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We have successfully synthesized chiral β-amino trifluoromethyl alcohol (2S,3S)-7a, which is a key intermediate in the production of AE-3763, by stereoselective reduction of N-Cbz-protected 5-hydroxy-5-(trifluoromethyl)-1,3-oxazolidine 4 prepared from L-valine in 3 steps followed by alkaline hydrolysis. This new method can be applied to the industrial-scale synthesis of AE-3763.

The 3-D structure of liquid atomization behavior through a cylindrical nozzle is numerically investigated and visualized by a new type of integrated simulation technique. CFD (Computational Fluid Dynamics) analysis focused on the consecutive breakup of a liquid column, formation of liquid film, and generation of droplets of a cylindrical flow in the outlet section of the nozzle. Utilizing the governing equations for high-speed atomizing nozzle flow based on the LES-VOF model in conjunction with the CSF model, an integrated parallel computation is performed to clarify the detailed atomization process of a cylindrical nozzle flow and to acquire data, which is difficult to confirm by experiment, such as atomization length, liquid core shape, distribution droplet sizes, spray angle and droplet velocity profiles. According to the present analysis, the atomization rate and the droplets-gas two-phase flow characteristics are found to be controlled by the turbulence perturbation upstream of the injector nozzle, hydrodynamic instabilities at the gas-liquid interface, and shear stresses between the liquid core and periphery of the jet.

In our search for a new agent, human neutrophil elastase (HNE) inhibitor, for the treatment of acute respiratory failure, we rationally designed and synthesized a series of peptide-based carboxylic acid-containing transition-state inhibitors. The presence of valyl moiety is found to be essential for potent in vitro inhibitory activity and also prevention of an undesirable toxicity. Of these, compound 9m has the most potent in vivo effect on HNE-induced lung hemorrhage in hamsters.

Lymphoepithelioma-like carcinoma (LELC) in the bladder is uncommon with a reported incidence of 0.4%–1.3% of all bladder carcinomas. In Japan, some occurrences of LELC have been reported in the renal pelvis and ureter but only two in the bladder. A bladder tumor was identified in a 70-year-old man suffering from macroscopic hematuria for 2 months. Sections of the transurethral tumor resection showed invasive high-grade urothelial carcinoma. The patient was diagnosed with local invasive bladder tumor, and cystectomy with ileal conduit formation was performed. The final pathological evaluation was predominant LELC with urothelial carcinoma. We present a new case of LELC in the bladder and performed a review of all published cases of LELC in the urinary tract to obtain its characteristics and prognostic guide.

A 74-year-old woman presenting with bilateral ureteral stricture was referred to our hospital. She had undergone radical hysterectomy and adjuvant irradiation therapy for cervical cancer in 2000. Double-J stents were inserted in both the ureters and replaced at regular intervals. Eighteen months after ureteral stenting, she complained of gross hematuria and was managed with hemostatic agents. During a routine replacement of the right double-J stent, massive bleeding was observed from the urethra which continued intermittently. The source of bleeding was not identified on computed tomography and angiography. We kept her at rest, which reduced the bleeding. However, she required intermittent transfusions. Angiography was performed at the time of bleeding on March 5, 2011. A uretero-internal pudendal artery fistula was found, and coil embolization was performed. Thereafter, hematuria did not recur up to the last followup in July 2011.

Tumor-to-tumor metastasis is a rare phenomenon. From our review of the international literature, around 150 cases have been reported since it was first documented by Campbel in 1868. Renal clear cell carcinoma is well known to be the most common recipient of tumor-to-tumor metastasis in all tumors. However, renal chromophobe cell carcinoma has not been reported to be a recipient. Here, we report a first case of colorectal carcinoma metastatic to chromophobe renal cell carcinoma.

Laparoendoscopic single-site surgery (LESS) is a step toward the development of minimally invasive surgery. It is initially difficult for surgeons with limited experience to perform the surgery. We describe two cases of left adrenalectomy with a LESS combined with the addition of an accessory port. After a 2.5-cm skin incision was made at the level of the paraumbilicus to insert the primary 12-mm trocar for the laparoscope, a 5-mm nonbladed trocar was placed through the skin incision side-by-side with the primary trocar. A second 3-mm nonbladed trocar was then placed along the anterior axillary line; a multichannel trocar was not used as a single port. Both adrenalectomies were completed successfully. In patients with a minor adrenal tumor, a combined technique using LESS and an additional port is easier than LESS alone and may, therefore, be a bridge between the conventional laparoscopic approach and LESS.

We present here the patient undergoing laparoendoscopic single-site (LESS) retroperitoneal radical nephrectomy while receiving hemodialysis. An 81-year-old man under hemodialysis for 6 years was incidentally discovered to have two left renal masses with acquired cystic disease of the kidney (ACDK). A 4-cm flank incision for GelPort was made. Three trocars were inserted into the retroperitoneum through GelPort. After division of the renal vessels and ureter, the kidney was placed into the extraction bag and was retrieved through flank incision without any extra skin incision. There were no intraoperative and postoperative complications. This procedure offers an effective, minimally invasive therapeutic alternative to the standard laparoscopic technique in high-risk end-stage renal disease patients.

第25回宇宙利用シンポジウム(2009年1月14日-15日, 宇宙航空研究開発機構宇宙科学研究本部相模原キャンパス), The Twenty-fifth Space Utilization Symposium (January 14-15, 2009: ISAS/JAXA Sagamihara, Japan), Maintenance of skeletal muscle requires responses to mechanicals stresses caused by stretch of muscles, which was demonstrated by effects of exercise and gravity. The stress responses include factors intrinsic to muscle and extrinsic ones. The formers include IGF-1, and the latters include membrane-anchored Neuregulin/ARIA (acetylcholine receptor inducing activity) generated in neuronal cells. Some of ADAM (A Disintegrin And Metalloprotease) family proteases modulate the ectodomain shedding of various membrane proteins, such as membrane-anchored growth factors. Meltrin beta(ADAM19) is expressed in the peripheral nervous system, and mediates the ectodomain shedding of Neuregulin. We report here roles of Meltrin beta in the formation of the NMJ. The zone of acetylcholine receptor a mRNA distribution was broader and excess sprouting of motor nerve terminals was more prominent in Meltrin beta deficient than in wild-type embryonic diaphragms, suggesting roles of Meltrin beta in the regulation of Neuregulin. Neuregulin has various isoforms including Type I, II, and III. We isolated cDNAs encoding these three isoforms from zebrafish (Danio rerio). In situ hybridization revealed temporally and spatially regulated expression of each Neuregulin isoform during development. Moreover, we found that swimming caused dramatic upregulated expression of Neuregulin, suggesting that this gene is sensitive to stress. We are currently trying to clarify roles of Neuregulin in zebrafish muscle and nervous system by injecting morpholino oligonucleotides against each form of Neuregulin., 形態: カラー図版あり, 資料番号: AA0064297046