the receptor polypeptides are provided.

PCT/US1998/027405, December 23, 1998

Methods of using chemical libraries to search for new kinase inhibitors

The generation of selective inhibitors for specific protein kinases would provide new tools for analyzing signal transduction pathways and possibly new therapeutic agents. We have invented an approach to the development of selective protein kinase inhibitors based on the unexpected binding mode of 2,6,9-trisubstituted purines to the ATP binding site of human CDK2.

PCT/US1998/016388, August 6, 1998

Purine inhibitor of protein kinases, G proteins and polymerases

The present invention relates to purine analogs having general formula (I) or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4 and R5 are independently members selected from the group consisting of H, C1-C8 straight-chain, branched-chain, saturated and unsaturated alkyl, C1-C8 straight-chain, branched-chain, saturated and unsaturated substituted alkyl, aryl and substituted aryl, that inhibit, inter alia, protein kinases, G-proteins and polymerases.