公开(公告)号：US20090068282A1

公开(公告)日：2009-03-12

申请号：US12288382

申请日：2008-10-20

Applicant: Gunther Schlingloff ,  Torsten Wieprecht ,  Frank Bachmann ,  Josef Dannacher ,  Marie-Josee Dubs ,  Menno Hazenkamp ,  Grit Hansler (-Richter) ,  Brigitte Schmidt ,  Albert Schneider ,  Peter Weingartner

Inventor： Gunther Schlingloff ,  Torsten Wieprecht ,  Frank Bachmann ,  Josef Dannacher ,  Marie-Josee Dubs ,  Menno Hazenkamp ,  Grit Hansler (-Richter) ,  Brigitte Schmidt ,  Albert Schneider ,  Peter Weingartner

IPC: A01N59/00 ,  A01N25/00 ,  D21C3/20 ,  A01P1/00 ,  C07D213/22

CPC classification number: B01J31/1815 ,  B01J23/34 ,  B01J2231/70 ,  B01J2231/72 ,  B01J2531/16 ,  B01J2531/46 ,  B01J2531/72 ,  B01J2531/842 ,  B01J2531/845 ,  B01J2531/847 ,  C07D213/61 ,  C07D213/68 ,  C07D213/74 ,  C07F13/005 ,  C11D3/3932 ,  D06L4/10 ,  D06L4/12 ,  D06P5/02 ,  D06P5/153 ,  D21C9/1036 ,  D21C9/163

Abstract: Use of metal complex compounds of formula [LnMemXp]zYq  (1), wherein Me is manganese, titanium, iron, cobalt, nickel or copper, X is a coordinating or bridging radical, n and m are each independently of the other an integer having a value of from 1 to 8, p is an integer having a value of from 0 to 32, z is the charge of the metal complex, Y is a counter-ion, q=z/(charge Y), and L is a ligand of formula wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10 and R11 are each independently of the others hydrogen; unsubstituted or substituted C1-C18alkyl or aryl; cyano; halogen; nitro; —COOR12 or —SO3R12 wherein R12 is in each case hydrogen, a cation or unsubstituted or substituted C1-C18alkyl or aryl; —SR13, —SO2R13 or —OR13 wherein R13 is in each case hydrogen or unsubstituted or substituted C1-C18alkyl or aryl; —N(R13)—NR′13R″13 wherein R13, R′13 and R″13 are as defined above for R13; —NR14R15 or —N⊕R14R15R16 wherein R14, R15 and R16 are each independently of the other(s) hydrogen or unsubstituted or substituted C1-C18alkyl or aryl, or R14 and R15 together with the nitrogen atom bonding them form an unsubstituted or substituted 5-, 6- or 7-membered ring which may optionally contain further hetero atoms; with the proviso that R1, R2, R3, R4, R5, R6, R7, R8, R9, R10 and R11 are not simultaneously hydrogen, as catalysts for oxidation reactions, and the novel metal complex compounds of formula (1) and the novel ligands of formula (2).

Abstract translation: 使用式<？in-line-formula description =“In-line Formulas”end =“lead”？> [LnMemXp] zYq（1），<？in-line-formula description =“In-line 其中Me为锰，钛，铁，钴，镍或铜，X为配位基或桥键基团，n和m各自独立地为1〜 8，p为0〜32的整数，z为金属络合物的电荷，Y为抗衡离子，q = z /（电荷Y），L为下式的配体，式中R1， R2，R3，R4，R5，R6，R7，R8，R9，R10和R11各自独立地为氢; 未取代或取代的C 1 -C 18烷基或芳基; 氰基; 卤素; 硝基 -COOR 12或-SO 3 R 12，其中R 12在各种情况下为氢，阳离子或未取代或取代的C 1 -C 18烷基或芳基; -SR 13，-SO 2 R 13或-OR 13，其中R 13各自为氢或未取代或取代的C 1 -C 18烷基或芳基; -N（R13）-NR'13R''13其中R13，R'13和R'13如上对R13所定义; -NR14R15或-N⊕R14R15R16，其中R14，R15和R16各自独立地为氢或未取代或取代的C1-C18烷基或芳基，或者R14和R15与其键合的氮原子一起形成未取代或取代的5 可以任选地含有其它杂原子的6-或7-元环; 条件是R 1，R 2，R 3，R 4，R 5，R 6，R 7，R 8，R 9，R 10和R 11不同时为氢，作为氧化反应的催化剂，并且式（1）和新颖的新型金属络合物 式（2）的配体。

公开(公告)号：US20080293684A1

公开(公告)日：2008-11-27

申请号：US11658546

申请日：2005-07-26

Applicant: Anthony B Pinkerton ,  Jean-Michel Vernier ,  Rowena V. Cube ,  John H. Hutchinson ,  Dehua Huang ,  Celine Bonnefous ,  Steven P. Govak ,  Theodore Kamenecka

Inventor： Anthony B Pinkerton ,  Jean-Michel Vernier ,  Rowena V. Cube ,  John H. Hutchinson ,  Dehua Huang ,  Celine Bonnefous ,  Steven P. Govak ,  Theodore Kamenecka

IPC: A61K31/397 ,  C07D311/02 ,  A61K31/353 ,  A61K31/12 ,  C07C49/213 ,  C07D211/72 ,  A61K31/44 ,  A61K31/505 ,  C07D239/02 ,  C07D217/22 ,  A61K31/472 ,  A61K31/497 ,  C07D401/02 ,  C07D213/24 ,  A61K31/4427 ,  C07D471/04 ,  A61K31/437 ,  A61K31/4245 ,  A61P25/08 ,  A61P25/24 ,  A61P25/18 ,  C07D213/62 ,  A61K31/444 ,  A61K31/343 ,  C07D307/77 ,  C07D473/28 ,  A61K31/522 ,  A61K31/41 ,  C07D257/04 ,  C07D263/58 ,  A61K31/423 ,  A61K31/428 ,  C07D277/20 ,  C07D205/02 ,  C07D271/10 ,  C07D215/58 ,  A61K31/47 ,  C07D403/02 ,  C07D417/02 ,  A61K31/427

CPC classification number: C07D311/16 ,  C07C45/71 ,  C07C49/84 ,  C07C69/734 ,  C07C69/92 ,  C07C217/76 ,  C07C217/92 ,  C07C235/42 ,  C07C255/54 ,  C07C323/12 ,  C07D205/04 ,  C07D209/08 ,  C07D213/30 ,  C07D213/53 ,  C07D213/64 ,  C07D213/65 ,  C07D213/68 ,  C07D213/70 ,  C07D213/71 ,  C07D213/74 ,  C07D213/84 ,  C07D213/89 ,  C07D215/20 ,  C07D217/02 ,  C07D231/56 ,  C07D233/20 ,  C07D233/60 ,  C07D235/06 ,  C07D235/08 ,  C07D235/10 ,  C07D235/16 ,  C07D235/18 ,  C07D239/34 ,  C07D257/04 ,  C07D263/58 ,  C07D271/10 ,  C07D277/74 ,  C07D307/80 ,  C07D311/22 ,  C07D311/24 ,  C07D311/58 ,  C07D401/04 ,  C07D417/04 ,  C07D471/04 ,  C07D473/38

Abstract: The present invention is directed to compounds which are potentiators of metabotropic glutamate receptors, including the mGluR2 receptor, and which are useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which metabotropic glutamate receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which metabotropic glutamate receptors are involved.

Abstract translation: 本发明涉及作为代谢型谷氨酸受体的增强剂（包括mGluR2受体）的化合物，其可用于治疗或预防与谷氨酸能力障碍相关的神经和精神病学障碍以及其中涉及代谢型谷氨酸受体的疾病。 本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在预防或治疗涉及代谢型谷氨酸受体的疾病中的用途。

公开(公告)号：US07456285B2

公开(公告)日：2008-11-25

申请号：US11497444

申请日：2006-08-01

Applicant: Gunther Schlingloff ,  Torsten Wieprecht ,  Frank Bachmann ,  Josef Dannacher ,  Marie-Josée Dubs ,  Menno Hazenkamp ,  Grit Hänsler (-Richter) ,  Brigitte Schmidt ,  Albert Schneider ,  Peter Weingartner

Inventor： Gunther Schlingloff ,  Torsten Wieprecht ,  Frank Bachmann ,  Josef Dannacher ,  Marie-Josée Dubs ,  Menno Hazenkamp ,  Grit Hänsler (-Richter) ,  Brigitte Schmidt ,  Albert Schneider ,  Peter Weingartner

IPC: C07F15/00

CPC classification number: B01J31/1815 ,  B01J23/34 ,  B01J2231/70 ,  B01J2231/72 ,  B01J2531/16 ,  B01J2531/46 ,  B01J2531/72 ,  B01J2531/842 ,  B01J2531/845 ,  B01J2531/847 ,  C07D213/61 ,  C07D213/68 ,  C07D213/74 ,  C07F13/005 ,  C11D3/3932 ,  D06L4/10 ,  D06L4/12 ,  D06P5/02 ,  D06P5/153 ,  D21C9/1036 ,  D21C9/163

Abstract: Use of metal complex compounds of formula [LnMemXp]zYq,  (1) wherein Me is manganese, titanium, iron, cobalt, nickel or copper, X is a coordinating or bridging radical, n and m are each independently of the other an integer having a value of from 1 to 8, p is an integer having a value of from 0 to 32, z is the charge of the metal complex, Y is a counter-ion, q=z/(charge Y), and L is a ligand of formula wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10 and R11, are each independently of the others hydrogen; unsubstituted or substituted C1-C18alkyl or aryl; cyano; halogen; nitro; —COOR12 or —SO3R12 wherein R12 is in each case hydrogen, a cation or unsubstituted or substituted C1-C18alkyl or aryl; —SR13, —SO2R13 or —OR13 wherein R13 is in each case hydrogen or unsubstituted or substituted C1-C18alkyl or aryl; —N(R13)—NR′13R″13 wherein R13, R′13 and R″13 are as defined above for R13; —NR14R15 or —N⊕R14R15R16 wherein R14, R15 and R16 are each independently of the other(s) hydrogen or unsubstituted or substituted C1-C18alkyl or aryl, or R14 and R15 together with the nitrogen atom bonding them form an unsubstituted or substituted 5-, 6- or 7-membered ring which may optionally contain further hetero atoms; with the proviso that R1, R2, R3, R4, R5, R6, R7, R8, R9, R10 and R11 are not simultaneously hydrogen, as catalysts for oxidation reactions, and the novel metal complex compounds of formula (1) and the novel ligands of formula (2).

公开(公告)号：US20080255155A1

公开(公告)日：2008-10-16

申请号：US11874261

申请日：2007-10-18

Applicant: Stephane Raeppel ,  Oscar Saavedra ,  Stephen Claridge ,  Arkadii Vaisburg ,  Frederic Gaudette ,  Ljubomir Isakovic ,  Robert Deziel

Inventor： Stephane Raeppel ,  Oscar Saavedra ,  Stephen Claridge ,  Arkadii Vaisburg ,  Frederic Gaudette ,  Ljubomir Isakovic ,  Robert Deziel

IPC: A61K31/506 ,  C07D239/42 ,  C07D413/02 ,  A61K31/4439 ,  C12N5/00 ,  A61P35/00 ,  C12N9/99 ,  C07D401/02 ,  C07D211/72

CPC classification number: C07D403/12 ,  C07D213/68 ,  C07D401/12 ,  C07D403/14

Abstract: This invention relates to compounds that inhibit protein tyrosine kinase activity. In particular the invention relates to compounds, compositions and methods for the inhibition of kinase activity. The invention also provides compounds, compositions and methods for treating cell proliferative diseases and conditions.

Abstract translation: 本发明涉及抑制蛋白酪氨酸激酶活性的化合物。 特别地，本发明涉及抑制激酶活性的化合物，组合物和方法。 本发明还提供了用于治疗细胞增殖性疾病和病症的化合物，组合物和方法。

公开(公告)号：US07425641B2

公开(公告)日：2008-09-16

申请号：US10938804

申请日：2004-09-10

Applicant: Uwe Ries ,  Henning Priepke ,  Armin Heckel ,  Herbert Nar ,  Wolfgang Wienen ,  Jean Marie Stassen

Inventor： Uwe Ries ,  Henning Priepke ,  Armin Heckel ,  Herbert Nar ,  Wolfgang Wienen ,  Jean Marie Stassen

IPC: C07D272/02 ,  C07D211/06 ,  A61K31/40 ,  A61K31/445

CPC classification number: C07D295/185 ,  C07C257/18 ,  C07C311/21 ,  C07C311/46 ,  C07C2601/08 ,  C07D207/12 ,  C07D211/46 ,  C07D213/68 ,  C07D295/135 ,  C07D295/192

Abstract: The present invention relates to carboxylic acid amides of general formula wherein R1 to R5, Ar, m and n are defined as in claim 1, the tautomers, stereoisomers, mixtures thereof, the prodrugs and the salts thereof which have valuable properties. The compounds of the above general formula I wherein R5 denotes a cyano group are valuable intermediate products for preparing the other compounds of general formula I, and the compounds of the above general formula I wherein R5 denotes one of the amidino groups mentioned in claim 1 have valuable pharmacological properties, particularly an antithrombotic activity and a factor Xa-inhibiting activity.

Abstract translation: 本发明涉及通式其中R 1至R 5，Ar，m和n如权利要求1所定义的羧酸酰胺，互变异构体，立体异构体，混合物 其前体药物及其盐具有有价值的性质。 其中R 5表示氰基的上述通式I的化合物是制备其它通式I化合物的有价值的中间产物，以及上述通式I的化合物，其中R 1， 5 表示权利要求1中提及的脒基之一具有有价值的药理学性质，特别是抗血栓形成活性和因子Xa抑制活性。

公开(公告)号：US07390923B2

公开(公告)日：2008-06-24

申请号：US10561231

申请日：2004-06-24

Applicant: Jari Ratilainen ,  Anu Moilanen ,  Olli Törmäkangas ,  Arja Karjalainen ,  Paavo Huhtala ,  Gerd Wohlfahrt ,  Pekka Kallio

Inventor： Jari Ratilainen ,  Anu Moilanen ,  Olli Törmäkangas ,  Arja Karjalainen ,  Paavo Huhtala ,  Gerd Wohlfahrt ,  Pekka Kallio

IPC: C07C233/05 ,  C07C231/00 ,  A61K31/16

CPC classification number: C07C235/24 ,  C07C237/04 ,  C07C255/54 ,  C07C255/58 ,  C07C275/34 ,  C07C311/08 ,  C07C323/20 ,  C07D213/64 ,  C07D213/65 ,  C07D213/68

Abstract: Compounds of formula (I) wherein R1 to R4, X and A are as defined in the claims and pharmaceutically acceptable salts and esters thereof, are disclosed. The compounds of formula (I) possess utility as tissue-selective androgen receptor modulators (SARM) and are useful in hormonal therapy, e.g., in the treatment or prevention of male hypogonadism and age-related conditions such as andropause.

Abstract translation: 公开了其中R 1至R 4，X和A如权利要求中所定义的式（I）化合物及其药学上可接受的盐和酯。 式（I）化合物具有作为组织选择性雄激素受体调节剂（SARM）的功效，并且可用于激素治疗，例如用于治疗或预防男性性腺机能减退和与年龄有关的疾病如肛裂。

公开(公告)号：US20070249838A1

公开(公告)日：2007-10-25

申请号：US11539940

申请日：2006-10-10

Applicant: Christopher Woltermann ,  Douglas Sutton

Inventor： Christopher Woltermann ,  Douglas Sutton

IPC: C07D211/86

CPC classification number: C07D213/68 ,  C07F7/0803

Abstract: Substituted alkylmetal reagents such as (trimethylsilylmethyl)lithium are reacted with pyridinic compounds to produce functionalized pyridinic compounds.

Abstract translation: 将取代的烷基金属试剂如（三甲基甲硅烷基甲基）锂与吡啶化合物反应以产生官能化的吡啶化合物。

公开(公告)号：US20070225365A1

公开(公告)日：2007-09-27

申请号：US11578694

申请日：2005-04-08

Applicant: Amjad Ali ,  Joann Bohn ,  Qiaolin Deng ,  Zhijian Lu ,  Peter Sinclair ,  Gayle Taylor ,  Christopher Thompson ,  Nazia Quraishi

Inventor： Amjad Ali ,  Joann Bohn ,  Qiaolin Deng ,  Zhijian Lu ,  Peter Sinclair ,  Gayle Taylor ,  Christopher Thompson ,  Nazia Quraishi

IPC: A61K31/216 ,  C07C69/612

CPC classification number: C07C271/20 ,  C07C233/18 ,  C07C271/16 ,  C07C271/22 ,  C07C279/08 ,  C07C311/04 ,  C07C311/08 ,  C07C317/32 ,  C07D209/08 ,  C07D213/40 ,  C07D213/64 ,  C07D213/65 ,  C07D213/68 ,  C07D213/89 ,  C07D215/12 ,  C07D215/26 ,  C07D217/02 ,  C07D217/14 ,  C07D261/08 ,  C07D271/06 ,  C07D307/52 ,  C07D307/79 ,  C07D333/20 ,  C07D333/22 ,  C07D333/28

Abstract: Compounds of Formula I, including pharmaceutically acceptable salts of the compounds, are CETP inhibitors, and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis. In the compounds of Formula 1, A1 and A2 are each an aromatic ring, a 5-6-membered heterocyclic ring, an aromatic ring fused to a heterocyclic ring, a phenyl ring fused to a heterocyclic ring, or a cycloalkyl ring.

Abstract translation: 式I化合物，包括化合物的药学上可接受的盐，是CETP抑制剂，可用于培养HDL-胆固醇，降低LDL-胆固醇，以及治疗或预防动脉粥样硬化。 在式1化合物中，A 1和A 2各自为芳环，5-6元杂环，稠合至杂环的芳环， 与杂环稠合的苯环或环烷基环。

公开(公告)号：US20070155733A1

公开(公告)日：2007-07-05

申请号：US11562675

申请日：2006-11-22

Applicant: Jonathan DIMMOCK ,  Umashankar DAS

Inventor： Jonathan DIMMOCK ,  Umashankar DAS

IPC: A61K31/541 ,  A61K31/5377 ,  A61K31/497 ,  A61K31/445 ,  C07D417/02 ,  C07D413/02 ,  C07D403/02 ,  C07D211/54

CPC classification number: C07D409/14 ,  C07D213/68

Abstract: The present invention relates to 4-piperidone derivatives represented by the following formula (I) and the acid addition salts thereof. The method of preparation and antineoplastic activity of the said compounds are disclosed. A number of the compounds possess submicromolar IC50 and CC50 values and have a selective toxicity for colon cancers and leukemic cells. In addition, many of the compounds are able to reverse multidrug resistance.

Abstract translation: 本发明涉及由下式（I）表示的4-哌啶酮衍生物及其酸加成盐。 公开了所述化合物的制备方法和抗肿瘤活性。 许多化合物具有亚微米IC 50和CC 50值，对结肠癌和白血病细胞具有选择性毒性。 此外，许多化合物能够逆转多药耐药性。

公开(公告)号：US20070149533A1

公开(公告)日：2007-06-28

申请号：US11636609

申请日：2006-12-07

Applicant: Emily Calderwood ,  Matthew Duffey ,  Alexandra Gould ,  Paul Greenspan ,  Bheemashankar Kulkarni ,  Matthew LaMarche ,  Robyn Rowland ,  Ming Tregay ,  Tricia Vos

Inventor： Emily Calderwood ,  Matthew Duffey ,  Alexandra Gould ,  Paul Greenspan ,  Bheemashankar Kulkarni ,  Matthew LaMarche ,  Robyn Rowland ,  Ming Tregay ,  Tricia Vos

IPC: A61K31/53 ,  A61K31/517 ,  A61K31/506 ,  A61K31/501 ,  A61K31/502 ,  A61K31/4709 ,  A61K31/497 ,  A61K31/427 ,  C07D417/14 ,  C07D413/14 ,  C07D405/14 ,  C07D403/14

CPC classification number: C07D401/04 ,  C07D213/68 ,  C07D213/73 ,  C07D213/75 ,  C07D213/78 ,  C07D213/81 ,  C07D401/12 ,  C07D401/14 ,  C07D405/12 ,  C07D405/14 ,  C07D413/04 ,  C07D413/12 ,  C07D413/14 ,  C07D471/04

Abstract: The present invention provides novel bicyclic compounds useful as inhibitors of protein kinases. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various diseases.

Abstract translation: 本发明提供了可用作蛋白激酶抑制剂的新型双环化合物。 本发明还提供包含本发明化合物的药物组合物和使用该组合物治疗各种疾病的方法。