公开(公告)号：US20250042908A1

公开(公告)日：2025-02-06

申请号：US18913624

申请日：2024-10-11

Applicant: GALDERMA HOLDING S.A.

Inventor： Craig Steven HARRIS ,  Loïc Jean-Marc Frédéric TOMAS

IPC: C07D487/04 ,  A61K31/519 ,  C07C55/08 ,  C07C59/245

Abstract: The present technology provides the crystalline phosphate, malonate, and malate salts of 3-(2-amino-1,3-benzoxazol-5-yl)-1-(1,3-dimethylbutyl)pyrazolo[3,4-d]pyrimidine-4,6-diamine. The present technology further provides methods for preparing the various forms, compositions containing them, and methods related to modulation of mTOR. In particular, the present crystalline compounds and compositions may be used to treat mTOR-mediated disorders and conditions, including, e.g., dermatological disorders related to a disorder of keratinization with a proliferative, inflammatory and/or immuno-allergic component.

公开(公告)号：US10421755B2

公开(公告)日：2019-09-24

申请号：US15712279

申请日：2017-09-22

Applicant: Novartis AG

Inventor： Wolfgang Marterer ,  Mahavir Prashad ,  Edwin Bernard Villhauer ,  Liladhar Murlidhar Waykole ,  James Anthony Vivelo ,  Bertrand Sutter ,  Jean-Claude Bianchi ,  Raeann Wu ,  Denis Har ,  Piotr H. Karpinski ,  Massimo Pignone ,  Doris Stingelin ,  Eckart Buerger

IPC: C07D453/02 ,  A61K9/20 ,  A61K31/194 ,  A61K31/439 ,  C07C55/08 ,  C07C55/10 ,  C07C57/145 ,  C07C57/15 ,  C07C51/41

Abstract: The present invention relates to salts of (R)-3-(6-(4-methylphenyl)-pyridin-3-yloxy)-1-aza-bicyclo[2.2.2]octane, to methods for making them or their precursors, to pharmaceutical compositions comprising them, and to their use as medicaments.

公开(公告)号：US10100032B2

公开(公告)日：2018-10-16

申请号：US15367808

申请日：2016-12-02

Applicant: AMPLIO PHARMA, LLC

Inventor： Scott L. Childs ,  Shreenivas R. Lingireddy ,  Nathan Barishansky

IPC: C07D401/04 ,  A61K31/4035 ,  C07C55/07 ,  C07C55/08 ,  C07C59/255 ,  C07C65/03 ,  C07C275/02 ,  C07C69/84

Abstract: The invention relates to novel crystalline forms of 3-(4-amino-l-oxo-l,3 dihydro-isoindol-2-yl)-piperidine-2,6-dione, including a novel urea cocrystal of 3-(4-amino-l-oxo-l,3 dihydro-isoindol-2-yl)-piperidine-2,6-dione; a novel gallic acid cocrystal of 3-(4-amino-l-oxo-1,3 dihydro-isoindol-2-yl)-piperidine-2,6-dione; a novel propyl gallate cocrystal of 3-(4-amino-l-oxo-1,3 dihydro-isoindol-2-yl)-piperidine-2,6-dione; and a novel L-tartaric acid cocrystal of 3-(4-amino-1-oxo-1,3 dihydro-isoindol-2-yl)-piperidine-2,6-dione. The preparation and characterization of the novel crystalline forms according to various embodiments of the invention are described. The invention also relates to pharmaceutical compositions containing the novel crystalline forms, and the therapeutic use of the novel crystalline forms.

公开(公告)号：US20180009801A1

公开(公告)日：2018-01-11

申请号：US15712279

申请日：2017-09-22

Applicant: Novartis AG

Inventor： Wolfgang Marterer ,  Mahavir Prashad ,  Edwin Bernard Villhauer ,  Liladhar Murlidhar Waykole ,  James Anthony Vivelo ,  Bertrand Sutter ,  Jean-Claude Bianchi ,  Raeann Wu ,  Denis Har ,  Piotr H. Karpinski ,  Massimo Pignone ,  Doris Stingelin ,  Eckart Buerger

IPC: C07D453/02 ,  A61K31/439 ,  C07C55/10 ,  C07C57/145 ,  C07C51/41 ,  A61K9/20 ,  C07C57/15 ,  A61K31/194 ,  C07C55/08

Abstract: The present invention relates to salts of (R)-3-(6-(4-methylphenyl)-pyridin-3-yloxy)-1-aza-bicyclo[2.2.2]octane, to methods for making them or their precursors, to pharmaceutical compositions comprising them, and to their use as medicaments.

公开(公告)号：US09670177B2

公开(公告)日：2017-06-06

申请号：US15011420

申请日：2016-01-29

Applicant: BIOMED VALLEY DISCOVERIES, INC.

Inventor： Gary DeCrescenzo ,  Dean Welsch ,  Jon G. Selbo ,  Ekaterina V. Albert ,  Emily M. Rigsbee

IPC: A61K31/4439 ,  C07D401/04 ,  C07C55/08 ,  A61K45/06

CPC classification number: C07D401/04 ,  A61K31/4439 ,  A61K45/06 ,  C07B2200/13 ,  C07C55/08

Abstract: The present invention provides a malonate salt of a compound of formula (I): which is a crystalline salt. Also provided are pharmaceutical compositions that include the provided malonate salt and methods of using the provided crystalline forms and pharmaceutical compositions for the treatment of cancer.

公开(公告)号：US20170114034A1

公开(公告)日：2017-04-27

申请号：US15115063

申请日：2015-01-30

Applicant: EGIS GYÓGYSZERGYÁR ZRT.

Inventor： Istvan LING ,  Gyorgy JEGES ,  Gyorgyi KOVANYINE LAX ,  Balazs VOLK ,  Peter GREGOR ,  Jeno Peter SERES ,  Andras DANCSO ,  Zoltan VARGA ,  Eva SZABO

IPC: C07D295/096 ,  C07C59/265 ,  C07C55/10 ,  C07C55/08 ,  C07C309/29 ,  C07C53/10 ,  C07C55/07 ,  C07C65/10

CPC classification number: C07D295/096 ,  C07B2200/13 ,  C07C53/10 ,  C07C55/07 ,  C07C55/08 ,  C07C55/10 ,  C07C59/265 ,  C07C65/10 ,  C07C309/29 ,  C07D295/08

Abstract: The invention relates to an improved process for the preparation of pharmaceutical active ingredients and also to high purity salts and pharmaceutical compositions prepared by said process. More particularly the invention relates to an economical process for the preparation of the compound having the international non-proprietary name (INN) vortioxetine and the chemical nomenclature 1-[2-(2,4-dimethyl-phenylsulfanyl)-phenyl]-piperazine. Vortioxetine corresponds to the following Formula Still more particularly the invention relates to the preparation of high purity vortioxetine L-(+)-mandelate salt of the Formula IX, the conversion of this salt into other highly pure salts and also to the formulation of said salts.

公开(公告)号：US20160244465A1

公开(公告)日：2016-08-25

申请号：US15045305

申请日：2016-02-17

Applicant: Eli Lilly and Company

Inventor： Simon James Richards ,  Erik James Hembre ,  Jose Eduardo Lopez ,  Leonard Larry Winneroski, Jr. ,  Timothy Andrew Woods ,  Jennifer Anne McMahon

IPC: C07D513/04 ,  C07C55/08 ,  C07C309/30

CPC classification number: C07D513/04 ,  A61K31/542 ,  A61P25/28 ,  C07C55/08 ,  C07C309/30

Abstract: The present invention provides a compound of Formula II: or a pharmaceutically acceptable salt thereof.

Abstract translation: 本发明提供式II的化合物或其药学上可接受的盐。

公开(公告)号：US20160230198A1

公开(公告)日：2016-08-11

申请号：US15019963

申请日：2016-02-09

Applicant: GeneSys Consulting, LLC

Inventor： Goutham N. Vemuri

IPC: C12P7/46 ,  C12N9/00 ,  C12N9/16 ,  C07C55/08

CPC classification number: C12P7/46 ,  C12N9/16 ,  C12N9/93 ,  C12Y301/02017 ,  C12Y602/01017

Abstract: Microorganisms and methods are provided for biological synthesis of methylmalonic acid and derivatives thereof. Engineered microorganisms such as bacteria, yeast, and fungi are configured to produce or overproduce methylmalonic acid and/or derivatives thereof. Methods involve the use of such engineered microorganisms to produce methylmalonic acid and/or derivatives thereof from carbon sources. Methods may include production in a fermenter and optional purification of the product.

Abstract translation: 微生物和方法用于生物合成甲基丙二酸及其衍生物。 诸如细菌，酵母和真菌的工程微生物被配置成产生或过度生产甲基丙二酸和/或其衍生物。 方法涉及使用这种工程化的微生物从碳源生产甲基丙二酸和/或其衍生物。 方法可以包括在发酵罐中的生产和产品的任选的纯化。

公开(公告)号：US09321747B2

公开(公告)日：2016-04-26

申请号：US14370634

申请日：2013-01-04

Applicant: DAIICHI SANKYO COMPANY, LIMITED ,  UBE INDUSTRIES, LTD.

Inventor： Yukinori Kawai ,  Noriaki Iwase ,  Osamu Kikuchi ,  Katsunori Takata ,  Takahiro Motoyama ,  Masahiko Hagihara

IPC: C07D401/14 ,  C07C55/24 ,  C07C55/08 ,  C07C309/04

CPC classification number: C07D401/14 ,  C07C55/08 ,  C07C55/24 ,  C07C309/04

Abstract: The present invention provides a salt of a substituted pyridine compound which has excellent CETP inhibition activity and is useful as a medicament. The present invention provides a salt of a compound represented by general formula (I): wherein R1 is optionally substituted alkoxy or the like.

Abstract translation: 本发明提供了具有优异的CETP抑制活性并可用作药物的取代的吡啶化合物的盐。 本发明提供由通式（I）表示的化合物的盐：其中R 1是任选取代的烷氧基等。

公开(公告)号：US09133142B2

公开(公告)日：2015-09-15

申请号：US13188689

申请日：2011-07-22

Applicant: Michael Gruss ,  Magda Kraszewski

Inventor： Michael Gruss ,  Magda Kraszewski

IPC: A61K31/137 ,  A61K31/455 ,  C07D213/80 ,  C07D275/06 ,  C07C55/02 ,  C07C55/08 ,  C07C55/20 ,  C07C57/15 ,  C07C63/08 ,  C07C63/36 ,  C07C65/11 ,  C07C215/54 ,  C07D239/545 ,  C07D291/06

CPC classification number: C07D275/06 ,  A61K31/137 ,  A61K31/455 ,  C07B2200/07 ,  C07C55/02 ,  C07C55/08 ,  C07C55/20 ,  C07C57/15 ,  C07C63/08 ,  C07C63/36 ,  C07C65/11 ,  C07C215/54 ,  C07D213/80 ,  C07D239/545 ,  C07D291/06

Abstract: A salt or cocrystal of 3-(3-dimethylamino-1-ethyl-2-methyl-propyl)-phenol (component a) and at least one acid component (b1) or at least one acid component (b2), wherein the salt or cocrystal of component (a) and component (b2) is present in crystalline and/or amorphous form, a pharmaceutical composition comprising said salt or cocrystal, and a method of treating pain in a subject in need thereof by administering an effective amount of said salt or cocrystal.

Abstract translation: 3-（3-二甲基氨基-1-乙基-2-甲基 - 丙基） - 苯酚（组分a）和至少一种酸组分（b1）或至少一种酸组分（b2）的盐或共结晶，其中盐 组分（a）和组分（b2）的共结晶以结晶和/或无定形的形式存在，包含所述盐或共结晶的药物组合物和通过施用有效量的所述有效量的所述有机溶剂治疗需要的受试者的疼痛的方法 盐或共晶。