序号 专利名 申请号 申请日 公开(公告)号 公开(公告)日 发明人
21 POLYUREA POLYMERS FROM SECONDARY POLYETHER POLYAMINES PCT/US2004020955 2004-06-30 WO2005007732A3 2005-03-31 POSEY MARK L; HILLMAN KENNETH M; WHEWELL CHRISTOPHER J
Provided herein are polyurea polymers made from an organic isocyanate and a polyamine component, wherein the polyamine component comprises a polyether polyamine in which the nitrogen atoms are secondary. The polyurea polymers of the invention are useful in a wide range of end-use applications and possess superior physical properties over polyurea polymers of the prior art. Methods for producing the polyurea polymers are also disclosed.
22 METHOD FOR TREATING BLOOD CANCERS PCT/US2022072091 2022-05-03 WO2022236270A1 2022-11-10 KULKARNI ADITYA; BHATIA KISHOR; ZHOU JIANLI
A method for treating a subject in need thereof having a bone or blood cancer, or a cancer that metastasizes to bone that includes administering to the subject an effective amount of hydroxyureamethyl acylfulvene.
23 PROCESS FOR PREPARING 1,2-BENZISOTHIAZOLINE-3-ONE PCT/EP2021000131 2021-10-25 WO2022089774A1 2022-05-05 BAUM RÜDIGER; BITTERMANN HOLGER; YANG ZHENGHAO; CHAOQIANG ZHANG; ZHANG CHANGHUA; ZHENG QINGLIN
The invention relates to a process for preparing 1,2'-benzisothiazoline-3-one according to formula (I), comprising the following steps: (a) reacting a 2-halogenbenzonitrile compound of general formula (II) with a reaction mixture, containing: (i) alkaline sulphide and/or alkaline hydrogen sulphide and (ii) an alkyl halide compound, represented by general formula (III): R1X (III) for producing an intermediate product of general formula (IV), and (b) reacting the intermediate product of general formula (V) obtained in step (a) with a halogenating agent or an oxidant and subsequent reaction of the 2-(alkylsulfoxy)benzonitrile with an acid to form 1,2-benzisothiazoline-3-one as well as a halide compound of general formula (V) R1X (V).
24 고분자 수지에 고정된 이온성 액체계 촉매 및 이를 이용한 N,N'-치환 우레아의 제조 방법 PCT/KR2015/013255 2015-12-04 WO2016093562A1 2016-06-16 김용진; 느윙뒤손; 소정은; 신승한; 조진구

본 발명은 고분자 수지 담지체에 화학적으로 고정화된 질소 함유 유기 양이온 및 그의 음이온을 포함하는 이온성 촉매 및 이 촉매 존재 하에서 아민 화합물과 이산화탄소를 반응시켜 N,N'-치환 우레아를 선택적으로 제조하는 방법에 관한 것이다. 본 발명에서 제조되는 치환 우레아들은 모두 카바메이트를 거쳐서 이소시아네이트로 쉽게 전환이 가능하고, 이소시아네이트는 폴리올과의 반응을 통해 폴리우레탄으로 전환될 수 있는 중요한 전구체 화합물로 사용될 수 있다. 한편, 본 발명에서의 고분자 수지 담지체에 고정된 이온성 액체계 촉매는 여러 번의 재사용이 가능하므로 경제적이라는 추가적인 장점이 있다.

25 (메트)아크릴레이트 화합물, 이로부터 유도된 반복단위를 포함하는 코폴리머 및 호모폴리머 PCT/KR2015/010210 2015-09-25 WO2016052953A1 2016-04-07 박광승; 이미린; 박준욱; 허은수; 전성현

본 명세서는 (메트)아크릴레이트 화합물, 이로부터 유도된 반복단위를 포함하는 코폴리머 및 호모폴리머에 관한 것이다.

26 HISTONE DEACETYLASE INHIBITORS PCT/US2005/024514 2005-07-08 WO2006017216A1 2006-02-16 BELVEDERE, Sandro; HAMBLETT, Christopher Laurence; MILLER, Thomas, A.; WITTER, David, J.; YAN, Jiaming

This invention relates to hydroxamic acid derivatives having a urea linkage, that are inhibitors of histone deacetylase (HDAC), and are useful in the prevention and/or treatment of cellular proliferative diseases, for example cancer, autoimmune, allergic and inflammatory diseases, diseases of the central nervous system (CNS) such as neurodegenerative diseases, and in the prevention and/or treatment of restenosis.

27 MODULATORS OF CERAMIDASE AND METHODS OF USE BASED THEREON PCT/US2002/022151 2002-07-11 WO2003005965A3 2003-01-23 BIELAWSKA, Alicja; HANNUN, Yusuf, A.; SZULC, Zdzislaw; USTA, Julnar; EL BAWAB, Samer

The present invention relates to compounds which can be used as inhibitors of mitochondrial ceramidase, in particular human mitochondrial ceramidase. The invention also relates to methods of designing and making the compounds, as well as methods screening for compounds that inhibit mitochondrial ceramidase. The invention also relates to the use of the compounds as a regulator of the level of ceramide by inhibiting ceramidase activity. The invention also relates to methods for the prevention and treatment of diseases associated with cell overproliferation and sphingolipid signal transduction including cancer, cardiovascular diseases, and inflammation.

28 BENZENE RING-CONTAINING COMPOUND HAVING ANALGESIC EFFECT, PREPARATION METHOD THEREFOR, AND USE THEREOF PCT/CN2024121886 2024-09-27 WO2025067473A1 2025-04-03 ZHANG WENSHENG; DENG CHAOYI; LUO XUDONG; DENG YU; LIU JIN; LI CHENYANG; LU JUNYU; ZHU TAO; LUO FENGMING
A benzene ring-containing compound having an analgesic effect, a preparation method therefor, and the use thereof, which relate to the field of pharmaceutical chemistry. The compound is a compound represented by formula I, or a stereoisomer thereof, or a pharmaceutically acceptable salt thereof, or a solvate thereof, or a crystal form thereof, or a prodrug thereof, or a metabolite thereof, or a deuterated derivative thereof. The compound has a uniquely advantageous analgesic effect, is highly safe when used, has only mild toxic side effects, and no dependence develops during use. Therefore, the compound has wide application prospects in the preparation of analgesic pharmaceuticals, and provides a new option when clinically preparing a drug with an analgesic effect.
29 PROCESS FOR PREPARING 1,2-BENZISOTHIAZOLINE-3-ONE PCT/EP2021000131 2021-10-25 WO2022089774A8 2023-04-06 BAUM RÜDIGER; BITTERMANN HOLGER; YANG ZHENGHAO; ZHANG CHAOQIANG; ZHANG CHANGHUA; ZHENG QINGLIN
The invention relates to a process for preparing 1,2'-benzisothiazoline-3-one according to formula (I), comprising the following steps: (a) reacting a 2-halogenbenzonitrile compound of general formula (II) with a reaction mixture, containing: (i) alkaline sulphide and/or alkaline hydrogen sulphide and (ii) an alkyl halide compound, represented by general formula (III): R1X (III) for producing an intermediate product of general formula (IV), and (b) reacting the intermediate product of general formula (V) obtained in step (a) with a halogenating agent or an oxidant and subsequent reaction of the 2-(alkylsulfoxy)benzonitrile with an acid to form 1,2-benzisothiazoline-3-one as well as a halide compound of general formula (V) R1X (V).
30 COMPOSITIONS AND METHODS FOR TREATING ALZHEIMER'S DISEASE AND PARKINSON'S DISEASE PCT/US2017/054473 2017-09-29 WO2018064559A1 2018-04-05 SALENTINE, Christopher G.; MALEFYT, Thomas R.

The present invention is directed to tablets for oral administration to a subject, comprising a therapeutically effective amount of SYN120 or a pharmaceutically acceptable salt thereof, wherein the tablet is substantially free of lactose. The present invention is also directed to methods for treating diseases or conditions including Alzheimer's disease and/or Parkinson's disease, comprising administering to a patient in need thereof tablets regarding the same.

31 AGONISTS OR PARTIAL AGONISTS OF THE HISTAMINE SITE OF THE NMDA RECEPTOR FOR USE IN THE TREATMENT OF CENTRAL NERVOUS SYSTEM DISEASES PCT/EP2017/070637 2017-08-14 WO2018033525A1 2018-02-22 ARMAND, Vincent; BURBAN-PREVOST, Aude; FAUCARD, Raphaël; ARRANG, Jean-Michel

This invention relates to compounds that are agonists or partial agonists of the histamine site of the NMDA receptor, the method of preparation thereof and applications thereof.

32 (HYDROXYETHYL)UREAS AS INHIBITORS OF ALZHEIMER'S BETA-AMYLOID PRODUCTION PCT/US0125267 2001-08-10 WO0214264A3 2002-05-30 WOLFE MICHAEL S; SELKOE DENNIS J
Novel (hydroxyethyl)ureas are described. These compounds are effective inhibitors of certain aspartyl proteases, notably secretases involved in the enzymatic cleavage of amyloid precursor protein (APP) to yield amyloid- beta peptide. Methods are provided for administering the novel compunds to treat beta -amyloid-associated diseases, notably Alzheimer's disease.
33 (HYDROXYETHYL)UREAS AS INHIBITORS OF ALZHEIMER'S BETA-AMYLOID PRODUCTION PCT/US2001/025267 2001-08-10 WO02014264A2 2002-02-21
Novel (hydroxyethyl)ureas are described. These compounds are effective inhibitors of certain aspartyl proteases, notably secretases involved in the enzymatic cleavage of amyloid precursor protein (APP) to yield amyloid- beta peptide. Methods are provided for administering the novel compunds to treat beta -amyloid-associated diseases, notably Alzheimer's disease.
34 Cancer Cell Targeting Using Nanoparticles EP13162789.5 2008-03-31 EP2644594A1 2013-10-02 Zale, Stephen E.; Ali, Mir Mukkaram

The present invention generally relates to polymers and macromolecules, in particular, to polymers useful in particles such as nanoparticles. One aspect of the invention is directed to a method of developing nanoparticles with desired properties. In one set of embodiments, the method includes producing libraries of nanoparticles having highly controlled properties, which can be formed by mixing together two or more macromolecules in different ratios. One or more of the macromolecules may be a polymeric conjugate of a moiety to a biocompatible polymer. In some cases, the nanoparticle may contain a drug. Other aspects of the invention are directed to methods using nanoparticle libraries.

35 Functional monomers for molecular recognition and catalysis EP09151310.1 2001-01-25 EP2065365A3 2009-06-24 Sellergren, Börje; Hall, Andrew; Chenon, Karine; Karmalkar, Rohini

The present invention refers to new classes of polymerisable monomers, to molecularly imprinted polymers obtainable by polymerisation of at least one of the monomers and a crosslinking monomer in the presence of a template molecule. The obtained polymers may be used for separation of enantiomers, diastereomers of the template molecule, and also for separation of the template molecule or template molecule analogues from structurally related compounds.

36 Carbodiimide und Verfahren zu deren Herstellung EP99104113.8 1999-03-02 EP0940389A2 1999-09-08 Kokel, Nicolas Dr.; Häberle, Karl Dr.; Kraus, Rupert Dr.

Bei einer Temperatur von 25°C feste Carbodiimide enthaltend Carbodiimidstrukturen sowie Urethan- und/oder Harnstoffstrukturen, wobei die Carbodiimidstrukturen an nicht-aromatische Kohlenwasserstoffatome gebunden sind.

37 Substituted benzylurea derivatives and medicine containing the same EP97118069.0 1997-10-17 EP0839803A1 1998-05-06 Kanamaru, Yoshihiko; Hirota, Hiroyuki; Shibata, Akihiro; Komoto, Teruo; Naito, Hiroyuki; Tachibana, Koichi; Ohtsuka, Mari; Ishii, Fumio; Sato, Susumu

Disclosed herein are substituted benzylurea derivatives represented by the following general formula (1): wherein R1 and R2 are independently H, a halogen atom, or an alkyl or alkoxyl group, R3 is a phenyl or heterocyclic group which may be substituted, n is an integer of 1-6, and R4 is a phenyl group which may be substituted, or salts thereof, and medicines comprising such a derivative as an active ingredient. The derivatives or salts thereof strongly inhibit only ACAT in macrophages and are hence useful as prophylactic and therapeutic agents for arteriosclerosis.

38 Verfahren zur Herstellung von blockierten harnstoffgruppenhaltigen Polyisocyanaten sowie die danach hergestellten Produkte EP88115942.0 1988-09-28 EP0321658B1 1993-06-16 Gras, Rainer, Dr.
39 Urées substituées, leur procédé de préparation et leur application notamment dans l'ennoblissement des fibres cellulosiques EP88400686.7 1988-03-22 EP0285500B1 1992-01-02 Wilhelm, Didier; Gelabert, Antonio; Blanc, Alain
40 Verfahren zur Herstellung von blockierten harnstoffgruppenhaltigen Polyisocyanaten sowie die danach hergestellten Produkte EP88115942.0 1988-09-28 EP0321658A1 1989-06-28 Gras, Rainer, Dr.

Eine direkte Umsetzung von Polyisocyanaten und Polyaminen erfolgt heftig und nicht kontrollierbar. Deshalb ist es notwendig, das Po­lyisocyanat in blockierter Form einzusetzen. Bei bisher bekannten Verfahren war es nicht möglich, die gewünschten halbblockierten Addukte zu erhalten, man erhielt größere Anteile vollständig blok­kiertes Produkt neben nicht umgesetztem Polyisocyanat. Die weitere Umsetzung mit Polyaminen war erfolglos.

Die Herstellung von blockierten, harnstoffhaltigen Polyisocyanaten wurde durch den Einsatz halbblockierter Polyisocyanate möglich, die sich durch Zugabe von Blockierungsmittel zu mehrfach über­schüssigem Polyisocyanat bilden, gefolgt von einer Dünnschichtde­stillation und anschließendem Umsatz mit Polyaminen im NCO/Amino­gruppen-Verhältnis von 1 bis 1,3:1 bis 1:1.

Die blockierten, harnstoffhaltigen Polyisocyanate werden insbeson­dere für PUR-Lacke eingesetzt.

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