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![Salt forms of 1-[(4-methyl-quinazolin-2-yl)methyl]-3-methyl-7-(2-butyn-1-yl)-8-(3-(R)-amino-piperidin-1-yl)-xanthine](/abs-image/US/2015/12/15/US09212183B2/abs.jpg.150x150.jpg)
1.发明授权Salt forms of 1-[(4-methyl-quinazolin-2-yl)methyl]-3-methyl-7-(2-butyn-1-yl)-8-(3-(R)-amino-piperidin-1-yl)-xanthine 有权1 - [（4-甲基 - 喹唑啉-2-基）甲基] -3-甲基-7-（2-丁炔-1-基）-8-（3-（R） - 氨基 - 哌啶-1-基 - 基） - 黄嘌呤公开(公告)号：US09212183B2
公开(公告)日：2015-12-15
申请号：US14273753
申请日：2014-05-09
Applicant: Peter Sieger , Waldemar Pfrengle
Inventor： Peter Sieger , Waldemar Pfrengle
IPC: A01N43/90 , A61K31/52 , C07D473/00 , C07D473/04 , A61K31/185 , A61K31/19 , A61K31/192 , A61K31/194 , A61K31/522 , C07C59/06 , C07C59/235 , C07C63/08 , C07C65/05 , C07C65/10 , C07C309/04 , C07C309/29
CPC classification number: C07D473/04 , A61K31/185 , A61K31/19 , A61K31/192 , A61K31/194 , A61K31/522 , C07C59/06 , C07C59/235 , C07C63/08 , C07C65/05 , C07C65/10 , C07C309/04 , C07C309/29
Abstract: The present invention relates to novel salt forms of 1-[(4-methyl-quinazolin-2-yl)methyl]-3-methyl-7-(2-butyn-1-yl)-8-(3-(R)-amino-piperidin-1-yl)-xanthine, processes for making these novel salts, and pharmaceutical compositions comprising such novel salts. The invention also relates to the use of these novel salts in the treatment of type 2 diabetes.
Abstract translation: 本发明涉及1 - [（4-甲基 - 喹唑啉-2-基）甲基] -3-甲基-7-（2-丁炔-1-基）-8-（3-（R） - 氨基 - 哌啶-1-基） - 黄嘌呤，制备这些新型盐的方法，以及包含这些新型盐的药物组合物。 本发明还涉及这些新型盐在治疗2型糖尿病中的用途。
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2.发明申请SUBSTITUTED QUINAZOLINES, THE PREPARATION THEREOF AND THE USE THEREOF IN PHARMACEUTICAL COMPOSITIONS 有权取代喹诺酮类药物的制备及其在药物组合物中的应用公开(公告)号：US20140228283A1
公开(公告)日：2014-08-14
申请号：US14232418
申请日：2012-07-13
Applicant: Waldemar Pfrengle , Markus Frank , Thomas Klein
Inventor： Waldemar Pfrengle , Markus Frank , Thomas Klein
IPC: C07D473/06 , A61K45/06 , A61K31/522
CPC classification number: C07D473/06 , A61K31/155 , A61K31/4439 , A61K31/522 , A61K45/06 , C07D473/04
Abstract: The present invention relates to substituted quinazolines of formula (I) wherein X and Y are defined as in claim 1, the tautomers, stereoisomers, mixtures and salts thereof, which have valuable pharmacological properties, particularly an inhibitory effect on the activity of the enzyme dipeptidylpeptidase-W (DPP-IV).
Abstract translation: 本发明涉及式（I）的取代喹唑啉，其中X和Y如权利要求1所定义，其互变异构体，立体异构体，混合物和盐具有有价值的药理学性质，特别是对酶二肽基肽酶的活性的抑制作用 -W（DPP-IV）。
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公开(公告)号：US08101763B2
公开(公告)日：2012-01-24
申请号：US12601571
申请日：2008-05-09
Applicant: Waldemar Pfrengle , Werner Rall , Joerg Brandenburg , Rolf Herter
Inventor： Waldemar Pfrengle , Werner Rall , Joerg Brandenburg , Rolf Herter
IPC: C07D451/10 , C07D265/36
CPC classification number: C07D451/10
Abstract: The invention relates to a novel method for producing scopine esters of the general formula (1), wherein X—, R, R1, R2, R3, R4, R3′, R4′, R6 and R6′ can have the meanings indicated in the claims and in the description.
Abstract translation: 本发明涉及一种制备通式（1）的扇叶酯的新方法，其中X，R，R 1，R 2，R 3，R 4，R 3'，R 4'，R 6和R 6'可以具有 声明和说明书。
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公开(公告)号：US20100174067A1
公开(公告)日：2010-07-08
申请号：US12601571
申请日：2008-05-09
Applicant: Waldemar Pfrengle , Werner Rall , Joerg Brandenburg , Rolf Herter
Inventor： Waldemar Pfrengle , Werner Rall , Joerg Brandenburg , Rolf Herter
IPC: C07D265/36
CPC classification number: C07D451/10
Abstract: The invention relates to a novel method for producing scopine esters of the general formula (1), wherein X—, R, R1, R2, R3, R4, R3′, R4′, R6 and R6′ can have the meanings indicated in the claims and in the description.
Abstract translation: 本发明涉及一种制备通式（1）的扇叶酯的新方法，其中X，R，R 1，R 2，R 3，R 4，R 3'，R 4'，R 6和R 6'可以具有 声明和说明书。
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5.发明申请PROCESS FOR THE PREPARATION OF CHIRAL 8-(3-AMINOPIPERIDIN-1YL)-XANTHINES 有权制备8-（3-氨基哌啶-1-基） - 辛糖的方法公开(公告)号：US20090192314A1
公开(公告)日：2009-07-30
申请号：US12413851
申请日：2009-03-30
Applicant: Waldemar PFRENGLE , Thorsten PACHUR , Thomas NICOLA , Adil DURAN
Inventor： Waldemar PFRENGLE , Thorsten PACHUR , Thomas NICOLA , Adil DURAN
IPC: C07D401/04
CPC classification number: C07D401/04 , C07B2200/07 , C07D473/04 , C07D473/06
Abstract: The invention relates to an improved process for preparing enantiomerically pure 8-(3-aminopiperidin-1-yl)-xanthines.
Abstract translation: 本发明涉及制备对映体纯的8-（3-氨基哌啶-1-基） - 黄嘌呤的改进方法。
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Patent Agency Ranking
公开(公告)号：US07084146B2
公开(公告)日：2006-08-01
申请号：US09840488
申请日：2001-04-23
Applicant: Klaus-Juergen Pees , Guenter Krummel , Henry Van Tuyl Cotter , Guido Albert , Annerose Rehnig , Leslie May , Waldemar Pfrengle
Inventor： Klaus-Juergen Pees , Guenter Krummel , Henry Van Tuyl Cotter , Guido Albert , Annerose Rehnig , Leslie May , Waldemar Pfrengle
IPC: C07D487/04 , A01N43/90
CPC classification number: C07D487/04 , A01N43/90
Abstract: The novel compounds of formula I: wherein R1 is hydrogen or methyl; R2 is hydrogen, or an optionally substituted alkyl, alkenyl, alkynyl, alkadienyl or phenyl group; Hal is halogen; and L1 through L5 are each hydrogen, halogen, alkyl, alkoxy or nitro, provided that at least one of L1 through L5 represents nitro or alkoxy; show selective fungicidal activity. The new compounds are processed with carriers and adjuvants to fungicidal compositions.
Abstract translation: 式I的新化合物：其中R 1是氢或甲基; R 2是氢或任选取代的烷基，烯基，炔基，链二烯基或苯基; 卤素是卤素; 和L 1至L 5各自为氢，卤素，烷基，烷氧基或硝基，条件是L 1至L 2中的至少一个， SUP> 5表示硝基或烷氧基; 显示选择性杀真菌活性。 新的化合物用载体和佐剂加工成杀真菌剂。
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公开(公告)号：US06284762B1
公开(公告)日：2001-09-04
申请号：US09272917
申请日：1999-03-19
Applicant: Waldemar Pfrengle
Inventor： Waldemar Pfrengle
IPC: A01N4390
CPC classification number: C07D487/04 , A01N43/90
Abstract: The novel compounds of formula I: (R1, R2, R3, L1, L2 and Hal are defined in the specification) show selective fungicidal activity. These compounds may be processed with carriers, and optionally an adjuvant, to produce fungicidal compositions.
Abstract translation: 式I的新化合物：（R1，R2，R3，L1，L2和Hal在说明书中定义）显示选择性杀真菌活性。 这些化合物可以用载体和任选的佐剂加工，以产生杀真菌组合物。
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8.发明授权Substituted quinazolines, the preparation thereof and the use thereof in pharmaceutical compositions 有权取代喹唑啉，其制备方法及其在药物组合物中的用途公开(公告)号：US08962636B2
公开(公告)日：2015-02-24
申请号：US14232418
申请日：2012-07-13
Applicant: Waldemar Pfrengle , Markus Frank , Thomas Klein
Inventor： Waldemar Pfrengle , Markus Frank , Thomas Klein
IPC: A61K31/522 , A61K45/06 , C07D473/06 , A61K31/155 , A61K31/4439 , C07D473/04
CPC classification number: C07D473/06 , A61K31/155 , A61K31/4439 , A61K31/522 , A61K45/06 , C07D473/04
Abstract: The present invention relates to substituted quinazolines of formula (I) wherein X and Y are defined as in claim 1, the tautomers, stereoisomers, mixtures and salts thereof, which have valuable pharmacological properties, particularly an inhibitory effect on the activity of the enzyme dipeptidylpeptidase-IV(DPP-IV).
Abstract translation: 本发明涉及式（I）的取代喹唑啉，其中X和Y如权利要求1所定义，其互变异构体，立体异构体，混合物和盐具有有价值的药理学性质，特别是对酶二肽基肽酶的活性的抑制作用 -IV（DPP-IV）。
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![9-[4-(3-chloro-2-fluoro-phenylamino-7-methoxy-quinazoline-6-yloxy]-1,4-diaza-spiro[5.5]undecane-5-one dimaleate, use thereof as a medicament and method for the production thereof](/abs-image/US/2014/12/09/US08906931B1/abs.jpg.150x150.jpg)
9.发明授权9-[4-(3-chloro-2-fluoro-phenylamino-7-methoxy-quinazoline-6-yloxy]-1,4-diaza-spiro[5.5]undecane-5-one dimaleate, use thereof as a medicament and method for the production thereof 有权9- [4-（3-氯-2-氟 - 苯基氨基-7-甲氧基 - 喹唑啉-6-基氧基）-1,4-二氮杂 - 螺[5.5]十一烷-5-酮二马来酸二乙酯，其作为药物的用途和 制备方法公开(公告)号：US08906931B1
公开(公告)日：2014-12-09
申请号：US14471147
申请日：2014-08-28
Applicant: Waldemar Pfrengle , Guenther Huchler , Markus Ostermeier , Peter Sieger
Inventor： Waldemar Pfrengle , Guenther Huchler , Markus Ostermeier , Peter Sieger
IPC: C07D401/00 , A01N43/54 , A61K31/517
CPC classification number: C07D241/38 , C07D239/70 , C07D403/12
Abstract: The present invention relates to a compound of formula (I), which has valuable pharmacological properties, particularly an inhibiting effect on signal transduction mediated by tyrosine kinases, processes for stereoselectively preparing these compounds, particularly pharmaceutical formulations suitable for inhalation and their use for the treatment of diseases, particularly tumoral diseases, benign prostatic hyperplasia and diseases of the lungs and airways.
Abstract translation: 本发明涉及式（I）化合物，其具有有价值的药理学性质，特别是对由酪氨酸激酶介导的信号转导的抑制作用，立体选择性制备这些化合物的方法，特别是适用于吸入的药物制剂及其用于治疗 的疾病，特别是肿瘤疾病，良性前列腺增生和肺和气道疾病。
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10.发明授权Process for the preparation of chiral 8-(3-aminopiperidin-1-yl)-xanthines 有权手性8-（3-氨基哌啶-1-基） - 黄嘌呤的制备方法公开(公告)号：US08883805B2
公开(公告)日：2014-11-11
申请号：US13782149
申请日：2013-03-01
Applicant: Waldemar Pfrengle , Thorsten Pachur , Thomas Nicola , Adil Duran
Inventor： Waldemar Pfrengle , Thorsten Pachur , Thomas Nicola , Adil Duran
IPC: C07D473/04 , C07D473/06
CPC classification number: C07D401/04 , C07B2200/07 , C07D473/04 , C07D473/06
Abstract: The invention relates to an improved process for preparing enantiomerically pure 8-(3-aminopiperidin-1-yl)-xanthines.
Abstract translation: 本发明涉及制备对映体纯的8-（3-氨基哌啶-1-基） - 黄嘌呤的改进方法。
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