INHIBITORS OF THE INFLUENZA A VIRUS M2 PROTON CHANNEL

Provided are compounds that are capable of modulating the activity of the influenza A virus via interaction with the M2 transmembrane protein. Also provided are methods for treating an influenza A-affected disease state or infection comprising administering a composition comprising one or more compounds that have been identified as being capable of interaction with the M2 protein. 2. The compound according to wherein X and Y are each independently methylene or ethylene.3. The compound according to wherein X is methylene and Y is ethylene.4. The compound according to wherein at least one of Rand Ris hydrogen.5. The compound according to wherein one of Rand Ris carbonyl claim 4 , amino claim 4 , carboxyl claim 4 , cyano claim 4 , or —CH(R)(R).6. The compound according to wherein n is 1 or 2 claim 5 , except that if n is 1 claim 5 , both X and Y are methylene claim 5 , and both Rand Rare hydrogen claim 5 , then one of Rand Ris not carbonyl.7. The compound according to wherein one of Rand Ris —CH(R)(R).8. The compound according to wherein one of Rand Ris amino10. A composition comprising a compound according to and a pharmaceutically acceptable carrier claim 1 , diluent claim 1 , or excipient. This application is a divisional of U.S. Ser. No. 12/848,197, filed Aug. 1, 2010 (now allowed), the entire contents of which are hereby incorporated herein by reference.The present invention pertains to, among other things, compounds and methods for modulating the activity of the influenza virus.The M2 protein is found in the viral envelope of influenza A virus and functions as a highly selective, pH-regulated proton channel important for the life cycle of the virus. Unlike neuraminidase inhibitors, rimantadine and amantadine are anti-viral agents capable of blocking the tetrameric M2 channel. In 2006, the CDC issued an alert instructing clinicians to avoid using M2 ion-channel inhibitors during influenza season due to the extraordinarily high frequency of amantadine resistance in ...

Isomer-enriched 3-caranlactams and polyamides based thereon with high optical purity and adjustable crystallinity for high-performance applications

The present invention relates to a process for the preparation of an isomer-enriched mixture of 3S- and 3R-caranone from 3-carane epoxide, a 3S-caranone obtained therefrom, a process for the production of 3S-caranlactam from 3-carene, a process for the production of 3R-caranlactam from 3-carene, a 3S-caranoxime, a 3S-caranlactam, a 3S-polycaranamide, a 3R-polycaranamide, a 3S/3R-co-polycaranamide, a 3S-caranlactam-laurolactam co-polycaranamide, a 3R-caranlactam-laurolactam co-polycaranamide, a 3S-caranlactam-3R-caranlactam-laurolactam co-polycaranamide, a 3S-caranlactam-caprolactam co-polycaranamide, a 3R-caranlactam-caprolactam co-polycaranamide, as well as a 3S/3R-caranlactam-caprolactam co-polycaranamide.

7-MEMBERED FUSED HETEROCYCLES AND METHODS OF THEIR SYNTHESIS

Disclosed are a new method for synthesizing 7-membered fused heterocycles and compounds synthesized by the new method. The method involves a dual activation strategy using an N-heterocyclic carbene catalyst as a first Lewis base and another second Lewis base. Compounds synthesized by the disclosed method may include new benzoxopinone compounds, as well as benzoxepane compounds and benzoazepinone compounds that optionally may be derived from the disclosed benzoxopinone compounds. 4. The compound of claim 1 , wherein Ris an aromatic system selected from a group consisting of phenyl claim 1 , naphthyl claim 1 , and pyridinyl claim 1 , which optionally is substituted with C-Calkyl claim 1 , halo claim 1 , or C-Calkoxy.6. The compound of claim 1 , wherein Ris H or an electron-donating group selected from a group consisting of C-Calkyl and C-Calkoxy.10. The compound of claim 7 , wherein Ris an aromatic system selected from a group consisting of phenyl claim 7 , naphthyl claim 7 , and pyridinyl claim 7 , which optionally is substituted with C-Calkyl claim 7 , halo claim 7 , or C-Calkoxy.12. The compound of claim 7 , wherein Ris H or an electron-donating group selected from a group consisting of C-Calkyl and C-Calkoxy.17. The compound of claim 13 , wherein Ris H or an electron-donating group selected from a group consisting of C-Calkyl and C-Calkoxy.20. The method of claim 18 , wherein LG is Br claim 18 , Cl claim 18 , or a sulfonate ester. The present application claims the benefit of priority under 35 U.S.C. §119(e) to U.S. Provisional Patent Application No. 61/870,966, filed on Aug. 28, 2013, the content of which is incorporated herein by reference in its entirety.This invention was made with government support under grant number R01 GM073072 awarded by the National Institutes of Health. The government has certain rights in the invention.The field of the invention relates to 7-membered fused heterocycles and their methods of synthesis. In particular, the field of the ...

LAPPACONITINE DERIVATIVE WITH ANALGESIC ACTIVITY, AND PREPARATION AND APPLICATION THEREOF

Provided herein are a lappaconitine derivative of formula (I), and a preparation and application thereof. 7. An analgesic composition , comprising:{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'the compound of , or a stereoisomer, a deuterated compound, a solvate, a prodrug, a metabolite or a pharmaceutically acceptable salt thereof, and'}a pharmaceutically acceptable excipient.8. A method for relieving pain in a subject in need thereof , comprising:{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'administering to the subject a pharmaceutically effective amount of the compound of , or a stereoisomer, a deuterated compound, a solvate, a prodrug, a metabolite or a pharmaceutically acceptable salt thereof.'}9. The method of claim 8 , wherein a median lethal dose of the compound is higher than a median lethal dose of lappaconitine. This application claims the benefit of priority from Chinese Patent Application No. 202110419203.4, filed on Apr. 19, 2021. The content of the aforementioned application, including any intervening amendments thereto, is incorporated herein by reference in its entirety.This application relates to pharmaceutical preparation, and more particularly to a lappaconitine derivative with analgesic activity, and a preparation and application thereof.Lappaconitine (LA) is a C18-diterpenoid alkaloid naturally occurring in the root of Nakai of the Ranunculaceae family, and is usually prepared into lappaconitine hydrobromide for clinical application. It has been reported that lappaconitine has analgesia, anti-inflammatory, apocatastasis and antipyretic effects.Lappaconitine is particularly prominent in relieving inflammatory pain due to the excellent anti-inflammatory activity, and has been clinically used in the treatment of pain caused by rheumatoid arthritis. Yue Jianhua (Yue J. The analysis of treatment effect on urethra syndrome by lappaconitini hydrobromidum and amitriptylinum [J]1996, 17(2):1. DOI: CNKI:SUN:QHYX.0.1996-02-023) as reported that ...

BENZAZEPINES AS SEROTONIN 5-HT2C RECEPTOR LIGANDS AND USES THEREOF

The present invention generally relates to a series of compounds, to pharmaceutical compositions containing the compounds, and to use of the compounds and compositions as therapeutic agents. More specifically, compounds of the present invention are benzazepine compounds. These compounds are serotonin receptor (5-HT) ligands and are useful for treating diseases, disorders, and conditions wherein modulation of the activity of serotonin receptors (5-HT) is desired (e.g. addiction, anxiety, depression, obesity, and others). 2. A compound as in claim 1 , wherein Ris H.8. A compound according to claim 1 , wherein R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , Rare H; and Rand Rtogether with the atoms which they are attached form a 5-membered carbocycle ring claim 1 , substituted with one or more of each of R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , and R.9. A compound according to claim 8 , wherein Rand Rare both H.10. A compound according to claim 8 , wherein Rand Rare both F.11. A compound according to claim 8 , wherein Ris aryl and Ris H.12. A compound according to claim 1 , wherein said compound is selected from the group consisting of:1,2,3,6,7,8,9,10-octahydro-8-aza-cyclohepta[e]indene;1-Methyl-1,2,3,6,7,8,9,10-octahydro-8-aza-cyclohepta[e]indene;1-Ethyl-1,2,3,6,7,8,9,10-octahydro-8-aza-cyclohepta[e]indene;1-Cyclopropyl-1,2,3,6,7,8,9,10-octahydro-8-aza-cyclohepta[e]indene;1-Propyl-1,2,3,6,7,8,9,10-octahydro-8-aza-cyclohepta[e]indene;4-Chloro-1-ethyl-1,2,3,6,7,8,9,10-octahydro-8-aza-cyclohepta[e]indene;1-Ethyl-4-iodo-1,2,3,6,7,8,9,10-octahydro-8-aza-cyclohepta[e]indene;1-Ethyl-4-fluoro-1,2,3,6,7,8,9,10-octahydro-8-aza-cyclohepta[e]indene;1-Phenyl-1,2,3,6,7,8,9,10-octahydro-8-aza-cyclohepta[e]indene;4-Chloro-1-phenyl-1,2,3,6,7,8,9,10-octahydro-8-aza-cyclohepta[e]indene;1-Pyridin-3-yl-1,2,3,6,7,8,9,10-octahydro-8-aza-cyclohepta[e]indene;4-Fluoro-1-pyridin-3-yl-1,2,3,6,7,8,9,10-octahydro-8-aza-cyclohepta[e]indene;1,1-Dimethyl-1, ...

ELECTROLUMINESCENT MATERIAL AND DEVICE

Disclosed are an electroluminescent material and device. The compound is a compound formed by connecting an indole- and pyrrole-fused azamacrocycle to triazine or a similar structure thereof at a specific position and is used as the host material of the electroluminescent device. These novel compounds have significantly reduced evaporation temperature and better thermal stability, can effectively reduce energy consumption, which more facilitates the device manufacturing process, and in addition, can also effectively improve device efficiency and reduce device drive voltage, which can provide better device performance. Further disclosed are an electroluminescent device, a compound formulation, and a display assembly. 2. The compound according to claim 1 , wherein the ring A claim 1 , the ring B claim 1 , and the ring C are claim 1 , at each occurrence identically or differently claim 1 , selected from a five-membered carbocyclic ring claim 1 , an aromatic ring having 6 to 18 carbon atoms claim 1 , or a heteroaromatic ring having 3 to 18 carbon atoms;preferably, the ring A, the ring B, and the ring C are, at each occurrence identically or differently, selected from a five-membered carbocyclic ring, a benzene ring, a five-membered heteroaromatic ring, or a six-membered heteroaromatic ring.4. The compound according to claim 3 , wherein R and Rare claim 3 , at each occurrence identically or differently claim 3 , selected from the group consisting of: hydrogen claim 3 , deuterium claim 3 , halogen claim 3 , substituted or unsubstituted heteroalkyl having 1 to 20 carbon atoms claim 3 , a substituted or unsubstituted heterocyclic group having 3 to 20 ring atoms claim 3 , substituted or unsubstituted arylalkyl having 7 to 30 carbon atoms claim 3 , substituted or unsubstituted alkoxy having 1 to 20 carbon atoms claim 3 , substituted or unsubstituted aryloxy having 6 to 30 carbon atoms claim 3 , substituted or unsubstituted alkenyl having 2 to 20 carbon atoms claim 3 , ...

AZEPANE DERIVATIVES AND METHODS OF TREATING HEPATITIS B INFECTIONS

Provided herein are compounds useful for the treatment of HBV infection in a subject in need thereof, pharmaceutical compositions thereof, and methods of inhibiting, suppressing, or preventing HBV infection in the subject. 135-. (canceled)37. A pharmaceutical composition comprising a compound of claim 36 , or a pharmaceutically acceptable salt thereof claim 36 , together with a pharmaceutically acceptable carrier.38. A method of treating an HBV infection in an individual in need thereof claim 36 , comprising administering to the individual a therapeutically effective amount of a compound of .3945-. (canceled)46. The method of claim 38 , further comprising administering to the individual at least one additional therapeutic agent selected from the group consisting of a HBV polymerase inhibitor claim 38 , immunomodulatory agents claim 38 , pegylated interferon claim 38 , viral entry inhibitor claim 38 , viral maturation inhibitor claim 38 , literature-described capsid assembly modulator claim 38 , reverse transcriptase inhibitor claim 38 , a cyclophilin/TNF inhibitor claim 38 , a TLR-agonist claim 38 , an HBV vaccine claim 38 , and a combination thereof.47. The method of claim 46 , wherein the therapeutic agent is a reverse transcriptase inhibitor claim 46 , and is at least one of Zidovudine claim 46 , Didanosine claim 46 , Zalcitabine claim 46 , 2′ claim 46 ,3′-dideoxyadenosine claim 46 , Stavudine claim 46 , Lamivudine claim 46 , Abacavir claim 46 , Emtricitabine claim 46 , Entecavir claim 46 , Apricitabine claim 46 , Atevirapine claim 46 , ribavirin claim 46 , acyclovir claim 46 , famciclovir claim 46 , valacyclovir claim 46 , ganciclovir claim 46 , valganciclovir claim 46 , Tenofovir claim 46 , Adefovir claim 46 , cidofovir claim 46 , Efavirenz claim 46 , Nevirapine claim 46 , Delavirdine claim 46 , and Etravirine.48. The method of claim 46 , wherein the therapeutic agent is a TLR agonist claim 46 , and wherein the TLR agonist is selected from the group consisting ...

ELECTROLUMINESCENT DEVICE

Provided is an electroluminescent device. The electroluminescent device includes an anode, a cathode and an organic layer disposed between the anode and the cathode, where the organic layer includes at least a first compound having a structure of H-L-E and a second compound having a general formula of M(L)(L)(L). The novel material combination consisting of the first compound and the second compound can enable the electroluminescent device to obtain a lower voltage, higher efficiency and an ultra-long lifetime and can provide better device performance. Further provided are a display assembly and a compound combination. 2. The electroluminescent device of claim 1 , wherein in Formula 1 claim 1 , the ring A claim 1 , the ring B and the ring C are claim 1 , at each occurrence identically or differently claim 1 , selected from an aromatic ring having 6 to 18 carbon atoms or a heteroaromatic ring having 3 to 18 carbon atoms.6. The electroluminescent device of claim 1 , wherein the E is selected from substituted or unsubstituted triazinyl.10. The electroluminescent device of claim 1 , wherein in the second compound claim 1 , the metal M is selected from Ir claim 1 , Rh claim 1 , Re claim 1 , Os claim 1 , Pt claim 1 , Au or Cu; preferably claim 1 , the M is selected from Ir claim 1 , Pt or Os; more preferably claim 1 , the M is Ir.13. The electroluminescent device of claim 12 , wherein in Formula 3-6 to Formula 3-11 claim 12 , at least one of Yand Yis N;{'sub': 4', '3, 'preferably, in Formula 3-6, Formula 3-7, Formula 3-9, Formula 3-10 and Formula 3-11, Yis N; and in Formula 3-8, Yis N.'}14. The electroluminescent device of claim 12 , wherein in Formula 3-6 to Formula 3-13 claim 12 , Yand Yare claim 12 , at each occurrence identically or differently claim 12 , selected from CR claim 12 , and Y claim 12 , Y claim 12 , Yand Yare claim 12 , at each occurrence identically or differently claim 12 , selected from CR.15. The electroluminescent device of claim 12 , wherein in ...

Monomer, polymer, and method of making the same

Ein Monomer mit der allgemeinen Formel: wobei R 1 irgendeine Substitution ist; R 2 irgendeine Substitution ist; R 1 und R 2 miteinander verknüpft sein können, um einen gesättigten oder ungesättigten Ring zu bilden, L eine reaktive Abgangsgruppe darstellt; X und Y jeweils unabhängig CR 2 , O, BR, NR, SiR 2 , S, S=O, SO 2 , PR oder P=O(R) darstellen, wobei R bei jedem Auftreten unabhängig aus H oder einem Substituenten ausgewählt ist, Z eine Einfachbindung oder ein zweiwertiges Atom oder Gruppe darstellt, wobei X, Z, Y einen unkonjugierten Ring oder Kette bildet, unter der Voraussetzung, dass wenigstens eines aus R 1 und R 2 eine Aryl- oder Heteroarylgruppe ist, wenn Z eine Einfachbindung ist.

Monomer, polymer, and method of making it

A monomer having the general formula: in which R 1 is any substitution; R 2 is any substitution; R 1 and R 2 may be linked to form a saturated or unsaturated ring; L represents a reactive leaving group; X and Y each independently represent CR 2 , O, BR, NR, SiR 2 , S, S═O, SO 2 , PR or P═O(R) wherein R in each occurrence is independently selected from H or a substituent; Z represents a single bond or a divalent atom or group, wherein X—Z—Y forms an unconjugated ring or chain, with the proviso that at least one of R 1 and R 2 is an aryl or heteroaryl group if Z is a single bond.

Monomer, polymer, and method of making it

본 발명은 하기 화학식 a의 단량체를 개시한다: 화학식 a 상기 식에서, R 1 은 임의의 치환기이고, R 2 는 임의의 치환기이고, R 1 및 R 2 는 연결되어 포화 또는 불포화 고리를 형성할 수 있고, L은 반응성 이탈기를 나타내고, X 및 Y는 각각 독립적으로 CR 2 , O, BR, NR, SiR 2 , S, S=O, SO 2 , PR 또는 P=O(R)을 나타내고, 이때 R은 각각 독립적으로 H 및 치환기로부터 선택되고, Z는 단일 결합, 또는 2가 원자 또는 기를 나타내고, X-Z-Y는 비컨쥬게이트된 고리 또는 쇄를 형성하되, Z가 단일 결합인 경우 R 1 및 R 2 중 하나 이상은 아릴 또는 헤테로아릴 기이다. The present invention discloses monomers of formula (a) A In this formula, R 1 is an arbitrary substituent, R 2 is an arbitrary substituent, R 1 and R 2 may be connected to form a saturated or unsaturated ring, L represents a reactive leaving group, X and Y each independently represent CR 2 , O, BR, NR, SiR 2 , S, S═O, SO 2 , PR or P═O (R), wherein each R is independently selected from H and substituents And, Z represents a single bond, or a divalent atom or group, XZY forms a beacon-gated ring or chain wherein at least one of R < 1 > and R < 2 > is an aryl or heteroaryl group when Z is a single bond.

Novel lapaconitine oxidized derivative and use thereof

본 발명은 신규한 라파코니틴 유도체와 약제학적으로 허용 가능한 이의 염, 이의 제조방법 및 골 형성 촉진 활성을 이용한 의학적 용도에 관한 것이다. 상기 라파코니틴 유도체는 줄기세포의 조골모세포로의 분화를 유도하며, 골다공증 동물모델에 투여시 골밀도를 증가시키고, 골 형성을 유도하므로 골다공증과 같은 골 관련 질환의 예방, 개선 또는 치료 용도로 유용하게 사용될 수 있다.

AZABICYCLOALCANES AND THEIR PRECURSORS, THEIR PREPARATION METHODS AND THEIR APPLICATIONS

NEW TETRACYCLIC COMPOUNDS AND THEIR PREPARATION

Azabicycloalkanes and precursors thereof

Abstract of the Disclosure: Novel substituted azabicycloalkanes of the general formula

Derivatives of aminomethyl dibenzo[b,f]cyclopropa[d]-oxepin -azepine and thiepin

Novel oxidized lappaconitine derivative and use thereof

The present invention relates to a novel lappaconitine derivative and a pharmaceutically acceptable salt thereof, a preparation method therefor, and a medical use thereof using osteogenesis-promoting activity. The lappaconitine derivative induces the differentiation of stem cells into preosteoblasts, and increases bone density when administered to an osteoporosis animal model, and induces osteogenesis, and thus can be effectively used for preventing, alleviating, or treating bone-related diseases such as osteoporosis.

NEW TETRACYCLICAL COMPOUNDS AND THEIR PREPARATION.

Carbamazepine derivatives

The present invention provides a novel carbamazepine hydrazide compound suitable for covalent attachment to a polymer particle reagent, having the general formula ##STR1## The present invention also provides a novel carbamazepine acid compound suitable for attachment to proteins for the production of carbamazepine immunogens. The carbamazepine antigen of the present invention has the following general structure: ##STR2## where X is C═O, CH 2 or SO 2 ; Y is C═O, CH 2 , SO 2 ; R is an alkyl and P is a protein or a hapten.

Tetracyclic compounds

Benzazepine derivatives

Compounds of the general formula <IMAGE> (R1,2 = H, OH, halogen, alkyl, NO2, amino, mono- or dialkylamino, CF3, CN, amide, CH3CO, alkoxy or R1+2 = methylenedioxy or together with the benz ring form a naphthalene, tetrahydronaphthalene, dihydrobenzopyran, dihydrobenzofuran or indane system; R3 = H, halogen, alkyl, alkoxy; R4 = H, alkyl, allyl, propargyl, cyclopropyl; R5 = H, Me) and their salts are antihypertensive agents.

Substituted 7,12-methano dibenzazocines and 8,13-methano dibenzazonines

Substituted 7,12-methano-dibenzazocines and 8,13-methanodibenzazonines, e.g., 7,12-dihydro-6,13-dimethyl-7,12-methano-6H-dibenz [c,f] azocine, are prepared by cyclizing 3-benzylamino or 3-phenethylamino -2-alkyl-indan-1-ols and are useful as anti-inflammatory agents.

Azabicyclo alkane and precursor thereof

Patent FR2346002B1

PROCESS FOR THE PREPARATION OF BENZAZEPINE DERIVATIVES

Beschrieben wird ein Verfahren zur Herstellung von Benzazepinderivaten der aus dem Formelblatt hervorgehenden Formel oder von pharmazeutisch annehmbaren Salzen hiervon, worin R tief 1 und R tief 2 jeweils unabhaengig Wasserstoff, Hydroxy, Halogen, C tief 1-C tief 3-Alkyl, Nitro, Amino, Mono- oder Di-C tief 1-C tief 3-alkylamino, Trifluormethyl, Nitril, Amid, Acetyl oder C tief 1-C tief 3-Alkoxy sind oder zusammengenommen mit dem Benzolring, an den sie gebunden sind, ein Naphthalin-, Tetrahydronaphthalin-, Dihydrobenzopyran-, Dihydrobenzofuran- oder Indansystem bilden, R tief 3 jeweils unabhaengig Wasserstoff, Halogen, C tief 1-C tief 3-Alkyl oder C tief 1-C tief 3-Alkoxy ist, R tief 4 Wasserstoff, C tief 1-C tief 4-Alkyl, Allyl, Propargyl oder Cyclopropyl ist, R tief 5 Wasserstoff oder Methyl ist, mit der Massgabe, dass R tief 1, R tief 2, R tief 3, R tief 4 und R tief 5 nicht alle gleichzeitig Wasserstoff sein duerfen, und mit der weiteren Massgabe, dass, falls beide Reste R tief 3 Wasserstoff sind und einer der Reste R tief 1 oder R tief 2 Hydroxy ist, der andere der Reste R tief 1 und R tief 2 nicht Wasserstoff oder Hydroxy sein darf, durch verschiedene, an sich bekannte Verfahren. Die hiernach erhaeltlichen neuen Verbindungen sind antihypertensive Mittel, die sich von den bekannten antihypertensiven Mitteln vor allem dadurch auszeichnen, dass sie vasodilatorisch wirksam sind, ohne gleichzeitig eine Tachykardie zu verursachen.

Improvements in or relating to benzazepine derivatives.

Amino-1H-3-benzazepine derivatives, useful as antihypertensive agents, are described herein. These derivatives are prepared by conventional methods, such as heating the corresponding 2-thione or 2-alkoxy compound with an amine, alkylating the corresponding 2-amino compound or de-etherifying the corresponding 6, 7, 8 or 9-alkoxy compound.

Azabicycloalkanes, precursors thereof, process for their preparation and pharmaceutical preparations comprising them

Novel substituted azabicycloalkanes and methods of preparing the same are disclosed. These compounds are useful as analgetic agents which exhibit a tendency towards low physical dependence.

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신규한 라파코니틴 유도체 및 이의 용도

본 발명은 신규한 라파코니틴 유도체, 이의 제조방법 및 골 형성 촉진 활성을 이용한 약학적 용도에 관한 것이다. 상기 라파코니틴 유도체는 줄기세포의 조골모세포로의 분화를 유도하고, 골다공증 동물모델에 투여하면 골밀도를 증가시키며, 골절 동물모델에서는 골 형성을 유도하므로 골다공증과 같은 골 관련 질환의 예방, 개선 또는 치료 용도와 더불어 물리적 외상에 의한 비질환성 골절 치료에 유용하게 사용될 수 있다.

Novel oxidized lappaconitine derivative and use thereof

The present invention relates to a novel lappaconitine derivative and a pharmaceutically acceptable salt thereof, a preparation method therefor, and a medical use thereof using osteogenesis-promoting activity. The lappaconitine derivative induces the differentiation of stem cells into preosteoblasts, and increases bone density when administered to an osteoporosis animal model, and induces osteogenesis, and thus can be effectively used for preventing, alleviating, or treating bone-related diseases such as osteoporosis.

新型高乌甲素衍生物及其用途

本发明涉及一种新型高乌甲素衍生物、其制备方法以及利用骨生成促进活性的药学用途。所述高乌甲素衍生物诱导干细胞向成骨细胞的分化，如果施用于骨质疏松动物模型其增加骨密度，并在骨折动物模型中诱导骨生成，因此能够有效地用于预防、改善或治疗骨质疏松等骨相关疾病，以及用于物理性创伤引起的非疾患性骨折治疗。

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酰亚胺化芴酮衍生物及其中间体、制备方法和应用

本发明涉及有机合成和有机电子领域，尤其涉及酰亚胺化芴酮衍生物及其中间体、制备方法和应用，所述酰亚胺化芴酮衍生物的结构通式如结构式（Ⅰ）或（Ⅱ）所示： 。本发明中的酰亚胺化芴酮衍生物是在芴酮结构中引入酰亚胺和吸电子基团进行修饰，因此使得整个分子结构形成强缺电子结构单元。从而能够与富电子的给体结构单元通过共价键连接构筑D‑A型的π共轭体系，有效地促进分子内的电荷转移，调节分子的前线轨道能级，从而能够在有机半导体领域具有巨大的应用潜力。

一种电致发光材料及器件

公开了一种电致发光材料及器件。所述化合物是具有吲哚和吡咯稠合氮杂大环与三嗪及其类似结构通过特定的位置连接而成的化合物，可用作电致发光器件中的主体材料。这些新型化合物具有显著降低的蒸镀温度，具有更好的热稳定性，并能有效降低能耗，更有利于器件制作过程，此外还能有效提升器件效率、降低器件的驱动电压，能提供更好的器件性能。还公开了一种电致发光器件、一种化合物配方和一种显示组件。

富含异构体的3-蒈烷内酰胺和基于此的具有高光学纯度和可调结晶度的高性能用途用聚酰胺

本发明涉及由3‑环氧蒈烷制备由3S‑蒈酮和3R‑蒈酮构成的富含异构体的混合物的方法、由此获得的3S‑蒈酮、由3‑蒈烯制备3S‑蒈烷内酰胺的方法、由3‑蒈烯制备3R‑蒈烷内酰胺的方法、3S‑蒈烷基肟、3S‑蒈烷内酰胺、3S‑聚蒈烷酰胺、3R‑聚蒈烷酰胺、3S/3R‑共聚蒈烷酰胺、3S‑蒈烷内酰胺‑月桂精内酰胺‑共聚蒈烷酰胺、3R‑蒈烷内酰胺‑月桂精内酰胺‑共聚蒈烷酰胺、3S‑蒈烷内酰胺‑3R‑蒈烷内酰胺‑月桂精内酰胺‑共聚蒈烷酰胺、3S‑蒈烷内酰胺‑己内酰胺‑共聚蒈烷酰胺、3R‑蒈烷内酰胺‑己内酰胺‑共聚蒈烷酰胺以及3S‑蒈烷内酰胺‑3R‑蒈烷内酰胺‑己内酰胺‑共聚蒈烷酰胺。

Isomer-enriched 3-caranlactams and polyamides based on them having high optical purity and adjustable crystallinity for high-performance applications

The present invention relates to a method for producing an isomer-enriched mixture of 3S- and 3R-caranon of 3-caran epoxide, a 3S-caranon obtained therefrom, a method for producing 3S-caranlactam from 3-carene, a method for producing 3R-caranlactam from 3-carene, and relates to a 3S-caranoxim, a 3S-caranlactam, a 3S-polycaranamide, a 3R-polycaranamide, a 3S/3R-co-polycaranamide, a 3S-caranlactam laurinlactam co-polycaranamide, a 3R-caranlactam laurinlactam co-polycaranamide, a 3S-caranlactam 3R-caranlactam laurinlactam co-polycaranamide, a 3S-caranlactam caprolactam co-polycaranamide, a 3R-caranlactam caprolactam co-polycaranamide, and to a 3S-caranlactam 3R-caranlactam caprolactam co-polycaranamide.

富含异构体的3-蒈烷内酰胺和基于此的聚酰胺

本发明涉及由3‑环氧蒈烷制备由3S‑蒈酮和3R‑蒈酮构成的富含异构体的混合物的方法、由此获得的3S‑蒈酮、由3‑蒈烯制备3S‑蒈烷内酰胺的方法、由3‑蒈烯制备3R‑蒈烷内酰胺的方法、3S‑蒈烷基肟、3S‑蒈烷内酰胺、3S‑聚蒈烷酰胺、3R‑聚蒈烷酰胺、3S/3R‑共聚蒈烷酰胺、3S‑蒈烷内酰胺‑月桂精内酰胺‑共聚蒈烷酰胺、3R‑蒈烷内酰胺‑月桂精内酰胺‑共聚蒈烷酰胺、3S‑蒈烷内酰胺‑3R‑蒈烷内酰胺‑月桂精内酰胺‑共聚蒈烷酰胺、3S‑蒈烷内酰胺‑己内酰胺‑共聚蒈烷酰胺、3R‑蒈烷内酰胺‑己内酰胺‑共聚蒈烷酰胺以及3S‑蒈烷内酰胺‑3R‑蒈烷内酰胺‑己内酰胺‑共聚蒈烷酰胺。

이성질체가 풍부한 3-카란락탐 및 이에 기반한 높은 광학 순도 및 조정 가능한 결정도를 갖는 고성능 용도의 폴리아미드

본 발명은 3-카란 에폭사이드로부터 3S- 및 3R-카라논의 이성질체가 풍부한 혼합물을 제조하는 방법, 그로부터 수득된 3S-카라논, 3-카렌으로부터 3S-카란락탐을 제조하는 방법, 3-카렌으로부터 3R-카란락탐을 제조하는 방법, 3S-카란옥심, 3S-카란락탐, 3S-폴리카란아미드, 3R-폴리카란아미드, 3S/3R-코-폴리카란아미드, 3S-카란락탐-라우로락탐 코-폴리카란아미드, 3R-카란락탐-라우로락탐 코-폴리카란아미드, 3S-카란락탐-3R-카란락탐-라우로락탐 코-폴리카란아미드, 3S-카란락탐-카프로락탐 코-폴리카란아미드, 3R-카란락탐-카프로락탐 코-폴리카란아미드, 및 3S/3R-카란락탐-카프로락탐 코-폴리카란아미드에 관한 것이다.

異性体富化された３−カランラクタム並びに高い光学純度及び高性能用途のために調整可能な結晶性を有する上記ラクタムをベースとするポリアミド

本発明は、3S-及び3R-カラノンからの異性体富化された混合物を3-カランエポキシドから製造するための方法、この方法から得られる3S-カラノン、3S-カランラクタムを3-カレンから製造するための方法、3R-カランラクタムを3-カレンから製造するための方法、3S-カランオキシム、3S-カランラクタム、3S-ポリカランアミド、3R-ポリカランアミド、3S/3R-コ-ポリカランアミド、3S-カランラクタム-ラウロラクタム-コ-ポリカランアミド、3R-カランラクタム-ラウロラクタム-コ-ポリカランアミド、3S-カランラクタム-3R-カランラクタム-ラウロラクタム-コ-ポリカランアミド、3S-カランラクタム-カプロラクタム-コ-ポリカランアミド、3R-カランラクタム-カプロラクタム-コ-ポリカランアミド、並びに3S-カランラクタム-3R-カランラクタム-カプロラクタム-コ-ポリカランアミドに関する。【選択図】なし

Isomeren-angereicherte 3-caranlactame und darauf basierende polyamide mit hoher optischer reinheit und einstellbarer kristallinität für hochleistungsanwendungen

Die vorliegende Erfindung betrifft ein Verfahren zur Herstellung eines Isomeren- angereicherten Gemisches aus 3S- und 3R-Caranon aus 3-Caranepoxid, ein daraus gewonnenes 3S-Caranon, ein Verfahren zur Herstellung von 3S-Caranlactam aus 3-Caren, ein Verfahren zur Herstellung von 3R-Caranlactam aus 3-Caren, ein 3S-Caranoxim, ein 3S-Caranlactam, ein 3S-Polycaranamid, ein 3R-Polycaranamid, ein 3S/3R-Co-Polycaranamid, ein 3S-Caranlactam-Laurinlactam-Co-Polycaranamid, ein 3R-Caranlactam-Laurinlactam-Co-Polycaranamid, ein 3S-Caranlactam-3R-Caranlactam- Laurinlactam-Co-Polycaranamid, ein 3S-Caranlactam-Caprolactam-Co-Polycaranamid, ein 3R-Caranlactam-Caprolactam-Co-Polycaranamid, sowie 3S-Caranlactam-3R- Caranlactam-Caprolactam-Co-Polycaranamid.

Isomeren-angereicherte 3-Caranlactame und darauf basierende Polyamide mit hoher optischer Reinheit und einstellbarer Kristallinität für Hochleistungsanwendungen

Die vorliegende Erfindung betrifft ein Verfahren zur Herstellung eines Isomeren-angereicherten Gemisches aus 3S- und 3R-Caranon aus 3-Caranepoxid, ein daraus gewonnenes 3S-Caranon, ein Verfahren zur Herstellung von 3S-Caranlactam aus 3-Caren, ein Verfahren zur Herstellung von 3R-Caranlactam aus 3-Caren, ein 3S-Caranoxim, ein 3S-Caranlactam, ein 3S-Polycaranamid, ein 3R-Polycaranamid, ein 3S/3R-Co-Polycaranamid, ein 3S-Caranlactam-Laurinlactam-Co-Polycaranamid, ein 3R-Caranlactam-Laurinlactam-Co-Polycaranamid, ein 3S-Caranlactam-3R-Caranlactam-Laurinlactam-Co-Polycaranamid, ein 3 S-Caranlactam-Caprolactam-Co-Polycaranamid, ein 3R-Caranlactam-Caprolactam-Co-Polycaranamid, sowie 3S-Caranlactam-3R-Caranlactam-Caprolactam-Co-Polycaranamid.

Treatment of diarrhoea

신규한 라파코니틴 유도체 및 이의 용도

본 발명은 신규한 라파코니틴 유도체, 이의 제조방법 및 골 형성 촉진 활성을 이용한 약학적 용도에 관한 것이다. 상기 라파코니틴 유도체는 줄기세포의 조골모세포로의 분화를 유도하고, 골다공증 동물모델에 투여하면 골밀도를 증가시키며, 골절 동물모델에서는 골 형성을 유도하므로 골다공증과 같은 골 관련 질환의 예방, 개선 또는 치료 용도와 더불어 물리적 외상에 의한 비질환성 골절 치료에 유용하게 사용될 수 있다.

一种芴衍生物、电子元件和电子装置

本发明涉及有机电致发光材料技术领域，尤其涉及一种芴衍生物及其在电子元件和电子装置中的应用。所述芴衍生物的结构式如式(I)所示；本发明提供的式(I)所示化合物，具有七元环及以上多元环结构。将该化合物应用在有机电致发光元件中，可显著降低驱动电压、提高发光效率和寿命；

전계발광재료 및 그 소자

전계발광재료 및 소자를 개시하였다. 상기 화합물은 인돌과 피롤이 아자마크로사이클에 융합되어, 트리아진 및 그 유사한 구조와 특정된 위치를 통해 연결되어 형성된 화합물로서, 유기 전계발광소자에서 호스트 재료로 사용될 수 있다. 이러한 신규 화합물은 현저하게 낮아진 증착 온도, 더 나은 열 안정성을 구비하고 에너지 소모를 효과적으로 줄일 수 있어 소자 제조과정에 더 유리하며, 또한 소자 효율을 효과적으로 향상시킬 수 있고 소자의 구동 전압을 낮추며 더 나은 소자 성능을 제공할 수 있다. 전계발광소자, 화합물 제제 및 디스플레이 부품을 더 개시하였다.

Novel lappaconitine derivative and use thereof

The present invention pertains to a novel lappaconitine derivative, a method for producing same, and a pharmaceutical use thereof using osteogenesis-promoting activity. The lappaconitine derivative induces the differentiation of stem cells into osteoblasts, increases bone mineral density when administered to animal models of osteoporosis, and induces bone formation in animal models of bone fracture, and thus can be advantageously used for preventing, ameliorating, or treating bone-related diseases such as osteoporosis, as well as treating non-disease fractures caused by physical trauma.

Novel oxidized lappaconitine derivative and use thereof

Process for preparing decahydrocyclopent(c)azepines

Azepine derivatives

2-Substituted-5a-aryl-decahydrocyclopent[c]azepines are useful as analgesics having mixed narcotic antagonist and agonist properties. [US4141893A]

Decahydrocyclopent (c) azepines

Verfahren zur herstellung von neuen decahydrocyclopent(c)azepinen und ihren saeure- additionssalzen

Sposob wytwarzania dziesieciowodorocyklopenta/c/azepin

Method of producing new decahydrocyclopentano azepsposob wytwarzania nowych dziesieciowodorocyklopenta c azepin ines

Decahydrocyclopent(c)azepines

Process for obtaining decahydroyclopene(c)azepine

Способ получени декагидроциклопент-/с/-азепинов или их солей

Forfarande for framstellning av dekahydrocyklopent-(c)azepiner med terapeutisk verkan

Procedeu de preparare a unor decahidrociclopent (c) azepine

Process for preparing decahydrocyclopent(c)azepines

5a-aryl-decahyrocyclopenta(c) azepines and pharmaceutical compositions

Werkwijze ter bereiding van farmaceutische pre- paraten en werkwijze ter bereiding van nieuwe decahydrocyclopent(c)azepinen.

Decahydrocyclopent(c)azepines

Decahydrocyclopent(c)azepines

2-Substituted-5a-aryl-decahydrocyclopent[c]azepines are useful as analgesics having mixed narcotic antagonist and agonist properties.

Fremgangsmaade til fremstilling af decahydrocyclopent (c)-azepiner

Verfahren zur herstellung von decahydrocyclopent eckige klammer auf c eckige klammer zu azepinen

Decahydrocyclopento (c) azepines a activite analgesique

Decahydrocyclopenta *c* azepines

Decahydrocyclopento(c)azepines, a activite analgesique

L'invention concerne des dérivés de décahydrocyclopentoØcõ azépine de formule :

Novel lappaconitine derivative and use thereof

異性体富化された３－カランラクタム並びに高い光学純度及び高性能用途のために調整可能な結晶性を有する上記ラクタムをベースとするポリアミド

5-Azatricyclo-[4.3.1.1?]-undecan-Derivate,Verfahren zu ihrer Herstellung und ihre Verwendung zur Herstellung von Arzneipraeparaten

新規なラパコニチン酸化誘導体及びその用途

4-azatricyclo(4.3.1.13,8)undecan and related compounds

THIS INVENTION RELATES TO A NOVEL SERIES OF COMPOUNDS CHARACTERIZED PARTICULARLY BY THE AZATRICYCLO(4.3.1.1**3,8) UNDECANE RING. THESE INCLUDE 4-AZATRICYCLO(4.3.1.1**3,8) UNDECANE-5-ONE, 4-AZATICYCLO(4.3.1.1**3,8) UNDECANE AND NITROGEN SUBSTITUTED DERIVATIVES OF EACH OF THESE AND THEIR SALTS. THE COMPOUNDS ARE USEFUL AS ANTIVIRAL, CARDIOVASCULAR OR ANTINFLAMMATORY AGENTS, OR AS INTERMEDIATES FOR SUCH SUBSTANCES.

Dibenzopyrazinium azepine treatment for diarrhoea

下痢治療薬

(57)【要約】本公報は電子出願前の出願データであるた め要約のデータは記録されません。

Hexahydrobenzazocines

1, 2, 3, 4, 5, 6-hexahydro-1,6-methano-3-benzazocine

[UNK]

[UNK]

Bridged benzazepines

Peri-condensed benzazepines

Decahydrocyclopent/c/azepine und verfahren zu ihrer herstellung

Anvendelse af pentacycliske forbindelser

[UNK]

Processo para a preparcao de derivados de benzazepina

Bridged benzazepines,their preparation and pharmaceutical compositions containing them

Bridged benzazepines

Compounds of formula (I) or a pharmaceutically acceptable salt thereof, wherein R represents H, alkyl, allyl, or (a); n represents 0 or 1; R1 and R2 may be the same or different and each independently represents H, OH, C1-C4 alkyl or Ar; with the proviso that R1 and R2 may not both be OH, and with the further proviso that when n is 0, R1 is C1-C4 alkyl or Ar, R2 is CH3 and R4 is H; R3 and R4 may be the same or different and each independently represents H or C1-C4 alkyl; G represents H, (R5, R6)NCO- or ArNHCO-; R5 and R6 may be the same or different and each independently represents H, C1-C4, alkyl, or Ar; Ar represents phenyl or substituted phenyl; Y and Z may be the same or different and each independently represents H, halo, C1-C4 alkyl, C1-C4 alkoxy, or C1-C4 haloalkyl are described. The compounds of formula (I) are useful as agents in the treatment of psychoses and drug dependence. The compounds of formula (I) also provide an analgesic effect in a mammal.

一种电致发光材料及器件

公开了一种电致发光材料及器件。所述化合物是具有吲哚和吡咯稠合氮杂大环与三嗪及其类似结构通过特定的位置连接而成的化合物，可用作电致发光器件中的主体材料。这些新型化合物具有显著降低的蒸镀温度，具有更好的热稳定性，并能有效降低能耗，更有利于器件制作过程，此外还能有效提升器件效率、降低器件的驱动电压，能提供更好的器件性能。还公开了一种电致发光器件、一种化合物配方和一种显示组件。

一种芴衍生物、电子元件和电子装置

本发明涉及有机电致发光材料技术领域，尤其涉及一种芴衍生物及其在电子元件和电子装置中的应用。所述芴衍生物的结构式如式(I)所示；本发明提供的式(I)所示化合物，具有七元环及以上多元环结构。将该化合物应用在有机电致发光元件中，可显著降低驱动电压、提高发光效率和寿命；

新型高乌甲素衍生物及其用途

本发明涉及一种新型高乌甲素衍生物、其制备方法以及利用骨生成促进活性的药学用途。所述高乌甲素衍生物诱导干细胞向成骨细胞的分化，如果施用于骨质疏松动物模型其增加骨密度，并在骨折动物模型中诱导骨生成，因此能够有效地用于预防、改善或治疗骨质疏松等骨相关疾病，以及用于物理性创伤引起的非疾患性骨折治疗。

新型高乌甲素氧化衍生物及其用途

本发明涉及一种新型高乌甲素衍生物和其药学上可接受的盐、其制备方法以及利用骨生成促进活性的医学用途。所述高乌甲素衍生物诱导干细胞向成骨细胞的分化，当施用于骨质疏松动物模型时，其使骨密度增加并诱导骨生成，因此能够以预防、改善或治疗如骨质疏松症的骨相关疾病的用途所使用。

新型高乌甲素氧化衍生物及其用途

本发明涉及一种新型高乌甲素衍生物和其药学上可接受的盐、其制备方法以及利用骨生成促进活性的医学用途。所述高乌甲素衍生物诱导干细胞向成骨细胞的分化，当施用于骨质疏松动物模型时，其使骨密度增加并诱导骨生成，因此能够以预防、改善或治疗如骨质疏松症的骨相关疾病的用途所使用。

酰亚胺化芴酮衍生物及其中间体、制备方法和应用

本发明涉及有机合成和有机电子领域，尤其涉及酰亚胺化芴酮衍生物及其中间体、制备方法和应用，所述酰亚胺化芴酮衍生物的结构通式如结构式（Ⅰ）或（Ⅱ）所示： 。本发明中的酰亚胺化芴酮衍生物是在芴酮结构中引入酰亚胺和吸电子基团进行修饰，因此使得整个分子结构形成强缺电子结构单元。从而能够与富电子的给体结构单元通过共价键连接构筑D‑A型的π共轭体系，有效地促进分子内的电荷转移，调节分子的前线轨道能级，从而能够在有机半导体领域具有巨大的应用潜力。

신규한 라파코니틴 유도체 및 이의 용도

본 발명은 신규한 라파코니틴 유도체, 이의 제조방법 및 골 형성 촉진 활성을 이용한 약학적 용도에 관한 것이다. 상기 라파코니틴 유도체는 줄기세포의 조골모세포로의 분화를 유도하고, 골다공증 동물모델에 투여하면 골밀도를 증가시키며, 골절 동물모델에서는 골 형성을 유도하므로 골다공증과 같은 골 관련 질환의 예방, 개선 또는 치료 용도와 더불어 물리적 외상에 의한 비질환성 골절 치료에 유용하게 사용될 수 있다.

富含异构体的3-蒈烷内酰胺和基于此的具有高光学纯度和可调结晶度的高性能用途用聚酰胺

本发明涉及由3‑环氧蒈烷制备由3S‑蒈酮和3R‑蒈酮构成的富含异构体的混合物的方法、由此获得的3S‑蒈酮、由3‑蒈烯制备3S‑蒈烷内酰胺的方法、由3‑蒈烯制备3R‑蒈烷内酰胺的方法、3S‑蒈烷基肟、3S‑蒈烷内酰胺、3S‑聚蒈烷酰胺、3R‑聚蒈烷酰胺、3S/3R‑共聚蒈烷酰胺、3S‑蒈烷内酰胺‑月桂精内酰胺‑共聚蒈烷酰胺、3R‑蒈烷内酰胺‑月桂精内酰胺‑共聚蒈烷酰胺、3S‑蒈烷内酰胺‑3R‑蒈烷内酰胺‑月桂精内酰胺‑共聚蒈烷酰胺、3S‑蒈烷内酰胺‑己内酰胺‑共聚蒈烷酰胺、3R‑蒈烷内酰胺‑己内酰胺‑共聚蒈烷酰胺以及3S‑蒈烷内酰胺‑3R‑蒈烷内酰胺‑己内酰胺‑共聚蒈烷酰胺。

7-membered fused heterocycles and methods of their synthesis

Disclosed are a new method for synthesizing 7-membered fused heterocycles and compounds synthesized by the new method. The method involves a dual activation strategy using an N-heterocyclic carbene catalyst as a first Lewis base and another second Lewis base. Compounds synthesized by the disclosed method may include new benzoxopinone compounds, as well as benzoxepane compounds and benzoazepinone compounds that optionally may be derived from the disclosed benzoxopinone compounds.

Inhibitors of the influenza A virus M2 proton channel

Provided are compounds that are capable of modulating the activity of the influenza A virus via interaction with the M2 transmembrane protein. Also provided are methods for treating an influenza A-affected disease state or infection comprising administering a composition comprising one or more compounds that have been identified as being capable of interaction with the M2 protein.