|
[½»Á÷]
¸¡Ã×ÿÖÜרÀû¿ìѶ£º2014Äê3Ô£¨Ò»£©ÒÑÓÐ4È˲ÎÓë
1. WO 2014023258
±êÌâ: Pyrazole carboxamide compounds, compositions and methods of use
ÉêÇëÈË: ÂÞÊÏ£»»ùÒòÌ©¿Ë
ÓÅÏÈȨÈÕÆÚ¼°Ïà¹ØרÀû¹«¿ªºÅ: 2012 US 682063£»2013 US 764930£»2013 US 764434
Ïà¹ØºòÑ¡Ò©ÎïÀàÐÍ: С·Ö×ÓÒ©Îï
Ïà¹ØºòÑ¡Ò©Îﻯѧ½á¹¹:
ÊÊÓ¦Ö¢: Ñ×Ö¢
רÀûÕªÒª: Provided herein are compounds of formula (AA): N N H HN O N N R R 6 A (R a ) p, (AA) stereoisomers or a pharmaceutically acceptable salt thereof, wherein A, R a, p, R and R 6 are defined herein, compositions including the compounds and methods of manufacturing and using the compounds for the treatment of diseases.
±¸×¢: ITK (EMT) ¼¤Ã¸ÒÖÖƼÁ¿ÉÒÔÓÃÓÚÖÎÁÆÑ×Ö¢¡£Ò»¸öʾÀýÐÔ»¯ºÏÎï¶ÔITKµÄ»îÐÔΪKiСÓÚ0.1 nM.
2. WO 2014025854
±êÌâ: Piperidine amide derivatives as HIV attachment inhibitors
ÉêÇëÈË: °ÙʱÃÀÊ©¹ó±¦
ÓÅÏÈȨÈÕÆÚ¼°Ïà¹ØרÀû¹«¿ªºÅ: 2012 US 681306
Ïà¹ØºòÑ¡Ò©ÎïÀàÐÍ: С·Ö×ÓÒ©Îï
Ïà¹ØºòÑ¡Ò©Îﻯѧ½á¹¹:201403060102
ÊÊÓ¦Ö¢: HIV¸ÐȾ
רÀûÕªÒª: Compounds of Formula I, including pharmaceutically acceptable salts thereof: formule (I): wherein A is selected from the group consisting of:formule (II) and wherein Z is selected from the group consisting of: formule (III):,, and. are useful as HIV attachment inhibitors.
±¸×¢: HIV Õ³¸½ÒÖÖƼÁ¿ÉÒÔÓÃÓÚÖÎÁÆHIV¸ÐȾ¡£Ò»¸öʾÀýÐԵĻ¯ºÏÎïÔÚMT-2ϸ°ûÖжÔHIV-1µÄ»îÐÔΪEC50=0.20 nM¡£
3. WO 2014023815
±êÌâ: New antibacterial compounds
ÉêÇëÈË: ÑîÉ
ÓÅÏÈȨÈÕÆÚ¼°Ïà¹ØרÀû¹«¿ªºÅ: 2012 EP 180103
Ïà¹ØºòÑ¡Ò©ÎïÀàÐÍ: С·Ö×ÓÒ©Îï
Ïà¹ØºòÑ¡Ò©Îﻯѧ½á¹¹:201403060103
ÊÊÓ¦Ö¢: ϸ¾ú¸ÐȾ
רÀûÕªÒª: The present invention is related to novel compounds of formula (I) that may inhibit the activity of the FabI enzyme, and which are useful in the treatment of bacterial infections. It further relates to pharmaceutical compositions comprising these compounds, and chemical processes for preparing these compounds.
±¸×¢: Ï©õ£»ù ¨C £¨õ£»ùÔØÌåµ°°×£©»¹ÔøFablÒÖÖƼÁ¿ÉÒÔÓÃÓÚÖÎÁÆϸ¾ú¸ÐȾ¡£Ò»¸öʾÀýÐÔ»¯ºÏÎï¿ÉÒÔÒÖÖƽð»ÆÉ«ÆÏÌÑÇò¾úATCC 29213 Fabl£¬ÆäIC50´ïµ½0.407356 mcg/ml¡£
4. WO 2014024119
±êÌâ: Heterocyclic amides as ITK inhibitors
ÉêÇëÈË: ¸ñÂ×Âí¿Ë
ÓÅÏÈȨÈÕÆÚ¼°Ïà¹ØרÀû¹«¿ªºÅ: 2012 IN 2888£»2012 IN 2257£»2013 IN 762£»2012 US 717224£»2012 US 696439
Ïà¹ØºòÑ¡Ò©ÎïÀàÐÍ: С·Ö×ÓÒ©Îï
Ïà¹ØºòÑ¡Ò©Îﻯѧ½á¹¹:201403060104
ÊÊÓ¦Ö¢: Ïø´£»ÂýÐÔ×èÈûÐԷβ¡£»ÌØÒìÐÔƤÑ×£»Àà·çʪÐԹؽÚÑ×£»¹ýÃôÐÔ±ÇÑ×
רÀûÕªÒª: The present invention is directed to heterocyclic amide compounds of formula (I) as Tec kinase inhibitors, in particular ITK (interleukin-2 inducible tyrosine kinase) inhibitors. Also provided herein are processes for preparing compounds described herein, intermediates used in their synthesis, pharmaceutical compositions thereof, and methods for treating or preventing diseases, conditions and/or disorders mediated by ITK.
±¸×¢: ITK (EMT)ÒÖÖƼÁ¿ÉÒÔÓÃÓÚÖÎÁÆÏø´¡¢ÂýÐÔ×èÈûÐԷμ²²¡¡¢Æ¤Ñס¢Àà·çʪÐԹؽÚÑס¢¹ýÃôÐÔ±ÇÑס¢¶à·¢ÐÔÓ²»¯Ö¢¡¢ÌÛÍ´µÈ¼²²¡¡£±¾×¨ÀûÖеÄÌṩµÄ²¿·ÖʾÀý»¯ºÏÎïIC50СÓÚ50 nM ¡£
5. WO 2014023367
±êÌâ: Carboxamide or sulfonamide substituted nitrogen-containing 5-membered heterocycles as modulators for the orphan nuclear receptor RORgamma
ÉêÇëÈË: Phenex Pharmaceuticals AG
ÓÅÏÈȨÈÕÆÚ¼°Ïà¹ØרÀû¹«¿ªºÅ: 2012 US 681296£»2012 EP 5789
Ïà¹ØºòÑ¡Ò©ÎïÀàÐÍ: С·Ö×ÓÒ©Îï
Ïà¹ØºòÑ¡Ò©Îﻯѧ½á¹¹:201403060105
ÊÊÓ¦Ö¢: ¼¡Î®Ëõ²àË÷Ó²»¯Ö¢£»Ïø´£»IÐÍÌÇÄò²¡£»³¦Ñ×£»¶à·¢ÐÔÓ²»¯Ö¢£»Òøм²¡£»Àà·çʪÐԹؽÚÑ×£»¼¹ÖùÑ×
רÀûÕªÒª: The invention provides modulators for the orphan nuclear receptor RORy and methods for treating RORy mediated diseases by administering these novel RORy modulators to a human or a mammal in need thereof. Specifically, the present invention provides carboxamide containing cyclic compounds of Formula (1) to Formula (5) and the enantiomers, diastereomers, tautomers, /V-oxides, solvates and pharmaceutically acceptable salts thereof.
±¸×¢: ROR gamma ÊÜÌåµ÷¿Ø¼Á¿ÉÒÔÓÃÓÚÖÎÁÆÑ×Ö¢¡¢×ÔÉíÃâÒߣ¬È缡ήËõÐÔ¼¹ËèâüË÷Ó²»¯Ö¢¡¢¶à·¢ÐÔÓ²»¯Ö¢¡¢Å£Æ¤Ñ¢¡¢Àà·çʪÐԹؽÚÑס¢¹ýÃôÐÔʪÕîµÈ¡£Ò»¸öʾÀýÐԵĻ¯ºÏÎïÔÚBL-21ϸ°ûÖÐÏÔʾÒÖÖÆRORgammaµÄ»îÐÔΪpIC50Ϊ6.3nM¡£
6. WO 2014023385
±êÌâ: Pyridopyrimidine derivatives as protein kinase inhibitors
ÉêÇëÈË: Ĭ¿Ë
ÓÅÏÈȨÈÕÆÚ¼°Ïà¹ØרÀû¹«¿ªºÅ: 2012 EP 5716
Ïà¹ØºòÑ¡Ò©ÎïÀàÐÍ: С·Ö×ÓÒ©Îï
Ïà¹ØºòÑ¡Ò©Îﻯѧ½á¹¹:201403060106
ÊÊÓ¦Ö¢: Ïø´£»Ö×Áö£»¶à·¢ÐÔÓ²»¯Ö¢£»Àà·çʪÐԹؽÚÑ×£»ºì°ßÀÇ´¯
רÀûÕªÒª: Compounds of the formula (I) in which R, R1 and R2 have the meanings indicated in Claim 1, are inhibitors of Syk, and can be employed, inter alia, for the treatment of cancer, rheumatoid arthritis and / or systemic lupus
±¸×¢: Syk¼¤Ã¸ÒÖÖƼÁ¿ÉÒÔÓÃÓÚ¶àÖÖ¼²²¡µÄÖÎÁÆ£¬ÈçÖ×Áö¡¢Àà·çʪÐԹؽÚÑס¢ºì°ßÀÇ´¯¡¢Ïø´¡¢¶à·¢ÐÔÓ²»¯Ö¢¡¢ÌÇÄò²¡¡¢ÌÆÊÏ×ÛºÏÖ¢µÈ¡£Ò»¸öʾÀýÐÔ»¯ºÏÎï¶ÔSykµÄÒÖÖÆ»îÐÔΪIC500.1 mcM ¡£
7. WO 2014023673£»US 2014044674
±êÌâ: Interleukin-10 fusion proteins and uses thereof
ÉêÇëÈË: ÂÞÊÏ
ÓÅÏÈȨÈÕÆÚ¼°Ïà¹ØרÀû¹«¿ªºÅ: 2012 EP 179709
Ïà¹ØºòÑ¡Ò©ÎïÀàÐÍ: Èںϵ°°×
ÊÊÓ¦Ö¢: Ñ×Ö¢£»³¦Ñ×£»Àà·çʪÐԹؽÚÑ×
רÀûÕªÒª: The present invention generally relates to fusion proteins of antibodies and interleukin-10 (IL-10). In addition, the present invention relates to polynucleotides encoding such fusion proteins, and vectors and host cells comprising such polynucleotides. The invention further relates to methods for producing the fusion proteins of the invention, and to methods of using them in the treatment of disease.
±¸×¢: ÓÉIgGÀ࿹ÌåºÍIL-10·Ö×Ó×é³ÉµÄÈںϵ°°×¿ÉÒÔÓÃÓÚÑ×Ö¢µÄÖÎÁÆ»òÔ¤·À£¬ÌرðÊÇÑ×Ö¢ÐÔ³¦¼²²¡ºÍÀà·çʪ¹Ø½ÚÑ×µÄÖÎÁÆ¡£Ò»¸öʾÀýÐÔµÄÈںϵ°°×¿ÉÒÔ°ÐÏòÈËÔ´FAP¡£¸ÃÈںϵ°°×¿ÉÒÔÒÖÖÆLPSÓÕµ¼µÄÇ°Ñ×ÐÔϸ°û»îËØ£¨IL-6, IL-1betaºÍTNF-alpha£©µÄ²úÎÆäEC50·Ö±ðΪ0.054, 0.049ºÍ0.017 nM¡£
8. WO 2014023674
±êÌâ: Piperazino[1,2-a]indol-1-ones and [1,4]diazepino[1,2-a]indol-1-one
ÉêÇëÈË: ÂÞÊÏ
ÓÅÏÈȨÈÕÆÚ¼°Ïà¹ØרÀû¹«¿ªºÅ: 2012 EP 179381
Ïà¹ØºòÑ¡Ò©ÎïÀàÐÍ: С·Ö×ÓÒ©Îï
Ïà¹ØºòÑ¡Ò©Îﻯѧ½á¹¹:201403060108
ÊÊÓ¦Ö¢: ½¹ÂÇ£»°¢¶û×Ⱥ£Ä¬£»ÒÖÓô£»Öзç
רÀûÕªÒª: The present invention relates to compounds of general formula (I), wherein R1 is hydrogen, halogen, lower alkyl, lower alkoxy, lower alkoxy substituted by halogen or cyano; R2 is hydrogen, lower alkyl or lower alkyl substituted by halogen; R3 is phenyl, benzo[1,3]dioxolyl, 2,3-dihydro-benzofuran-5-yl or a 5- and 6-membered heteroaryl, wherein phenyl and the 5- and 6-membered heteroaryl groups may be substituted by one or more substituents, selected from cyano, nitro, amino and lower di-alkylamino, lower alkyl sulfonyl, lower alkoxy, lower alkoxy substituted by halogen, halogen, lower alkyl, lower alkyl substituted by halogen or lower alkyl substituted by hydroxyl; X is -CH(lower alkyl)-, -CH2-, -CH2CH2- or �CH(lower alkyl)CH2-; R is hydrogen or lower alkyl; n is 1 or 2; or to a pharmaceutically acceptable acid addition salt, to a racemic mixture or to its corresponding enantiomer and/or optical isomers thereof. The compounds may be used for the treatment of schizophrenia, obsessive-compulsive personality disorder, major depression, bipolar disorders, anxiety disorders, normal aging, epilepsy, retinal degeneration, traumatic brain injury, spinal cord injury, post-traumatic stress disorder, panic disorder, Parkinson¡¯s disease, dementia, Alzheimer¡¯s disease, mild cognitive impairment, chemotherapy-induced cognitive dysfunction, Down syndrome, autism spectrum disorders, hearing loss, tinnitus, spinocerebellar ataxia, amyotrophic lateral sclerosis, multiple sclerosis, Huntington¡¯s disease, stroke, radiation therapy, chronic stress, abuse of neuro-active drugs, such as alcohol, opiates, methamphetamine, phencyclidine and cocaine.
±¸×¢: Éñ¾ÏµÍ³µ÷½ÚÀ໯ºÏÎï¿ÉÒÔÓÃÓÚÖÎÁƽ¹ÂÇ¡¢°¢¶û×Ⱥ£Ä¬¡¢ÒÖÓôºÍÖзçµÈ¼²²¡¡£Ò»¸öʾÀýÐԵĻ¯ºÏÎïµÄEC150=0.002 mcM¡£
9. WO 2014026054
±êÌâ: CD20 scFv-ELPs methods and therapeutics
ÉêÇëÈË: University of Southern California (USC)
ÓÅÏÈȨÈÕÆÚ¼°Ïà¹ØרÀû¹«¿ªºÅ: 2012 US 682029
Ïà¹ØºòÑ¡Ò©ÎïÀàÐÍ: Èںϵ°°×
ÊÊÓ¦Ö¢: ×ÔÉíÃâÒߣ»Ö×Áö
רÀûÕªÒª: Disclosed herein are recombinant polypeptides comprising an elastin-like peptide (ELP) and a scFv, or a biological equivalent of the scFv. Also disclosed are compositions containing scFv-ELP polypeptides and methods of use.
±¸×¢: °üº¬µ¯ÐÔµ°°×ÑùëÄ£¨ELP£©Èںϵ¥Á´¿¹Ì壨scFv£©µÄÖØ×é¶àëÄ¿ÉÒÔÓÃÓÚÖÎÁÆ°©Ö¢ºÍ×ÔÉíÃâÒßÀ༲²¡¡£Ò»¸öÓÉÀûÍ×Îôµ¥¿¹ÑÜÉúµÄ¿¹CD20µÄscFvµ¥Á´¿¹ÌåÈÚºÏELP(A-192)µÄÈںϵ°°×scFv-ELPs¿ÉÒÔÑÓ»ºÖ×ÁöÉú³¤²¢ÑÓ³¤Éú´æÆÚ¡£
10. WO 2014023814
±êÌâ: New antibacterial compounds
ÉêÇëÈË: ÑîÉ
ÓÅÏÈȨÈÕÆÚ¼°Ïà¹ØרÀû¹«¿ªºÅ: 2012 EP 180100
Ïà¹ØºòÑ¡Ò©ÎïÀàÐÍ: С·Ö×ÓÒ©Îï
Ïà¹ØºòÑ¡Ò©Îﻯѧ½á¹¹:2014030601010
ÊÊÓ¦Ö¢: ϸ¾ú¸ÐȾ
רÀûÕªÒª: The present invention is related to novel compounds of formula (I) that may inhibit the activity of the FabI enzyme, and which are useful in the treatment of bacterial infections. It further relates to pharmaceutical compositions comprising these compounds, and chemical processes for preparing these compounds.
±¸×¢: Ï©õ£»ù ¨C £¨õ£»ùÔØÌåµ°°×£©»¹ÔøFablÒÖÖƼÁ¿ÉÒÔÓÃÓÚÖÎÁÆϸ¾ú¸ÐȾ¡£Ò»¸öʾÀýÐÔ»¯ºÏÎï¿ÉÒÔÒÖÖƽð»ÆÉ«ÆÏÌÑÇò¾úATCC 29213 Fabl£¬ÆäIC50´ïµ½0.27 mcg/ml¡£´ËÍâÆäÒ²¶ÔS. aureus ATCC 29213 and S. aureus ATCC 29213¾ßÓлîÐÔ£¬·Ö±ðΪIC90 = 0.24 ºÍ0.21 mcg/ml¡£
11. WO 2014025708
±êÌâ: Compounds that are S1P modulating agents and/or ATX modulating agents
ÉêÇëÈË: Biogen Idec Inc.
ÓÅÏÈȨÈÕÆÚ¼°Ïà¹ØרÀû¹«¿ªºÅ: 2012 US 679984
Ïà¹ØºòÑ¡Ò©ÎïÀàÐÍ: С·Ö×ÓÒ©Îï
Ïà¹ØºòÑ¡Ò©Îﻯѧ½á¹¹:2014030601011
ÊÊÓ¦Ö¢: ¶à·¢ÐÔÓ²»¯Ö¢£»ÌÛÍ´£»Àà·çʪÐԹؽÚÑ×
רÀûÕªÒª: Compounds of formula (I) can modulate the activity of one or more SIP receptors and/or the activity of autotaxin (ATX).
±¸×¢: ENPP2ÒÖÖƼÁ»òSIPµ÷½Ú¼Á¿ÉÓÃÓÚÀà·çʪÐԹؽÚÑ׹ؽÚÑס¢¶à·¢ÐÔÓ²»¯Ö¢ºÍÌÛÍ´¡¢Ö×Áö¡¢ÃâÒߵȼ²²¡µÄÖÎÁÆ¡£ ʾÀýÐÔ»¯ºÏÎï¶ÔENPP2µÄIC50СÓÚ0.5 mcM¡£
12. WO 2014025709
±êÌâ: Compounds that are S1P modulating agents and/or ATX modulating agents
ÉêÇëÈË: Biogen Idec Inc.
ÓÅÏÈȨÈÕÆÚ¼°Ïà¹ØרÀû¹«¿ªºÅ: 2012 US 679992
Ïà¹ØºòÑ¡Ò©ÎïÀàÐÍ: С·Ö×ÓÒ©Îï
Ïà¹ØºòÑ¡Ò©Îﻯѧ½á¹¹:2014030601012
ÊÊÓ¦Ö¢: ¶à·¢ÐÔÓ²»¯Ö¢£»ÌÛÍ´£»Àà·çʪÐԹؽÚÑ×
רÀûÕªÒª: Compounds of formula (I) can modulate the activity of one or more SIP receptors and/or the activity of autotaxin (ATX).
±¸×¢: ENPP2ÒÖÖƼÁ»òSIPµ÷½Ú¼Á¿ÉÓÃÓÚÀà·çʪÐԹؽÚÑ׹ؽÚÑס¢¶à·¢ÐÔÓ²»¯Ö¢ºÍÌÛÍ´¡¢Ö×Áö¡¢ÃâÒߵȼ²²¡µÄÖÎÁÆ¡£ ʾÀýÐÔ»¯ºÏÎï¶ÔENPP2µÄIC50СÓÚ0.5 mcM¡£
13. WO 2014025850
±êÌâ: Tricyclic amidine derivatives as HIV attachment inhibitors
ÉêÇëÈË: °ÙʱÃÀÊ©¹ó±¦
ÓÅÏÈȨÈÕÆÚ¼°Ïà¹ØרÀû¹«¿ªºÅ: 2012 US 681336
Ïà¹ØºòÑ¡Ò©ÎïÀàÐÍ: С·Ö×ÓÒ©Îï
Ïà¹ØºòÑ¡Ò©Îﻯѧ½á¹¹:2014030601013
ÊÊÓ¦Ö¢: HIV¸ÐȾ
רÀûÕªÒª: Compounds of Formula I, including pharmaceutically acceptable salts thereof: (F) wherein A is selected from the group consisting of: (F) and;(F) and wherein Z is: (F) are useful as HIV attachment inhibitors.
±¸×¢: HIV Õ³¸½ÒÖÖƼÁ¿ÉÒÔÓÃÓÚÖÎÁÆHIV¸ÐȾ¡£Ò»¸öʾÀýÐԵĻ¯ºÏÎïÔÚMT-2ϸ°ûÖжÔHIV-1µÄ»îÐÔΪEC50=1.83nM¡£
14. WO 2014025852
±êÌâ: Tricyclic alkene derivatives as HIV attachment inhibitors
ÉêÇëÈË: °ÙʱÃÀÊ©¹ó±¦
ÓÅÏÈȨÈÕÆÚ¼°Ïà¹ØרÀû¹«¿ªºÅ: 2012 US 681329
Ïà¹ØºòÑ¡Ò©ÎïÀàÐÍ: С·Ö×ÓÒ©Îï
Ïà¹ØºòÑ¡Ò©Îﻯѧ½á¹¹:2014030601014
ÊÊÓ¦Ö¢: HIV¸ÐȾ
רÀûÕªÒª: Compounds of Formula (I), including pharmaceutically acceptable salts thereof: wherein A is selected from the group consisting of: and wherein Z is: are useful as HIV attachment inhibitors.
±¸×¢: HIV Õ³¸½ÒÖÖƼÁ¿ÉÒÔÓÃÓÚÖÎÁÆHIV¸ÐȾ¡£Ò»¸öʾÀýÐԵĻ¯ºÏÎïÔÚMT-2ϸ°ûÖжÔHIV-1µÄ»îÐÔΪEC50=0.28 nM¡£
15. WO 2014022936
±êÌâ: Chlamydia antigen compositions and uses thereof
ÉêÇëÈË: University of British Columbia
ÓÅÏÈȨÈÕÆÚ¼°Ïà¹ØרÀû¹«¿ªºÅ: 2012 US 680836
Ïà¹ØºòÑ¡Ò©ÎïÀàÐÍ: Èںϵ°°×
ÊÊÓ¦Ö¢: ÒÂÔÌå¸ÐȾ
רÀûÕªÒª: The present invention provides in part fusion proteins derived from Chlamydia spp. The present invention also provides in part methods for treating or preventing Chlamydia infection using the fusion proteins.
±¸×¢: ÃâÒß×éºÏÎïÀàµÄÈںϵ°°×¿ÉÒÔ×÷ΪÒßÃ磬ÓÃÓÚÒÂÔÌå¸ÐȾµÄÔ¤·ÀºÍÖÎÁÆ¡£±¾×¨ÀûÖУ¬Èںϵ°°× Chlamydia¿¹ÌåչʾÁËÁ¼ºÃÁË¿¹ÒÂÔÌå¸ÐȾ»îÐÔ¡£
16. WO 2014022767
±êÌâ: Dihydropyridone P1 as factor XIa inhibitors
ÉêÇëÈË: °ÙʱÃÀÊ©¹ó±¦
ÓÅÏÈȨÈÕÆÚ¼°Ïà¹ØרÀû¹«¿ªºÅ: 2013 US 787081£»2012 US 679197
Ïà¹ØºòÑ¡Ò©ÎïÀàÐÍ: С·Ö×ÓÒ©Îï
Ïà¹ØºòÑ¡Ò©Îﻯѧ½á¹¹:2014030601016
ÊÊÓ¦Ö¢: Ѫ˨
רÀûÕªÒª: The present invention provides compounds of Formula (X)Formula(X), or stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, wherein all the variables are as defined herein. These compounds are selective factor XIa inhibitors or dual inhibitors of FXIa and plasma kallikrein. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating thromboembolic and/or inflammatory disorders using the same.
±¸×¢: ÄýѪÒò×ÓXIaºÍ/»ò¼¤ëÄÊÍ·ÅøB£¨Ñª½¬¼¤ëÄÊÍ·Åø; KLKB1£©¿ÉÒÔÓÃÓÚÖÎÁÆѪ˨¡£ÑªË¨Ë¨ÈûÐÔ²¡Ö¢Èç²»Îȶ¨ÐÍÐĽÊÍ´£¬¼±ÐÔ¹Ú×´¶¯Âö×ÛºÏÕ÷£¬ÐÄ·¿ÏËάÐÔ²ü¶¯£¬Ðļ¡¹£Èû£¬¶ÌÔÝÐÔȱѪ·¢×÷£¬Öз磬¶¯ÂöÖàÑùÓ²»¯£¬ÍâÖÜ×èÈûµÄÖÎÁÆÓÐÓõÄÒÖÖƼÁ¶¯Âö¼²²¡£¬¾²ÂöѪ˨Ðγɣ¬ÄÔ¶¯ÂöѪ˨Ðγɣ¬ÄÔ£¬ÉöºÍ·Î˨ÈûµÈ¡£±¾×¨ÀûÖеĵÄʾÀý»¯ºÏÎï¶ÔÄýѪÒò×ÓXIaºÍKLKB1µÄ KiÖµ·Ö±ðΪ 0.05ºÍ 0.56 nM¡£
17. WO 2014022766£»US 2014038969
±êÌâ: Dihydropyridone P1 as factor XIa inhibitors
ÉêÇëÈË: °ÙʱÃÀÊ©¹ó±¦
ÓÅÏÈȨÈÕÆÚ¼°Ïà¹ØרÀû¹«¿ªºÅ: 2013 US 957609£»2012 US 679197£»2013 US 786992
Ïà¹ØºòÑ¡Ò©ÎïÀàÐÍ: С·Ö×ÓÒ©Îï
Ïà¹ØºòÑ¡Ò©Îﻯѧ½á¹¹:2014030601017
ÊÊÓ¦Ö¢: Ѫ˨
רÀûÕªÒª: The present invention provides compounds of Formula (VIII): or stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, wherein all the variables are as defined herein. These compounds are selective factor XIa inhibitors or dual inhibitors of FXIa and plasma kallikrein. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating thromboembolic and/or inflammatory disorders using the same.
±¸×¢: ÄýѪÒò×ÓXIaºÍ/»ò¼¤ëÄÊÍ·ÅøB£¨Ñª½¬¼¤ëÄÊÍ·Åø; KLKB1£©¿ÉÒÔÓÃÓÚÖÎÁÆѪ˨¡£ÑªË¨Ë¨ÈûÐÔ²¡Ö¢Èç²»Îȶ¨ÐÍÐĽÊÍ´£¬¼±ÐÔ¹Ú×´¶¯Âö×ÛºÏÕ÷£¬ÐÄ·¿ÏËάÐÔ²ü¶¯£¬Ðļ¡¹£Èû£¬¶ÌÔÝÐÔȱѪ·¢×÷£¬Öз磬¶¯ÂöÖàÑùÓ²»¯£¬ÍâÖÜ×èÈûµÄÖÎÁÆÓÐÓõÄÒÖÖƼÁ¶¯Âö¼²²¡£¬¾²ÂöѪ˨Ðγɣ¬ÄÔ¶¯ÂöѪ˨Ðγɣ¬ÄÔ£¬ÉöºÍ·Î˨ÈûµÈ¡£±¾×¨ÀûÖеĵÄʾÀý»¯ºÏÎï¶ÔÄýѪÒò×ÓXIaºÍKLKB1µÄ KiÖµ·Ö±ðΪ 0.25ºÍ 0.7 nM¡£
18. WO 2014022752
±êÌâ: Macrocycles as Pim inhibitors
ÉêÇëÈË: °²½ø
ÓÅÏÈȨÈÕÆÚ¼°Ïà¹ØרÀû¹«¿ªºÅ: 2012 US 679521
Ïà¹ØºòÑ¡Ò©ÎïÀàÐÍ: С·Ö×ÓÒ©Îï
Ïà¹ØºòÑ¡Ò©Îﻯѧ½á¹¹:2014030601018
ÊÊÓ¦Ö¢: Ö×Áö
רÀûÕªÒª: The invention relates to compounds of formula (1), and salts thereof. In some embodiments, the invention relates to inhibitors or modulators of Pim-1 and/or Pim-2, and/or Pim-3 protein kinase activity or enzyme function. In still further embodiments, the invention relates to pharmaceutical compositions comprising compounds disclosed herein, and their use in the prevention and treatment of Pim kinase related conditions and diseases, preferably cancer.
±¸×¢: Pim¼¤Ã¸¿ÉÒÔÓÃÓÚÖÎÁÆÖ×Áö¡£Pim·ÖΪPim1¡¢Pim2¡¢Pim3µÈÈýÖÖÑÇÐÍ¡£ ±¾×¨ÀûµÄ»¯ºÏÎï¶Ô Pim-1, Pim-2, Pim-1-Mn and Pim-2-MnµÄ»îÐÔ·Ö±ðΪIC50 = 0.000209¡¢0.000286¡¢0.0000498ºÍ0.0000634 mcM¡£
19. WO 2014022744
±êÌâ: Indole-substituted pyrrolopyrimidinyl inhibitors of Uba6
ÉêÇëÈË: Millennium Pharmaceuticals, Inc.
ÓÅÏÈȨÈÕÆÚ¼°Ïà¹ØרÀû¹«¿ªºÅ: 2012 US 679109
Ïà¹ØºòÑ¡Ò©ÎïÀàÐÍ: С·Ö×ÓÒ©Îï
Ïà¹ØºòÑ¡Ò©Îﻯѧ½á¹¹:2014030601019
ÊÊÓ¦Ö¢: Ö×Áö
רÀûÕªÒª: Disclosed are chemical entities that inhibit Uba6, each of which is a compound of Formula /: Formula (I) or a pharmaceutically acceptable salt thereof, wherein R*1 is -H or -CH3; and Y is Formula (II) or Formula (III), wherein R2 is -H, -CH3 or C1-4 alkyloxycarbonyl; and RS7.1, RS7.2 and RS8.1 are defined herein; pharmaceutical compositions comprising the chemical entities; and methods of using the chemical entities. These chemical entities are useful for treating disorders, particularly cell proliferation disorders, including cancers.
±¸×¢: UBA6øÒÖÖƼÁ¿ÉÒÔÓÃÓëÖÎÁÆÖ×Áö¼²²¡¡£Ò»¸öʾÀýÐÔ»¯ºÏÎï¶ÔÈËÔ´ÖØ×éhis-UBA6øµÄIC50СÓÚ50nM¡£
20. EP 2692357£»WO 2014020062
±êÌâ: Novel anti-Plasmodium parasite antibodies
ÉêÇëÈË: Fraunhofer-Gesellschaft zur Foerderung der angewandten Forschung eV
ÓÅÏÈȨÈÕÆÚ¼°Ïà¹ØרÀû¹«¿ªºÅ: 2012 US 679380£»2012 EP 179315
Ïà¹ØºòÑ¡Ò©ÎïÀàÐÍ: ¿¹Ìå
ÊÊÓ¦Ö¢: Õï¶Ï£»Å±¼²
רÀûÕªÒª: The technology provided herein relates to novel human antibodies against Plasmodium parasites, in particular against the malaria parasite Plasmodium falciparum. The present disclosure pertains to antibodies against merozoite surface protein 10 (MSP10). These antibodies have high affinity e.g. to Plasmodium falciparum schizonts and merozoites, inhibit the reinvasion of merozoites into erythrocytes and thereby neutralize parasitic multiplication.
±¸×¢: ÈË¿¹Ìå»òÆ俹ԿÉÒÔÌØÒìÐԵĽáºÏMSP10£¬ÇÒ¿ÉÒÔÓÃÓÚű¼²µÄÕï¶ÏºÍÖÎÁÆ¡£±¾×¨ÀûÖÐÁоٵÄÈ˵¥¿Ë¡IgG1 kappa¿¹ÌåչʾÁ˶ÔEGF Óò1µÄÌØÒìÐÔÇ׺ÍÁ¦¡£
21. WO 2014022343
±êÌâ: 7-Hydroxy-indolinyl antagonists of P2Y1 receptor
ÉêÇëÈË: °ÙʱÃÀÊ©¹ó±¦
ÓÅÏÈȨÈÕÆÚ¼°Ïà¹ØרÀû¹«¿ªºÅ: 2012 US 678151
Ïà¹ØºòÑ¡Ò©ÎïÀàÐÍ: С·Ö×ÓÒ©Îï
Ïà¹ØºòÑ¡Ò©Îﻯѧ½á¹¹:2014030601021
ÊÊÓ¦Ö¢: Ѫ˨
רÀûÕªÒª: The present invention provides compounds of Formula (I): Formula (I) as defined in the specification and compositions comprising any of such novel compounds. These compounds are antagonists of P2Y1 receptor which may be used medicaments.
±¸×¢: P2Y1ÊÜÌåÞ׿¹¼Á¿ÉÒÔÓÃÓÚÖÎÁÆѪ˨¡£±¾×¨ÀûÖÐÁоٵĻ¯ºÏÎïÔÚHEK-293ϸ°ûÖУ¬Ki=11.3nM¡£
22. WO 2014022253
±êÌâ: Amino-heteroaryl 7-hydroxy-spiropiperidine indolinyl antagonists of P2Y1 receptor
ÉêÇëÈË: °ÙʱÃÀÊ©¹ó±¦
ÓÅÏÈȨÈÕÆÚ¼°Ïà¹ØרÀû¹«¿ªºÅ: 2012 US 678190
Ïà¹ØºòÑ¡Ò©ÎïÀàÐÍ: С·Ö×ÓÒ©Îï
Ïà¹ØºòÑ¡Ò©Îﻯѧ½á¹¹:2014030601022
ÊÊÓ¦Ö¢: Ѫ˨
רÀûÕªÒª: The present invention provides compounds of Formula (I): as defined in the specification and compositions comprising any of such novel compounds. These compounds are antagonists of P2Y1 receptor which may be used as medicaments.
±¸×¢: P2Y1ÊÜÌåÞ׿¹¼Á¿ÉÒÔÓÃÓÚÖÎÁÆѪ˨¡£±¾×¨ÀûÖÐÁоٵĻ¯ºÏÎïÔÚHEK-293ϸ°ûÖУ¬Ki=16 nM¡£
23. WO 2014021281
±êÌâ: Partially saturated nitrogen-containing heterocyclic compound
ÉêÇëÈË: Taisho Pharmaceutical Co., Ltd.
ÓÅÏÈȨÈÕÆÚ¼°Ïà¹ØרÀû¹«¿ªºÅ: 2012 JP 168828
Ïà¹ØºòÑ¡Ò©ÎïÀàÐÍ: С·Ö×ÓÒ©Îï
Ïà¹ØºòÑ¡Ò©Îﻯѧ½á¹¹:2014030601023
ÊÊÓ¦Ö¢: ƶѪ
רÀûÕªÒª: Provided is a compound which is represented by general formula (I¡¯) and has an excellent PHD2-inhibiting activity or a pharmaceutically acceptable salt thereof. (In the general formula (I¡¯), W, Y, R2, R3, R4 and Y4 are as defined in the description.)
±¸×¢: ȱÑõÓÕµ¼Òò×Ó£¨HIF£©¸¬°±õ£ôÇ»¯Ã¸2£¨PHD2£©ÒÖÖƼÁ¶ÔƶѪ֢µÄÖÎÁÆÓÐЧ¡£±¾×¨ÀûÖеĻ¯ºÏÎïÔÚ293FTϸ°ûÖпÉÒÔÒÖÖÆPHD2£¬ÆäIC50=14 nM¡£
24. WO 2014020350
±êÌâ: PAR2 receptor antagonists
ÉêÇëÈË: Proximagen Ltd.
ÓÅÏÈȨÈÕÆÚ¼°Ïà¹ØרÀû¹«¿ªºÅ: 2012 GB 13700£»2013 GB 52069
Ïà¹ØºòÑ¡Ò©ÎïÀàÐÍ: С·Ö×ÓÒ©Îï
Ïà¹ØºòÑ¡Ò©Îﻯѧ½á¹¹:2014030601024
ÊÊÓ¦Ö¢: Ñ×Ö¢£»Ö×Áö£»ÌØÒìÐÔƤÑ×£»³¦Ñ×£»³¦Ò××ÛºÏÕ÷£»ÌÛÍ´£»Òøм²¡
רÀûÕªÒª: Compounds of formula (I) or pharmaceutically acceptable salts, solvates or hydrates thereof wherein P, Q, X, Y, R1, R2, R3, R10, R11, and R12 are as defined in the claims, and the use those compounds in medicine.
±¸×¢: PAR2Þ׿¹¼Á¿ÉÒÔÓÃÓÚÖÎÁÆÑ×Ö¢¡¢Ö×Áö¡¢ÌÛÍ´¡¢Òøм²¡µÈ¼²²¡¡£±¾×¨ÀûÖеÄʾÀý»¯ºÏÎï¶ÔPAR2µÄIC500.1 mcM¡£
25. WO 2014022728£»US 2014038952
±êÌâ: Substituted 5-(quinazolin-2-yl)pyrimidin-2-amine derivatives useful as PI3K/mTOR inhibitors for the treatment of cancer
ÉêÇëÈË: Endo Pharmaceuticals Inc.
ÓÅÏÈȨÈÕÆÚ¼°Ïà¹ØרÀû¹«¿ªºÅ: 2013 US 957470£»2012 US 678694
Ïà¹ØºòÑ¡Ò©ÎïÀàÐÍ: С·Ö×ÓÒ©Îï
Ïà¹ØºòÑ¡Ò©Îﻯѧ½á¹¹:2014030601025
ÊÊÓ¦Ö¢: Ö×Áö£»Ñ×Ö¢
רÀûÕªÒª: The present application provides novel substituted quinazoline and pyrido-pyrimidine compounds of formula (I) and pharmaceutically acceptable salts, prodrugs, and solvates thereof. Also provided are methods for preparing these compounds. These compounds are useful in co-regulating PI3K and/or mTOR activity by administering a therapeutically effective amount of one or more of the compounds to a patient. By doing so, these compounds are effective in treating conditions associated with the dysregulation of the PI3K/AKT/mTOR pathway. Advantageously, these compounds perform as dual PI3K/mTOR inhibitors. A variety of conditions can be treated using these compounds and include diseases which are characterized by inflammation or abnormal cellular proliferation. In one embodiment, the disease is cancer.
±¸×¢: PI3Kalpha/mTOR(FRAP1)ÒÖÖƼÁ¿ÉÒÔÓÃÓÚÖÎÁÆÑ×Ö¢ºÍÖ×Áö¡£ ±¾×¨ÀûÖеĻ¯ºÏÎïÔÚH1047R¡¢E545K ºÍmTORµÄIC50¾ùСÓÚ50 nM£¬¶Ô PI3K beta and gammaµÄIC50¾ùСÓÚ500 nM£¬¶ÔPI3KdeltaµÄIC50 1mcM¡£
26. US 2014045856£»US 2014045857£»WO 2014019979
±êÌâ: 4-Methyl-2,3,5,9,9b-pentaaza-cyclopenta[a]naphthalenes
ÉêÇëÈË: ²ªÁÖ¸ñÒó¸ñº²
ÓÅÏÈȨÈÕÆÚ¼°Ïà¹ØרÀû¹«¿ªºÅ: 2012 EP 178713
Ïà¹ØºòÑ¡Ò©ÎïÀàÐÍ: С·Ö×ÓÒ©Îï
Ïà¹ØºòÑ¡Ò©Îﻯѧ½á¹¹:2014030601026
ÊÊÓ¦Ö¢: °¢¶û×Ⱥ£Ä¬£»¼ÇÒäȱÏÝ
רÀûÕªÒª: The invention relates to 4-methyl-2,3,5,9,9b-pentaaza-cyclopenta[a]naphthalene derivatives of general formula (I) which are inhibitors of phosphodiesterase 2 and/or 10, useful in treating central nervous system diseases and other diseases. In addition, the invention relates to processes for preparing pharmaceutical compositions as well as processes for manufacture the compounds according to the invention.
±¸×¢: PDE2AºÍ/»òPDE10AÒÖÖƼÁ¿ÉÒÔÓÃÓÚÖÎÁÆ°¢¶û×Ⱥ£Ä¬ºÍ¼ÇÒäȱÏݵȾ«ÉñÀ༲²¡¡£±¾×¨ÀûÖеÄÒ»¸öʾÀýÐÔ»¯ºÏÎï·Ö±ðÔÚ¶ÔPDE2AµÄIC50 = 0.071mcM£¬¶ÔPD10AµÄIC50 = 3.01mcM¡£
27. WO 2014019908
±êÌâ: Substituted pyrroles active as kinases inhibitors
ÉêÇëÈË: Nerviano Medical Sciences Srl
ÓÅÏÈȨÈÕÆÚ¼°Ïà¹ØרÀû¹«¿ªºÅ: 2012 EP 178946
Ïà¹ØºòÑ¡Ò©ÎïÀàÐÍ: С·Ö×ÓÒ©Îï
Ïà¹ØºòÑ¡Ò©Îﻯѧ½á¹¹:2014030601027
ÊÊÓ¦Ö¢: ¶¯ÂöÖàÑùÓ²»¯£»Ö×Áö£»ÃâÒߣ»HIV¸ÐȾ£»Éñ¾ÍËÐм²²¡£»Ç°ÁÐÏÙÔöÉú£»Òøм²¡£»Öзç
רÀûÕªÒª: The present invention relates to substituted pyrrole compounds which modulate the activity of protein kinases and are therefore useful in treating diseases caused by dysregulated protein kinase activity, in particular Jak family kinases. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising these compounds, and methods of treating diseases utilizing such compounds or the pharmaceutical compositions containing them.
±¸×¢: Janus ¼¤Ã¸ÒÖÖƼÁ¿ÉÒÔÓÃÓÚÖÎÁÆÖ×Áö¡¢¶¯ÂöÖàÑùÓ²»¯¡¢ÃâÒߵȶàÖÖ¼²²¡¡£±¾×¨ÀûÖÐÌṩµÄʾÀý»¯ºÏÎï¶ÔJak1, Jak2 ºÍ Tyk2 µÄ IC50¾ùΪ0.001 mcM¡£
28. WO 2014019023
±êÌâ: alpha7 Nicotinic acetylcholine receptor modulators and uses thereof-I
ÉêÇëÈË: Bionomics Ltd.
ÓÅÏÈȨÈÕÆÚ¼°Ïà¹ØרÀû¹«¿ªºÅ: 2012 AU 903296£»2013 AU 900167
Ïà¹ØºòÑ¡Ò©ÎïÀàÐÍ: С·Ö×ÓÒ©Îï
Ïà¹ØºòÑ¡Ò©Îﻯѧ½á¹¹:2014030601028
ÊÊÓ¦Ö¢: ÈÏÖªÕÏ°£»Ñ×Ö¢£»Éñ¾ÍËÐÐÐÔ¼²²¡£»Éñ¾ÌÛÍ´
רÀûÕªÒª: The present invention relates to chemical compounds of formula (I), with the substituents as described in the specification, useful in the positive modulation of the alpha 7 nicotinic acetylcholine receptor (a7 nAChR). The invention also relates to the use of these compounds in the treatment or prevention of a broad range of diseases in which the positive modulation of a7 nAChR is advantageous, including neurodegenerative and neuropsychiatric diseases and also neuropathic pain and inflammatory diseases.
±¸×¢: alpha7 Ñ̼îÒÒõ£µ¨¼îÊÜÌ壨nAChRµÄ£©µÄµ÷½Ú¼Á¿É×÷ΪÑ×Ö¢¡¢ÈÏÖªÕÏ°¡¢Éñ¾ÌÛÍ´µÈ¼²²¡µÄÖÎÁÆÓÃ;¡£±¾×¨ÀûÌṩµÄʾÀý»¯ºÏÎï¶ÔÓÚ alpha7ÊÜÌå¾ßÓкܺõĻîÐÔ¡£
29. WO 2014018887
±êÌâ: ATX modulating agents
ÉêÇëÈË: Biogen Idec Inc.
ÓÅÏÈȨÈÕÆÚ¼°Ïà¹ØרÀû¹«¿ªºÅ: 2012 US 676698
Ïà¹ØºòÑ¡Ò©ÎïÀàÐÍ: С·Ö×ÓÒ©Îï
Ïà¹ØºòÑ¡Ò©Îﻯѧ½á¹¹:2014030601029
ÊÊÓ¦Ö¢: ¶à·¢ÐÔÓ²»¯Ö¢£»ÂýÐÔÌÛÍ´£»Àà·çʪÐԹؽÚÑ×
רÀûÕªÒª: Compounds of formula (I) can modulate the activity of autotaxin (ATX).
±¸×¢: ENPP2ÒÖÖƼÁ»òSIPµ÷½Ú¼Á¿ÉÓÃÓÚÀà·çʪÐԹؽÚÑ׹ؽÚÑס¢¶à·¢ÐÔÓ²»¯Ö¢ºÍÌÛÍ´¡¢Ö×Áö¡¢ÃâÒߵȼ²²¡µÄÖÎÁÆ¡£ ʾÀýÐÔ»¯ºÏÎï¶ÔENPP2µÄIC50СÓÚ100 nM¡£
30. WO 2014018881
±êÌâ: ATX modulating agents
ÉêÇëÈË: Biogen Idec Inc.
ÓÅÏÈȨÈÕÆÚ¼°Ïà¹ØרÀû¹«¿ªºÅ: 2012 US 676705
Ïà¹ØºòÑ¡Ò©ÎïÀàÐÍ: С·Ö×ÓÒ©Îï
Ïà¹ØºòÑ¡Ò©Îﻯѧ½á¹¹:2014030601030
ÊÊÓ¦Ö¢: ¶à·¢ÐÔÓ²»¯Ö¢£»ÂýÐÔÌÛÍ´£»Àà·çʪÐԹؽÚÑ×
רÀûÕªÒª: Disclosed are bicyclic aryl compounds of formula (I), that can modulate the activity of the autotaxin (ATX) enzyme. This invention further relates to compounds that are ATX inhibitors, and methods of making and using such compounds in the treatment of demyelination due to injury or disease, as well as for treating proliferative disorders such as cancer.
±¸×¢: ENPP2ÒÖÖƼÁ»òSIPµ÷½Ú¼Á¿ÉÓÃÓÚÀà·çʪÐԹؽÚÑ׹ؽÚÑס¢¶à·¢ÐÔÓ²»¯Ö¢ºÍÌÛÍ´¡¢Ö×Áö¡¢ÃâÒߵȼ²²¡µÄÖÎÁÆ¡£ ʾÀýÐÔ»¯ºÏÎï¶ÔENPP2µÄIC50СÓÚ100 nM¡£
31. WO 2014018919
±êÌâ: Seriniquinones, melanoma-specific anticancer agents
ÉêÇëÈË: University of California, Oakland
ÓÅÏÈȨÈÕÆÚ¼°Ïà¹ØרÀû¹«¿ªºÅ: 2012 US 676427
Ïà¹ØºòÑ¡Ò©ÎïÀàÐÍ: С·Ö×ÓÒ©Îï
Ïà¹ØºòÑ¡Ò©Îﻯѧ½á¹¹:2014030601031
ÊÊÓ¦Ö¢: Ö×Áö
רÀûÕªÒª: Accordingly, there are provided, inter alia, derivatives of seriniquinone and methods useful for the treatment of cancer, and in particular treatment of melanoma and prostate cancer.
±¸×¢: SeriniquinonesÑÜÉúÎï¿ÉÒÔ×÷ΪdermcidinÒÖÖƼÁͨ¹ýÓÕµ¼µòÍöµÄ»úÖÆÓÃÓÚÖ×Áö£¬ÓÈÆäÊǺÚÉ«ËØÁöºÍÇ°ÁÐÏÙ°©µÄÖÎÁÆ¡£±¾×¨ÀûÖеÄʾÀý»¯ºÏÎï¶Ô·ÇСϸ°û·Î°©Ï¸°û¡¢Éö°©¡¢Âѳ²°©¡¢Ç°ÁÐÏÙ°©¡¢ÈéÏÙ°©µÈϸ°ûµÄÒÖÖÆ»îÐÔ´ïµ½10 mcM¡£
32. WO 2014016300
±êÌâ: Glucagon analogues
ÉêÇëÈË: Zealand Pharma A/S
ÓÅÏÈȨÈÕÆÚ¼°Ïà¹ØרÀû¹«¿ªºÅ: 2012 US 674706£»2013 DK 360£»2013 US 785611
Ïà¹ØºòÑ¡Ò©ÎïÀàÐÍ: ¶àëÄ
Ïà¹ØºòÑ¡Ò©Îﻯѧ½á¹¹:2014030601032
ÊÊÓ¦Ö¢: µÍѪÌÇ
רÀûÕªÒª: The present invention relates to glucagon analogues and their medical use, for example in the treatment of hypoglycaemia. In particular, the present invention relates to stable glucagon analogues suitable for use in a liquid formulation.
±¸×¢: GCGRÊÜÌ弤¶¯¼Á¿ÉÒÔÓÃÓÚµÍѪÌÇ¡¢·ÊÅÖ¡¢¸ßѪѹ¡¢¶¯ÂöÖàÑùÓ²»¯µÈ¼²²¡µÄÖÎÁÆ¡£±¾×¨ÀûÖеÄʾÀý»¯ºÏÎï¶ÔÈËÔ´GCGRµÄEC50 = 0.15 nM¡£
33. EP 2689786£»WO 2014016312
±êÌâ: HPV/CyaA-based chimeric proteins and their uses in the induction of immune responses against HPV infection and HPV-induced disorders
ÉêÇëÈË: Genticel SA
ÓÅÏÈȨÈÕÆÚ¼°Ïà¹ØרÀû¹«¿ªºÅ: 2012 EP 305898
Ïà¹ØºòÑ¡Ò©ÎïÀàÐÍ: ÒßÃç
Ïà¹ØºòÑ¡Ò©Îﻯѧ½á¹¹:
ÊÊÓ¦Ö¢: ÈéÍ·×´Áö²¡¶¾¸ÐȾ
רÀûÕªÒª: The invention relates to a chimeric protein comprising or consisting of, from N-terminal to C-terminal, (a) a N-terminal part of a Bordetella CyaA protein (b) a heterologous polypeptide comprising antigens originating from different HPVs, and (c) a C-terminal part of a Bordetella CyaA protein. The invention also relates to a polynucleotide encoding this chimeric protein. A composition comprising at least one chimeric protein(s) of the invention and the prophylactic and/or therapeutic uses of said composition are also part of the invention.
±¸×¢: ÓÐE7µ°°×ÑÜÉúÎï×é³ÉµÄ¶àëÄ¿ÉÒÔ×÷ΪÒßÃ磬ÓÃÓÚHPV¸ÐȾµÄÖÎÁÆ¡£±¾×¨ÀûÌṩÁ˶ÔHPV¸ÐȾÓÐЧµÄÒßÃç¡£
34. FR 2993562;WO 2014016507
±êÌâ: Novel selective compounds inhibiting CYP26A1 useful in cosmetic and pharmaceutical compositions
ÉêÇëÈË: Galderma Research & Development, SNC
ÓÅÏÈȨÈÕÆÚ¼°Ïà¹ØרÀû¹«¿ªºÅ: 2012 FR 57128
Ïà¹ØºòÑ¡Ò©ÎïÀàÐÍ: С·Ö×ÓÒ©Îï
Ïà¹ØºòÑ¡Ò©Îﻯѧ½á¹¹:2014030601034
ÊÊÓ¦Ö¢: Ƥ·ô²¡
רÀûÕªÒª: The present invention relates to novel compounds or to any of the salts thereof having the general formula (I), to the pharmaceutical and cosmetic compositions containing said compounds as well as to the use of said compounds and compositions for the treatment of diseases.
±¸×¢: ϸ°ûÉ«ËØ P450 CYP26A1ÒÖÖƼÁ¿ÉÒÔÓÃÓÚÖÎÁÆƤ·ôÀ༲²¡¡£±¾×¨ÀûÖеÄÒ»¸öʾÀý»¯ºÏÎï¶Ô CYP26A1µÄAC50 = 0.19 mcM£»¶ÔCYP26B1µÄAC50 = 50.33 mcM¡£
35. WO 2014016787
±êÌâ: Peptide-based compounds and uses thereof to treat beta-amyloid accumulation
ÉêÇëÈË: Pharma Bio, LLC.
ÓÅÏÈȨÈÕÆÚ¼°Ïà¹ØרÀû¹«¿ªºÅ: 2012 US 675205
Ïà¹ØºòÑ¡Ò©ÎïÀàÐÍ: ¶àëÄ
Ïà¹ØºòÑ¡Ò©Îﻯѧ½á¹¹:2014030601035
ÊÊÓ¦Ö¢: °¢¶û×Ⱥ£Ä¬
רÀûÕªÒª: The present application relates to novel peptide-based compounds, optionally comprising an immunoactive built-in adjuvant, compositions comprising these compounds and their use, in particular for the treatment of diseases, disorders or conditions characterized by or associated with ß- amyloid accumulation. In particular, the present application includes compounds of Formula I, and compositions and uses thereof: [Ra-NP]m-Lp (I).
±¸×¢: ¿ÉÒÔÒÖÖƦÂ-µí·ÛÑùµ°°×µÄ¶àëÄ¿ÉÒÔÓÃ×÷°¢¶û×Ⱥ£Ä¬¡¢ÌÆÊÏ×ÛºÏÖ¢µÈ¼²²¡µÄÖÎÁÆ¡£±¾×¨ÀûÌṩÁ˾ÐÞÊεÄÓÃÓÚÒÖÖƦÂ-µí·ÛÑùµ°°×µÄ¶àëĽṹ¡£ |
» ÊÕ¼±¾ÌûµÄÌÔÌùר¼ÍƼö
» ²ÂÄãϲ»¶
» ±¾Ö÷ÌâÏà¹Ø¼ÛÖµÌùÍƼö£¬¶ÔÄúͬÑùÓаïÖú:
|