公开(公告)号：US20180208544A1

公开(公告)日：2018-07-26

申请号：US15744272

申请日：2016-07-08

申请人： PIRAMAL ENTERPRISES LIMITED

发明人： Ashutosh JAGTAP ,  Milind GHARPURE ,  Navnath SHINDE ,  Navnath PATIL ,  Changdev RAUT ,  Dhileepkumar KRISHNAMURTHY

IPC分类号： C07C227/06 ,  C07C253/30 ,  C07C229/20

CPC分类号： C07C227/06 ,  C07C229/20 ,  C07C253/30 ,  C07C255/41 ,  C07C229/34

摘要： The present invention provides an improved process for the preparation of 3-(4-chlorophenyl)-3-cyanopropanoic acid (compound (A)) and further its transformation to Baclofen (I). The process comprises reaction of compound (II) with Glyoxylic acid to obtain 3-(4-chlorophenyl)-3-cyanoacrylic acid (III); followed by the ‘in-situ’ reduction of (III) in the presence of a reducing agent to provide the compound (A). Alternatively, the compound (A) is obtained by the process comprising reacting 2-(4-chlorophenyl)acetonitrile (II) with haloacetic acid (IV) in the presence of a base. The compound 3-(4-chlorophenyl)-3-cyanopropanoic acid (A) undergoes hydrogenation in the presence of a metal catalyst and ammonia solution to provide Baclofen (I).

公开(公告)号：US09908843B2

公开(公告)日：2018-03-06

申请号：US15101582

申请日：2014-12-05

申请人： Canbex Therapeutics Limited

发明人： David Selwood

IPC分类号： C07C233/83 ,  C07C231/12 ,  C07C303/40 ,  C07C311/46 ,  C07D207/06 ,  C07C311/06 ,  C07C311/13 ,  C07C233/87 ,  C07C255/41 ,  C07D213/64 ,  C07D295/10 ,  C07C253/30 ,  C07D211/16 ,  C07D277/30

CPC分类号： C07C233/83 ,  C07C231/12 ,  C07C233/87 ,  C07C253/30 ,  C07C255/41 ,  C07C303/40 ,  C07C311/06 ,  C07C311/13 ,  C07C311/46 ,  C07D207/06 ,  C07D211/16 ,  C07D213/64 ,  C07D277/30 ,  C07D295/10

摘要： The present invention relates to a compound of formula I, or a pharmaceutically acceptable salt thereof: (I) wherein: n is 0 or 1; R1 is selected from H, alkyl and aralkyl, wherein said alkyl and aralkyl groups may be optionally substituted by one or more OH groups; X is a group selected from —C≡C—(CH2)p—; —C(R5)═C(R6)—(CH2)q—; and —C(R5)(R6)C(R7)(R8)—(CH2)r-; where each of R5, R6, R7 and R8 is independently H or alkyl, and each of p, q and r is independently 1, 2, 3, 4 or 5; Y is a group selected from: CN; COOR2; CONR3R4; SO2NR9R10; NR12COR13; NR14SO2R15; and a heterocyclic group selected from oxadiazolyl, thiazolyl, iso-thiazolyl, oxazolyl, iso-oxazolyl, pyrazolyl and imidazolyl; where each of R2, R3 and R4 is independently H or alkyl; or R3 and R4 are linked, together with the nitrogen to which they are attached, to form a 5 or 6-membered heterocycloalkyl or heterocycloalkenyl group, said heterocycloalkyl or heterocycloalkenyl group optionally containing one or more further groups selected from O, N, CO and S, and where each of R9, R10, R11, R12, R13, R14 and R15 is independently H or alkyl. Further aspects of the invention relate to the use of such compounds in the preparation of a medicament for the treatment of a muscular disorder, pain, or for controlling spasticity or tremors, for example, spasticity in MS.

公开(公告)号：US09611246B2

公开(公告)日：2017-04-04

申请号：US14792421

申请日：2015-07-06

申请人： HALLSTAR INNOVATIONS CORP.

发明人： Craig A. Bonda ,  Shengkui Hu ,  Qing Jean Zhang ,  Zhihui Zhang

IPC分类号： C07C255/41 ,  C07C69/618 ,  C07D335/12 ,  C07D311/82 ,  A61K8/37 ,  A61K8/40 ,  A61K8/49 ,  A61Q17/04 ,  C07C325/04 ,  C07C327/22 ,  C07C255/34 ,  C07C255/40 ,  A61K8/35 ,  A61K41/00 ,  A61K47/14 ,  A61K47/16 ,  A61K47/22

CPC分类号： C07D335/12 ,  A61K8/35 ,  A61K8/37 ,  A61K8/40 ,  A61K8/494 ,  A61K8/498 ,  A61K8/4986 ,  A61K41/0071 ,  A61K47/14 ,  A61K47/16 ,  A61K47/22 ,  A61K2800/522 ,  A61Q17/04 ,  C07C69/618 ,  C07C255/34 ,  C07C255/40 ,  C07C255/41 ,  C07C325/04 ,  C07C327/22 ,  C07C2603/18 ,  C07C2603/24 ,  C07D311/82 ,  Y10T428/249921

摘要： The present disclosure relates, according to some embodiments, to molecules, including conjugated fused polycyclic molecules, that may receive excited state energy from other molecules (e.g., light-absorbing molecules) or directly from the irradiation sources. According to some embodiments, the disclosure relates to molecules, including conjugated fused polycyclic molecules, that may resolve (e.g., quench, dissipate) excited state energy, normally by way of releasing it as heat. (e.g., as heat). Conjugated fused polycyclic molecules of various structures are disclosed including Formula III: The disclosure further relates to methods of use and/or therapy using molecules of Formulas I, II, and/or III.

公开(公告)号：US20160304441A1

公开(公告)日：2016-10-20

申请号：US15101582

申请日：2014-12-05

申请人： CANBEX THERAPEUTICS LIMITED

发明人： David Selwood

IPC分类号： C07C233/83 ,  C07D277/30 ,  C07C311/46 ,  C07C303/40 ,  C07D213/64 ,  C07C253/30 ,  C07D295/10 ,  C07D207/06 ,  C07D211/16 ,  C07C231/12 ,  C07C255/41

CPC分类号： C07C233/83 ,  C07C231/12 ,  C07C233/87 ,  C07C253/30 ,  C07C255/41 ,  C07C303/40 ,  C07C311/06 ,  C07C311/13 ,  C07C311/46 ,  C07D207/06 ,  C07D211/16 ,  C07D213/64 ,  C07D277/30 ,  C07D295/10

摘要： The present invention relates to a compound of formula I, or a pharmaceutically acceptable salt thereof : (I) wherein: n is 0 or 1; R1 is selected from H, alkyl and aralkyl, wherein said alkyl and aralkyl groups may be optionally substituted by one or more OH groups; X is a group selected from —C≡C—(CH2)p—; —C(R5)═C(R6)—(CH2)q—; and —C(R5)(R6)C(R7)(R8)—(CH2)r—; where each of R5, R6, R7 and is independently II or alkyl, and each of p, q and r is independently 1, 2, 3, 4 or 5; Y is a group selected from: CN; COOR2; CONR3R4; SO2NR9R10; NR12COR13; NR14SO2R15; and a heterocyclic group selected from oxadiazolyl, thiazolyl, isothiazolyl, oxazolyl, iso-oxazolyl, pyrazolyl and imidazolyl; where each of R2, R3 and R4 is independently H or alkyl; or R3 and R4 are linked, together with the nitrogen to which they are attached, to form a 5 or 6-membered heterocycloalkyl or heterocycloalkenyl group, said heterocycloalkyl or heterocycloalkenyl group optionally containing one or more further groups selected from O, N, CO and S, and where each of R9, R10, R11, R12, R13, R14 and R15 is independently H or alkyl. Further aspects of the invention relate to the use of such compounds in the preparation of a medicament for the treatment of a muscular disorder, pain, or for controlling spasticity or tremors, for example, spasticity in MS.

公开(公告)号：US09388124B2

公开(公告)日：2016-07-12

申请号：US13996549

申请日：2011-12-22

申请人： Gunnar Grue-Sørensen ,  Xifu Liang ,  Thomas Högberg

发明人： Gunnar Grue-Sørensen ,  Xifu Liang ,  Thomas Högberg

IPC分类号： C07C251/44 ,  C07C233/56 ,  C07C251/48 ,  C07C255/23 ,  C07C255/41 ,  C07C69/013 ,  C07C69/24 ,  C07C69/533 ,  C07C69/54 ,  C07C69/608 ,  C07C69/614 ,  C07C69/616 ,  C07C69/60 ,  C07C69/618

CPC分类号： C07C255/41 ,  C07C69/013 ,  C07C69/24 ,  C07C69/533 ,  C07C69/54 ,  C07C69/60 ,  C07C69/608 ,  C07C69/614 ,  C07C69/616 ,  C07C69/618 ,  C07C233/56 ,  C07C251/44 ,  C07C251/48 ,  C07C255/23 ,  C07C2601/14 ,  C07C2603/86

摘要： The invention relates to compounds of general formula (I) wherein R is (C1-C7)alkyl, (C2-C7)alkenyl or (C2-C7)alkynyl; wherein R is substituted with R1; and pharmaceutically acceptable salts, hydrates, or solvates thereof, for use—alone or in combination with one or more other pharmaceutically active compounds—in therapy, for preventing, treating or ameliorating diseases or conditions responsive to stimulation of neutrophil oxidative burst, responsive to stimulation of keratinocyte IL-8 release or responsive to induction of necrosis.

摘要翻译： 本发明涉及通式（I）的化合物，其中R是（C 1 -C 7）烷基，（C 2 -C 7）烯基或（C 2 -C 7）炔基; 其中R被R 1取代; 其药学上可接受的盐，水合物或溶剂合物，用于单独或与一种或多种其它药学活性化合物组合用于治疗，用于预防，治疗或改善响应刺激的中性粒细胞氧化性突发的反应的疾病或病症 的角质形成细胞IL-8释放或响应于坏死的诱导。

公开(公告)号：US20160168083A1

公开(公告)日：2016-06-16

申请号：US15047431

申请日：2016-02-18

申请人： REGENTS OF THE UNIVERSITY OF MINNESOTA

发明人： Venkatram R. Mereddy ,  Lester R. Drewes ,  Mohammed Abrar Alam ,  Sravan K. Jonnalagadda ,  Shirisha Gurrapu

IPC分类号： C07C255/41 ,  C07D311/16 ,  C07D407/14 ,  C07D295/155

CPC分类号： C07C255/41 ,  C07C255/63 ,  C07D207/09 ,  C07D295/155 ,  C07D311/12 ,  C07D311/16 ,  C07D405/04 ,  C07D407/14

摘要： The invention provides compounds of formula I: or a salt thereof as described herein. The invention also provides pharmaceutical compositions comprising a compound of formula I, processes for preparing compounds of formula I, intermediates useful for preparing compounds of formula I and therapeutic methods for treating cancer or treating autoimmune diseases or preventing transplant rejection using compounds of formula I.

摘要翻译： 本发明提供了本文所述的式I化合物或其盐。 本发明还提供包含式I化合物的药物组合物，制备式I化合物的方法，可用于制备式I化合物的中间体和用于治疗癌症或治疗自身免疫性疾病或使用式I化合物预防移植排斥的治疗方法。

公开(公告)号：US20160145199A1

公开(公告)日：2016-05-26

申请号：US14899883

申请日：2014-07-04

申请人： UNIVERSITE DE STRASBOURG ,  CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE

发明人： Alain Wagner ,  Oleksandr Koniev

IPC分类号： C07C255/43 ,  C07C255/41 ,  C07C255/35 ,  C07C255/34 ,  C07D249/06 ,  C07C331/28 ,  C07C335/22 ,  C07F7/08 ,  C07F5/04 ,  C07D207/452 ,  C07K19/00 ,  C12N9/36 ,  C07K14/705 ,  C07K16/28 ,  C07K16/30 ,  C07C255/44

CPC分类号： C07C255/43 ,  C07B2200/05 ,  C07C255/34 ,  C07C255/35 ,  C07C255/37 ,  C07C255/41 ,  C07C255/42 ,  C07C255/44 ,  C07C271/16 ,  C07C271/22 ,  C07C271/28 ,  C07C275/42 ,  C07C309/42 ,  C07C319/02 ,  C07C323/42 ,  C07C323/60 ,  C07C331/28 ,  C07C335/22 ,  C07C2602/24 ,  C07D207/452 ,  C07D207/46 ,  C07D249/06 ,  C07D265/38 ,  C07D311/82 ,  C07D311/88 ,  C07D337/04 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D495/04 ,  C07F5/04 ,  C07F7/08 ,  C07F7/081 ,  C07F9/5442 ,  C07K1/13 ,  C07K14/70596 ,  C07K16/2863 ,  C07K16/30 ,  C07K16/32 ,  C07K19/00 ,  C07K2317/24 ,  C07K2317/76 ,  C12N9/2462 ,  C12Y302/01017 ,  G01N33/58 ,  G01N33/84

摘要： The present invention relates to a process for labeling compounds comprising thiol moieties with 3-arylpropiolonitrile compounds, to 3-arylpropiolonitrile compounds substituted with tag moieties and to specific 3-arylpropiolonitrile linkers.

摘要翻译： 本发明涉及将含有3-芳基丙炔腈化合物的硫醇部分的化合物标记为被标记部分取代的3-芳基丙炔腈化合物和特定3-芳基丙炔腈接头的方法。

公开(公告)号：US20160002200A1

公开(公告)日：2016-01-07

申请号：US14792437

申请日：2015-07-06

申请人： HALLSTAR INNOVATIONS CORP.

发明人： Craig A. Bonda ,  Shengkui Hu ,  Qing Jean Zhang ,  Zhihui Zhang

IPC分类号： C07D335/12 ,  C07C255/41 ,  C07C69/618 ,  C07D311/82

CPC分类号： C07D335/12 ,  A61K8/35 ,  A61K8/37 ,  A61K8/40 ,  A61K8/494 ,  A61K8/498 ,  A61K8/4986 ,  A61K41/0071 ,  A61K47/14 ,  A61K47/16 ,  A61K47/22 ,  A61K2800/522 ,  A61Q17/04 ,  C07C69/618 ,  C07C255/34 ,  C07C255/40 ,  C07C255/41 ,  C07C325/04 ,  C07C327/22 ,  C07C2603/18 ,  C07C2603/24 ,  C07D311/82 ,  Y10T428/249921

摘要： The present disclosure relates, according to some embodiments, to molecules, including conjugated fused polycyclic molecules, that may receive excited state energy from other molecules (e.g., light-absorbing molecules) or directly from the irradiation sources. According to some embodiments, the disclosure relates to molecules, including conjugated fused polycyclic molecules, that may resolve (e.g., quench, dissipate) excited state energy, normally by way of releasing it as heat. (e.g., as heat). Conjugated fused polycyclic molecules of various structures are disclosed including Formula III: The disclosure further relates to methods of use and/or therapy using molecules of Formulas I, II, and/or III.

公开(公告)号：US20150038466A1

公开(公告)日：2015-02-05

申请号：US14369674

申请日：2012-12-31

申请人： ECOLE NATIONALE SUPERIEURE DE CHIMIE DE CLERMONT FERRAND ,  UNIVERSITE D'AUVERGNE CLERMONT I

发明人： Sylvie Ducki ,  Khalil Bennis ,  Alain Eschalier ,  Jérôme Busserolles ,  Florian Lesage ,  Nuno Rodriguez ,  Delphine Vivier

IPC分类号： C07C57/60 ,  C07F9/09 ,  C07D209/42 ,  C07C229/34 ,  C07C255/41 ,  C07D307/54

CPC分类号： C07C57/60 ,  C07C229/34 ,  C07C255/41 ,  C07C2601/14 ,  C07D209/18 ,  C07D209/42 ,  C07D307/54 ,  C07F9/09 ,  C07F9/12

摘要： The present invention relates to the use of compounds for the treatment or prevention of pain in mammals, in particularly in human beings, and also to a process for preparing these compounds.

摘要翻译： 本发明涉及化合物用于治疗或预防哺乳动物，特别是人类疼痛的用途，以及这些化合物的制备方法。

公开(公告)号：US20140235446A1

公开(公告)日：2014-08-21

申请号：US14131891

申请日：2012-07-11

申请人： Marc Mosrin ,  Harald Jakobi ,  Alfred Angermann ,  Elmar Gatzweiler ,  Isolde Häuser-Hahn ,  Ines Heinemann ,  Christopher Hugh Rosinger ,  Stefan Lehr ,  Stefan Schnatterer

发明人： Marc Mosrin ,  Harald Jakobi ,  Alfred Angermann ,  Elmar Gatzweiler ,  Isolde Häuser-Hahn ,  Ines Heinemann ,  Christopher Hugh Rosinger ,  Stefan Lehr ,  Stefan Schnatterer

IPC分类号： A01N43/80 ,  A01N37/34 ,  A01N43/32 ,  A01N37/42 ,  A01N43/56 ,  A01N43/16

CPC分类号： A01N43/80 ,  A01N37/34 ,  A01N37/42 ,  A01N43/16 ,  A01N43/32 ,  A01N43/56 ,  C07C255/40 ,  C07C255/41 ,  C07C255/56 ,  C07C255/62 ,  C07C255/66 ,  C07C2601/10 ,  C07C2601/16 ,  C07C2602/44 ,  C07D231/12 ,  C07D231/16 ,  C07D231/20 ,  C07D261/08 ,  C07D319/06

摘要： The compounds of the formula (I) in which L represents a radical of the formula and A1, B1 and A2 and B2 are as defined in Claim 1, are suitable as herbicides for the control of harmful plants or as plant growth regulators. The compounds can be prepared by the process of Claim 12.

摘要翻译： 式（I）的化合物，其中L代表下式的基团，A1，B1和A2和B2如权利要求1所定义，适合作为用于控制有害植物或作为植物生长调节剂的除草剂。 化合物可以通过权利要求12的方法制备。